Background:The aim of the present study was to compare the antibacterial effects of coffee extract with those of 0.2% sodium fluoride and chlorhexidine (CHX) mouthrinses on Streptococcus mutans and Lactobacillus plantarum in vitro.Materials and Methods:In this experimental in vitro study, the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and disk diffusion method were determined for different concentrations of coffee extract, 0.2% CHX, and 0.2% fluoride against S. mutans and L. plantrum. Data were analyzed using Kruskal–Wallis analysis. Statistical significance level was established at P < 0.05.Results:The MIC of coffee was achieved at 62.5 and 500 mg/mL against S. mutans and L. plantarum, respectively. The MBC against S. mutans was 125 mg/mL. The diameter of the zone of inhibition around S. mutans for pure coffee extract (100%), CHX (0.2%), and fluoride was 19.8 mm, 9.92 mm, and 0, respectively. At a concentration of 6.25%–100%, coffee had a significantly larger zone of inhibition compared to CHX and fluoride) P = 0.01). The MBC of coffee and fluoride was 0 against L. plantarum. The lowest inhibitory concentration belongs to CHX (MIC: 0.624 mg/ml for L. plantarum and 0.125 mg/ml for S. mutans).Conclusion:The coffee had an antibacterial effect against S. mutans on 62.5–1000 mg/ml concentrations. The zone of inhibition around S. mutans for higher concentrations of coffee (6.25%–100%) was significantly higher than that of CHX and fluoride 0.2%. Bacteriostatic effect of coffee against L. plantarum was obtained at 500–1000 mg/ml. However, coffee and fluoride did not show any bactericidal effects against L. plantarum.
Pyrazinoic acid or pyrazine-2-carboxylic acid (PA), due to its nitrogenous heteroaromatic ring, can be explored as an anticancer agent. Here, a series of twenty novels PA derivatives have been synthesized and characterized using IR, NMR, and mass spectrums. Their cytotoxic activity was evaluated against three different cancer cell lines, including lung (A549), breast (MCF-7), and colon (HT-29). P16, the most potent compound, showed moderate cytotoxicity with IC 50 of 6.11 μM, 10.64 μM, and 14.92 μM, against the A549, MCF-7, and HT-29 cell lines, respectively. Furthermore, the effect of this compound against MRC5 as a non-tumoral lung cell line, exhibited a selectivity index of 9.02. The apoptotic induction activity of P16 was also performed on the A549 cell line. The results showed that as the concentration of the compound increases (from 3 to 6 μM), the percentage of induction of apoptosis increases from 8.54% to 72.4%. Electrophoretic gel mobility shift assays showed that P16 was also able to ROS induce DNA cleavage in the presents of H 2 O 2 (1.0 mM) in dose-dependent manner. Molecular docking was also applied to anticipate the binding locations and the binding of the synthesized compound with Bcl-2 apoptosis regulator and DNA as their proposed targets.
This study aims to probe into new series of heterobimetallic Pt II −Au I complexes with a general formula of [Pt(p-MeC 6 H 4 )(dfppy)(μ-dppm)Au(NHC)]OTf, NHC = IPr, 2; IMes, 3; dfppy = 2-(2,4-difluorophenyl)pyridinate; dppm = 1,1bis(diphenylphosphino)methane, which are the resultant of the reaction between [Pt(p-MeC 6 H 4 )(dfppy)(κ 1 -dppm)], 1, with [AuCl(NHC)], NHC = IPr, B; IMes, C, in the presence of [Ag(OTf)]. In the heterobimetallic complexes, the dppm ligand is settled between both metals as an unsymmetrical bridging ligand. Several techniques are employed to characterize the resulting compounds. Moreover, the photophysical properties of the complexes are investigated by means of UV−vis and photoluminescence spectroscopy. Furthermore, the experimental study is enriched by ab initio calculations (density functional theory (DFT) and time-dependent DFT (TD-DFT)) to assess the role of Pt and Au moieties in the observed optical properties. It is revealed that 1−3 is luminescent in the solid state and solution at different temperatures. In addition, the achieved results indicate the emissive properties of 1−3 are originated from a mixed 3 IL/ 3 MLCT excited state with major contribution of intraligand charge transfer (dfppy). A comparative study is conducted into the cytotoxic activities of starting materials and 1−3 against different human cancer cell lines such as the pancreas (MIA-PaCa2), breast (MDA-MB-231), cervix (HeLa), and noncancerous breast epithelial cell line (MCF-10A). The achieved results suggest the heterobimetallic Pt II −Au I species as optimal compounds that signify the existence of cooperative and synergistic effects in their structures. The complex 3 is considered as the most cytotoxic compound with the maximum selectivity index in our screened complex series. Moreover, it is disclosed that 3 effectively causes cell death by inducing apoptosis in MIA-PaCa2 cells. Furthermore, the finding results by fluorescent cell microscopy manifest cytoplasmic staining of 3 rather than nucleus.
Hepatic dysfunction is primarily caused by nonalcoholic fatty liver disease (NAFLD). Recently, berberine (BBR) has attracted researchers’ interest with its hepatic protective property. A systematic review was conducted to evaluate the effects of BBR and its mechanisms of action in the management of NAFLD and its complications. The guidelines of the Preferred Reporting Items for Systematic Review and Meta-Analysis (PRISMA) statements were applied to perform the study. Embase, Web of Science, Google Scholar, Science Direct, PubMed, ProQuest, and Scopus databases were searched up until March 2023. According to the inclusion criteria, finally, 65 studies were entered into the study. The evidence provided in the study revealed that BBR could regulate the development of NAFLD via several mechanisms of action namely lowering body weight, modulating lipid and glucose metabolism, and reducing inflammation and oxidative stress (OS). The current systematic review demonstrated the beneficial effects of BBR on NAFLD and its associated metabolic disorders including dyslipidemia, obesity, and insulin resistance through regulating lipid metabolism, facilitating β-oxidation of fatty acids, and mitigating the accumulation of triglycerides in hepatocytes. These beneficial effects make BBR a potential therapeutic approach and an efficient agent in the management of NAFLD and its related risk factors. There is an insufficient number of clinical trials addressing the effects of BBR in humans, so conducting more human research in the future is recommended.
Pyrazinoic acid or pyrazine-2-carboxylic acid (PA), due to its nitrogenous heteroaromatic ring, can be explored as an anticancer agent. Here, a series of twenty novels PA derivatives have been synthesized and characterized using IR, NMR, and mass spectrums. Their cytotoxic activity was evaluated against three different cancer cell lines, including lung (A549), breast (MCF-7), and colon (HT-29). P16, the most potent compound, showed moderate cytotoxicity with IC50 of 6.11 μM, 10.64 μM, and 14.92 μM, against the A549, MCF-7, and HT-29 cell lines, respectively. Furthermore, the effect of this compound against MRC5 as a non-tumoral lung cell line, exhibited a selectivity index of 9.02. The apoptotic induction activity of P16 was also performed on the A549 cell line. The results showed that as the concentration of the compound increases (from 3 to 6 μM), the percentage of induction of apoptosis increases from 8.54% to 72.4%. Electrophoretic gel mobility shift assays showed that P16 was also able to ROS induce DNA cleavage in the presents of H2O2 (1.0 mM) in dose-dependent manner. Molecular docking was also applied to anticipate the binding locations and the binding of the synthesized compound with Bcl-2 apoptosis regulator and DNA as their proposed targets.
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