Application of Microbial Biotransformation for the New Drug Discovery Using Natural Drugs as Substrates

Abstract

This review describes microbial transformation studies of natural drugs, its importance in correlating them with the corresponding metabolism (biotransformation) in animal system and in the structural modification of complex drug molecules, which are difficult to obtain synthetically. Emphasis is laid on the potential microorganisms, which mimic the pathways of mammalian metabolism and which involve in stereoselective, regiospecific and selective conversions of natural drugs to their derivatives by microorganisms, which are more useful and difficult to synthesize. This paper describes the present state-of-art, will elucidate the additional possibilities with microbial biotransformation of natural drugs, i.e., comparison of microbial transformation with mammalian metabolism and possibility of producing novel molecules, which are difficult to produce by other means.

Biotransformation of Artemisinin Mediated through Fungal Strains for Obtaining Derivatives with Novel Activities

“…The importance and usefulness of microbial transformation in carrying out a variety of chemical conversions is well documented in the previously published reports [21,22].…”

Microbial Metabolism of Biologically Active Secondary Metabolites from Nerium oleander L.

“…Microbial models may constitute an alternative to animal models as they can mimic the mammalian metabolism. 26) Microorganisms have been widely utilized as models of drug metabolism to predict the fate of xenobiotics in mammalian systems. 27) Since this method often gives sufficient quantities of metabolites, complete chemical structures and pharmacological activities could be detected.…”

Biotransformation of 3-hydroxydibenzo-a-pyrone into 3,8 dihydroxydibenzo-a-pyrone and aminoacyl conjugates by Aspergillus niger isolated from native shilajit

“…The DBP-converting factor is perhaps a metabolism related enzyme which by oxidation forms 3,8(OH) 2 -DBP; which acts as a substrate for further enzymatic reactions like conjugation with amino acids to form aminoacyl conjugates and render these compounds more water-soluble and hence more bioavailable. In certain cases, these mechanisms are operative in the fungi not only to detoxify the toxic substance, but also to make them beneficial for the organism (Venisetty and Ciddi, 2003).…”

“…Conceivably, the use of microorganisms constitutes an interesting alternative to study this type of transformation. Additionally, microbial oxidations have advantages over classical organic synthetic procedures (Schmid et al 2001;Boaventura et al 2004), since they are carried out in environment friendly and mild conditions and use biodegradable reagents and they are generally stereoand regio-selective (Venisetty and Ciddi, 2003;de Carvalho and da Fonseca, 2006).…”