The purpose of this research was to determine how Rhizopogon luteolus extract (RLE) affects rat cecal ligation and puncture (CLP)-induced sepsis. Wistar albino rats were randomly assigned to six groups (n = 8). (1) Sham group; (2) CLP group; (3) CLP+1
The ruthenium, palladium, and silver complexes with N-heterocyclic carbene (NHC) ligands have been widely studied for promising anticancer activities, and they have been found to exhibit strong cytotoxic activity toward a range of cancer cells. However, the ruthenium and palladium NHC complexes have been less studied compared to silver and gold NHC complexes as antimicrobial agents. Herein, Ag, Ru, and Pd complexes of a benzimidazol-2-ylidene ligand bearing p-nitrobenzyl and diisopropylaminoethyl groups were synthesized and characterized by FT-IR, H-1 NMR and C-13 NMR spectroscopy, elemental analysis and mass spectrometry. The molecular and crystal structures of 2 and 4 were confirmed by the single-crystal X-ray diffraction (SC-XRD) method. All compounds were tested for antibacterial and antifungal activities and the minimum inhibitory concentrations were determined. The results indicates that some compounds exert effective antibacterial activity against Gram-negative and four Gram-positive bacterial strains and two yeast strains. Ag complex 2 had great antibacterial activity against Staphylococcus aureus at MIC value of 12.5 mu g/mL. However, the presence of ruthenium in the structure of the compounds increased overall antibacterial and antifungal activity.
Schiff bases (imines or azomethines) are versatile ligands synthesized from the condensation of amino compounds with active carbonyl groups and used for many pharmaceutical and medicinal applications. In our study, we aimed to determine the cytotoxic, antifungal and larvicidal activities of biologically potent bis-sulfonamide Schiff base derivatives that were re-synthesized by us. For this aim, 16 compounds were re-synthesized and tested for their cytotoxic, antifungal and larvicidal properties. Among this series, compounds A1B2, A1B4, A4B2, A4B3, and A4B4 were shown to have cytotoxic activity against tested cancer lung cell line (A549). The most potent antifungal activity was observed in compounds A2B1 and A2B2 against all fungi. A1B1 showed the strongest larvicidal effect at all concentrations at the 72nd h (100% mortality). These obtained results demonstrate that these type of bis-substituted compounds might be used as biologically potent pharmacophores against different types of diseases.
The olive (Olea europaea L.) is one of the most important plants grown in many Mediterranean countries that has a high economic value. Olives, which are specific to each region, have different bioactive components. In this study, we investigated the phenolic/flavonoid contents, as well as antioxidant, antimicrobial, and antithrombotic activities of the fruit, leaf, and seed extracts obtained from the Halhalı olive grown in Arsuz district of Hatay, Turkey. Antioxidant activities of the phenolic compounds found in the olive fruit, seed, and leaf extracts were determined by employing established in vitro systems. Total phenolics were determined as gallic acid equivalents, while total flavonoids were determined as quercetin equivalents. Also, we evaluated a possible interaction between oleuropein and aggregation-related glycoproteins of the platelet surface via docking studies. The extracts showed effective antioxidant activity. The seed extract had the highest phenolic content of 317.24 μg GAE, while the fruit extract had the highest flavonoid content of 4.43 μg. The highest potential for metal chelating activity was found in the leaf extract, with an IC50 value of 13.33 mg/mL. Also, the leaf extract showed higher levels of antioxidant, antithrombotic, and antimicrobial activity, compared to the fruit and seed extracts. The docking scores of oleuropein against the target molecules GPVI, α2β1, and GPIbα were calculated as –3.798, –4.315, and –6.464 kcal/mol, respectively. The olive fruit, leaf, and seed extracts used as experimental material in our study have remarkable antioxidant, antimicrobial, and antithrombotic potential.
