Introduction
            
                  The ability to explore the outside world
                                    and compare old and new information is critical for animal's survival. The
                                    proper exploratory behavior in novel unpredictable situations (brought about by
                                    weather changes, activity of other animals, etc.) allows distinguishing
                                    meaningful and ignoring not important novel stimuli and their combinations.
                                    Habituation, one of the simplest forms of non-associative learning, is the
                                    mechanism providing an animal with the means to dampen the perception of repetitive neutral stimuli and
                                    be ready to effectively detect a novel stimulus with a yet unknown significance,
                                    and therefore is vitally important for the interaction of an organism with its
                                    environment [1-3]. Both response to novelty and habituation change with age,
                                    but molecular mechanisms underlying these changes remain mostly unknown.
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  Recently we have demonstrated that a deficiency of the
                                    transcription factor BMAL1 in mice results in accelerated aging [4]. BMAL1
                                    activity is critical for the operation of the circadian clock - a genetically
                                    determined time-keeping system generating 24-hour oscillations in physiology
                                    and behavior known as the circadian rhythms [5]. The involvement of the
                                    circadian clock in the control of brain-based activities such as sleep [6],
                                    reward behavior [7,8] and regulation of mood [9,10] has been reported.
                                    Recently, a connection between the circadian clock and memory has been
                                    suggested: mice with deficiencies of different components of the circadian
                                    clock demonstrate impairments of some types of memory and learning [11]. Here
                                    we hypothesize that the circadian clock is involved in the regulation of the
                                    adaptation to the new environment, and investigate this hypothesis using a set
                                    of circadian mutants - mice with targeted disruptions of circadian genes Bmal1
                                    or Cry1 and Cry2, or with the mutation of the Clock
                                    [12-14] gene. These genes encode proteins representing the core components of
                                    the circadian clock. Transcription factors BMAL1 and CLOCK form a transcription
                                    complex activating expression of target genes including circadian transcription
                                    repressors CRY1 and CRY2. In turn, CRY1 and CRY2 suppress activity of the
                                    BMAL1:CLOCK complex, including their own expression, thus generating a negative
                                    feedback loop; expression of several other genes important for the functional
                                    clock (i.e. Per1, 2 and 3) is also under the transcription control of
                                    the BMAL1:CLOCK complex [15].
                        
            
            
            
            
            
            
            
            
            
            
            
            
           
          
             Results
            
            
            
                  
                     Hyperactivity
                                              and impaired habituation of Bmal1-/- mice
                                          
                    
                          The exploratory behavior of the wild type
                                                and Bmal1-/- mice in novel environment was tested in the open field
                                                paradigm (OF). For this, 3-months old male mice were placed in a bright-lit
                                                50x50 inches square box and monitored for the pattern of their exploratory
                                                behavior for 1 hour with 5-min resolution. In order to assess intersessional
                                                habituation, animals were exposed to the same environment 24 hours later. 
                                                Activity of Bmal1-/-  mice in novel environment was strikingly different
                                                from that of wild type mice. Bmal1-/- mice demonstrated significantly
                                                increased locomotion (horizontal activity) on day1 [F[1,5] = 19.21, P = 0.007]
                                                and day2 [F[1,5] = 27.36, P = 0.0004] (Figure 1, left panel).  Total distance
                                                traveled by Bmal1-/- animals during 1h on days 1 and 2 of the OF
                                                experiment was respectively 2.7-fold and 4.7-fold higher than that of the wild
                                                type mice. The pattern of activity in wild type and Bmal1-/- mice was
                                                also very different. As expected based on previous studies [1,16], on day1 the
                                                distance traveled by wild type mice during the first 15 min of the OF session
                                                was 3.1-fold higher than during the last 15 min [t-test P <0.0001]; on day2,
                                                it was 2.8-fold higher [t-test P <0.001]. Such a decrease with time on both
                                                first and second days of the experiment results from animals' habituation to a
                                                new environment within each OF session. When compared to day1, total activity
                                                of wild type mice on day2 was also significantly reduced [F[1,5] = 13.37, P =
                                                0.015] (Figure 1 and 5, left), indicating that a long-term memory reflecting
                                                experience obtained on day1 has been formed [17]. In contrast, on day1 the
                                                difference in distance traveled by Bmal1-/- mice during the first 15 min
                                                of the OF session was only 1.6-fold higher than during the last 15 min [t-test
                                                P <0.01], whereas there was no difference on day2. Remarkably, the total
                                                distances traveled by Bmal1-/- mice during the first and the second days
                                                were virtually identical (Figure 5, lower left), and no statistically
                                                significant difference was detected between days 1 and 2 of the test [F[1,5] =
                                                3.83, P = 0.107] (Figure1, left).
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          In
                                                the same experiments, vertical (rearing) activity was measured by registering
                                                the sequential crossing of beams up and down in vertical direction. Similar to
                                                the difference in horizontal activity, total rearing activity of Bmal1-/-
                                                mice was significantly increased compared to wild type animals (2.3-fold and
                                                4.7-fold on days 1 [F[1,5] = 13.92, P = 0.014] and 2 [F[1,5] = 22.57, P =
                                                0.00031], respectively (Figure 1, right panel).  On day2 wild type mice
                                                demonstrated 1.9-fold reduction in total rearing activity [F[1,5] = 24.34, P =
                                                0.004], whereas no difference between the two days was detected in Bmal1-/-
                                                animals [F[1,5] = 0.37, P = 0.568] (Figure 5, lower right). In contrast to
                                                differences displayed in   horizontal activity, animals of both genotypes
                                                displayed similar rearing activity during the first 5 min of exposure to the
                                                new environment. After this, rearing activity of wild type animals gradually
                                                decreased, whereas in Bmal1-/- mice it increased and stayed elevated for
                                                the duration of testing (Figure 1, right). On day 2, the temporal pattern of
                                                rearing activity in animals of both genotypes did not differ much from the one
                                                displayed on day1. Taken together, these data indicate that deficiency in core
                                                circadian component, BMAL1, affects not only rhythmicity in locomotor activity,
                                                but other patterns of behavior as well. Specifically, when placed in a new
                                                environment, BMAL1-deficient mice display novelty-induced hyperactivity in
                                                locomotion and rearing behavior, and deficits in inter- and intrasessional
                                                habituation.
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                   
            
