In vitro Activity of Diospyrin and Derivatives against Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei brucei

Essential oil of Origanum species is well known for antimicrobial activity, but only a few have been evaluated in narrow spectrum antiprotozoal assays. Herein, we assessed the antiprotozoal potential of Turkish Origanum onites L. oil and its major constituents against a panel of parasitic protozoa. The essential oil was obtained by hydrodistillation from the dried herbal parts of O. onites and analyzed by Gas Chromatography-Flame Ionization Detector (GC-FID) and Gas Chromatography coupled with Mass Spectrometry (GC-MS). The in vitro activity of the oil and its major components were evaluated against Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani, and Plasmodium falciparum. The main component of the oil was identified as carvacrol (70.6%), followed by linalool (9.7%), p-cymene (7%), γ-terpinene (2.1%), and thymol (1.8%). The oil showed significant in vitro activity against T. b. rhodesiense (IC50 180 ng/mL), and moderate antileishmanial and antiplasmodial effects, without toxicity to mammalian cells. Carvacrol, thymol, and 10 additional abundant oil constituents were tested against the same panel; carvacrol and thymol retained the oil’s in vitro antiparasitic potency. In the T. b. brucei mouse model, thymol, but not carvacrol, extended the mean survival of animals. This study indicates the potential of the essential oil of O. onites and its constituents in the treatment of protozoal infections.

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In vitro activity of commercial formulation and active principle of trypanocidal drugs against blooststreams forms of Trypanosoma brucei gambiense

AFRICAN JOURNAL OF BIOTECHNOLOGY ◽

10.5897/ajb2003.000-1095 ◽

2003 ◽

Vol 2 (11) ◽

pp. 474-476 ◽

Cited By ~ 1

Author(s):

Lekane Likeufack Clarisse ◽

Kohagne Tongue Lisette ◽

Truc Philippe

Keyword(s):

Trypanosoma Brucei ◽

Vitro Activity ◽

Active Principle ◽

In Vitro Activity ◽

Commercial Formulation ◽

Trypanosoma Brucei Gambiense ◽

Trypanocidal Drugs

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In vitro activity of anti-leishmanial drugs against Leishmania donovani is host cell dependent

Journal of Antimicrobial Chemotherapy ◽

10.1093/jac/dkp500 ◽

2010 ◽

Vol 65 (3) ◽

pp. 508-511 ◽

Cited By ~ 83

Author(s):

K. Seifert ◽

P. Escobar ◽

S. L. Croft

Keyword(s):

Host Cell ◽

Leishmania Donovani ◽

Vitro Activity ◽

In Vitro Activity

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Antitrypanosomal Activities of Proteasome Inhibitors

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.46.6.2038-2040.2002 ◽

2002 ◽

Vol 46 (6) ◽

pp. 2038-2040 ◽

Cited By ~ 24

Author(s):

Joseph Nkemgu-Njinkeng ◽

Vera Rosenkranz ◽

Michael Wink ◽

Dietmar Steverding

Keyword(s):

Drug Development ◽

Trypanosoma Brucei ◽

Proteasome Inhibitors ◽

Vitro Activity ◽

In Vitro Activity ◽

Data Support ◽

Nanomolar Range

ABSTRACT Seven peptidyl proteasome inhibitors were tested for in vitro activity against Trypanosoma brucei bloodstream forms. Two compounds showed activity in the low nanomolar range. In general, trypanosomes were more susceptible to the compounds than were human HL-60 cells. The data support the potential of proteasome inhibitors for rational antitrypanosomal drug development.

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