The prevalence of candidosis in denture wearers is as well established as its treatment with antifungal agents (AAs). However, little research has been done regarding the effects of AAs on denture base surfaces. Therefore, the aim of this study was to evaluate the effects of fluconazole (FLU), nystatin (NYS) and propolis orabase gel (PRO) on poly (methyl-methacrylate) (PMMA) surfaces. Deionized water and orabase gel without any active component were used as control groups. Conventional heat-polymerized (Clássico) and microwave-polymerized (Onda Cryl) acrylic resins were used. After polymerization, the specimens were polished and had their surfaces evaluated for roughness, free energy and Knoop hardness. Subsequently, specimens were immersed in AAs and controls for 14 days at 35±2 ºC and all variables were measured again. Data were analyzed statistically by 2-way ANOVA followed by Tukey's test ( α=0.05). Roughness results showed similar behavior for both PMMA resins, with PRO reaching the highest values and differing significantly from the other AAs (p<0.05). No statistically significant differences (p>0.05) were found between the two PMMA resins or between NYS and FLU as regards surface free energy. In conclusion, PRO was able to induce changes in PMMA surface properties, such as roughness, which could be related to microbial adhesion.
A espécie Pilocarpus microphyllus Stapf. recebe a designação geral de jaborandi, fonte industrial de pilocarpina, utilizada no tratamento do glaucoma. O jaborandi contém vários alcalóides secundários. A epiisopilosina foi submetida a testes farmacológicos para determinação da DL50’ screening hipocrático e determinação do peso corporal dos animais sobreviventes da DL50. A análise dos resultados revelou que a epiisopilosina apresentou DL50 duas vezes maior que a pilocarpina. Os animais que sobreviveram à determinação da DL50 ganharam peso no período de 14 dias de observação. A eplisopilosina demonstrou ser um estimulante periférico do sistema nervoso parassimpático, semelhante à pilocarpina, somente em altas doses.
Pilocarpus microphyllus Stapf. (Rutaceae) is a source for industrial isolation of pilocarpine, alkaloid used in the treatment of glaucoma. It contains several secondary alkaloids; one of them being eplisopilosine. Pharmacological evaluation showed DL50 value of epiisopilosine two times higher than of pilocarpine. Epiisopilosine also showed to be a pilocarpine-like peripheric stimulant of parasympatic nervous system, although in higher dosis
RESUMOA partir do fim da Segunda Guerra Mundial passaram a ser elaboradas regulamentações internacionais para o desenvolvimento de Pesquisas envolvendo seres humanos. Para a realização destas pesquisas é essencial que principios éticos tais como autonomia e vulnerabilidade do sujeito da pesquisa sejam respeitados. Considerando a importancia do conhecimento dos pesquisadores sobre os aspectos éticos envolvidos na pesquisa com seres humanos, o presente estudo tem como objetivo discutir estes aspectos dentro de um contexto histórico. Nos dias atuais, pesquisas incluindo grupos vulneráveis e pessoas com autonomia reduzida são comumente realizadas e, apesar da existência de normas internacionais e nacionais, além de códigos e diretrizes publicadas a este respeito, muitas destas são realizadas desrespeitando a ética e os princípios morais, ferindo a dignidade humana. Pala vras-cha veBioética; Autonomia Pessoal; Vulnerabilidade.O Cirurgiã-Dentista, Mestre em Cariologia FOP/UNICAMP.
Background: Chalcones substituted by methoxyl groups have presented a broad spectrum of bioactivities, including antifungal, antibacterial and antiproliferative effects. However, a clear and unambiguous investigation about the relevance of this substituent on the chalcone framework has not been described. Objective: The purpose of this work is to assess the antibacterial, antifungal and antiproliferative activities of two series of seventeen synthesized regioisomeric methoxychalcones. Series I and II were constituted by chalcones substituted by methoxyl groups on rings A (5–12) and B (13–21), respectively. In addition, the library of methoxychalcones was submitted to in silico drug-likeness and pharmacokinetics properties predictions. Methods: Methoxychalcones were synthesized and their structures were confirmed by NMR spectral data analyses. Evaluations of antimicrobial activity were performed against five species of Candida, two Gram-negative and five Gram-positive species. For antiproliferative activity, methoxychalcones were evaluated against four human tumorigenic cell lines, as well as human non-tumorigenic keratinocytes. Drug-likeness and pharmacokinetics properties were predict using Molinspiration and PreADMET toolkits. Results: In general, chalcones of series I are the most potent antifungal, antibacterial and antiproliferative agents. 2’,4’,5’-Trimethoxychalcone (11) demonstrated potent antifungal activity against Candida krusei (MIC = 3.9 µg/mL), eight times more potent than fluconazole (reference antifungal drug). 3’-Methoxychalcone (6) displayed anti-Pseudomonas activity (MIC = 7.8 µg/mL). 2’,5’-Dimethoxychalcone (9) displayed potent antiproliferative effect against C-33A (skin), A-431 (skin) and MCF-7 (breast), with IC50 values ranging from 7.7 to 9.2 µM. Its potency was superior to curcumin (reference antiproliferative compound), which exhibited IC50 values ranging from 10.4 to 19.0 µM. Conclusion: Our studies corroborated the relevance of methoxychalcones as antifungal, antibacterial and antiproliferative agents. In addition, we elucidated influence of the position and number of methoxyl groups toward bioactivity. In silico predictions indicated good drug-likeness and pharmacokinetics properties to library of methoxychalcones.
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