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Houel, E.; Gonzalez, G.; Bessière, J.-M.; Odonne, G.; Eparvier, V.; Deharo, E.; Stien, D. |
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Therapeutic switching: From antidermatophytic essential oils to new leishmanicidal products |
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Journal Article |
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2015 |
Publication |
Memorias do Inst. Oswaldo Cruz |
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110 |
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1 |
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106-113 |
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Antifungal agents; Antiparasitic agents; Leishmania; Peritoneal macrophages – sesquiterpenes; Therapeutic switching |
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Abstract |
This study examined whether the antidermatophytic activity of essential oils (EOs) can be used as an indicator for the discovery of active natural products against Leishmania amazonensis. The aerial parts of seven plants were hydrodistilled. Using broth microdilution techniques, the obtained EOs were tested against three strains of dermatophytes (Trichophyton mentagrophytes, Microsporum gypseum and Microsporum canis). To compare the EOs antifungal and antiparasitic effects, the EOs activities against axenic amastigotes of L. amazonensis were concurrently evaluated. For the most promising EOs, their antileishmanial activities against parasites infecting peritoneal macrophages of BALB/c mice were measured. The most interesting antifungal candidates were the EOs from Cymbopogon citratus, Otacanthus azureus and Protium heptaphyllum, whereas O. azureus, Piper hispidum and P. heptaphyllum EOs exhibited the lowest 50% inhibitory concentration (IC50) values against axenic amastigotes, thus revealing a certain correspondence between both activities. The P. hispidum EO was identified as the most promising product in the results from the infected macrophages model (IC50: 4.7 μg/mL, safety index: 8). The most abundant compounds found in this EO were sesquiterpenes, notably curzerene and furanodiene. Eventually, the evaluation of the antidermatophytic activity of EOs appears to be an efficient method for identifying new potential drugs for the treatment of L. amazonensis. |
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Export Date: 17 March 2015 |
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EcoFoG @ webmaster @ |
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587 |
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Houel, E.; Fleury, M.; Odonne, G.; Nardella, F.; Bourdy, G.; Vonthron-Sénécheau, C.; Villa, P.; Obrecht, A.; Eparvier, V.; Deharo, E.; Stien, D. |
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Antiplasmodial and anti-inflammatory effects of an antimalarial remedy from the Wayana Amerindians, French Guiana: Takamalaimë (Psidium acutangulum Mart. ex DC., Myrtaceae) |
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Journal Article |
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Year |
2015 |
Publication |
Journal of Ethnopharmacology |
Abbreviated Journal |
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166 |
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279-285 |
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Psidium acutangulum; Plasmodium; Cytokines; Antimalarial; French Guiana; Traditional medicine |
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Abstract |
Ethnopharmacological relevance:
Field investigations highlighted the use of Psidium acutangulum Mart. ex DC (syn. P. persoonii McVaugh), a small tree used by the Wayana Amerindians in Twenke–Taluhwen and Antecume–Pata, French Guiana, for the treatment of malaria, and administered either orally in the form of a decoction or applied externally over the whole body. This use appears limited to the Wayana cultural group in French Guiana and has never been reported anywhere else. Our goal was to evaluate the antimalarial and anti-inflammatory activities of a P. acutangulum decoction to explain the good reputation of this remedy.
Materials and methods:
Interviews with the Wayana inhabitants of Twenke–Taluhwen and Antecume–Pata were conducted within the TRAMAZ project according to the TRAMIL methodology, which is based on a quantitative and qualitative analysis of medicinal plant uses. A decoction of dried aerial parts of P. acutangulum was prepared in consistency with the Wayana recipe. In vitro antiplasmodial assays were performed on chloroquine-resistant FcB1 ([3H]-hypoxanthine bioassay) and 7G8 (pLDH bioassay) P. falciparum strains and on chloroquine sensitive NF54 ([3H]-hypoxanthine bioassay) P. falciparum strain. In vitro anti-inflammatory activity (IL-1β, IL-6, IL-8, TNFα) was evaluated on LPS-stimulated human PBMC and NO secretion inhibition was measured on LPS stimulated RAW murine macrophages. Cytotoxicity of the decoction was measured on L6 mammalian cells, PBMCs, and RAW cells. A preliminary evaluation of the in vivo antimalarial activity of the decoction, administered orally twice daily, was assessed by the classical four-day suppressive test against P. berghei NK65 in mice.
Results:
The decoction displayed a good antiplasmodial activity in vitro against the three tested strains, regardless to the bioassay used, with IC50 values of 3.3 µg/mL and 10.3 µg/mL against P. falciparum FcB1 and NF54, respectively and 19.0 µg/mL against P. falciparum 7G8. It also exhibited significant anti-inflammatory activity in vitro in a dose dependent manner. At a concentration of 50 µg/mL, the decoction inhibited the secretion of the following pro-inflammatory cytokines: TNFα (−18%), IL-1β (−58%), IL-6 (−32%), IL-8 (−21%). It also exhibited a mild NO secretion inhibition (−13%) at the same concentration. The decoction was non-cytotoxic against L6 cells (IC50>100 µg/mL), RAW cells and PBMC. In vivo, 150 µL of the decoction given orally twice a day (equivalent to 350 mg/kg/day of dried extract) inhibited 39.7% average parasite growth, with more than 50% of inhibition in three mice over five. The absence of response for the two remaining mice, however, induced a strong standard deviation.
