Abstract Two competing models have been proposed to explain the mechanism by which a sperm activates an egg at fertilization. One postulates a receptor while the other relies on fusion as the primary means of signal transduction. This study looked for a soluble activation factor which could act as a diffusible messenger between the fused sperm and egg. S purpuratus sperm were lysed with 1% Triton to bring all solubilizable proteins and factors into solution. In a second set of experiments, sperm were permeabilized with hypotonic solution and then suspended in an extraction buffer of high salt and pH 8, designed to bring only soluble cytoplasmic elements into solution. Both sets of extracts were microinjected into eggs and activation was monitored by looking for the rise of the fertilization membrane. Under the various conditions used in this study, no soluble fraction from sperm activated the eggs when microinjected. Introduction We tend to think of fertilization as the beginning of the development of a new organism, despite the fact that reproduction is a cyclical process, as that old adage about the chicken and the egg illustrates so aptly. But fertilization does give the impression of a beginning, even on the molecular level. This is especially true when we look at sea urchins. Eggs from these animals remain in a relatively quiescent metabolic state until fertilization. Fusion of the two gametes and the transfer of paternal genetic material is accompanied by the reinitiation of the cell cycle and an increase in egg metabolism, DNA and protein synthesis. As a problem of signal transduction, this activation of the egg is compelling, since so many aspects of the cell are affected. Two very early events which are thought to be central to reinitiating protein synthesis and metabolism are the wave of intracellular calcium release which crosses the egg and the increase in cytoplasmic pH. Calcium especially has been manipulated in experiments with fertilization or parthenogenic activation (Whitaker and Steinhart, 1985; Swann and Whitaker, 1986; Turner et al, 1986; Steinhart and Epel, 1974; Steinhart et al, 1977; Brandriff et al, 1975). These seem to demonstrate its importance as a fundamental component of egg activation. But the calcium rise itself is not the initiating signal; inositol trisphosphate (IP3) seems to be the messenger responsible for releasing calcium from internal stores (Swann and Whitaker, 1986, Swann et al, 1987; Busa et al, 1985). There is one report claiming that IP3 itself could be released from the sperm after fusion and so activate the egg directly (Iwasa et al, unpublished). Others have observed a turnover of egg plasma membrane inositol lipids during early fertilization (Ciapa and Whitaker, 1986) and propose that IP3 is a second messenger. If this is true the question becomes how the sperm initiates IPa generation. In any case, the question which is still to be answered asks about the nature of the initiating signal of activation. Two models are generally presented to account for the mechanism of egg activation. The first postulates a receptor-mediated signal between the sperm and the egg. The second proposes a diffusible activating factor which enters the egg after fusion establishes cytoplasmic continuity. In its most common version, this model draws an analogy with the IP second messenger system in other cells (Berridge and Irvine, 1984). The proposed receptor would activate a G-protein which in turn activates phospholipase C to cleave membrane phosphatidyl inositols into IP3 and diacylglycerol (figure 1). Experiments in sea urchins (Swann and Whitaker, 1986; Turner et al, 1986) and Xenopus (Busa et al, 1985) have demonstrated that microinjected IPa will cause calcium release and the calcium-dependent cortical granule exocytosis. In addition, the cytoplasmic concentration of IPa increases during fertilization (Ciapa and Whitaker, 1986), suggesting that IPa is a relevant messenger in vivo. The existence of a receptor and G-protein are much more dubious. Kline et al (1985) found that Xenopus oocytes expressing muscarinic acetylcholine or serotonin receptors could be artificially activated by neurotransmitter. Since the receptors couple to G-proteins, their ability to trigger activation indicates the existence of endogenous G-proteins with the ability to cause calcium release. However, the physiological relevance of the experiment is unclear. Experiments which tried to manipulate the G-protein with toxins or GTP analogs have given ambiguous results. Microinjection of GTP-B-S, a G-protein inhibitor, will inhibit cortical granule exocytosis as a result of fertilization by sperm (Turner et al, 1986). The same injections will also inhibit cortical granule exocytosis by microinjected IP3. As the inhibitor of the G-protein must