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Congenital toxoplasmosis, caused by the opportunistic protozoan parasite T. gondii, can cause stillbirths, miscarriages and fetal abnormalities, as well as encephalitis and chorioretinitis in newborns. Available treatment options rely on antiparasitic drugs that have been linked to serious side effects, high toxicity and the development of drug-resistant parasites. The search for alternative therapeutics to treat this disease without acute toxicity for the mother and child is essential for the advancement of current therapeutic procedures. The present study aimed to unravel the mode of the anti-T. gondii action of Rottlerin, a natural polyphenol with multiple pharmacological properties described. Herein, we further assessed the antiparasitic activity of Rottlerin against T. gondii infection on the human trophoblastic cells (BeWo cells) and, for the first time, on human villous explants. We found that non-cytotoxic doses of Rottlerin impaired early and late steps of parasite infection with an irreversible manner in BeWo cells. Rottlerin caused parasite cell cycle arrest in G1 phase and compromised the ability of tachyzoites to infect new cells, thus highlighting the possible direct action on parasites. An additional and non-exclusive mechanism of action of Rottlerin involves the modulation of host cell components, by affecting lipid droplet formation, mitochondrial function and upregulation of the IL-6 and MIF levels in BeWo cells. Supporting our findings, Rottlerin also controlled T. gondii proliferation in villous explants with low toxicity and reduced the IL-10 levels, a cytokine associated with parasite susceptibility. Collectively, our results highlighted the potential use of Rottlerin as a promising tool to prevent and/or treat congenital toxoplasmosis.
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AIM: This paper reports on the antimycobacterial activity of the oleoresins and extracts obtained from Copaifera spp. MATERIALS & METHODS: The minimum inhibitory concentration (MIC) and fractional inhibitory concentration index techniques helped to evaluate the effect of these oleoresins and extracts against six strains of mycobacteria that cause tuberculosis. RESULTS & CONCLUSION: Among the assayed oleoresins and plant extracts, the Copaifera langsdorffii, Copaifera duckei, Copaifera reticulata and Copaifera trapezifolia oleoresins provided the lowest MIC values against some of the tested strains. The combination of Copaifera spp. samples with isoniazid did not evidence any synergistic action. Some Copaifera spp. oleoresins may represent a future source for the discovery of new antimycobacterial drugs due to their low MIC values.
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Considering the impact of dental caries on public health and the wide biological potential described for species belonging to the genus Pinus, here we investigate the antibacterial activity of the P. elliottii and P. tropicalis resins and of the diterpene dehydroabietic acid (DHA) against cariogenic bacteria. For this purpose, we have determined the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) of the resins and of the diterpene. We have also investigated the biofilm inhibition ability (through MBIC50 determination), as well as the synergistic effect (through fractional inhibitory concentration index) and the cytotoxic potential (through XTT assay) of the P. elliottii and P. tropicalis resins. The resins gave promising MIC and MBC values, which ranged from 12.5 to 400 µg/mL; DHA provided MIC and MBC values ranging from 25 to 400 µg/mL. The MICB50 values ranged from 0.78 to 400 µg/mL for the resins. Neither additive nor synergistic effects emerged for the combinations of one of the resins with chlorhexidine. The cytotoxic activity was ≥312.5 and ≥156.3 µg/mL for the P. elliottii and P. tropicalis resins, respectively. The resins showed antibacterial activity against planktonic and sessile cariogenic bacteria. These data are relevant and encourage further research into these plants, which may contribute to the discovery of new substances that can inhibit the growth of cariogenic microorganisms and reduce the incidence of dental caries.