Eight benzimidazole precursors (L), namely 1-allyl-benzimidazole, 1-methallyl-benzimidazole, 1-isopropyl-benzimidazole, 1-(3-methyloxetan-3-yl)methyl-benzimidazole, 1-allyl-5,6-dimethyl-benzimidazole, 1-methallyl-5,6dimethyl-benzimidazole, 1-isopropyl-5,6-dimethyl-benzimidazole and 1-(3-methyloxetan-3-yl)methyl-5,6dimethyl-benzimidazole, were coordinated to cobalt(II) and zinc(II) cations to form complexes of the type [MCl2L2]. Single-crystal X-ray structures were determined for two cobalt(II) and for one zinc(II) complexes and confirmed their tetrahedral molecular geometry. The antibacterial and antifungal activities of these two series of cobalt(II) and zinc(II) complexes were studied against Gram-negative (Escherichia coli, Pseudomonas aeruginosa, Acinetobacter baumannii and Klebsiella pneumoniae), Gram-positive (Staphylococcus aureus, methicillin-resistant S. aureus and Enterococcus faecalis) bacteria and fungal strains (Candida albicans and Candida glabrata). Overall, cobalt(II) complexes were more effective than the zinc(II) complexes against all microorganisms. The most significant results were obtained with the two dichloro-bis(1-allyl-5,6-dimethylbenzimidazole)-cobalt(II) and dichloro-bis(1-methallyl-5,6-dimethylbenzimidazole)-cobalt(II) complexes against Candida albicans and Candida glabrata fungi with measured minimal inhibitory concentrations as low as 0.024 mu mol/mL, values close to those obtained with the commercially available drug Flucanozole (0.020 mu mol/mL).
A series of new silyl-substituted benzimidazolium salts were synthesized in good yield by the reaction of 1-(dimethylvinylsilyl)methylbenzimidazole and various alkyl halides. These salts were characterized by spectroscopic techniques. Also, crystal structure of 2c has been determined by the single-crystal X-ray diffraction method. Newly synthesized compounds were tested for antibacterial and antifungal activities and the minimum inhibitory concentrations were determined. The results indicates that some of compounds exert effective antibacterial activity against four Gram (-) bacterial and four Gram (+) bacterial strains and two yeast strains.
Abstract N-Heterocyclic carbene-based silver complexes (Ag-NHCs) have been widely used as organometallic drug candidates in medicinal and pharmaceutical chemistry research due to their low toxicity. Due to the success of Ag-NHCs in biological applications, interest in the synthesis and applications of such compounds is increasing rapidly. Therefore, in this study, ten Ag-NHC complexes containing benzimidazol-2-ylidene ligand were synthesized and characterized by 1H NMR, 13C NMR, FT-IR spectroscopies and elemental analyses. The antimicrobial activity of Ag-NHCs was tested against some standard culture collections of Gram-negative, Gram-positive bacterial strains and fungal strains, which are the most frequently isolated among the society and hospital acquired infectious microorganisms as potential metallopharmaceutical agents. The Ag-NHC complexes showed effective antimicrobial activity against microorganisms with MIC values between 6.25 and 100 μg/mL. Graphical Abstract
The reaction of N-substituted benzimidazole with 4-bromobutyronitrile gives the corresponding benzimidazolium salts as N-heterocyclic carbene (NHC) precursors. Silver(I) carbene complexes are synthesized by the reaction of the corresponding benzimidazolium salts with Ag2O in dichloromethane. These new NHC precursors and Ag-NHC complexes were characterized by spectroscopy techniques and also screened for their antibacterial activities against the standard bacterial strains Escherichia coli, Pseudomonas aeruginosa, Acinetobacter baumannii, Klebsiella pneumoniae, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, and Enterococcus faecalis, and the standard fungal strains Candida albicans and Candida glabrata, and promising results were achieved. The compounds were also analyzed by density functional theory (DFT)/time-dependent DFT and docking methods.
In the present study, we have synthesized Ag, Rh, and Ir complexes of a silyl-substituted NHC ligand in order to investigate their biological properties. Firstly, Ag-NHC (2) complex was synthesized by the interaction of Ag2O with benzimidazolium iodide (1). Rh-(3) and Ir-NHC (4) complexes were synthesized by the transmetalation reaction between Ag-NHC and [M(cod)Cl]2 (M = Rh or Ir) dimers. The complexes were characterised by NMR spectroscopy and elemental analyses, and crystal structures of Rh-and Ir-NHC (3 and 4) were also reported. The cytotoxic effects of the complexes were tested on four human cancer cell lines and the antimicrobial activities of the complexes were tested against a panel of nine pathogenic microorganisms. The complexes performed com-parable or better activity than standards, cisplatin and AgNO3.