be acting after the release of calcium, the G-protein itself cannot therefore be responsible for the calcium wave (Whitaker and Crossley, in press; Turner et al, communication). The receptor model is certainly attractive for its elegance: a receptor mediated event sets off a self-propagating wave of 1P3 generation and calcium release while DAG activates protein kinase C, raising pH and perhaps even causing membrane fusion. However, the failure to demonstrate a critical role for G-proteins early in activation in vivo seriously undermines the strength of this model. In the alternative model, fusion of sperm and egg allows the diffusion of an activating factor into the egg cytoplasm. This factor could act in a number of ways, either acting locally to set off the IPa cascade or to release some egg factor, or by diffusing itself to release calcium from the egg’s internal stores (figure 2). An increase in membrane capacitance can be measure almost simultaneously with the sperm-gated hyperpolarization, that is to say from the initiation of sperm-egg contact (McCulloh and Chambers, 1986). This implies that fusion of the plasma membranes is the first event of fertilization. However, dye transfer and EM experiments first detect fusion 4 to 8 seconds after the initial contact (Hinkley et al, 1986; Longo et al, 1986) implying that cytoplasmic continuity is not necessarily the first event. Whitaker et al (1989) try to resolve the discrepancy which a complex model involving transient fusion which becomes permanent later by the action of calcium, released locally by the diffusible activating factor from the sperm. Despite the intricacies of their model, it does not constitute evidence for the existence of the putative activating factor. If an activating factor exists, its activity could be found in and presumably purified from solubilized sperm cytoplasm. Isolating an activity would be the best possible demonstration of the model. Several small molecules, including calcium, cGMP and IPz are known to activate eggs when microinjected, but there are reasons to believe none of these are the relevant diffusible messenger. The biggest problem with using any of these in a model is the high concentration at which they would need to be present to play the role of diffusible activator. For example, Whitaker predicts that cGMP would have to be present in sperm at approximately 1M to be effective (Whitaker and Crossley, in press). There have been two reports of activity isolated in sperm extracts: one in hamster (Swann, 1990) and the other in sea urchin (Dale et al, 1985). Swann has reported the isolation of a sperm protein which will cause microinjected eggs to reproduce the occilations of calcium characteristic of activated hamster eggs. The experiments described here explored various protocols for solubilizing sperm in an attempt to describe a sperm-derived activating factor. Based on the results discussed above, this search focussed on a protein which could act as a diffusible messenger from the sperm cytoplasm to the egg cytoplasm. Materials and Methods Gametes: Eggs were collected by shaking and then inverting S purpuratus females over sea water. The eggs were stored in a 16° C water bath with gentle stirring and were used in experiments within four hours of collection. Sperm were collected dry from males microinjected with a small amount of 5M KCl into the body cavity. Sperm were stored at 4° C and were generally used within 24 hours of collection. Extractions: Sea urchin sperm cannot be homogenized easily to release cytoplasmic proteins. Instead, two methods of extraction were used to bring soluble molecules into solution. The "brute force" method employed a 1% Triton lysis buffer while the "finesse" method permeabilized sperm in hypotonic but inert conditions and then extracted presumably only cytoplasmic proteins in a high salt, high pH buffer. I will briefly outline the strategy of each method here and, as the primary results of the experiments were modifications in procedure, the next section will trace through the procedural variations tried along with the effects of each experiment. To begin all Triton extraction experiments, 4 to 8 ml sperm were suspended in glycine rinse (see table 1 for composition of all buffers) and then centrifuged. The rinse was repeated three times to remove sea water, semen proteins and salts which might contaminate the extraction buffer. Lysis buffer was then added to the sperm and the suspension was mixed slowly for 2 hrs at 4 C. Following lysis, the sperm suspensions were centrifuged at 100,000g for 1 hr at 4° C to remove DNA and undissolved components. The supernatant was collected and became the crude extract for microinjection. Later experiments tried to purify and concentrate the extract for reasons which will be discussed