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Central depressant effects of Piper tuberculatum Jacq essential oil in mice

Food Bioscience 2022年第4期48卷 620-629页

作者： Valterlúcio dos Santos Sales Francisco Romero Cabral Emmily Petícia do Nascimento Sales Tatyelle Bezerra Carvalho Maria Haiele Nogueira costa Victor Afonso Pereira de Oliveira Cristina Kelly de Souza Rodrigues Francisco Rodolpho Sobreira dantas Nobrega de Figueiredo daniel Souza Bezerra Gyllyandeson de Araújo Delmondes Henrique Douglas Melo Coutinho jose galberto martins da costa Irwin Rose Alencar de Menezes Cícero Francisco Bezerra Felipe Marta Regina Kerntopf Universidade Regional do Cariri Departamento de Química Biol´ogicaCratoCear´aBrazil Universidade Federal de S˜ao Paulo-Departamento de Fisiologia S˜ao PauloSPBrazil Faculdade de Ciˆencias M´edicas da Santa Casa de S˜ao Paulo S˜ao PauloSPBrazil Universidade Federal da Paraíba Departamento de Biologia MolecularJo˜ao PessoaParaíbaBrazil

This study aims to investigate the toxicity and possible effects and mechanism of action of the essential oil obtained from the Piper tuberculatum Jacq.‘s fruit(EOPT)on the central nervous system(CNS)of *** the Hippocratic test,it was observed ambulation reduction,sedation,piloerection and mortality of 25%at the dose of 1000 mg/kg and 50%at the dose of 5000 mg/*** results found demonstrate that the EOPT is endowed with a possible depressant effect,and is characterized by a likely sedative(open field test),anxiolytic-like(elevated plus maze test),anticonvulsant(pentylenetetrazole-induced seizure test)and hypnotic action(pentobarbital-induced sleeping time).These effects may possibly occur due to the interaction between the monoterpenes,present in its essential oil,and the GABAergic pathway confirmed by reversion of the effects by ***,these results demonstrate the therapeutic potential and the validation of the ethnopharmacological use of this species in the treatment of disorders affecting the central nervous system.

关键词： Piper tuberculatum Jacq. Essential oil Sedative Anxiolytic Hypnotic

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Chemical profile and antimicrobial activity of Secondatia floribunda A. DC(Apocynaceae)

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Asian Pacific Journal of Tropical Biomedicine 2017年第8期7卷 739-749页

作者： daiany Alves Ribeiro Sarah Soares damasceno Aline Augusti Boligon Irwin Rose Alencar de Menezes Marta Maria de Almeida Souza Joségalberto martins da costa Programa de Pós-Graduacao em Etnobiologia e Conservacao da Natureza Universidade Regional do Cariri Departamento de Química Biológica Laboratório de Pesquisas de Produtos NaturaisUniversidade Regional do Cariri Laboratório de Fitoquímica Universidade Federal de Santa Maria Departamento de Química Biológica Laboratório de Farmacologia e Química MolecularUniversidade Regional do Cariri Departamento de Ciências Biológicas Laboratório de Ecologia VegetalUniversidade Regional do Cariri

To establish the chemical profile, and to evaluate the antibacterial and modulatory activity of the ethanolic extracts of the stalk’s inner bark and heartwood of Secondatia *** of total phenols and flavonoids was determined by the Folin-Ciocalteu method and aluminum chloride, respectively. Phenolic compounds were identified and quantified by HPLC-daD (High Performance Liquid Chromatography-Diodearray Detector) and the Infrared Spectroscopy was performed using the measure by Attenuated Total Reflectance with Fourier Transform (ATR-FTIR). Antibacterial assays for determination of the Minimum Inhibitory Concentration (MIC) and modification of aminoglycosides were performed by *** spectra showed similar characteristics, having among its main absorption bands hydroxyl group (OH). The antibacterial activity showed clinically significant results for the strains of Staphylococcus aureus and Escherichia coli. In modulation assay, synergic and antagonistic effect for both extracts was observed. Heartwood extract in combination with antibiotics showed a significant MIC reduction at 19.8% (P datia floribunda suggesting that it is clinically relevant source of a new antibacterial therapy, especially due to the presence of significant levels of phenolic compounds.