            
            
            
            
            
            
            
            
            
                  
                     BMAL1
                                              is expressed in hippocampal and cortical neurons
                                          
                    
                          BMAL1
                                                is expressed in many different tissues and organs. Brain-specific Bmal1
                                                expression at the mRNA level has been demonstrated for the suprachiasmatic
                                                nucleus of the anterior hypothalamus (SCN),  the residence of the master
                                                circadian clock, as well as for other brain regions including the cortex and
                                                hippocampus formation [12,18]. To investigate the distribution of BMAL1
                                                protein in the brain, we performed in situ immunofluorescent staining
                                                using BMAL1-specific antibody (Figure 2a). High expression of
                                                BMAL1 was detected in the pyramidal neurons of the hippocampus and in the
                                                neurons of the subiculum and enthorhinal cortex of wt mice. Neurons of the
                                                neocortex were also positive for BMAL1. Specificity of the signal was confirmed
                                                by the parallel staining of the brains of Bmal1-/- mice. Thus, BMAL1
                                                protein is expressed in brain structures associated with memory formation.
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          
                              
                                
                                Figure 1. Open field analysis of exploratory activity and habituation of wild type and Bmal1-/- mice. 
                                                                            Locomotor and rearing activity were measured in 5 min increments during 1
                                                                            hr. (Upper panel) locomotor and rearing activity of wt and Bmal1-/-
                                                                            mice on day1; (middle panel) relative locomotor activity (normalized to
                                                                            average distance covered on day1) and relative rearing activity (normalized
                                                                            to average rearing level on day1) of wt mice on days 1 and 2; (lower panel)
                                                                            relative locomotor and rearing activity  of Bmal1-/- mice on days 1
                                                                            and 2 (* P<0.05).
                                                        
                                
                               
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          
                              
                                
                                Figure 2. Expression of circadian proteins in brain structures. (a)
                                                                                Immunostaining of sagittal brain sections of wt and Bmal-/- mice
                                                                                with BMAL1 specific antibodies. Counterstaining with DAPI was used to
                                                                                detect nuclei. Pyramidal neurons of hippocampal areas CA1 and CA3, granular
                                                                                cells of the dentate gyrus and neurons of subiculum expressing BMAL1 are
                                                                                shown. (b) Circadian profile of Cry1 and Per2 mRNAs in
                                                                                the brain of wt (filled circles) and Bmal1-/- mice (open circles) as
                                                                                measured by real-time PCR. (* p<0.05).
                                                        
                                
                               
                    
                    
                    
                    
                    
                   
            
            
            
            
            
            
            
            
            
            
                  
                     BMAL1
                                              deficiency disrupts circadian expression of mPer2 and mCry1 genes
                                              in the brain
                                          
                    
                          In
                                                complex with CLOCK (or its close tissue-specific homolog, NPAS2) BMAL1 controls
                                                rhythmic expression of target genes, and BMAL1 deficiency results in disruption
                                                of rhythmic pattern of gene expression in the SCN and liver [12]. We decided to
                                                investigate how the absence of BMAL1 will affect the expression of BMAL1 target
                                                genes in the brain. As demonstrated in Figure 2b, rhythmic pattern of
                                                expression of two core circadian genes, mPer2 and mCry1 in the
                                                brain of BMAL1-deficient animals was significantly impaired with the mPer2
                                                gene being mostly down-regulated and mCry1 up-regulated. This pattern of
                                                expression was previously observed in the SCN and liver of Bmal1-/- mice
                                                and was attributed to the dual role of the BMAL1:CLOCK complex in transcription
                                                regulation [19]. Importantly, both PER2 and
                                                CRY1 were recently implicated in memory and learning [20,21].
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                   
            
