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目的:研究夏枯草的化学成分及其体外抗肿瘤活性。方法:运用硅胶,十八烷基硅烷键合硅胶填料(ODS),羟丙基葡聚糖凝胶(Sephadex LH-20)等色谱方法,对夏枯草经甲醇超声提取物进行分离纯化,根据理化性质,1H-NMR和13C-NMR,并参考文献综合解析化合物结构。通过噻唑蓝(MTT)法,分别设置空白组,阳性药物组(不同浓度顺铂),不同浓度试验药物组;对化合物抗乳腺癌细胞MCF-7,MDA-MB-231以及对正常乳腺细胞MCF-10A的活性进行筛选。结果:从夏枯草中分离鉴定了11个化合物,分别为反式-异迷迭香酸葡萄糖苷(1),反式-迷迭香酸葡萄糖苷甲酯(2),迷迭香酸(3),迷迭香酸甲酯(4),咖啡酸-3-葡萄糖苷(5),丹参素(6),丹参素甲酯(7),3,4-二羟基苯甲醛(8),(3R,5S,6S,7E,9R)-megastigman-7-ene-3,5,6,9-tetrol 9-O-β-D-glucopy-ranoside(9),(-)-syringaresinol-4-O-13-D-glucopyranoside(10),16-氧-17-去甲基-3β,24-二羟基齐墩果-12-烯-3-O-β-D-葡糖醛酸苷(11);化合物4对各细胞的抑制率达88%以上,化合物2,8同时对MCF-7和MCF-10A的抑制率达60%以上,化合物3仅对MCF-7的抑制活性达60%以上。结论:化合物9,10为首次从夏枯草中分离得到。体外抗肿瘤活性筛选表明,化合物2~4,8对乳腺癌细胞MCF-7有明显抑制作用,化合物4对乳腺癌细胞MDA-MB-231有较强的抑制作用;但化合物2,4,8同时对正常乳腺细胞也有明显抑制作用;而化合物3能选择性的抑制肿瘤细胞。
Objective: To study the chemical constituents of Prunella vulgaris and its anti-tumor activity in vitro. Methods: Ultrasonic extracts of Prunella vulgaris were separated and purified by silica gel, octadecylsilane bonded silica gel packing (ODS) and Sephadex LH-20, Nature, 1H-NMR and 13C-NMR, and the reference structure of a comprehensive analysis of compounds. The MTT method was used to set up the blank group, the positive drug group (different concentrations of cisplatin) and the test drug group with different concentrations. The anti-MCF-7, MDA-MB-231 and normal MCF -10A activity screening. Results: Eleven compounds were isolated and identified from Prunella vulgaris L., which were trans-isorhamnoglucoside (1), trans-rosmarinic acid glucoside methyl ester (2), rosmarinic acid (4), caffeic-3-glucoside (5), danshensu (6), danshensu methyl ester (7), 3,4- dihydroxybenzaldehyde (8), 3R, 5S, 6S, 7E, 9R) -megastigman-7-ene-3,5,6,9-tetrol 9-O-β- D-glucopyranoside (9), (-) - syringaresinol-4-O -13-D-glucopyranoside (10), 16-oxo-17-normethyl-3β, 24- dihydroxyolean- 12-ene-3-O-β-D-glucuronide (11) The inhibitory rate of compound 4 to all the cells was more than 88%. The inhibitory rate of compound 2 and 8 to MCF-7 and MCF-10A was more than 60% and that of compound 3 to MCF-7 was more than 60%. Conclusion: Compounds 9 and 10 were isolated from Prunella vulgaris for the first time. In vitro antitumor activity screening showed that compound 2 ~ 4,8 had a significant inhibitory effect on breast cancer cell MCF-7, while compound 4 had a stronger inhibitory effect on breast cancer cell MDA-MB-231; however, compounds 2, 4, At the same time on normal breast cells also have significant inhibitory effect; and compound 3 can selectively inhibit tumor cells.