Assessment of potential antimicrobial activity of Ocimum basilicum extract and chlorhexidine against Socransky's complex pathogens of oral cavity: An in vitro study.

Background and Objective: Periodontitis is a multifactorial disease initiated by periodontal pathogens and progresses further in destruction of periodontium. Hence, the objective of this study was to test the efficacy of Ocimum basilicum seeds extract on periodontal pathogens. Materials and Methods: O. basilicum seeds were authenticated from a recognized taxonomist. They were coarsely powdered; ethanol-based extract preparation was done by the Soxhlet method and aqueous-based extract by hot infusion procedure. Extracts so obtained were assessed for minimum inhibitory concentration, minimum bactericidal concentration, zone of inhibition, and time-kill assay of O. basilicum seeds extract on periodontal pathogens, and comparatively evaluated the effectiveness against 0.12% chlorhexidine (CHX) gluconate in triplicates. Kruskal-Wallis Test was employed wherein the statistical significance was set at P ≤ 0.05. Results: The concentration of O. basilicum ethanolic extract against periodontal pathogens was determined to be 10 mg/ml, whereas 4.7 mg/ml of aqueous extract was proven effective against periodontal pathogens. Similarly, aqueous extract of O. basilicum developed a wider zone against periodontal pathogens compared to ethanol-based O. basilicum extract. Statistically significant difference found in the effectiveness between both extract and CHX. Conclusion: The antibacterial activity was evident in both the extracts of O. basilicum against anaerobic periodontal pathogens. However, it was more pronounced in aqueous extract, but lower compared to CHX.

Microbial approaches for pharmaceutical wastewater recycling and management for sustainable development: A multicomponent approach.

A microbial-driven approach for effluent treatment, recycling, and management of Pharmaceutical and Personal Care Products (PPCPs) has been undertaken to mitigate the menace of water contamination. Bioremediation processes are mainly considered the first preference in pharmaceutical wastewater recycling and management. PPCPs are reported as one of the primary sources of emerging contaminants in various water matrices, which raises concern and requires efficient management. Their widespread utilization, persistently high level, and resistance to breaking down make them one of the potentially dangerous compounds causing harm to the ecosystem. Continually increasing PPCPs level PPCPs contaminants in water bodies raised concern for human health as they can produce potential risks with harmful and untoward impacts on our health. PPCPs are composed of multiple diverse compounds used by humans and animals, which include biopharmaceuticals, vitamins and nutritional supplements, antibiotics, counter-prescription drugs, cosmetics products, and unused pharmaceutical products. Personal care products are found to be bioaccumulative, reduce water quality and potentially impact ecological health. However, continual exposure to PPCPs in aquatic organisms, impacts their endocrine function disruption, gene toxicity, and antibiotic resistance. Decreased water quality may result in an outbreak of various water-borne diseases, which could have acute or long-term health complications and may result in an outbreak of various water-borne diseases, which could have acute or long-term effects on public and community health. Polluted water consumption by humans and animals produces serious health hazards and increased susceptibility to water-borne diseases such as carcinogenic organic or inorganic contaminants and infectious pathogens present in water bodies. Many water resource recovery facilities working on various conventional and advanced methods involve the utilization of microbes for filtration and advanced oxidation processes. Therefore, there is an immense need for bioremediation techniques facilitated by mixed cultures of bacteria, algae, and other microbes that can be used as an alternative approach for removing pharmaceutical content from effluent. This review highlights the various sources of PPCPs and their impacts on soil and water bodies, resulting in bioaccumulation. Different techniques are utilized to detect PPCPs, and various control strategies imply controlling, recycling, and managing waste.

Antimicrobial Efficacy of Essential Oils and Their Combination Against Microorganisms Associated With Postradiation Therapy in Patients With Head and Neck Cancer: An In Vitro Study.