            
            
            
            
            
            
            
            
            
                  
                     BMAL1
                                              deficiency results in disruption of ROS homeostasis in the brain
                                          
                    
                          Aging is associated with increased oxidative stress in
                                                many tissues, including the brain. Recently, oxidative stress and misbalance in
                                                reactive oxygen/nitrogen species (ROS/RNS) homeostasis was proposed as a
                                                mechanism for age-dependent changes in brain physiology, including decline in
                                                memory and learning [22]. Previously we have demonstrated that BMAL1 is
                                                directly involved in the regulation of ROS/RNS homeostasis, and that
                                                accelerated aging characteristic for  Bmal1-/- mice, at least in part,
                                                can be attributed to excessive production of ROS in some tissues of Bmal1-/-
                                                animals [4]. This prompted us to compare the levels of ROS in the brain of wild
                                                type and Bmal1-/- mice.
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          
                              
                                
                                Figure 3. BMAL1 deficiency disrupts ROS homeostasis in the brain.  (a) ROS
                                                                                level in the brain of wt and Bmal1-/- mice was detected in the indicated
                                                                                time points of the circadian cycle. (b) Average ROS level in the
                                                                                brain of wt and Bmal1-/- mice for 24h (* P<0.05).
                                                        
                                
                               
                    
                    
                    
                    
                    
                          To
                                                account for possible daily fluctuations, the level of ROS was measured in
                                                brains of wild type and Bmal1-/- mice collected throughout the day every
                                                4 hrs. The level of ROS in the total brain extracts did not show any obvious
                                                circadian pattern; however, at each time point it was significantly higher in Bmal1-/-
                                                mice (except for the time of maximum level of ROS for the wild type (CT34)). As
                                                a result, in mutant mice the average daily levels of ROS in the brain were 20%
                                                higher [t-test P < 0.01] (Figure3b). Thus, BMAL1 deficiency results in
                                                excessive production of ROS and chronic oxidative stress in the brain, which
                                                may affect various brain-specific metabolic processes including memory
                                                formation.
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                   
            
            
            
            
            
            
            
            
            
            
                  
                     Deficiency
                                              of circadian proteins CLOCK and CRY1,2 differentially alters habituation and
                                              exploratory activity
                                          
                    
                          The
                                                observed behavioral phenotype of Bmal1-/- mice may result from
                                                desynchronization of physiological activity of neurons due to disruption of the
                                                circadian oscillator. On the other hand, it may be unique to Bmal1-/-
                                                mice and result from disruption of the BMAL1-dependent control of tissue
                                                homeostasis. To discriminate between these two possible mechanisms in the
                                                regulation of hyperactivity and habituation, we studied the exploratory
                                                behavior of arrhythmic mice with disrupted activity of other circadian
                                                proteins.
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          We have chosen mice with the deficiency
                                                of the two Cry genes (Cry1,2-/- double knockout mice) and mice with the homozygous mutation of the BMAL1 transcription
                                                partner, CLOCK (Clock/Clock mutant mice). Previous work has shown that
                                                these two models, along with the Bmal1-/- model, may be approximated by
                                                two opposite functional states of the BMAL1:CLOCK transcription complex. Thus,
                                                functional deficiency in BMAL1 or CLOCK proteins results in the absence of
                                                transactivation of the target genes, while the absence of the CRY1,2 proteins
                                                cause constantly elevated expression of circadian target genes. All these
                                                mutants demonstrate disruption of rhythmic pattern of locomotor activity and at
                                                the gene expression level [12-14].
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          Cry1,2-/- and Clock/Clock mice were placed in novel
                                                environment, similarly to experiments described for wild type and Bmal1-/-
                                                animals. In contrast to Bmal1-/- mice, they did not demonstrate
                                                hyperactivity in locomotion: the activity of Clock/Clock on day1 was
                                                indistinguishable from that of the wild type [F[1,5] = 1.77, P = 0.241], while Cry1,2-/-
                                                animals were even less active [F[1,5] = 3.23, P = 0.132] (Figure 4 and 5, left
                                                panels). Both Clock/Clock [F(11,55) = 13.12, P<0.001] and Cry1,2-/-
                                                [F(11,55) = 8.02, P<0.001] mice showed intrasessional habituation on day1
                                                similar to that of the wild type mice: distance traveled during the last 15
                                                minutes decreased more than 2 fold compared to the first 15 minutes. On day2, Clock/Clock
                                                mice demons-trated the level of locomotor activity indistinguishable [F[1,5] =
                                                3.95, P = 0.103] from that on day1.  Thus, although Clock/Clock mice
                                                showed intrasessional habituation similar to wild type (both on days 1 and 2),
                                                there was no intersessional habituation (no significant difference between days
                                                1 and 2). These data suggest that that Clock/Clock mutant mice have
                                                normal formation of the immediate memory of novel context and impaired
                                                long-term memory. Locomotor activity of Cry1,2-/- mice on day2 was
                                                significantly lower than on day1 (Figures 4 and 5, left) (2.0 folds, [F[1,5] =
                                                27.19, P = 0.003]), suggesting that Cry1,2-/- demonstrate both intra-
                                                and intersessional habituation.
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          While the level of horizontal activity of Clock/Clock
                                                mutants was similar to the horizontal activity of wild type mice, Clock/Clock
                                                mutants demonstrated elevated rearing activity [F[1,5] = 7.65,  P = 0.04],
                                                which was intermediate between that of wild type and Bmal1-/- animals (Figure 4 and 5, right). In contrast with the case of locomotion (normal intarsessional
                                                habituation and no intersessional habituation), there was no difference in rearing activity of Clock/Clock mutants between
                                                day1 and day2 [F[1,5] = 0.44, P = 0.538], and only insignifi-cant decrease in
                                                rearing between the first and the last 15 min of the experiment on both days
                                                (T-test P = 0.1 and P = 0.6, respectively). Rearing behavior of Cry1,2-/-
                                                mice on day1 was similar to wt (with a tendency to be lower) (T-test=0.6) (Figure 5, right); however, rearing activity of Cry1,2-/- on day2 constantly
                                                remained at the habituated level and was significantly lower than wt [F[1,5] =
                                                48.63, P<0.001] (Figure 4, right).
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          
                              
