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KMID : 0043320120350010019
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Archives of Pharmacal Research
2012 Volume.35 No. 1 p.19 ~ p.26
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Cytotoxic oleane-type triterpene saponins from Glochidion eriocarpum
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Nhiem Nguyen Xuan
Thu Vu Kim
Kiem Phan Van
Minh Chau Van
Tai Bui Huu
Quang Tran Hong
Cuong Nguyen Xuan
Yen Pham Hai
Boo Hye-Jin
Kang Jung-Il
Kang Hee-Kyoung
Kim Young-Ho
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Abstract
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The anticancer activity of ten compounds from the aerial parts of Glochidion eriocarpum were evaluated on two human cancer cell lines, HL-60 and HCT-116. Compounds 1?4 displayed highly potent cytotoxic activity on the HCT-116 cancer cell line with IC50 values ranging of 0.41∼1.16 μM. Compounds 1?4 significantly inhibited the HL-60 cell line with IC50 values ranging of 4.51∼6.33 μM. These results suggested that the benzoyl group at the C-22 position in oleane-type triterpene saponins was essential for cytotoxicity towards tumor cells. Moreover, compounds 2 and 3 showed more potent cytotoxicity than compounds 1 and 4 against HL-60 and HCT-116 cells. With respect to the mechanism underlying cytotoxicity, compounds 1?4 increased chromatin condensation, a typical apoptotic characteristic in HL-60 and HCT-116 cells. In the mechanism of apoptosis induction, compounds 1?4 reduced Bcl-2 expression, whereas the expression of Bax was increased compared to controls in HCT-116 cells. In addition, compounds 1?4 decreased the level of procaspase-3. The cleavage of poly (ADP-ribose) polymerase (PARP), a vital substrate of effector caspase, was observed in HCT-116 cells. Furthermore, the induction of apoptosis was also accompanied by an activation of extracellular signal-regulated kinase (ERK) and p38 kinase in HCT-116 cells. These findings provide evidence demonstrating that the pro-apoptotic effects of compounds 1?4 are mediated through the activation of ERK and p38 in HCT-116 cells.
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KEYWORD
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Glochidion eriocarpum, Euphorbiaceae, Triterpenoid saponin, Glochierioside, Cytotoxic activity, Apoptosis
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