Abstract The snail Calliostoma canaliculatum secretes a yellow mucous ('Yellow Stuff' or YS) in response to attack from predatory starfish Pisaster giganteus and Pycnopodia helianthoides. Previous studies have shown that YS inhibits the opening of voltage-gated potassium channels, and the active component responsible for this action is proposed to be a serotonin dimer derivative, 6-bromo-2-mercaptotryptamine. Because serotonin is a crucial neurotransmitter in invertebrates, components of YS may also have an effect on the behaviour of neural networks where serotonin plays a role. Several lines of experiments were carried out to identify any possible relationships between the actions of these two compounds. Behavioural studies on the brittle star Ophiopteris papillosa, showed a similar response to both these compounds - immediate arm retraction. Results from these experiments established a biologically relevant concentration of YS for further testing. Control experiments carried out in Shaker potassium channels expressed in Xenopus oocytes demonstrated that at this concentration, YS did not lead to a slowing of K-current activation. Additional experiments were performed using the buccal ganglia of Aplysia californica. B cells in this ganglia contain serotonin receptors and many of the cells and synaptic connections are modulated by serotonin. Single electrode recordings from B cells after application of serotonin demonstrated a marked increase in spontaneous activity (action potentials and post-synaptic potentials). Subsequent application of YS significantly decreased this activity, and further application of serotonin after YS had been washed away, renewed activity. This suggests that in the neural circuits involved in stimulation by serotonin, YS may function as an antagonist, and therefore Yellow Stuff may be acting in invertebrates via neuromodulatory pathways that involve serotonin. 2 Introduction The gastropod Calliostoma canaliculatum which lives in the kelp forest of Monterey Bay has an interesting and aggressive escape mechanism that distinguishes it from other snails of this genus. In order to escape from its predators, the seastars Pycnopodia helianthoides and Pisaster giganteus, C. canaliculatum, it will secrete a yellow mucous (Yellow Stuff or YS), from its hypobranchial gland, that causes the seastar to retract its tube feet or to physically move away from the exudate. Previous studies (Bryan et al, 1997) focused on the behavioural response of the seastars to this exudate, but attempts at purifying and identifying this compound were unsuccessful. It was only recently that an active component of Yellow Stuff was identified (Sack et al) to be 6-bromo-2-mercaptotryptamine, a serotonin dimer derivative (fig 1). This compound affects Shaker potassium channels expressed in Xenopus oocytes. The most prominent effects of 6BrMT (or raw Yellow Stuff) are a marked slowing of activation kinetics and a reduction of peak potassium current amplitude. However, there have been no tests of either Yellow Stuff or 6BrMT on any serotonergic system despite the obvious structural similarity of serotonin and 6BTMT. The goal of this investigation was to demonstrate a relationship between Yellow Stuff and serotonin using a variety of different lines of experiments, and more specifically to determine if Yellow Stuff was behaving in an agonistic or an antagonistic manner in relation to serotonin. Materials and Methods Specimens: Specimens of Calliostoma canaliculatum and Ophiopteris papillosa were collected from Monterey Bay by Sealife Supply (Sand City, CA). Pycnopodia helianthoides was collected from the Great Tide Pool in Pacific Grove, CA. Aplysia californica were from the National Resource for Aplysia, University of Miami, FL.. Immediately after arrival all organisms were placed in separate holding tanks with circulating natural seawater at 12°C. Yellow Stuff Extraction: In order to extract the hypobranchial gland, the snail was anaesthesised in a solution of 7.5% MgCl2 in dH2O and natural seawater (mixed in a 1:2 ratio) for 15 minutes. The shell of the snail was then cracked with a vise, and the snail was pinned down in order to extract its gland. The average mass of a gland was 0.040g. 0.8ml of natural seawater was then added and the gland was homogenized. The supernatant was then removed and centrifuged at 12,000 RPM for 15 minutes. This solution of YS had a concentration of 0.05g/ml of NSW. This solution was fürther diluted by 100 times with seawater for use in the experiments below. All solutions were kept at 4°C until ready for use. Seastar response to Yellow Stuff and serotonin: Individual Ophiopteris papillosa were placed in a plastic container measuring 15cm by 20cm by 1Ocm containing 1800ml of natural seawater. Äfter each assay, the container was rinsed and the seawater replaced. The seastars acclimated in the box for five minutes before any tests were carried out A variety