基于谱效关系分析的 Melastoma dodecandrum Lour 活性成分及其对人宫颈癌细胞的抑制作用研究

Song Qian, Zuhua Wang, Xiuping Ma, Huiyi Ming, Jing Liu, Jing Yang, Teng Chen, Linli Liu, Jibian Ban, Jiangtao Guo
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摘要

民族药物 Melastoma dodecandrum Lour.(MDL)是一种重要的药用植物,具有潜在的抗肿瘤作用,已被提出作为有前途的抗癌药物,但其治疗作用的物质基础尚不清楚,缺乏深入研究。本研究采用 CCK-8 法研究了不同 MDL 提取物对不同妇科肿瘤细胞的体外抗肿瘤作用。采用UPLC法测定和比较了从不同产品领域和市场采集的21批次MDL样品的有效成分。在此基础上,利用指纹图谱相似性软件对数据进行处理,并采用多元统计方法进一步分析了MDL指纹图谱与抗人宫颈癌活性之间的相关性。结果表明,MDL的水提取物、粗多糖、总多酚、水提取物的乙酸乙酯馏分和50%乙醇提取物等5种提取物对人宫颈癌HeLa细胞和SiHa细胞均有抑制作用,其中MDL的总多酚对人宫颈癌细胞有较强的抑制作用。此外,MDL 总多酚的指纹图谱有 16 个共同峰,利用二极管阵列和紫外光谱检测了 6 个共同峰,其中第 1 峰(没食子酸)、第 4 峰(原儿茶酸)、第 12 峰(未知)和第 15 峰(鞣花酸)与 SiHa 细胞的 IC50 值呈负相关,且所有变量重要度值均大于 1。结果表明,MDL抑制人宫颈癌SiHa细胞的主要活性成分可能是没食子酸、原儿茶酸和鞣花酸的协同作用,进一步的谱效关系分析为MDL的质量控制和抗宫颈癌新药的开发提供了重要的参考和依据。
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Study on the Active Components and Inhibiting Effect of Melastoma dodecandrum Lour. on Human Cervical Cancer Cells Based on Spectrum–Effect Relationship Analysis
The ethnic drug Melastoma dodecandrum Lour. (MDL) is an important medicinal plant with potential antitumor properties, which have been proposed as promising anticancer agents, but the material basis for its therapeutic effect is still unclear and lacks in-depth research. In this study, the in vitro antitumor effects of different MDL extracts in different gynecological tumor cells were investigated by CCK-8 assay. The active components of 21 batches of MDL samples collected from different product areas and markets were determined and compared by the UPLC method. On this basis, the data was processed with the fingerprint similarity software, and the correlation between MDL fingerprint and antihuman cervical cancer activity was further analyzed by a multivariate statistical method. Five kinds of MDL extracts, including the aqueous extract, the crude polysaccharide, the total polyphenol, the ethyl acetate fraction of the aqueous extract and 50% ethanol extract, had inhibitory effects on human cervical cancer HeLa and SiHa cells, among which total polyphenols of MDL showed stronger inhibition effect on human cervical cancer cells. In addition, the fingerprint of the total polyphenols of MDL had sixteen common peaks, and six common peaks were checked by using diode array and UV spectra, among which peak 1 (gallic acid), peak 4 (protocatechuic acid), peak 12 (unknown), and peak 15 (ellagic acid) were negatively correlated with the IC50 value of the SiHa cells, and all variable importance values were greater than 1. Our data demonstrated that the main active components of MDL inhibiting human cervical cancer SiHa cells may be the synergistic effect of gallic acid, protocatechuic acid and ellagic acid, and the further spectrum-effect relationship analysis provides an important reference and basis for the quality control and the development of new anticervical cancer drug of MDL.
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