Eight known phytochemicals, four sesquiterpenes and four flavonoids of Zingiber zerumbet were screened against α-glucosidase enzyme, aldose reductase enzyme and antiglycation property under in vitro conditions. The results established kaempferol-3-O-methylether as a potent inhibitor of α-glucosidase enzyme with an IC50 value of 7.88 μM. In aldose reductase enzyme inhibition assay, all the compounds except zerumbone epoxide showed good to excellent inhibition properties. Among these, the flavonoid compounds were found to be potent aldose reductase inhibitors compared with the four sesquiterpenes. In addition, compounds such as α-humulene, kaempferol, kaempferol-3-O-methylether and 3″,4″-O-diacetylafzelin displayed potent antiglycation properties. From overall results, we found that kaempferol and kaempferol-3-O-methylether are potent inhibitors of α-glucosidase enzyme, aldose reductase enzyme and glycation reaction, the three main targets of drugs for the treatment of diabetes and its complications.
A strategy for the synthesis of novel zerumbone derivatives via a regioselective palladium catalyzed decarboxylative coupling reaction using arene carboxylic acids is described. This methodology involves double bond repositioning from endocyclic to exocyclic. The preliminary in vitro analysis reveals that most of the newly synthesized derivatives are potent -glucosidase enzyme inhibitors. -(AJISH, K. R.; DHANYA, B. P.; JOSEPH, N.; RANI, M. P.; RAGHU, K. G.; VINEETHA, V. P.; RADHAKRISHNAN*, K. V.; Tetrahedron Lett. 55 (2014) 3, 665-670, http://dx.
A straightforward method for the synthesis of novel derivatives of zerumbone via palladium-and rhodium-catalyzed regio-and diastereoselective 1,4-conjugate addition using boronic acids is developed. The reaction is general for aryl boronic acids containing both electron-donating and electron-withdrawing groups.
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