Natural Products as Sources of New Drugs from 1981 to 2014

Abstract

This contribution is a completely updated and expanded version of the four prior analogous reviews that were published in this journal in 1997, 2003, 2007, and 2012. In the case of all approved therapeutic agents, the time frame has been extended to cover the 34 years from January 1, 1981, to December 31, 2014, for all diseases worldwide, and from 1950 (earliest so far identified) to December 2014 for all approved antitumor drugs worldwide. As mentioned in the 2012 review, we have continued to utilize our secondary subdivision of a "natural product mimic", or "NM", to join the original primary divisions and the designation "natural product botanical", or "NB", to cover those botanical "defined mixtures" now recognized as drug entities by the U.S. FDA (and similar organizations). From the data presented in this review, the utilization of natural products and/or their novel structures, in order to discover and develop the final drug entity, is still alive and well. For example, in the area of cancer, over the time frame from around the 1940s to the end of 2014, of the 175 small molecules approved, 131, or 75%, are other than "S" (synthetic), with 85, or 49%, actually being either natural products or directly derived therefrom. In other areas, the influence of natural product structures is quite marked, with, as expected from prior information, the anti-infective area being dependent on natural products and their structures. We wish to draw the attention of readers to the rapidly evolving recognition that a significant number of natural product drugs/leads are actually produced by microbes and/or microbial interactions with the "host from whence it was isolated", and therefore it is considered that this area of natural product research should be expanded significantly.

Isoaaptamine Induces t-47D Cells Apoptosis and Autophagy via Oxidative Stress

“…They exhibited anti-HIV, anti-fungal, anti-photoaging, anti-infective, anti-fouling, antidepressant, anti-viral, anti-malarial, and cytotoxic activities [13][14][15][16][17][18][19]. Even a bronchodilator drug, benafentrine, has been developed on the basis of benzo[c] [1,6]naphthyridines nucleus and acted as a phosphodiesterase III/IV inhibitor [51].…”

“…They are characterized by the presence of a benzo[de] [1,6]naphthyridine ring in their framework. All aaptamines were obtained from Demospongiae, a class of marine sponges, (also called "horny sponges" or "siliceous sponges"), the largest class in the phylum Porifera.…”

Molecular beacons to identify gifted microbes for genome mining

“…These predictions have been confirmed experimentally, 7,8 and generalized to actinomycetes and other bacterial taxa with large genomes. [9][10][11][12][13][14][15][16] NPs continue to be important sources of new and novel chemical scaffolds for drug discovery, 17,18 and actinomycetes, particularly Streptomyces species, continue to be the most productive sources. 4,19,20 To access the enormous untapped cryptic SM coding capacity of actinomycetes, it is critical to develop robust approaches to activate gene cluster expression.…”

Phytotherapy: Present State of the Issue

“…Активные компоненты некоторых из них послужили основой для создания официнальных лекар-ственных препаратов. Более того, анализ, проведенный в 2007 г. Национальным институтом США по изучению рака (National Cancer Institute, NCI), показал, что дей-ствующие вещества для 2/3 лекарственных препара-тов, разработанных в предшествующие 25 лет, имели природное происхождение [1]. При изучении составля-ющих компонентов противоопухолевых средств, исполь-зуемых на протяжении периода с 1940 по 2014 г., из одобренных 175 малых молекул 49% были веще-ствами натурального происхождения [1] (например, противоопухолевое средство паклитаксел содержит в своем составе компоненты тиса коротколистного; лат.…”

“…Артемизин -пре-парат на основе полыни однолетней (Artemisia annua) -в настоящее время используется во многих странах в качестве первой линии при лечении малярии в связи с возрастающей устойчивостью малярийного плазмодия ПЕДИАТРИЧЕСКАЯ ФАРМАКОЛОГИЯ /2016/ ТОМ 13/ № 5 к препаратам предыдущего поколения [2]. Поиск лекар-ственных веществ в природе актуален и в настоящее время [1,3].…”