Том 22, № 3 (2024)

Medicine

Cavity Disinfection with Natural Agents and their Efficacy: A Review on Recent Literature

Dey S., Deshmukh S.

Аннотация

The success of a dental restoration can be altered by the amount of residual bacteria present under the cavity which over time cause deterioration of adhesive cement by microleakage or secondary caries. Cavity disinfectant application on the cavity walls performs a cleansing action to decrease the bacterial load and improve the longevity of restorations. Although a wide variety of such chemical disinfectants have been in use, their cytotoxic effects have led to the increasing popularity of natural agents. These materials possess antimicrobial, antioxidant and anti-inflammatory properties, which effectively disinfect cavity walls while, at the same time, being cheaper, less toxic, and more patient-friendly.

:Some of these agents have also been proven to improve the bond strength of resin to dentin by preventing collagen degradation and MMP inhibition. Propolis, aloe vera, chitosan, green tea, liquorice etc., are derived from parts of plants or animals and have been tested to be efficacious and, in some cases, superior to chemical alternatives without any erosive effect on dentin.

:Although there is a lack of enough In vivo evidence to advocate the use of these products as an adjunct in dental therapy, recent studies have yielded promising results, which increases the scope for future clinical research. This review aims to highlight the properties and effectiveness of a few of such natural agents as potential cavity disinfectants.

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Prevalence and Antibiogram of Escherichia coli Isolated from Children Under Five Years of Age Presented with Acute Diarrhoea: Cross Sectional Study from a Tertiary Care Centre in South India

Thattil S., Ajith T.

Аннотация

Aim:The study aimed to analyze the prevalence and antibiogram of E. coli isolated from stool sample cultures collected from children below five years of age who were presented with acute diarrhoea in a tertiary care centre.

Background:Multidrug-resistant strains of diarrheagenic E. coliremain a major public health concern for greater morbidity and mortality. Antibiotic resistance and susceptibility patterns of E. coli were found to vary with geographical location.

Objective:To determine the prevalence and antibiogram of E. coli isolated from cultures of diarrhoea stool samples collected from children below five years of age from laboratory records.

Methods:A cross-sectional study was designed to analyze the report on stool culture of children (aged below five years) presented with acute diarrhea during the period between 2017 and 2020. The prevalence of E. coli and its antibiogram were analyzed. The data were subjected to statis-tical analysis.

Results:A total of 245 diarrhoea stool samples results were analyzed. E. coli was confirmed in 176 samples (72%). More number of isolates (51/176, 28.9%) were found in children below one year of age with male dominance. Amoxicillin resistance was found in all the E. coli strains isolated with no significant difference (p=0.2233) between genders and age groups below and above one year. A significant difference (p=0.0001) was found between male and female chil-dren of age below and above one year for cefotaxime and ciprofloxacin resistance. Polymyxin B (72%) followed by imipenem (69%) sensitivity was exhibited by the isolated E. coli strains.

Conclusion:E. coli isolates were more sensitive to polymyxin B and imipenem while they were most resistant to amoxicillin. Effective antibiotic treatment strategies should be developed to control E. coli infections in children.

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Development of Phytoconstituents from Spathodea campanulata Flowers as Potential Antimalarial Agents

Geevarghese A., Emimmal M., Elizabeth I., Krishnan P., Sumathi S., Perumal T.

Аннотация

Background:Considering the majority of pharmaceutical firms focus on using herbal remedies as an alternative source of essential components, herbal remedies are extremely significant to pharmacological researchers. Spathodea campanulata is one of the members of the Bignoniaceae family. It is popular for its curative properties

Aim:This research aimed to assess the possibility of bioactive elements and antioxidant impacts of the methanol fraction of Spathodea campanulata flowers.

Objectives:The objective of this research was to assess the achievable bioactive elements and antioxidant impacts of the methanol fraction of Spathodea campanulata flowers.

Methods:GC-MS was adopted to identify the phytoconstituents present in the extract. In the present study, we utilized computational modelling with the Schrödinger Maestro 11.2 edition to make benefit of interactions among 42 bio-active components and anti-malarial targets (1LDG and 2ANL).