                                
                                Figure 4. Open field analysis of exploratory activity and habituation of Clock/Clock and Cry1,2-/- mice.  Relative locomotor and rearing
                                                                            activity of Clock/Clock and Cry1,2-/-  mice on days 1 and 2
                                                                            (normalized to the average distance/activity level on day1) (* P<0.05).
                                                        
                                
                               
                    
                    
                    
                    
                    
                          Taken together, these results demonstrate a correlation
                                                between the level of activity and memory formation on one hand and transcription
                                                status of the BMAL1:CLOCK complex on the other.
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          
                              
                                
                                Figure 5.   Exploratory
                                                                                    activity of wild type and circadian mutant mice. (Upper panel)
                                                                            Locomotor and rearing activity measured in 5 min increments during 1 hr on
                                                                            day1 for wt (diamonds), Bmal1-/- (squares), Clock/Clock
                                                                            (triangles) and Cry1,2-/- (crosses) mice. Statistically significant
                                                                            difference with wt activity is shown as p values. Difference between wt, Clock/Clock
                                                                            and Cry1,2-/- locomotor activities, and between rearing activities
                                                                            of Bmal1-/- vs. Clock/Clock and wt vs. Cry1,2-/- is
                                                                            not statistically significant. (Lower panel) Cumulative traveled
                                                                            distance and rearing activity on days 1 and 2; For upper panels p values of
                                                                            statistically significant differences between wild type and circadian
                                                                            mutants are indicated. For lower panels * P<0.05.
                                                        
                                
                               
                    
                    
                    
                    
                    
                   
            
            
            
            
            
            
            
            
            
            
                  
                     Deficiency
                                              in activity of the core circadian proteins BMAL1, CLOCK or CRY1,2 results in
                                              different behavioral patterns in the open field
                                          
                    
                          Cumulative
                                                data on locomotor and rearing activities showing significant differences
                                                between the animals of all tested genotypes are summarized in Figure 5. Thus,
                                                total distance traveled by Bmal1-/- mice on both days greatly exceeded
                                                the distance traveled by the wild type [day1 fold 2.8, t-test P <0.01; day2
                                                fold 4.7, P <0.001], Clock/Clock [day1 fold 2.3, t-test P <0.01;
                                                day2 fold 2.4, P <0.01], or Cry1,2-/- [day1 fold 3.9, t-test P
                                                <0.001; day2 fold 6.9, P <0.001] animals (Figure5, left panels). Cry1,2-/-
                                                mice demonstrated the lowest level of horizontal activity, while the locomotion
                                                of the Clock/ Clock animals was comparable to that of the wild type. Remarkably, the horizontal activity of Bmal1-/-
                                                and Clock/Clock mutants remained the same on both days of the experiment, whereas wild type and Cry1,2-/-
                                                animals demonstrated significant reduction in activity on day2 [wt fold 2.0
                                                t-test P <0.02; Cry1,2-/- fold 2.1, P <0.01] (Figure 5, lower
                                                left). Rearing activity of Bmal1-/- and Clock/Clock animals was
                                                elevated compared to wt [Bmal1-/- day1 fold 2.3, t-test P <0.01, day2
                                                fold 4.7, P <0.001; Clock/Clock day1 fold 1.8, P <0.01, day2 fold
                                                3.2, P <0.001] and showed no differences between the two sessions. In
                                                contrast, wild type and Cry1,2-/- mice showed low rearing activity and
                                                robust intra- and intersessional habituation  (Figure 5, right panels).
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          
                              
