Trypanocidal activity of Lychnophora staavioides Mart. (Vernonieae, Asteraceae)

Takeara, Renata; Albuquerque, Sérgio de; Lopes, Norberto Peporine; Lopes, João Luís Callegari

doi:10.1078/094471103322331430

Cited by 45 publications

(35 citation statements)

References 20 publications

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“…Esta substância apresentou uma porcentagem de atividade tripanossomicida de 63,2 ± 4,1%, já a tectochrysina demonstrou 38,5 ± 8,3 % e o chrysoeriol 32,7 ± 7,1% de redução dos parasitas sangüíneos. Todas estas substâncias foram ativas na dose de 500 µg/mL (Takeara et al, 2003). Do extrato clorofórmico de Moquinia kingii foi obtida a apigenina que apresentou ação contra tripomastigotas in vitro (Schinor et al, 2004).…”

Section: Flavonóidesunclassified

Substâncias da natureza com atividade anti-Trypanosoma cruzi

Saúde-Guimarães¹,

Faria²

2007

Rev. bras. farmacogn.

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RESUMO:A doença de Chagas, uma zoonose causada por Trypanosoma cruzi, afeta em todo o mundo cerca de 16 a 18 milhões de pessoas. Sua transmissão ocorre através das fezes de triatomíneos, insetos hematófagos conhecidos como barbeiro. Atualmente, a principal forma de transmissão da doença de Chagas em áreas urbanas é por meio de transfusão de sangue contaminado. A violeta de genciana é o único agente que pode ser empregado na quimioprofi laxia de sangue destinado à transfusão. No entanto, existem algumas restrições ao seu uso. A quimioterapia disponível para a doença de Chagas não é efi caz uma vez que as drogas disponíveis nifurtimox e benznidazol são ativas apenas na fase aguda da doença e apresentam sérios efeitos colaterais. Várias substâncias isoladas de plantas foram avaliadas como agentes anti-T. cruzi, objetivando encontrar drogas com menos efeitos colaterais e maior efi cácia para a quimioprofi laxia e quimioterapia da doença de Chagas. Nesta revisão são apresentadas as substâncias de origem natural com atividade anti-T. cruzi.

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Section: Flavonóidesunclassified

Substâncias da natureza com atividade anti-Trypanosoma cruzi

Saúde-Guimarães¹,

Faria²

2007

Rev. bras. farmacogn.

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“…Their biological activities have been attributed to sesquiterpene lactones, lignans, and caffeoylquinic acid derivatives isolated from polar extracts of the leaves and roots (Santos et al, 2005). The trypanocidal activity of Lychnophora species has been attributed to flavanoids, sesquiterpene lactones, and caffeoylquinic acids isolated from their alcoholic extracts (Takeara et al, 2003).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of the bactericidal and trypanocidal activities of triterpenes isolated from the leaves, stems, and flowers of Lychnophora pinaster

Abreu¹,

Takahashi²,

Duarte³

et al. 2011

Rev. bras. farmacogn.

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Abstract:The phytochemical investigation on the aereal parts of Lychnophora pinaster Mart., Asteraceae, was carried to isolation of triterpenes. 3-O-Acetyllupeol (1), 3-O-acetyl-pseudotaraxasterol (2), and 3-O-acetyl-α-amyrin (3) were isolated from hexanic extract and 4,4-dimethyl-cholesta-22,24-dien-5-ol (4), α-amyrin (5), and lupeol (6) were isolated from hexanic/dichlorometanic extract of the leaves. Compounds Δ 7 -bauerenyl acetate (7), friedelin (8), stigmasterol (9), and sitosterol (10) were isolated from the hexanic/dichlorometanic extract of the stems. The steroids 9 and 10 were also isolated from the hexanic/dichlorometanic extract of the flowers. Triterpenes 1, 3, 4, and 7 are described for the first time in the genus Lychnophora. The apolar fractions of the leaf and stem extracts and some isolated triterpenes showed low trypanocidal activity. Moreover, apolar fractions of the leaf and stem extracts and 5 showed antibacterial action against Staphylococcus aureus.

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“…They are also common constituents of medicinal plants, and the therapeutic effects of many traditional medicines have been ascribed to these phytochemicals. We and others have recently identified several types of flavonoids as antiprotozoal principles of plant extracts (3,9,12,17,32,33), but a comprehensive study of their structure-activity relationships (SARs) has not been conducted so far. Therefore, it was our interest to assess the in vitro trypanocidal and leishmanicidal activities of a large flavonoid library, as well as a panel of other related phenolic and phenylpropanoid compounds; draw SARs, if possible; and determine their antiparasitic selectivities.…”

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Antitrypanosomal and Antileishmanial Activities of Flavonoids and Their Analogues: In Vitro, In Vivo, Structure-Activity Relationship, and Quantitative Structure-Activity Relationship Studies

Taşdemir

Kaiser²,

Brun³

et al. 2006

Antimicrob Agents Chemother

438

233

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Trypanosomiasis and leishmaniasis are important parasitic diseases affecting millions of people in Africa, Asia, and South America. In a previous study, we identified several flavonoid glycosides as antiprotozoal principles from a Turkish plant. Here we surveyed a large set of flavonoid aglycones and glycosides, as well as a panel of other related compounds of phenolic and phenylpropanoid nature, for their in vitro activities against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, and Leishmania donovani. The cytotoxicities of more than 100 compounds for mammalian L6 cells were also assessed and compared to their antiparasitic activities. Several compounds were investigated in vivo for their antileishmanial and antitrypanosomal efficacies in mouse models. Overall, the best in vitro trypanocidal activity for T. brucei rhodesiense was exerted by 7,8-dihydroxyflavone (50% inhibitory concentration [IC 50 ], 68 ng/ml), followed by 3-hydroxyflavone, rhamnetin, and 7,8,3,4-tetrahydroxyflavone (IC 50 s, 0.5 g/ml) and catechol (IC 50 , 0.8 g/ml). The activity against T. cruzi was moderate, and only chrysin dimethylether and 3-hydroxydaidzein had IC 50 s less than 5.0 g/ml. The majority of the metabolites tested possessed remarkable leishmanicidal potential. Fisetin, 3-hydroxyflavone, luteolin, and quercetin were the most potent, giving IC 50 s of 0.6, 0.7, 0.8, and 1.0 g/ml, respectively. 7,8-Dihydroxyflavone and quercetin appeared to ameliorate parasitic infections in mouse models. Generally, the test compounds lacked cytotoxicity in vitro and in vivo. By screening a large number of flavonoids and analogues, we were able to establish some general trends with respect to the structure-activity relationship, but it was not possible to draw clear and detailed quantitative structure-activity relationships for any of the bioactivities by two different approaches. However, our results can help in directing the rational design of 7,8-dihydroxyflavone and quercetin derivatives as potent and effective antiprotozoal agents.

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Trypanocidal activity of Lychnophora staavioides Mart. (Vernonieae, Asteraceae)

Cited by 45 publications

References 20 publications

Substâncias da natureza com atividade anti-Trypanosoma cruzi

Substâncias da natureza com atividade anti-Trypanosoma cruzi

Evaluation of the bactericidal and trypanocidal activities of triterpenes isolated from the leaves, stems, and flowers of Lychnophora pinaster

Antitrypanosomal and Antileishmanial Activities of Flavonoids and Their Analogues: In Vitro, In Vivo, Structure-Activity Relationship, and Quantitative Structure-Activity Relationship Studies

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