scholarly journals Exploring Antiparasitic Molecule Sources from Timber by-Product Industries—Leishmanicidal and Trypanocidal Compounds from Clathrotropis brunnea Amshoff

2020 ◽  
Vol 11 ◽  
Author(s):  
Fernando Torres ◽  
Sara M. Robledo ◽  
Wiston Quiñones ◽  
Gustavo Escobar ◽  
Rosendo Archbold ◽  
...  
Keyword(s):  
Cutaneous Leishmaniasis ◽  
Ethanol Extract ◽  
Leishmania Braziliensis ◽  
Moderate Activity ◽  
Hamster Model ◽  
Cutaneous Ulcer ◽  
Pure Substances ◽  
Pharmacological Potential ◽  
Median Effective Concentration

Through bioguided in vitro assays, the leishmanicidal and trypanocidal effects of an ethanol extract, seven fractions, and two pure substances obtained from Clathrotropis brunnea Amshoff sawdust were established. The effectiveness of the two metabolites was confirmed in a hamster model of cutaneous Leishmaniasis by Leishmania braziliensis and in Balb/c mice infected by Trypanosoma cruzi. In vitro, 3,5-dimethoxystilbene was the most active against L. braziliensis amastigotes, with a median lethal concentration (LC50) of 4.18 μg/ml (17.40 μM) and a selectivity index of 3.55, but showed moderate activity for T. cruzi, with a median effective concentration (EC50) value of 27.7 μg/ml (115.36 μM). Flavanone pinostrobin, meanwhile, showed high activity against L. braziliensis, with an EC50 of 13.61 μg/ml (50.39 μM), as well as for T. cruzi, with an EC50 of 18.2 μg/ml (67.38 μM). The animal model assay of cutaneous Leishmaniasis showed that 50% of the hamsters treated with pinostrobin were definitively cured the cutaneous ulcer, and 40% showed an improvement, with a reduction in the size of the of 84–87%. Moreover, Balb/c mice experimentally infected with T. cruzi and treated for 25 days with pinostrobin experienced a reduction in their parasitemia by 71%. These results demonstrate the high potential of C. brunnea Amshoff against cutaneous Leishmaniasis and American trypanosomiasis and indicate the pharmacological potential of waste from the wood industry, which has tons of potentially useful chemicals for the development of new medicines.

scholarly journals In VitroAnti-Plasmodial Activity ofTrigonella foenum–graecumL.

2010 ◽  
Vol 7 (4) ◽  
pp. 441-445 ◽  
Author(s):  
M. Palaniswamy ◽  
B. V. Pradeep ◽  
R. Sathya ◽  
J. Angayarkanni
Keyword(s):  
Ethanol Extract ◽  
Traditional Healers ◽  
Active Principle ◽  
Test Plant ◽  
Moderate Activity ◽  
Inhibition Assay ◽  
Phytochemical Screening ◽  
Solvent Systems ◽  
Fenugreek Leaves

Developing countries, where malaria is one of the most prevalent diseases, still rely on traditional medicine as a source for the treatment of this disease. For the present study,Trigonella foenum-graecumL. (fenugreek) were collected from Coimbatore, Tamilnadu, India. The test plant has been used in India by traditional healers for the treatment of fever as well as other diseases. The active principle was extracted out in different solvent systems to assess the anti-plasmodial potential, with an aim that they can further be utilized to formulate drugs.In vitroanti-plasmodial assay of the extracted fractions of fenugreek leaves was carried out using laboratory adapted chloroquine sensitive and resistantPlasmodium falciparumisolates. Schizont maturation inhibition assay was adopted to analyze the potential of the extracts. Ethanol extract (50%) seemed to possess profound anti-plasmodial activity with IC50value of 8.75 ± 0.35 µg ml−1and 10.25 ± 0.35 µg ml−1against chloroquine sensitive and resistantP. falciparumisolates, respectively. Among the investigated six fractions of the plant extracts, two were found to have significant anti-plasmodial activity with IC50values <10 µg ml−1, namely ethanol and butanol extracts. Two extracts chloroform and ethyl acetate showed moderate activity with IC50values ranging from 10 to 20 µg ml−1, and the other two extracts, hexane and water appeared to be inactive with IC50values >85 µg ml−1. In addition, preliminary phytochemical screening of the various extracts indicated the presence of alkaloids, saponin, tannin like phenolic compounds, flavonoids and steroids.

