RESUMO
Cardiac hypertrophy is an independent risk factor of many cardiovascular diseases. Several cardiovascular protective properties of Cymbopogon proximus have been reported. However, no reports investigating the direct effect of C. proximus essential oil on the heart are available. The goal of this study was to explore the cardioprotective effect of C. proximus on cardiac hypertrophy and fibrosis. Male albino rats were administered C. proximus essential oil in the presence or absence of hypertrophic agonist isoproterenol. Cardiac hypertrophy and fibrosis were assessed using real-time polymerase chain reaction (PCR) and histological examination. Pre- treatment of rats with C. proximus decreased the ratio of heart weight to body weight and gene expression of hypertrophy markers atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and ß-myosin heavy chain (ß-MHC), which were induced by isoproterenol. Moreover, C. proximus prevented the increase in gene expression of fibrosis markers procollagen I and procollagen III and alleviated the collagen volume fraction caused by isoproterenol. The pre- treatment with C. proximus essential oil conferred cardio-protection against isoproterenol- induced cardiac hypertrophy and fibrosis.
Assuntos
Cardiomegalia/tratamento farmacológico , Cymbopogon/química , Fibrose/tratamento farmacológico , Coração/efeitos dos fármacos , Isoproterenol/efeitos adversos , Miócitos Cardíacos/efeitos dos fármacos , Óleos Voláteis/farmacologia , Animais , Fator Natriurético Atrial/metabolismo , Cardiomegalia/induzido quimicamente , Cardiomegalia/metabolismo , Cardiomegalia/patologia , Colágeno Tipo I/metabolismo , Colágeno Tipo III/metabolismo , Fibrose/metabolismo , Fibrose/patologia , Cromatografia Gasosa-Espectrometria de Massas , Injeções Intraperitoneais , Masculino , Miocárdio/citologia , Miocárdio/metabolismo , Miocárdio/patologia , Miócitos Cardíacos/citologia , Cadeias Pesadas de Miosina/metabolismo , Peptídeo Natriurético Encefálico/metabolismo , Óleos Voláteis/administração & dosagem , Óleos Voláteis/análise , Óleos Voláteis/uso terapêutico , Substâncias Protetoras/farmacologia , RatosRESUMO
Four new sesquiterpene lactones, 4α-hydroxy-guaia-10(14),11(13)-diene-12,6α-olide (1), 4α-hydroxy-9α-acetoxy-guaia-1(10),2-diene-12,6α-olide (4), 4α-hydroxy-9ß-acetoxy-guaia-1(10),2-diene-12,6α-olide (5), and 1α,4α-dihydroxy-9α-acetoxy-guaia-10(14),2-diene-12,6α-olide (6), were isolated from the aerial parts of Anthemis scrobicularis. Their structures were elucidated on the basis of their IR, NMR, and MS spectroscopic data. In addition, two known sesquiterpene lactones micheliolide (2) and achillin (3) were also isolated. The cytotoxicity of some of the isolated compounds was tested against HCT 116, HepG-2, and MCF-7 cell lines. Micheliolide and 4α-hydroxy-guaia-10(14),11(13)-diene-12,6α-olide showed pronounced inhibitory activity while 4α-hydroxy-9α-acetoxy-guaia-1(10),2-diene-12,6α-olide showed weak activity.
Assuntos
Anthemis/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Lactonas/isolamento & purificação , Lactonas/farmacologia , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologia , Antineoplásicos Fitogênicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Células HCT116 , Células Hep G2 , Humanos , Lactonas/química , Células MCF-7 , Estrutura Molecular , Sesquiterpenos/química , Sesquiterpenos de Guaiano/química , Sesquiterpenos de Guaiano/isolamento & purificação , Sesquiterpenos de Guaiano/farmacologiaRESUMO
The emergence of antibiotic-resistant strains of Pseudomonas aeruginosa (P. aeruginosa) presents a substantial obstacle in medical environments. To effectively tackle this problem, we suggest an innovative approach: employing a delivery system based on nanogels to administer lemongrass essential oil (LGO). Developed PVA and PLGA nanoparticle formulation efficiently encapsulates LGO with 56.23% encapsulation efficiency by solvent extraction technique, preserving stability and bioactivity. Nanogel: 116 nm size, low polydispersity (0.229), -9 mV zeta potential. The nanogel's controlled release facilitated targeted LGO delivery via pH-controlled dissolution. Pure LGO had the highest release rate, while LGO-NP and LGO-NP-CG exhibited slower rates. In 15 h, LGO-NP released 50.65%, and LGO-NP-CG released 63.58%, releasing 61.31% and 63.58% within 24 h. LGO-NP-CG demonstrated superior antioxidant activity, a lower MIC against P. aeruginosa, and the most potent bactericidal effect compared to other formulations. This underscores the versatile efficacy of LGO, suggesting its potential to combat antibiotic resistance and enhance treatment effectiveness. Moreover, employing a nanogel-based delivery approach for LGO offers an efficient solution to combat drug resistance in P. aeruginosa infections. By employing strategies such as nanogel encapsulation and controlled release, we can enhance the effectiveness of LGO against antibiotic-resistant strains. This study establishes a robust foundation for exploring innovative approaches to treating P. aeruginosa infections using nanomedicine and paves the way for investigating novel methods of delivering antimicrobial drugs. These efforts contribute to the ongoing battle against antibiotic resistance.
