Li Simeng, Chou Guixin, Hseu Youcheng, Yang Hsinling, Kwan Hiuyee, Yu Zhiling
The MOE Key Laboratory for Standardization of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Cai Lun Road 1200, Zhangjiang Hi-Tech Park, Shanghai 201210, PR China.
Chem Cent J. 2013 Sep 23;7(1):159. doi: 10.1186/1752-153X-7-159.
Flos Genkwa (yuanhua in Chinese), the dried flower buds of Daphne genkwa Sieb.et Zucc. (Thymelaeaceae), is a traditional Chinese medicinal herb mainly used for diuretic, antitussive, expectorant, and anticancer effects. However, systematic and comprehensive studies on Flos Genkwa and its bioactivity are limited.
After confirmation of the anti-tumor activity, the 95% ethanolic extract was subjected to successive solvent partitioning to petroleum ether, dichloromethane, n-butanol, and water soluble fractions. Each fraction was tested using the same biological activity model, and the dichloromethane fraction had the highest activity. The dichloromethane fraction was subjected to further chromatographic separation for the isolation of compounds 1-13. Among the 13 compounds, the diterpene esters (compounds 10-13) showed anticancer activity, whereas the flavonoids, lignanoids, and peptides showed moderate activity. Compound 13 was a new daphnane diterpenoid, which was named genkwanin VIII.The preliminary antitumor mechanism of yuanhuacine was studied by protein expression and cell cycle analysis in MCF-7 cancer cells.
The present investigation tends to support the traditional use of Flos Genkwa for treating cancer. Through bioassay-guided fractionation and isolation techniques, the CH2Cl2 fraction was determined as the active fraction of the flower buds of D. genkwa, and the anti-tumor activity was ascribable to the compounds 10-13.
芫花为瑞香科植物芫花Daphne genkwa Sieb.et Zucc.的干燥花蕾，是一种传统的中药材，主要用于利尿、止咳、祛痰及抗癌。然而，关于芫花及其生物活性的系统全面研究较为有限。
在确认其抗肿瘤活性后，将95%乙醇提取物依次用石油醚、二氯甲烷、正丁醇和水溶性部分进行溶剂分配。每个部分都使用相同的生物活性模型进行测试，二氯甲烷部分活性最高。对二氯甲烷部分进行进一步色谱分离以分离化合物1 - 13。在这13种化合物中，二萜酯（化合物10 - 13）显示出抗癌活性，而黄酮类、木脂素类和肽类显示出中等活性。化合物13是一种新的瑞香烷二萜，命名为芫花素VIII。通过对MCF - 7癌细胞的蛋白质表达和细胞周期分析研究了芫花酯甲的初步抗肿瘤机制。
本研究倾向于支持芫花治疗癌症的传统用途。通过生物活性导向的分离和纯化技术，确定二氯甲烷部分为芫花花蕾的活性部分，其抗肿瘤活性归因于化合物10 - 13。