Background Head and neck cancer ranks as the sixth most common cancer globally. Reduced saliva production brought on by postradiation therapy upsets the delicate balance between bacterial load and a weakened immune system. Oral hygiene is commonly neglected in patients who have undergone radiotherapy and they often develop dry mouth, mucositis due to radiation therapy, etc., as side effects. Despite being a part of the current standard, chlorhexidine carries numerous disadvantages such as taste alteration, teeth staining, and dry mouth. An extensive review of the literature demonstrates the antibacterial properties of essential oils (EOs) derived from plant materials, which may be able to prevent the development of such opportunistic microorganisms in the oral cavity. Methodology The cinnamon bark EO and Cajeput EO were procured and checked for their solubility. The final ratio at which the oils were found to be soluble was the 1:1 (w/v) ratio. The minimum inhibitory concentration (MIC) of cinnamon bark oil (Cinnamomum verum) and Cajeput oil (Melaleuca leucadendron) against Staphylococcus aureus, Enterococcus faecalis, and Candida albicans was determined by serial dilution method using Resazurin dye, and the minimum bactericidal concentration (MBC) was done by a spread plating method. The polyherbal mouthwash was subjected to cytotoxicity assay against human gingival fibroblasts. All the experiments were performed in triplicates. Results The overall results showed that cinnamon bark EO had the strongest efficacy against S. aureus (0.33 ± 0.14 mg/mL) and E. faecalis (0.41 ± 0.14 mg/mL), but not against C. albicans (2.85 ± 2.11 mg/mL). Cajeput EO showed the least efficacy against all the groups; whereas the combination of EOs proved to be the most efficacious and showed good antimicrobial activity against these most commonly encountered microorganisms in head and neck cancer postradiotherapy. Conclusions Cinnamon and Cajeput EOs in combination proved to be effective in this in vitro study against the most common microorganisms encountered in patients with head and neck cancer postradiotherapy and are comparable to 0.2% chlorhexidine.

A Cross-Sectional Study on Molecular Detection of Helicobacter pylori cytotoxin-associated gene A and 16SrRNA Gene from Gastric Biopsy Specimens.

INTRODUCTION: The aim of the study is relative proportion of cytotoxin-associated gene A (cagA) virulence marker in Helicobacter pylori isolates and gastric biopsy samples by polymerase chain reaction (PCR). METHODS: This cross-sectional study was conducted at a tertiary care hospital setting. Gastric biopsy tissues from 200 patients, suffering from upper gastrointestinal tract disorders, were examined for H. pylori infection using methods, such as hematoxylin and eosin (H and E) staining, 16S rRNA (Ribosomal ribonucleic acid), and cagA gene PCR. Chi-square and kappa statistics were used to find the association and agreement between the tests, respectively; P ≤ 0.05 was considered statistically significant. Screening tests' accuracy was calculated in terms of sensitivity and specificity along with positive and negative predictive values. RESULTS: Out of 200 patients, H. pylori was detected in 14.5%, 48.5%, and 31% patients by H and E staining, 16S rRNA, and cagA PCR, respectively. Sensitivity and specificity of cagA PCR as compared to H and E staining were 89.6% and 78.9%, respectively. CONCLUSIONS: CagA detection directly from biopsy specimen by PCR can potentially and rapidly determine the patient's status, especially when at a higher risk of peptic ulcer.

Psychrophiles: A journey of hope.

Psychrophiles are organisms living in extremely cold conditions within the temperature range of -20°C to +10°C. These organisms survive in harsh environment by modulating their genetic make-up to thrive in extremely cold conditions. These cold-adaptations are closely associated with changes in the life forms, gene expression, and proteins, enzymes, lipids, etc. This review gives a brief description of the life and genetic adaptations of psychrophiles for their survival in extreme conditions as well as the bioactive compounds that are potential antimicrobials.

One pot synthesis, in silico study and evaluation of some novel flavonoids as potent topoisomerase II inhibitors.

A library of novel flavonoid derivatives with diverse heterocyclic groups was designed and efficiently synthesized. Structures of the newly synthesized compounds 4a-i and 8a-l have been characterized by 1H NMR, 13C NMR, MS and elemental analysis. Anticancer activities were evaluated against MCF-7, A549, HepG2 and MCF-10A by MTT based assay. Compared with the positive control Adriamycin, compounds 4a, 4b, 4c, 4d, 8d, 8e and 8j were found to be most active anti-proliferative compounds against human cancer cell line. We found that compounds 4a and 4c exhibited inhibition of enzyme topoisomerase II with IC50 values 10.28 and 12.38 µM, respectively. In silico docking study of synthesized compounds showed that compounds 4a and 4c have good binding affinity toward topoisomerase IIα enzyme and have placed in between DNA base pair at active site of enzyme. In silico ADME prediction results that flavonoid coumarin analogues 4a-i could be exploited as an oral drug candidate.

