Solvent free synthesis of active 5-benzylidine-1, 3-thiazolidine-2,4-dione derivatives

Present communication describes the attempts made to improve the yields of thiazolidinedione group of derivatives keeping in view of their anti-cancer activity. 5-benzylidine-1,3-thiazolidine-2,4-dione derivatives were the active substrates belonging to α-glucosidase inhibitor classification. These were prepared by the reaction of 4-((Z)-(2,4-dioxothiazolidin-5-ylidene) methyl) benzaldehyde with aromatic/hetero aromatic ketones in the presence of potassium hydroxide and ethanol as solvent. Synthesis of 5-benzylidine-1, 3-thiazolidine-2,4-dione derivatives has been optimized under solvent free condition by screening with different bases in order to achieve the required target (of improving the yields). The solvent free condition has resulted in excellent improvement in yields and reduced the manufacturing cost significantly.

Critical Assessment of In Vitro Screening of α-Glucosidase Inhibitors from Plants with Acarbose as a Reference Standard

Postprandial hyperglycemia is treated with the oral antidiabetic drug acarbose, an intestinal α-glucosidase inhibitor. Side effects of acarbose motivated a growing number of screening studies to identify novel α-glucosidase inhibitors derived from plant extracts and other natural sources. As “gold standard”, acarbose is frequently included as the reference standard to assess the potency of these candidate α-glucosidase inhibitors, with many outperforming acarbose by several orders of magnitude. The results are subsequently used to identify suitable compounds/products with strong potential for in vivo efficacy. However, most α-glucosidase inhibitor screening studies use enzyme preparations obtained from nonmammalian sources (typically Saccharomyces cerevisiae), despite strong evidence that inhibition data obtained using nonmammalian α-glucosidase may hold limited value in terms of identifying α-glucosidase inhibitors with actual in vivo hypoglycemic potential. The aim was to critically discuss the screening of novel α-glucosidase inhibitors from plant sources, emphasizing inconsistencies and pitfalls, specifically where acarbose was included as the reference standard. An assessment of the available literature emphasized the cruciality of stating the biological source of α-glucosidase in such screening studies to allow for unambiguous and rational interpretation of the data. The review also highlights the lack of a universally adopted screening assay for novel α-glucosidase inhibitors and the commercial availability of a standardized preparation of mammalian α-glucosidase.

COMPARISON OF α –GLUCOSIDASE INHIBITORY ACTIVITY OF Moringa oleifera ETHANOLIC EXTRACT

The purpose of this research was to determine the α-glucosidase enzyme inhibitory activity of Moringa oleifera plant samples collected from the three geographical areas viz., Saragi, Bacuhau, and Batumatongka of Southeast Sulawesi Indonesia. Ethanol extract of Moringa leaves was prepared by the maceration method using 95% ethanol. The estimation of α –glucosidase inhibitory activity of this extract was performed in vitro. The results of the study showed that ethanolic extract of three Moringa samples i.e. Sarangi, Bacuhau, and Batumatongka had the IC50value of 18.62, 10.18, 10.58 ppm, respectively while IC50value for the acarbose positive control was reported 11.54ppm. From the results of this study, it can be concluded that ethanolic extract of Moringa could inhibit α –glucosidase and this potential was similar to the commercial α –glucosidase inhibitor acarbose.