Conotoxins: a Case for their Cause of the Rapid Evolutionary Radiation of Conus


Andy Malishenko

Colorado State University
Fort Collins, Colorado 80523

4/22/94

INTRODUCTION 
	Cone snails are one of the most diverse and dominant predators in 
the coral reef.  Their recent appearance and rapid speciation is enough 
to catch any body's eye interested  in stories of adaptive radiation.  
In this paper I will propose and support that the rapid evolution of 
cone snails is due to their unique venom.

CONE SNAIL BIOLOGY
	Cone snails of the genus Conus inhabit tropical waters at varying 
shallow depths.  They get their name from the distinctive conical shape 
of their shell.  The designs on the shells are beautifully intricate and 
some shells are worth a small forture (See Figure 1).  The greatest 
diversity of cone snails can be found in subtidal choral reefs of 
Thailand and Indonesia but their geographic range extends throughout the 
Indio-Pacific region (Kohn 1975, Olivera 1990).  They are nocturnal 
predators of a remarkably broad phylogenetic range of prey including 
polychaete worms, hemichordata, cephalopods, other gastropods, bivalves, 
fish, and Crustacea (Nybakken 1990 Miller 1989).  They have a very 
specialized feeding mechanism involving the use of a hollow tooth at the 
end of the proboscis used to stab and envenomate prey (See Figure 2 and 
3) (Kantor 1990).  The toxins in the venom act very rapidly.  The fish 
hunting snail, Conus prupurascens can paralyze its prey in about two 
seconds (See Figure 1) (Olivera 1991).  This quick action is especially 
important if you are a snail trying to catch a fish!  The mollusc hunter 
Conus textile's venom induces peristaltic convulsions in its prey.  
Again useful as many molluscs tend to retreat into their shell upon 
attack.  The convulsions apparently prevent this from occurring 
(Woodward 1990).  Let's take a close look at the evolution of the cone 
snails.

PHYLOGENY AND EVOLUTION
	Cone Snails are molluscs of Class Gastropoda, Order Neogastropoda, 
and Superfamily Toxoglossa.  Toxoglossa contains the families 
Terebridae, Turridae, and Conidae.  The specialized mode of feeding 
described above is exclusive to the Toxoglossa.  Most, but  not all, of 
its members feed in this way (Kantor 1990).  The only living members of 
the Family Conidae are Conus species.  Distinctions between Turridae and 
Conidae are very vague and some taxonomists include both in Conidae.  
Taxonomic classification of the Toxoglossa varies depending on who is 
writing the paper but the above is not iconoclastic (Kohn 1990).
	The first Cone Snails appeared after the Cretaceous-Tertiary 
boundary approximately 55 million years before the end of the 
Pleistocene epoch (Kohn 1990).  Current counts of species in the genus 
Conus are around 500, making it perhaps the largest single molluscan 
genus (Olivera 1991).  Figure 4 shows a kite diagram of Conus species.  
You can see an expansion of the genus through the upper Miocene where 
species number drops as we enter the Pliocene.  This reduction in 
species number of most gastropods and other invertebrates is 
characteristic of this epoch (Raup 1976).  Then very rapid speciation 
occurs in the Pleistocene leading to the recent count of 500 (Kohn 
1990).  Geographic radiations occurred as well, expanding their 
geographic range from Coastal European origins to the Indio-Pacific 
region (Kohn 1990).
	The striking feature of Conus evolution is the large number of 
species contained in the single genus that only appeared since the 
extinction of the dinosaurs.  Attempts to explain this rapid 
evolutionary radiation fall generally along two lines.  Did Conus find a 
new adaptive zone to invade or did some "key innovation" (usually 
morphological) occur that helped them succeed (Kohn 1990)?  As with most 
adaptive radiation stories, the answer is unclear.  The answer to 
weather Conus entered a new adaptive zone is difficult to say.  The main 
evidence for this would come from the fossil record which has so far not 
proved to be very elucitory.  I feel that the key innovation hypothesis 
warrants a closer look as these are no ordinary venomous snails.  Their 
venom is very unusual.

