Chang Eun Ju, Lee Won Jung, Cho Sung Hee, Choi Sang Won
Department of Food Science and Nutrition, Catholic University of Daegu, Hayang, Gyeongbuk 712-702, Korea.
Arch Pharm Res. 2003 Aug;26(8):620-30. doi: 10.1007/BF02976711.
The proliferative effects of thirty Oriental medicinal herbs on MCF-7 (estrogen-sensitive breast cancer cell line) and ROS 17/2.8 osteoblast-like cells were determined using the MTT assay. Methanol extracts from several herbs was found to show proliferative activity on the above two cell lines in the range of 5 to 100 microg/mL. Among these active herbs, the methanol extract from the rhizomes of Drynaria fortunei showed the most potent proliferative activity, and the cell proliferations were significantly increase by 136 and 158% in the MCF-7 and ROS 17/2.8 cells, respectively, when treated with 100 microg/mL. Through a bioassay-guided separation, eight flavonoids, including four new flavan-3-ols and two propelargonidins, together with the known (-)-epiafzelechin and naringin, were isolated. Their chemical structures were characterized as (-)-epiafzelechin (1), (-)-epiafzelechin-3-O-beta-D-allopyranoside (2), (-)-epiafzelechin-3-O-(6"-O-acetyl)-beta-D-allopyranoside (3), 4beta-carboxymethyl-(-)-epiafzelechin methyl ester (4), 4beta-carboxymethyl-(-)-epiafzelechin sodium salt (5), naringin (6), (-)-epiafzelechin-(4beta-->8)-4beta-carboxymethylepiafzelechin methyl ester (7) and (-)epiafzelechin-(4beta-->8, 2beta-->O-->7)-epiafzelechin-(4beta-->8)-epiafzelechin (8) by extensive 1D and 2D NMR spectroscopy. Most of these flavonoids, in the range of 10(-15) to approximately 10(-6) M, accelerated the proliferation of MCF-7 cell, with compounds 7 and 8, in the range of 10(-15) to approximately 10(-12) M, showing especially potent proliferation effects. Meanwhile, seven flavonoids, with the exception of compound 4, stimulated the proliferation of ROS 17/2.8 cells in the range of 10(-15) to approximately 10(-6) M, with compounds 5-8 especially accelerating the proliferation, in dose-dependent manners (10(-15) to approximately 10(-9) M), and their proliferative effect was much stronger than that of E2 and genistein. These results suggest that propelargonidin dimers and trimers isolated from the rhizomes of Drynaria fortunei may be useful as potential phytoestrogens, which play important physiological roles in the prevention of postmenopausal osteoporosis.
采用MTT法测定了30种东方药草对MCF-7（雌激素敏感乳腺癌细胞系）和ROS 17/2.8成骨样细胞的增殖作用。发现几种药草的甲醇提取物对上述两种细胞系在5至100μg/mL范围内显示出增殖活性。在这些活性药草中，骨碎补根茎的甲醇提取物显示出最强的增殖活性，当用100μg/mL处理时，MCF-7和ROS 17/2.8细胞中的细胞增殖分别显著增加136%和158%。通过生物活性导向分离，分离出8种黄酮类化合物，包括4种新的黄烷-3-醇和2种原花青定，以及已知的（-）-表阿夫儿茶素和柚皮苷。通过广泛的一维和二维核磁共振光谱将它们的化学结构表征为（-）-表阿夫儿茶素（1）、（-）-表阿夫儿茶素-3-O-β-D-阿洛吡喃糖苷（2）、（-）-表阿夫儿茶素-3-O-（6″-O-乙酰基）-β-D-阿洛吡喃糖苷（3）、4β-羧甲基-（-）-表阿夫儿茶素甲酯（4）、4β-羧甲基-（-）-表阿夫儿茶素钠盐（5）、柚皮苷（6）、（-）-表阿夫儿茶素-（4β→8）-4β-羧甲基表阿夫儿茶素甲酯（7）和（-）表阿夫儿茶素-（4β→8,2β→O→7）-表阿夫儿茶素-（4β→8）-表阿夫儿茶素（8）。这些黄酮类化合物中的大多数在10^（-15）至约10^（-6）M范围内促进MCF-7细胞的增殖，化合物7和8在10^（-15）至约10^（-12）M范围内显示出特别强的增殖作用。同时，除化合物4外，7种黄酮类化合物在10^（-15）至约10^（-6）M范围内刺激ROS 17/2.8细胞的增殖，化合物5-8尤其以剂量依赖性方式（10^（-15）至约10^（-9）M）加速增殖，并且它们增殖作用比E2和染料木黄酮强得多。这些结果表明，从骨碎补根茎中分离出的原花青定二聚体和三聚体可能作为潜在的植物雌激素有用，并在预防绝经后骨质疏松症中发挥重要的生理作用。
