Search for a lead compound based on antiausteric activity

2016 Fiscal Year Final Research Report

• Project/Area Number: 25460117
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Natural medicines
• Research Institution: Hokuriku University (2014-2016); University of Toyama (2013)
• Principal Investigator: Tezuka Yasuhiro 北陸大学, 薬学部, 教授 (70236975)
• Project Period (FY): 2013-04-01 – 2017-03-31
• Keywords: 膵臓がん / 栄養飢餓耐性解除 / 和漢薬 / 活性成分 / 抗がん剤 / 穿心蓮

Outline of Final Research Achievements

Preferential cytotoxicity of 24 extracts was determined against PANC-1 and PSN-1 human pancreatic cancer cells and extracts of Andrographis Herba, Isodonis Herba, and Licopodium showed activities. Then, phytochemical investigation of the 70% EtOH extract of Andrographis Herba led to the isolation of 21 known compounds consisting of six labdane-type diterpenes, six flavones, three flavanones, two sterols, a fatty acid, a phthalate, a triterpene, and a monoterpene. Among them, 14-deoxy-11,12-didehydroandrographolide displayed the most potent preferential cytotoxicity against PANC-1 and PSN-1 cells with PC50 values of 10.0 microM and 9.27 microM, respectively. Microscopical observation, double staining with ethidium bromide (EB) and acridine orange (AO), and flow cytometry with propidium iodide/annexin V double staining indicated that 14-deoxy-11,12-didehydroandrographolide triggered apoptosis-like cell death in NDM with an amino acids and/or serum-sensitive mode.

Free Research Field

天然物化学