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PURPOSE: To isolate Candida spp. from dental prosthesis users' saliva and to evaluate the isolates for the presence of several virulence factors. This research also aimed to investigate the antifungal activity of 3 commercial mouthwashes/oral antiseptic formulations containing 0.12% chlorhexidine, 0.07% cetylpyridinium, or 0.075% cetylpyridinium against planktonic and sessile (biofilm mode) yeast cells. MATERIALS AND METHODS: Forty-three Candida yeasts were isolated from 32 of 70 selected patients, and the virulence factors of C. albicans, C. krusei, C. glabrata, C. tropicalis, and C. parapsilosis species were investigated by polymerase chain reaction (PCR) and proteinase in plates. Minimum inhibitory concentration (MIC), and in vitro biofilm assay evaluated the antifungal activity of antiseptics. RESULTS: C. albicans, C. krusei, C. glabrata, C. tropicalis, and C. parapsilosis were detected in mono and mixed cultures. Only C. albicans displayed genes related to adhesion and proteinases (ALS2, ALS3, SAP1, and SAP3). The aspartate proteinase activity was found in 60.46% of isolates. The tested antiseptic formulations exhibited a MIC less than 1.25% toward yeasts in the planktonic mode. According to XTT ((2,3-bis(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide) assay results, most Candida isolates and all mixed cultures formed biofilms within 24 hours. The evaluated antiseptic formulations were also active against biofilms. CONCLUSION: Most virulence factors investigated here (ALS2, ALS3, SAP1, and SAP3) occurred in the majority of the Candida spp. isolates, especially in C. albicans. The tested mouthwash formulations were effective against all the yeast isolates in both the planktonic and sessile growth modes. Developing alternative therapies that can avoid or control biofilm formation is necessary to prevent oral candidiasis and other Candida spp. infections.
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Antiinfecciosos Locales , Prótesis Dental , Antifúngicos , Biopelículas , Candida , Humanos , Pruebas de Sensibilidad Microbiana , Factores de VirulenciaRESUMEN
Trees of the Copaifera genus are native to the tropical regions of Latin America and Western Africa. Copaifera sp is widely used as a popular medicine and it has various ethnopharmacological indications, including gonorrhea, bronchitis, asthma, skin ulcers, ulcers, sore throat, uterine infections, general inflammations, cancer, and leishmanioses. Kaurenoic acid is a naturally occurring diterpene found in Copaifera and has been used as an anti-inflammatory, treatment of ulcer, leishmaniasis, and cancer. Bearing in mind the fact that the Ames test is an excellent tool to assess the safety of extracts, oils, and phytochemicals isolated from medicinal plants, from it, we evaluate the mutagenic potential of four species, between oleoresins (C. oblongifolia; C. langsdorffii) and leaves extracts (C. lucens; C. multijuga), of the Copaifera genus and also of kaurenoic acid, which is one of its major compounds. The results showed that the Copaifera spp. and kaurenoic acid did not induce an increase in the number of revertant colonies, without mutagenic effect in experiments, in the all concentrations evaluated by Ames test. The results obtained in our study support the safe use of the Copaifera genus medicinal plants selected and of kaurenoic acid.
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Resumo Introdução A saúde bucal na atenção primária à saúde, com profissionais da Odontologia aptos nesse campo de atuação, tem sido descrita como promissora estratégia para se promover saúde. Objetivo Identificar e descrever as articulações intersetoriais e suas contribuições para a formação do profissional em Odontologia e para a saúde bucal de crianças de um município paulista. Material e método Pesquisa de campo, do tipo transversal, de abordagem mista e de caráter intervencionista. Dados secundários foram obtidos dos prontuários e relatórios de estagiários em Odontologia. Foram realizados atendimentos odontológicos a 455 crianças da rede básica de ensino e oito entrevistas com os familiares das crianças faltosas aos atendimentos. Foi utilizada estatística descritiva, com frequência simples e porcentagem, e Análise de Conteúdo para os dados qualitativos. Resultado Verificou-se que 42% das crianças encontravam-se em situação de alto risco à doença cárie. Os traumas e medos, e o escasso conhecimento de higiene bucal das crianças e dos pais influenciaram negativamente no cuidado com a saúde bucal. No consultório odontológico, as fragilidades apontadas pelos familiares foram o despreparo profissional, que vão desde questões técnicas até formas de abordagem pessoal. Conclusão Conclui-se que a prática na atenção primária à saúde aproximou os universitários da realidade social e ampliou e diversificou os cenários de ensino-aprendizagem com maior tempo para educação em saúde. Contudo, há necessidade de mais pesquisas sobre as experiências curriculares efetivas nessa temática.
