Poligapolide, a PI3K/Akt Inhibitor in Immunodeficiency Virus Type 1 TAT-Transduced CHME5 Cells, Isolated from the Rhizome of Polygala tenuifolia
スポンサーリンク
概要
- 論文の詳細を見る
The rhizome of Polygala tenuifolia <span style="font-variant: small-caps;">WILLD</span> (PT, family Polygalaceae) has been used in traditional Chinese medicine for inflammation, dementia, amnesia, neurasthenia and cancer. The phosphoinositide 3-kinase (PI3K)/Akt inhibitor(s) was isolated from PT by using the cytoprotective phenotype of human immunodeficiency virus type 1 (HIV-1) Tat-transduced CHME5 cells against lipopolysaccharide/cycloheximide. We isolated 9 constituents (1)–(9) from ethyl acetate fraction of PT, which potently showed anti-cytoprotective effect against HIV-1 TAT-transduced cells. Of them, (9R)-(−)-9-peptandecanolide (2), a new compound named poligapolide, most potently abolished the cytoprotective effect of HIV-1 Tat-transduced CHME5 cells. The compound (2) inhibited the phosphorylation of Akt and its downstream molecule, glycogen synthase kinase-3 beta (GSK3β) in PI3K/Akt cell survival signaling pathway, but did not suppress the phosphorylation of PI3K and pyruvate dehydrogenase lipoamide kinase isozyme 1. Based on these finding, poligapolide may abolish the cytoprotective phenotype of HIV-1 Tat-transduced CHME5 cells by inhibiting Akt phosphorylation in PI3K/Akt pathway.
- 公益社団法人 日本薬学会の論文
公益社団法人 日本薬学会 | 論文
- Effects of Nutrition Support Team Services on Outcomes in ICU Patients
- The Mechanisms of Insulin Secretion and Calcium Signaling in Pancreatic β-Cells Exposed to Fluoroquinolones
- Intrathecal Ketamine and Pregabalin at Sub-effective Doses Synergistically Reduces Neuropathic Pain without Motor Dysfunction in Mice
- Discovering Some Novel 7-Chloroquinolines Carrying a Biologically Active Benzenesulfonamide Moiety as a New Class of Anticancer Agents
- Novel Insights into Disease Modeling Using Induced Pluripotent Stem Cells