School of Chinese Medicine
Identification and evaluation of apoptotic compounds from Garcinia oligantha
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.
Bioorganic and Medicinal Chemistry Letters
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This research was supported by the National Natural Science Foundation of China (No. 21002085, 81073014 and 81173485), and Open Fund of the Key Laboratory of Ethnic Medicine Resource Chemistry (Yunnan University of Nationalities), State Ethnic Affairs Commission & Ministry of Education (No. MZY100105), start-up funds of Yunnan University of Nationalities, and Academic Research Fund (AcRF) Tier 1 grant from Minister of Education in Singapore.
Anticancer drug, Garcinia oligantha, Xanthone, Apoptosis, Caspase-3
Gao, Xue-Mei, Ting Yu, Ming-zhu Cui, Jian-Xin Pu, Xue Du, Quan-Bin Han, Qiu-fen Hu, Tian-Cheng Liu, Kathy Qian Luo, and Hong-Xi Xu. "Identification and evaluation of apoptotic compounds from Garcinia oligantha." Bioorganic and Medicinal Chemistry Letters 22.6 (2012): 2350-2353.