Abstract Introduction Oral health in primary health care, with qualified dental professionals in this field, has been described as a promising strategy to promote health. Objective To identify and describe intersectoral articulations, and their contributions to dental professional education, and oral health of children from a city of São Paulo - Brazil. Material and method Field research, cross-sectional, mixed approach and interventionist character. Secondary data were obtained from medical records and reports of dental interns. Dental visits were performed to 455 children from the basic education system and eight interviews with the family members of the children who missed the visits. Descriptive statistics, with simple frequency and percentage, and Content Analysis were used for qualitative data. Result It was found that 42% of the children were at high risk for caries disease. Traumas, fears and poor knowledge of oral hygiene of children and parents had a negative influence on oral health care. In the dental office the weaknesses pointed out by family members were professional unpreparedness, ranging from technical issues to forms of personal approach. Conclusion It is concluded that the practice in primary health care brought the students closer to social reality, expanded and diversified the teaching-learning scenarios with longer time for health education. However, there is a need for further research on effective curriculum experiences in this area.
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Humanos , Niño , Atención Primaria de Salud , Salud Bucal , Estrategias de Salud Nacionales , Educación en Salud , Colaboración Intersectorial , Accesibilidad a los Servicios de SaludRESUMEN
Foodborne diseases (FBDs) are a serious public health concern worldwide. In this scenario, preservatives based on natural products, especially plants, have attracted researchers' attention because they offer potential antimicrobial action as well as reduced health impact. The genus Copaifera spp., which is native of tropical South America and West Africa, contains several species for which pharmacological activities, including antibacterial effects, have been described. On the basis of minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), antibiofilm activity (inhibition and eradication), preservative capacity, and Ames test, we evaluated the antibacterial, preservative, and mutagenic potential of Copaifera spp. oleoresins against the causative agents of FBDs. The Copaifera duckei, Copaifera reticulata, Copaifera paupera, and Copaifera pubiflora oleoresins displayed promising MIC/MBC values-from 12.5 to 100 µg/mL-against Staphylococcus aureus (American Type Culture Collection [ATCC] 29213), Listeria monocytogenes (ATCC 15313), and Bacillus cereus (ATCC 14579). C. duckei, C. reticulata, C. paupera, and C. pubiflora oleoresin concentrations ranging from 25 to 200 µg/mL and from 100 to 400 µg/mL inhibited biofilm formation and eradicated biofilms, respectively. The oleoresins did not exert mutagenic effects and had superior food preservative action to sodium benzoate (positive control). In conclusion, Copaifera oleoresins exhibit potential antibacterial activity and are not mutagenic, which makes them a promising source to develop novel natural food preservatives to inhibit foodborne pathogens.
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Right to health intertwines with right to the city: guaranteed access to healthy urban spaces reduces inequities among the population, so that disadvantaged groups can also enjoy positive urbanization effects. In this sense, interconnection between right to the city and right to health promotes equity. This article seeks to explore the interconnection between right to the city and right to health on the basis of an integrative review guided by the question 'What knowledge about right to the city and right to health has been produced in the light of equity?' For this purpose, we analyzed evidence available in the literature indexed in PubMed/Medline, Lilacs, and SciELO between 1986 and 2016. Over this three-decade span, we identified the presence of different degrees of right to the city and right to health in the formulation of policies and in social movement agendas. Formulations regarding population growth moved away from the rights agenda, but in a later phase of democratic consolidation, the fight for rights to health re-emerged. In a third moment of the political visibility of excluded geographical spaces and multiple identity agendas, the struggle to ensure everyone's right to the city came on strong in the game.