of compounds were tested: 1:10 and 1:100 YS, ImM 5-HT, O.1mM 5-HT, 1mM octopamine, and 1mM 5-hydroxytryptophan.. Using a Pipetman, 5Oul of the compound, was slowly ejected Icm away from the seastar’s arm. Care was taken to ensure that the force of the ejected liquid did not cause a reaction from the seastar. Controls were carried out by applying 50ul of natural seawater Icm away from the seastar’s arm. Äfter each assay, the seastar was returned to its tank, and a different seastar used. The same seastar would not be used more than once a day to avoid desensitization. Together there were 6 Ophiopteris papillosa, and over a period of two weeks each seastar was used in an average of 12 assays. Similar trials were performed on the single Pycnopodia helianthoides specimen. Behavioural responses to application of the test solutions were classified using a scale of 0 to 3, where 0 = no reaction, 1 = arm tip recoil, 2 = whole arm recoil, and 3 = whole arm recoil accompanied by movement of seastar away from application site. Data were analysed using the chi-squared test. Intracellular recordings from Aplysia buccal ganglion Buccal ganglia from Aplysia californica were excised, and desheathed in order to expose the B cells. Once excised and desheathed the cells were healthy for up to 36 hours if stored in natural seawater at 4°C. The ganglia was pinned to a layer of Sylgard at the bottom of a perfusion chamber. Recordings were performed in this chamber with volume 1.5ml. An input tube for fresh seawater and output tube operated by a vacuum pump allowed the solution in the chamber covering the ganglia to be replaced at anytime. Once the ganglia was desheathed, it was hard to specifically identify particular cells, however it was unnecessary to pinpoint the exact cells as it was an area of the ganglion that was of specific interest. This area was the region with the Bl and B2 cells (bottom half of the ganglion) in which many cells are recognised as having serotonin receptors (Gerschenfeld and Paupardin-Tritsch, 1974). These neurons were impaled with a single micro-electrode that were filled with 3M KCl. Recordings were done at room temperature. Three different protocols were followed. A baseline recording of the cell was taken for 3 minutes with the ganglia immersed in fresh seawater. 50ul of 1:100 YS was then added to the bath using a Pipetman, and a recording was taken immediately after this for 3 minutes. 2. A baseline recording of the cell was taken for 3 minutes. 5O0ul of 1mM 5-HT was then added to the bath and a recording taken for 3 minutes. 50ul of 1:100 YS was then added into the same bath without perfusing the previous solution out, and a recording was taken for another 3 minutes. 3. A baseline recording of the cell was taken, 5Oul of 1mM 5-HT was then added, a recording taken for 3 minutes, followed by addition of 50ul 1:100 YS and another recording taken for 3 minutes. The ganglia was then perfused with natural seawater for several minutes in order to wash away all the compounds previously added. 5Oul of 5- HT was then added again to the bath, and a third recording was taken of the cell. In addition, control recordings of 10 minutes were run to ensure that the effect of YS on the cell was not confounded by the decrease in serotonin induced activity. Because desensitization of the cells in the ganglia to both YS and 5-HT was a potential problem, only a few recordings could be used from each freshly desheathed ganglia. Voltage clamp: In conjunction with Michael Hughes, voltage clamp was performed on Shaker A6-46 channels expressed in Xenopus oocytes bathed in ND96. 2 glass microelectrodes with resistances between 0.7 and 2.0 M£2 were inserted just below the surface of the oocyte membrane and a holding potential of -60mV was established using a conventional two-electrode voltage clamp. Ooctyes were subjected to voltage pulses lasting 25 ms and stepped at 10 mV increments between -50 and 40 mV. 1:100 dilution of YS was added to the bath by perfusion. A family of Ig traces at various voltages were recorded upon establishment of a successful voltage clamp; after a control solution change to ND96 in a 1:100 dilution with seawater, and again after the addition of 1:100 YS. To wash out the YS, 3-4 ml of ND96 in 1:100 dilution of seawater was used (to control for the effects of natural seawater). The solution of YS used was from the same stock of YS used for the intracellular recordings on the buccal ganglia. Results Preliminary behavioural studies showed that Ophiopteris papillosa responded to Yellow Stuff, although it is not a predator of C. canaliculatum. This class of echinoderms is unique in its anatomy, in that it has giant axons present in the radial nerve cord which run the length of each arm and mediate rapid escape responses (Yee et al, 1986). As a result this seastar demonstrates a very visible and easily classifiable response to noxious chemicals. Responses to