Anti-inflammatory and Anti-HIV Compounds from Swertia bimaculata

Planta Medica ◽  
2017 ◽  
Vol 83 (17) ◽  
pp. 1368-1373 ◽  
Author(s):  
Miao Dong ◽  
Li-Qiu Quan ◽  
Wei-Feng Dai ◽  
Shi-Li Yan ◽  
Chin-Ho Chen ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Ethanol Extract ◽  
Moderate Activity ◽  
Nitric Oxide Production ◽  
X Ray Diffraction ◽  
Oxide Production ◽  
New Compounds ◽  
Anti Hiv ◽  
Hiv 1

AbstractThree new compounds (1 – 3), including a sesterterpenoid, aspterpenacid C (1), with an unusual 5/3/7/6/5 pentacyclic skeleton, together with seven known ones (4 – 10), were isolated from the ethanol extract of the traditional Chinese medicinal plant Swertia bimaculata. Their structures were elucidated on the basis of the methods of spectroscopic NMR, MS, and computational chemistry. The structure of 1 was further confirmed by single-crystal X-ray diffraction analysis. Compounds 1 – 10 were tested for activities on the inhibition of nitric oxide production and HIV-1 replication in vitro. Compound 1 exhibited moderate activity in inhibiting nitric oxide production (IC50 = 16.1 µM) and HIV-1 replication (EC50 = 1.35 µM).

scholarly journals Development of a Novel Formulation with Hypericin To Treat Cutaneous Leishmaniasis Based on Photodynamic Therapy inIn VitroandIn VivoStudies

2015 ◽  
Vol 59 (9) ◽  
pp. 5804-5813 ◽  
Author(s):  
Andrés Montoya ◽  
Alejandro Daza ◽  
Diana Muñoz ◽  
Karina Ríos ◽  
Viviana Taylor ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Cutaneous Leishmaniasis ◽  
Hypericum Perforatum ◽  
Topical Formulation ◽  
Hamster Model ◽  
Content Type ◽  
Intracellular Amastigotes ◽  
Infected Cells

ABSTRACTAn evaluation of the leishmanicidal activityin vitroandin vivoof hypericin, an expanded-spectrum photosensitizer found inHypericum perforatum, is presented. Hypericin was evaluated against intracellular amastigotesin vitroofLeishmania(Viannia)panamensis. A topical formulation containing 0.5% hypericin was developed and assayedin vivoin a hamster model of cutaneous leishmaniasis. Results demonstrate that hypericin induces a significant antiamastigote effectin vitroagainstL. panamensisby decreasing the number of parasites inside infected cells. The topical formulation of 0.5% hypericin allows healing ofL. panamensis-induced lesions upon a topical application of 40 mg/day plus visible-light irradiation (5 J/cm2, 15 min), twice a week for 3 weeks.

scholarly journals In VitroSensitivity of PairedLeishmania(Viannia)braziliensisSamples Isolated before Meglumine Antimoniate Treatment and after Treatment Failure or Reactivation of Cutaneous Leishmaniasis

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Cibele Baptista ◽  
Luciana de Freitas Campos Miranda ◽  
Maria de Fátima Madeira ◽  
Leonor Laura Pinto Leon ◽  
Fátima Conceição-Silva ◽  
...  
Keyword(s):  
Treatment Failure ◽  
Cutaneous Leishmaniasis ◽  
Drug Exposure ◽  
Lethal Dose ◽  
Poor Response ◽  
Leishmania Braziliensis ◽  
Meglumine Antimoniate ◽  
Intralesional Administration ◽  
The Difference

