Author: ScienceIn

Herein we synthesized new indole-thiazolidine-2,4-dione coupled isoxazoles (7a-n) via simple reactions like N-propargylation, Knoevenagel condensation and copper (I) catalysed one pot regioselective reactions. All the newly synthesized compounds were characterized by 1H-NMR, 13C-NMR and Mass spectra and they were screened for in vitro anticancer activity against three human cancer cell lines like A549 (lung), MCF-7 (breast), and SKOV3 (ovarian) using MTT assay and etoposide was used as the standard drug. As per the results the compounds 7e, 7f and 7g where shown selectivity towards A549 cell line with IC₅₀ values of 5.27 µM, 3.14 µM and 6.25 µM respectively and they are high active than etoposide. Further in vitro tubulin polymerization assay on three potent compounds (7e, 7f and 7g) revealed that compounds 7e and 7f have exhibited potency than standard combretastatin A-4 with IC₅₀ values 0.82 and .044 mM respectively.

URN:NBN:sciencein.cbl.2023.v10.531

Yucca gloriosa L. has been comprehensively assessed in vitro and in vivo for its action against asthma. Y. gloriosa L. is a rich source of phenolic compounds such as gloriosaols A-E and yuccaols A-E, which exhibit potent antioxidant activity. Gloriosaols A-E and yuccaols A-E are structurally related to corticosteroids. The current study describes the in silico docking of some important anti-asthmatic phytoconstituents from the plant Y. gloriosa L. with molecular targets of asthma. Toward the recognition of the binding methods of these pharmacologically dynamic components, molecular modelling studies were carried out with target proteins, i.e., interleukin (IL)-6 (1N26), IL-13 (3LB6) and TNF-α (2AZ5), using in silico molecular docking. The components demonstrated encouraging binding interactions with the amino acid residues at the active sites of these proteins, authenticating their verified efficiency as anti-asthmatic agents. The current research, in addition, provides insight into the possible herbal drug-receptor interaction and synthetic drug montelukast sodium receptor interaction, for the possible management of asthma.

URN:NBN:sciencein.cbl.2023.v10.509

Present investigation aimed to study the antimycobacterial potential of Mentha piperita essential oil fractions, identify its active constituents by GC-MS and preparation of nanoemulsion from biologically active fraction. Four oil fractions (R1, R2, R3, R4) were collected during hydrodistillation of Mentha piperiata leaves and tested in the two of mycobacterial strains by conventional disc diffusion method. Oil fractions R2 and R3 demonstrated maximum zone of inhibition of 39 mm and 36 mm in Mycobacterium smegmatis, 33 mm and 31 mm in Mycobacterium bovis BCG respectively at a dilution of 75% in DMSO compared to standard drug isoniazid (23 mm in 4 µg/ml). GC-MS analysis of the most active fraction R2 reveals the presence of menthol (70.69%), isomenthone (14.63%) and neomenthol (6.82%) as major constituents. To enhance bioavailability of oil fraction, the nanoemulsions were prepared from R2 by sonication method. Nanoemulsions, N1 and N2 prepared by varying surfactant concentrations were tested in Mycobacterium bovis BCG using quantitative and colorimetric resazurin microtiter assay (REMA). Nanoemulsions, N1 and N2 have shown 97-100 % bacterial growth inhibition at 3.125 % concentration in the culture medium compared with the culture control.

URN:NBN:sciencein.cbl.2023.v10.507

Metformin is a widely used anti-diabetic drug that enhances glycaemic control by advancing the insulin sensitivity abatement of intestinal glucose absorption. Due to its versatility, it is also emerging as an abused drug leading to toxicity and fatal conditions. Detection of metformin with the existing qualitative and quantitative approaches necessitate complex and intricate instrumentation, fully facilitated laboratories, and trained scientist and technicians. Henceforth, in the current study, we have developed a hand-held electronic device-based detection system for metformin using the basic principles of spectrophotometry. It is based on the formation of a yellowish-green color complex (wavelength 680nm) which involves the oxidative coupling of 3-methyl 2-benzothiozoline hydrazone (MBTH) catalyzed by iron. The method developed has been optimized at different pH, reaction temperature, and reaction time and found to be specific, sensitive, and linear in the range of concentration 100-1000 µg/ml with the limit of detection (LOD) of 120.5 µg/ml.

URN:NBN:sciencein.cbl.2023.v10.486

Cancer is one of the most fatal diseases of recent times that causes several deaths every year. The disease variations in different parts of the world, the impact of available medical facilities, and other socio-economic factors have impacted the proper management of this disease. The comparative statistical data of cancer types like breast, prostate, colon, lung, lymph, blood, brain, and kidney cancers can be used to design treatment strategies and therapeutics development. With the advancement of science, several drugs besides diagnostic methods have emerged to control respective cancer and have assisted in curing this disease to some extent. The comparative statistics analysis for cancer about current prevalence is included here to bring a clear framework for the efforts towards future drug development to manage this disease. The availability of new diagnostics and therapeutics and advanced medical facilities in clinics impact cancer statistics. An evaluation of current trends and statistics of cancer pathology vis-à-vis theranostics (diagnostics as well as therapeutics) progress with possible application in clinical settings constitutes the core part of the discussion in this review.

URN:NBN:sciencein.cbl.2023.v10.451

The one-pot synthesis of some novel imidazole-isoxazole hybrids (5a-5n) and their in vitro antibacterial evaluation against Bacillus subtilis and Staphylococcus aureus was described herein. Among all, compounds 5f, 5g, 5i and 5j displayed greater zone of inhibition on Staphylococcus aureus than the standard streptomycin. Besides, compounds 5f, 5g, 5h, 5i, 5j and 5k displayed higher zone of inhibition towards Bacillus subtilis than the standard. Lastly, minimum inhibitory concentration (MIC) studies of active compounds 5f, 5g, 5h, 5i, 5j and 5k showed that the compounds 5i and 5j having lesser MIC values on Staphylococcus aureus and Bacillus subtilis than the standard.

URN:NBN:sciencein.cbl.2022.v9.425