Science et thérapie du cancer

Bioassay-guided Isolation of New Antitumor Agent from Ficus faveolata (Wall. ex Miq.)

Abstract

Ala Ud Din, Ghias Uddin, Nusrat Hussain, Ajmal Khan, Inamullah Khan, Anwar Ali Shad and Mohammad Iqbal Choudary

Ficus species have been used in both Ayurvedic and Traditional Chinese Medicine (TCM); however the medicinal uses of these species are widely found and originated in Middle East. The phytochemical study of Ficus foveolata was under taken with small scale extraction of stem (300 g) for cytotoxic screening and dereplication purpose. The crude methanolic extract of Ficus was partitioned into different fractions of hexane, dichloromethane and methanol. All the five fractions FA, FB, FC, FD and FE were screened for their anti-proliferative effect in the disk diffusion assay (In vitro) against six cancer cell lines. The bioassay-guided isolation of a new antitumor agent (Ficusonolide; 3α-hydroxylean-12-en-29, 19α-olide (1)) was carried out from the methanolic extract (FB) of Ficus faveolata. Its structure was elucidated on the basis of extensive spectroscopic techniques (IR, MS and NMR). The pure compound 1 was evaluated against twelve cell cancer lines for the determination of its antiproliferative potency. In disk diffusion assay the dichloromethane fraction (FB) showed excellent activity at very low concentration. The compound 1 exhibited strong and selective activity against two cancer cell lines: H116 (Human colon adenocarcinoma) and H125 (Human lung adenocarcinoma) with the IC50=7.8 μg/ml and 11.0 μg/ ml respectively. The selectivity and potency of the pure compound 1 was in concordance with the activity profile of the fraction FB and ethno-medicinal uses of this plant. This small project on local medicinal plants has opened new vista for future research work on indigenous medicinal plants. The compound 1 can be used a template compound for further studies, as a chemotherapeutic agents against cancer.