关键词： Chemical composition HPLC Cinchonain Natural product Modification resistance

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In vitro antileishmanial effects of Physalis angulata root extract on Leishmania infantum

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Journal of Integrative Medicine 2018年第6期16卷 404-410页

作者： Bruno jose martins da Silva Sandro Wilson Gomes Pereira Ana Paula Drummond Rodrigues jose Luiz martins Do Nascimento Edilene Oliveira Silva Laboratory of Structural Biology Institute of Biological SciencesFederal University of PardBelemPard 66075-110Brazil National Institute of Science and Technology in Structural Biology and Bioimaging(INCT-INBEB) Rio de Janeiro 21941-901Brazil Laboratory of Electron Microscopy Department of Health SurveillanceMinistry of HealthEvandro Chagas InstituteBelemPard 66087-082Brazil Laboratory of Molecular and Cellular Neurochemistry Institute of Biological SciencesFederal University of PardBelemPard 66075-110Brazil National Institute of Science and Technology in Neuroimmunomodulation(INCT-NIM) Rio de Janeiro 21040-360Brazil

Objective： In the present study, we evaluated the effects of the aqueous extract of Physalis angulata root （AEPa） on Leishmania infanturn proliferation, morphology, and the driving mechanism in leishmanicidal activity and modulatory action on macrophages. Methods： I., infantum promastigotes were treated with 50 and 100 μg/mL AEPa for 72 h and then antipro- mastigote assay was performed by counts in a Newbauer chamber, morphological changes were analyzed by transmission electron microscopy and the mechanism of the leishmanicidal activity was detected. In addition, macrophages were infected with L. infantum and were used to evaluate anti-amastigote activity of AEPa and effects of AEPa on cytokine secretion after 72-hour treatment. Results： Treatment with AEPa reduced the numbers ofL infantum promastigotes （50% inhibitory concen- tration （ICso） = 65.9μg/mL; selectivity index （SI）= 22.1） and amastigotes （ICso = 37.9 μg/mL; SI = 38.5） compared with the untreated control. Amphotericin B reduced 100% of the promastigote numbers after 72 h of treatment （IC50 = 0.2μg/mL）. AEPa induced several morphological changes and increased the production of reactive oxygen species and apoptotic death in promastigotes after treating for 72 h. AEPa （100 μg/mL） promoted tumor necrosis factor-α secretion in macrophages infected with L. infantum after 72 h of treatment, but did not induce an increase in this cytokine in noninfected macrophages. In addition, AEPa showed no cytotoxic effect on J774-A1 cells （50% cytotoxic concentration 〉1000μg/mL）. Conclusion： AEPa presented antileishmanial activity against the promastigotes and amastigotes of I.. infantum without macrophage cytotoxicity; these results show that natural products such as P. angulata have leishmanicidal potential and in the future may be an alternative treatment for leishmaniasis.

关键词： Leishmanicidal activity Leishmania infantum Reactive oxygen species Apoptosis Physalis angulata

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Anti-inflammatory effects ofα-humulene andβ-caryophyllene on pterygium fibroblasts

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International Journal of Ophthalmology(English edition) 2022年第12期15卷 1903-1907页

作者： Magda Massae Hata Viveiros Márcia Guimarães Silva Joségalberto martins da costa Anselmo Gomes de Oliveira Carolina Rubio Carlos Roberto Padovani Cláudia Aparecida Rainho Silvana Artioli Schellini Department of Ophthalmology School of Medicine of BotucatuSão Paulo State University–UNESPBotucatuSao Paulo 18618-000Brazil Department of Pathology School of Medicine of BotucatuSão Paulo State University–UNESPBotucatuSao Paulo 01049-010Brazil Department of Biological Chemistry Regional University of CaririCratoCeará66100-900Brazil Department of Pharmacology School of Pharmaceutical SciencesSão Paulo State University–UNESPAraraquaraSao Paulo 01049-010Brazil Biological Sciences Institute of Biosciences of BotucatuSão Paulo State University–UNESPBotucatuSao Paulo 01049-010Brazil Department of Biostatistics São Paulo State University–UNESPBotucatuSao Paulo 01049-010Brazil

AIM:To investigate the anti-inflammatory effects of the sesquiterpenesα-humulene andβ-caryophyllene on pterygium ***:Primary cultures of pterygium fibroblasts were *** passage pterygium fibroblasts were exposed toα-humulene andβ-caryophyllene separately and *** cell viability was assessed by 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide(MTT)assay at 12,24,48,and 72h after *** levels of the inflammatory cytokines interleukin(IL)-1β,IL-6,IL-8,tumor necrosis factor(TNF)-αand IL-10 in the conditioned culture medium were assessed by enzymelinked immunosorbent assay(ELISA)at 12,24 and 48h after *** were statistically analyzed using Friedman repeated measures analysis of variances on ***:The 25μmol/Lβ-caryophyllene induced significant decrease in the IL-6 production by pterygium fibroblasts 48h after the exposure(P=0.041).The levels of IL-1β,IL-8,IL-10,and TNF-αwere very low and had no statistically significant variations af ter exposure toα-humulene,β-caryophyllene,or both compounds ***:The exposure to 25μmol/L ofβ-caryophyllene significantly reduce the production of IL-6 by pterygium fibroblasts after *** sesquiterpene may be a potential alternative adjuvant agent for the treatment of pterygium.

