Evaluation of in vitro activity and ultrastructural changes in Leishmania amazonensis caused by sesquiterpene lactones from Calea pinnatifida (Asteraceae)

The dewaxed dichloromethane extract of Urolepis hecatantha and the compounds isolated from it were tested for their in vitro activity on Trypanosoma cruzi epimastigotes and Leishmania infantum promastigotes. The extract of U. hecatantha showed activity against both parasites with IC50 values of 7 µg/mL and 31 µg/mL, respectively. Fractionation of the dichloromethane extract led to the isolation of euparin, jaceidin, santhemoidin C, and eucannabinolide. The sesquiterpene lactones eucannabinolide and santhemoidin C were active on T. cruzi with IC50 values of 10 ± 2 µM (4.2 µg/mL) and 18 ± 3 µM (7.6 µg/mL), respectively. Euparin and santhemoidin C were the most active on L. infantum with IC50 values of 18 ± 4 µM (3.9 µg/mL) and 19 ± 4 µM (8.0 µg/mL), respectively. Eucannabinolide has also shown drug-like pharmacokinetic and toxicity properties.

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In vitro activity of chlorophyll A and B in Photodynamic Therapy on Leishmania (Leishmania) amazonensis

International Journal of Infectious Diseases ◽

10.1016/j.ijid.2018.04.4096 ◽

2018 ◽

Vol 73 ◽

pp. 299

Author(s):

L.D.S. Braga ◽

D.S.S.L. Lera ◽

Á. C. F.H.R. Milaré ◽

W. Caetano ◽

S.M.A. Aristides ◽

...

Keyword(s):

Photodynamic Therapy ◽

Chlorophyll A ◽

Leishmania Amazonensis ◽

Vitro Activity ◽

In Vitro Activity ◽

Chlorophyll A And B

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In vitro activity of the essential oil of Cymbopogon citratus and its major component (citral) on Leishmania amazonensis

Parasitology Research ◽

10.1007/s00436-009-1578-7 ◽

2009 ◽

Vol 105 (6) ◽

pp. 1489-1496 ◽

Cited By ~ 71

Author(s):

Marta Regina Santin ◽

Adriana Oliveira dos Santos ◽

Celso Vataru Nakamura ◽

Benedito Prado Dias Filho ◽

Izabel Cristina Piloto Ferreira ◽

...

Keyword(s):

Essential Oil ◽

Leishmania Amazonensis ◽

Vitro Activity ◽

In Vitro Activity ◽

Cymbopogon Citratus

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In vitro and in silico Activity of Iridoids Against Leishmania amazonensis

Current Drug Discovery Technologies ◽

10.2174/1570163814666171002102058 ◽

2019 ◽

Vol 16 (2) ◽

pp. 173-183

Author(s):

Maria Helena Vendruscolo ◽

Gustavo Machado das Neves ◽

Luciano Porto Kagami ◽

Luiz Carlos Rodrigues Junior ◽

Maria Luísa Nunes Diehl ◽

...

Keyword(s):

Natural Products ◽

In Silico ◽

Leishmania Amazonensis ◽

Vitro Activity ◽

In Vitro Activity ◽

Leishmanicidal Activity ◽

Leishmania Spp ◽

Pharmacophoric Model ◽

Molecular Modeling Studies

Background: Leishmaniasis reaches millions of people around the world. The control of the disease is difficult due to the restricted access to the diagnosis and medication, and low adherence to the treatment. Thus, more efficient drugs are needed and natural products are good alternatives. Iridoids, natural products with reported leishmanicidal activity, can be exploited for the development of anti- Leishmania drugs. The aim of this study was to isolate and to investigate the in vitro activity of iridoids against Leishmania amazonensis and to compare the activity in silico of these compounds with those reported as active against this parasite. Methods: Iridoids were isolated by chromatographic methods. The in vitro activity of asperuloside (1) and geniposide (2) from Escalonia bifida, galiridoside (3) from Angelonia integerrima and theveridoside (4) and ipolamiide (5) from Amphilophium crucigerum was investigated against promastigote forms of Leishmania amazonensis. Molecular modeling studies of 1-5 and iridoids cited as active against Leishmania spp. were performed. Results: Compounds 1-5 (5-100 µM) did not inhibit the parasite survival. Physicochemical parameters predicted for 1-5 did not show differences compared to those described in literature. The SAR and the pharmacophoric model confirmed the importance of maintaining the cyclopentane[C]pyran ring of the iridoid, of oxygen-linked substituents at the C1 and C6 positions and of bulky substituents attached to the iridoid ring to present leishmanicidal activity. Conclusion: The results obtained in this study indicate that iridoids are a promising group of secondary metabolites and should be further investigated in the search for new anti-Leishmania drugs.

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