Progress in fluorescence biosensing and food safety towards point-of-detection (PoD) system

The detection of pathogens in food substances is of crucial concern for public health and for the safety of the natural environment. Nanomaterials, with their high sensitivity and selectivity have an edge over conventional organic dyes in fluorescent-based detection methods. Advances in microfluidic technology in biosensors have taken place to meet the user criteria of sensitive, inexpensive, user-friendly, and quick detection. In this review, we have summarized the use of fluorescence-based nanomaterials and the latest research approaches towards integrated biosensors, including microsystems containing fluorescence-based detection, various model systems with nano materials, DNA probes, and antibodies. Paper-based lateral-flow test strips and microchips as well as the most-used trapping components are also reviewed, and the possibility of their performance in portable devices evaluated. We also present a current market-available portable system which was developed for food screening and highlight the future direction for the development of fluorescence-based systems for on-site detection and stratification of common foodborne pathogens

Simple and rapid RP-HPLC method to determine the purity of the anti-retroviral drug lamivudine

In the present study, a high performance liquid chromatographic method was developed and validated for determination of chromatographic purity and stress stability of the anti-retroviral drug lamivudine. The different analytical performance parameters such as linearity, precision, specificity, limit of detection, limit of quantification, robustness and ruggedness were determined according to International Conference on harmonization ICH Q2B guidelines. Chromatography was carried out by gradient technique on a reverse phase C-18 Inertsil ODS 3V using Agilent Chemstation 1200 series equipped with photo diode array detector (λ = 273nm) with mobile phase based and optimized depending on the polarity of the molecule. All the system suitability parameters were found within the range. The proposed method is highly sensitive, precise and hence successfully applied to the chromatographic purity of lamivudine active pharmaceutical ingredient (API).Colegio de Farmacéuticos de la Provincia de Buenos Aire

A comprehensive review on biological activities of oxazole derivatives

Abstract The utility of oxazole as intermediates for the synthesis of new chemical entities in medicinal chemistry have been increased in the past few years. Oxazole is an important heterocyclic nucleus having a wide spectrum of biological activities which drew the attention of researchers round the globe to synthesize various oxazole derivatives and screen them for their various biological activities. The present review article aims to review the work reported on therapeutic potentials of oxazole scaffolds which are valuable for medical applications during new millennium

Anticancer Potential of Triazine Scaffold: A Brief Review

Triazine is an important class of heterocyclic compounds. Triazine is a six-membered heterocyclic compound with three carbons replaced by nitrogen in the benzene ring. Triazine and its compounds exhibit a wide variety of pharmacological activity such as antifungal, anti-HIV, anticancer, antioxidant, anti-inflammatory, analgesic, antihypertensive, antiviral, antimalarial, antiprotozoal, and antibacterial. The triazine ring has been modified at different positions to generate new molecules. The structure of the new derivatives was characterized by common analytical method. Some examples of triazine compounds commonly used in rational medicine are: Ceftriaxone as an antimicrobial agent and 6-Azacytosine as an antiviral agent. The present review article enumerates on the biological potential of triazine and how it is beneficial to discover more new compounds that could be better in terms of efficacy and lesser toxicity

To Evaluate In Vitro Acetylcholinesterase Inhibitory Activity of Various Indian Medicinal Plants

Medicinal herbs are active in curing various disorders by their distinct characteristics. In this research, antioxidant and acetylcholinesterase (AChEI) inhibitory activity of Achyranthes aspera, Psidium guajava, Anthocephalus cadamba, Carissa carandas, Caesalpinia bonduc, Indian medicinal plants have been evaluated by collecting and extracting selected plants parts by using different solvents followed by assessment of AChEI inhibitory activity by autographic assay (TLC method) and microplate assay (Ellman method). Further assessment of antioxidant activity of selected plants by 2, 2-diphenyl-1-picrylhydryzyl method was done. In autographic assay, C. bonduc had more AChE inhibitory potential than other selected plants. In microplate assay method, C. bonduc has shown lowest IC50 value among all other extracts, suggesting its highest enzymatic inhibitory potential and C. carandas has been shown highest IC50 value, suggesting a lower enzymatic inhibitory potential. The Rf value of C. bonduc, A. aspera, P. guajava, A. cadamba, and C. carandas was found to be 0.71, 0.5, 0.3, 0.45 and 0.2, respectively. From the results, leaves of P. guajava showed good antioxidant potential and C. bonduc seeds showed maximum cholinesterase inhibitory activity