O direito à saude se interconecta com o direito à cidade na medida em que, ao se garantir espaços urbanos saudáveis para a população, garante-se também a redução de iniquidades e a expansão do usufruto dos efeitos positivos da urbanização a grupos postergados e desfavorecidos. A interconexão entre o direito à cidade e o direito à saúde é hipotetizado como propulsor necessário à promoção da equidade. Este artigo busca explorar esta interconexão entre o direito à cidade e o direito à saúde, ancorado em uma revisão integrativa, norteada pela questão: Qual o conhecimento produzido sobre o direito à cidade e o direito à saúde à luz da equidade? Analisaram-se evidências disponíveis na literatura indexadas no PubMed/Medline, Lilacs e SciELO, entre 1986 e 2016. Foram identificados nas três décadas analisadas distintos níveis de presença do direito à cidade e do direito à saúde na formulação de políticas e na agenda de revindicações dos movimentos sociais. Formulações em torno do crescimento populacional afastam da agenda os direitos, enquanto numa fase posterior o adensamento democrático revitaliza a luta pelos direitos à saúde. Num terceiro momento de visibilização política dos espaços geográficos excluídos e das agendas identitárias, entra forte no jogo a luta pelo direito de todos e todas à cidade.
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Política de Salud , Derechos Humanos , Salud Urbana , Población Urbana , Equidad en Salud , Humanos , Política , UrbanizaciónRESUMEN
Resumo O direito à saude se interconecta com o direito à cidade na medida em que, ao se garantir espaços urbanos saudáveis para a população, garante-se também a redução de iniquidades e a expansão do usufruto dos efeitos positivos da urbanização a grupos postergados e desfavorecidos. A interconexão entre o direito à cidade e o direito à saúde é hipotetizado como propulsor necessário à promoção da equidade. Este artigo busca explorar esta interconexão entre o direito à cidade e o direito à saúde, ancorado em uma revisão integrativa, norteada pela questão: Qual o conhecimento produzido sobre o direito à cidade e o direito à saúde à luz da equidade? Analisaram-se evidências disponíveis na literatura indexadas no PubMed/Medline, Lilacs e SciELO, entre 1986 e 2016. Foram identificados nas três décadas analisadas distintos níveis de presença do direito à cidade e do direito à saúde na formulação de políticas e na agenda de revindicações dos movimentos sociais. Formulações em torno do crescimento populacional afastam da agenda os direitos, enquanto numa fase posterior o adensamento democrático revitaliza a luta pelos direitos à saúde. Num terceiro momento de visibilização política dos espaços geográficos excluídos e das agendas identitárias, entra forte no jogo a luta pelo direito de todos e todas à cidade.
Abstract Right to health intertwines with right to the city: guaranteed access to healthy urban spaces reduces inequities among the population, so that disadvantaged groups can also enjoy positive urbanization effects. In this sense, interconnection between right to the city and right to health promotes equity. This article seeks to explore the interconnection between right to the city and right to health on the basis of an integrative review guided by the question 'What knowledge about right to the city and right to health has been produced in the light of equity?' For this purpose, we analyzed evidence available in the literature indexed in PubMed/Medline, Lilacs, and SciELO between 1986 and 2016. Over this three-decade span, we identified the presence of different degrees of right to the city and right to health in the formulation of policies and in social movement agendas. Formulations regarding population growth moved away from the rights agenda, but in a later phase of democratic consolidation, the fight for rights to health re-emerged. In a third moment of the political visibility of excluded geographical spaces and multiple identity agendas, the struggle to ensure everyone's right to the city came on strong in the game.
