Lin Chao-Zhan, Zhu Chen-Chen, Hu Min, Wu Ai-Zhi, Bairu Zeren-Dawa, Kangsa Suolang-Qimei
Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Guangzhou 510405, P.R. China.
School of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou 510006, P.R. China.
J Intercult Ethnopharmacol. 2014 Jul-Sep;3(3):123-7. doi: 10.5455/jice.20140619030232. Epub 2014 Jul 3.
Antioxidant activity is one of the important indexes for estimating medicinal value for the traditional Chinese medicine. The aim of this study is to investigate the antioxidant activity of 11 flavonoids mainly revealing luteolin as mother nucleus isolated from Pyrethrum tatsienense.
The antioxidant activity of 11 flavonoids was measured in vitro using the classical 1,1-diphenyl-2-picrylhydrazyl removal method. The percentages of scavenging activity of 11 flavonoids were analyzed by taking the choice of a-tocopherol as positive drugs, and the scavenging activity was plotted against the sample concentration to obtain the IC50 values.
Ten flavonoids containing phenolic hydroxyl groups have different levels of antioxidant activity. Antioxidant activity mainly depends on the numbers and the substitutional positions of phenolic hydroxyls in B ring. When C-3', 4' positions in B ring of flavonoids are replaced by hydroxyl groups, the antioxidant activity improved remarkably. Phenolic hydroxyl groups in A ring contribute some to antioxidant activity because of the electrophilic effect of C ring, and the numbers and substitutional positions of methoxyl and glycosyl have a little effect on the antioxidant activity.
Structure-activity relationships of antioxidant activity about flavonoids isolated from P. tatsienense are concluded, which will be beneficial to deep understanding the pharmacological functions of this Tibetan medicine in vivo from the point of antioxidation.
抗氧化活性是评价中药药用价值的重要指标之一。本研究旨在探讨从川西小黄菊中分离得到的以木犀草素为母核的11种黄酮类化合物的抗氧化活性。
采用经典的1,1-二苯基-2-苦基肼自由基清除法体外测定11种黄酮类化合物的抗氧化活性。以α-生育酚为阳性对照药,分析11种黄酮类化合物的清除活性百分比,并以清除活性对样品浓度作图得到半数抑制浓度(IC50)值。
10种含酚羟基的黄酮类化合物具有不同程度的抗氧化活性。抗氧化活性主要取决于B环上酚羟基的数目和取代位置。当黄酮类化合物B环的C-3'、4'位被羟基取代时,抗氧化活性显著提高。由于C环的亲电作用,A环上的酚羟基对抗氧化活性有一定贡献,而甲氧基和糖基的数目及取代位置对抗氧化活性影响较小。
总结了川西小黄菊黄酮类化合物抗氧化活性的构效关系,这将有助于从抗氧化角度深入了解这种藏药在体内的药理作用。