School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan.
J Agric Food Chem. 2011 Apr 27;59(8):3649-56. doi: 10.1021/jf104718g. Epub 2011 Mar 10.
Vitis thunbergii Sieb. and Zucc. var. taiwaniana Lu is an endemic plant in Taiwan used as a dietary supplement for bone health. In this study, human chondrocytes were induced to produce COX-2, MMP-3, -13, and PGE(2) by LPS. An (18)F-FDG microPET imaging system was used to evaluate the anti-inflammatory arthritic effects in vivo. Six stilbenes, resveratrol (1), (+)-ε-viniferin (2), ampelopsin C (3), ampelopsin A (4), (-)-vitisin B (5), and (+)-vitisin A (6), were isolated from the stem part of V. thunbergii, which displayed the strongest PGE(2) inhibition. Among these compounds, 1 significantly decreased COX-2 activity, PGE(2), MMP-3, and -13 production in vitro, and (18)F-FDG uptake and serum PGE(2) in rabbits in vivo. Anti-inflammatory effects were enhanced through the combined usage of 1 and other oligostilbenes. Taken together, the synergistic effects of 1 and oligostilbenes resulted in stem part extracts with lower 1 content displaying the better anti-inflammatory arthritis effects.
三叶崖爬藤是台湾特有的植物，常被当作保健食物，用于维持骨骼健康。本研究中，利用脂多糖（LPS）诱导人类软骨细胞产生环氧化酶-2（COX-2）、基质金属蛋白酶-3（MMP-3）、-13（MMP-13）和前列腺素 E2（PGE2）。我们采用 18F-FDG 微 PET 成像系统评估体内的抗炎关节炎疗效。从三叶崖爬藤的茎部分离得到 6 种二苯乙烯类化合物，包括白藜芦醇（1）、（+）-ε-viniferin（2）、ampelopsin C（3）、ampelopsin A（4）、（-）-vitisin B（5）和（+）-vitisin A（6）。这些化合物中，1 对 PGE2 的抑制作用最强。体外实验表明，1 能显著降低 COX-2 活性、PGE2、MMP-3 和 MMP-13 的产生，体内实验也表明，1 能降低兔 18F-FDG 摄取和血清 PGE2 水平。1 与其他寡二苯乙烯联合使用时，抗炎效果增强。总之，1 与寡二苯乙烯的协同作用使茎部提取物在低 1 含量下表现出更好的抗关节炎作用。
