title: Effects of alpha-hederin and thymoquinone, constituents of Nigella sativa, on human cancer cell lines.
abstract: The separate effects of alpha-hederin and thymoquinone, the two principal bioactive constituents of Nigella sativa, on four human cancer cell lines [A549 (lung carcinoma), HEp-2 (larynx epidermoid carcinoma), HT-29 (colon adenocarcinoma) and MIA PaCa-2 (pancreas carcinoma)] were investigated. Alpha-hederin was also examined as a pro-drug. Each assessment quantified both cytotoxic and apoptotic/necrotic effects. Alpha-hederin and thymoquinone separately induced a dose- and time-dependent effect on the cell lines tested. HEp-2 cells were the most sensitive, exhibiting apoptosis with a higher incidence following thymoquinone treatment. Pre-treatment of cells with alpha-hederin, followed by thymoquinone or cisplatin, did not enhance the cytotoxicity or apoptosis induced by either drug. So, the membrane-perforating properties associated with saponins, here represented by alpha-hederin, enhance neither cytotoxicity nor apoptosis of these cancer cells.
authors.affiliation: Department of Zoology, University College Dublin, Belfield, Dublin 4, Ireland.
authors.forename: Sara
authors.initials: S
authors.lastname: Rooney
authors.forename: M F
authors.initials: MF
authors.lastname: Ryan
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy; D017209:Apoptosis / Q000187:drug effects; D016227:Benzoquinones / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003110:Colonic Neoplasms / Q000188:drug therapy; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D019073:HT29 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D007822:Laryngeal Neoplasms / Q000188:drug therapy; D008175:Lung Neoplasms / Q000188:drug therapy; D009336:Necrosis; D009369:Neoplasms / Q000188:drug therapy*; D031881:Nigella sativa / Q000737:chemistry; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D010190:Pancreatic Neoplasms / Q000188:drug therapy; D011355:Prodrugs / Q000494:pharmacology; D012503:Saponins / Q000494:pharmacology*
chemical_list: D016227:Benzoquinones; D004365:Drugs, Chinese Herbal; D011355:Prodrugs; D012503:Saponins; C010177:beta-hederin; D009828:Oleanolic Acid; C003466:thymoquinone