application of various compounds are summarised in fig. 2A. Seawater (the negative control) induced almost all level 0 responses, thus indicating that the force of ejection of the liquid from the Pipetman was not large enough to induce a behavioural response from the seastar’s sensitive arms. Application of both dilutions of Yellow Stuff resulted in a large percentage of level 2 and a significant number of level 3 responses. A chi-squared test concluded that the differences in frequency of each of the 4 levels was highly significant (p-value of «0.01). Application of YS at dilutions over 1:100 did not result in any significant responses (data not shown). Application of both concentrations of 5-HT also caused a high proportion of level 1 and level 2 reactions (p- value of £ 0.01). To show that this behavioural effect was not common to all biological peptides and amines, octopamine another common invertebrate neurotransmitter was applied. Over 60% of the responses were level 0, similar to application of natural seawater. Application of 5- hydroxytryptophan (the precursor to 5-hydroxytryptamine), resulted in an even spread of reactions from level 0 to level 3, and did not show any statistically significant differences between the frequency of the responses in the 3 levels. Pisaster giganteus did not respond to either 5-HT or Yellow Stuff in a manner that was easy to identfy in a reasonable period of time, therefore this species was not used.. As there was only one Pycnopodia specimen, the results may not be as valid as that of the Ophiopteris, but the response of this specimen did correspond with previous literature (Bryan et al, 1997). Again, as can be seen in fig. 2B, natural seawater did not elicit a response in Pycnopodia, while both YS and 5-HT resulted in a noticeably strong response. The Pycnopodia’s response to octopamine was similar to the response seen in Ophiopteris. Based on these results, it would appear that there is relationship between serotonin and Yellow Stuff in these seastars as both compounds elicited escape responses that could not be induced with octopamine or 5-hydroxytryptophan. These behavioural results give further credence to the idea that 6BrMT may act biologically by interacting with serotonergic pathways Intracellular recordings from the buccal ganglia of Aplysia californica In order to further investigate any effects Yellow Stuff may have on serotonergic pathways, a suitable assay based on the buccal ganglia of Aplysia was utilised. The buccal ganglia (see fig. 3) contains a central pattern generator (CPG) that mediates rhythmic movements of the buccal apparatus during feeding. The activity in the CPG is modulated by extrinsic serotonergic inputs from the giant cerebral neurons (Evgeni et al, 2000) making these cells an appropriate assay for comparison of YS and 5-HT. In experiments where 1:100 YS was applied to the bath without the presence of 5-HT, there is a clear trend - the application of YS did not change the baseline activity of the cell (see figs. 4A and B). The firing activity of the cell continued after application of YS, and although throughout a 3 minute recording the frequency of the action potentials in a cell does not usually remain constant (bursts of activity are seen followed by periods of relative inactivity), there was no discernable effect of YS on the activity of the cell, e.g. no PSPs were produced after application of YS, and the shape of the action potential remained the same. The B cells are primarily pacemaker cells firing regular action potentials but there were some that had a quiet baseline (see fig. 5A). In the cells that did not display any spontaneous activity (either in the form of post-synaptic potentials or action potentials) application of 5-HT to the bath resulted in the appearance of regular action potentials (fig. 5B) indicating 5-HT had an excitatory effect on the ganglia. Subsequent application of YS in the same chamber resulted in an immediate silencing of the cell - no further action potentials were seen (fig. 5C). In order to determine whether the effect of YS was reversible, the chamber and ganglia were perfused with natural seawater after the application of 5-HT and YS. After the application of ImM 5-HT following perfusion with seawater, the excitatory effect of serotonin was seen again to a similar extent of that seen after the first application of 5-HT. Fig. 6B shows an EPS. with an increase in the firing frequency of the action potentials situated over the small depolarising wave. This is not seen after application of YS (fig. 6C), but reappears after application of 5-HT (fig. 6D). The traces shown in these figures are representative of each of the 3 minute recordings. Effect of 1:100 YS on Shaker potassium channels Previous work (Sack et al) determined that application of 6BrMT at uM concentrations to Xenopus oocytes expressing Shaker potassium channels resulted in a marked slowing of activation