RESUMO
The objective of this study was to develop an innovative gallic-acid (GA) drug delivery system that could be administered transdermally, resulting in enhanced therapeutic benefits and minimal negative consequences. The method employed involved the preparation of poly(lactic-co-glycolic acid) (PLGA) nanoparticles loaded with GA through nanoprecipitation-denoted GA@PLGANPs. The results reveal that this strategy led to perfectly spherical, homogeneous, and negatively charged particles, which are suitable for administration via skin patches or ointments. A further analysis indicates that these GA@PLGANPs exhibit remarkable antioxidant activity as well as potent antibacterial effects against a diverse range of microorganisms, making them ideal candidates for numerous applications. Additionally, it has been observed that these nanoparticles can effectively mitigate oxidative stress while also significantly inhibiting microbial growth by exerting detrimental effects on bacterial cell walls or membranes. In conclusion, on the basis of the findings presented in this study, there is strong evidence supporting the potential use of GA@PLGANPs as an effective therapy option with reduced side effects compared to conventional drug delivery methods.
RESUMO
Researchers are actively exploring potential bioactive compounds to enhance the effectiveness of Lisuride (Lis) in treating Parkinson's disease (PD) over the long term, aiming to mitigate the serious side effects associated with its extended use. A recent study found that combining the dietary flavonoid Tiliroside (Til) with Lis has potential anti-Parkinson's benefits. The study showed significant improvements in PD symptoms induced by 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) when Til and Lis were given together, based on various behavioral tests. This combined treatment significantly improved motor function and protected dopaminergic neurons in rats with PD induced by MPTP. It also activated important molecular pathways related to cell survival and apoptosis control, as indicated by the increased pAkt/Akt ratio. Til and Lis together increased B-cell lymphoma 2 (Bcl-2), decreased caspase 3 activity, and prevented brain cell decay. Co-administration also reduced tumor necrosis factor alpha (TNF-α) and Interleukin-1 (IL-1). Antioxidant markers such as superoxide dismutase (SOD), catalase, and reduced glutathione significantly improved compared to the MPTP-induced control group. This study shows that using Til and Lis together effectively treats MPTP-induced PD in rats, yielding results comparable to an 8 mg/kg dose of levodopa, highlighting their potential as promising Parkinson's treatments.
RESUMO
The current research aimed to assess the Babchi oil nanoemulsion-based hydrogel prepared using biosurfactants through a low-energy emulsification process for the topical management of psoriasis. The emulsification capacity and solubilities of many nanoemulsion constituents such as surfactants, co-surfactants, and oil were considered to determine the range of concentration of the constituents. Pseudoternary phase diagrams were created using the method of titration. Nanoemulgel structure, morphology, micromeritics, conductivity, and viscosity were all optimized. The assessment of the Babchi oil nanoemulgel included particle size, polydispersity index (PDI), drug content, pH, spreadability, rheological management, ex vivo drug study, 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging ability, in vitro drug release, release kinetics, and dermatokinetics. The selected ratios of the surfactant mixture (Smix) taken were 3:1. The entrapment efficiency estimated was 91.298%. The zeta potential of Babchi oil was observed to be -24.93 mV at 25 °C with water as a dispersant, viscosity as 0.887 cP, and material absorption as 0.01 nm. The size distribution of the particle was 108 nm by the intensity and the conductivity observed was 0.03359 mS/cm. The cumulative amount of Babchi oil penetrated and fluxed by nanoemulgel was considered larger (p ≤ 0.05) than the conventional formulations. Skin retention was observed to be good with decreased lag time. The formulation followed the Higuchi Korsmeyer for Fickian Peppas model for in vitro drug release studies. The oil was most effective on the epidermal layer of the skin for treatment. It was established that the Babchi oil nanoemulgel formulation had superior permeability capabilities for topical and transdermal administration and is a viable alternative to traditional formulations.