Chemoresistance in Ovarian Cancer: Prospects for New Drugs.

This review focuses on the conventional treatment, signaling pathways and various reasons for drug resistance with an understanding of novel methods that can lead to effective therapies. Ovarian cancer is amongst the most common gynecological and lethal cancers in women affecting different age groups (20-60). The survival rate is limited to 5 years due to diagnosis in subsequent stages with a reoccurrence of tumor and resistance to chemotherapeutic therapy. The recent clinical trials use the combinatorial treatment of carboplatin and paclitaxel on ovarian cancer after the cytoreduction of the tumor. Predominantly, patients are responsive initially to therapy and later develop metastases due to drug resistance. Chemotherapy also leads to drug resistance causing enormous variations at the cellular level. Multifaceted mechanisms like drug resistance are associated with a number of genes and signaling pathways that process the proliferation of cells. Reasons for resistance include epithelial-mesenchyme, DNA repair activation, autophagy, drug efflux, pathway activation, and so on. Determining the routes on the molecular mechanism that target chemoresistance pathways are necessary for controlling the treatment and understanding efficient drug targets can open light on improving therapeutic outcomes. The most common drug used for ovarian cancer is Cisplatin that activates various chemoresistance pathways, ultimately causing drug resistance. There have been substantial improvements in understanding the mechanisms of cisplatin resistance or chemo sensitizing cisplatin for effective treatment. Therefore, using therapies that involve a combination of phytochemical or novel drug delivery system would be a novel treatment for cancer. Phytochemicals are plant-derived compounds that exhibit anti-cancer, anti-oxidative, anti-inflammatory properties and reduce side effects exerted by chemotherapeutics.

Ultrasound assisted synthesis of tetrazole based pyrazolines and isoxazolines as potent anticancer agents via inhibition of tubulin polymerization.

In search of new active molecules against MCF-7, A549 and HepG2, tetrazole based pyrazoline and isoxazoline derivatives under both conventional and ultrasonic irradiation method were designed and efficiently synthesized. Structures of newly synthesized compounds 5a-h and 6a-h were characterized by 1H NMR, 13C NMR, MS and elemental analysis. Several derivatives were found to be excellent cytotoxic against MCF-7, A549 and HepG2 cell lines characterized by lower IC50 values (0.78-3.12 µg/mL). Compounds 5b and 5c demonstrated an antiproliferative effect comparable to that of CA-4. Western blot analysis revealed that, reported compounds accumulate more tubulin in the soluble fraction. Docking studies suggested that, binding of these compounds mimics at the colchicine site of tubulin. In vitro study revealed that the tetrazole based pyrazolines and isoxazolines may possess ideal structural requirements for further development of novel therapeutic agents.

Green, unexpected synthesis of bis-coumarin derivatives as potent anti-bacterial and anti-inflammatory agents.

A green and efficient protocol has been developed and a series of coumarin based pyrano[3,2-c]chromene derivatives (2) have been synthesized using multi-component reaction (MCR) approach. Unexpected 3-coumarinyl-3-pyrazolylpropanoic acids (3) and C4-C4 chromenes (5) have been isolated instead of expected product 4 by the reaction of compound (2) in formic acid at 90 °C for about 4-5 h and at 130 °C for about 8-10 h respectively. Further, C4-C4chromenes (5) formation was confirmed by intramolecular cyclization of compounds (3). These compounds were screened for their biological activities and most of them exhibited promising antibacterial activity. The anti-inflammatory assay was evaluated against HRBC membrane stabilization method and the compounds exhibit excellent anti-inflammatory activity. Molecular docking study has been performed for all the synthesized compounds with Klebsiella pneumoni aeacetolactate synthase and results obtained are quite promising.

Formulation of thermoreversible gel of cranberry juice concentrate: Evaluation, biocompatibility studies and its antimicrobial activity against periodontal pathogens.

