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

Baumgartner L.
•
SOSA, SILVIO
•
Atanasov A. G.
altro
Stuppner H.
2011
  • journal article

Periodico
JOURNAL OF NATURAL PRODUCTS
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 (111) in terms of their putative anti-inflammatory activity. The dichloromethane extract (ID50 77 μg/cm2) as well compounds 111 (ID50 0.310.60 μmol/cm2) exhibited topical antiedematous properties comparable to those of indomethacin (ID50 0.29 μmol/cm2) 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 NFkB, cyclooxygenase-1 and -2, 5-lipoxygenase, and microsomal prostaglandin E2 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.
DOI
10.1021/np200343t
WOS
WOS:000294242800015
SCOPUS
2-s2.0-80052175121
Archivio
http://hdl.handle.net/11368/2391259
Diritti
metadata only access
Soggetti
  • Krameria lappacea

  • Krameriaceae

  • lignans

  • anti-inflammatory act...

  • Croton oil

Web of Science© citazioni
51
Data di acquisizione
Jun 16, 2022
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