This study evaluated thein vitrosensitivity of pairedLeishmania braziliensissamples isolated from the same patient before pentavalent antimonial treatment (Sample A) and after treatment failure or cutaneous leishmaniasis reactivation (Sample B) in patients undergoing intralesional administration or injections (5 mgSbV/kg/d) of meglumine antimoniate. Fourteen samples from 7 patients were studied. After 24 h of drug exposure, 50% lethal dose (LD50) values for promastigotes ranged from 0.37 mg/mL to 5.86 mg/mL for samples obtained before treatment (A) and 0.89 mg/mL to 7.80 mg/mL for samples obtained after treatment (B). After 48 h, LD50values ranged from 0.37 mg/mL to 5.75 mg/mL and 0.70 mg/mL to 7.68 mg/mL for A and B samples, respectively. After 48 h, LD50values for amastigotes ranged from 11.7 to 44.3 μg/mL for A samples and 13.7 to 52.7 μg/mL for B samples. Of 7 patients, 1 discontinued treatment and 6 were cured after retreatment with amphotericin B (4 cases) or meglumine antimoniate (2 cases). Overall the B samples had higher LD50values than A samples; however the difference was not significant. These results do not support the hypothesis that low-dose and intralesional treatments induce selection of resistant parasitesin vitroand suggest that other factors may influence therapeutic outcome in patients with poor response to initial treatment.

scholarly journals Antileishmanial and cytotoxic activities of four Andean plant extracts from Colombia

2020 ◽  
Vol 13 (10) ◽  
pp. 2178-2182
Author(s):  
Wilson Cardona-G ◽  
Sara Robledo ◽  
Fernando Alzate ◽  
Andrés F. Yepes ◽  
Cristian Hernandez ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Plant Extracts ◽  
Ethyl Acetate Extract ◽  
Ethanol Extract ◽  
Cytotoxic Activities ◽  
Moderate Activity ◽  
Leishmania Panamensis ◽  
Ethanol Extracts ◽  
Ethyl Acetate Extracts

Background and Aim: Licania salicifolia (L.S) Cuatrec., Persea ferruginea (P.F) Kunth, Oreopanax floribundus (O.F), and Psychotria buchtienii (P.B) belong to the families Chrysobalanaceae, Lauraceae, Araliaceae, and Rubiaceae, respectively, which have been used as medicines by communities in the Andes. This study evaluated the leishmanicidal and cytotoxic activities of alcohol and non-alcohol extracts from four Andean plant extracts (L.S, O.F, P.F, and P.B). Materials and Methods: Extracts were obtained by percolation with solvents of different polarities – hexane, dichloromethane, ethyl acetate, and ethanol. Phytochemical screening was conducted based on reported methods. All products were evaluated in vitro to determine the leishmanicidal activity against amastigotes of Leishmania panamensis and cytotoxicity against U937 cells. Results: Flavonoids, triterpenes, and tannins were the main secondary metabolites found. From the results, dichloromethane extracts from O.F and P.B, ethanol extract from P.B, and ethyl acetate extracts of all plants were active, with EC50 <30 μg/mL. Ethyl acetate was the most active extract, which showed EC50 values of 9.8, 14.1, 23.7, and 25.5 μg/mL, for L.S, P.B, O.F, and P.F, respectively. Hexane extracts from P.B and O.F exhibited moderate activity with EC50 values of 84.8 and 87.4 μg/mL, respectively. Hexane and ethanol extracts from O.F, ethyl acetate, and ethanol extracts from L.S, and all extracts from P.F were not toxic. Alternatively, hexane and dichloromethane extracts from L.S and P.B as well as dichloromethane and ethyl acetate extracts from O.F displayed high toxicity. Conclusion: Based on the activity we observed, ethyl acetate extract can continue in its usage in the search for new antileishmanial drugs, mainly ethyl acetate extract from L.S showed activity comparable to meglumine antimoniate and was not cytotoxic.

scholarly journals PARTICIPAÇÃO DOS RECEPTORES TOLL-LIKE NA RESPOSTA A INFECÇÃO in vitro POR Leishmania (Viannia) braziliensis: UMA REVISÃO DE LITERATURA

2021 ◽  
Vol 2 (1) ◽  
pp. 54
Author(s):  
Anna Clara Silva Fonseca ◽  
Nathália Brígida de Oliveira ◽  
Daniela Camargos Costa
Keyword(s):  
Cutaneous Leishmaniasis ◽  
Natural Killer ◽  
Leishmania Braziliensis ◽  
Toll Like Receptors ◽  
American Cutaneous Leishmaniasis ◽  
Tnf Α ◽  
Mucosal Leishmaniasis

