Natural products: A continuing source of novel drug leads

Abstract

1. Background Nature has been a source of medicinal products for millennia, with many useful drugs developed from plant sources. Following discovery of the penicillins, drug discovery from microbial sources occurred and diving techniques in the 1970s opened the seas. Combinatorial chemistry (late 1980s), shifted the focus of drug discovery efforts from Nature to the laboratory bench. 2. Scope of Review This review traces natural products drug discovery, outlining important drugs from natural sources that revolutionized treatment of serious diseases. It is clear Nature will continue to be a major source of new structural leads, and effective drug development depends on multidisciplinary collaborations. 3. Major Conclusions The explosion of genetic information led not only to novel screens, but the genetic techniques permitted the implementation of combinatorial biosynthetic technology and genome mining. The knowledge gained has allowed unknown molecules to be identified. These novel bioactive structures can be optimized by using combinatorial chemistry generating new drug candidates for many diseases. 4 General Significance: The advent of genetic techniques that permitted the isolation / expression of biosynthetic cassettes from microbes may well be the new frontier for natural products lead discovery. It is now apparent that biodiversity may be much greater in those organisms. The numbers of potential species involved in the microbial world are many orders of magnitude greater than those of plants and multi-celled animals. Coupling these numbers to the number of currently unexpressed biosynthetic clusters now identified (>10 per species) the potential of microbial diversity remains essentially untapped.

Urban park soil microbiomes are a rich reservoir of natural product biosynthetic diversity

“…Microbial diversity surveys indicate that NYC is also home to diverse bacterial and fungal communities (9,10). Although bacteria produce a tremendous diversity of small molecules, nonribosomal peptide (NRP) and polyketide (PK) biosynthesis is responsible for producing many of the most biomedically important NPs characterized from bacteria (1,11). Both biosynthetic systems follow the same paradigm wherein molecules are generated in an iterative building process, using enzymes that are composed of conserved domains organized into modules (Fig.…”

In Vitro Antioxidant Activity, Antimicrobial and Preliminary Cytotoxic Activity of Cynometra Ramiflora- A Mangrove Plant

“…Plant derived natural products have been the single most productive source of leads for the discovery of novel drugs (Cragg and Newman, 2013). However, the global efforts remain still invigorated by the numerous attempts to analyze bioactivity and search for bioactive compounds from plant sources.…”

Penares sp sponge from Menjangan Island-water West Bali National Park: Isolation of Cytotoxic Compounds

“…Laut menutupi hampir 70% luas permukaan bumi, sehingga organisma laut hadir sebagai sumber pene muan senyawa baru yang Correspondence author: Erna Prawita Setyowati Email : erna_prawita@ugm.ac.id sangat potensial untuk dikembangkan lebih lanjut menjadi obat (Cragg and Newman, 2013). Spons (filum Porifera) merupakan organisma multiseluler, tak bertulang belakang dengan tubuh berpori.…”