Current Chemical Biology - Volume 16, Issue 2, 2022

Background: Leishmaniasis is a multifaceted disease that is prevalent worldwide. It is an epidemic, tropical/subtropical disease caused by macrophage infection by compulsive leishmania genus intracellular parasites affecting millions of people across the globe. Methods: The demand for effective and safe molecules in the field of leishmaniasis is still an active research area. The lack of widely effective anti-leishmanial drugs, therefore, means a critical need for the production of modern, effective, affordable, and safe drugs for leishmaniasis care. In the recent past, many new pharmacophores have been synthesized and evaluated for their antileishmanial activity. Conclusion: Many important heterocycles have proved to be effective against various leishmanial strains in terms of both safety and efficacy. In this article, we have attempted to review the different pharmacophores discovered in the past few years with the potential anti-leishmanial property.

Aristolochia longa is a plant belonging to the genus Aristolochia, family Aristolochiaceae, whose rhizomes represent the most important part used in the pharmaceutical field mainly due to its richness in bioactive molecules. Several investigations have shown numerous biological properties, including antibacterial, antifungal, anti-inflammatory, antioxidant, and anti-cancer activities. Besides, many chemical components such as alkaloids, glycosides, phenolic compounds, tannins, flavonoids, terpenoids, and saponins have been isolated, and their structures have been elucidated. However, Aristolochia longa is still not investigated. Therefore, more studies should be conducted to discover other biological activities of Aristolochia longa, as well as those of other species from the same genus, and identify compounds responsible for these activities.

Background: AIDS is a complicated disease, and the underlying complication makes a total cure impossible. This demands the vigorous need for suitable anti-HIV agents. Styrylquinoline, a quinolone derivative, emerged as a potent HIV-IN inhibitor. Objective: This study aims to construct an easily transferable and reproducible model that relates the biological activities of styrylquinoline derivatives to their molecular descriptors. Methods: 2D Quantitative structure-activity relationship (QSAR) studies were carried out on a series of 36 styrylquinoline derivatives. Results: The technique of recursive feature elimination with random forests was used to select the descriptors rich in information regarding biological activity. The selected descriptors were used in QSAR studies based on multiple linear regression (MLR) and multiple nonlinear regression (MNLR). The performance of models was evaluated by internal and external validations. The values of R²pred and Q²LOO for the MLR model are 0.814 and 0.713, respectively, while the MNLR model has R²pred and Q²LOO values of 0.810 and 0.699, respectively. Conclusion: The information obtained from 2D-QSAR models will aid in gaining a better understanding of the structural requirements for creating novel HIV-IN inhibitors.

Background: Tetrachloromethane (CCl4) is a highly toxic environmental pollutant that causes specific and serious damage to various organs of animals and humans. The study of its effect on physiological and biochemical processes in the mammalian organism is very important, despite the severe restrictions on the use of tetrachloromantane in recent years. The fact is that they can be used as a model for many toxicological studies. Objective: The experimental studies aimed at exploring the ameliorative effects of L-glutamic acid (LGlu) on CCl4 toxicity in the myocardium, lung tissues and blood of male rats. Methods: Rats were exposed to CCl4, and later rats were treated with L-Glu. The GSH level and the activities of antioxidant enzymes were studied. In addition to this, the content of lipid peroxidation products was monitored. Results: The obtained results suggest that CCl4 causes oxidative stress in rat tissues, accompanied by an increase in lipid peroxidation products and a decrease in glutathione peroxidase (GPx), glutathione reductase (GR), glutathione transferase (GST), glucose-6-phosphate dehydrogenase (G6PDH), superoxide dismutase (SOD), catalase (CAT) activities and reduced glutathione (GSH) content. The enzymatic activity in tissues of rats treated with L-Glu was restored. Moreover, the changes, which were observed in the studied parameters, showed to be less significant compared to CCl4 treated group. Conclusion: These results suggest that L-Glu inhibits free radical processes. In summary, this study demonstrates the feasibility of the administration of L-Glu supplementation, which could be used to protect and mitigate the CCl4-induced oxidative stress.

Introduction: Contact lenses coated with antibacterial agents may reduce the risk of microbial keratitis; however, to the best of our knowledge, such contact lenses are not available on the market. Methods: We determined the ability of zinc oxide nanoparticles (ZnO-NPs)-loaded soft contact lenses to prevent the adhesion of Staphylococcus aureus and Pseudomonas aeruginosa. Commercially acquired sterile silicone hydrogel contact lenses were soaked in ZnO-NPs (#130;50 nm) suspensions of various concentrations, and the stability of the ZnO-NPs coating on contact lenses over 28 days was monitored using a UV-vis spectrophotometer. The cytotoxicity effects of ZnO-NPs on human corneal epithelial cells were evaluated using a lactate dehydrogenase (LDH) kit. Results: The results showed that the ZnO-NPs coating on contact lenses was optimal from day seven onward. In the following assays, optimally, ZnO-NP-coated contact lenses were incubated with S. aureus and P. aeruginosa suspensions (1 x 10⁵ colony forming unit) for 24 hr at 37°C, followed by enumeration using the plating method. Our data showed that 100 ppm of ZnO-NPs coating on contact lenses reduced the adhesion of 69.9% and 74.6% of S. aureus and P. aeruginosa significantly (p<0.05). The confocal laser scanning microscopic analyses were consistent with our bacterial adhesion findings. Low cytotoxicity against human corneal epithelial cells was observed even at the highest concentration of 300 ppm. Conclusion: This study provides insights into the potential role of ZnO-NPs in developing contact lenses with antibacterial properties.