Introdução: A Leishmania braziliensis é um protozoário da família Trypanosomatidae responsável pelo desenvolvimento de uma das formas dermotrópicas da doença denominada leishmaniose mucosa (LM). O parasito é intracelular obrigatório e se multiplica dentro dos macrófagos e monócitos de seus hospedeiros. Os receptores tolllike (TLR) são glicoproteínas transmembrana presentes nas células de defesa, principalmente Natural Killer, macrófagos e células dendríticas, que reconhecem estruturas microbianas e que promovem uma série de sinais que produzem citocinas próinflamatórias importantes para que a resposta imune inata seja efetiva, como por exemplo TNF-α, IL-10 e TGF-β. Objetivo: Realizar revisão da literatura a respeito do papel dos receptores Toll-like na resposta à infecção in vitro por L. braziliensis. Material e métodos: Realizado no formato de revisão integrativa, a pesquisa abrangeu artigos científicos das bases de dados SCIELO e PUBMED. Os descritores utilizados foram “American Cutaneous leishmaniasis”, “Leishmania braziliensis”, “mucosal leishmaniasis” e “Toll-like receptors”. Foram selecionados artigos acadêmicos originais, escritos na língua inglesa, que foram publicados no período de 2014 a 2020, obtendo -se 20 artigos. Após a leitura dos títulos e resumos e ao adotar os critérios de exclusão, foram selecionados 12 artigos originais para a presente revisão. Resultados: As pesquisas selecionadas avaliaram 147 pacientes com diagnóstico histopatológico de Leishmaniose Cutânea (LC). Os pacientes que apresentavam LM, concomitantemente possuíam uma maior expressão de células TCD4+, TCD8+, IL-10+ e TGF-β+ em comparação com aqueles que possuíam LC, que expressavam uma menor quantidades dessas citocinas. Em oposição, o TNF-α em pacientes com LC, encontrava-se aumentado se comparada a LM. Na análise relacionada a TLR-2 e TLR-4, houve uma maior expressão em monócitos nos pacientes com LC associadas a L. braziliensis e que o bloqueio dos TRL reduziu as respostas oxidativas das células de pacientes com LC. Conclusão: Diante dos resultados é possível concluir que a maior expressão de TLR-2 e TLR-4 promove a hiper-reatividade de citocinas pró-inflamatórias e consequente pré-disposição para desenvolvimento da doença. Portanto, seu bloqueio é eficaz para redução das lesões. Esse dado demonstra a relação e o papel dos TLR na infecção por L. braziliensis, trazendo importantes esclarecimentos para a resposta imune e desenho vacinal.

scholarly journals PD-1 Blockade Modulates Functional Activities of Exhausted-Like T Cell in Patients With Cutaneous Leishmaniasis

2021 ◽  
Vol 12 ◽  
Author(s):  
Renan Garcia de Moura ◽  
Luciana Polaco Covre ◽  
Carlos Henrique Fantecelle ◽  
Vitor Alejandro Torres Gajardo ◽  
Carla Baroni Cunha ◽  
...  
Keyword(s):  
T Cells ◽  
T Cell ◽  
Cutaneous Leishmaniasis ◽  
Cell Function ◽  
Parasite Clearance ◽  
Skin Lesions ◽  
T Cell Subsets ◽  
Leishmania Braziliensis ◽  
T Cell Function