below. The first approach to concentrating the extract was to separate out the small molecules on a Sephadex G-25 desalting column eluted with ammonium bicarbonate, and then to evaporate the elutant to leave a protein pellet to be redissolved in a few hundred microliters of microinjection buffer. Twenty drop fractions were collected and a spot assay (5ul from each tube spotted on Whatman filter paper and developed five minutes in Comassie blue) performed to idetify tubes with proteins. Those with protein were pooled, dried and redissolved in a few hundred microliters of fluorescent microinjection buffer. The second method concentrated extracts by adding ammonium sulfate to 90% saturation to precipitated proteins. The precipitate was collected, redissolved in microinjection buffer and then dialysed overnight to remove the excess ammonium sulfate. To permeabilize sperm without detergent, 1 ml dry sperm was diluted into 12 ml of 25% sea water (75% distilled water) and then 8 or 10 mi 1 mM MgCl, 10 mM phosphate, pH 6.5, was added to completely swell at least 90% of the sperm. Suspensions were centrifuged at 3000g for 5 minutes in a Sorvall centrifuge and the supernatant removed. The sperm were re-suspended in a high salt, pH 8 buffer (table 1, trial 2) to solubilize proteins. Sperm were mixed slowly at 4 C for 30 minutes and then spun at 3000g in an Eppendorf variable centrifuge. Supernatant was collected and carboxyfluoresceine added to aid visualization during microinjection. Microinjections: Jelly coats were first removed from the eggs by passing them through a 90 micrometer Nitex mesh filter three times. De¬ jellied eggs were stuck to plastic Petri dishes coated with protamine sulfate (3 or 5 mg/ml in distilled water). Dishes were then placed on a water- cooled microscope stage (16° C). The sample to be microinjected was loaded into a pipet pulled from 1 mm capillary tubes at 15 amps on à Nargishe micropipet puller (Scientific Instruments Inc). Pipets were mounted on a micromanipulator and pressure was delivered using a hand¬ built air valve at 35 psi for approximately 100ms. This generally resulted in a delivered volume equal to about 1% of the egg's volume. Eggs were viewed on a Zeiss epifluorescence microscope and successful microinjections were monitored using the fluorescein filter set. The assay for activation in the experiments presented here was the rise of the fertilization membrane within about a minute of injection. Only eggs in which the pipet entry did not itself cause visible damage were counted in these experiments. Every experiment included the control injection of the relevant buffer without sperm proteins. As a positive control for fertilizability of the eggs, including those which had been microinjected, each plate of eggs was fertilized by viable sperm after microinjections were completed with that batch. In general, no batch of eggs remained under the microscope for longer than 45 minutes. Results None of the extraction procedures described above resulted in a solution which activated microinjected eggs. In this section I want to explain the changes made in the protocol as the study went along and at the same time look at the actual numbers of injections versus activations, which are summarized in table 2. Triton Extacts The composition of the original 1% Triton buffer contained glycerol and inhibitors of proteases and phophatases to protect proteins from degradation due to enzymes released during lysis and to increase stability of proteins. Seven microinjections of extract resulted in 10 one partial activation, while five injections of the buffer alone, raised no membranes. The presence of a partial activation indicated that a higher concentration might be necessary to find the activity, since low concentration injections of IPa and cGMP result in partial membranes also (Ciapa, personal communication). The first concentration was performed in the speed-vac. Glycerol was left out of the lysis buffer (Triton 2 in table 1). The extract was desalted on a Sephadex G-25 column eluted with 10 mM ammonium bicarbonate, which was expected to evaporate during drying. The dried proteins were redissolved in the microinjection buffer. As table 2 illustrates, the lysis buffer resulted in low background partial activation, while injections of dried G-25 fractions without proteins resulted in six non-activated eggs. The extract injections had encouraging results: in one set of 8 injections, three were partially and one was fully activated. In a second set of injections, six of nine eggs had strangely flattened sides where they had been round originally. This happened again later with one of the hypotonic extractions and its interpretation is uncertain. The shape of the eggs resembled that of partially activated eggs but they lacked the membrane. In order to see whether the extract could be concentrated by an additional ten-fold, as Ciapa's experiments with IPz indicated might be necessary, the procedure was repeated with greater volumes of sperm. 