Results:In the methanol extract of the Spathodea campanulata flowers, phytochemical research revealed the presence of terpenoids, glycosides, carbohydrates, steroids, and flavonoids. Forty-two phytoconstituents, notably methyl-beta-d-galactopyranoside, 4-hydroxybenzoic acid, and 1,2- ethanediol monobenzoate, were determined through GC-MS analysis. Docking analysis of 42 bioactive compounds demonstrated that 1,2-ethanediol mono benzoate, 4-hydroxy benzoic acid, and methyl.beta.-d-galactopyranoside had higher G-Scores with 1LDG and 2ANL.

Conclusion:In this work, multiple phytoconstituents discovered in a methanol extract of the S. campanulata flower were determined. As a result of this research, four phytoconstituents from the flower extracts may be created as an exciting new therapy for malaria.

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Use of Pharmacophore Modeling, 3D-atom-based QSAR, ADMET, Docking, and Molecular Dynamics Studies for the Development of Psoralen-based Derivatives as Antifungal Agents

Asgaonkar K., Patil S., Chitre T., Prabhu A., Shevate K., Sagar A., Naik A.

Аннотация

result:The top ranked hypothesis AHRRR_1 was taken into consideration when designing the library of potential NCE's.In order to check the drug likeliness of the compounds, all 36 designed NCE's were subjected to ADMET prediction using QikProp tool. The majority of compounds have good partition coefficient index (less than five), and Qplog HERG value was found to be less, making them safer and less toxic.C- 4, 6, 9, 13, 15, 22, 24, 27, 31, 33 have shown compliance to Lipinski’s rule with zero violations. The majority of the compounds had greater binding affinity than the standard Ketoconazole. Three compounds C-9, 24 and 27 have the good hydrophobic and hydrogen bonding interactions required for antifungal activity.The Compounds 9, 24 and 27 showed good stability after 100ns molecular simulation simulations.

other:Nil

Background::The mortality and morbidity rates in patients caused by fungi are ex-tremely high. 3-4 % of species of fungi like Candida and Aspergillus are responsible for >99% of invasive fungal infections.

Aim::The goal of the current work was to use several In-silico methods, such as Pharmacophore modeling and 3D-QSAR, to design New chemical entities (NCEs) that have antifungal activity.

Material & Method::A dataset of 40 Psoralen derivatives was taken from available literature, and then, the pharmacophore hypothesis and 3D-QSAR model development were generated using Schrodinger 2023-1 software. After designing a library of 36 compounds, they were sub-jected to ADMET prediction. Screened compounds from the ADMET study were docked with 14 alpha demethylase CYP51 (PDB ID: 3LD6) using Schrödinger software. Molecular dynam-ics (MD) simulation studies were performed on PDB-3LD6 using Desmond-v7.2.

Results & Discussion::The top-ranked hypothesis, AHRRR_1, was taken into consideration when designing the library of potential NCEs.In order to check the drug likeliness of the com-pounds, all 36 designed NCEs were subjected to ADMET prediction using the QikProp tool. The majority of compounds have a good partition coefficient index (less than five). Qplog HERG value was found to be less, making them safer and less toxic. C- 4, 6, 9, 13, 15, 22, 24, 27, 31, and 33 have shown compliance with Lipinski’s rule with zero violations. Compounds C-9, C-13, C-22, C-24, and C-27 have shown better docking scores than the standard Ketocon-azole. Compounds C-9, 24, and 27 have shown a greater number of hydrophobic and hydrogen bond interactions in comparison with the other compounds. Compounds 9, 24, and 27 showed good stability after 100ns molecular simulation simulations.

Conclusion::In the current work, the application of insilico methods such as pharmacophore hypothesis, 3D QSAR, ADMET study, docking, and simulation studies have helped to optimize Psoralen pharmacophore for potential antifungal activity. Therefore, the outcomes of the present study could provide insights into the discovery of new potential alpha demethylase inhibitors with improved selectivity and activity against fungal infections.

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Potentials of TPC and TFC as Free Radical Scavengers and Microbial Growth Inhibitors in Himalayan Endemic Artemisia sieversiana Ehrhl Ex Willd. (Asteraceae) Plant from Northeastern, Pakistan

Hussain A., Rasheed H., Khan M., Bokhari S.

