Antileishmanial activities

Miltefosin The antileishmanial activity of this anticancer drug was discovered in the mid-1980s. It is the first oral drug available to treat visceral and cutaneous/mucocutaeous leishmaniasis. However, the registration process is slow. 

Di GC, De MM, Chiron J, Delmas F (2005) Synthesis and antileishmanial activities of 4, 5-di-substituted acridines as compared to their 4-mono-substituted homologues. Bioorg Med Chem 13 5560-5568... 

Licochalcone (50) is a natural product that is isolated from the roots of Chinese liquorice and is reported to have antileishmanial activity [49]. A series of chromene-substituted chalcones related to licochalcone have been reported to have antileishmanial activity [50]. Compound 51 was reported to have an IC50 of 1.2 pM against Leishmania major promastigotes versus meglumine antimoniate (IC50 =30 pM). Various compounds related to 51 have potent antileishmanial activity (IC50 < 3 pM) with potency similar to 51, but they did not show cytotoxicity. 

Delorenzi JC, Attias M, Gattass CR, Andrade M, Rezende C, Pinto AC, Henriques AT, Bou-Habib DC and Saraiva EM. 2001. Antileishmanial activity of indole alkaloid from Peschiera australis. Antimicrob Agents Chemother 45(5) 1349-1354. 

Stager, S., et al., Both intcrlcukin-4 (IL-4) and IL-4 receptor alpha signaling contribute to the development of hepatic granulomas with optimal antileishmanial activity, Infect. Immun. 71, 8, 4804, 2003. 

In one experiment, LC-AmB was compared with AmBisome (small unilamellar liposomes). LC-AmB was found to have an ED50 of 0.19 mg/kg and an ED90 of 0.51 mg/kg, whereas for AmBisome both these parameters were below 0.20 mg/kg, the lowest dose tested. In another experiment, LC-AmB was compared with Abelcet and showed a better reduction of parasite burden after three injections of 1 mg/kg, but there were not sufficient data to allow ED50 values to be calculated (22). Therefore, we can conclude that this new AmB formulation retains antileishmanial activity in vivo, but it is difficult to position it with respect to other formulations. 

Loiseau PM, et al. Design and antileishmanial activity of amphotericin B-loaded stable ionic amphiphile biovector formulations. Antimicrob Agents Chemother... 

Larabi M, et al. Toxicity and antileishmanial activity of a new stable lipid suspension of amphotericin B. Antimicrob Agents Chemother 2003 47 3774. 

Castillo D, Arevalo J, Herrera F, Ruiz C, Rojas R, Rengifo E, Vaisberg A, Lock D, Le-mesre JL, Gomitzka H, Sauvain M. Spirolactone Iridoids might be responsible for the Antileishmanial Activity of a Peruvian Traditional Remedy Made with Himatanthus sucuuba (Apocynaceae). Journal of Ethnopharmacology 2007 112(2) 410-414. 

Iwli et al [97] have reports based on the evaluation of plant-extract of D. multiradiata for antileishmanial activity using a mechanism-based radiorespirometric micro-technique. Extracts were found to be active at concentrations of 50 pg/ml or less against a visceral leishmania isolate. A number of Dorstenia species used traditionally as anti-snake venom were subjected to a pharmacological screening process and were found to possess analgesic and anti-inflammatory activities [98]. Many of the flavonoids isolated from African Dorstenia show moderate to good antioxidant activities [Croft, unpublished results]. The cytotoxic properties of... 

A-(nitrobenzimidazol-2-yl)pyridinium derivatives have been synthesized in order to study their antiprotozoal activity [693-695], A H and 13C NMR study has been carried out for structural determination of these compounds (S13C in Table 3.25). Quantitative structure-activity relationships (QSAR) between the in vitro antileish-manial activity of /V- ben zazolylpyridinium salts and their 13C NMR chemical shifts have been studied in order to determine the influence of benzimidazole substituents upon antileishmanial activity [695],... 

Rastogi N, Singh VR et al (2006) Microwave mediated aminomethylation and antileishmanial activity of 2- 4 -(2 ,4 -dichlorobenzyloxy)-phenyl -l,3,4-oxadiazolin-5-thiones and 3- 4 -(2 ,4 -dichlorobenzyloxy)phenyl -4-phenyl-l,2,4-triazolin-5-thiones. Ind J Heterocycl Chem 16 5-8... 

Annona muricata L. - graviola Severe insomnia Leaves (infusion or decoction, ingested) Caboclos [56,57] Acetogenins [86,87] neurotoxic benzylisoquinoline derivatives [88] essential oil [89,90] alkaloids [91,92] flavonoids and terpenoids [93] Striatal neurodegeneration [252] atypical parkinsonism [253] antileishmanial activity [254] antidepressive activity [91]... 

New RRC, Chance ML, Thomas SC, et al. Antileishmanial activity of antimonials entrapped in liposomes. Nature 1978 272 55-56. 

Girault, S., Grellier, R, Berecibar, A., Maes, L., Mouray, E., Lemiere, R, Debreu, M.-A., Davioud-Charvet, E., Sergheraert, C. Antimalarial, antitrypanosomal, and antileishmanial activities and cytotoxiciy of bis(9-amino-6-chloro-2-methoxyacridines) influence of the linker. J. Med. Chem. 2000, 43, 2646-2654. 

J. M. Nicolas, P. Pirson, and B. Leclef. Acetylated LDL as a vehicle for antiinfections drugs preparation and antileishmanial activity of acetylated-LDL containing ketoconazole-oleate. Ann. Top. Med. Parasitol. 8i(40) 325-336 (1990). 

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