11 For these next two experiments extracts were lyophilized instead of evaporated in the Speed Vac to prevent denaturation by heating. Unfortunately, after this treatment, the proteins did not redissolve easily, making microinjection impossible due to the particulate nature of the sample. The final approach to concentrating Triton extracts used ammonium sulfate salt added to 90% to precipitate and thus separate proteins from the lysis buffer. The precipitate was then resuspended in a small volume of the microinjection buffer and dialyzed to remove excess salt. In nine microinjections, one activated, which seemed due to the injection itself, not the buffer. Hypotonic Extraction The second extraction strategy did not result in a very concentrated solution. Presumably, however, it was enriched in the activating factor. These experiments were based on Tilney's (1979) description of hypotonic solutions which swell the sperm without lysing them, and his observation that actin in the acrosomal vesicle is inert if swollen sperm are left at pH 6.5, but goes into solution at pH 8. The first two experiments used 10 mM EGTA in the extraction buffer (Trial 2, compl in table 1) which was added after removing the hypotonic solution. While many eggs were injected without activation, the general rate of fertilization when sperm were added was poor among the injected eggs. The poor fertilization could be attributed to too high a concentration of 12 EGTA, which buffers calcium release during the fertilization events, and so prevents the calcium-dependent cortical granule exocytosis. No concentration of EGTA could serve its original function of effectively buffering the extra calcium from hypotonic solution and sperm which remained in the pellet and at the same time not be too high for microinjection itself (in which case it would buffer the activation calcium wave). Therefore the procedure was modified to remove excess calcium by rinsing the sperm three times in the hypotonic solution (each resuspension followed by centrifugation in the Sorvall) before adding the extraction buffer, now at 0.1 mM EGTA (trial 2, comp 2 in table 1). Even under these conditions microinjection did not seem to activate the eggs, although the high background activity in controls made it difficult to know if a low level of activation activity was present. Twenty one injections of extract included six partial membranes, but even the microinjection buffer itself gave 30% activations with this batch of eggs. Discussion There are at least three possible reasons why the procedures described above have failed to demonstrate the existence of a sperm¬ derived, diffusible activating factor. Most obvious is that the activity may not exist. However, the methods have potential weaknesses which may be responsible for the negative results. First, it is possible that the 13 procedures used failed to bring the relevant factor into solution. Second, the relevant factor may be in the extracts, only in concentrations too low for the microinjected solution to imitate the effects of the sperm during fertilization. Finally, the purification and concentration which was attempted may have resulted in denaturation and loss of activity. It is possible that the factor was not pulled into solution. If, for example the factor is transferred between the two gametes plasma membranes and so is lipophilic, not hydrophilic. These experiments searched for proteins rather than lipids because Swann’s results in hamster indicate that an activating protein can be isolated from the sperm in that system. At the same time, it is important to remember that species vary, so sea urchins may not use a protein. There is ground to criticize the hypotonic permeabilization as likely not to have brought the factor into solution. Although at least some number of proteins were extracted, there was also loss of proteins in the rinses which preceded the extraction buffer. It is interesting to note that the two reports of isolated sperm factors in the literature use very simple techniques. Swann (1990) extracts directly into hypotonic solution and Dale et al (1985) isolate their product in distilled water. I did not repeat the Dale et al procedure partly because proteins tend not to be stable in distilled water but largely because it seems likely that there is enough calcium in the final injection medium to cause the activation they 14 observed. Even if the extraction procedure is successful, activation may not be observed if the factor is not present in high enough concentrations. Sperm are very small cells with little cytoplasm