title: Cytotoxicity of Triptolide and Triptolide loaded polymeric micelles in vitro.
abstract: Triptolide (TP), a diterpenoid triepoxide purified from the Chinese herb Tripterygium wilfordii Hook F is characterized by strong anti-tumor effects on various cancer cells. Except its anti-tumor effects, TP also shows multiple pharmacological side activities, such as anti-inflammatory, immune-suppressive and male anti-fertility. In order to reduce these side effects, especially the immuno-suppressive activity when used to cure cancer, a novel polymeric micelle system containing TP (TP-PM) was constructed. The immune-modulation effects of TP-PM have been evaluated by previous studies. In this study, we compared the cytotoxicity of TP and TP-PM on Jurkat and HT29 cells. Therefore, we determined the cell viability, membrane integrity, cell proliferation, apoptosis, and caspase 3/7 activity after exposure to TP and TP-PM. The results demonstrated that actually low concentrated TP and TP-PM could induce an inhibition of cell growth and proliferation as well as membrane damage in both tumor cell lines. TP and TP-PM induced apoptosis and caused activation of caspase 3/7 even at low concentrations. Both formulations destroyed the membrane of Jurkat cells, nevertheless, TP-PM showed stronger pernicious effects. In general, TP-PM induced in both tested cell lines stronger effects than TP. Therefore, polymeric micelles can be considered as promising carriers for TP in cancer therapy.
authors.affiliation: Department of General Surgery, Tongji Hospital, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, PR China.
authors.forename: Shunzhen
authors.initials: S
authors.lastname: Zheng
authors.forename: Karin
authors.initials: K
authors.lastname: Löw
authors.forename: Sylvia
authors.initials: S
authors.lastname: Wagner
authors.forename: Xiangliang
authors.initials: X
authors.lastname: Yang
authors.forename: Hagen
authors.initials: H
authors.lastname: von Briesen
authors.forename: Shengquan
authors.initials: S
authors.lastname: Zou
mesh_terms: D018906:Antineoplastic Agents, Alkylating / Q000633:toxicity*; D017209:Apoptosis / Q000187:drug effects; D053148:Caspase 3 / Q000378:metabolism; D053179:Caspase 7 / Q000378:metabolism; D002460:Cell Line; D045744:Cell Line, Tumor; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004224:Diterpenes / Q000633:toxicity*; D004337:Drug Carriers / Q000633:toxicity*; D004365:Drugs, Chinese Herbal / Q000633:toxicity; D004852:Epoxy Compounds / Q000633:toxicity; D006801:Humans; D007166:Immunosuppressive Agents / Q000633:toxicity*; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D008823:Micelles; D010616:Phenanthrenes / Q000633:toxicity*; D011091:Polyesters / Q000633:toxicity*; D011092:Polyethylene Glycols / Q000633:toxicity*
chemical_list: D018906:Antineoplastic Agents, Alkylating; D004224:Diterpenes; D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; D004852:Epoxy Compounds; D007166:Immunosuppressive Agents; D008823:Micelles; D010616:Phenanthrenes; D011091:Polyesters; C561465:methoxy poly(ethylene glycol)-block-poly(lactic acid); C001899:triptolide; D011092:Polyethylene Glycols; D007770:L-Lactate Dehydrogenase; D053148:Caspase 3; D053179:Caspase 7