Objective: In this century, with the prolonged life expectancy, chronic diseases have become the most important cause of mortality and morbidity in the world and in our country. Frequent drug-drug interactions have made it necessary to update the doses of drugs in multiple drug use. In our study, we aimed to observe how the drugs that are frequently prescribed by physicians in the treatment of chronic and infectious diseases, together with standard bacteria and fungi strains in in vitro environment, change the effects of each other.Methods: By combining antibiotic discs and drugs that are commonly used in chronic diseases (acetylsalicylic acid, amlodipine, atorvastatin, warfarin, metoprolol and clopidogrel) in in vitro environment, we determined the drug interactions (synergy/antagonism) by Kirby Bauer disk diffusion method.Results: While most of the discs placed on the culture of Candida albicans through impregnation of drugs showed potentiation synergism with itraconazole and fluconazole, other microorganisms showed synergistic and sometimes antagonistic interactions with different drugs and antibiotics, whereas some of the drugs did not show any interaction with antibiotic discs.Conclusion: Due to the strong relationship between advanced age and the number of prescribed drugs and the frequency of possible drug-drug interactions, the elderly people especially are susceptible to this situation. Infections caused by resistant bacteria cause an increase in disease/death rates and treatment costs. With the awareness that the only difference between drug and poison is the dose, all health professionals especially doctors and pharmacists and patients have a responsibility towards the rational use of drugs.
Natural mushrooms are one of the important elements of the ecosystem. It has been preferred by people from past to present because of its nutritional and medicinal potentials. In this study, antioxidant, oxidant and antimicrobial potential of Trametes hirsuta (Wulfen) Lloyd has been determined. In addition, phenolic compounds in its fruiting body have been scanned. The antioxidant and oxidant potential was determined using Rel Assay kits. Antimicrobial potential was determined using the agar dilution method. Phenolic contents were scanned on the HPLC device. As a result of the studies, the presence of different levels of Gallic acid, Catechin, 4-Hydroxybenzoic acid and Epicatechin were observed in T. hirsuta. TAS value of T hirsuta was determined 3.466 +/- 0.148 mmol/L, TOS value was 13.482 +/- 0.234 mu mol/L and OSI value was 0.390 +/- 0.018. Antimicrobial activity of T. hirsuta was found to be effective at 100, 200 and 400 mu g/mL concentrations. As a result of the studies, it has been determined that T hirsuta has antioxidant and antimicrobial potential.
Herein, we report the synthesis, characterisation and preliminary biological evaluation of two novel silver(i) complexes of type [AgL2](NO3)3 (3 and 4) with ionic N-donor benzimidazoles. The complexes have been synthesized by the reaction of 1.5 equivalents of silver nitrate and N-donor benzimidazoles containing an imidazolium core at the 2-position (1 and 2) in ethanol. The X-ray analysis of 4 shows that it has two free imidazolium cores and the charge is balanced with three nitrate anions. A study by the combination of NMR, IR, LC-MS and elemental analysis techniques also suggests that the complexes have this structure both in the solid-state and solution. The complexes are highly soluble and stable in water. Cytotoxicity evaluation against four cancerous human cells and one non-cancerous human cell revealed that the complexes have no significant anti-growth effect. However, the complexes showed a remarkable antimicrobial effect at normalized minimum inhibitory concentrations (normalized MICs) in the range of 33-268 μM against a panel of microorganisms consisting of Gram-negative and Gram-positive bacteria, and fungi.
