4.4 Article

Anti-cancer and anti-inflammatory new vakognavine-type alkaloid from the roots of Aconitum carmichaelii

期刊

TETRAHEDRON LETTERS
卷 57, 期 52, 页码 5881-5884

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2016.11.065

关键词

Vakognavine-type alkaloid; Aconitum carmichaelii; Anti-cancer activity; Anti-inflammatory activity

资金

  1. Macao Science and Technology Development Fund [086/2013/A3]
  2. Natural Science Foundation of China [51428303]
  3. Sino-Africa Joint Research Project [SAJC20160233]

向作者/读者索取更多资源

Vakognavine-type alkaloids are a rare kind of diterpenoid alkaloid isolated from Delphinium and Aconitum species. During our research on the chemical constituents of the roots of Aconitum carmichaelii, a new vakognavine-type alkaloid (1) along with a known vakognavine-type alkaloid, trifoliolasine E (2), and two known hetisine-type alkaloids (3 and 4) were obtained. The structures were elucidated by a combination of high resolution ESI-MS, 1D and 2D NMR spectra. Compound 1 showed strong inhibitory effects on HT-29, SGC-7901, and HepG2 cell lines with IC50 values of 0.948, 0.983, and 3.645 mu M, respectively, while trifoliolasine E (2) exhibited moderate activities. Compound 1 was also found to dose-dependently inhibit the activity of cyclooxygenase-2 (COX-2) with an IC50 value of 29.75 mu M. To the best of our knowledge, this is the first report on the bioactivity of vakognavine-type diterpenoid alkaloids. (C) 2016 Published by Elsevier Ltd.

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