关键词： pterygium fibroblasts β-caryophyllene α-humulene cytokines

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LC–MS characterization, anti-kinetoplastide and cytotoxic activities of natural products from Eugenia jambolana Lam. and Eugenia uniflora

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Asian Pacific Journal of Tropical Biomedicine 2017年第9期7卷 836-841页

作者： Celestina Elba Sobral de Souza Ana Raquel Pereira da Silva Janaina Esmeraldo Rocha Maria Celeste Vega Gomez Míriam Rolóm Cathia Coronel José galberto martins da costa Manoel L.C.Netto Larissa A.Rolim Henrique Douglas Melo Coutinho Laboratório de Microbiologia e Biologia Molecular Universidade Regional do Cariri Center for the Development of Scientific Research Moisés Bertoni Foundation/Díaz Gill Laboratories Laboratório de Pesquisa de Produtos Naturais Universidade Regional do Cariri Centro Universitário Dr.Leao Sampaio–UNILEAO Universidade Federal do Vale do Sao Francisco–UNIVASF

Objective: To evaluate the trypanocidal, leishmanicidal and cytotoxic activity of Eugenia jambolana(E. jambolana) and Eugenia uniflora(E. uniflora) extracts and ***: The products were characterized by LC–MS. Antiparasitic assays were performed and cytotoxicity was evaluated in fibroblastos. In vitro assays were performed using spectrophotometric evaluation. All assays were performed in ***: The results showed that the extracts and the tannic fraction from E. jambolana inhibited 100% of the epimastigote lines. The ethanolic extract was the most efficient in all concentrations tested against the three parasite strains. In the cytotoxicity assay the flavonoid fraction showed low toxicity. All E. uniflora samples showed cytotoxicity at the highest concentration tested, but the extract showed no toxic effect on the fibroblasts at the lowest concentration. The flavonoid and tannic fractions were more efficient against Leishmania braziliensis promastigotes compared to the extract. However, the extracts and the tannic fraction were more effective against Leishmania infantum strains. The effect on epimastigote cells was observed at all concentrations tested, with all E. uniflora samples. However, the samples were more effective at the highest concentration, where there was inhibition in 100% of the Trypanosoma cruzi ***: The species E. jambolana and E. uniflora presented antiparasitic activity against all tested parasite strains, indicating that these species can serve as an alternative therapy as they were efficient in the tests performed. The E. uniflora extract and the E. jambolana flavonoid fraction presented a low cytotoxicity, opening the floor for new biological studies.

关键词： Antiparasitic effect Cytotoxicity Eugenia jambolana Eugenia uniflora

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Medicinal plants from the Brazilian Amazonian region and their antileishmanial activity:a review

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Journal of Integrative Medicine 2018年第4期16卷 211-222页

作者： Bruno jose martins da Silva Amanda Anastacia Pinto Hage Edilene Oliveira Silva Ana Paula Drummond Rodrigues Laboratory of Parasitology and Laboratory of Structural Biology Institute of Biological SdencesFederal University of PardBelemPard 66075-110Brazil National Institute of Science and Technology in Structural Biology and Bioimaging Rio de JaneiroRio de Janeiro 21941-901Brazil Laboratory of Electron Microscopy Department of Health SurveillanceMinistry of HealthEvandro Chagas InstituteBelemPard 66087-082Brazil

Leishmaniasis, a neglected disease caused by Leishmania protozoans, primarily affects people in tropical and subtropical areas. Chemotherapy based on the use of pentavalent antimonials, amphotericin B, paromomycin, miltefosine and liposomal amphotericin B is currently the only effective treatment. However, adverse effects, long-term treatment and the emergence of parasite resistance have led to the search for alternative treatments. Natural products used in traditional medicine provide an unlimited source of molecules for the identification of new drugs, and the Amazon region has abundant biodiversity that includes several species of plants and animals, providing a rich source of new products and com- pounds. Although the literature describes numerous promising compounds and extracts for combating Leishmania protozoans, the results of such research have not been embraced by the pharmaceutical industry for the development of new drugs. Therefore, this review focused on the antileishmanial activity of extracts, isolated compounds and essential oils commonly used by the local population in the Brazilian Amazonian region to treat several illnesses and described in the literature as promising compounds for combating leishmaniasis.

