benzofurans and marsupsin

The aim of this research was to formulate Marsupsin-phospholipid complex (M-P Complex) in attempt to increase the bioavailability of marsupsin and to characterize this new formulation along with its evaluation. Marsupsin-phospholipid complex was formulated by mechanical dispersion method. In this new formulation, complex formation was confirmed by carrying out transmission electron microscopy (TEM), IR, (1)H-NMR and RP-HPLC analysis. TEM showed M-P Complex diameter range of 0.05-0.5 microm. The entrapment efficiency of M-P Complex was found to be 44%. In vitro release study revealed its first order release profile. Mean blood serum concentration vs time curve of marsupsin was of first order after oral administration of M-P Complex in albino rabbits which clearly showed remarkably increased bioavailability of M-P Complex than standardized marsupsin. The average value of C(max) and T(max) of M-P Complex were found to be 3.02 mg/ml and 10.2 h, respectively. Hence the findings demonstrate that complexing marsupsin with phospholipids results in better oral bioavailability and improved biological response than free form of standardized marsupsin.

Topics: Animals; Benzofurans; Cresols; Diabetes Mellitus; Diffusion; Drug Carriers; Drug Compounding; Drug Evaluation, Preclinical; Hypoglycemic Agents; Materials Testing; Phospholipids; Rabbits; Rats; Treatment Outcome

Glucose levels in rats with hyperglycemia induced by streptozotocin were determined after i.p. administration of marsupsin (1), pterosupin (2), and pterostilbene (3), three important phenolic constituents of the heartwood of Pterocarpus marsupium. Marsupsin and pterostilbene significantly lowered the blood glucose level of hyperglycemic rats, and the effect was comparable to that of 1,1-dimethylbiguanide (metformin).

Topics: Animals; Benzofurans; Blood Glucose; Body Weight; Cresols; Diabetes Mellitus, Experimental; Female; Glucosides; Hypoglycemic Agents; Male; Metformin; Phenols; Plants, Medicinal; Rats; Stilbenes; Wood

Serum lipid levels in rats with hyperlipidemia induced by diet as well as by Triton were determined after oral administration of EtOAc extract of Pterocarpus marsupium heartwood and its flavonoid constituents, marsupsin [1], pterosupin [2], and liquiritigenin [3]. Administration of EtOAc extract for 14 consecutive days produced a significant reduction of serum triglyceride, total cholesterol, and LDL- and VLDL-cholesterol levels without any significant effect on the level of HDL-cholesterol. Liquiritigenin and pterosupin were able to effect a significant fall in serum cholesterol, LDL-cholesterol, and atherogenic index, pterosupin being additionally effective in lowering serum triglyceride.

Topics: Animals; Anticholesteremic Agents; Benzofurans; Cholesterol; Cresols; Diet; Flavanones; Flavonoids; Glucosides; Hyperlipidemias; Hypolipidemic Agents; Lipids; Male; Phenols; Plant Extracts; Plants; Polyethylene Glycols; Rats; Triglycerides