Author: ScienceIn

Chemical composition and additive inhibitory activity of combination of Mentha piperita, Cinnamonum vernum & Jasminum officinale essential oils as an alternative therapy against Dermatophytosis

The antifungal potential of Peppermint, Cinnamon & Jasmine essential oils alone and in combination, against common causes of superficial fungal infections in humans was investigated via in-vitro investigations, in order to determine a suitable dosage for use in clinical trials. Antimycotic activity of three plant derived Essential oils (EOs) namely Mentha piperita, Cinnamonum vernum & Jasminum officinale were evaluated against Trichophyton equinum and Microsporum canis, causative agent of zoonotic dermatophytosis by Disc diffusion method alone and in mixture and further determination of Minimum Inhibitory Concentration (MIC) by modified Microdilution method. Chemical compositions of M.piperita, C.vernum & J. officinale essential oil were determined by Gas chromatography Mass spectrometry (GC-MS). In M.piperita essential oil, thirteen compounds, C.vernum, ten compounds and J. officinale, fifteen compounds were identified by GC-MS. The excellent antidermatophytic activity of mixture of oils was found against M.canis & T.equinum as compared to single oils and standard drugs used. The results concluded that the combination of three essential oils showed remarkable and excellent inhibitory activity against fungal pathogens and can be used as an alternative topical therapy for the treatment of dermatophytosis after undergoing clinical trials and also regarded as an environmentally safe mode of diseases control.

URN:NBN:sciencein.cbl.2023.v10.550

The synthesis of new hybrid [1,2,4] triazolo [3,4-b][1,3,4]thiadiazine derivatives of imidazole (5a – 5m) and their structure determination using ¹HNMR, ¹³CNMR and mass spectral analysis were described. The in vitro cytotoxic activity of the compounds (5a – 5m) against three human cancer cell lines like MCF-7 and MDA-MB-231 (breast), alveolar (A-549) revealed that the compounds 5c, 5d, 5f, 5g, and 5m have shown greater activity against breast cancer cell lines than the remaining compounds. Compounds 5d and 5f have shown equipotent activity compared to the standard. In vitro tyrosine kinase EGFR inhibition assay for the same more potent compounds (5c, 5d, 5f, 5g, and 5m) revealed that 5f has more potent inhibiting power with an IC₅₀ value of 0.412±0.05 μM and 5d has equipotent inhibiting power with an IC₅₀ value of 0.436±0.07 μM compared to erlotinib (IC₅₀=0.423±0.03).

URN:NBN:sciencein.cbl.2023.v10.548

The expanding field of bioorthogonal chemistry has demonstrated significant potential in advancing reproductive medicine. This comprehensive review elucidates the multifaceted applications of bioorthogonal chemistry across various aspects of reproductive medicine, including gamete biology, energetics and metabolic regulations of gametes, targeted drug delivery, detection and therapeutic of endometriosis and polycystic ovarian syndrome (PCOS), developments of diagnostic tools and new management approaches to reproductive cancers. In gamete biology, bioorthogonal reactions enable the precise manipulation and tracking of biomolecules within gametes, thus facilitating a deeper understanding of gamete development, maturation, and interaction. Bioorthogonal chemistry also plays an indispensable role in deciphering the intricate energetics and metabolic regulations governing gamete function and competence, consequently fostering the development of novel therapeutic interventions. Targeted drug delivery, utilizing bioorthogonal click chemistry, can improve the specificity and efficacy of pharmacological treatments in reproductive disorders, such as endometriosis and PCOS. In the realm of reproductive diagnostics, bioorthogonal chemistry engenders innovative tools for sensitive and noninvasive detection of reproductive anomalies. Finally, the integration of bioorthogonal strategies in studying reproductive cancers can uncover new molecular targets for therapeutics, leading to more effective treatment modalities. Collectively, this review highlights the paramount importance of bioorthogonal chemistry in revolutionizing reproductive medicine and fostering breakthroughs in the comprehension and management of reproductive health.

URN:NBN:sciencein.cbl.2023.v10.545

Herein, synthesis of new Nilutamide-isoxazoles (5a-5n) via Cu(I)-promoted one-pot reaction between 1-(but-3-yn-1-yl)-5,5-dimethyl-3-(4-nitro-3-(trifluoromethyl)phenyl)imidazolidine-2,4-dione (3) and several aldehydes (4a-4n) in benign aq. ^tbutanol as key approach has been reported. The in vitro growth inhibition activity of all these compounds revealed that the majority of compounds were more active against DU-145 in comparison to PC3. Particularly, compounds 5f, 5h and 5k showed greater activity against DU-145 than the standard drug 5-Fluoro Uracil with IC₅₀ values <30 mM. whereas compound 5g showed comparable activity against DU-145 cell line with the positive control. The Epidermal growth factor receptor (EGFR) is well known to be expressed in DU-145 cancer cells, the most potent compounds 5f, 5h and 5k were then screened for their inhibitory potential against tyrosine kinase EGFR and found that compounds 5f and 5k showed remarkable inhibition with MIVs 93.4% and 91.3% respectively, while compound 5h displayed good inhibition (MIV = 84.6%) as compared to the Erlotinib.

URN:NBN:sciencein.cbl.2023.v10.542

A library of twenty novel analogues of fluorinated, N-(3-hydroxy-1-phenyl-4-(4-phenylpiperazin-1-yl)alkyl)amides containing different amino acids were synthesized and tested for the activity against Plasmodium falciparum (Pf3D7) culture. All the tested compounds showed TC₅₀ values >100 µM on HepG2 cells. Hit analogues 12c and 12e, displayed IC₅₀ values in the sub-micromolar range, i.e., 0.696±0.0462 µM and 0.9377±0.0461 µM, respectively. Compounds 12c and 12e were also evaluated in combination with artemisinin, which slightly improved the activity of both the compounds with IC₅₀ values of 0.19 µM and 0.26 µM, respectively. For compounds 12c and 12e, in-silico studies were carried out. Overall, results obtained from both in vitro and in-silico studies, indicated that 12c and 12e were hit compounds with maximum potency.

URN:NBN:sciencein.cbl.2023.v10.543

The search for an antidiabetic drug is going on three fronts: technological (for instance, development of an artificial pancreas), biological (such as pancreas and islet cell transplants), and pharmacological. Our review focusses on the role of polyphenolics in pharmacological research for T2DM. Being the most abundant antioxidants in human diets, dietary polyphenols have proven efficacy against a variety of diseases in both animal and human trials. Here, the authors present a review of advances in using polyphenols obtained from diet against diabetes and metabolic syndrome. Authors have discussed the role of polyphenols in disease management, and their sources. In addition to that, current knowledge of prevalent pathways of their action in cases of diabetes and metabolic syndrome have been discussed. The future directions and perspectives about diet polyphenols as a good alternative to first-line drug interventions have been included.