ObjectiveTo evaluate the impact of vaginal microbiota on pregnancy outcomes in women undergoing assisted reproduction.DesignA prospective cohort study.SettingA university‐based assisted reproductive technology (ART) centre.Population223 women undergoing ART treatment.MethodsPrior to embryo transfer, vaginal samples were collected from the posterior fornix. Vaginal microbiota identification was carried out using next‐generation sequencing and categorised according to the V3–V4 hypervariable region in the 16S rRNA gene region.Main outcome measuresART clinical outcomes (implantation, clinical pregnancy rates and live birth rates).ResultsThe live birth rate in women with community state type (CST)‐I (39%) was higher than that in women with CST‐III (21.5%) but the difference was not statistically significant (P = 0.052). The relative abundance of Lactobacillus was lower in women who failed to become pregnant (NP group) (67.71%) than in women who became pregnant (PR group) (79.72%). However, this difference was not statistically significant (P = 0.06). In the NP group, the relative abundance of Streptococcus (7.81%) and Gardnerella (9.40%) was higher than that in the PR group (relative abundance of Streptococcus and Gardnerella was 2.28% and 5.56%, respectively). The abundance of Streptococcus was found to be statistically significantly different between the two study groups (P = 0.014). Linear discriminant analysis (LDA) further validated that Streptococcus had the highest contribution (LDA score >4.0) to the difference between these two groups.ConclusionsStreptococcus has the highest contribution to the distinction between the PR and NP groups.Tweetable abstractA relatively high abundance of Streptococcus in the vaginal microbiota may be associated with a lower ART success rate.
Tuberculosis is an infectious disease, which is caused by the Mycobacterium tuberculosis complex. This disease leads to up to 1.3 million deaths out of more than eight million cases every year. A prodrug called isoniazid has been proven to be effective and widely used in the treatment of infections caused by tuberculosis. Despite its use for more than six decades clinically, the action mechanism of this prodrug is yet to be elucidated. INH action agains mycobacteria requires catalase−peroxidase (KatG) function, and IN-NAD adduct formation is catalyzed in vitro by M. tuberculosis KatG under a variety of conditions. Low-intensity EMF (Electromagnetic Field) has been used in the₂rapeutic practices in addition to its use in telecommunication systems and food protection. EMF is used in medicine and food industries especially for its bactericidal effects. In this study, we aimed to investigate the effects of weak magnetic field application and the addition of NAD and H₂O₂ on the action mechanism of isoniazid. We added H₂O₂ and NAD individually and together, to the different groups at varying concentrations. Also, one experimental group was exposed to a 5mT, 50Hz magnetic field for 4 to 5 hours per day (total of 45 hours in 10 days). The agar proportion method was used to evaluate the results. It was determined that the addition of 100 μM NAD and H₂O₂ together increased the effectiveness of isoniazid to some extent. However, the application of a weak magnetic field did not change the effectiveness of the drug.
Catechol-containing imidazolium (four) and benzimidazolium chlorides (eight) were synthesized to evaluate their antimicrobial properties. All the compounds were fully characterized using 1 H and 13 C nuclear magnetic resonance, liquid chromatography-mass spectrometry, infrared spectroscopic methods, and elemental analyses. Antimicrobial activities of the compounds were tested against the bacteria Escherichia coli, Pseudomonas aeruginosa, Acinetobacter baumannii, Klebsiella pneumoniae, Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Enterococcus faecalis, and the fungal strains Candida albicans and Candida glabrata, and promising results were achieved. The two most important benzyl-substituted benzimidazolium chlorides, 3l and 3k, showed comparable activity to vancomycin against MRSA.
In this study, biological activities and phenolic contents of endemic Ferulago platycarpa Boiss. & Bal. were determined. Within the scope of biological activity, antimicrobial activity, antioxidant and oxidant status of plant extracts were determined. Phenolic contents were determined by using HPLC. Antimicrobial activity was determined against bacteria and fungus strains using the modified agar method. Antioxidant and oxidant status were calculated with Rel Assay kits. Gallic, chlorogenic, cinnamic, syringic acids, epicatechin, catechin and quercetin were found in the plant. It was also determined that the plant has antioxidant and antimicrobial potential. But, because of higher TOS value, it was considered that the plants, which were collected from region suitable for OSI value, could be a natural antioxidant source.
A series of symmetrical and nonsymmetricalN,N-disubstituted benzimidazolium salts were synthesized asN-heterocyclic carbene precursors. These salts were treated with Ag2O to afford their corresponding mononuclear Ag(I)-NHC complexes. These compounds were characterized by spectroscopy techniques and analyzed by DFT/TDDFT and docking methods. Also, the structures of2aand2ewere determined by single-crystal X-ray crystallography. These new Ag-NHC complexes were screened for their antibacterial activities against Gram-positive, Gram-negative bacteria, fungi, and nosocomial agents.