The Cytotoxicities Against Two Human Cancer Cell Lines Of The Constituents From Four Natural Products

In the first chapter, we have investigated the anti-cancer activities of four natural products (AA2from Leonurus japonicus, SDC7921from Hedyotidis chrysotricha, Q3and Q4from Gentiana dahurica Fisch) against human hepatocellular carcinoma (HCC) cell lines SK-Hep-1for the first time. The results showed that AA2, SDC7921, Q3and Q4had different degree of the effect to inhibit the growth of SK-Hep-1cells. Only AA2and SDC7921had the abilities to inhibit the migration of SK-Hep-1cells. The caspase3/7assay results revealed that AA2, SDC7921and Q4, but not Q3, increased the activities of caspase3/7. Flow cytometry (FCM) was utilized to detect the apoptosis and cell cycle of the SK-Hep-1cells treated by AA2, SDC7921, Q3and Q4. Only AA2was found to induce the apoptosis of SK-Hep-1cells, as well as blockage at the G2/M phase of the cell cycle.In the second chapter, we investigated the cytotoxicities of compounds isolated from Meliatoosendan against human breast cancer cell line MCF-7. The results demonstrated that some of them inhibited the proliferation of MCF-7with very low IC50values. The mechanism of these inhibitory effects needs further investigation.The significant meanings of the four compounds working on hepatocellular carcinoma and human breast cancer are list as follow:1) AA2(compound name is not presented, for the involving paper has not been published yet); SDC7921is (24S)-Ergostane-3β,5α,6β-triol; Q3is2α,3β,24-trihydroxy-urs-12-en-28-oic acid;Q4is2a-hydroxyursolic acid. So far it is the first time to investigate the anti-cancer activity of these four natural products against SK-Hep-1. This research is of significance for the development of new drugs for hepatocellular carcinoma treatment.2) The compounds with cytotoxicity against MCF-7cells are come from M. toosendan. Compounds1-10are new tetracyclic triterpenoids. Compound13is a novel steroid. Compounds14-17and compound20are known compounds. It is the first time to investigate cytotoxicities of these new compounds; it is also the first to test the cytotoxicities of these known compounds against MCF-7. Therefore, this research is significant for the development of new drugs for human breast cancer.