and would therefore be expected to contain only a small amount of factor. However, sperm have an advantage over microinjection in acting very locally. Fusion followed by diffusion would result in a very high effective concentration immediately adjacent to the plasma membrane. In contrast, the pipet tip goes farther into the cell than adjacent to the membrane, and the injection pressure sends the microinjected solution in towards the center of the cell. It follows that a higher concentration of material would therefore have to be microinjected in order to achieve the same effective concentration at the membrane as a single fusing sperm achieves. Assuming that the entire sperm head contains the activating factor and that our procedure resulted in 100% recovery, we calculated that the microinjection in the first Triton extraction could be equivalent to 10 to 30 sperm. Since neither assumption is true, and even this estimate is fairly low, lack of concentration is certainly a valid consideration. A second reason for assuming that concentration could be an important variable is the partial activations which were occasionally observed. The meaning of a partial activation is hard to assess. If there is nothing wrong with the egg, so that it is capable of raising a membrane 15 through cortical granule exocytosis, then elevation of a section of the membrane would seem an abnormal event. The abnormality of the event is increased if the model which proposes a self-propagating cascade is correct (figure 1). One could explain partial activation consistently if a diffusible factor is needed above a certain concentration in order to cause calcium release from the entire egg. In this case, a partial activation could mean that the activating factor is simply not present in a high enough concentration to release calcium beyond a given distance from point of fusion or microinjection. Microinjection of both IPa and cGMP will result in primarily partial membrane elevation if the concentration is ten-fold less than that giving all complete activation (Ciapa, personal communication). Thus if we believe in a a diffusible activator, finding partial activation urges that the extract be concentrated in the hopes of increasing the amount of factor above the threshold. A second explanation for partial activation is the existance of not one but two or even several factors which act in different ways to trigger activation. For example, there may be a locally acting factor which causes the partial activation while a second factor is needed to begin the self- propagating wave. In this case, our extract may contain only one of the necessary components of full activation. Again concentrating the solution might result in our finding full activity, especially as multiple factors could exist in smaller amounts and achieve a result through amplification. 16 Desalting followed by lyophilization and ammonium sulfate precipitation were used to concentrate the extract. Using lyophilization resulted in concentrations of 19 and 23 mg/ml protein in the injection buffer, a significant increase. However, this may not have been enough. The hypotonic permeabilization resulted in a much more dilute extract at 77 mg/ml, but it probably did not contain nuclear proteins, such as histones, or membrane proteins, making it perhaps more concentrated in the relevant cytoplasmic factors. In order to concentrate these extracts further, the procedure would have to be modified to avoid concentrating KCl and the difficulties in lypohilization solved first. Lyophilizing, while it avoided heat, presented additional technical problems since the activity could be lost by denaturation with the loss of salt. The desalting column was eluted with ammonium bicarbonate so that the proteins could be dried and concentrated without also increasing salt and buffer concentrations. Unfortunately, the dried proteins did not fully redissolve in the buffer, indicating that in fact there could have been significant denaturation. The ammonium sulfate was used as an alternative method of concentrating without drying; yet that extraction also failed to activate microinjected eggs. Despite the lack of activation in the one ammonium sulfate experiment, work could be done to improve the procedure. The extract was made with a small volume of sperm and perhaps a greater volume, 17 followed by fractionation as opposed to mass precipitation, could give a cleaner extract with more likelihood of activating eggs if the factor exists. A second potential improvement could be the use of detergents other than Triton. Not all detergents are alike in what they will solubilize and perhaps octylglucoside or another detergent would successfully solubilize the activity where Triton had failed. Such a detergent would have the additional advantage