Practical progress and new drugs for changing patterns of leishmaniasis

Olliaro, Piero; Bryceson, A. D. M.

doi:10.1016/0169-4758(93)90231-4

Cited by 211 publications

(130 citation statements)

References 41 publications

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“…Seu tratamento é feito à base de antimoniais pentavalentes (Sb +5 ), anfotericina B e pentamidinas (isotionato e mesilato), quimioterápicos de alto custo, usados por via parenteral, requerendo um período de administração prolongado, causando efeitos adversos, como: alterações cardíacas, renais, pancreáticas e hepáticas (Olliaro;Bryceson, 1997;Yardley, 2002).…”

Section: Introductionunclassified

Efeito leishmanicida in vitro de Stachytarpheta cayennensis (Rich.) Vahl (Verbenaceae)

Moreira¹,

Costa²,

Lopes³

et al. 2007

Rev. bras. farmacogn.

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RESUMO:ABSTRACT: "In vitro leishmanicidal effect of Stachytarpheta cayennensis (Rich.) Vahl (Verbenaceae)". Leishmanicidal activity of the hydroalcoholic extract of Stachytarpheta cayennensis, species that is usually employed in ulcers caused by Leishmania, was evaluated in vitro using Leishmania braziliensis and L. amazonensis promastigotes forms. The hydroalcoholic extract was prepared from dried leaves and used in L. amazonensis and L. braziliensis promastigotes cultures at concentrations of 500 to 32.5 g/mL. After 24 hours the promastigotes forms were quantifi ed and the IC 50 was calculated. The cytotoxicity of the extract was evaluated using peritoneal macrophages. The extract presented a dose and specie-dependent leishmanicidal effect to Leishmania promastigotes, mainly to the L. braziliensis ones. The cytotoxic effect was not observed in macrophage cultures. In conclusion, the hydroalcoholic extract of S. cayennensis inhibits the growing of Leishmania promastigotes forms in vitro accounting for the folk use of this vegetal in skin ulcers caused by Leishmania.

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Section: Introductionunclassified

Efeito leishmanicida in vitro de Stachytarpheta cayennensis (Rich.) Vahl (Verbenaceae)

Moreira¹,

Costa²,

Lopes³

et al. 2007

Rev. bras. farmacogn.

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“…(Croft, 1988;Who, 1996). A rising problem is the changing patterns of sensitivity in antimonials (Olliaro & Bryceson, 1993;Berman, 1997).…”

Section: Introductionmentioning

confidence: 99%

Recent advances in the fight against leishmaniasis with natural products

et al. 1999

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Summary :The active compounds obtained from some medicinal plants used traditionally worldwide for the treatment of leishmaniasis are reviewed. Among these active molecules described in recent literature are quinoline alkaloids such as alkyl-2 quinoline and aryl-2 quinoline from Galipea longiflora, isoquinoline alkaloids such as isoguattouregidine from Guatteria foliosa, indole alkaloids such as conodurine and gabunine from Pescheiera van heurkii, terpenes such as jatrogrossidione from Jatropha grossidentata, acetogenins such as senegalene from Annona senegalensis and lignans such as (+)nyasol from Asparagus africanus. Other natural compounds with antileishmanial activity are coumarins, chalcones, lactones, tetralones and saponins. Some of them are known antiprotozoal natural products. These compounds could be used as templates to discover new and effective drugs against leishmaniasis.KEY WORDS : antileishmanial, leishmaniasis, natural products, alkaloids, terpenes, quinones, coumarins, chalcones, acetogenins, lactone, lignan. Résumé : DONNÉES RÉCENTES SUR LES COMPOSÉS ACTIFS DE PLANTES MÉDICINALES UTILISÉES DANS LE TRAITEMENT DE LA LEISHMANIOSE

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“…Antimony remains the therapeutic cornerstone in all regions; however, antimony is expensive, toxic and requires administration of high doses resulting in serious side effects. [11][12][13] Therefore, there remains an urgent need for development of less toxic drugs that are effective against all forms of leishmaniases. The search of new drugs against leishmaniasis, potentially compounds and their derivatives have been described in the literature.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, X-ray crystal structure and theoretical calculations of antileishmanial neolignan analogues

Nascimento¹,

Santos²,

Santos³

et al. 2010

J. Braz. Chem. Soc.

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A síntese e a estrutura cristalina por difração de raios-X de dois análogos de neolignanas, 2-(4-clorofenil)-1-feniletanona (20) e 2-[tio(4-clorofenil)]-1-(3,4-dimetoxifenil)propan-1-ona (12) são descritas. O composto 12 apresenta atividade intracelular contra Leishmania donovani e Leishmania amazonensis de amastigotas que causam a leishmaniose tegumentar e visceral. Além disso, a teoria do funcional de densidade (DFT) com o funcional híbrido B3LYP foi empregado para calcular um conjunto de descritores moleculares para dezenove análogos sintéticos de neolignanas com atividades antileishmaniose. Posteriormente, a análise discriminante stepwise foi realizada para investigar possíveis relações entre a estrutura molecular e atividades biológicas. Por meio dessa análise os compostos foram classificados em dois grupos ativos e inativos de acordo com seu grau de atividade biológica, e as propriedades mais importantes foram as cargas de alguns átomos, a afinidade eletrônica e o ClogP.The synthesis and X-ray crystal diffraction structure of two analogues of neolignans, 2-(4-chlorophenyl)-1-phenylethanone (20) and 2-[(4-chlorophenyl)thio]-1-(3,4-dimethoxyphenyl) propan-1-one (12) is described. The compound 12 presents activity against intracellular Leishmania donovani and Leishmania amazonensis amastigotes that cause cutaneous and visceral leishmaniasis. In addition, the density functional theory (DFT) with the B3LYP hybrid functional was employed to calculate a set of molecular descriptors for nineteen synthetic analogues of neolignans with antileishmanial activities. Afterwards, the stepwise discriminant analysis was performed to investigate possible relationship between the molecular descriptors and biological activities. Through this analysis the compounds were classified into two groups active and inactive according to their degree of biological activities, and the more important properties were charges on some key atoms, electronic affinity and ClogP.

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Practical progress and new drugs for changing patterns of leishmaniasis

Cited by 211 publications

References 41 publications

Efeito leishmanicida in vitro de Stachytarpheta cayennensis (Rich.) Vahl (Verbenaceae)

Efeito leishmanicida in vitro de Stachytarpheta cayennensis (Rich.) Vahl (Verbenaceae)

Recent advances in the fight against leishmaniasis with natural products

Synthesis, X-ray crystal structure and theoretical calculations of antileishmanial neolignan analogues

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