Aim: α-Glucosidase inhibitors are important oral antidiabetic drugs that are used alone or in combination therapy. Materials & methods: In this regard, 1,3,4-thiadiazoles–1,2,3-triazoles were designed, synthesized and evaluated for α-glucosidase enzyme inhibition. Results: The applied synthesis protocol involved a ‘click’ reaction between a novel alkyne derived from a 1,3,4-thiadiazole derivative and phenylacetamide azides. The hybrid (9n) bearing 2-methyl and 4-nitro substituents was the best inhibitor with an IC50 value of 31.91 μM (acarbose IC50 = 844.81 μM). The blind molecular docking study of the best derivative (9n) showed that it interacted with the allosteric site's amino acid residues of α-glucosidase. Conclusion: 'Click'-inspired potential α-glucosidase inhibitors (1,3,4-thiadiazole–1,2,3-triazole hybrids) were identified and structure–activity relationship and kinetic and molecular docking studies accomplished.
Background:
Sorghum, a wonder millet, is well known for its beneficial phytochemical profiles. In comparative terms, juice from sweet sorghum has better commercial potential as syrup in several food-based applications. Various sweet sorghum differs in their profile of various phytochemicals, which can impact the commercial potential of sweet sorghum juice.
Methods:
Our previous works on cultivars developed at ICAR-IIMR were screened for phytochemical, sugar and mineral profile. To give a holistic view of the phytochemical profile of sweet sorghum varieties, the present study is attempted to evaluate the total phenolic and flavonoid content, antihyperglycaemic and cytotoxic profile of the components present in the varieties CSV19SS, SSV84, SSV74. The phytochemical footprint of sweet sorghum juice was studied through HRLCMS.
Results:
The results showed ethyl acetate extract of SSV84 having potential antihyperglycemic effects with an IC50 of 22.156 ± 0.9 µg/ml (α-glucosidase) and 0.070 ± 0.02 mg/ml (α-amylase) with a comparatively higher phenolic (232.6 ± 1 mg GAE/g) and flavonoid (138.18 ± 0.9 mg QE/g) content. The chloroform extract of SSV 84 showed a higher cytotoxic effect at an IC50 of 165.502 ± 7 µg/ml (HeLa cells) and 237.895 ± 15 µg/ml (Hep G2 cells). HRLCMS profile of SSV 84 showed the presence of long-chain fatty acids in hexane extract. Anthraquinones, carotenoids, xanthophylls, cinnamic acid and derivatives, and isoflavones were present in chloroform extract, while Ethyl acetate extract was rich in phenolic acids and also consisted of coumarins, quinones, alkaloids, and terpenoids.
Conclusion:
The high cytotoxic and antihyperglycemic activities of extracts can be attributed to the presence of these phytochemicals.
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