of being removable through dialysis, a much gentler way of removing small molecules than the desalting column. Given the possibility that the model might be wrong, in future experiments, it would be worthwhile to try applying extracts to the outside of eggs from which the vitelline layer had been removed. FIGURE LEGEND Figure 1: Model for activation of the egg through a G-protein-linked receptor. Binding of sperm to the putative receptor activates a G¬ protein which diffuses through the membrane to activate phospholipase C. This enzyme cleaves polyphosphatidyl inositol in the membrane to generate IPa and DAG. IP releases calcium from internal stores while DAG activates protein kinase C. Calcium feeds back to increase PLC activity and, together with the rise in pH, increases protein synthesis and causes the other events of activation. Figure 2: Three models for the action of a diffusible factor in activating the egg. Such a factor could trigger a self-propagating cascade, such as the cascade proposed to accompany receptor mediated activation (figure 1). Alternatively the factor itself could diffuse through out the egg and cause calcium release directly. Finally, the factor might act locally to release a greater amount of a diffusible factor from the egg. For example, the sperm factor might cause an amplified local production of IPz which would then diffuse through the cytoplasm and activate the egg. Table 1: Composition of all buffers used in the experiments described. Trial 1 refers to the experiments with Triton as the primary means of solubilizing. Trial 2 buffers are those into which sperm were placed for extraction after having been swollen with 1 mM MgCl, 10 mM phosphate buffer, pH 6.5. Table 2: Results from all experiments. The experiment labelled Triton 1 was performed using the first Triton buffer (see table 1) and without spinning the sperm suspension at 100,000 g. The second triton experiment (Triton 2) also used the first Triton buffer, this time with the centrifugation step. The control in both of these experiments is the lysis buffer diluted into the microinjection buffer at the same ratio used with the sample. Triton 3 used the second triton buffer (see table 1) and centrifugation, followed by desalting on the Sephadex G-25 column and then drying using the Speed Vac. Controls here include lysis buffer and the blanks of column fractions without proteins also dried and then redisolved in microinjection buffer. The fourth Triton experiment also used Triton buffer 2. This time concentration was accomplished using ammonium sulfate precipitation at 90% saturation with the salt. The first three experiments with hypotonic treatment, followed by extraction buffer all used the first composition of extraction buffer as listed in table 1. Controls here are the extraction buffer itself, made visible by adding carboxyfluorescein directly. For all three of these experiments the fertilization rate when sperm were added was very low among injected eggs. Thus for the last experiment, a second extraction buffer composition was used with lower EGTA, while excess calcium was removed by washing. 20 Receptor Model of Activation: plasma membrane C receptor Figure 1 G-protein phospholpase C P3 Calcium —polyphosphatidyl inositol PAG protein kinase C pH increase cortical granule exocytosis protein and DNA synthesis Ihree models for activation by a diffusable factor: direct diffusion self-propagating cascade Figure 2 egg factor diffusion Table 1 Trial 1 PIPES MgCl, Glycerol Triton inhibitorsa Butfer KC EGTA — Triton 150 50 10% 1% yes Triton 2 150 10 50 1% yes — — Microinjection 480 20 O.1 Trial 2 EGTA TAPS Mgoia Butfer KC 480 Comp1 10 480 Comp1 O.1 a: 2 mM vanadate, 10 mM sodium pyrophosphate, 10 mg/mi aprotinin, 10 mg/mi leupeptin, 1.4 mM bacitracine, 10 mM NaF, 1 mM DTT, 1 mM PMSE Iable 2 Experiment Triton 1 control Triton 2 control Triton 3 control (lysis buffer) control (blanks Triton 4 control Hypo/Ext 1 Hypo/Ext 2 control Hypo/Ext 3 control Hypo/Ext 4 control total injections 15 17 34 6 9 16 31 16 6 21 activations full partial 0 3 flattened 0 1 0 5 bubbles 7 flattened 2 flattened 1 2 flattened 3 flattened Literature cited Berridge, MJ, and Irvine, RF (1984) Inositol trisphosphate, a novel second messenger in cellular signal transduction. 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(1989) How does a sperm activate a sea urchin egg? in press Whitaker M, and Steinhardt RA (1985) lonic signaling in the sea urchin egg at fertilization. In: Metz, CB and Monroy, A (eds) Biology of fertilization. Academic Press Inc, New York pp168-223 22 Whitaker, M., Swann, K., Crossley, I. (1989) What happens during the latent period at fertilization. In: Nuccitelli, R., Cherr, G. N., Clark W. H. jr (eds) Mechanisms of egg activation. Plenum, New York pp 157-171