The present work aims to investigate the efficacy of thermoreversible gel of cranberry juice concentrate (CJC) as local drug delivery for the treatment of periodontitis. CJC was initially tested for its antimicrobial activities like MIC, MBC, antiadhesion, antibiofilm and time kill assay against the panel of organisms (S. mutans (SM), E. faecalis (EF), A. actinomycetemcomitans (AA), P. gingivalis (PG), T. forsythia (TF)) responsible for periapical and periodontal infections. Antimicrobial activity of CJC showed MIC value of 50mg/ml and MBC value of 100mg/ml with desirable antiadhesion (83-90%) and antibiofilm activity (70-85%). CJC was evaluated for its biocompatibility using periodontal fibroblasts by cell based MTT assay and found to be nontoxic. Influence of CJC on periodontopathogen PG derived virulence factors (fimA and kgp) was studied using real time polymerase chain reaction (RT-PCR) technique wherein down regulation of selected genes demonstrated inhibitory effect against PG virulence factors. Thermoreversible gel of CJC was formulated by cold method using poloxamer 407 as thermosensitive polymer and carbopol 934 as mucoadhesive polymer and evaluated for its gelation temperature, viscosity, gel strength and mucoadhesive strength. Comparison of optimized thermoreversible gel of CJC (500mg/ml) with commercially available chlorhexidine gluconate gel (0.2%) using agar well diffusion demonstrated equal zone of inhibition against SM, EF, AA, PG & TF. Hence the formulated thermoreversible gel of CJC could serve as a novel herbal alternative to currently available periodontal treatment modalities.

Design and synthesis of novel phenyl -1, 4-beta-carboline-hybrid molecules as potential anticancer agents.

A series of beta-carbolines with other heterocycles linked by phenyl ring has been designed and synthesized. The key intermediates 3 and 5 were synthesized by condensing tryptamine and teraldehyde via Pictet- Spengler method. All the newly synthesized compounds were tested for their anticancer activity against sixty human cell lines at NCI. The five dose results of compounds 3 and 7a showed enhancement of anticancer activity (GI50 values range from 1.00 to 7.10 µM) against all the cell lines in comparison with some of earlier molecules. In addition to this protein binding and CT-DNA intercalation studies showed molecules are highly potential. The molecular docking studies, which support the multiple mode of interaction with DNA, moreover the synthesized compounds 3 and 7a are more potential and possess drug -like nature.

Design, synthesis and pharmacological analysis of 5-[4'-(substituted-methyl)[1,1'-biphenyl]-2-yl]-1H-tetrazoles.

In the present paper 5-[4'-({4-[(4-aryloxy)methyl]-1H-1,2,3-triazol-1-yl}methyl)[1,1'-biphenyl]-2-yl]-1H-tetrazoles (5a-g) and [2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl-substituted-1-carbodithioates (11h-q) have been designed and synthesized. These compounds were subjected to docking (against AT1 receptor protein enzyme in complex with Lisinopril), in vitro angiotensin converting enzyme inhibition, anti-proliferative, anti-inflammatory screening (through egg albumin denaturation inhibition and red blood cell membrane stabilization assay) and finally anti-fungal activity analyses. Some of the compounds have shown significant pharmacological properties.

Synthesis, characterization and molecular docking studies of substituted 4-coumarinylpyrano[2,3-c]pyrazole derivatives as potent antibacterial and anti-inflammatory agents.

A green, eco-friendly and efficient protocol has been developed and synthesized a series of coumarin based pyrano[2,3-c]pyrazole derivatives (3) by multi-component reaction (MCR). Unexpected 3-coumarinyl-3-pyrazolylpropanoic acids (4) have been isolated by the reaction of compound (3) in acidic conditions. Further, intramolecular cyclization of compounds (4) leads to C4C4 chromons (9) and these compounds were screened for their biological activities using array of techniques. Most of the compounds exhibited promising antibacterial activity, in particular Gram-positive bacteria. The anti-inflammatory assay was evaluated against protein denaturation as well as HRBC membrane stabilization methods and compounds exhibit excellent anti-inflammatory activity in both methods. Molecular docking study has been performed for all the synthesized compounds with S. aureus dihydropteroate synthetase (DHPS) and results obtained are quite promising.