Laportea ovalifolia (Scham and Thonn) is widly use in Cameroon for the treatment of diabetes mellitus. The present study was designed to evaluate the antidiabetic and hypolipidaemic effects of aqueous extract of Laportea ovalifolia aerial part in normal and alloxan diabetic rats. Diabetes was induced by intraperitoneal injection of alloxan (150 mg kg -1 body weight). The treatment was given for 2 weeks. After the treatment a significant reduction was observed in fasting serum glucose levels in the treated diabetics rats. L. ovalifolia treatment showed considerable lowering of serum total cholesterol, triglycerides, LDL cholesterol, T.C/HDL.C and an increase in HDL cholesterol in the treated diabetic group. These results suggest that the Laportea ovalifolia aqueous extract of the aerial part possesses antidiabetic and hypolipideamic effects in alloxan-induced diabetic rats.
Where the action is: Changing the vinyl groups of hematin anhydride to either ethyl or hydrogen groups results in increased solubility (see picture; Por=porphyrin). Determination of the weak binding constants of the antimalarial drug chloroquine to dimers of these hematin anhydride analogues suggests that solution‐phase heme/drug interactions alone are unlikely to be the origin of the action of the drug.
Solution NMR has been used in tandem with a diamagnetic non-iron heme model compound as a simple and effective tool to rapidly probe the structures of the bound complexes formed between the metalloporphyrin and antimalarial drugs from the 4-aminoquinoline, 4-methylenehydroxylquinoline, and 8-aminoquinoline subfamilies. The ability of gallium(III) protoporphyrin IX to mimic heme chemistry is exploited. The 4-aminoquinolines quinacrine and amodiaquine and two novel 3-halo chloroquine analogues are found to bind to the metalloporphyrin through hydrogen-bonding and stacking interactions, while halofantrine and the 4-methylenehydroxylquinolines, quinine and mefloquine bind through the alcohol group of the drug. In each case, detailed structural information is available from the NMR assessment. The mefloquine model is confirmed crystallographically. The 8-aminoquinoline primaquine does not interact strongly. These tools show promise for future applications in assessing antimalarials in preclinical development for heme-binding drug targets.
2‐Aryl‐4‐methyl‐5‐acetylthiazoles, which were prepared from arylthioamides and chloroacetylacetone, were treated with 6‐substituted‐3‐formylchromones or arylaldehydes to give a series of eighteen new thiazolylchalcones in good yields. The structures of all the synthesized compounds were characterized by 1H NMR, 13C NMR, and ES‐MS spectrometry. Additionally, the crystal structures of two of these chalcones were determined by X‐ray diffraction analysis.
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