                                
                                Figure 6.   Circadian
                                                                                    mutant mice do not demonstrate anxiety phenotype. (Upper panel,
                                                                                    left) Average horizontal velocity for all genotypes measured during 1h
                                                                            on days 1 and 2.  Average velocity does not significantly differ between wt
                                                                            and Bmal1-/- animals; slight (~15%) but statistically significant
                                                                            decrease in average velocity is detected for Clock/Clock and Cry1,2-/-
                                                                            mice compared with wt and Bmal1-/-.  (Upper panel, right)
                                                                            Cumulative time spent in the center for all genotypes measured during 1 hr
                                                                            on days 1 and 2. (Lower panel) Time spent in the center square of
                                                                            the open field arena on days 1 and 2 by wt, Clock/Clock, Bmal1-/-,
                                                                            and Cry1,2-/- mice. *P<0.05.
                                                        
                                
                               
                    
                    
                    
                    
                    
                   
            
            
            
            
            
            
            
            
            
            
                  
                     Circadian
                                              mutants demonstrate normal or decreased anxiety levels in the open field
                                          
                    
                          The increase/decrease in the distance
                                                traveled by different circadian mutants may result from either differences in
                                                time spent in motion vs. rest time, or from the differences in the velocity
                                                among the genotypes. However, an average velocity of animals, calculated based
                                                on horizontal distance and time in horizontal motion, was mostly uniform in
                                                animals of all genotypes, except for Clock and Cry1,2-/-  mice
                                                that showed slight (~15%) but statistically significant reduction of speed
                                                [t-test P <0.05] (Figure 6, upper left). This suggests that Bmal1-/-
                                                and Clock/Clock mice were in  fact longer in motion,
                                                whereas Cry1,2-/- were less in motion on both days when compared to wild
                                                type, rendering a hyperactivity phenotype for Bmal1-/- and Clock/Clockanimals.
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                          High
                                                locomotor and rearing activity and deficit of contextual habituation often
                                                correlate with elevated level of anxiety, which can be accessed by the amount
                                                of time spent in the center of the OF (a risk-taking behavior) [23]. To
                                                evaluate the level of anxiety in animals of all four circadian genotypes, we
                                                compared the time they spent in the central zone of the OF (Figure 6). On day1
                                                of the experiment, Bmal1-/- and wild type mice spent about 14% of the
                                                time in the central zone, while the corresponding time in Cry1,2-/- and Clock/Clock
                                                mice was more than two-fold higher (37% and 30% respectively [t-test P
                                                <0.01]) (Figure 6, upper right).  The differences between the wild type and Bmal1-/-,
                                                and between Clock/Clock and Cry1,2-/- animals were not
                                                significant. Compared to day1, the amount of time spent in the center on day2
                                                was not changed in Bmal1-/- , whereas in wild type and Cry1,2-/-
                                                mice it was decreased two-fold [t-test P <0.01]. Interestingly, cumulative center
                                                time of Clock/Clock mice on day2 showed even a tendency for increase but
                                                did not reach statistical significance. Thus, none of the tested circadian
                                                mutants displayed a pro-anxiety phenotype in the open field paradigm. On the
                                                contrary, Clock/Clock and Cry1,2-/- demonstrated opposite, more
                                                risk-taking behavior. A decrease in center time on day2 observed in wild type
                                                and Cry1,2-/- mice correlates with a decrease in total locomotor and
                                                vertical exploratory activity (indicative of habituation).  Bmal1-/- again
                                                did not demonstrate any difference in performance between days 1 and  2, while Clock/Clock
                                                mutant mice demonstrated an increase in time spent in the center.
                                                Interestingly, mice of different genotypes had different patterns of the
                                                risk-taking behavior. Wild type mice "took the risk" of short raids in the
                                                middle of the brightly-lit arena during the first 30 min and then moved mainly
                                                along the walls or sit in one of the corners (Figure 6, middle left). Bmal1-/-
                                                mice continued to move across the center during the entire session (Figure 6,
                                                lower left). Both Cry1,2-/- and Clock/Clock mice had an increase
                                                in time spent in the center after first 10 min, during which they had prolonged
                                                periods of sitting in the middle of the arena - a very unlikely behavior for wt
                                                mice (Figure 6, middle and lower right). These data clearly demonstrate the
                                                lack of correlation between the locomotor/rearing activity and time spent in
                                                the center of the open field in different circadian mutants. Thus, hyperactive Bmal1-/-
                                                demonstrated "normal" level of anxiety, while both hyperactive Clock/Clock
                                                and hypoactive Cry1,2-/- had decreased level of anxiety. Therefore,
                                                hyperactivity and deficit of contextual habituation of Bmal1-/- and Clock/Clock
                                                cannot be explained by the increase in the level of anxiety in these mice.
                                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                    
                   
