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Antileishmanial activity evaluation of adunchalcone, a new prenylated dihydrochalcone from Piper aduncum L.
Fitoterapia. 2014 Sep; 97:28-33.F

Abstract

Bioactivity-guided fractionation of EtOH extract from the leaves of Piper aduncum L. (Piperaceae) afforded a new dihydrochalcone, named adunchalcone. Its structure was elucidated on the basis of their spectroscopic data, primarily NMR and MS. Adunchalcone was evaluated against promastigote forms of Leishmania (L.) amazonensis, L. (V.) braziliensis, L. (V.) shawi, and L. (L.) chagasi and displayed 50% effective concentrations (EC50) of 11.03, 26.70, and 11.26 μM, as well as selective indexes of 4.86, 2.01, 4.76 and 0.50, respectively. This compound was also tested against intracellular forms of L. (L.) amazonensis, displaying weak activity, in comparison to reference drug amphotericin B. However, despite reduced effect of adunchalcone against amastigotes of L. (L.) amazonensis, this work opens the perspective to use this particular molecule as a scaffold for the design of novel and selective drug candidates for neglected diseases, mainly leishmaniasis.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Dal Picolo CR
Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, São Paulo, Brazil.
Bezerra MP
Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, São Paulo, Brazil.
Gomes KS
Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, São Paulo, Brazil.
Passero LF
Laboratório de Patologia de Moléstias Infecciosas (LIM-50), Departamento de Patologia, Faculdade de Medicina, Universidade de São Paulo, São Paulo, Brazil.
Laurenti MD
Laboratório de Patologia de Moléstias Infecciosas (LIM-50), Departamento de Patologia, Faculdade de Medicina, Universidade de São Paulo, São Paulo, Brazil.
Martins EG
Departamento de Botânica, Instituto de Biociências, Universidade de São Paulo, São Paulo, Brazil.
Sartorelli P
Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, São Paulo, Brazil.
Lago JH
Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, São Paulo, Brazil. Electronic address: joao.lago@unifesp.br.

MeSH

AnimalsAntiparasitic AgentsChalconesHydroxybenzoatesLeishmaniaMice, Inbred BALB CMicrobial Sensitivity TestsPiper

Pub Type(s)

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

Language

eng

PubMed ID

24862066

Citation

Dal Picolo, Camilla R., et al. "Antileishmanial Activity Evaluation of Adunchalcone, a New Prenylated Dihydrochalcone From Piper Aduncum L." Fitoterapia, vol. 97, 2014, pp. 28-33.
Dal Picolo CR, Bezerra MP, Gomes KS, et al. Antileishmanial activity evaluation of adunchalcone, a new prenylated dihydrochalcone from Piper aduncum L. Fitoterapia. 2014;97:28-33.
Dal Picolo, C. R., Bezerra, M. P., Gomes, K. S., Passero, L. F., Laurenti, M. D., Martins, E. G., Sartorelli, P., & Lago, J. H. (2014). Antileishmanial activity evaluation of adunchalcone, a new prenylated dihydrochalcone from Piper aduncum L. Fitoterapia, 97, 28-33. https://doi.org/10.1016/j.fitote.2014.05.009
Dal Picolo CR, et al. Antileishmanial Activity Evaluation of Adunchalcone, a New Prenylated Dihydrochalcone From Piper Aduncum L. Fitoterapia. 2014;97:28-33. PubMed PMID: 24862066.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antileishmanial activity evaluation of adunchalcone, a new prenylated dihydrochalcone from Piper aduncum L. AU - Dal Picolo,Camilla R, AU - Bezerra,Mariana P, AU - Gomes,Kaio S, AU - Passero,Luiz Felipe D, AU - Laurenti,Marcia D, AU - Martins,Euder Glendes A, AU - Sartorelli,Patricia, AU - Lago,João Henrique G, Y1 - 2014/05/24/ PY - 2014/03/07/received PY - 2014/05/15/revised PY - 2014/05/16/accepted PY - 2014/5/28/entrez PY - 2014/5/28/pubmed PY - 2015/4/22/medline KW - Adunchalcone KW - Antileishmanial KW - Dihydrochalcone KW - Piper aduncum KW - Piperaceae SP - 28 EP - 33 JF - Fitoterapia JO - Fitoterapia VL - 97 N2 - Bioactivity-guided fractionation of EtOH extract from the leaves of Piper aduncum L. (Piperaceae) afforded a new dihydrochalcone, named adunchalcone. Its structure was elucidated on the basis of their spectroscopic data, primarily NMR and MS. Adunchalcone was evaluated against promastigote forms of Leishmania (L.) amazonensis, L. (V.) braziliensis, L. (V.) shawi, and L. (L.) chagasi and displayed 50% effective concentrations (EC50) of 11.03, 26.70, and 11.26 μM, as well as selective indexes of 4.86, 2.01, 4.76 and 0.50, respectively. This compound was also tested against intracellular forms of L. (L.) amazonensis, displaying weak activity, in comparison to reference drug amphotericin B. However, despite reduced effect of adunchalcone against amastigotes of L. (L.) amazonensis, this work opens the perspective to use this particular molecule as a scaffold for the design of novel and selective drug candidates for neglected diseases, mainly leishmaniasis. SN - 1873-6971 UR - https://www.unboundmedicine.com/medline/citation/24862066/Antileishmanial_activity_evaluation_of_adunchalcone_a_new_prenylated_dihydrochalcone_from_Piper_aduncum_L_ DB - PRIME DP - Unbound Medicine ER -