Anti-proliferative and apoptosis-inducible activity of Sarcodonin G from Sarcodon scabrosus in HeLa cells.
Anti-proliferative and apoptosis-inducible activity of Sarcodonin G from Sarcodon scabrosus in HeLa cells.
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DOI：
10.3892/ijo_00000142
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发表时间：
2009
影响因子：
5.2
通讯作者：
Mei Dong;Shi-ping Chen;K. Kita;Yoshinobu Ichimura;Wenzhi Guo;Sa Lu;S. Sugaya;T. Hiwasa;M. Takiguchi;N. Mori;Atsushi Kashima;K. Morimura;M. Hirota;N. Suzuki
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文献类型：
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作者：
Mei Dong;Shi-ping Chen;K. Kita;Yoshinobu Ichimura;Wenzhi Guo;Sa Lu;S. Sugaya;T. Hiwasa;M. Takiguchi;N. Mori;Atsushi Kashima;K. Morimura;M. Hirota;N. Suzuki
目前正在寻找植物来源的二萜，特别是具有抗炎活性的二萜，其对人类癌细胞也具有抗增殖作用。从蘑菇Sarcodon scabrosus中分离的一种杯烷型二萜Sarcodonin G（SG）已被报道具有抗炎活性，在测试的4种杯烷型二萜中最大程度地抑制了HeLa细胞的增殖。SG显示出20 μ M的IC 50（50%抑制浓度），在用化学品培养细胞后2天通过MTT测定法估计。HeLa细胞的SG处理导致剂量依赖性的凋亡事件的产生，例如DNA梯状化（<或=100 μ M）。此外，SG处理的HeLa细胞显示caspase-3和caspase-9的激活和Bax/Bcl-2比值的增加，通过Western blot分析。半胱天冬酶抑制剂Z-VAD-FMK可减弱SG处理对HeLa细胞的抗增殖作用。SG还显示出对其他5种人类癌细胞系的抗增殖作用，IC 50值为20-40 μ M。由于这些抗增殖作用，通过可能的半胱天冬酶激活，SG有望成为一种新的抗增殖剂值得进一步研究。
There is an ongoing search for plant-derived diterpenes, especially for diterpenes with anti-inflammatory activity that also have anti-proliferative effects on human cancer cells. A cyathane-type diterpene, Sarcodonin G (SG), isolated from the mushroom Sarcodon scabrosus and already reported to have anti-inflammatory activity, inhibited proliferation of HeLa cells to the greatest extent among 4 cyathane diterpenes tested. SG showed an IC50 (50% inhibition concentration) of 20 microM, estimated by MTT assay 2 days after culture of cells with the chemical. SG treatment of HeLa cells resulted in dose-dependent generation of apoptotic events such as DNA-laddering (< or =100 microM). Moreover, SG-treated HeLa cells showed activation of caspase-3 and caspase-9 and increase of Bax/Bcl-2 ratios, as analyzed by Western blot analysis. The anti-proliferative effects of SG treatment on HeLa cells were lessened by a caspase inhibitor, Z-VAD-FMK. SG also showed anti-proliferative effects toward 5 other human cancer cell lines with IC50 values of 20-40 microM. Because of these anti-proliferative effects via possible caspase activation, SG holds promise of being a novel anti-proliferative agent deserving further investigation.