Аннотация

Background:In various microorganisms, various defense mechanisms have evolved against the commercially available antimicrobial agents with increased resistance. Natural antimi-crobial agents of plant origin are better alternatives when an infectious disease arises due to resistant microbial strains. Here, we have evaluated the efficacy of total phenolics and total flavonoids with antioxidant and antimicrobial potential of Artemisia sieversiana Ehrhl Ex Willd. plant extracted with methanol, ethyl acetate, ethanol, n-hexane, and chloroform using soxhlet procedures

Methods:The evaluation of TPC was achieved with Folin-Ciocalteu’s reagent method and quanti-tative estimation of TFC was done with the aluminum chloride colorimetric method. The antioxi-dant activities were estimated using FRSA-DPPH and TAC methods. The inhibitory activities of five solvent extracts of A. sieversiana against 2 gram-positive and 2 gram-negative pathogenic bac-terial strains (B. subtilis, P. aerogenosa, S. aureus, and E. coli) were evaluated using the well dif-fusion technique.

Results:The highest percentage yields of A. sieversiana extracts were obtained in ethanol (4.8 g, 12.1%) and methanol (4.01 g, 10%), while minimum extract yield was obtained in n-hexane (0.53 g, 1.34%). Both phenolics and flavonoids were higher in ethanol, methanol, and ethyl acetate ex-tracts while minimal in n-hexane extracts. Ethanol extract has shown maximum (69%) DPPH ac-tivity with a lower IC50 value (181 µg/ml), while the highest IC50 values of 330 and 325µg/ml were recorded for n-hexane and ethyl acetate extracts. The ethyl acetate and chloroform extracts dis-played overall highest TAC values. All the tested extracts of A. sieversiana exhibited variable in-hibitory effects in a dose-dependent manner against the tested bacterial strains with minimum 9.08 ± 0.23 to maximum 21.23 ± 7.04 mm inhibition zones. Methanol and ethyl acetate extracts at 2 to 4 mg/ml showed greater MIC results against P. aeruginosa in comparison to the B. subtilis strain.

Conclusion:The extracts of A. sieversiana have been found to be rich in TPC and TFC with re-markable antibacterial and antioxidant efficacies, and the plant extracts could be employed as pos-sible alternatives to synthetic drugs in various nutraceutical and pharmaceutical industries.

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Effect of Toll-like Receptor-3 Antagonist on Viral Asthma Exacerbations Via a TLR3/dsRNA Complex Pathway

Arora S., Singh K., Saha S., Kumar S., Khalid M., Akram W., Alam S., Sahu K., Agrawal M., Chaudhary H.

Аннотация

Background:The Toll-like receptor-3 (TLR3) ligand Poly(I:C) has been shown to induce a viral aggravation of severe asthma by identifying double-stranded RNA (dsRNA). This study aimed to evaluate the therapeutic role of the TLR3/dsRNA complex inhibitor-calbiochem compound in the treatment of Poly(I:C)-induced viral asthma exacerbations through the ovalbu-min-induced asthma model in Swiss albino mice.

Methods:Poly(I:C) and Ovalbumin drugs were injected in mice to sensitize (i.p. on 0, 7, and 14th day) and challenge (i.n. on the 21st and 22nd days). In contrast, the treatment drug TLR3/dsRNA complex inhibitor-calbiochem was given on the 21st and 22nd days intraperitoneally within the study period. In-vivo measurements were carried out in BALF and serum for pro-inflammatory cytokines, inflammatory leukocyte counts, lactate dehydrogenase (LDH) and nitrite levels, lungs/body weight index, and lung tissue histopathology using H and E staining in mice airways.

Results:High levels of cytokines (NF-κB, IL-1β, IL-5, RANTES, MIP-2, and MCP-1) are seen in groups exposed to OVA and Poly (I:C). Further, inflammatory leukocyte cell counts, lung-body weight (LW/BW) index, airway hyperresponsiveness (AHR), and lung tissue damage sug-gest exacerbations in mice airways. On the other hand, TLR3/dsRNA complex inhibitor-calbio-chem and dexamethasone significantly reversed these changes toward normal levels.

