Since herpes simplex virus type 1 (HSV-1) infection is so widespread, several antiviral drugs have been developed to treat it, among which are uracil nucleosides. However, there are major problems with the current medications such as severe side-effects and drug resistance. Here we present some newly synthesized cyclic and acyclic uracil nucleosides that showed very promising activity against HSV-1 compared to acyclovir.
Pyrroles and its fused forms possess antimicrobial activities, they can easily interact with biomolecules of living systems. A series of substituted pyrroles, and its fused pyrimidines and triazines forms have been synthesised, all newly synthesised compound structures were confirmed by spectroscopic analysis. Generally, the compounds inhibited growth of some important human pathogens, the best effect was given by: 2a, 3c, 4d on Gram-positive bacteria and was higher on yeast ( C. albican s), by 5c on Gram-negative bacteria and by 5a then 3c on filamentous fungi (A. fumigatus and F. oxysporum ). Such results present good antibacterial and antifungal potential candidates to help overcome the global problem of antibiotic resistance and opportunistic infections outbreak. Compound 3c gave the best anti-phytopathogenic effect at a 50-fold lower concentration than Kocide 2000, introducing a safe commercial candidate for agricultural use. The effect of the compounds on DNA was monitored to detect the mode of action.
Background Individuals with hyperlipidemia are two times more likely to develop atherosclerotic cardiovascular disease (ASCVD) as opposed to those with controlled serum total cholesterol (TC) levels. Considering the documented adverse events of the current lipid-lowering medications which ultimately affect patient’s compliance, substantial efforts have been made to develop new therapeutic strategies. Probiotics, on the other hand, are reported to have lipid-lowering activity with the added benefit of being generally well-tolerated making it an appealing adjuvant therapy. Methods A total of fifty Lactic acid bacteria (LAB) were isolated from raw milk (human and animal) and dairy products. Isolates demonstrating promising in vitro cholesterol removal capabilities were morphologically and biochemically characterized. Lastly, two bacterial candidates were selected for evaluation of their potential hypolipidemic activity using a laboratory animal model. Statistical differences between the means were analyzed by one-way analysis of variance (ANOVA) followed by Tukey’s post-hoc test. A p-value < 0.05 was considered statistically significant. Results Most of the isolates demonstrated an in vitro cholesterol removal activity. The six LAB isolates showing the highest cholesterol removal activity (36.5–55.6%) were morphologically and biochemically identified as Lactobacillus, Pediococcus, and Lactococcus species. The results demonstrated two promising antihyperlipidemic candidates, a Lactococcus lactis ssp. lactis with an in vivo significant reduction of serum triglycerides (TG) levels by 34.3%, and a Pediococcus sp. that was able to significantly reduce both the serum TC and TG levels by 17.3% and 47.0%, respectively, as compared to the diet-induced hyperlipidemic animal group. Conclusion This study further supports the growing evidence regarding the antihyperlipidemic activity among probiotics, presenting them as a promising therapeutic approach for the management of hyperlipidemia.
Objectives:The continuous reporting of bacterial resistance to antibiotics is an ongoing challenge that can be lifethreatening. Actions to develop new chemicals to overcome the bacterial resistance has gained a significant importance. Methods: A series of ketene S,N-acetals 4a-k and their pyrazoles 6a-k were synthesized and their structures were established by spectral data. Membrane permeability predictions and in vitro antimicrobial activity against multi-drug resistant (MDR) Gram-positive bacteria and other microorganisms was determined. The binding affinity with DNA gyrase was assessed using in silico studies in comparison to ciprofloxacin then the gyrase inhibition assay was conducted to detect the mode of action. Results: All the synthesized compounds have a good affinity to pass through the phospholipid membrane of Staphylococcus aureus (S. aureus). Compound 6g exhibited the most potent antibacterial activity with MIC values ranged between 16 and 32 µg/mL. The compound also showed a higher binding affinity than ciprofloxacin with DNA gyrase in the in silico studies and this effect was clearly shown by a very good IC50 value of the gyrase inhibition assay. Conclusions: According to our data, compound 6g is a possible candidate to act against MDR bacteria and its main mode of action is through inhibition of the gyrase enzyme, further modifications are still required to enhance its activity.
Aim Ocular health greatly impacts the quality of life, and diabetes-mellitus (DM) is a major cause of several visual diseases. Likewise, microbiomes have a pivotal role in eye health. The aim was to study the effect of DM, both type-1 (T1DM) and type-2 (T2DM) on the ocular microbiome. Methods and results a total of 70 subjects were recruited for this study and divided into 2 main groups: healthy non-diabetic (n = 18) and diabetic (28 T1DM and 24 T2DM). The ocular surface (OS) microbiome was more diverse in the healthy group than in the diabetic one. Taxonomic analysis revealed Proteobacteria as the main phylum (healthy non-diabetic 41.8%, T1DM 50.6%, T2DM 52.5%), besides Streptococcus (healthy non-diabetic 16%, T1DM 26.75%, T2DM 29.20%) and Paracoccus (healthy non-diabetic 17%, T1DM 34.85%, T2DM 37.47%) as the main genera. No significant diversity was found between T1DM and T2DM on both phylum and genus levels; yet genera Brevundimonas and Leptotrichia were more significantly predominant in T1DM. Conclusion Two pathogenic genera, Streptococcus and Paracoccus, were more predominant in the DM group than in the healthy one.
The current coronavirus disease (COVID-19) pandemic poses a significant challenge for human microbiota researchers around the world, as the causes and long-term repercussions of infection at the gastrointestinal (GI) level are still unknown. Original research publications, clinical investigations, epidemiological reports, and review-type articles about human intestine infection with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and the possible repercussions on the microbiota were reviewed in the current study. Furthermore, the following aspects of COVID-19 have been discussed: Epidemiology, human sensitivity, the impact of dietary habits on the intestinal microbiota, and the impact of comorbid metabolic disorders like obesity, inflammatory bowel disease (IBD), and diabetes on the intestinal microbiota. According to the studies, health, age, and nutritional condition are linked to specific bacterial populations in the gut, which may influence the clinical course of COVID-19 infection. Changes in the faecal microbiota were linked to the severity of SARS-CoV-2 and COVID-19 infections. Patients with metabolic and GI issues are likely to have a moderate-to-high risk of SARS-CoV-2 infection, implying that gut dysbiosis plays a direct role in COVID-19 severity. However, further work is needed to identify COVID-19's initial GI symptoms so that early management can be attempted.
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