            
            
            
            
            
            
            
            
           
          
             Discussion
            
                  Decline in mental performance, including
                                    deficits in memory formation, learning and adaptation to novelty are hallmarks
                                    of aging. At the same time, it is well documented that the activity of the
                                    circadian clock decreases with age [24]. Reciprocal relationships between the
                                    decline in the circadian clock activity and deterioration in mental performance
                                    are currently a subject for active discussions [25]. In this study we propose
                                    that the activity of the circadian proteins is important for adaptation to
                                    novelty, which is one of the aspects of daily interactions between an organism
                                    and its changing environment. Our results demonstrate that habituation to
                                    novelty is differentially altered in mice with a deficiency/mutation of the
                                    core circadian genes Bmal1, Clock, or Cry1 and Cry2  and
                                    correlates with the transcription activity status of the BMAL1:CLOCK: [CRY1,2]  complex.
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  Exploration behavior is thought to be induced by a novelty
                                    detected by the hippocampus which works as a comparator of the stored spatial
                                    "maps" - memory of visited places - and perception of an unknown space. As the
                                    animal acquires information of the new space, a novel spatial map is generated
                                    and exploratory behavior ceases (which is referred to as intrasession
                                    habituation in the open field paradigm, and depends on working memory). When
                                    placed in the same environment on consequent days, mice demonstrate
                                    significantly reduced exploratory activity, which is interpreted as a sign of
                                    acquiring of long-term memory about the place (intersessional habituation)
                                    [1-3,17]. Thus, habituation is thought to depend on short- and long-term
                                    memory [26-28]. Deficiency in the intrasession habituation of Bmal1-/-
                                    mice is indicative for working memory impairments. Recently, circadian
                                    modulation of short-term memory was shown in Drosophila [29] and humans [30].  Severe
                                    deficiency in the intersession habituation demonstrated by Bmal1-/- and Clock/Clock
                                    mice both in locomotion and rearing suggests that Bmal1-/- and Clock/Clock
                                    mice lack memory of the previous day experience and allows speculating that
                                    transcription activity of the BMAL1:CLOCK complex is necessary for the LTM
                                    formation, which requires de novo synthesis of both RNA and protein 
                                    [31].  Importantly, LTM was shown to depend on time of the day for LTM
                                    acquisition/retrieval [32], which may reflect daily fluctuations in BMAL1:CLOCK
                                    transcription activity.  Facilitation of both intra- and intersession
                                    habituation demonstrated by Cry1,2-/- mice further strengthens the role
                                    of BMAL1, CLOCK and CRY1,2-associated transactivation and transrepression of
                                    gene expression in memory function. Interestingly, although Cry1,2-/-
                                    mice exhibit a deficit in time-place learning, which was attributed to
                                    disrupted time-keeping system, no deficits were observed in learning abilities
                                    of Cry1,2-/- mice in several not-time associated learning tasks [21].
                                    Our results suggest that LTM and/or STM formation in these animals is
                                    facilitated; however, more specific learning/memory tests are necessary to
                                    dissect various types of memory influenced by CRY1,2 as well as other circadian
                                    proteins. These observations and several recent reports indicate a close
                                    connection between the activity of the circadian system and memory formation.
                                    Circadian cycling was recently proposed as a mechanism for the proper memory
                                    consolidation [33], probably through the circadian oscillation of MAP kinase
                                    activity reported in the mouse hippocampus [34]. Circadian modulation of memory
                                    formation has been shown for different model organisms such as Aplysia,
                                    Drosophila, zebrafish and rodents; a growing body of evidence implicates the
                                    circadian regulation of learning and cognitive performance in humans [11]. More
                                    data on specific roles of individual circadian proteins in different forms of
                                    memory are accumulated from studies of mice with deficiencies in these
                                    proteins. Thus, mice deficient in NPAS2 have
                                    impaired cued and contextual fear memory [35]. Per2-/- mice demonstrate
                                    impairment in trace fear memory, but not in cued fear memory [20]. Per1-/-
                                    mice exhibit spatial learning deficits in the radial arm maze [18]. 
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  Exposure to a novel environment is mildly stressful and
                                    inherently arousing experience for mice [1-3]. Failure of the Bmal1-/- mice
                                    to habituate within a single session could also be attributed to their
                                    inability to cope with the novelty-induced stress resulting from functional
                                    disruption of one or several brain modulatory systems [2], which might be the
                                    cause of hyperactivity in both locomotion and rearing in these mice. Indeed,
                                    the circadian clock is involved in control of the rate-limiting enzyme in the
