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乌尼莫利纳叶中2α-羟基五环三萜酸的局部抗炎活性

Topical anti-inflammatory activity of 2alpha-hydroxy pentacyclic triterpene acids from the leaves of Ugni molinae.

作者信息

Aguirre María C, Delporte Carla, Backhouse Nadine, Erazo Silvia, Letelier María Eugenia, Cassels Bruce K, Silva Ximena, Alegría Sergio, Negrete Rosa

机构信息

Laboratory of Natural Products, Department of Pharmacological and Toxicological Chemistry, Faculty of Chemical and Pharmaceutical Sciences, University of Chile, Santiago 1.

出版信息

Bioorg Med Chem. 2006 Aug 15;14(16):5673-7. doi: 10.1016/j.bmc.2006.04.021. Epub 2006 May 11.

DOI:10.1016/j.bmc.2006.04.021
PMID:16697209
Abstract

Leaf extracts of Ugni molinae Turcz. are used in the Chilean cosmetic industry on the assumption that they have decongestant, regenerative, and anti-aging properties. A bioassay-guided fractionation of this plant material showed that some extracts have potent anti-inflammatory activities. Further fractionation led to the isolation and identification of betulinic acid, a mixture of ursolic and oleanolic acids, and the 2alpha-hydroxy derivatives alphitolic, asiatic, and corosolic acids. The latter three were evaluated in vivo in the mouse ear assay for their topical anti-inflammatory activity, inducing inflammation with either arachidonic acid (AA) or 12-O-tetradecanoylphorbol-13 acetate (TPA). Only corosolic acid was active in the AA assay, with similar potency to nimesulide, but all three triterpene acids inhibited TPA-induced inflammation with potencies comparable to that of indomethacin.

摘要

智利番荔枝(Ugni molinae Turcz.)的叶提取物被用于智利的化妆品行业,因为人们认为它们具有减轻充血、再生和抗衰老的特性。对这种植物材料进行生物测定导向的分级分离表明,一些提取物具有强大的抗炎活性。进一步分级分离导致了桦木酸、熊果酸和齐墩果酸的混合物以及2α-羟基衍生物α-香树脂醇酸、积雪草苷酸和科罗索酸的分离和鉴定。后三种物质在小鼠耳部试验中进行了体内局部抗炎活性评估,分别用花生四烯酸(AA)或12-O-十四烷酰佛波醇-13-乙酸酯(TPA)诱导炎症。只有科罗索酸在AA试验中具有活性,效力与尼美舒利相似,但所有三种三萜酸都能抑制TPA诱导的炎症,效力与吲哚美辛相当。

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