Kudsuphilactone B，一种从五味子果实中分离的去甲三萜，诱导人卵巢癌 A2780 细胞的半胱天冬酶依赖性细胞凋亡,Archives of Pharmacal Research

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Kudsuphilactone B，一种从五味子果实中分离的去甲三萜，诱导人卵巢癌 A2780 细胞的半胱天冬酶依赖性细胞凋亡
Archives of Pharmacal Research ( IF 6.9 ) Pub Date : 2017-02-22 , DOI: 10.1007/s12272-017-0902-5
Miran Jeong ₁ , Hye Mi Kim ₂ , Hyun Ji Kim ₃ , Jung-Hye Choi ₁ , Dae Sik Jang _{1,

2}

Affiliation

对五味子果实的植物化学研究导致了 19 种化合物的分离和表征。分离物的结构被确定为五味子甲素、脱氧五味子甲素、当归苷H、gomisin A、gomisin J、(-)-gomisin L1、(-)-gomisin L2、五味子素C、gomisin N、内消旋二氢愈创木酸、kadsuphilactone B、 α-ylangenol、α-ylangenyl acetate、β-chamigrenal、β-chamigrenic酸、4-羟基苯甲酸、原儿茶酸、p-甲基香芹酚和吲哚-3-乙酸。其中，一些木脂素和去甲三萜在人卵巢和子宫内膜癌细胞中显示出细胞毒活性。特别是，去甲三萜 kadsuphilactone B 在 A2780 和 Ishikawa 细胞中表现出显着的细胞毒活性，IC50 值低于 25 μM。Kadsuphilactone B 诱导细胞凋亡并刺激 caspase-3、-8 和 -9 的活化以及聚（ADP-核糖）聚合酶的裂解。Caspase 抑制剂减弱了 kudsuphilactone B 的促凋亡活性。此外，kadsuphilactone B 改变了 B 细胞淋巴瘤 2 (Bcl-2) 家族蛋白的表达水平。此外，MAPK 的激活受 kadsuphilactone B 以剂量依赖性方式调节。总之，这些结果表明，kadsuphilactone B 通过调节 Bcl-2 家族蛋白和 MAPK 信号传导诱导人癌细胞中的半胱天冬酶依赖性细胞凋亡。kadsuphilactone B 改变了 B 细胞淋巴瘤 2 (Bcl-2) 家族蛋白的表达水平。此外，MAPK 的激活受 kadsuphilactone B 以剂量依赖性方式调节。总之，这些结果表明，kadsuphilactone B 通过调节 Bcl-2 家族蛋白和 MAPK 信号传导诱导人癌细胞中的半胱天冬酶依赖性细胞凋亡。kadsuphilactone B 改变了 B 细胞淋巴瘤 2 (Bcl-2) 家族蛋白的表达水平。此外，MAPK 的激活受 kadsuphilactone B 以剂量依赖性方式调节。总之，这些结果表明，kadsuphilactone B 通过调节 Bcl-2 家族蛋白和 MAPK 信号传导诱导人癌细胞中的半胱天冬酶依赖性细胞凋亡。

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Kudsuphilactone B, a nortriterpenoid isolated from Schisandra chinensis fruit, induces caspase-dependent apoptosis in human ovarian cancer A2780 cells

A phytochemical study on the fruits of Schisandra chinensis led to the isolation and characterization of nineteen compounds. The structures of the isolates were determined to be schizandrin, deoxyschizandrin, angeloylgomisin H, gomisin A, gomisin J, (−)-gomisin L1, (−)-gomisin L2, wuweizisu C, gomisin N, meso-dihydroguaiaretic acid, kadsuphilactone B, α-ylangenol, α-ylangenyl acetate, β-chamigrenal, β-chamigrenic acid, 4-hydroxybenzoic acid, protocatechuic acid, p-methylcarvacrol, and indole-3-acetic acid. Of these, some lignans and a nortriterpene showed cytotoxic activity in human ovarian and endometrial cancer cells. In particular, a nortriterpenoid kadsuphilactone B exhibited significant cytotoxic activity with IC50 values below 25 μM in both A2780 and Ishikawa cells. Kadsuphilactone B induced apoptotic cell death and stimulated the activation of caspase-3, -8, and -9 and the cleavages of poly (ADP-ribose) polymerase. Caspase inhibitors attenuated the pro-apoptotic activity of kudsuphilactone B. In addition, kadsuphilactone B altered the expression levels of B cell lymphoma 2 (Bcl-2) family proteins. Moreover, activation of MAPKs was modulated by kadsuphilactone B in a dose-dependent manner. Taken together, these results show that kadsuphilactone B induces caspase-dependent apoptosis in human cancer cells via the regulation of Bcl-2 family protein and MAPK signaling.

更新日期：2017-02-22

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