kinetics and a reduction in the peak amplitude of Ig (fig. 7B). These effects were also seen when raw exudate was used (Sack, personal communication). However 1:100 dilution of YS used in the present study only resulted in a decrease in peak current amplitude, and no significant decrease in activation rate (Fig. 7A). The implications of this will be discussed in greater detail below. Discussion The results from the three different lines of experiments in this study indicate that Yellow Stuff is behaving via some serotonergic pathway. The behavioural studies provided a base for the latter electrophysiological experiements, by demonstrating a relationship between YS and serotonin that was not seen with other biological substances. These behavioural results thus provided a justification for further comparison of the two substances, and more importantly determined the threshold concentration beyond which no visible response from the seastars was observed. This dilution of YS was then used in all subsequent electrophysiology experiments The voltage clamp experiment demonstrated that at 1:100 dilution, YS was not affecting the activation kinetics of Shaker potassium channels, and the intracellular recordings from the Aplysia buccal ganglia clearly demonstrated the effect of YS on serotonergic activity. In 1974 Gerschenfeld and Paupardin-Tritsch first convincingly demonstrated that 5-HT functioned in Aplysia californica as a neurotransmitter by showing that of the 13 cells they studied in the buccal ganglia, nine had an excitatory response and four had an inhibitory response due to specific serotonin receptors. Using iontophoretic methods of application, they demonstrated that 5-HT resulted in pronounced EPSPs in buccal ganglia cells. The results obtained in this present study are therefore in accordance with previous literature, showing serotonin behaving in an excitatory fashion, either generating pronounced excitatory post- 10 synaptic potentials or in a few cases initiating action potentials. The application of YS after 5- HT resulted in a significant decrease of serotonin-induced activity. Thus, YS at a 1:100 dilution appears to be functioning as an antagonist of 5-HT. The buccal ganglia is responsible for generating rhythmic chewing and swallowing motions in the buccal apparatus through the central pattern generator (CPG) which produces buccal motor programmes, BMPs. The CPG receives extrinsic serotonergic inputs, e.g. from the serotonergic metacerebral cell (MCC) which synthesises 5-HT. Perfusion of a semi-intact head with 5-HT induced swallowing-like movements, seen in intracellular recordings as an increase in excitability, thus demonstrating that 5-HT is an important neuromodulator in the buccal ganglia system (Evgeni et al, 2000). As can be seen from fig. 5B and 6B, the application of 5-HI induced a large excitatory effect seen in most of the recordings as an increase in PSPs (as most of the B cells tested were pacemakers), and in the cells that were not pacemakers, this excitation was in the form of action potentials. Application of 1:100 YS after 5-HT resulted in a significant decrease in the cell’s activity indicating that YS functions as a serotonin antagonist. In addition. the application of 5-HT after perfusion of the ganglia with natural seawater (fig. 6D) resulted in the return of excitatory activity, therefore suggesting YS could be a reversible antagonist. Because the recordings were on intact ganglia where the cells were still a part of a large neural network, there is not enough evidence to determine whether YS is behaving as an antagonist on a cellular level or on the whole serotonergic system, although the structural similarities between 5-HT and 6BrMT provides strong indication that it might be antagonising at the cellular level. To determine whether YS is an antagonist of 5-HT at the receptor level would require isolation of the B cell and many more tests to be performed. 11 The lack of effect of 1:100 Yellow Stuff on Shaker potassium channels is consistent with the argument that YS is behaving antagonistically to serotonin. 6BrMT has a well documented effect on Shaker potassium channels - a reduction of peak potassium current amplitude and a reduced activation rate (Sack et al). With 1:100 YS, only one of these effects was visible (fig. 7A), therefore at this dilution YS has a much smaller effect on Shaker potassiuam channel kinetics. Since 1:100 YS has a pronounced effect on the serotonergic system of the buccal ganglia it is likely that at this dilution, YS is interacting via serotonergic pathways and not predominantly on Shaker potassium channels. It is very likely that this antagonistic effect is primarily due to the presence of 6BrMT, a serotonin analogue. Conclusions 6BrMT has a well documented effect on Shaker potassium channels, but the fact that a low concentration of raw Yellow Stuff suppresses serotonin induced activity in the buccal ganglia