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Cytotoxic clerodane diterpenoids from Croton crassifolius.

Authors :: Tian JL
Yao GD
Wang YX
Gao PY
Wang D
Li LZ
Lin B
Huang XX
Song SJ
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Mar 01; Vol. 27 (5), pp. 1237-1242. Date of Electronic Publication: 2017 Jan 20.
Publication Year :: 2017
Abstract: Hepatocellular carcinoma (HCC) is the most common type of liver cancer, and treatment options for HCC are limited. In addition, the discovery of new natural compounds with anti-hepatocarcinoma activity is attracting increasing attention. For this reason, phytochemical investigation of Croton crassifolius led to the isolation of 17 diterpenoids, including three new clerodane diterpenoids, named crassifolius A-C (1-3), along with 14 known ones (4-17). Their structures were established by 1D, 2D NMR, HR-ESI-MS, detailed calculated electronic circular dichroism (ECD) spectra and the assistance of quantum chemical predictions (QCP) of <superscript>13</superscript> C NMR chemical shifts. The cytotoxicities of all these compounds against human liver cancer lines (HepG2 and Hep3B) were determined. Among them, compound 1 exhibited good cytotoxicity with IC <subscript>50</subscript> value of 17.91μM against human liver tumor cells Hep3B. Following further studies of the anti-tumor mechanism of compound 1-induced cell growth inhibition, we found that compound 1 caused apoptotic cell death in Hep3B cells by detecting morphologic changes and Western blotting analysis.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)