Manuscript Title:

CONOTOXIN’S PHARMACOLOGICAL CHARACTERIZATION AND APPLICATIONS: A REVIEW

Author:

MARIAN JEREMY D. AGGABAO, JIMIWELL R. BERNABE, ARIAL JOY J. RODEROS, ELIJSHA MEARI A. GABRIEL, PRINCESS CASEY BANTIGUE, ANALETTE M. GUINTO, ALVIN N. CARIL, NOEL A. SAGUIL

DOI Number:

DOI:10.17605/OSF.IO/CYH9N

Published : 2023-06-10

About the author(s)

1. MARIAN JEREMY D. AGGABAO - Research Assistant, Research Institute for Science and Technology (RIST) and currently pursuing a master’s degree program in biology at the Polytechnic University of the Philippines, Sta. Mesa, Manila, Philippines.
2. JIMIWELL R. BERNABE - Research Assistant, Research Institute for Science and Technology (RIST) and currently pursuing a Master’s Degree program in biology at the Polytechnic University of the Philippines, Sta. Mesa, Manila, Philippines.
3. ARIAL JOY J. RODEROS - Research Assistant, Research Institute for Science and Technology (RIST) and currently pursuing a Master’s Degree program in biology at the Polytechnic University of the Philippines, Sta. Mesa, Manila, Philippines.
4. ELIJSHA MEARI A. GABRIEL - Research Assistant, Research Institute for Science and Technology (RIST) and currently pursuing a Master’s Degree program in biology at the Polytechnic University of the Philippines, Sta. Mesa, Manila, Philippines.
5. PRINCESS CASEY BANTIGUE - Research Assistant under the Research Institute for Science and Technology (RIST) and currently pursuing a Master’s Degree program in biology at the Polytechnic University of the Philippines, Sta. Mesa, Manila, Philippines.
6. ANALETTE M. GUINTO - Researcher, Research Institute for Science and Technology (RIST) of the Polytechnic University of the Philippines, Sta. Mesa, Manila, Philippines.
7. ALVIN N. CARIL - Researcher, Research Institute for Science and Technology (RIST) of the Polytechnic University of the Philippines, Sta. Mesa, Manila, Philippines.
8. NOEL A. SAGUIL - Chief of the Center for Engineering and Technology Research (CETR), under the Research Institute for Science and Technology (RIST) of the Polytechnic University of the Philippines, Sta. Mesa, Manila, Philippines.

Full Text : PDF

Abstract

Conotoxins from marine cone snails are small, disulfide-rich peptides that act with specificity on various receptors and channels, making these powerful probes to study the properties of voltage and ligandgated ion channels. Conotoxin drug candidates have shown remarkable therapeutic promise in managing pain, addiction, and neurodegenerative disorders. A systematic review following th e PRISMA guidelines was conducted to assess the pharmacological effects of conotoxins on various channels and receptors and the conotoxins’ effects in broader in vivo and in vitro biological assays. PubMed and Google Scholar articles assessing the ability of conotoxins to inhibit receptors and channels and the conotoxins-induced biological response were eligible for inclusion. Twenty-seven studies met the inclusion criteria. Studies of alpha conotoxin reported the peptide as an excellent tool for distinguishing neuronal and muscle nAChRs and have a high potency of blocking nAChRs even at nanomolar concentrations. While μ-conotoxin isolated from piscivorous Conus potently blocks sodium channels, with μ-GIIIA and μ-GIIIB abolishing the twitch response of the muscle. δ-GmVIA slows down the sodium-current inactivation, while δ-TxVIA does not. ω-TxVII significantly and reversibly blocked the L-type Ca2+ current. However, all the evidence reported in this review was obtained from studies with a serious risk of bias due to a lack of blind outcome assessment, thereby limiting the strength of the pieces of evidence. Blinded RCTs may improve confidence in concluding the biological effects of various conotoxins.


Keywords

Calcium channel, Conotoxin, Conus, nicotinic acetylcholine receptor, PRISMA, pharmacology, sodium channel.