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Title: Identification and evaluation of apoptotic compounds from Garcinia Oligantha
Authors: Han, Quan-Bin
Gao, Xue-Mei
Yu, Ting
Cui, Ming-Zhu
Pu, Jian-Xin
Du, Xue
Hu, Qiu-Fen
Liu, Tian-Cheng
Luo, Kathy Qian
Xu, Hong-Xi
Issue Date: 2012
Source: Gao, X. M., Yu, T., Cui, M. z., Pu, J. X., Du, X., Han, Q. b., Hu, Q. f., Liu, T. C., Luo, K. Q.,& Xu, H. X. (2012). Identification and evaluation of apoptotic compounds from Garcinia oligantha. Bioorganic & Medicinal Chemistry Letters, 22(6), 2350-2353.
Series/Report no.: Bioorganic & medicinal chemistry letters
Abstract: Four new compounds, oliganthins A–D (1–4), and one known caged xanthone gaudichaudione H (5) were isolated from the stems of Garcinia oligantha. The structures of the new compounds were elucidated by spectroscopic evidences. All of the five compounds were evaluated for their apoptosis-inducing effects using HeLa-C3 cells which have been genetically engineered to produce a fluorescent biosensor capable of detecting caspase-3 activation. All of them induced cell apoptosis at 10 μM or lower concentrations. The apoptotic activity of oliganthins A, B and gaudichaudione H were further confirmed by detecting the cleavage of PARP, which is the substrate of activated caspase-3, in these compounds-treated cells using the method of Western blot. Moreover, the values of IC50 were measured for all five compounds on HeLa cells using the MTT assay. Among them, gaudichaudione H had the lowest IC50 value of 0.90 μM, while the other four new compounds had IC50 values of 1.58, 1.52, 4.15, and 7.82 μM, respectively. These results show that gaudichaudione H has the strongest apoptosis-inducing effect and cell growth inhibition effect among these xanthones and it may have the potential to be developed into a new anticancer agent.
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2012.01.068
Fulltext Permission: none
Fulltext Availability: No Fulltext
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