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Humanos , Población Urbana , Salud Urbana , Política de Salud , Derechos Humanos , Política , Urbanización , Equidad en SaludRESUMEN
The popular use of Annona muricata L. is based upon a range of medicinal purposes, and the plant exhibits biological activities including antihyperglycemic, antiparasitic, and antitumor activities. The objectives of this study were to examine the antioxidant, cytotoxic, and genotoxic potential of the hydroalcoholic extract of A. muricata leaves (AMEs), as well as its effects on genotoxicity induced by methyl methanesulfonate (MMS) and hydrogen peroxide (H2O2). The results using 2,2-diphenyl-1-picrylhydrazyl assay showed that AME was able to scavenge 44.71% of free radicals. The extract significantly reduced the viability of V79 cells in the clonogenic assay at concentrations ≥8 µg/ml. No significant differences in micronucleus (MN) frequency were observed between V79 cell cultures treated with different concentrations of the extract (0.125, 0.25, 0.5, and 1 µg/ml) and negative control. When AME concentrations were combined with MMS, data revealed no marked differences from mutagen alone. In contrast, significant reductions in the frequencies of MN were noted in cultures treated with AME combined with H2O2 compared to H2O2 alone. In vivo studies found no significant differences in the frequencies of micronucleated polychromatic erythrocytes (MNPCEs) between animals treated with different AME doses compared to control. Animals treated with AME doses of 125 and 250 mg/kg and MMS exhibited significantly higher frequencies of MNPCE compared to mutagen alone. In conclusion, under current experimental conditions, AME was not genotoxic and exerted a modulatory effect on DNA damage depending upon the experimental conditions. The extract did not influence markedly MMS-induced genotoxicity in in vitro test system. However, the extract increased DNA damage induced by mutagen in mice. In V79 cells, AME reduced the genotoxicity produced by H2O2, and this protective effect was attributed in part to the antioxidant activity of AME.
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Annona/química , Antioxidantes/química , Daño del ADN , Genoma de Planta/efectos de los fármacos , Inestabilidad Genómica/efectos de los fármacos , Hojas de la Planta/química , Compuestos de Bifenilo/química , Peróxido de Hidrógeno/química , Metilmetanosulfonato/química , Picratos/química , Extractos Vegetales/toxicidadRESUMEN
Fungi can cause various diseases, and some pathogenic fungi have been detected in the water of dental equipment. This environment offers suitable conditions for fungal biofilms to emerge, which can facilitate mycological contamination. This study verified whether the water employed in the dental units of two dental clinics at the University of Franca was contaminated with fungi. This study also evaluated the ability of the detected fungi to form biofilms. The high-revving engine contained the largest average amount of fungi, 14.93 ± 18.18 CFU/mL. The main fungal species verified in this equipment belonged to the genera Aspergillus spp., Fusarium spp., Candida spp., and Rhodotorula spp. Among the isolated filamentous fungi, only one fungus of the genus Fusarium spp. did not form biofilms. As for yeasts, all the Candida spp. isolates grew as biofilm, but none of the Rhodotorula spp. isolates demonstrated this ability. Given that professionals and patients are often exposed to water and aerosols generated by the dental procedure, the several fungal species detected herein represent a potential risk especially to immunocompromised patients undergoing dental treatment. Therefore, frequent microbiological monitoring of the water employed in dental equipment is crucial to reduce the presence of contaminants.
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Equipo Dental/microbiología , Contaminación de Equipos , Microbiología del Agua , Aspergillus/aislamiento & purificación , Candida/aislamiento & purificación , Fusarium/aislamiento & purificación , Humanos , Micosis/microbiología , Rhodotorula/aislamiento & purificaciónRESUMEN
The compounds terrein (1), butyrolactone I (2), and butyrolactone V (3) were isolated from the ethyl acetate extract (EtOAc) of the endophytic fungus Aspergillus terreus-F7 obtained from Hyptis suaveolens (L.) Poit. The extract and the compounds presented schistosomicidal activity against Schistosoma mansoni; at 100 µg/mL for EtOAc extract, 1297.3 µM for compound 1, 235.6 µM for compound 2, and 454.1 µM for compound 3, they killed 100% of the parasites after 72 h of treatment. Compounds 1, 2, and 3 exerted moderate leishmanicidal activity against Leishmania amazonensis (IC50 ranged from 23.7 to 78.6 µM). At 235.6 and 227.0 µM, compounds 2 and 3, respectively, scavenged 95.92 and 95.12% of the DPPH radical (2,2-diphenyl-1-picryl-hydrazyl), respectively. Regarding the cytotoxicity against the breast tumor cell lines MDA-MB-231 and MCF-7, compound 2 gave IC50 of 34.4 and 17.4 µM, respectively, while compound 3 afforded IC50 of 22.2 and 31.9 µM, respectively. At 117.6 µM, compound 2 inhibited the growth of and killed the pathogen Escherichia coli (ATCC 25922). Compounds 1, 2, and 3 displayed low toxicity against the normal line of human lung fibroblasts (GM07492A cells), with IC50 of 15.3 × 103, 3.4 × 103, and 5.8 × 103 µM, respectively. This is the first report on (i) the in vitro schistosomicidal and leishmanicidal activities of the EtOAc extract of A. terreus-F7 and compounds 1, 2, and 3; and (ii) the antitumor activity of compounds 2 and 3 against MDA-MB-231 and MCF-7 cells.
