Development and characterisation of buccal dispersible film, syrup and effervescent granules of extemporaneous antigout remedy.

Homemade medicinal remedies used to treat both acute and chronic ailments for centuries need to be transformed into modern evidence-based dosage forms. Therefore, the present study aimed to develop buccal dispersible film, syrup and effervescent granules of an extemporaneous antigout homemade remedy. The dosage forms were prepared using holistic remedy (HR) as an active entity and excipients masking disagreeable features. The dosage forms and HR were subjected to physicochemical evaluation, and standardised by a reversed-phase HPLC method using chlorogenic acid, caffeic acid, vanillin, and ferulic acid as analytical standards. The standardised dosage forms were investigated for antigout activity using an appropriate model. The dosage forms were found to be physically elegant and phytochemically aligned with HR. The developed dosage forms contained the selected markers and possessed antigout activity. Hence, these standardised and evidence-based dosage forms may have wider acceptance in the market compared to HR.

Design, synthesis, biological evaluation and molecular docking studies of quinoline-anthranilic acid hybrids as potent anti-inflammatory drugs.

Despite the high global prevalence, rheumatoid arthritis lacks a satisfactory treatment. Hence, the present study is undertaken to design and synthesize novel anti-inflammatory compounds. For this, quinoline and anthranilic acid, two medicinally-privileged moieties, were linked by pharmacophore hybridization, and following their computational assessments, three hybrids 5a-c were synthesized in good over all yields. The in vitro and in vivo anti-inflammatory potential of these hybrids was determined by anti-denaturation and anti-proteinase, and carrageenan-induced paw edema models. The computational studies of these hybrids revealed their drug-likeness, optimum pharmacokinetics, and less toxicity. Moreover, they demonstrated high binding affinity (-9.4 to -10.6 kcal mol-1) and suitable binding interactions for TNF-α, FLAP, and COX-II. A three-step synthetic route resulted in the hybrids 5a-c with 83-86% yield of final step. At 50 µg mL-1, the antiprotease and anti-denaturation activity of compound 5b was significantly higher than 5a and 5c. Furthermore, 5b significantly reduced the edema in the right paw of the rats that received carrageenan. The results of this study indicate the medicinal worth of the novel hybrids in treating inflammatory disorders such as rheumatoid arthritis.

Microscopic, phytochemical and antibacterial studies of Zizyphus oxyphylla Edgew. leaves.

Microscopic, phytochemical and pharmacological profiles are required for correct identification of a plant material to ensure consistent efficacy and safety. But such data are not available for the leaf of an important medicinal plant, Zizyphus oxyphylla Edgew. (Family: Rhamnaceae). Therefore, the current study aimed to investigate leaves of the plant for microscopic, phytochemical and antibacterial studies. Powdered material was subjected to microscopy, proximate analyses and estimation of total primary metabolites. Then, different types of extracts prepared using various solvents in order of increasing polarity were screened for antibacterial activity against seven standard strains. The most active extract was hydrolyzed and aglycone enriched fraction was extracted and screened for antibacterial activity. The powder microscopy indicated the presence of vascular bundles filled with cuboidal calcium oxalate crystals, anisocytic stomata and xylary vessels with reticulate and scalariform thickenings. Proximate features and primary metabolites provided characteristic identifying patterns. The most active extract (methanol) upon acidic hydrolysis exhibited higher activity against B. bronchiseptica (26.01±0.01 mm), S. aureus (26.00±0.00 mm), P. aeruginosa (24.03±0.02 mm) and M. luteus (24.02± 0.00 mm). The results of the current study provide identifying microscopic and phytochemical profiles that may be useful for correct identification of leaves of the plant. Aglycone enriched extract is having remarkable antibacterial activity hence may be used for activity-guided isolation.

COVID-19 vaccines: Development, strategies, types and vaccine usage hesitancy / Vacunas contra la COVID-19: desarrollo, estrategias, tipos y reticencia al uso de la vacunación

Vaccine development using different platforms is one of the important strategies to address coronavirus disease pandemic. The global need for vaccines requires effective vaccine approaches and collaboration between pharmaceutical and biotechnological companies, governments and the industrial and academic sectors. About 72 percent of the vaccine candidates are being developed by the private sector, while 28 percent are carried out by the public sector and different non-profit organizations. COVID-19 vaccines are based on complete viruses (inactivated or attenuated), viral vectors (replicating or not), antigenic subunits (proteins or peptides), nucleic acids (RNA or DNA) or virus-like particles. Important aspects of vaccine development include manufacturing flexibility, speed, cost, safety, cellular and humoral immunogenicity, vaccine stability and cold chain maintenance. Vaccines can be prepared using different manufacturing platforms, computational biology, gene synthesis, structure-based antigen design and protein engineering. Individual confidence, convenience and complacency are factors that affect the attitude towards acceptance of COVID-19 vaccination. This could be complicated by socio-demographic, psychologic, cognitive and cultural factors(AU)

El desarrollo de vacunas utilizando diferentes plataformas es una de las estrategias importantes para abordar la pandemia de COVID-19. La necesidad mundial de vacunas requiere enfoques de vacunas eficaces y la colaboración entre las empresas farmacéuticas y biotecnológicas, los gobiernos y los sectores industrial y académico. Alrededor del 72 por ciento de los candidatos vacunales están siendo desarrolladas por el sector privado, mientras que el 28 por ciento, por el sector público y diferentes organizaciones sin fines de lucro. Las vacunas contra la COVID-19 se basan en virus completos (inactivados o atenuados), vectores virales (replicantes o no), subunidades antigénicas (proteínas o péptidos), ácidos nucleicos (ARN o ADN) o partículas similares a virus. Aspectos importantes del desarrollo de vacunas incluyen la flexibilidad de fabricación, la velocidad, el costo, la seguridad, la inmunogenicidad celular y humoral, la estabilidad de la vacuna y el mantenimiento de la cadena de frío. Las vacunas se pueden preparar con precisión utilizando diferentes plataformas de fabricación, biología computacional, síntesis de genes, diseño de antígenos basado en estructuras e ingeniería de proteínas. La confianza individual, la conveniencia y la complacencia son factores que afectan la actitud hacia la aceptación de la vacunación contra la COVID-19. Esto podría complicarse por factores sociodemográficos, psicológicos, cognitivos y culturales(AU)

In vitro antioxidant potential and antiproliferative activity of Aesculus indica seed extract against hepatocellular carcinoma cell line.

Therapeutic secondary metabolites have gained immense attention in recent years due to their effective medicinal properties. Aesculus indica is a medicinally important plant being traditionally used for various ailments. The present study aimed to determine the antioxidant and antiproliferative activities of seeds of A. indica. The crude methanolic seed extract was prepared and subjected to sequential fractionation in increasing polarity. The extract and its fractions were investigated for antioxidant activities using various in vitro assays. Further, the extract along with its potential antioxidant fractions were analyzed for their cytotoxic activity against HepG2, human hepatocyte carcinoma cells through bioassays. The results showed highly significant antioxidant potential of methanolic extract of A. indica seeds and two of its fractions prepared with chloroform and ethyl acetate. The studies on hepatocyte carcinoma cells further revealed that the extract and two of its potential antioxidant fractions significantly induced cytotoxicity and inhibited migration, proliferation, clonogenicity and 3D growth of HepG2 cells. It is therefore, concluded that A. indica possess significant antioxidant and cytotoxic potential against HepG2 cells and with further research can be proposed for therapeutic interventions.