Plants and microbes as drug targets . Prof. H.S. Prakash Department of Biotechnology University of Mysore Manasagangotri, Mysore 570 006 . Higher plants – a rich source of novel compounds. 400,000 higher plant species 10% characterized chemically
Prof. H.S. Prakash
Department of Biotechnology
University of Mysore
Manasagangotri, Mysore 570 006
Candida, Cryptococcus, Geotrichum, Issatchenkia, Kloeckera, Kluyveromyces, Pichia (including Hansenula polymorpha = P. angusta), Rhodotorula, Rhodosporidium, Schizosaccharomyces pombe, Torulopsis, Trichosporon, Trigonopsis variabilis, Yarrowia lipolytica and Zygosaccharomyces rouxii
Reduction of C=O bonds
dollar anticancer drug
A large number of secondary metabolites have been extracted, isolated and characterized from endophytic microbes, especially from fungal endophytes
Camptothecin has been obtained from fungal endophytes isolated from the inner bark of the plant Nothapodytes foetida from the western coast of India.
Some alkaloids produced by endophytic fungi are also anticancer agents.
Wagenaar et al. isolated three novel cytochalasins from an endophyte Rhinocladiella sp. with potential antitumor activity against selected neoplastic cell lines
Rubrofusarin B is cytotoxic to the colon cancer cell line SW1116 (IC5O: 4.5 μg mL-1), and aurasperone A (18) is inhibitory to xanthine oxidase (XO) (IC50: 10.9 μM).
Rubrofusarin B fonsecinone A, asperpyrone B and aurasperone A by fractionation of the extract of Aspergillus niger IFB-E003, an endophyte of Cynodon dactylon.
Guignardic acid was detected in the culture broth of an endophytic Guignardia sp. obtained from Spondias mombin
Xanthoviridicatin E and F are two novel quinine related metabolites produced by an endophytic Penicillium chrysogenum colonizing an unidentified plant. These metabolites inhibit the cleavage reaction of HIV-1 integrase with IC50 values of 6 and 5 uM, respectively
Phomol is a novel polyketide lactone from Phomopsis sp., present in the medicinal plant Erythrina crista-galli
Microcarpalide, a novel microfilament disrupting agent with weak cytotoxicity to mammalian cells, was characterized from an unidentified fungus in Ficus microcarpa
Antimicrobial compounds from fungal Endophytes: Anti-bacterial
A new anti-inflammatory compound, 5, 7-dimethoxy- 4-p- ethoxylphenylcoumarin (118), and 5, 7-dimethoxy-4-phenylcoumarin (119) were isolated from endophytic Streptomyces aureofaciens CMUAc130
Anti-viral metabolites: Four new cyclohexadepsipeptides, pullularins A–D (120-123), were isolated from the endophytic fungus Pullularia sp. BCC 8613. Pullularin A exhibited activities against the malaria parasite Plasmodium falciparum K1 (IC50 3.6 μg mL-1) and herpes simplex virus type 1
TLC profile of Piperine
ELISA, RT-PCR, RIA, Particle agglutination, cell-based assays, cell culture, HPLC, Genomic sequence
Informatic integration of ‘omics’data sets (bottom up approach)
Computer modeling of disease or organ system from literature (top-down approach to target selection, clinical indication and clinical trial design)
Use of complex human cell system themselved to interpret and predict the biological activities of drugs and gene targets (direct experimental approach)
Ligand binding, receptor dimerization and downstream signalling