2. Academic Validation
  3. Molecular decodification of gymnemic acids from Gymnema sylvestre. Discovery of a new class of liver X receptor antagonists

Molecular decodification of gymnemic acids from Gymnema sylvestre. Discovery of a new class of liver X receptor antagonists

  • Steroids. 2015 Apr;96:121-31. doi: 10.1016/j.steroids.2015.01.024.
Barbara Renga 1,  Carmen Festa 2,  Simona De Marino 2,  Simone Di Micco 3,  Maria Valeria D'Auria 2,  Giuseppe Bifulco 3,  Stefano Fiorucci 1,  Angela Zampella 4
Affiliations

Affiliations

  • 1 Department of Surgery and Biomedical Sciences, Nuova Facoltà di Medicina, P.zza L. Severi, 1-06132 Perugia, Italy.
  • 2 Department of Pharmacy, University of Naples "Federico II", Via D. Montesano, 49, I-80131 Naples, Italy.
  • 3 Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 132, 84084 Fisciano (Salerno), Italy.
  • 4 Department of Pharmacy, University of Naples "Federico II", Via D. Montesano, 49, I-80131 Naples, Italy. Electronic address: angela.zampella@unina.it.
PMID: 25668616 DOI: 10.1016/j.steroids.2015.01.024
Abstract

The individual chemical components of commercial extract of Gymnema sylvestre, a medicinal plant used in the traditional systems of the Indian medicine for its antidiabetic and hypolipidemic properties, were isolated and evaluated for their capability to act as modulators of nuclear and membrane receptors involved in glucose and lipid homeostasis. The study disclosed for the first time that individual gymnemic acids are potent and selective antagonists for the β isoform of LXR. Indeed the above activity was shared by the most abundant aglycone gymnemagenin (10) whereas gymnestrogenin (11) was endowed with a dual LXRα/β antagonistic profile. Deep pharmacological investigation demonstrated that gymnestrogenin, reducing the expression of SREBP1c and ABCA1 in vitro, is able to decrease lipid accumulation in HepG2 cells. The results of this study substantiate the use of G. sylvestre extract in LXR mediated dislypidemic diseases.

Keywords

Gymnema sylvestre; Gymnemic acids; Liver-X-receptor; Steroid nuclear receptors.

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