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首页> 美国卫生研究院文献>Evidence-based Complementary and Alternative Medicine : eCAM >Anticancer Effects of Sinocrassulosides VI/VII from Silene viscidula on HeLa Cells
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Anticancer Effects of Sinocrassulosides VI/VII from Silene viscidula on HeLa Cells

机译：粘黏层中华cra子VI / VII对HeLa细胞的抗癌作用

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Natural products are becoming increasingly important in chemoprevention and for cancer therapy. Silene viscidula (S. viscidula), a traditional Chinese herb, has long been used as an anti-inflammatory and neuroleptic agent. However, the anticancer activity of S. viscidula has remained unclear. In this study, 16 compounds were extracted from S. viscidula. Among those compounds, sinocrassulosides VI/VII, an inseparable isomer mixture, possess the strongest inhibitory activity on HeLa cells with the IC50 value of 2.37 μM. Mechanism studies found that sinocrassulosides VI/VII downregulated the expression of cyclin D1 and decreased retinoblastoma (Rb) phosphorylation, which arrested HeLa cells in the G1 phase. Also, sinocrassulosides VI/VII could induce senescence via the upregulation of p16 and a significant increase of β-galactosidase (β-gal) staining. Our results suggest that sinocrassulosides VI/VII may be a new therapeutic potential agent for cervical cancer. In addition, we explored the structure-activity relationships of three groups of the configurational isomer with similar chemical structure from S. viscidula. We first demonstrated that the length of the ester chains linked to the carboxyl group of the glucuronic acid residue could affect the potent cytotoxicity. This finding will open new avenues for developing effective anticancer compounds by modifying the components derived from plants in nature.
机译：天然产物在化学预防和癌症治疗中变得越来越重要。 Silene viscidula（S. viscidula）是一种传统中草药，长期以来一直用作抗炎和抗精神病药。但是，粘链链球菌的抗癌活性仍不清楚。在这项研究中，从粘链葡萄球菌中提取了16种化合物。在这些化合物中，芥子油苷VI / VII是一种不可分离的异构体混合物，对HeLa细胞具有最强的抑制活性，IC50值为2.37μM。机制研究发现，sinocrassulosides VI / VII下调了细胞周期蛋白D1的表达，并降低了视网膜母细胞瘤（Rb）磷酸化，从而使HeLa细胞停滞在G1期。此外，中华oc糖苷VI / VII可能通过上调p16和显着增加β-半乳糖苷酶（β-gal）染色来诱导衰老。我们的结果表明，中华sin子VI / VII可能是宫颈癌的一种新的潜在治疗剂。此外，我们探索了三组具有相似化学结构的构象异构体的构效关系。我们首先证明，与葡萄糖醛酸残基的羧基连接的酯链的长度可能会影响有效的细胞毒性。这一发现将通过修饰自然界中植物衍生的成分，为开发有效的抗癌化合物开辟新途径。

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