Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymes

Mannich bases (2a–d) of aromatic amines were synthesized by using a conventional microwave technique under solvent-free conditions and characterized by IR and NMR (1H and 13C) and elemental analysis. The inhibitory effects of the synthesized Mannich bases were examined in vitro by using hydratase and esterase assays on carbonic anhydrase I and II isozymes (hCA, EC 4.2.1.1) purified from human erythrocyte cells. Acetazolamide was used as the control compound. The values of IC50, the half-maximum inhibitory concentration, were found for hydratase and esterase activities. Only two compounds (2b and 2d) exhibited poor hCA I and hCA II inhibition effects on esterase activity. In contrast, compounds 2a and 2c could be used as carbonic anhydrase activators as a result of the increased esterase activity of hCA I and hCA II isozymes.

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ChemInform Abstract: Molybdate Sulfuric Acid (MSA): An Efficient Reusable Catalyst for the Synthesis of Tetrahydrobenzo[4,5]imidazo[2,1-b]quinazolin-1(2H)-ones under Solvent-Free Conditions and Evaluation of Their in vitro Bioassay.

ChemInform ◽

10.1002/chin.201526229 ◽

2015 ◽

Vol 46 (26) ◽

pp. no-no

Author(s):

Mudumala Veeranarayana Reddy ◽

Gangireddy Chandra Sekhar Reddy ◽

Yeon Tae Jeong

Keyword(s):

Sulfuric Acid ◽

Solvent Free ◽

Reusable Catalyst ◽

In Vitro Bioassay ◽

Solvent Free Conditions

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In Vitro α-Glucosidase and α-Amylase Inhibitory Activities of Free and Bound Phenolic Extracts from the Bran and Kernel Fractions of Five Sorghum Grain Genotypes

Foods ◽

10.3390/foods9091301 ◽

2020 ◽

Vol 9 (9) ◽

pp. 1301

Author(s):

Yun Xiong ◽

Ken Ng ◽

Pangzhen Zhang ◽

Robyn Dorothy Warner ◽

Shuibao Shen ◽

...

Keyword(s):

Digestive System ◽

Inhibitory Concentration ◽

Inhibitory Effect ◽

Inhibitory Effects ◽

Phenolic Contents ◽

Inhibitory Activities ◽

Sorghum Grain ◽

Global Health Challenge ◽

Phenolic Extracts

Diabetes is a global health challenge. Currently, an effective treatment for diabetes is to reduce the postprandial hyperglycaemia by inhibiting the carbohydrate hydrolysing enzymes in the digestive system. In this study, we investigated the in vitro α-glucosidase and α-amylase inhibitory effects of free and bound phenolic extracts, from the bran and kernel fractions of five sorghum grain genotypes. The results showed that the inhibitory effect of sorghum phenolic extracts depended on the phenolic concentration and composition. Sorghum with higher phenolic contents generally had higher inhibitory activity. Among the tested extracts, the brown sorghum (IS131C)-bran-free extract (BR-bran-free, half-maximal inhibitory concentration (IC50) = 18 ± 11 mg sorghum/mL) showed the strongest inhibition against α-glucosidase which was comparable to that of acarbose (IC50 = 1.39 ± 0.23 mg acarbose/mL). The red sorghum (Mr-Buster)-kernel-bound extract (RM-kernel-bound, IC50 = 160 ± 12 mg sorghum/mL) was the most potent in inhibiting α-amylase but was much weaker compared to acarbose (IC50 = 0.50 ± 0.03 mg acarbose/mL).

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