Patients infected by Leishmania braziliensis develop debilitating skin lesions. The role of inhibitory checkpoint receptors (ICRs) that induce T cell exhaustion during this disease is not known. Transcriptional profiling identified increased expression of ICRs including PD-1, PDL-1, PDL-2, TIM-3, and CTLA-4 in skin lesions of patients that was confirmed by immunohistology where there was increased expression of PD-1, TIM-3, and CTLA-4 in both CD4+ and CD8+ T cell subsets. Moreover, PDL-1/PDL-2 ligands were increased on skin macrophages compared to healthy controls. The proportions PD1+, but not TIM-3 or CTLA-4 expressing T cells in the circulation were positively correlated with those in the lesions of the same patients, suggesting that PD-1 may regulate T cell function equally in both compartments. Blocking PD-1 signaling in circulating T cells enhanced their proliferative capacity and IFN-γ production, but not TNF-α secretion in response to L. braziliensis recall antigen challenge in vitro. While we previously showed a significant correlation between the accumulation of senescent CD8+CD45RA+CD27- T cells in the circulation and skin lesion size in the patients, there was no such correlation between the extent of PD-1 expression by circulating on T cells and the magnitude of skin lesions suggesting that exhausted-like T cells may not contribute to the cutaneous immunopathology. Nevertheless, we identified exhausted-like T cells in both skin lesions and in the blood. Targeting this population by PD-1 blockade may improve T cell function and thus accelerate parasite clearance that would reduce the cutaneous pathology in cutaneous leishmaniasis.

scholarly journals Granzyme B Produced by Natural Killer Cells Enhances Inflammatory Response and Contributes to the Immunopathology of Cutaneous Leishmaniasis

2019 ◽  
Vol 221 (6) ◽  
pp. 973-982 ◽  
Author(s):  
Taís M Campos ◽  
Fernanda O Novais ◽  
Maíra Saldanha ◽  
Rúbia Costa ◽  
Morgana Lordelo ◽  
...  
Keyword(s):  
T Cells ◽  
Nk Cells ◽  
Cutaneous Leishmaniasis ◽  
Natural Killer ◽  
Cd8 T Cells ◽  
Granzyme B ◽  
Skin Lesions ◽  
Interferon Γ ◽  
Leishmania Braziliensis

Abstract Background Skin lesions from patients infected with Leishmania braziliensis has been associated with inflammation induced by cytotoxic CD8+ T cells. In addition, CD8+ T cell-mediated cytotoxicity has not been linked to parasite killing. Meanwhile, the cytotoxic role played by natural killer (NK) cells in cutaneous leishmaniasis (CL) remains poorly understood. Methods In this study, we observed higher frequencies of NK cells in the peripheral blood of CL patients compared with healthy subjects, and that NK cells expressed more interferon-γ, tumor necrosis factor (TNF), granzyme B, and perforin than CD8+ T cells. Results We also found that most of the cytotoxic activity in CL lesions was triggered by NK cells, and that the high levels of granzyme B produced in CL lesions was associated with larger lesion size. Furthermore, an in vitro blockade of granzyme B was observed to decrease TNF production. Concclusions Our data, taken together, suggest an important role by NK cells in inducing inflammation in CL, thereby contributing to disease immunopathology.

scholarly journals Effect ofCentella asiaticaon Oxidative Stress and Lipid Metabolism in Hyperlipidemic Animal Models

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Yun Zhao ◽  
Ping Shu ◽  
Youzhi Zhang ◽  
Limin Lin ◽  
Haihong Zhou ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Lipid Metabolism ◽  
Metabolic Diseases ◽  
Centella Asiatica ◽  
Ethanol Extract ◽  
Hypolipidemic Effect ◽  
Mice Model ◽  
Hamster Model

Hyperlipidemia and many other metabolic diseases are related to oxidative stress.Centella asiaticais a traditional Chinese medicine whose antioxidant effect in vitro has been reported. We are interested in whether it possesses this effect in vivo and hence modulates lipid metabolism. Therefore, experiments were carried out on mice and golden hamsters regarding its antioxidant and hypolipidemic effect. We observed that a fraction (CAF3) of the ethanol extract (CAE) ofCentella asiaticahad a cholesterol decrease of 79% and a triglyceride decrease of 95% in acute mice model, so CAF3 was further investigated in high-fat-fed hamster model. It was shown that CAF3 increased SOD and GSH-Px activities and decreased MDA level, and it also improved TC, TG, LDL-C, HDL-C, AST, and ALT levels. L-CAT and SR-BI gene expression in hamsters were increased. Taken together, our data suggest that the CAF3 fraction ofCentella asiaticahas antioxidant and hypolipidemic properties.

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