Lantz R C, Chen G J, Solyom A M, Jolad S D, Timmermann B N
Department of Cell Biology and Anatomy, University of Arizona, Tucson, AZ, USA.
Phytomedicine. 2005 Jun;12(6-7):445-52. doi: 10.1016/j.phymed.2003.12.011.
Major compounds of several commonly used botanicals, including turmeric, have been purported to have anti-inflammatory actions. In order to test the anti-inflammatory activity of compounds isolated from rhizomes of Curcuma longa L. (Zingiberaceae), we have established an in vitro test system. HL-60 cells were differentiated and exposed to lipopolysaccharide (LPS) from Escherichia coli (1 microg/ml) in the presence or absence of botanical compounds for 24 h. Supernatants were collected and analyzed for the production of tumor necrosis factor alpha (TNF-alpha) and prostaglandin E2 (PGE2) using standard ELISA assays. Water-soluble extracts were not cytotoxic and did not exhibit biological activity. Organic extracts of turmeric were cytotoxic only at concentrations above 50 microg/ml. Crude organic extracts of turmeric were capable of inhibiting LPS-induced TNF-alpha (IC50 value = 15.2 microg/ml) and PGE2 (IC50 value = 0.92 microg/ml) production. Purified curcumin was more active than either demethoxy- or bisdemethoxycurcumin. Fractions and subfractions of turmeric extracts collected via preparative HPLC had differing biological activity, ranging from no activity to IC50 values of < 1 microg/ml. For some fractions, subfractionation resulted in a loss of activity, indicating interaction of the compounds within the fraction to produce an anti-inflammatory effect. A combination of several of the fractions that contain the turmeric oils was more effective than the curcuminoids at inhibiting PGE2. While curcumin inhibited COX-2 expression, turmeric oils had no effect on levels of COX-2 mRNA.
包括姜黄在内的几种常用植物药的主要化合物据称具有抗炎作用。为了测试从姜黄（姜科）根茎中分离出的化合物的抗炎活性，我们建立了一个体外测试系统。HL-60细胞被诱导分化，并在存在或不存在植物化合物的情况下，暴露于来自大肠杆菌的脂多糖（LPS，1微克/毫升）中24小时。收集上清液，使用标准ELISA测定法分析肿瘤坏死因子α（TNF-α）和前列腺素E2（PGE2）的产生。水溶性提取物没有细胞毒性，也没有表现出生物活性。姜黄的有机提取物仅在浓度高于50微克/毫升时具有细胞毒性。姜黄的粗有机提取物能够抑制LPS诱导的TNF-α（IC50值=15.2微克/毫升）和PGE2（IC50值=0.92微克/毫升）的产生。纯化的姜黄素比去甲氧基姜黄素或双去甲氧基姜黄素更具活性。通过制备型HPLC收集的姜黄提取物的级分和亚级分具有不同的生物活性，范围从无活性到IC50值<1微克/毫升。对于某些级分，亚分级导致活性丧失，表明级分内化合物之间的相互作用产生了抗炎效果。几种含有姜黄油的级分组合在抑制PGE2方面比姜黄素类更有效。虽然姜黄素抑制COX-2表达，但姜黄油对COX-2 mRNA水平没有影响。
