Curcuma longa L. constituents inhibit sortase A and staphylococcus aureus cell adhesion to fibronectin
Curcuma longa L. constituents inhibit sortase A and staphylococcus aureus cell adhesion to fibronectin
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DOI：
10.1021/jf051765z
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发表时间：
2005-11-16
影响因子：
6.1
通讯作者：
Kim, JH
中科院分区：
文献类型：
--
作者：
Park, BS;Kim, JG;Kim, JH
研究了姜黄根茎成分对金黄色葡萄球菌ATCC 6538p细菌表面蛋白转肽酶A的抑制作用。将分离得到的化合物(1-4)与阳性对照对羟基苯甲酸(PHMB)进行了活性比较。通过光谱分析，确定其生物活性成分为姜黄素类化合物姜黄素(1)、去甲氧基姜黄素(2)和双脱甲氧基姜黄素(3)。姜黄素是一种有效的山梨酸酶A抑制剂，其IC50值为13.8+/-0.7mUg/mL。双去甲氧基姜黄素(IC50=31.9+/-1.2 mU/mL)和去甲氧基姜黄素(IC50=23.8+/-0.6 mU/m L)优于PHMB(IC50=40.6+/-1.2 mU/m L)。分离得到的3个化合物(1-3)对金黄色葡萄球菌Newman菌株无生长抑制活性，最小抑菌浓度(MIC)大于200 mU g/m L。姜黄素对金黄色葡萄球菌细胞与纤维连接蛋白的黏附也有很强的抑制作用。姜黄素对纤维连接蛋白结合活性的抑制突出了其通过抑制索酸酶活性来治疗金黄色葡萄球菌感染的潜力。这些结果表明，姜黄素可能是开发细菌排序酶A抑制剂的候选药物。
The inhibitory activity of Curcuma longa L. (turmeric) rhizome constituents against sortase A, a bacterial surface protein anchoring transpeptidase, from Staphylococcus aureus ATCC 6538p was evaluated. The activity of the isolated compounds (1-4) was compared to that of the positive control, p-hydroxymecuribenzoic acid (pHMB). The biologically active components of C. longa rhizome were characterized by spectroscopic analysis as the curcuminoids curcumin (1), demethoxycurcumin (2), and bisdemethoxycurcumin (3). Curcumin was a potent inhibitor of sortase A, with an IC50 value of 13.8 +/- 0.7 mu g/mL. Bisdemethoxycurcumin (IC50 = 31.9 +/- 1.2 mu g/mL) and demethoxycurcumin (IC50 = 23.8 +/- 0.6 mu g/mL) were more effective than pHMB (IC50 = 40.6 +/- 1.2 mu g/mL). The three isolated compounds (1-3) showed no growth inhibitory activity against S. aureus strain Newman, with minimum inhibitory concentrations (MICs) greater than 200 mu g/mL. Curcumin also exhibited potent inhibitory activity against S. aureus cell adhesion to fibronectin. The suppression of fibronectin-binding activity by curcumin highlights its potential for the treatment of S. aureus infections via inhibition of sortase activity. These results indicate that curcumin is a possible candidate in the development of a bacterial sortase A inhibitor.