                                    biosynthesis of dopamine - tyrosine hydrolase (TH, also known as monooxygenase)
                                    expression; TH expression is reduced in Per1-deficient mice [9], whereas
                                    it is greatly elevated in Clock/Clock mutants [8]. Significant
                                    hyperactivity in the open field was reported for several transgenic mice with
                                    disturbed dopamine regulation [36]. Interestingly, recently was shown that
                                    modulation of the hippocampus-dependent memory by attention is
                                    dopamine-mediated [37]. Further study on dopamine level and bioavailability in
                                    circadian mutants will help to determine whether the observed changes in the
                                    activity of circadian mutants occur through dopamine-dependent or independent
                                    mechanisms. On the other hand, hyperactivity is often associated with elevated
                                    anxiety [38]; however, the anxiety level of Bmal1-/- mice did not
                                    significantly differ from the wild animals judging by the time spent in the
                                    center of the arena. Importantly, hyperactivity of Bmal1-/- mice was
                                    associated with novelty, because average home cage activity does not differ
                                    between wt and Bmal1-/- animals [12]. In contrast, Clock/Clock
                                    mutant mice exhibited the pattern of horizontal activity similar to wild type;
                                    however, their rearing activity was almost two-fold higher compared with wt.
                                    Horizontal locomotion correlates with cognitive component of exploratory
                                    behavior, while rearing behavior is considered to reflect motivational
                                    component [28]; together with the fact that Clock/Clock mutants spent in
                                    the center of the open field arena twice more time than wt animals, these data
                                    suggest that Clock/Clock mice demonstrate enhanced activity-based
                                    arousal and reduced anxiety, which is in good agreement with observations made
                                    by [39]. In sharp contrast to Bmal1-/- and Clock/Clock mutant
                                    mice, Cry1,2-/- mice were less active in the open field experiments; at
                                    the same time, time spent in the center of the open field arena was almost
                                    three-fold higher in Cry1,2-/- mice when compared to wild type and Bmal1-/-,
                                    and was comparable with that of the Clock/Clock mutants - the pattern
                                    which can be interpreted as a sign of greatly reduced anxiety in these animals.
                                    These observations reinforce the previously reported data on the involvement of
                                    the circadian proteins in the regulation of mood [8,9]. 
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  ROS/RNS are important regulators of cellular signaling; any
                                    misbalance can be critical for brain physiology and affect various mental
                                    functions, [40-42], therefore, their production and detoxification are tightly
                                    controlled by the system of ROS/RNS-generating and antioxidant enzymes. Chronic
                                    oxidative stress in an aging brain is one of the main reasons for
                                    age-associated mental decline [22]. Here we show that BMAL1 deficiency
                                    significantly disturbs the normal ROS level in the brain. Thus, BMAL1-dependent
                                    control of ROS can be one of the potential mechanisms of the observed
                                    behavioral changes of the circadian mutants. Indeed, as already has been
                                    mentioned above, the circadian oscillation of MAP kinase activity in the
                                    hippocampus is critical for memory formation, although the mechanisms of cyclic
                                    activity of MAPK are unclear [34]. ROS are critical regulator of MAP kinase
                                    activation and MAP kinase signaling pathway [43], thus, the observed circadian
                                    oscillation of ROS level in the brain can be at least partially responsible for
                                    the oscillation of MAPK activity.
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  Using
                                    experimental settings within the open field paradigm, which embraces the
                                    established behavioral tests for exploration and adaptation to novelty in rodents,
                                    we have found that activity of the core circadian clock proteins BMAL1, CLOCK
                                    and CRY1,2 is necessary for the regulation of exploratory behavior in mice.
                                    Opposite phenotypes of Bmal1-/- and Clock/Clock mutant mice on
                                    one hand and Cry1,2-/- on the other suggest that the changes in the
                                    novelty-induced behavior in these animals are not the result of the general
                                    disruption of the circadian clock, but rather indicate that individual protein components of  the molecular clock
                                    play non-identical roles in habituation. Therefore, the exploratory performance
                                    depends on the mutual balance of activities of these proteins, while the
                                    general regulation of these activities by the circadian clock warrants the
                                    optimization of the performance. It is well documented that aging affects the
                                    circadian system [24]; here we suggest that aging also affects the mutual
                                    balance between circadian proteins, which in turn affects mental performance.
                                    Our results suggest the involvement of the circadian proteins in
                                    fundamental processes of memory formation, and
                                    encourage further investigations into the role of the circadian proteins in
                                    memory, learning behavior and age-associated mental decline.
                        