of Aplysia, provides a good indication that YS has multiple pathways through which it functions, one of which being through a serotonin pathway. Although this study primarily concentrated on the effect of YS on Aplysia, an organism which C. canaliculatum would not normally encounter in its ecological niche, the conclusion that YS functions antagonistically to 5-HT could help determine the mechanism of how YS elicits the escape response in its predators. This study also raises many more questions about the relationship of 6BrMT and YS to serotonin, not only in seastars, but in humans, where a serotonin antagonist has many pharmacological uses. 12 Acknowledgements 1 wish to thank everyone at Hopkins who has helped me during these last two months, especially the Fisher’ people (Anna, Ryan, Jane, Rachel) for keeping me company during the long days of electrophysiology, Mike for all the voltage-clamp work he did for me, the helpful people in Gilly’s lab, my housemate Tori for her continued support, Brett for all his rides home at 12am and Charles for making sure I ate dinner at lam.. Gilly - thank you for making sure I thought everything through before jumping in head first, for being a natural skeptic, for your love of paperclips, and for all the time and invaluable encouragement you supplied. Stuart - thank you for your amazing enthusiasm and energy you put into this project, and for helping me make sense of the complicated world of Aplysia. 13 References Bryan, P.J., J.B. McClintock, and M. Hamann (1997). Behavioural and Chemical Defenses of Marine Prosobranch Gastropod Calliostoma canaliculatum in Response to Sympatric Seastars. J. Chem Ecol 23: 645-658 Evgeni A. Kabotyanski, Douglas A. Baxter, Susan J. Cushman, and John H. Byrne (2000). Modulation of Fictive Feeding by Dopamine and Serotonin. J. Neurophysiol. 83: 374- 392. Gerschenfeld, H.M. and D. Paupardin-Tritsch (1974). Ionic Mechanisms and Receptor Properties Underlying the Responses of Molluscan Neurones to 5-Hydroxytryptamine. J. Physiol. 243: 427-456. Gerschenfeld, H.M. and D. Paupardin-Tritsch (1974). On The Transmitter Function of 5- Hydroxytryptamine At Excitatory and Inhibitory Monosynaptic Junctions. J. Physiol. 243: 457-481. Sack, J., W.P. Kelley, A.M. Wolters, R.A. Jockusch, J. Jurchen, E.R. Williams, J.V. Sweedler and W.F. Gilly. Slowing the Activation Kinetics of K-channels with BrMT, Novel Pharmacological Agent from a Marine Snail. Publication pending. Yee, A., J. Burkhardt and W.F. Gilly (1986). Mobilisation of a Coordinated Escape Response by Giant Axons in the Ophiuroid, Ophiopteris papillosa. J. Exp Biol 128: 287-305. Figure Legends The chemical structures of 5-HT and 6BrMT (a serotonin dimer derivative) Fig.1. Fig. 24 Behavioural response of Ophiopteris papillosa to various chemical stimuli. A total of 6 Ophiopteris were used in, each for 12 assays. Fig. 2B Behavioural response of Pycnopodia helianthoides to the same chemical stimuli. One specimen was used for the study. Fig. 3 Map of the B cells in the buccal ganglia of Aplysia californica Fig. 44 Baseline of a pacemaker cell in the buccal ganglia. Fig. 4B After application of 1:100YS to the bath. Trace is 5000ms and is representative of the whole recording. Fig. 5A Baseline of a non-pacemaker cell (no action potentials) Fig. 5B After application of 50 ul 1mM 5-HT to the bath. Regular action potentials generated. Fig. 5C Addition of 1:100 YS into the same chamber 3 min later. Action potentials no longer seen. Fig. 6A Baseline of a pacemaker cell Fig. 6B After application of 5-HT to the bath. EPSPs generated. Fig. 60 Subsequent application of 1:100 YS to the same bath. EPSPs no longer seen Fig. 6D After perfusion with seawater, 5-HT added again. EPSPs generated. Shaker sensitivity to control and 1:100 YS Fig. 7A Fig. 7B Shaker sensitivity to control and 6BrMT (Sack et al) Figures Fig 1 Serotonin NH. Ho. 5-H 6-bromo-2-mercaptotryptamine N. N -S—S- E B Fig 24 Fig. 2B Response of Ophiopteris to various compounds Elevel 0 Blevel 1 Dlevel 2 Dlevel 3 L 9 0 00 Compounds Response of Pycnopodia to various compounds Elevel Elevel Dlevel —evet II Compounds Fig. 3 B3 862 B11 B5 864/ 8b 766 88a B4 661 B7 863 T S2834 S1 B1 8314 Fe 832- S2 B2 from http:/www.biu. ac. il/LS/stafffsusswein/susswein2.html CBC 1683 BN-2 BN-1 mV mV Fig 44 ee e e e ehne e eae ethen e n en enanet Mtn, Time (5000ms) Fig. 4B ene gehenene e nen e ane ae n enen ene aeane ne aee aean aeee Tn.— Time (5000ms) 19 e mV mV Fig. 54 TEGeenens e onenann e Tn Time (5000ms) Fig. 5B . 120 ae 2 etetesetoe e et t ose e e s o P e 60000 Tme (ma) Time (5000ms) Fig. 5C 1 2 Fonchegea heh ehanhehengen eof ena enen h a ehgnedoshs e aoe er een o un oe e a n o 20 Time (5000ms) 20 Fig. 64 —t .. 1.. Time (5000ms) Fig. 6B 1 tt „1 Heetttttrtettreeetr — 4. Time (5000ms) Fig. 60 tt Time (5000ms) Fig. 6D t 11 Knettrttfrttttet Hettrt T Time (5000ms) Fig. 74 — Hughes (2001) Fig. 7B Sack et al 10 ms — 400 ms 5 UA 20 UA 22