Zhu Rui-Jing, Shen Xiao-Ling, Dai Ling-Lin, Ai Xiang-Ying, Tian Ru-Hua, Tang Rong, Hu Ying-Jie
Laboratory of Chinese Herbal Drug Discovery, Tropical Medicine Institute, Guangzhou University of Chinese Medicine, Guangzhou 510405, China.
Molecules. 2014 Sep 5;19(9):13965-75. doi: 10.3390/molecules190913965.
Marsdeniae tenacissimae Caulis (MTC) is a Chinese herbal medicine used mainly for treatment of cancer, whose pharmacologically active constituents responsible for its in vivo activity and clinical efficacy have not been clearly elucidated. In this study, total aglycones of MTC (ETA) showed the ability to sensitize KB-3-1, HeLa, HepG2 and K562 cells to paclitaxel treatment. More inspiringly, ETA markedly enhanced the antitumor activity of paclitaxel in nude mice bearing HeLa or KB-3-1 xenografts. Compared to treatment with paclitaxel alone, treatment with combination of paclitaxel and ETA achieved significant reduction in volume and weight of HeLa tumors (p<0.05), and remarkable inhibition to the growth of KB-3-1 tumors (p<10⁻⁶). ETA was characterized by the presence of a group of tenacigenin B ester derivatives, among which four reference compounds, 11α-O-tigloyl-12β-O-acetyltenacigenin B, 11α,12β-di-O-tigloyltenacigenin B, 11α-O-2-methylbutanoyl-12β-O-tigloyltenacigenin B, and 11α-O-(2-methylbutanoyl)-12β-O-benzoyltenacigenin B, accounted for 42.14% of the total peak area of 19 detectable components assayed by HPLC. Our study has identified ETA as a promising sensitizer for cancer chemotherapy.
通关藤茎（MTC）是一种主要用于治疗癌症的中药材，其体内活性和临床疗效的药理活性成分尚未明确阐明。在本研究中，MTC的总苷元（ETA）显示出使KB - 3 - 1、HeLa、HepG2和K562细胞对紫杉醇治疗敏感的能力。更令人鼓舞的是，ETA显著增强了紫杉醇在携带HeLa或KB - 3 - 1异种移植瘤的裸鼠中的抗肿瘤活性。与单独使用紫杉醇治疗相比，紫杉醇与ETA联合治疗使HeLa肿瘤的体积和重量显著减小（p<0.05），并对KB - 3 - 1肿瘤的生长有显著抑制作用（p<10⁻⁶）。ETA的特征是含有一组通关藤苷元B酯衍生物，其中四种对照化合物，11α - O - 惕各酰基 - 12β - O - 乙酰通关藤苷元B、11α,12β - 二 - O - 惕各酰基通关藤苷元B、11α - O - 2 - 甲基丁酰基 - 12β - O - 惕各酰基通关藤苷元B和11α - O -（2 - 甲基丁酰基）- 12β - O - 苯甲酰基通关藤苷元B，占通过高效液相色谱法测定的19种可检测成分总峰面积的42.14%。我们的研究已确定ETA是一种有前景的癌症化疗增敏剂。
