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来自越南巴豆的具有细胞毒性的贝壳杉烷二萜类化合物的对称二聚体。

Symmetric dimers of ent-kaurane diterpenoids with cytotoxic activity from Croton tonkinensis.

机构信息

Vietnam National Institute of Medicinal Materials, 3B Quangtrung, Hoankiem, Hanoi, Viet Nam.

出版信息

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1122-4. doi: 10.1016/j.bmcl.2011.11.116. Epub 2011 Dec 6.

Abstract

Breast cancer is the most common malignant tumor in women these days accounting for approximately 24% of all cancer. During our screening program searching for cytotoxic materials from natural products, two new symmetric dimers of ent-kaurane diterpenoid, crotonkinensins C (1) and D (2), with connectivity at C-17 were isolated from the leaves of the Vietnamese endemic medicinal plant Croton tonkinensis. Their structures were determined on the basis of physicochemical and spectroscopic data. Compound 2 showed a potent cytotoxic activity against MCF-7, tamoxifen-resistant MCF-7 (MCF-7/TAMR), adriamycin-resistant MCF-7 (MCF-7/ADR), and MDA-MB-231 breast cancer cell lines.

摘要

如今,乳腺癌是女性最常见的恶性肿瘤,约占所有癌症的 24%。在我们的天然产物细胞毒性物质筛选计划中,从越南特有药用植物大藤Croton tonkinensis 的叶子中分离得到了两个新的贝壳杉烷二萜对称二聚体,即克罗通宁 C(1)和 D(2),它们在 C-17 处相连。根据理化和光谱数据确定了它们的结构。化合物 2 对 MCF-7、他莫昔芬耐药 MCF-7(MCF-7/TAMR)、阿霉素耐药 MCF-7(MCF-7/ADR)和 MDA-MB-231 乳腺癌细胞系表现出很强的细胞毒性活性。

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