Charaterization of bumarsin, a 3-hydroxy-3-methylglutaryl-coenzyme reductase inhibitor from Mesobuthus martensii Karsch venom

CHAI, S.C., ARMUGAM, A., STRONG, P.N. and JEYASEELAN, K. (2012). Charaterization of bumarsin, a 3-hydroxy-3-methylglutaryl-coenzyme reductase inhibitor from Mesobuthus martensii Karsch venom. Toxicon, 60 (3), 272-279.

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Abstract

Scorpion venoms are rich sources of bioactive peptides and are widely known for their ion channel inhibiting properties. We have isolated, cloned and characterized a venom protein (Bumarsin) from the Chinese scorpion, Mesobuthus martensii Karsch. Bumarsin cDNA encodes a 8132 Da, 72 amino acid mature protein that most probably exists in its native form as a Cys-bridged homodimer. We have identified this novel protein to be an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity. 0.6 μM of Bumarsin inhibits 32% of the HMG-CoA reductase activity, in comparison to 10 μM simvastatin which only inhibits 35% of the activity. RT-PCR and SELDI-TOF mass spectrometric studies demonstrate that bumarsin regulates the expression of both genes and proteins involved in cholesterol homeostasis. Our results suggest that bumarsin may provide a model for the design of novel drugs that can be used to modulate cholesterol homeostasis.

Item Type:	Article
Research Institute, Centre or Group:	Biomedical Research Centre
Identification Number:	10.1016/j.toxicon.2012.04.352
Depositing User:	Marguerite Lyons
Date Deposited:	28 Sep 2012 11:21
Last Modified:	28 Sep 2012 11:21
URI:	http://shura.shu.ac.uk/id/eprint/6374

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