Drug Discovery Prospect from Untapped Species: Indications from Approved Natural Product Drugs

Abstract

Due to extensive bioprospecting efforts of the past and technology factors, there have been questions about drug discovery prospect from untapped species. We analyzed recent trends of approved drugs derived from previously untapped species, which show no sign of untapped drug-productive species being near extinction and suggest high probability of deriving new drugs from new species in existing drug-productive species families and clusters. Case histories of recently approved drugs reveal useful strategies for deriving new drugs from the scaffolds and pharmacophores of the natural product leads of these untapped species. New technologies such as cryptic gene-cluster exploration may generate novel natural products with highly anticipated potential impact on drug discovery.

Clustered Distribution of Natural Product Leads of Drugs in the Chemical Space as Influenced by the Privileged Target-Sites

“…The number of NPs profiled here is comparable to those of the earlier large-scale NP studies92126. Molecular fingerprints were used for representing NPs in the hierarchical clustering tree because of its demonstrated effectiveness in structural similarity searching, and its extensive applications in drug lead discovery122327282930.…”

“…We collected 442 NPLDs1327283435 and the information about their NP origin128 from the literature. We also collected 169,037 NPs from the ZINC24, TCM-ID29, TCM@Taiwan25, and other literatures3.…”

Techniques Adopted for Extraction of Natural Products Extraction Methods: Maceration, Percolation, Soxhlet Extraction, Turbo distillation, Supercritical Fluid Extraction

“…The examples are terpene pactitaxel from Taxus baccata and Vinca alkaloids from Cantharanthus roseus are the anticancer drugs derived from plants [9,10]. Numerous and varied biological targets are achieved due to the meaningful and interesting development of natural products and some of them are very important in health care system [11,12,13]. For example, small molecules from plants, animals and microorganisms play an important role in…”

Recent Advances in Developing Insect Natural Products as Potential Modern Day Medicines

“…Altogether, 939 nature-derived approved drugs were developed between 1961 and 2010 [4] but none of these were from insects and only a few originated from invertebrates such as leeches, sponges, and cone snails. Difficulties in species identification, drug toxicity, development costs, and large scale production [3] partially explain the reason for the slow progress in developing insect products as potential modern medicines.…”