Chemical composition and antimicrobial and cytotoxic activities of Antidesm abunius L.

It was deemed of interest to investigate Antidesm bunius aerial parts from phytochemical and biological points of view due to limited previous studies. Isolation and identification of phenolic compounds and evaluation of the potential antimicrobial and cytotoxic effects of A. bunius aerial parts was investigated. The petroleum ether (PEE) and 80% EtOH extracts (EE), as well as, n-hexane (HF), CHCl3 (CF), EtOAc (EAF), n-BuOH (BF) and H2O soluble fractions (WF) of the latter were prepared. Phytochemical study has been performed for isolation and identification of the major polyphenols. Antimicrobial activity, using diffusion agar technique, and potential cytotoxic effect against HepG2, MCF7 and HCT cell lines were evaluated. Malic acid (I), caffeic acid (II), methyl benzoate (III), (+)-catechin (IV), (-)-epicatechin (V), epicatechin-(4ß→8)-catechin (procynidin B1, VI) and epicatechin-(4ß→8)-epicatechin (procyanidin B2, VII) were isolated. Compounds I-VII showed strong to moderate antimicrobial activity, with MIC values in the range of 1.95-125µg/ml except for compounds 1 and IV, which did not show any effect. All tested samples showed dose dependent cytotoxic effect against all three tested cell lines. PEE showed strong cytotoxic activity (IC50=23.7-38.2µg/ml). Furthermore, compound VI showed potent cytotoxicity against HepG2, MCF7 and HCT cell lines (IC50=24.7, 16.5 and 18.0µg/ml) respectively. The strong to moderate antimicrobial activity and cytotoxic effect of the plant could be attributed to its content of phenolic acids, flavan-3-ols and/or proanthocyanidins. These findings were confirmed by results obtained for the isolated compounds.

Effect of precursors feeding and media manipulation on production of novel anticancer pro-drug camptothecin from endophytic fungus

We have established methodology for the isolation and characterization of a novel endophytic fungus from the inner bark of medicinal plant Nothapodytes foetida, which produced camptothecin in Sabouraud broth (SB) under shake flask conditions. Camptothecin and its related compounds are at present obtained by extraction from intact plants, but fungal endopytes may be an alternative source of production. In present study we have observed the effect of different nutrient combinations and precursors (tryptophan, tryptamine, geraniol, citral, mevalonic acid and leucine) on the accumulation of camptothecin by endophytic fungus Entrophospora infrequens. The precursors were fed either alone or in combinations (tryptophan and geraniol, tryptophan and citral, tryptophan and mevalonic acid, tryptophan and leucine). The highest camptothecin content was observed in the range of 503 ± 25µg/100g dry cell mass in Sabouraud medium. Camptothecin content in the medium was increased by 2.5 folds by the presence of tryptophan and leucine whereas the production with trytophan was also significantly different from other treatments. Furthermore, the effect of fungal camptothecin on the morphology of human cancer cell lines was also studied. The treated cells showed reduction in size, condensation of nucleus and the protoplasmic extensions were reduced. All these characteristics are found in apoptotic cells.

Effect of precursors feeding and media manipulation on production of novel anticancer pro-drug camptothecin from endophytic fungus.

We have established methodology for the isolation and characterization of a novel endophytic fungus from the inner bark of medicinal plant Nothapodytes foetida, which produced camptothecin in Sabouraud broth (SB) under shake flask conditions. Camptothecin and its related compounds are at present obtained by extraction from intact plants, but fungal endopytes may be an alternative source of production. In present study we have observed the effect of different nutrient combinations and precursors (tryptophan, tryptamine, geraniol, citral, mevalonic acid and leucine) on the accumulation of camptothecin by endophytic fungus Entrophospora infrequens. The precursors were fed either alone or in combinations (tryptophan and geraniol, tryptophan and citral, tryptophan and mevalonic acid, tryptophan and leucine). The highest camptothecin content was observed in the range of 503 ± 25µg/100g dry cell mass in Sabouraud medium. Camptothecin content in the medium was increased by 2.5 folds by the presence of tryptophan and leucine whereas the production with trytophan was also significantly different from other treatments. Furthermore, the effect of fungal camptothecin on the morphology of human cancer cell lines was also studied. The treated cells showed reduction in size, condensation of nucleus and the protoplasmic extensions were reduced. All these characteristics are found in apoptotic cells.