School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
Molecules. 2019 Jan 22;24(3):388. doi: 10.3390/molecules24030388.
Hayata is a traditional Chinese herbal medicine used to treat lung cancer, and its alkaloids, especially cepharanthine (CEP), were reported to be its effective ingredients. Therefore, the extraction of potential antitumor ingredients from the plant was of interest. We first explored the optimized solvent extraction of antitumor agents from Hayata guided by an in vitro antitumor activity assay. The solvent for extraction and its concentration, the liquid to material ratio, extraction duration, particle size, macerating time, and the frequency of extraction were investigated using a single-factor experiment. An orthogonal design (L9, 3⁴) was constructed to determine the suitable extraction conditions. The crude extract was then purified sequentially by macroporous adsorption resins (MR) for the enrichment of CEP. Under these optimal conditions, the yield of total alkaloids in the herbs was 3.4%, whereas the CEP content was 2.9%. Total alkaloids exhibited significant anti-proliferative activities in the A549 cell line. Our study provides means for the further development and use of the antitumor components from , which has potential for application in the pharmaceutical industry.
汉防己是一种传统的中草药，用于治疗肺癌，其生物碱，特别是汉防己甲素（CEP），被报道为其有效成分。因此，从植物中提取潜在的抗肿瘤成分引起了人们的兴趣。我们首先通过体外抗肿瘤活性测定指导，探索了从汉防己中优化抗肿瘤剂的溶剂提取。使用单因素实验研究了提取溶剂及其浓度、液料比、提取时间、粒径、浸渍时间和提取次数。构建正交设计（L9，3⁴）来确定合适的提取条件。然后，粗提取物通过大孔吸附树脂（MR）依次纯化，以富集 CEP。在这些最佳条件下，草药中总生物碱的收率为 3.4%，而 CEP 含量为 2.9%。总生物碱在 A549 细胞系中表现出显著的抗增殖活性。我们的研究为进一步开发和利用汉防己中的抗肿瘤成分提供了手段，有望在制药工业中得到应用。