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Aspergillus/química , Ciclopentanos/farmacología , Furanos/farmacología , Hyptis/microbiología , Lactonas/farmacología , 4-Butirolactona/análogos & derivados , 4-Butirolactona/aislamiento & purificación , Animales , Antihelmínticos/aislamiento & purificación , Antihelmínticos/farmacología , Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología , Antiprotozoarios/aislamiento & purificación , Antiprotozoarios/farmacología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Ciclopentanos/aislamiento & purificación , Endófitos/metabolismo , Furanos/aislamiento & purificación , Humanos , Lactonas/aislamiento & purificación , Leishmania/efectos de los fármacos , Células MCF-7 , Schistosoma/efectos de los fármacosRESUMEN
Persea americana Mill., commonly known as avocado, is a tree native to Central America that is widely used as a food source and for the treatment of diseases. This plant has various biological properties such as analgesic, anti-inflammatory and total cholesterol-lowering activity. In view of its pharmacological potential, we conducted a toxicogenetic study of the fruit pulp oil of P. americana (PAO) and investigated its influence on genotoxicity induced by methyl methanesulfonate (MMS) and doxorubicin. V79 cells and Swiss mice were used for the assays. The results showed no genotoxic effects of PAO in the in vitro or in vivo test systems. However, the highest PAO dose tested led to an increase in the levels of aspartate aminotransferase, indicating hepatic/tissue damage. This effect may be related to high concentrations of palmitic acid, the main component of PAO. Furthermore, PAO was effective in reducing the chromosome damage induced by MMS and doxorubicin. These results contribute to the safety assessment of PAO as a medicinal plant for human use.
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Aberraciones Cromosómicas/efectos de los fármacos , Daño del ADN/efectos de los fármacos , Frutas/química , Inestabilidad Genómica/efectos de los fármacos , Persea/química , Extractos Vegetales/toxicidad , Toxicogenética/métodos , Animales , Antibióticos Antineoplásicos/toxicidad , Aspartato Aminotransferasas/metabolismo , Bioensayo/métodos , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Cricetulus , Doxorrubicina/toxicidad , Fibroblastos/citología , Fibroblastos/efectos de los fármacos , Fibroblastos/metabolismo , Cromatografía de Gases y Espectrometría de Masas/métodos , Humanos , Pulmón/citología , Pulmón/efectos de los fármacos , Pulmón/metabolismo , Masculino , Metilmetanosulfonato/toxicidad , Ratones , Pruebas de MicronúcleosRESUMEN
Dental prosthesis supports Candida species growth and may predispose the oral cavity to lesions. C. tropicalis has emerged as a colonizer of prosthesis and has shown resistance to clinically used antifungal agents, which has increased the search for new antifungals. This work describes the effectiveness of fifteen essential oils (EOs) against C. tropicalis The EOs were obtained by hydrodistillation and were chemically characterized by gas chromatography-mass spectrometry. The antifungal activities of the EOs were evaluated by the microdilution method and showed that Pelargonium graveolens (Geraniaceae) (PG-EO) was the most effective oil. Geraniol and linalool were the major constituents of PG-EO. The 2,3-Bis-(2-Methoxy-4-Nitro-5-Sulfophenyl)-2H-Tetrazolium-5-Carboxanilide (XTT) assay showed that all the clinical C. tropicalis strains formed viable biofilms. Scanning electron microscopy examination of the biofilms revealed a complex architecture with basal layer of yeast cells and an upper layer of filamentous cells. Treatments with PG-EO, linalool, and geraniol significantly reduced the number of viable biofilm cells and inhibited biofilm formation after exposure for 48 h. PG-EO, geraniol, and linalool were not toxic to normal human lung fibroblasts (GM07492A) at the concentrations they were active against C. tropicalis Together, our results indicated that C. tropicalis is susceptible to treatment with PG-EO, geraniol, and linalool, which could become options to prevent or treat this infection.