关键词： Amazonian plants Leishmaniasis treatment Plant compounds Plant extracts Plant oils

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Antibacterial activity and inhibition against Staphylococcus aureus NorA efflux pump by ferulic acid and its esterified derivatives

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Asian Pacific Journal of Tropical Biomedicine 2021年第9期11卷 405-413页

作者： Patrícia Gonçalves Pinheiro Gilvandete Maria Pinheiro Santiago Francisco Erivaldo Freitas da Silva Ana Carolina Justino de Araújo Cícera Rejane Tavares de Oliveira Priscilla Ramos Freitas Janaína Esmeraldo Rocha JoséBezerra de Araújo Neto Maria Milene costa da Silva Saulo Relison Tintino Irwin Rose Alencar de Menezes Henrique Douglas Melo Coutinho Joségalberto martins da costa Departamento de Química Biológica Programa de Pos-Graduação em Química BiológicaUniversidade Regional do Cariri–URCACrato–CEBrazil Programa de Pós-Graduação em Química Centro de CiênciasUniversidade Federal do Ceará–UFCFortaleza–CEBrazil

Objective:To evaluate the inhibitory activity of ferulic acid and four of its esterified derivatives(methyl,ethyl,propyl,and butyl)against resistance mechanisms in Staphylococcus aureus ***:Ferulic acid derivatives were obtained by esterification with methanol,ethanol,propanol,and butanol,and then characterized by hydrogen and carbon-13 nuclear magnetic resonance *** minimum inhibitory concentrations(MIC)of ferulic acid and its esterified derivatives,ethidium bromide,and norfloxacin were obtained using the microdilution test,while the efflux pump inhibition test was conducted by examining reduction in the MICs of norfloxacin and ethidium *** docking was also carried out using the Schrodinger Suite 2015 molecular modeling software.A three-dimensional model of NorA efflux pump was generated using *** best scoring model was used as a receptor for ligand-receptor ***:The methyl and butyl ester derivatives did not demonstrate significant antimicrobial ***,a significant synergic effect was evidenced when norfloxacin was combined with the ethyl and propyl esterified *** docking study demonstrated favorable energy of interaction between ferulate derivatives and NorA,and amino acid residues TYR57,TYR58,and LEU255 were present commonly in stabilizing all *** PCA analysis corroborated the docking hypothesis that the lipophilic character and hydrogen bond interactions were the most relevant characteristics involved with NorA *** pharmacokinetic parameters of ferulic acid derivatives showed good ADMET properties,demonstrating that they can be easily absorbed and have no effect or inhibit the cytochrome P450 enzyme complex,revealing their potential as drug ***:This study provides strong evidence that the molecular basis for this activity is potentially due to the NorA efflux pump.

关键词： Ferulic acid Esterified derivatives Efflux pump Staphylococcus aureus Resistance mechanisms

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Antibacterial enhancement of antibiotic activity by Enterolobium contortisiliquum(Vell.)Morong

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Asian Pacific Journal of Tropical Biomedicine 2017年第10期7卷 945-949页

作者： Zildene de Sousa Silveira Nair Silva Macêdo Thiago Sampaio de Freitas Ana Raquel Pereira da Silva Joycy Francely Sampaio dos Santos Maria Flaviana Bezerra Morais-Braga José galberto martins da costa Raimundo Nonato Pereira Teixeira Jean Paul Kamdem Henrique Douglas Melo Coutinho Francisco Assis Bezerra da Cunha Laboratorio de Bioprospeccao do Semioarido Universidade Regional do CaririCratoBrazil Laboratorio de Microbiologia e Biologia Molecular Universidade Regional do CaririCratoBrazil Laboratorio de Pesquisas de Produtos Naturais Universidade Regional do CaririCratoBrazil Departamento de Ciencias biologicas Universidade Regional do Cariri-URCACratoCEP:63105-000Brazil Programa de Pos-graduacao em Bioprospeccao Molecular Universidade Regional do Cariri–URCACratoBrazil

