Atta-ur-Rahman
International Center for Chemical and Biological Sciences, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi-75270, Pakistan

Abstract:

Access to reliable ethnomedicinal knowledge, combined with modern tools of research such as LC-MS/MS, LC-NMR, LC-MS/NMR, etc., and high-throughput screening protocols are greatly facilitating the process of drug discovery from natural sources.

We have already investigated several hundred terrestrial and marine plants for their chemical and biological significance and isolated and identified over 2000 compounds of which some 600 turned out to be new and novel compounds with potential to be developed as medicines. In order to optimize the chances of finding novel leads, extensive primary biological screening and activity-guided fractionation and purification were carried out. State-of-the-art spectroscopic techniques, especially modern multi-dimensional NMR techniques, were utilized to elucidate the structures of bioactive natural molecules, rapidly and accurately. The bioassay protocols include antibacterial, antifungal, cytotoxicity, phytotoxicity, insecticidal, antileishmanial, antioxidant and enzyme inhibition activities. The results so far have been truly exciting as we have identified several new classes of potent cholinesterase, urease, phosphodiesterase, glucuronidase, and prolyl endopeptidase inhibitors. A large number of antioxidant secondary metabolites have also been identified. In the majority of cases, chemical and microbial derivatizations were carried out to study the structure-activity relationships.

A selection of these results illustrated by their potential application to treat diseases such as epilepsy, leishmania, and diabetes will be presented.

The revolutionary changes in the higher education scenario in Pakistan under the the tenure of the author as the  Minister of Science & Technology and the Minister responsible for Higher Education, which resulted in 600% increase in research publications, 1000% increase in citations, 300% increase in student enrolment and PhD output within a span of 8 years will also be described. These have attracted Nature to publish 4 Editorials in the last 3 years, calling it as a lesson for other developing countries to emulate.