Antileishmanial and immunomodulatory activities of lupeol, a triterpene compound isolated from Sterculia villosa

Das, Antu; Jawed, Junaid Jibran; Das, Mitali; Sandhu, Padmani; De, Utpal Chandra; Dinda, Biswanath; Akhter, Yusuf; Bhattacharjee, Surajit

doi:10.1016/j.ijantimicag.2017.04.022

Cited by 58 publications

(38 citation statements)

References 31 publications

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“…Similarly, Das et al . (2017) also described the reduction of parasite load in the spleen of infected mice after treatment of lupeol at 75 mg kg −1 . In addition, our study also established that the efficacy of lupeol at 50 mg kg −1 b.wt.…”

Section: Discussionmentioning

confidence: 98%

“…was comparatively higher than that observed at 25 mg kg −1 b.wt. These findings were consistent with previous studies which demonstrated that lupeol enhanced the production of Th1 cytokines and suppressed the Th2 cytokines (Wu et al ., 2013; Das et al ., 2017). Moreover, our study also showed that lupeol at higher dose and AmB had equal potential in augmenting the Th1 cytokines and repression of Th2 cytokines in the infected mice.…”

Section: Discussionmentioning

confidence: 99%

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Lupeol induces immunity and protective efficacy in a murine model against visceral leishmaniasis

2019

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The available chemotherapeutics for the cure of visceral leishmaniasis (VL) are linked with many detrimental effects. Moreover, VL is associated with the suppression of protective Th1 immune response of the host and induction of disease exaggerating Th2 immune response. Therefore, there is an urgent requirement of therapeutics which can augment the immune status of the host to cure this disease. In the current investigation, the antileishmanial potential of lupeol was monitored in vitro and in vivo in inbred BALB/c mice against Leishmania donovani. Lupeol showed potent antipromastigote activity via arresting parasites at sub G0/G1 phase in vitro. Lupeol significantly decreased the splenic parasite burden by inducing strong delayed-type hypersensitivity responses in contrary to untreated infected animals. The therapeutic efficacy of lupeol was observed to be similar to the reference drug, AmB. Treatment of infected animals with lupeol depicted enhanced levels of T cells and Th1 cytokines in contrast to only infected controls. Further lupeol treatment upregulated the levels of nuclear factor κ B and nitric oxide synthase genes and elevated the production of reactive oxygen species and nitric oxide. Unlike AmB, lupeol-treated infected animals did not show any toxicity. These findings are promising and indicate that lupeol can serve as a prototype drug for the cure of VL.

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Section: Discussionmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%

Lupeol induces immunity and protective efficacy in a murine model against visceral leishmaniasis

2019

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“…Mahanine inhibits JAK1 and Src which subsequently promotes the degradation of STAT3, an important transcription factor in macrophages that causes upregulation of IL-10 expression and suppression of Th1 responses ( Biswas et al, 2011 ; Lee et al, 2011 ; Das et al, 2014 ). While mahanine possesses its own unique immunomodulatory effects, several other natural compounds stimulate ROS and NO production in vitro including but not limited to, lupeol from Sterculia villosa , dehydroabietic acid from Pinus elliottii , and oil extracts from Nectandra species ( da Costa-Silva et al, 2015 ; Bosquiroli et al, 2017 ; Das et al, 2017 ; Goncalves et al, 2018 ). For example, Punica granatum , commonly known as pomegranate, has been shown to have antiparasitic and antioxidant properties ( Kaur et al, 2006 ).…”

Section: Host-targeted Therapeutics and Approaches For Treatment Of Lmentioning

confidence: 99%

Host-Directed Drug Therapies for Neglected Tropical Diseases Caused by Protozoan Parasites

et al. 2018

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The neglected tropical diseases (NTDs) caused by protozoan parasites are responsible for significant morbidity and mortality worldwide. Current treatments using anti-parasitic drugs are toxic and prolonged with poor patient compliance. In addition, emergence of drug-resistant parasites is increasing worldwide. Hence, there is a need for safer and better therapeutics for these infections. Host-directed therapy using drugs that target host pathways required for pathogen survival or its clearance is a promising approach for treating infections. This review will give a summary of the current status and advances of host-targeted therapies for treating NTDs caused by protozoa.

