Liu L J, Liu J N
Department of Pharmaceutical Engineering, Heilongjiang University, Key Laboratory of Chemical Engineering Process and Technology for High-efficiency Conversion, College of Heilongjiang Province, Harbin, 150080, China.
Indian J Pharm Sci. 2016 Jan-Feb;78(1):143-50. doi: 10.4103/0250-474x.180257.
The rhizome of Menispermum dauricum DC known as a traditional Chinese medicine, with high content of alkaloids, has been found to possess antitumor activity. In this research, an attempt to correlate fingerprinting with bioactivity was made for quality control of M. dauricum. Firstly, the cytotoxicity of extracts from ten batches of samples against human breast MCF-7 cancer cells was estimated by [3-(4, 5-dimethylthiazole-2-yl)-2, 5-diphenyltetrazoliumbromide] assay. Then, cytotoxic activity-integrated fingerprints were established by high performance liquid chromatography. Eight peaks were selected as the common peaks to evaluate the similarities of samples and hierarchical clustering analysis was used to identify and classify different samples into groups. Assays for determinations of total alkaloids and dauricine contents enabled cytotoxicity coefficient of each extract. The potential usefulness of employing cytotoxicity coefficient was investigated by a combination of Pearson correlation coefficients and multiple linear regression analysis as being the reliable parameter to evaluate the herbal extracts. The results indicated that the level of dauricine (peak 8 in the fingerprint) correlated closely with cytotoxicity and played a significant role in the cytotoxicity of Bei Dou-Gen and could be related to its antitumor properties. It is proposed that the cytotoxicity coefficient value with a cytotoxic activity-integrated fingerprint of key biomarkers (dauricine) may be useful indicators to adopt for the quality control of M. dauricum. The analysis of cytotoxic-activity-integrated fingerprint could correlate fingerprinting with bioactivities and would provide a reasonable strategy for quality control of complex mixture of herbal medicines.
蝙蝠葛根茎作为一种传统中药，生物碱含量高，已被发现具有抗肿瘤活性。本研究尝试将指纹图谱与生物活性相关联，用于蝙蝠葛的质量控制。首先，采用[3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐]法评估十批样品提取物对人乳腺癌MCF-7癌细胞的细胞毒性。然后，通过高效液相色谱法建立细胞毒性活性整合指纹图谱。选择八个峰作为共有峰来评估样品的相似度，并采用层次聚类分析对不同样品进行识别和分组。测定总生物碱和蝙蝠葛碱含量的方法可得出各提取物的细胞毒性系数。通过皮尔逊相关系数和多元线性回归分析相结合的方法研究了使用细胞毒性系数作为评估草药提取物可靠参数的潜在实用性。结果表明，蝙蝠葛碱（指纹图谱中的峰8）水平与细胞毒性密切相关，在北豆根的细胞毒性中起重要作用，可能与其抗肿瘤特性有关。建议将关键生物标志物（蝙蝠葛碱）的细胞毒性活性整合指纹图谱的细胞毒性系数值作为蝙蝠葛质量控制的有用指标。细胞毒性活性整合指纹图谱分析可将指纹图谱与生物活性相关联，为复杂草药混合物的质量控制提供合理策略。