Conclusions:
This study highlighted the in vitro antiplasmodial activity of the decoction of P. acutangulum aerial parts, used by Wayana Amerindians from the Upper-Maroni in French Guiana in case of malaria. Its antioxidant and anti-inflammatory potential, which may help to explain its use against this disease, was demonstrated using models of artificially stimulated cells. |
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0378-8741 |
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EcoFoG @ webmaster @ |
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649 |
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Houel, E.; Bertani, S.; Bourdy, G.; Deharo, E.; Jullian, V.; Valentin, A.; Chevalley, S.; Stien, D. |
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Title |
Quassinoid constituents of Quassia amara L. leaf herbal tea. Impact on its antimalarial activity and cytotoxicity |
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Journal Article |
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Year |
2009 |
Publication |
Journal of Ethnopharmacology |
Abbreviated Journal |
J. Ethnopharmacol. |
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126 |
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1 |
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114-118 |
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Quassia amara L.; Simaroubaceae; Leaf tea; Antimalarial activity; Cytotoxicity; Simalikalactone D |
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Aim of the study: Our objective was to assess whether it could be contemplated to recommend Quassia amara young leaf tea for treatment against malaria. and if yes. set up a standard protocol for preparing the herbal tea. Materials and methods: The leaf tea was extracted with methylene chloride and the organic extract was fractionated with HPLC. Pure compounds were characterized and their in vitro cytotoxicity and antiplasmodial activity was determined. Results and discussion: We discovered that antimalarial Quassia amara young leaf tea contains several quassinoids: simalikalactone D (SkD. 1), picrasin B (2). picrasin H (3), neoquassin (4), quassin (5), picrasin 1(6) and picrasin J (7). These last two compounds are new. In addition. our experiments demonstrate that both biological activity and cytotoxicity of the remedy may be attributed solely to the presence of SkD. Conclusion: In conclusion, this preparation Should not be recommended for treatment of malaria until a clinical Study in humans is performed with SkD. (C) 2009 Elsevier Ireland Ltd. All rights reserved |
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[Stien, Didier] Univ Antilles Guyane, CNRS, UMR Ecofog, Inst Enseignement Super Guyane, F-97337 Cayenne, France, Email: didier.stien@guyane.cnrs.fr |
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ELSEVIER IRELAND LTD |
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0378-8741 |
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ISI:000271790800015 |
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EcoFoG @ eric.marcon @ |
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94 |
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Heu, Katy ; Romoli, Ottavia ; Schonbeck, Johan Claes ; Ajenoe, Rachel ; Epelboin, Yanouk ; Kircher, Verena ; Houel, Emeline ; Estevez, Yannick ; Gendrin, Mathilde |
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The Effect of Secondary Metabolites Produced by Serratia marcescens on Aedes aegypti and Its Microbiota |
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Journal Article |
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2021 |
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Frontiers in Microbiology |
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12 |
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645701 |
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Serratia marcescens is a bacterial species widely found in the environment, which very efficiently colonizes mosquitoes. In this study, we isolated a red-pigmented S. marcescens strain from our mosquito colony (called S. marcescens VA). This red pigmentation is caused by the production of prodigiosin, a molecule with antibacterial properties. To investigate the role of prodigiosin on mosquito- S. marcescens interactions, we produced two white mutants of S. marcescens VA by random mutagenesis. Whole genome sequencing and chemical analyses suggest that one mutant has a nonsense mutation in the gene encoding prodigiosin synthase, while the other one is deficient in the production of several types of secondary metabolites including prodigiosin and serratamolide. We used our mutants to investigate how S. marcescens secondary metabolites affect the mosquito and its microbiota. Our in vitro tests indicated that S. marcescens VA inhibits the growth of several mosquito microbiota isolates using a combination of prodigiosin and other secondary metabolites, corroborating published data. This strain requires secondary metabolites other than prodigiosin for its proteolytic and hemolytic activities. In the mosquito, we observed that S. marcescens VA is highly virulent to larvae in a prodigiosin-dependent manner, while its virulence on adults is lower and largely depends on other metabolites |
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Frontiers Media |
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EcoFoG @ webmaster @ |
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1024 |
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Fu, T.; Touboul, D.; Della-Negra, S.; Houel, E.; Amusant, N.; Duplais, C.; Fisher, G.L.; Brunelle, A. |
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Tandem Mass Spectrometry Imaging and in Situ Characterization of Bioactive Wood Metabolites in Amazonian Tree Species Sextonia rubra |
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2018 |
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Analytical Chemistry |
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Anal. Chem. |
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90 |
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12 |
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7535-7543 |
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Driven by a necessity for confident molecular identification at high spatial resolution, a new time-of-flight secondary ion mass spectrometry (TOF-SIMS) tandem mass spectrometry (tandem MS) imaging instrument has been recently developed. In this paper, the superior MS/MS spectrometry and imaging capability of this new tool is shown for natural product study. For the first time, via in situ analysis of the bioactive metabolites rubrynolide and rubrenolide in Amazonian tree species Sextonia rubra (Lauraceae), we were able both to analyze and to image by tandem MS the molecular products of natural biosynthesis. Despite the low abundance of the metabolites in the wood sample(s), efficient MS/MS analysis of these γ-lactone compounds was achieved, providing high confidence in the identification and localization. In addition, tandem MS imaging minimized the mass interferences and revealed specific localization of these metabolites primarily in the ray parenchyma cells but also in certain oil cells and, further, revealed the presence of previously unidentified γ-lactone, paving the way for future studies in biosynthesis. |
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American Chemical Society |
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0003-2700 |
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doi: 10.1021/acs.analchem.8b01157 |
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EcoFoG @ webmaster @ |
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834 |
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