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标准化的富含巴西苏木素的苏木提取物的抗氧化、抗菌和抗炎活性。

Antioxidant, antibacterial, and anti-inflammatory activities of standardized brazilin-rich Caesalpinia sappan extract.

作者信息

Nirmal Nilesh Prakash, Panichayupakaranant Pharkphoom

机构信息

Excellent Research Laboratory, Phytomedicine and Pharmaceutical Biotechnology Excellence Center, Faculty of Pharmaceutical Sciences, Prince of Songkla Univesity, Hat-Yai, Songkhla , Thailand .

出版信息

Pharm Biol. 2015;53(9):1339-43. doi: 10.3109/13880209.2014.982295. Epub 2015 Apr 13.

Abstract

CONTEXT

Brazilin is a major active principle of Caesalpinia sappan L. (Leguminosae or Fabaceae). For industry aspects, brazilin-rich extract (BRE) has been prepared and standardized to contain 39% w/w brazilin. BRE may have more advantages than brazilin in term of a lower-cost production process.

OBJECTIVES

To investigate the antioxidant, antibacterial, and anti-inflammatory activities of BRE.

MATERIAL AND METHODS

BRE was prepared by a simple one-step purification of the crude ethanol extract of C. sappan heartwood (CSE) using a Diaion® HP-20 column. The antioxidant activities were determined using three methods, including DPPH radical scavenging, reducing power, and β-carotene bleaching assays, at concentration ranges of 1-10, 10-100, and 10-100 µg/mL, respectively. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of BRE (15.6-1000 µg/mL) against Gram-positive and Gram-negative bacteria were determined by the broth microdilution method. Anti-inflammatory activity of BRE (0.1-5 µg/mL) was evaluated as anti-denaturation activity using bovine serum albumin as a substrate.

RESULTS AND DISCUSSION

On the basis of β-carotene bleaching assay, BRE showed antioxidant activity with an EC50 value of 60.5 µg/mL, which was almost equal to that of pure brazilin (52.1 µg/mL). Gram-positive bacteria were more sensitive to all tested samples than Gram-negative bacteria. BRE possessed higher antibacterial activities than CSE, but lower than brazilin. MIC/MBC values of 62.5-125/125 and 250-500/250-500 µg/mL were obtained for BRE against Gram-positive and Gram-negative bacteria, respectively. A low concentration (0.1 µg/mL) of brazilin, BRE, and CSE showed anti-inflammatory activity by inhibiting protein denaturation up to 46.8, 54.1, and 61.9%, respectively.

摘要

背景

巴西苏木精是苏木(豆科)的主要活性成分。在工业方面,已制备出富含巴西苏木精的提取物(BRE)并进行标准化处理,使其含有39%(w/w)的巴西苏木精。就生产成本较低的生产工艺而言,BRE可能比巴西苏木精具有更多优势。

目的

研究BRE的抗氧化、抗菌和抗炎活性。

材料与方法

通过使用Diaion® HP - 20柱对苏木心材的粗乙醇提取物(CSE)进行简单的一步纯化来制备BRE。分别在1 - 10、10 - 100和10 - 100μg/mL的浓度范围内,使用三种方法测定抗氧化活性,包括DPPH自由基清除法、还原能力法和β - 胡萝卜素漂白法。采用肉汤微量稀释法测定BRE(15.6 - 1000μg/mL)对革兰氏阳性菌和革兰氏阴性菌的最低抑菌浓度(MIC)和最低杀菌浓度(MBC)。以牛血清白蛋白为底物,将BRE(0.1 - 5μg/mL)的抗炎活性评估为抗变性活性。

结果与讨论

基于β - 胡萝卜素漂白法,BRE表现出抗氧化活性,EC50值为60.5μg/mL,几乎与纯巴西苏木精(52.1μg/mL)相同。革兰氏阳性菌对所有测试样品比革兰氏阴性菌更敏感。BRE具有比CSE更高的抗菌活性,但低于巴西苏木精。BRE对革兰氏阳性菌和革兰氏阴性菌的MIC/MBC值分别为62.5 - 125/125和250 - 500/250 - 500μg/mL。低浓度(0.1μg/mL)的巴西苏木精、BRE和CSE通过抑制蛋白质变性分别表现出高达46.8%、54.1%和61.9%的抗炎活性。

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