Objective: To identify the main chemical classes of compounds from aqueous extract of Enterolobium contortisiliquum(E. contortisiliquum) seed bark and to evaluate its antibacterial activity, as well as its potential to increase the activity of antibiotics against strains of Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia ***: Different classes of compounds in the aqueous extract of E. contortisiliquum were evaluated based on the visual changes in the coloration and the formation of precipitate after the addition of specific reagents. The antibacterial activity of the extract and its potential to increase of antibiotic activity of antibiotics drugs, gentamicin and norfloxacin was determined by using the microdilution ***: Our results demonstrated that the following secondary metabolites were presented in E. contortisiliquum seed bark: flavones, flavonols, xanthones, flavononols,chalcones, aurones, flavones and catechins. The extract itself had very low antibacterial activity against all bacterial strains tested(MIC ≥ 1024 μg/m L), but there was an increase in the antibiotic activity of gentamicin and norfloxacin when combined in the subinhibitory concentration(i.e., MIC/8).Conclusions: Our data suggests that E. contortisiliquum seed bark may be an alternative source for new drugs with the potential to increase antibiotic activity against different strains of bacteria.

关键词： Antibiotic activity Enhancement Synergism Chemical compounds Bioactivity

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Feature reduction with PCA/ KPCA for gait classification with different assistive devices

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International Journal of Intelligent Computing and Cybernetics 2015年第4期8卷 363-382页

作者： Maria martins Cristina Santos Lino costa Anselmo Frizera Algoritimi Center Minho UniversityGuimarãesPortugal Electrical Engineering Department Federal University of Espirito SantoVitóriaBrazil

Purpose–The purpose of this paper is to propose a gait analysis technique that aims to identify differences and similarities in gait performance between three different assistive devices(ADs).Design/methodology/approach–Two feature reduction techniques,linear principal component analysis(PCA)and nonlinear kernel-PCA(KPCA),are expanded to provide a comparison of the spatio-temporal,symmetrical indexes and postural control parameters among the three different ***,a multiclass support vector machine(MSVM)with different approaches is designed to evaluate the potential of PCA and KPCA to extract relevant gait features that can differentiate between ***–Results demonstrated that symmetrical indexes and postural control parameters are better suited to provide useful information about the different gait patterns that total knee arthroplasty(TKA)patients present when walking with different *** combination of KPCA and MSVM with discriminant functions(MSVM DF)resulted in a noticeably improved *** combination demonstrated that,with symmetric indexes and postural control parameters,it is possible to extract with high-accuracy nonlinear gait features for automatic classification of gait patterns with ***/value–The information obtained with the proposed technique could be used to identify benefits and limitations of ADs on the rehabilitation process and to evaluate the benefit of their use in TKA patients.

关键词： Decision theory Support vector machines

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Renin-angiotensin system in the pathogenesis of liver fibrosis

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World Journal of Gastroenterology 2009年第21期15卷 2579-2586页

作者： Regina Maria Pereira Robson Augusto Souza dos Santos Filipi Leles da costa Dias Mauro martins Teixeira Ana Cristina Simoes e Silva Department of Pediatrics Faculty of MedicineFederal University of Minas Gerais Laboratory of Hypertension Department of Physiology and BiophysicsInstitute of Biological SciencesFederal University of Minas Gerais Laboratory of Immunopharmacology Department of Biochemistry and ImmunologyInstitute of Biological SciencesFederal University of Minas Gerais

Hepatic fibrosis is considered a common response to many chronic hepatic injuries. It is a multifunctional process that involves several cell types, cytokines, chemokines and growth factors leading to a disruption of homeostatic mechanisms that maintain the liver ecosystem. In spite of many studies regarding the development of fibrosis, the understanding of the pathogenesis remains obscure. The hepatic tissue remodeling process is highly complex, resulting from the balance between collagen degradation and synthesis. Among the many mediators that take part in this process, the components of the Renin angiotensin system （RAS） have progressively assumed an important role. Angiotensin （Ang） II acts as a profibrotic mediator and Ang-（1-7）, the newly recognized RAS component, appears to exert a counter-regulatory role in liver tissue. We briefly review the liver fibrosis process and current aspects of the RAS. This review also aims to discuss some experimental evidence regarding the participation of RAS mediators in the pathogenesis of liver fibrosis, focusing on the putative role of the ACE2-Ang-（1-7）- Mas receptor axis.

关键词： Hepatic fibrosis Renin angiotensin system Angiotensin II Angiotensin-(1-7) Receptor Mas Angiotensin converting enzyme 2

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