title: Cellular mechanisms of a new pyrazinone compound that induces apoptosis in SKOV-3 cells.
abstract: We screened a small molecular library that was designed and independently synthesized in vitro and found a new drug (MY-03-01) that is active against ovarian cancer. We established that MY-03-01 effectively inhibited SKOV-3 cell survival in a dose-dependent manner, based on cell viability rates, and that it not only induced SKOV-3 apoptosis by itself, but also did so synergistically with paclitaxel. Secondly, when MY-03-01 was applied at 40 μM, its hemolytic activity was less than 10%, compared with the control, and there was almost no damage to normal cells at this concentration. In addition, we used DAPI staining and flow cytometry to show that MY- 03-01 could significantly induce apoptosis of SKOV-3 cells. Finally, we found that MY-03-01 likely induced SKOV-3 apoptosis by activating caspase3 and caspase9 through the mitochondrial pathway.
authors.affiliation: Key Laboratory for Molecular Enzymology and Engineering of Ministry of Education, Jilin University, Changchun, China E-mail : shiw@jlu.edu.cn.
authors.forename: Guan
authors.initials: G
authors.lastname: Wang
authors.forename: Meng-Ying
authors.initials: MY
authors.lastname: Jiang
authors.forename: Ying
authors.initials: Y
authors.lastname: Meng
authors.forename: Hong-Rui
authors.initials: HR
authors.lastname: Song
authors.forename: Wei
authors.initials: W
authors.lastname: Shi
mesh_terms: D000081:Acetamides / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D015153:Blotting, Western; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D005260:Female; D005434:Flow Cytometry; D006461:Hemolysis / Q000187:drug effects*; D006801:Humans; D010051:Ovarian Neoplasms / Q000188:drug therapy / Q000473:pathology*; D011719:Pyrazines / Q000737:chemistry* / Q000494:pharmacology; D011817:Rabbits; D014407:Tumor Cells, Cultured
chemical_list: C000592921:2-chloro-N-(2-(1-oxo-3-(p-toly)pyrrolo(1,2-a)pyrazin-2(1H)-yl)acetamide; D000081:Acetamides; D000970:Antineoplastic Agents; D011719:Pyrazines