Application of TLC to Evaluate the Lipophilicity of Newly Synthesized Betulin Derivatives.

Designing a new drug has recently become a very important topic that many researches are concerned with. This work relates to a newly synthesized betulin and betulone derivatives which have anticancer activity. Thin-layer chromatography was applied to evaluate the lipophilicity of these triterpenes in order to find the correlation between theoretically and experimentally calculated values of lipophilicity and the structure of compounds investigated. Moreover, the relationships between lipophilicity and pharmacokinetic parameters or anticancer activity were carried out. The similarity analysis was also done for the purpose to divide the compounds investigated into groups pointing which of these can meet the criteria for medicine substances. The cluster analysis showed the differences in the compounds grouping in relation which the values of lipophilicity are considered, i.e., calculated by computer software or obtained experimentally by use of TLC. Analysis clearly shows that those theoretically calculated values of lipophilicity are strongly connected to the structure of the compounds.

Phloridzin, an Apple Polyphenol, Exerted Unfavorable Effects on Bone and Muscle in an Experimental Model of Type 2 Diabetes in Rats.

It is believed that apple fruits contain components with health-promoting effects, including some antidiabetic activity. One of the most known apple compounds is phloridzin, a glucoside of phloretin. Phloridzin and phloretin were reported to exert some favorable skeletal effects in estrogen-deficient rats and mice. The aim of the study was to investigate the effects of phloridzin on musculoskeletal system in rats with type 2 diabetes induced by a high-fat diet (HFD) and streptozotocin (STZ). The experiments were performed on mature female Wistar rats, divided into control rats (fed a standard laboratory diet), HFD/STZ control rats, and HFD/STZ rats receiving phloridzin (20 or 50 mg/kg/day per os) for four weeks. Serum biochemical parameters, muscle mass and strength, bone mass, density, histomorphometric parameters and mechanical properties were determined. The HFD/STZ rats developed hyperglycemia, with decreases in the muscle mass and strength and profound osteoporotic changes. Phloridzin at 20 mg/kg markedly augmented the unfavorable effects of diabetes on the muscle mass and strength and decreased growth of bones, whereas, at 50 mg/kg, it did not affect most of the investigated musculoskeletal parameters. Results of the study indicate the possibility of unfavorable effects of phloridzin on the musculoskeletal system in conditions of hyperglycemia.