CONUS VENOM
	The venoms of the cone snails contain short peptides called 
Conotoxins.  Each species' venom contains a mixture of these toxic 
peptides along with other molecules.  Figure 5 shows an HPLC analysis of 
a peptide fraction from Conus Magnus venom.  One can see the multiple 
peaks and the biological activity induced in mice by each of theses 
fractions  (Olivera 1991).  In their active form, these peptides consist 
of only 10 to 30 amino acids.  They have a highly conserved cysteine 
"backbone" which provides for multiple cross-linked disulfide bonds as 
the peptide folds.   Many animals have toxic peptides with disulfide 
cross-linking but none are as short as the Conotoxins (Olivera 1991) .  
Conotoxins are originally translated into propeptides of intermediate 
length.  The cysteine residues, however,  are concentrated near the 
COOH-terminus.  Once the protein has folded, the N-terminus is cleaved 
and only the short, cysteine rich end of the peptide remains.  Figure 6 
illustrates the difference between conotoxins and other cysteine-rich 
peptide toxins  (Olivera 1990).  The cleaved N-terminus of conotoxins is 
believed to be involved in assisting the folding of the peptide (Olivera 
1990 Woodward 1990).
	Over 75 peptides from 10 venoms have been biochemically 
characterized with others being sequenced monthly.  Currently there are 
known to be three basic cysteine structural frameworks into which most 
of the conotoxins can be categorized.  (There are some Conus toxins 
without disulfide bonding but they are not as well characterized) 
(Olivera 1991).  These categories are distinguished by the position of 
the cysteine residues and the number of loops formed in the folded 
peptide as seen in Figure 7.
	The inter-cysteine residues of different conotoxins belonging to 
the same category are quite variable.  In fact, some believe they are 
hypervariable, denoting that there may be a special genetic mechanism 
used by the cone snails to create increased variability of these inter-
cysteine residues (Woodward 1990).  Further study needs to be done to 
elucidate the mechanism for this observed hypervariability.
	Within the major structural categories there are proposed 
subgroups based on the general makeup of the variable amino acids.  
Figure 8 show how the "four-loop" structural category can be broken down 
into more specific groups based on the charge of these variable inter-
cysteine residues.  This is the most well studied category of 
conotoxins.
	One more note about the sequence of these peptides involves the 
cleaved N-terminus region.  As I mentioned before, this is thought to be 
involved in controlling the folding of the peptide.  One would expect, 
therefore, that the sequence of this region would be highly conserved 
within a group of conotoxins.  As Figure 9 shows, three peptides of the 
King-Kong group exhibit this sequence conservation.

CONOTOXIN TARGETS
	These toxins exhibit their poisonous effect by blocking specific 
ion channels of nerve cells.  Figure 10 shows the specific channels that 
the three cysteine rich categories of conotoxins affect.
	This channel specificity is quite remarkable.  Many drugs used for 
medical purposes bind their desired target but also bind related targets 
which often produce unwanted side affects.  In contrast to most drugs 
conotoxins can discriminate among closely related receptor subtypes 
(Olivera 1990).  For example drugs such as dihydropyridine that is used 
to block calcium channels will bind such channels in smooth, skeletal, 
and cardiac muscle and well as neuronal tissue.  Omega-conotoxins bind 
only to the neuronal calcium channels.  One can easily see how this is a 
benefit to the cone snail.  If its main goal is paralysis, it doesn't 
want to waste its toxin by having it bind to channels irrelevant to the 
paralysis of its prey.  The other categories of conotoxins show this 
degree of specificity as well.  Mu-conotoxins discriminate between 
muscle and neuronal sodium channels.  Alpha-conotoxins block 
acetylcholine receptors only at the neuro-muscular junction and not 
inter-axonal (Olivera 1990).

WHAT A GREAT DESIGN
	To sum up all of this toxin business, we have a genus who's 
species produce toxins of unsurpassed specificity for behavioraly 
relevant targets in the nervous system of their prey.  These species 
have a constrained mechanism of producing toxins which enables them to 
create many variations on a theme.  Within a structural category, the 
rigid cysteine backbone and conserved folding apparatus combined with a 
hypervariability of inter-cysteine residues results in the ability of 
cone snails to produce a plethora of related peptides.  This way, new 
toxins can be produced that may have new specificities without risking 
complete loss of biological activity.  This strategy would be 
particularly useful if the targets of the toxins were related as well 
(Woodward 1990).  Well that is exactly the case with ion channels.  The 
evolutionary relatedness of ion channels is shown in Figure 11 from 
Hille 1992.
	The specificity of conotoxins is even more specific than this 
diagram reveals but it still illustrates the relatedness of the ion 
channels.  In summation, cone snails have developed a scheme for 
designing a variety of toxins that are very likely to be effective to 
their ends of prey capture.  They have not only produce effective, quick 
acting toxins, they also have a mechanism ideal for designing new 
peptides targeted to the nervous system of their prey.

