采用生物活性导向分离法从王瓜中分离抗癌成分。
Isolation of anticancer constituents from Cucumis prophetarum var. prophetarum through bioassay-guided fractionation.
机构信息
Department of Pharmacognosy, College of Pharmacy, King Khalid University, Abha, Saudi Arabia.
Kalexsyn, 4502 Campus Drive, Kalamazoo, MI, 49008, USA.
出版信息
BMC Complement Altern Med. 2018 Oct 9;18(1):274. doi: 10.1186/s12906-018-2295-5.
BACKGROUND
Cucumis prophetarum var. prophetarum is used in Saudi folk medicine for treating liver disorders and grows widely between Abha and Khamis Mushait City, Saudi Arabia.
METHODS
Bioassay-guided fractionation and purification were used to isolate the main active constituents of Cucumis prophetarum var. prophetarum fruits. These compounds were structurally elucidated using NMR spectroscopy, mass spectral analyses and x-ray crystallography. All fractions, sub-fractions and pure compounds were screened for their anticancer activity against six cancer cell lines.
RESULTS
The greatest cytotoxic activity was found to be in the ethyl acetate fraction, resulting in the isolation of five cucurbitacin compounds [E, B, D, F-25 acetate and Hexanorcucurbitacin D]. Among the cucurbitacins that were isolated and tested cucurbitacin B and E showed potent cytotoxicity activities against all six human cancer cell lines.
CONCLUSION
Human breast cancer cell lines were found to be the most sensitive to cucurbitacins. Preliminary structure activity relationship (SAR) for cytotoxic activity of Cucurbitacins against human breast cancer cell line MDA-MB-231 has been reported.
背景
在沙特阿拉伯，宁夏枸杞被用于治疗肝脏疾病，在阿巴哈和哈米斯·穆沙伊特市之间广泛生长。
方法
生物测定指导的分离和纯化用于分离宁夏枸杞果实的主要活性成分。这些化合物的结构通过 NMR 光谱、质谱分析和 X 射线晶体学进行阐明。所有的馏分、亚馏分和纯化合物都对其对六种癌细胞系的抗癌活性进行了筛选。
结果
发现乙酸乙酯部分具有最大的细胞毒性活性，导致分离出五种葫芦素化合物[E、B、D、F-25 乙酸酯和六氢诺葫芦素 D]。在所分离和测试的葫芦素中，葫芦素 B 和 E 对所有六种人癌细胞系均表现出很强的细胞毒性活性。
结论
发现人乳腺癌细胞系对葫芦素最为敏感。报道了初步的结构活性关系（SAR），用于葫芦素对人乳腺癌细胞系 MDA-MB-231 的细胞毒性活性。
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