Development of Novel Anticancer Agents from Natural Products

Abstract

Cancer is the second leading cause of death in the globe and plants have been used in the treatment of cancer since ancient times. Plants are the natural hub of promising anticancer agents. Spathodea campanulata P. Beauv and Duranta erecta L. are traditionally reported medicinal anticancer plant which lacks scientific exploration of the interesting anticancer moiety. newlineThe present work is aimed to develop some novel anticancer compounds from the leaves of Spathodea campanulata P. Beauv and stem of Duranta erecta. Dried powders of plants were extracted successively with n-hexane, chloroform, ethyl acetate, methanol, and water solvents to screen chemicals. The extracts were tested on breast, colon and leukemia (MCF-7, HT-29 and HL-60) cell lines using SRB assay for cytotoxic potential. The chloroform extract of the S. campanulata and D. erecta showed the highest percent inhibition of HL-60 cell lines in given concentrations. Bioactive extracts also exhibited remarkable in vitro antioxidant and brine shrimp cytotoxicity. Some chemicals were isolated from bioactive chloroform extract using column chromatography and purified using re-column and preparative TLC. The isolated compounds were identified by using physicochemical study and spectroscopy data like UV, FTIR, 1H NMR, 13C NMR and ESI-TOF MS. Stigmasterol, octadecenamide and umbelliferone were isolated from bioactive extracts of S. campanulata and ursolic acid, 1-hydroxy-2-napthoic acid, pyrocatechol and kaemferol from bioactive extracts of D. erecta and also studied for anticancer activity on cell lines by using SRB assay and in silico by molecular docking. Among these isolated compounds, octadecenamide (S. campanulata) and ursolic acid (D. erecta) showed good cytotoxic potential against acute Leukemia (HL 60) cells. In molecular docking studies, all isolated compounds were efficiently bound to target and support the in-vitro cytotoxic activity of the extract and compounds. newlineThe study showed that extracts of both the plants and isolated phytochemicals were active a