Nature: a vital source of leads for anticancer drug development

Abstract

Over 60% of the current anticancer drugs have their origin in one way or another from natural sources. Nature continues to be the most prolific source of biologically active and diverse chemotypes, and it is becoming increasingly evident that associated microbes may often be the source of biologically active compounds originally isolated from host macro-organisms. While relatively few of the actual isolated compounds advance to become clinically effective drugs in their own right, these unique molecules may serve as models for the preparation of more efficacious analogs using chemical methodology such as total or combinatorial (parallel) synthesis, or manipulation of biosynthetic pathways. In addition, conjugation of toxic natural molecules to monoclonal antibodies or polymeric carriers specifically targeted to epitopes on tumors of interest can lead to the development of efficacious targeted therapies. The essential role played by natural products in the discovery and development of effective anticancer agents, and the importance of multidisciplinary collaboration in the generation and optimization of novel molecular leads from natural product sources is reviewed.

Novel Tandem Biotransformation Process for the Biosynthesis of a Novel Compound, 4-(2,3,5,6-Tetramethylpyrazine-1)-4′-Demethylepipodophyllotoxin

“…The structural modification of natural products has been an essential pathway in the discovery and development of effective anticancer agents (9,10). A shorter and environmentally milder procedure to modify bioactive natural lead compound is an important goal for the next few years.…”

Should Seed Be an Alternative Source of Camptothecin From Nothapodytes nimmoniana and Chonemorpha fragrance?

“…The medicinal importance of a forest plant lies on the bioactive constituents it produces that have significant pharmacological activity and can be isolated with potentials for drug development. 1 The breakthrough on cytotoxicity of extract from plants led to the discovery of natural compounds with anticancer properties 2 and their development into drugs emanated from studies of extracts isolated from seeds. 1,2 Biosynthesis and yield of the compounds vary with forest species and with many, seeds are an important source of the alkaloids.…”

“…1 The breakthrough on cytotoxicity of extract from plants led to the discovery of natural compounds with anticancer properties 2 and their development into drugs emanated from studies of extracts isolated from seeds. 1,2 Biosynthesis and yield of the compounds vary with forest species and with many, seeds are an important source of the alkaloids. They offer a practical, cost-effective alternative to extraction from the natural population over chemical synthesis.…”

Induction of apoptosis in HT-29 cells by quercetin through mitochondria-mediated apoptotic pathway

“…Recently, more attention has been paid to naturally occurring chemopreventive compounds that can inhibit, retard, or reverse the process of multistage carcinogenesis with minimal toxicity. Over 60% of the current anticancer drugs have their origin in one way or another from natural sources (Cragg & Newman 2009). …”