According to the World Health Organization, more than 1 billion people are at risk of or are affected by neglected tropical diseases. Examples of such diseases include trypanosomiasis, which causes sleeping sickness; leishmaniasis; and Chagas disease, all of which are prevalent in Africa, South America, and India. Our aim within the New Medicines for Trypanosomatidic Infections project was to use (1) synthetic and natural product libraries, (2) screening, and (3) a preclinical absorption, distribution, metabolism, and excretion–toxicity (ADME-Tox) profiling platform to identify compounds that can enter the trypanosomatidic drug discovery value chain.
As part of an international research project, the marine fungal strain collection of the Helmholtz Centre for Ocean Research (GEOMAR) research centre was analysed for secondary metabolite profiles associated with anticancer activity. Strain MF458 was identified as Tolypocladium geodes, by internal transcribed spacer region (ITS) sequence similarity and its natural product production profile.
An extract of a culture of the fungus Galiella rufa yielded several new derivatives of pregaliellalactone (1) that were characterised by NMR and MS experiments. The tetraene 4 has been reported previously, but was in this investigation isolated in sufficient amounts for the determination of the configuration of the C-4/C-5 double bond which is Z, not E.
This study covers the isolation, testing, and identification of natural products with anticancer properties. Secondary metabolites were isolated from fungal strains originating from a variety of marine habitats. Strain culture protocols were optimized with respect to growth media composition and fermentation conditions. From these producers, isolated compounds were screened for their effect on the viability and proliferation of a subset of the NCI60 panel of cancer cell lines. Active compounds of interest were identified and selected for detailed assessments and structural elucidation using nuclear magnetic resonance.
Naturally-occurring compounds have been, and continue to be, an important source of new leads and of commercially successful products for various industrial sectors, notably pharmaceuticals and agrochemicals. The conference, Functional Molecules from Natural Sources, held at Magdalen College, Oxford, in July 2009 set out to highlight current trends, challenges and successes in the exploitation of natural products from microbial, plant and marine sources. Based on the proceedings of this conference, the main themes of this book are modern and emerging perspectives on natural product utilization and improved strategies for natural products exploitation. It provides case studies on important natural product leads (functional molecules) and their enhancement.
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Hypha Discovery is a UK-based CRO supporting pharmaceutical and agrochemical companies worldwide through the production of metabolites and new derivatives of drugs and agrochemicals in discovery and development.