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Design, Synthesis And Cytotoxic Evaluation Of O-Carboxamido Stilbene Analogues, Kok Hoong Leong
Design, Synthesis And Cytotoxic Evaluation Of O-Carboxamido Stilbene Analogues, Kok Hoong Leong
Kok Hoong Leong
Resveratrol, a natural stilbene found in grapes and wines exhibits a wide range of pharmacological properties. Resveratrol is also known as a good chemopreventive agent for inhibiting carcinogenesis processes that target kinases, cyclooxygenases, ribonucleotide reductase and DNA polymerases. A total of 19 analogues with an amide moiety were synthesized and the cytotoxic effects of the analogues on a series of human cancer cell lines are reported. Three compounds 6d, 6i and 6n showed potent cytotoxicity against prostate cancer DU-145 (IC50 = 16.68 μM), colon cancer HT-29 (IC50 = 7.51 μM) and breast cancer MCF-7 (IC50 = 21.24 μM), respectively, which …
Induction Of Apoptosis In Human Breast Cancer Cells Via Caspase Pathway By Vernodalin Isolated From Centratherum Anthelminticum(L.) Seeds, Kok Hoong Leong
Induction Of Apoptosis In Human Breast Cancer Cells Via Caspase Pathway By Vernodalin Isolated From Centratherum Anthelminticum(L.) Seeds, Kok Hoong Leong
Kok Hoong Leong
In this study, we showed that CACF inhibited growth of MCF-7 human breast cancer cells. CACF induced apoptosis in MCF-7 cells as marked by cell size shrinkage, deformed cytoskeletal structure and DNA fragmentation. To identify the cytotoxic compound, CACF was subjected to bioassay-guided fractionation which yielded 6 fractions. CACF fraction A and B (CACF-A, -B) demonstrated highest activity among all the fractions. Further HPLC isolation, NMR and LC-MS analysis of CACF-A led to identification of vernodalin as the cytotoxic agent in CACF-A, and -B. 12,13-dihydroxyoleic acid, another major compound in CACF-C fraction was isolated for the first time from Centratherum …