Matrine Derivatives as HIV Protease Inhibitors

Presented by Shefali Srivastava
Meredith College CSA Day 2020
#MeredithCSA

Abstract:
HIV/AIDS is caused by the Human Immunodeficiency Virus. Its life cycle consists of six steps: infection, reception at the cell, integration into the host DNA, production of non-functional polypeptide, cleavage of polypeptide, and rebudding from the affected cell. The cleavage of the polypeptide chain is catalyzed by the action of HIV protease - a possible target for enzyme inhibition. Oxymatrine is an alkaloid compound extracted from Sophora flacescens, a Chinese herb, which has been shown to increase cardiac function by reducing the risk of heart failure and cardiac fibrosis. Through previous research, this compound has also shown inhibition of the HIV protease enzyme, making it a possible treatment for HIV-AIDS. Currently, there is a huge demand to synthesize chemical derivatives of matrine to make compounds that are more hydrophilic for drug testing. Oxymatrinic and matrinic acid have been prepared and are being tested using the HIV protease assay. The purpose of this study was to explore the inhibition properties of matrinic acid derivatives on the HIV Protease enzyme. Over the course of this study, two derivatives of matrinic acid were synthesized: methyl ester of matrine and matrinamide. They were then tested on an HIV Protease assay to see if they inhibit the enzyme. Neither of the compounds showed any activity for inhibition. While they were both soluble in water, matrine methyl ester proved to be an activator of the HIV Protease enzyme, instead of an inhibitor. However, more research is required to purify the compounds synthesized.

[balthomas]

Yes uh, hello, may I please have an order of the chicken nuggets.... with Uhhh.... Sweet and sour sauce?


To uhhh.... Maybe just water?

Thanks!