Ayurveda: A Boon in Pandemics

Population around the world is dealing with an unrivalled pandemic of viral disease severe acute respiratory syndrome coronavirus 2 leading to severe acute respiratory syndrome. The novel coronavirus has affected people worldwide with more than 1.43 million confirmed cases and 82,100 deaths as per data recorded on April 8, 2020. The pandemic has elevated the distress in common people including the psychological conditions with symptoms such as depression and anxiety. The psychological distress is linked with variation in the functioning of immunological responses including high level risk for viral infections of the upper respiratory tract. The extent of pandemic requires exploration of traditional as well as modern knowledge systems obtainable worldwide. Use of traditional Chinese Medicinal system in Wuhan for the treatment of patients suffering from coronavirus disease 2019 (COVID-19) has set an example illustrating the efficiency of traditional ways of healthcare as an addition in treatment of patients of COVID-19. In India, Ayurveda is medicine system with historical roots encouraged by Government of India as “immune booster regime.” Implementation of Ayurvedic knowledge and administration of Ayurvedic dosages with the present scientific studies on related clinical settings is an efficient plan for intervention in India for the treatment of patients suffering from COVID-19. In accordance to severity of symptoms and stage of infection among the patients, Ayurvedic dose regime can be administered in both symptomatic and asymptomatic patients. Implementation of Ayurvedic medicinal system will ease learning and develop evidence as we cannot combat the reality that there is no evidence-based treatment for COVID-19. Therefore, Ayurvedic system of medicine should be implemented immediately to abate the impact of pandemic in terms of diminishing both psychological distress and risk of infection. Development of such elucidatory models will shed the light on the effectiveness of traditional medicines and medical practices during disease surges and could aid the symbiosis between traditional and modern medicinal system

Design, synthesis and biological evaluation of 3-(2-aminooxazol-5-yl)-2H-chromen-2-one derivatives

Abstract Background In view of wide range of biological activities of oxazole, a new series of oxazole analogues was synthesized and its chemical structures were confirmed by spectral data (Proton/Carbon-NMR, IR, MS etc.). The synthesized oxazole derivatives were screened for their antimicrobial and antiproliferative activities. Results and discussion The antimicrobial activity was performed against selected fungal and bacterial strains using tube dilution method. The antiproliferative potential was evaluated against human colorectal carcinoma (HCT116) and oestrogen- positive human breast carcinoma (MCF7) cancer cell lines using Sulforhodamine B assay and, results were compared to standard drugs, 5-fluorouracil and tamoxifen, respectively. Conclusion The performed antimicrobial activity indicated that compounds 3, 5, 6, 8 and 14 showed promising activity against selected microbial species. Antiproliferative screening found compound 14 to be the most potent compound against HCT116 (IC50 = 71.8 µM), whereas Compound 6 was the most potent against MCF7 (IC50 = 74.1 µM). Further, the molecular docking study has been carried to find out the interaction between active oxazole compounds with CDK8 (HCT116) and ER-α (MCF7) proteins indicated that compound 14 and 6 showed good dock score with better potency within the ATP binding pocket and may be used as a lead for rational drug designing of the anticancer molecule

Design, synthesis and biological potential of heterocyclic benzoxazole scaffolds as promising antimicrobial and anticancer agents

Abstract Background Benzoxazole is the most important class of heterocyclic compound in medicinal chemistry. It has been incorporated in many medicinal compounds making it a versatile heterocyclic compound that possess a wide spectrum of biological activities. Results The molecular structures of synthesized benzoxazole derivatives were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity against selected microbial species using tube dilution method and antiproliferative activity against human colorectal carcinoma (HCT 116) cancer cell line by Sulforhodamine B assay. Conclusion In vitro antimicrobial results demonstrated that compounds 4, 5, 7 and 16 showed promising antimicrobial potential. The in vitro anticancer activity indicated that compounds 4 and 16 showed promising anticancer activity against human colorectal cancer cell line (HCT 116) when compared to standard drug and these compounds may serve as lead compound for further development of novel antimicrobial and anticancer agents

Benzoxazole derivatives: design, synthesis and biological evaluation

Abstract Background A new series of benzoxazole analogues was synthesized and checked for their in vitro antibacterial, antifungal and anticancer activities. Results and discussion The synthesized benzoxazole compounds were confirmed by IR, 1H/13C-NMR, mass and screened for their in vitro antimicrobial activity against Gram-positive bacterium: Bacillus subtilis, four Gram-negative bacteria: Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi and two fungal strains: Candida albicans and Aspergillus niger using tube dilution technique and minimum inhibitory concentration (MIC) was noted in µM and compared to ofloxacin and fluconazole. Human colorectal carcinoma (HCT116) cancer cell line was used for the determination of in vitro anticancer activity (IC50 value) by Sulforhodamine B assay using 5-fluorouracil as standard drug. Conclusion The performed study indicated that the compounds 1, 10, 13, 16, 19, 20 and 24 had highest antimicrobial activity with MIC values comparable to ofloxacin and fluconazole and compounds 4, 6, 25 and 26 had best anticancer activity in comparison to 5-fluorouracil