The Aedes aegypti mosquito is the primary vector of dengue, a neglected disease and a serious public health problem in tropical countries. The control of this vector has been carried out using chemical insecticides, which impact human health. Thus, it is essential to develop natural larvicides that are less harmful to the environment. This study investigates the circadian cycle and larvicidal activity of essential oils from Croton blanchetianus against Aedes aegypti. The leaf oils were extracted by hydrodistillation and analyzed by GC–MS and GC–FID. The circadian study revealed variations in the chemical composition of oils extracted at different times of the day. The main constituents were α-pinene, β-phellandrene, eucalyptol, β-caryophyllene, bicyclogermacrene, and spathulenol. The larvicidal activity showed LC50 values at the following different collection times: 55.294 ± 3.209 μg/mL at 08:00 h; 95.485 ± 2.684 μg/mL at 12:00 h; and 64.883 ± 1.780 μg/mL at 17:00 h. Molecular docking simulations indicated that α-pinene, β-phellandrene, eucalyptol, and β-caryophyllene strongly interact with the active site of the sterol carrier protein, suggesting their role in larvicidal activity. These findings reinforce the potential of C. blanchetianus essential oils as an alternative for Aedes aegypti control. The predictive pharmacokinetic tests showed a PAMPA profile associated with high effective cellular permeability and microsomal stability, resulting from the metabolic stability of the derivatives (3) eucalyptol and (6) spathulenol, indicating that these compounds have the highest pharmacokinetic viability and low reactivity with respect to organ toxicity.
Background/Objectives: Nanoemulsions (NEs) possess properties that enhance the solubility, bioavailability and therapeutic efficacy of drugs. Chalcones are compounds known for their antifungal properties. In this study, we evaluated different emulsification techniques to create alginate nanoemulsions containing chalcone (1E,4E)-1,5-bis (4-methoxyphenyl) penta-1,4-dien-3-one (DB4OCH3). Our goal was to develop an antifungal formulation targeting Candida albicans strains. Methods: Ultrasound and ultrasound combined with high-speed homogenization techniques were used to prepare alginate-stabilized nanoemulsions. Particle size, zeta potential and encapsulation efficiency were evaluated. Additionally, in vitro release studies were conducted. Results: The combined emulsification technique produced stable nanoparticles with high encapsulation efficiency and antifungal activity, with a minimum inhibitory concentration of 8.75 μg/mL for the nanoemulsions compared to 312 µg/mL for free DB4OCH3. NEs’ effectiveness can be attributed to their ability to form nanodroplets efficiently, facilitating the solubilization of the chalcone in the oily phase. The particle size varied between 195.70 ± 2.69 and 243.40 ± 4.49 nm, with an increase in chalcone concentration leading to larger particle sizes. The zeta potential showed values from −91.77 ± 5.58 to −76.90 ± 4.44 mV. The UHS-7 sample exhibited an encapsulation efficiency of 92.10% ± 0.77, with a controlled in vitro release of 83% after 34 h. Molecular docking simulations showed that the aromatic nature of DB4OCH3 resulted in the formation of apolar interactions with aromatic residues located in the active site of the TMK, as observed in their respective co-crystallized inhibitors, within an affinity energy range that enables optimum specificity of the ligand for these two pathways. Pharmacokinetic analyses indicated high passive cell permeability and low hepatic clearance, and phase I metabolism reduces its oral bioavailability and metabolic stability, suggesting a promising active ingredient as an oral drug with control of the daily oral dose administered. Conclusions: The combined nanoemulsification technique led to the formation of finely dispersed nanodroplets that favored the solubilization of the chalcone in the oil phase, which led to a better performance in the antifungal properties. DB4OCH3 shows promise as an oral drug with controlled dosing.
31 August 2021 in Ambiente: Gestão e Desenvolvimento
O uso exagerado de combustíveis fósseis para atender à necessidade energética mundial, tem gerado graves danos ao meio ambiente, visto que esses, geram em sua queima uma grande quantidade de gases poluentes. Os biocombustíveis se apresentam como uma das alternativas mais viáveis para suprir a demanda energética mundial e minimizar os danos ao meio ambiente. Diante disso, várias políticas de incentivo à produção de biocombustíveis, foram criadas, com intuito de diminuir a dependência energética de fontes não renováveis e diminuir os impactos ambientais. A biomassa se apresenta como uma das melhores alternativas para produção de biocombustíveis. Nesse contexto, essa revisão teve como objetivo relatar sobre as quatro gerações de biocombustíveis, incluindo o tipo de matéria-prima e as tecnologias de conversão envolvidas nos biocombustíveis mais comercializados atualmente, como bioetanol e biodiesel.
Background/Objectives: Hydrazones are organic compounds with the general structure R2C=NNHR1, distinguished by their versatility and modifiability, and are widely used in various applications due to their physicochemical and biological properties. They exhibit anticancer, anti-inflammatory, antibiofilm, and antibacterial activities. Antibiotic-resistant bacteria pose a serious public health threat, employing mechanisms such as enzymatic inactivation and efflux pumps. This study evaluated the antibacterial activity of the hydrazone HDZH1,4BENZ, a hydralazine-derived compound, as well as its potential adjuvant effect in combination with antibiotics against Staphylococcus aureus strains expressing efflux pumps. Methods: The strains used were 1199B (NorA efflux pump-expressing) and K2068 (MepA efflux pump-expressing). All assays were conducted using the broth microdilution method in Brain Heart Infusion (BHI) medium. Initially, the intrinsic antibacterial activity of the compound was determined. Subsequently, modulation assays were performed to evaluate its potential effect on efflux pump activity, with a standard efflux pump inhibitor included as a positive control. Results: Although HDZH1,4BENZ did not demonstrate significant direct antibacterial activity, the results indicate that this hydrazone exerts a notable inhibitory effect on the NorA (Norfloxacin resistance efflux pump A) and MepA (Multidrug efflux protein A) efflux pumps in S. aureus, thereby enhancing the efficacy of antibacterial agents. Conclusions: The activity of the hydrazone was comparable to that of chlorpromazine, suggesting that it may represent a promising alternative in the fight against antibiotic-resistant bacterial infections.