Studies On The Chemical Components, Biological Activity And Pharmacokinetics Of Hemsleya Penxianensis

Hemsleya penxianensis, known as “Xue Dan” in Chinese, is widely distributed insouthwestern region of China, such as Yunnan, Sichuan and Guizhou provinces.H.penxianensis is listed in the Chinese Pharmacopoeia as a traditional herbal medicine for thetreatment of dysentery, enteritis, bronchitis, acute tonsillitis.Aim: To study the chemical constituents of H.penxianensis, and study their cytotoxic activityand pharmacokinetic characteristics in rats.Methods: The ethyl acetate extract was isolated and purified by Silica gel column, SephadexLH-20column, ODS column, pre-HPLC and re-crystallization techniques. Their structureswere determined on the basis of physical properties and spectroscopic data. The cytotoxicactivity of the isolated six compounds against H460(Human lung adenocarcinoma), SW-620(Human colon cancer), and COLO205(Human colon cancer) were evaluated by MTTmethod.Results: A phytochemistry investigation on the ethyl acetate extract of H.penxianensisresulted in the isolation of six compounds. Their structures were identified to behemslepenside A (1),16-O-acetyl-cucurbitacin F (2) and16,25-O-diacetyl-cucurbitacinF-2-O--D-glucopyranoside (3), together with three known analogues25-O-acetyl-23,24-dihydrocucurbitacin F (4),23,24-dihydrocucurbitacin F (5) and jinfushanoside A (6). Allof the isolated compounds were evaluated for their cytotoxic activity against H460, SW-620and COLO205by MTT method. The results showed that compounds1-6have a strong cytotoxicity. The pharmacokinetic study of23,24-dihydrocucurbitacin F (5) was evaluated inmale Wistar rats. After the rats were intravenously administrated, the plasma samplescollected at different time points were determined by liquid chromatography tandem massspectrometry. AUC(0-t)was811.615111.578g h L-1, t1/2was1.2851.390h, CL was3.6270.487L h kg-1, Vd was6.7217.429L kg-1.Conclusion: Six compounds were isolated from the ethyl acetate extract of H.penxianensis.Among them, compound1-3were new compounds, and all of them showed certain cytotoxicactivity against H460, SW-620and COLO205cell lines.