Conclusions:These results suggest that the novel compound TLR3/dsRNA complex inhibitor-calbiochem has a better therapeutic role than dexamethasone for managing inflammatory char-acteristics in asthmatic mice lungs and is a potent target for viral asthma exacerbations

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Exploring the Role of Cathelicidin Antimicrobial Peptide, Toll-Like Receptor 4, and HMGB-1 in Bacterial Infection

Febriza A., Idrus H., Kasim V.

Аннотация

method:This study is an experiment that uses a pre-post-test design. Mice balb/c were separated into three groups; group A received levofloxacin for five days, group B received a placebo, and group C was the control. Both groups, A and B, received an injection of S. Typhi strain thy1. Blood samples were taken from three groups on the 4th, 10th, and 30th day to calculate CAMP, TLR-4, and HMGB-1 mRNA gene expression levels. To determine bacterial colony, peritoneal fluid was taken three times on the 4th, 10th, and 30th day to calculate bacterial colony.

result:The expression of mRNA CAMP and bacterial colony count correlated negatively. The expression of HMGB-1 mRNA correlated with bacterial growth. Higher CAMP mRNA expression was found to relate to reduced bacterial colony count in groups A and B using linear regression.

Background and Aim:Lipopolysaccharides (LPS) from Salmonella typhi will attach with Toll-Like Receptor 4 (TLR-4) and trigger an inflammatory response to fight the pathogen. Due to infection, the HMGB1 is produced by immune cells or secreted passively from dead cells. Fur-thermore, the antimicrobial peptide, cathelicidin was secreted to neutralize and eliminate these path-ogens. This study aims to examine the interaction of Cathelicidin antimicrobial peptide (CAMP), TLR-4, and HMGB-1 on inhibiting bacterial growth in Salmonella infection.

Methods:This study is an experiment that uses a pre-post-test design. Mice balb/c were separated into three groups; group A received levofloxacin for five days, group B received a placebo, and group C was the control. Both groups, A and B, received an injection of S. Typhi strain thy1. Blood samples were taken from three groups on the 4th, 10th, and 30th day to calculate CAMP, TLR-4, and HMGB-1 mRNA gene expression levels. To determine bacterial colony, peritoneal fluid was taken three times on the 4th, 10th, and 30th day to calculate bacterial colony.

Results:Our finding observed that the expression of mRNA CAMP was inversely related to bacte-rial colony count, which means that higher CAMP mRNA expression was associated with reduced bacterial colony count in groups A and B. The expression of HMGB-1 mRNA was found to be positively correlated with bacterial growth in group A. Meanwhile, TLR-4 mRNA expression did not significantly correlate with bacterial colony count in any groups.

Conclusions:CAMP, TLR-4, and HMGB-1 affect bacterial infections. Higher expression CAMP mRNA levels lower colony counts. Meanwhile, decreasing TLR-4 and HMGB-1 mRNA expression were found during the study, due to reducing growth bacteria.

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β-lactamase and Plasmid-mediated Quinolone Resistance Determinants Among Proteus spp. Isolates at a Tertiary-care Hospital in Kolkata, India

Mallick A., Barik M., Sarkar S., Das S.

Аннотация

Background:Emerging antibiotic resistance (ABR) in Proteus spp., especially to third-generation cephalosporins (3GCc), carbapenems, and fluoroquinolones, challenges the treatment outcome and infection prevention. Limited studies pose a knowledge gap between them and ABR.

Methods:We investigated the in vitro efficacy of therapeutic options and prevalence of β-lac-tamase and plasmid-mediated quinolone resistance (PMQR) traits in 3GC- and/or fluoroquino-lone-nonsusceptible Proteus (P.) spp. (n=27) in Kolkata, India, during 2021–2022. P. mirabilis was commonly isolated (>80%) from superficial and urine samples. The majority of the isolates (48-78%) remained susceptible to piperacillin-tazobactam, meropenem, amikacin, cefoperazone-sulbactam, and cefepime.

Results:All isolates showed >0.2 multiple-antibiotic resistance index, with >65% being multi-drug and >30% being extensively drug-resistant. blaTEM (n=9), blaNDM (n=9), and qnrA (n=6) were commonly noted with the co-production of β-lactamases and PMQR in ten (37%) isolates. More than 50% of the isolates were devoid of the tested acquired genes.

Conclusion:The study concludes that superbugs dominate, with limited occurrence of plasmid-borne markers in this geographic location.

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