Chapter 15 - Hybrid Approach for Transformation for Betulin (an Anti-HIV Molecule)

Abstract

Betulin and betulinic acid are pentacyclic lupane-type triterpenes widely distributed in the plant kingdom, and commercially obtained from Betula species plants. A variety of biological actions have been recognized for betulin derivatives, such as anti-HIV, anticancer, antiinflammatory, and antimalarial properties. Betulin and betulinic acid are broadly isolated from white birch bark and selectively inhibit the growth of HIV-1. However, the poor water solubility of betulin hinders its pharmacological effectiveness and has inspired the search for some better hydrophilic derivatives. Here we summarize how various value addition practices have been in use over many decades and economical sources, such as the bark of Betula spp. Plant, are used to obtain betulin and betulinic acid derivatives obtained from different synthesis routes. Microbial transformation has been found to be a preferable option for getting betulinic acid derivatives with these derivatives being more effective than native molecules as potent anti-HIV molecules. Betulin and betulinic acid derivatives are prevailing and are good selective inhibitors of HIV-1. Based on their specific side-chain alterations, these molecules represent a remarkable anti-HIV group of molecules that can block either HIV-1 fusion or maturation or both together.