Natural product based leads to fight against leishmaniasis

Singh, Nisha; Mishra, Bhuwan B.; Bajpai, Surabhi; Singh, Rakesh Kumar; Tiwari, Vinod K.

doi:10.1016/j.bmc.2013.11.048

Cited by 173 publications

(118 citation statements)

References 230 publications

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“…Several studies have shown that alkaloids, flavonoids, chalcones, terpenoids, saponins, and phenolic compounds display antileishmanial effect (Sandjo et al, 2016;Singh et al, 2014;Wink, 2012). In the present study, HPLC-DAD was employed to evaluate the phytochemical profile of Q2.…”

Section: Discussionmentioning

confidence: 99%

Antileishmanial effects of the alkaloid-rich fraction of Quassia amara L.

Gabriel¹,

Amaral²,

Cortê-Real³

et al. 2016

J. Med. Plants Res.

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Control of leishmaniasis remains a challenge due the high toxicity of the chemotherapeutic drugs presently available. The ongoing search for better leishmanicidal compounds has brought herbal drugs into the limelight as safe and effective substitutes to conventional therapies which have various drawbacks. The current study was designed to evaluate the antileishmanial effect of Quassia amara against Leishmania amazonensis and Leishmania infantum. Different fractions (Hexane (Q1), dichloromethane (Q2), ethyl acetate (Q3) and butanol (Q4)) obtained from the liquid-liquid partition of the crude Q. amara methanol extract were tested against Leishmania promastigote forms. After 120 h of treatment with Q. amara fractions (1 to 500 µg/ml), the minimal inhibitory concentration (MIC) was determined using resazurin. The most active fraction (Q2) was analyzed using thin layer chromatography (TLC) and high performance liquid chromatography-diode array detector (HPLC-DAD) techniques. The effects of Q2 on parasite ultrastructure were investigated by transmission electron microscopy. In addition, Leishmania-infected macrophages were treated with Q2 in order to evaluate the anti-amastigote effect. Among the fractions tested, Q2 showed the highest activity against L. amazonensis and L. infantum promastigotes MIC values of 62.5 and 31.25 µg/ml, respectively. There were ultrastructural alterations, such as nuclear chromatin condensation, intense vacuolization and autophagic and myelin-like figures in parasites treated with Q2 (62.5 µg/ml). Macrophages previously infected with L. amazonensis and L. infantum promastigotes showed a drastic reduction in the number of parasites recovered in the supernatant after Q2 treatment at MIC values. The TLC and HPLC fingerprints of Q2 showed that alkaloids were the main chemical constituents in this fraction. The results presented herein showed that the alkaloid-rich fraction Q2 is a promising source of antileishmanial agents. Further investigation will be necessary in order to isolate and test the substance(s) responsible for the bioactivity.

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Section: Discussionmentioning

confidence: 99%

Antileishmanial effects of the alkaloid-rich fraction of Quassia amara L.

Gabriel¹,

Amaral²,

Cortê-Real³

et al. 2016

J. Med. Plants Res.

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“…Esse remédio, premiado na Exposição Universal de Londres de 1862, obtido do látex da árvore Ficus gomelleira, é uma mistura constituída pelos triterpenos pentacíclicos α-amirona e β-amirona, e os acetatos de de α e β-amirina. Trabalhos recentes da literatura científica mostram que os triterpenos presentes na doliarina de Peckolt têm ação antiparasitária (Singh et al, 2014 Lima (1826Lima ( -1910 foi publicada originalmente no periódico Brasil Médico, na coluna "Formulário prático", em 1906. Na publicação da Gazeta Médica da Bahia, em julho daquele ano foram reproduzidos alguns dos artigos de Wucherer publicados no mesmo periódico.…”

Section: Considerações Finaisunclassified

“Pós de doliarina e ferro”: um dos remédios importantes da Farmácia Peckolt

Silva

Dias

Pinto³

et al. 2015

Hist. cienc. saude-Manguinhos

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Resumo O farmacêutico Theodoro Peckolt é uma das mais importantes figuras da história da química de produtos naturais brasileira. Como outros farmacêuticos do século XIX que atuavam no Brasil, desenvolveu formulações que comercializava em sua farmácia, localizada no Rio de Janeiro, e que tiveram grande prestígio junto à população e à classe médica. O texto apresenta a relação entre a doença identificada inicialmente como opilação e a terapêutica utilizada no século XIX, destacando uma das formulações da Farmácia Peckolt – “Pós de doliarina e ferro”. O produto tem sua origem no látex da espécie Ficus gomelleira(figueira-branca ou gameleira). O artigo tem entre seus objetivos revelar a composição química, feita por métodos modernos de análise do látex deFicus gomelleira.

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“…In this context, in the last years several natural compounds and their synthetic analogues have been tested against Leishmania, and many of them have demonstrated potential as leishmanicidal agents (Changtam et al, 2010;Tipparaju et al, 2008;Marin et al, 2009;Mishra et al 2009a,b;Hussain et al, 2014;Singh et al, 2014). Stilbenes-based compounds are widely represented in nature (Shen et al, 2009;Riviere et al, 2012) and have become of particular interest to chemists and biologists because of their wide range of biological effects including chemopreventive, antitumor, antioxidant, antimicrobial, anti-inflammatory and antihistaminic activities (Hart, 1981;Fremont, 2000;Young and Chaplin, 2004).…”

Section: Introductionmentioning

confidence: 99%

In vitro antileishmanial activity of trans-stilbene and terphenyl compounds

Castelli

Bruno

Vitale

et al. 2016

Experimental Parasitology

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h i g h l i g h t s g r a p h i c a l a b s t r a c tWe evaluated the leishmanicidal activity of a pool of new stilbene and terphenyl derivatives. Therphenyl 11 showed a leshmanicidal activity higher than pentostam and TTAS. Therphenyl 11 induces apoptosis in Leishmania parasites while saving macrophages and normal cells. Currently available drugs present different drawbacks, so there is an urgent need to develop new, safe and cost-effective drugs against leishmaniasis. In this study we tested a small library of trans-stilbene and terphenyl derivatives against promastigote, amastigotes and intramacrophage amastigote forms of Leishmania infantum. Two compounds of the series, the trans-stilbene 3 and the terphenyl 11, presented the best activity and safety profiles. Terphenyl 11 showed a leshmanicidal activity higher than pentostam and the ability to induce apoptosis selectively in Leishmania infantum while saving macrophages and primary epithelial cells. Our data indicate that terphenyl compounds, as well as stilbenes, are endowed with leishmanicidal activity, showing potential for further studies in the context of leishmanial therapy.

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Natural product based leads to fight against leishmaniasis

Cited by 173 publications

References 230 publications

Antileishmanial effects of the alkaloid-rich fraction of Quassia amara L.

Antileishmanial effects of the alkaloid-rich fraction of Quassia amara L.

“Pós de doliarina e ferro”: um dos remédios importantes da Farmácia Peckolt

In vitro antileishmanial activity of trans-stilbene and terphenyl compounds

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