Diabetes is known as a multifactorial disease. The treatment of diabetes (Type II) is complicated due to the inherent patho-physiological factors related to this disease. One of the complications of diabetes is post-prandial hyperglycemia (PPHG). Glucosidase inhibitors, particularly α-amylase inhibitors are a class of compounds that helps in managing PPHG. Six ethno-botanically known plants having antidiabetic property namely, Azadirachta indica Adr. Juss.; Murraya koenigii (L.) Sprengel; Ocimum tenuflorum (L.) (syn: Sanctum); Syzygium cumini (L.) Skeels (syn: Eugenia jambolana); Linum usitatissimum (L.) and Bougainvillea spectabilis were tested for their ability to inhibit glucosidase activity. The chloroform, methanol and aqueous extracts were prepared sequentially from either leaves or seeds of these plants. It was observed that the chloroform extract of O. tenuflorum; B. spectabilis; M. koenigii and S. cumini have significant α-amylase inhibitory property. Plants extracts were further tested against murine pancreatic, liver and small intestinal crude enzyme preparations for glucosidase inhibitory activity. The three extracts of O. tenuflorum and chloroform extract of M. koenigi showed good inhibition of murine pancreatic and intestinal glucosidases as compared with acarbose, a known glucosidase inhibitor.
The mixed-ligand complexes [Cu(L)(maltol)] where L = 2,2'-bipyridine (bpy; 1), 1,10-phenanthroline (phen; 2), 1,10-phenanthroline-5,6-dione (phendione; 3), dipyrido[3,2-a:2',3'-c]phenazine (dppz; 4), and 4b,5,7,7a-tetrahydro-4b,7a-epiminomethanoimino-6H-imidazo[4,5-f][1,10]-phenanthroline-6,13-dione (bipyridylglycoluril; bpg; 5) have been synthesized and characterized by structural, analytical, and spectral methods. The single-crystal X-ray structures of 1, 2, and 5 exhibit a distorted square-pyramidal structure, with the polypyridyl ligands and maltol occupying equatorial positions and either a water or nitrate anion at the axial position. The N,N-dimethylformamide glass as well as the single-crystal electron paramagnetic resonance of the complexes confirms the distorted square-pyramidal structure. The DNA binding investigated using different techniques (absorption titration, viscosity, thermal melting, and fluorescence quenching) indicates the partial intercalation of the planar polypyridyl ligands into DNA. The complexes cleave plasmid pBR322 DNA by a hydrolytic mechanism. The kinetic aspects of DNA cleavage under pseudo-Michaelis-Menten and true Michaelis-Menten conditions as well as the phosphodiesterase activity using model 4-nitrophenylphosphate are also detailed. The cytotoxicity of the complexes against HeLa (cervical) cancer cell lines shows that synergy between the metal and ligands results in a significant enhancement in the cell death with IC(50) of approximately 150-270 microg mL(-1).
Diabetes mellitus is a metabolic syndrome characterized by an increase in the blood glucose level. Treatment of diabetes is complicated due to multifactorial nature of the disease. Azadirachta indica Adr. Juss and Bougainvillea spectabilis are reported to have medicinal values including antidiabetic properties. In the present study using invivo diabetic murine model, A. indica and B. spectabilis chloroform, methanolic and aqueous extracts were investigated for the biochemical parameters important for controlling diabetes. It was found that A. indica chloroform extract and B. spectabilis aqueous, methanolic extracts showed a good oral glucose tolerance and significantly reduced the intestinal glucosidase activity. Interestingly, A. indica chloroform and B. spectabilis aqueous extracts showed significant increase in glucose-6-phosphate dehydrogenase activity and hepatic, skeletal muscle glycogen content after 21 days of treatment. In immunohistochemical analysis, we observed a regeneration of insulin-producing cells and corresponding increase in the plasma insulin and c-peptide levels with the treatment of A. indica chloroform and B. spectabilis aqueous, methanolic extracts. Analyzing the results, it is clear that A. indica chloroform and B. spectabilis aqueous extracts are good candidates for developing new neutraceuticals treatment for diabetes.
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