Design, Synthesis, Characterization and in vivo Antidiabetic Activity Evaluation of Some Chalcone Derivatives.
Reads0
Chats0
TLDR
In this paper, the chalcone derivatives were evaluated for their relative antidiabetic activities in vivo using streptozotocin (STZ)-induced diabetic mice, and the compounds were assessed for their reduction in post-prandial hyperglycemia at 50 and 100 mg/kg dose levels against a standard drug, glibenclamide.Abstract:
Background Diabetes is one of the growing health problems worldwide, and scientists have been striving to find effective treatment methods. In this regard, chalcones have frequently been targeted by many researchers owing to their diverse biological activities. Methods Here, the Claisen-Schmidt condensation reaction was applied to synthesize five chalcone derivatives. The chalcone derivatives were evaluated for their relative antidiabetic activities in vivo using streptozotocin (STZ)-induced diabetic mice. Besides, the compounds were assessed for their reduction in postprandial hyperglycemia at 50 and 100 mg/kg dose levels against a standard drug, glibenclamide. In addition, the structure-activity relationship (SAR) was analyzed to determine the effect of structural modification in chalcones activity. Results A dose-dependent reduction in postprandial hyperglycemia was observed. The highest reduction in blood glucose level (BGL) was achieved by compound 3 at a dose of 100 mg/kg (39%). This was found to be even higher than glibenclamide (34.5%). In the STZ-induced diabetic animal model, all test compounds showed comparable efficacy with glibenclamide. The SAR analysis revealed that the incorporation of electron-donating groups at position 5 of the benzaldehyde ring and position 2 of the acetophenone ring is promising to increase the antihyperglycemic activities of chalcones. Conclusion The chalcone derivatives considered in this study could be used as potential lead compounds in the discovery of effective drugs to treat diabetes mellitus.read more
Citations
More filters
Journal ArticleDOI
Synthesis of Chalcones Derivatives and Their Biological Activities: A Review
TL;DR: In this paper , the most recent synthesis of chalcones bearing N, O, and/or S heterocycles, revealing their biological potential during the past decade (2010-2021).
Journal ArticleDOI
Discovery of chalcone derivatives as potential α-glucosidase and cholinesterase inhibitors: Effect of hyperglycemia in paving a path to dementia
Hanan A. Al-Ghulikah,Ehsan Ullah Mughal,Eslam B. Elkaeed,Nafeesa Naeem,Yasir Nazir,Abdullah Ibrahim Abdullah Alzahrani,Amina Sadiq,Syed Wadood Ali Shah +7 more
TL;DR: In this article , a series of fascinating chalcone derivatives 1C-14C has been designed and synthesized by Claisen-Schmidt condensation, and the target compounds were screened for in vitro α-glucosidase and cholinesterase inhibitory activities.
Journal ArticleDOI
Two Important Anticancer Mechanisms of Natural and Synthetic Chalcones
T Constantinescu,Alin Mihis +1 more
TL;DR: ATP-binding cassette subfamily G and tubulin pharmacological mechanisms decrease the effectiveness of anticancer drugs by modulating drug absorption and by creating tubulin assembly through polymerization by modulation.
Journal ArticleDOI
Facile synthesis, antimicrobial screening and docking studies of pyrrole-triazole hybrids as potential antimicrobial agents
Journal ArticleDOI
Antifungal Assay of some Novel Chalcone Derivatives
TL;DR: In this article , the antifungal assay of synthesized compounds against some pathogens viz Candida albicans, Trichophyton rubrum, Aspergillus niger, and T. mentago forum which are mainly responsible for the diseases in ornamental plants.
References
More filters
Journal ArticleDOI
IDF Diabetes Atlas: Global estimates for the prevalence of diabetes for 2015 and 2040.
Katherine Ogurtsova,J. D. da Rocha Fernandes,Yadi Huang,Ute Linnenkamp,Leonor Guariguata,Nam H. Cho,Nam H. Cho,David Cavan,Jonathan E. Shaw,Lydia Makaroff,Lydia Makaroff +10 more
TL;DR: Diabetes prevalence, deaths attributable to diabetes, and health expenditure due to diabetes continue to rise across the globe with important social, financial and health system implications.
Journal ArticleDOI
IDF Diabetes Atlas: Global estimates of diabetes prevalence for 2017 and projections for 2045.
Nam H. Cho,Nam H. Cho,Jonathan E. Shaw,Suvi Karuranga,Yadi Huang,J. D. da Rocha Fernandes,A.W. Ohlrogge,Belma Malanda +7 more
TL;DR: The new estimates of diabetes prevalence, deaths attributable to diabetes and healthcare expenditure due to diabetes present a large social, financial and health system burden across the world.
Journal ArticleDOI
Chalcone: A Privileged Structure in Medicinal Chemistry.
TL;DR: This review aims to highlight the recent evidence of chalcone as a privileged scaffold in medicinal chemistry and is expected to be a comprehensive, authoritative, and critical review of the chal cone template to the chemistry community.
Journal ArticleDOI
Single dose streptozotocin-induced diabetes: considerations for study design in islet transplantation models.
Michael C. Deeds,Jarett M. Anderson,Adam Armstrong,Dennis A. Gastineau,Henry J. Hiddinga,A Jahangir,Norman L. Eberhardt,Yogish C. Kudva +7 more
TL;DR: The literature is reviewed and data from pancreatic islet transplantation experiments using single high-dose STZ-induced DM in NCr athymic nude mice are provided with hopes of providing clarification for study design, suggesting refinements to the process, and developing a more humane process of chemical diabetes induction.
Journal ArticleDOI
Exploring Pharmacological Significance of Chalcone Scaffold: A Review
TL;DR: A review of the pharmacological activity of naturally occurring and synthetic chalcones, which highlights more recent pharmacological screening of these compounds, their mechanisms of action and relevant structure-activity relationships.