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“…É importante destacar que o Lupeol, um metabólito muito conhecido, exibiu atividade antiparasitária (Tabela 3), em um estudo esse triterpenóide apresentou valores significativos (IC50 de 65 ± 0,41 µg / mL e 15 ± 0,45 µg / mL) frente as formas promastigota e amastigota de Leishmania donovani, respectivamente (Das, 2017). Em outra investigação chalconas oxigenadas impediram o crescimento de promastigostas e amastigotas de leishmania em Research, Society andDevelopment, v. 9, n. 12, e45991211352, 2020 (CC BY 4.0) | ISSN 2525-3409 | DOI: http://dx.doi.org/10.33448/rsd-v9i12.11352 camundongos infectados com L. donovani inibindo a respiração do parasita e a atividade das desidrogenases mitocondriais (Zhai, et al, 1999).…”

Section: Resultsunclassified

Estudo in silico das atividades de compostos isolados de Bauhinia variegata Linn

Nunes

Gomes

Martins

et al. 2020

RSD

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A Bauhinia variegata Linn pertence à família Fabaceae e é utilizada popularmente como hipoglicemiante. Estudos fitoquímicos isolaram flavonoides, terpenos, esteroides e derivados do naftaleno, e por essa razão, este artigo objetiva descrever os resultados de farmacocinética, toxicidade e atividades biológicas obtidos em estudos in silico das moléculas isoladas para B. variegata. As bases de dados online para coleta dos dados foram: PreADMET e PASS online. Para o desenho das estruturas químicas e caracterização físico-química: MarvinSketch, Mcule property calculator e Chemicalize. Os resultados sugeriram que o Caempferol, 2'-hidroxi-4',6'- dimetoxi-3,4-metilenodioxichalcona, Campferol3-O-α-L-ramnosídeo, (2S)-5,7-dimetóxi-3’,4’-metilenodioxiflavanona e 5,6-dihidro-1,7-dihidroxi-3,4-dimetóxi-2-metildibenz[b,f]oxepina apresentaram melhor padrão farmacocinético, devido as características físico-químicas serem alinhadas com Lipinsk, entretanto, todos os compostos apresentaram inibição sobre o citocromo P450 (CYP). O Lupeol foi o mais favorável enquanto antineoplásico; o β-Sitosterol e o Heptatricontan-12, 13-diol capacidade antiviral; os flavonoides (Campferol3-O-α-L-ramnosídeo e 2'-hidroxi-4',6'- dimetoxi-3,4-metilenodioxichalcona) e o Lupeol atividade antiparasitária; o Campferol3-O-α-L-ramnosídeo e o Lupeol potencial anti-inflamatório. A ação hipoglicemiante não foi encontrada, mas a via de liberação do hormônio pode ser outra. Os compostos obtiveram resultados tóxicos nos diferentes níveis tróficos e em relação à avaliação da carcinogenicidade e mutagenicidade. Com base nestes aspectos, o Campferol3-O-α-L-ramnosídeo e o Lupeol parecem ser as moléculas mais promissoras em atividades biológicas, podendo atuar como antimaláricos, com modificações necessárias na sua estrutura para a diminuição dos seus efeitos tóxicos, bem como apresentando aspectos farmacocinéticos aceitáveis caso sejam candidatos à fármacos.

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Antileishmanial and immunomodulatory activities of lupeol, a triterpene compound isolated from Sterculia villosa

Cited by 58 publications

References 31 publications

Lupeol induces immunity and protective efficacy in a murine model against visceral leishmaniasis

Lupeol induces immunity and protective efficacy in a murine model against visceral leishmaniasis

Host-Directed Drug Therapies for Neglected Tropical Diseases Caused by Protozoan Parasites

Estudo in silico das atividades de compostos isolados de Bauhinia variegata Linn

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