Phloridzin Highly Accumulated in Malus rockii Rehder and Its Structure Revision and Hypolipidemic Activity

Phloridzin is a lead compound of the prestigious antidiabetic gliflozins. The present study found that phloridzin highly accumulated in Malus rockii Rehder. The content of phloridzin in M. rockii was the highest among wild plants, with the percentage of 15.54% in the dry leaves. The structure of phloridzin was revised by proton exchange experiments and extensive 2D NMR spectra. Phloridzin exhibited significant hypolipidemic activity in golden Syrian hamsters maybe by increasing the expression of CYP7A1, at the doses of 50 mg/kg and 200 mg/kg. The total performance of anti-hyperlipidemic effect of phloridzin may be superior to that of lovastatin, though lovastatin was more active than phloridzin. In addition, phloridzin exhibited moderate antimalarial activity with inhibition ratio of 31.3±10.9% at a dose of 25 mg/kg/day, and showed moderate analgesic activity with 28.0% inhibition at a dose of 50 mg/kg.

Impact of Shodhana on Semecarpus anacardium Nuts

Semecarpus anacardium is classified in Ayurveda under the category of toxic plants. However, this toxic plant is reported to possess anti-inflammatory activity, anti-arthritic effect, antioxidant activity, antimicrobial activity, anti- carcinogenic activity, hypoglycemic activity, cardioprotective, hepatoprotective, neuroprotective, and hypolipidemic activity etc. All these activities are attributed to its various constituents like phenolic compounds, flavonoids, carbohydrates, alkaloids, steroids, etc. In Ayurveda, a series of pharmaceutical procedures which converts a poisonous drug into a safe and therapeutically effective medicine is termed as Shodhana. Shodhana improves the yield, decreases the phenolic and flavonoid content; and converts toxic urushiol into nontoxic anacardol derivative thereby reducing toxicity of nuts of Semecarpus anacardium. There are reports of alteration in pharmacology and phytochemistry of nuts of Semecarpus anacardium due to Shodhana.

Prospects of creating a new medicine based on biologically active substances of bearberry leaves for correction of the metabolic syndrome

Topicality. The metabolic syndrome is pathogenetically interrelated metabolic disorders in the condition of a sick person. A large set of factors is involved in its occurrence. Risk factors include genetic predisposition, overeating, insulin resistance, obesity, bad habits, hypodynamics, stress and unfavorable environmental conditions. First of all, defects of the lipid and carbohydrate metabolism provoke a cascade of genetic, metabolic, hormonal, nervous, inflammatory and other reactions and disorders in cells, tissues and organs, causing the metabolic syndrome and associated diseases, such as diabetes, kidney and gallstone disease, hypertension, platelet hyperaggregation, etc. Therefore, the rational use of synthetic and herbal medicines in the complex correction of these disorders can slow down the development of the metabolic syndrome. Aim. To develop the method for obtaining a dry modified extract from bearberry, study its chemical composition, hypoglycemic and hypolipidemic activity in order to determine the prospects of its use for the correction of the metabolic syndrome. Materials and methods. The study object was a dry extract of bearberry leaves modified with cysteine. HPLC and spectrophotometry were used to analyze the extract obtained. The hypoglycemic and hypolipidemic activity of dry extracts of bearberry was studied in rats with insulin resistance. Results and discussion. The method for obtaining a dry modified extract from bearberry leaves was developed by adding cysteine. Phenologlycoside (arbutin), 2 phenolic acids (gallic and ellagic), 6 flavonoids, 8 saponins were identified in the extract, and their quantitative content was determined. Hyperoside and catechin were dominant among flavonoids, and ursolic acid, uvaol, and lupeol prevailed among saponins. The content of the main groups of phenolic compounds was determined in the extract by spectrophotometry. The introduction of the dry extract from bearberry leaves modified with cysteine has a normalizing effect on metabolic disorders on the background of a high-fructose diet; therefore, it can be a promising agent for the correction of the metabolic syndrome. Conclusions. As a result of the research conducted, a new dry extract from bearberry leaves modified with cysteine has been created. The phytochemical composition, hypoglycemic and hypolipidemic activities of the extract have been studied, indicating the prospects for its use to correct the metabolic syndrome.