WHERE'S THE BEEF
	The literature shows that cone snails have undergone rapid 
speciation and have expanded their geographic range in a relatively 
short (geologically speaking) period of time.  I proposed that this was 
due to a key innovation, namely the conotoxin venoms.  I have shown why 
I think the conotoxins are very ingenious and bound to (in my opinion) 
bring about success but I haven't given any proof to support my claim 
that the venoms are responsible for the success of Conus.  That is what 
this next section is about.

TEST OF VENOMS AS KEY INNOVATION
	In order for an innovation to be responsible for rapid 
evolutionary radiation, it must meet several criteria. (Adapted from 
Herera 1989 in Kohn 1990)
1.  Taxa with the feature diversify early in their evolutionary history.
2.  The novel feature is significant to the taxon and absent from its 
sister or ancestral taxon.
3.  Taxa with the feature become structurally and taxonomically more 
diverse than sister taxa lacking it.
	The diversification of the Conus genus has occurred over the past 
55 million years.  To date, every Conus species' venom that has been 
characterized has contained peptide venoms.  This tends to support the 
hypothesis that the peptide venoms have been around since the species 
origins.  If this were not the case, we might expect to see other genera 
in the family without peptide venoms.  Therefore we can conclude that 
the peptide venoms are possible candidates for a key innovation 
responsible for their rapid evolutionary radiation.
	Since the venom is important for prey capture by cone snails, it 
is obviously significant.  As for the rest of criterion number two, we 
must first decide what are the sister and ancestral taxa of Conus.  The 
most closely related genus to Conus would be contained in the family 
Turridae (Miller 1989).  It is not known weather this family is sister, 
ancestral, or neither (Kohn1990).  Reguardless, most believe there is 
some relationship between the two families so a comparrison is 
appropriate.  Unfortunately, the nature of the venoms of the genera in 
Turridae is not known (Kantor 1989).   Further study of the Turrids 
would help to answer this question.
	In satisfying the third criteria, the genus Conus has more species 
that any Turrid genus (or almost any molluscan genera for that 
matter)(Kay 1990).  Also the food types of Conus include polychaete 
worms, hemichordata, cephalopods, other gastropods, bivalves, fish, and 
crustacea whereas the entire family of Turridae is limited to polychaete 
worms, sipunculida, nemertea, and other molluscs (Miller 1989).  This 
shows higher diversity among the cone snails.   Also, the cone snails 
have morphologically different hollow teeth which correspond to 
differing prey types (See Figure 12) (Nybakken 1990).  This has not been 
shown in any Turrid genera.
	So that is the beef. If you were hoping for a quarter pounder I 
bet you were disappointed.  The truth of the matter is that there is not 
much known about the Turridae to provide a good comparison with Conus.  
Hopefully in the not so distant future we will have answers to some of 
the important questions (such as the nature of Turrid venoms and their 
feeding physiology) that will shed some light on this ambiguous yet 
still interesting story.

DEVILS ADVOCATE
	Even if you grant that the above criteria are met for conotoxins 
being a key inovation in Conus, this does not mean that they are 
responsible for their rapid evolutionary radiation.  It may be some 
other morphological feature or something completely different. Again, 
more study is needed to support the main thrust of this paper.

CONCLUSION
	Conotoxins are some of the most efficiently designed poisons known 
to man.  They are proving to be a valuable tool in medical research.  
Due to this fact, much funding is available for research on conotoxins 
and the literature is expanding as you are reading this.  Because 
scientist like science and not only the money they get to study, I 
believe we will learn much more about these toxins than just their 
pharmacological value.  There is a very interesting adaptive radiation 
story hidden in the sequences of the DNA of these small (but definitely 
not innocuous) cone snails which is just waiting to be unraveled by some 
curious scientist. 

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