Planta Med 2009; 75(4): 307-311
DOI: 10.1055/s-0028-1088382
Pharmacology
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

Oral Metabolism and Efficacy of Kalanchoe pinnata Flavonoids in a Murine Model of Cutaneous Leishmaniasis

Michelle F. Muzitano1 , 2 [*] , Camila A. B. Falcão2 , Elaine A. Cruz2 , Maria C. Bergonzi3 , Anna R. Bilia3 , Franco F. Vincieri3 , Bartira Rossi-Bergmann2 , Sônia S. Costa1
  • 1Núcleo de Pesquisas de Produtos Naturais, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil
  • 2Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil
  • 3Department of Pharmaceutical Sciences, University of Florence, Florence, Italy
Further Information

Publication History

Received: June 15, 2008 Revised: October 22, 2008

Accepted: October 30, 2008

Publication Date:
11 December 2008 (online)

Abstract

Leishmaniasis is a parasitic disease that threatens 350 million people worldwide. In a search for new antileishmanial drugs, the in vitro activity of flavonoids from Kalanchoe pinnata (Crassulaceae) was previously demonstrated in infected cells. In order to demonstrate the safety and oral activity of K. pinnata, flavonoids were evaluated in vivo in a murine model of cutaneous leishmaniasis. Daily oral doses of quercetin 3-O-α-L-arabinopyranosyl (1→2)-α-L-rhamnopyranoside, quercetin 3-O-α-L-rhamnopyranoside, and free quercetin (16 mg/kg body weight) all were able to control the lesion growth caused by Leishmania amazonensis and to significantly reduce parasite load. These flavonoids were as effective as the crude K. pinnata aqueous extract given at 320 mg/kg body weight. HPLC-DAD-MS analysis of the plasma of extract-treated mice suggested that quercetin and quercetin glucuronides are the main metabolites of K. pinnata quercetin glycosides. Our results indicate that K. pinnata quercetin glycosides are important active components of the aqueous extract and that they possess potent oral efficacy against cutaneous leishmaniasis.

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1 Current address: Centro de Biociências e Biotecnologia, Universidade Estadual do Norte Fluminense, Campos dos Goytacazes, RJ, Brazil

Prof. Dr. Sônia S. Costa

Núcleo de Pesquisas de Produtos Naturais

Universidade Federal do Rio de Janeiro

21941–902 Rio de Janeiro

RJ Brazil

Phone: +55-21-2562-6512

Fax: +55-21-2562-6512

Email: sscosta@nppn.ufrj.br

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