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Antifúngicos/farmacología , Biopelículas/efectos de los fármacos , Candida tropicalis/efectos de los fármacos , Aceites Volátiles/farmacología , Pelargonium/química , Monoterpenos Acíclicos , Antifúngicos/química , Antifúngicos/aislamiento & purificación , Antifúngicos/toxicidad , Candida tropicalis/fisiología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Fibroblastos/efectos de los fármacos , Fibroblastos/fisiología , Cromatografía de Gases y Espectrometría de Masas , Humanos , Pruebas de Sensibilidad Microbiana , Viabilidad Microbiana/efectos de los fármacos , Microscopía Electrónica de Rastreo , Monoterpenos/aislamiento & purificación , Monoterpenos/farmacología , Monoterpenos/toxicidad , Aceites Volátiles/química , Aceites Volátiles/aislamiento & purificación , Aceites Volátiles/toxicidad , Terpenos/aislamiento & purificación , Terpenos/farmacología , Terpenos/toxicidadRESUMEN
The benzofuran lignans egonol and homoegonol are found in all species of the genus Styrax. Since natural products are important sources of new anticancer drugs, this study evaluated the cytotoxic activity of a hydroalcoholic extract of the stems of S. camporum (SCHE) and their chemical markers, egonol (EG) and homoegonol (HE), against different tumor cell lines (B16F10, MCF-7, HeLa, HepG2, and MO59J). A normal human cell line (GM07492A) was included. Cytotoxic activity was evaluated at different treatment times (24, 48 and 72 h) using the XTT assay. More effective results were observed after 72 h of treatment. The lowest IC50 values were found for the HepG2 cell line, ranging from 11.2 to 55.0 µg/mL. The combination of EG and HE exerted higher cytotoxic activity than SCHE or treatment with either lignan alone, with the lowest IC50 (13.31 µg/mL) being observed for the MCF-7 line. Furthermore, treatment with these lignans was significantly more cytotoxic for some tumor cell lines compared to the normal cell line, GM07492A, indicating selectivity. These results suggest that these lignans may be used to treat cancer without affecting normal cells.
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Novel gold(I) and gold(III) complexes containing derivatives of D-galactose, D-ribose and D-glucono-1,5-lactone as ligands were synthesized and characterized by IR, (1)H, and (13)C NMR, high resolution mass spectra and cyclic voltammetry. The compounds were evaluated in vitro for their cytotoxicity against three types of tumor cells: cervical carcinoma (HeLa) breast adenocarcinoma (MCF-7) and glioblastoma (MO59J) and one non-tumor cell line: human lung fibroblasts (GM07492A). Their antitubercular activity was evaluated as well expressed as the minimum inhibitory concentration (MIC90) in µg/mL. In general, the gold(I) complexes were more active than gold(III) complexes, for example, the gold(I) complex (1) was about 8.8 times and 7.6 times more cytotoxic than gold(III) complex (8) in MO59J and MCF-7 cells, respectively. Ribose and alkyl phosphine derivative complexes were more active than galactose and aryl phosphine complexes. The presence of a thiazolidine ring did not improve the cytotoxicity. The study of the cytotoxic activity revealed effective antitumor activities for the gold(I) complexes, being more active than cisplatin in all the tested tumor cell lines. Gold(I) compounds (1), (2), (3), (4) and (6) exhibited relevant antitubercular activity even when compared with first line drugs such as rifampicin.