Facile synthesis and in silico studies of benzothiazole-linked hydroxypyrazolones targeting α-amylase and α-glucosidase.

Aim: The objective of the present investigation was to design and synthesize new heterocyclic hybrids comprising benzothiazole and indenopyrazolone pharmacophoric units in a single molecular framework targeting α-amylase and α-glucosidase enzymatic inhibition. Materials & methods: 20 new benzothiazole-appended indenopyrazoles, 3a-t, were synthesized in good yields under environment-friendly conditions via cycloaddition reaction, and assessed for antidiabetic activity against α-amylase and α-glucosidase, using acarbose as the standard reference. Results: Among all the hydroxypyrazolones, 3p and 3r showed the best inhibition against α-amylase and α-glucosidase, which finds support from molecular docking and dynamic studies. Conclusion: Compounds 3p and 3r have been identified as promising antidiabetic agents against α-amylase and α-glucosidase and could be considered valuable leads for further optimization of antidiabetic agents.

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Revisiting the ethnomedicinal, ethnopharmacological, phytoconstituents and phytoremediation of the plant Solanum viarum Dunal.

Solanum viarum, a perennial shrub, belongs to the family Solanaceae known for its therapeutic value worldwide. As a beneficial remedial plant, it is used for treating several disorders like dysentery, diabetes, inflammation, and respiratory disorders. Phytochemistry studies of this plant have shown the presence of steroidal glycoside alkaloids, including solasonine, solasodine, and solamargine. It also has flavonoids, saponins, minerals, and other substances. S. viarum extracts and compounds possess a variety of pharmacological effects, including antipyretic, antioxidant, antibacterial, insecticidal, analgesic, and anticancer activity. Most of the heavy metals accumulate in the aerial sections of the plant which is considered a potential phytoremediation, a highly effective method for the treatment of metal-polluted soils. We emphasize the forgoing outline of S. viarum, as well as its ethnomedicinal and ethnopharmacological applications, the chemistry of its secondary metabolites, and heavy metal toxicity. In addition to describing the antitumor activity of compounds and their mechanisms of action isolated from S. viarum, liabilities are also explained and illustrated, including any significant chemical or metabolic stability and toxicity risks. A comprehensive list of information was compiled from Science Direct, PubMed, Google Scholar, and Web of Science using different key phrases (traditional use, ethnomedicinal plants, western Himalaya, Himachal Pradesh, S viarum, and biological activity). According to the findings of this study, we hope that this review will inspire further studies along the drug discovery pathway of the chemicals extracted from the plant of S. viarum. Further, this review shows that ethnopharmacological information from ethnomedicinal plants can be a promising approach to drug discovery for cancer and diabetes.

Recent advancement of nanomedicine-based targeted delivery for cervical cancer treatment.

Cervical cancer is a huge worldwide health burden, impacting women in impoverished nations in particular. Traditional therapeutic approaches, such as surgery, radiation therapy, and chemotherapy, frequently result in systemic toxicity and ineffectiveness. Nanomedicine has emerged as a viable strategy for targeted delivery of therapeutic drugs to cancer cells while decreasing off-target effects and increasing treatment success in recent years. Nanomedicine for cervical cancer introduces several novel aspects that distinguish it from previous treatment options such as tailored delivery system, precision targeting, combination therapies, real-time monitoring and diverse nanocarriers to overcome the limitations of one another. This abstract presents recent advances in nanomedicine-based tailored delivery systems for the treatment of cervical cancer. Liposomes, polymeric nanoparticles, dendrimers, and carbon nanotubes have all been intensively studied for their ability to transport chemotherapeutic medicines, nucleic acids, and imaging agents to cervical cancer cells. Because of the way these nanocarriers are designed, they may cross biological barriers and preferentially aggregate at the tumor site, boosting medicine concentration and lowering negative effects on healthy tissues. Surface modification of nanocarriers with targeting ligands like antibodies, peptides, or aptamers improves specificity for cancer cells by identifying overexpressed receptors or antigens on the tumor surface. Furthermore, nanomedicine-based techniques have made it possible to co-deliver numerous therapeutic drugs, allowing for synergistic effects and overcoming drug resistance. In preclinical and clinical investigations, combination treatments comprising chemotherapeutic medicines, gene therapy, immunotherapy, and photodynamic therapy have showed encouraging results, opening up new avenues for individualized and multimodal treatment regimens. Furthermore, the inclusion of contrast agents and imaging probes into nanocarrier systems has enabled real-time monitoring and imaging of treatment response. This enables the assessment of therapy efficacy, the early diagnosis of recurrence, and the optimization of treatment regimens.