            
            
            
            
            
            
            
            
            
            
            
            
           
          
             Experimental
                                  procedures
            
                  Animals.
                            Bmal1-/-mice were obtained from Dr. C.
                                    Bradfield (University of Wisconsin)  [12], Clock mutant mice were
                                    obtained from Dr. J. Takahashi (Northwestern University) [13], and Cry1,2-/-knockout mice were obtained from Dr. A. Sancar (University of North
                                    Carolina at Chapel Hill) [14]; details of target gene knockout strategies and
                                    animal generations can be found in the above cited publications. All mutants
                                    were backcrossed to C57BL/6J inbred strain (The Jackson Laboratory, Bar Harbor,   ME, USA) for 12 generations. Wild type and Bmal1-/- mice were
                                    generated by breeding of Bmal1+/- males with Bmal1+/- females. Clock
                                    mutants were generated by breeding of Clock/Clock males with Clock/wt
                                    females, Cry1,2-/- were generated by breeding of Cry1,2-/- males
                                    with Cry1+/-, Cry2-/- females. Wild type mice generated as a result of Bmal1+/-
                                    breeding were used as a control for all experiments (since after 10 backcross
                                    generations the line is 99% genetically identical to the recipient strain,
                                    mutants (backcrossed to C57BL/6J for 12 generations) and wild type were
                                    considered as congenic with C57BL/6J background).  For all experiments wild
                                    type and mutant mice were randomly picked from several independent litters. 
                                    Animals were maintained on a 12:12 light:dark cycle with lights on at 7:00 am,
                                    on regular diet. For tissue collection animals were transferred to constant
                                    darkness and tissue samples were collected with 4 hour intervals beginning
                                    after 34 hours of exposure to DD, immediately frozen on dry ice and stored at -
                                    80°C. All animal studies were conducted in accordance with the regulations of
                                    the Committee on Animal Care and Use at Cleveland State University and Roswell
                                    Park Cancer Institute.
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  Open field exploration.
                             A mouse was
                                    placed in the bright-lit 50x50 inches Plexiglas square box, and the activity of
                                    the animal was monitored with 16x16 photobeam activity system (San Diego
                                    Instruments). Animal activity was recorded every 5 minutes during 1 hour on the
                                    day1 and day2 (24h later), and analyzed using Open Field Software. All
                                    experiments were performed with 3-4 month old male mice between 11 am and 4 pm,
                                    at least 6 animals of each genotype were analyzed.
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  RNA isolation and real-time PCR analysis.  
                            Total RNA was isolated from the brain with TriZol
                                    reagent (Invitrogen) according to the manufacturer's protocol. RNA quantitation
                                    was performed using TaqMan real-time RT-PCR, relative mRNA abundance was
                                    calculated using the comparative delta-Ct method with GAPDH mRNA as standard. Procedure
                                    and primer sequence was previously described [19].
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  Immunohistochemical analysis.
                             Frozen brain coronal sections (10 μm)
                                    were fixed with 4% PFA dissolved in PBS (pH 7.5) for 10 min, permeabilized with
                                    0.5% Triton X-100 for 5 min. The sections were incubated with primary
                                    anti-BMAL1 antibodies raised in guinea pig  followed by incubation with donkey
                                    anti-guinea pig secondary antibody labeled with DyLight488 (Jackson
                                    ImmunoResearch laboratories), incubated for 1 min with 
                                    4'-6-Diamidino-2-phenylindole (DAPI, 300nM, Invitrogen), mounted under cover
                                    slips using Fluoromount G  media (SouthernBiotech). The slides were kept in the
                                    dark at +4oC until use. Microphotographs were taken with the aid of
                                    Leica DMR upright microscope equipped with Princeton Instruments MicroMax 5
                                    MHz-cooled CCD camera and ImagePro software.
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  ROS
                                            analysis.
                             ROS levels were determined in tissue extracts using
                                    ROS sensitive fluorescent dye as described elsewhere [4]. Briefly, brain was
                                    immediately frozen on dry ice and stored at -70o C until analysis.
                                    After mixing with 10 volumes of homogenization buffer and normalizing by
                                    protein content, brain extracts were mixed with dichlorodihydrofluorescein
                                    (DCF) in homogenization buffer and incubated in the dark at 37 o C
                                    for 30 min. Fluorescence at 495/535nm was measured using Victor2 Wallac
                                    microplate reader (Perkin Elmer). At least 3 animals were used for analysis for
                                    every time point and genotype.
                        
            
            
            
            
            
            
            
            
            
            
            
            
                  Statistical
                                            analysis.
                             Six male mice of each
                                    genotype were used for all experiments. Data are shown as mean + standard
                                    deviation. SigmaStat software package was used for analysis. Effects of
                                    genotype (circadian mutants versus wild type) and novel/familiar environment
                                    (day1 versus day2) on behavioral variables collected in open field experiments
                                    were tested for significance with Two Way Repeated Measures ANOVA. Bonferoni
                                    t-test was used for all pairwise multiple comparison procedures. Unpaired
                                    Student's t-test was used for comparison of total activities between day1 and
                                    day2 for the same genotype or the same day for different genotypes. Unpaired
                                    Student's t-test was used for comparison of between genotype variations in
                                    relative gene expression and ROS level at different time points. P<0.05 was
                                    considered as statistically significant.
                        
            
            
            
            
            
            
            
            
            
            
            
            
           
          We
                        thank Yelena Kondratova for the editorial help. This work was supported by
                        start-up fund and AHA grant 0835155N to R.V.K. and NIH grants CA102522 and
                        GM075226 to M.P.A.
            
            The authors of this manuscript have no conflict of
                            interests to declare.