Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.

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Baumgartner L, Sosa S, Atanasov AG, Bodensieck A, Fakhrudin N, Bauer J, Favero GD, Ponti C, Heiss EH, Schwaiger S, Ladurner A, Widowitz U, Loggia RD, Rollinger JM, Werz O, Bauer R, Dirsch VM, Tubaro A, Stuppner H

Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.

J Nat Prod. 2011 Aug 26;74(8):1779-86. doi: 10.1021/np200343t. Epub 2011 Jul 29.

PubMed ID

21800856 [ View in PubMed

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Abstract

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 (ID(5)(0) 77 mug/cm(2)) as well compounds 1-11 (ID(5)(0) 0.31-0.60 mumol/cm(2)) exhibited topical antiedematous properties comparable to those of indomethacin (ID(5)(0) 0.29 mumol/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-kappaB, 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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Troglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	400	N/A	N/A	Details
Zileuton	Arachidonate 5-lipoxygenase	IC 50 (nM)	6300	N/A	N/A	Details