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Leishmanicidal constituents from the leaves of Piper rusbyi.
Planta Med. 2007 Mar; 73(3):206-11.PM

Abstract

The kavapyrone (+)-(7 R,8 S)-epoxy-5,6-didehydrokavain (1) and the chalcone flavokavain B (2) were isolated from Piper rusbyi as the bioactive components by bioassay-guided fractionation, using an in vitro assay against promastigote forms of three Leishmania strains. In addition, the new kavapyrone, (7 R,8 R/7 S,8 S)-dihydroxy-5,6-didehydrokavain (3), which is very likely an artifact, and four known compounds (4-7) were isolated. Their structures were elucidated on the basis of spectral analysis, and the absolute configurations of compounds 1 and 3 were established by CD studies and the modified Mosher ester procedure, respectively. All compounds were evaluated for in vitro leishmanicidal activity. The most active compounds 1 (IC50=81.9 microM) and 2 (IC50=11.2 microM) were also evaluated in vivo against a New World strain of cutaneous leishmaniasis, and the results showed the efficacy of 2 at a dose of 5 mg/kg/day. Compounds 1 and 3 were also assayed as reversal agents against a multidrug-resistant Leishmania tropica line, but were found to be inactive.

Authors+Show Affiliations

Flores N
Instituto Universitario de Bio-Orgánica Antonio González, Universidad de La Laguna, Tenerife, Canary Islands, Spain.
Cabrera G
No affiliation info available
Jiménez IA
No affiliation info available
Piñero J
No affiliation info available
Giménez A
No affiliation info available
Bourdy G
No affiliation info available
Cortés-Selva F
No affiliation info available
Bazzocchi IL
No affiliation info available

MeSH

AnimalsAntiprotozoal AgentsLeishmaniaLeishmaniasisParasitic Sensitivity TestsPhytotherapyPiperPlant ExtractsPlant Leaves

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17354169

Citation

Flores, Ninoska, et al. "Leishmanicidal Constituents From the Leaves of Piper Rusbyi." Planta Medica, vol. 73, no. 3, 2007, pp. 206-11.
Flores N, Cabrera G, Jiménez IA, et al. Leishmanicidal constituents from the leaves of Piper rusbyi. Planta Med. 2007;73(3):206-11.
Flores, N., Cabrera, G., Jiménez, I. A., Piñero, J., Giménez, A., Bourdy, G., Cortés-Selva, F., & Bazzocchi, I. L. (2007). Leishmanicidal constituents from the leaves of Piper rusbyi. Planta Medica, 73(3), 206-11.
Flores N, et al. Leishmanicidal Constituents From the Leaves of Piper Rusbyi. Planta Med. 2007;73(3):206-11. PubMed PMID: 17354169.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Leishmanicidal constituents from the leaves of Piper rusbyi. AU - Flores,Ninoska, AU - Cabrera,Gabriela, AU - Jiménez,Ignacio A, AU - Piñero,Jose, AU - Giménez,Alberto, AU - Bourdy,Genevieve, AU - Cortés-Selva,Fernando, AU - Bazzocchi,Isabel L, Y1 - 2007/03/12/ PY - 2007/3/14/pubmed PY - 2007/6/21/medline PY - 2007/3/14/entrez SP - 206 EP - 11 JF - Planta medica JO - Planta Med VL - 73 IS - 3 N2 - The kavapyrone (+)-(7 R,8 S)-epoxy-5,6-didehydrokavain (1) and the chalcone flavokavain B (2) were isolated from Piper rusbyi as the bioactive components by bioassay-guided fractionation, using an in vitro assay against promastigote forms of three Leishmania strains. In addition, the new kavapyrone, (7 R,8 R/7 S,8 S)-dihydroxy-5,6-didehydrokavain (3), which is very likely an artifact, and four known compounds (4-7) were isolated. Their structures were elucidated on the basis of spectral analysis, and the absolute configurations of compounds 1 and 3 were established by CD studies and the modified Mosher ester procedure, respectively. All compounds were evaluated for in vitro leishmanicidal activity. The most active compounds 1 (IC50=81.9 microM) and 2 (IC50=11.2 microM) were also evaluated in vivo against a New World strain of cutaneous leishmaniasis, and the results showed the efficacy of 2 at a dose of 5 mg/kg/day. Compounds 1 and 3 were also assayed as reversal agents against a multidrug-resistant Leishmania tropica line, but were found to be inactive. SN - 0032-0943 UR - https://www.unboundmedicine.com/medline/citation/17354169/Leishmanicidal_constituents_from_the_leaves_of_Piper_rusbyi_ DB - PRIME DP - Unbound Medicine ER -