期刊
JOURNAL OF NATURAL PRODUCTS
卷 74, 期 8, 页码 1779-1786出版社
AMER CHEMICAL SOC
DOI: 10.1021/np200343t
关键词
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资金
- Austrian Science Fund (FWF) [NFN S10703-B03, S10704-B03, S10705-B03]
The roots of Krameria lappacea are used traditionally against oropharyngeal inflammation. So far, the astringent and antimicrobial properties of its proanthocyanidin constituents are considered to account for the anti-inflammatory effect. The aim of the present study was to characterize pharmacologically a lipophilic extract of K. lappacea roots and several isolated lignan derivatives (1-11) in terms of their putative anti-inflammatory activity. The dichloromethane extract (ID50 77 mu g/cm(2)) as well compounds 1-11 (ID50 0.31-0.60 mu mol/cm(2)) exhibited topical antiedematous properties comparable to those of indomethacin (ID50 0.29 mu mol/cm(2)) in a mouse ear in vivo model. Two of the most potent compounds, 2-(2-hydroxy-4-methoxyphenyl)-5-(3-hydroxypropyl)benzofuran (5) and (+)-conocarpan (7), were studied regarding their time-dependent edema development and leukocyte infiltration up to 48 h after croton oil-induced dermatitis induction, and they showed activity profiles similar to that of hydrocortisone. In vitro studies of the isolated lignan derivatives demonstrated the inhibition of NF-kappa B, cyclooxygenase-1 and -2, 5-lipoxygenase, and microsomal prostaglandin E-2 synthase-1 as well as antioxidant properties, as mechanisms possibly contributing to the observed in vivo effects. The present findings not only support the ethnopharmacological use of K lappacea roots but also reveal that the isolated lignan derivatives contribute strongly to the anti-inflammatory activity of this herbal drug.
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