TY - JOUR
T1 - Chemical constituents with leishmanicidal activity from a pink-yellow cultivar of Lantana camara var. aculeata (L.) collected in Central Mexico
AU - Delgado-Altamirano, Ronna
AU - López-Palma, Rosa Isela
AU - Monzote, Lianet
AU - Delgado-Domínguez, José
AU - Becker, Ingeborg
AU - Rivero-Cruz, José Fausto
AU - Esturau-Escofet, Nuria
AU - Vázquez-Landaverde, Pedro A.
AU - Rojas-Molina, Alejandra
N1 - Publisher Copyright:
© 2019 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2019/2/2
Y1 - 2019/2/2
N2 - Lantana camara (L.) is employed by several ethnical groups to treat numerous diseases. Although there are no ethnomedical reports on its use against leishmaniasis, organic extracts prepared from L. camara were shown to display leishmanicidal activity. In the present study, we carried out a bioassay-guided fractionation of the dichloromethane extract from Mexican L. camara in order to identify the compounds responsible for the leishmanicidal activity. Eighteen chromatographic fractions (FI-FXVIII) were evaluated in vitro against Leishmania mexicana and L. amazonensis. FII, FX, FXI, FXV, and FXVI showed significant activity against both Leishmania strains, the most potent of which was FXV. Eicosane (1), squalene (2), β-ionone (3), caryophyllene oxide (4), β-caryophyllene (5), hexanoic acid (6), tiglic acid (7), a mixture of lantanilic (8) and camaric (9) acids, and lantadene B (10) were identified and obtained from the active fractions and evaluated for their leishmanicidal activity. The mixture of lantanilic (8) and camaric (9) acids (79%/21%) was the most potent one (half maximal inhibitory concentration (IC 50 ) = 12.02 ± 0.36 µM). This study indicates that this cultivar of L. camara has high potential for the development of phytomedicines or as a source of natural products, which might represent lead compounds for the design of new drugs against leishmaniasis.
AB - Lantana camara (L.) is employed by several ethnical groups to treat numerous diseases. Although there are no ethnomedical reports on its use against leishmaniasis, organic extracts prepared from L. camara were shown to display leishmanicidal activity. In the present study, we carried out a bioassay-guided fractionation of the dichloromethane extract from Mexican L. camara in order to identify the compounds responsible for the leishmanicidal activity. Eighteen chromatographic fractions (FI-FXVIII) were evaluated in vitro against Leishmania mexicana and L. amazonensis. FII, FX, FXI, FXV, and FXVI showed significant activity against both Leishmania strains, the most potent of which was FXV. Eicosane (1), squalene (2), β-ionone (3), caryophyllene oxide (4), β-caryophyllene (5), hexanoic acid (6), tiglic acid (7), a mixture of lantanilic (8) and camaric (9) acids, and lantadene B (10) were identified and obtained from the active fractions and evaluated for their leishmanicidal activity. The mixture of lantanilic (8) and camaric (9) acids (79%/21%) was the most potent one (half maximal inhibitory concentration (IC 50 ) = 12.02 ± 0.36 µM). This study indicates that this cultivar of L. camara has high potential for the development of phytomedicines or as a source of natural products, which might represent lead compounds for the design of new drugs against leishmaniasis.
KW - Bio-directed fractionation
KW - Camaric acid
KW - Lantadene b
KW - Lantana camara
KW - Lantanilic acid
KW - Leishmania amazonensis
KW - Leishmania mexicana
KW - Leishmanicidal activity
KW - Triterpenes
UR - http://www.scopus.com/inward/record.url?scp=85061863537&partnerID=8YFLogxK
U2 - 10.3390/ijms20040872
DO - 10.3390/ijms20040872
M3 - Artículo
C2 - 30781602
AN - SCOPUS:85061863537
SN - 1661-6596
VL - 20
JO - International Journal of Molecular Sciences
JF - International Journal of Molecular Sciences
IS - 4
M1 - 872
ER -