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Screening of natural derived compounds for anti-inflammatory and anti-infective properties: our experience

Throughout history people have used plants and natural derived products to cure and prevent diseases. Although the healing properties of plants have been known for a long time, the ability to better exploit the uniqueness of plant therapeutics expanded as a result of the dramatic advantages in biochemical engineering, molecular genomics, analytical chemistry separation techniques, molecular characterizations and screening for the new pharmaceuticals. It seems that discovery, development and manufacturing of botanical therapeutics, either isolated from plants and different organisms or delivered as food constituents, is likely to be a major area of plant biotechnology expansion in the twenty-first century. The challenges is to integrate identification and genetic manipulation of complex biosynthetic pathways in plants for natural sources derived therapeutics and other organisms with better characterizations of genetic targets for the prevention and treatment of complex diseases. However, an important process as well is the development of detection, validation and manufacturing technologies that are compatible with diverse phytochemical mixtures. This goes together with development of the new systems and assays for better selection of promising hits – high throughput screening (HTS). HTS is system for analyzing compound libraries and natural products in order to identify new therapeutic hits and leads on potential targets. HTS arose in last ten years, as 96 well microtitre plates took over from test tubes as the receptacle of choice for biological assays. In combination with combinatorial chemistry it resulted in a paradigm shift from knowledge-based sequential synthesis and testing to parallel processing of multiple compounds. With the objective to improve success rates and cycle times for discovering new hits, HTS is set to become one of the cornerstones of drug discovery. In PLIVA d.d. we introduced dedicated Screening Unit in mid 2000. with screenings of selected targets in anti-infective and anti-inflammatory area. The compounds we screened are produced in house and are acquired from different providers. Among them there are some genuine natural compounds, as well as, specific classes of natural compounds known as biologically active molecules. Our experience in developing an integrated approach in screening these molecules, challenges for selected assays, and hit-set selection will be described.

screening; natural derived compounds; anti-inflammatory; anti-infective

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