Lab Scale Extracted Conditions of Polyphenols from Thinned Peach Fruit Have Antioxidant, Hypoglycemic, and Hypolipidemic Properties

Thinned peach polyphenols (TPPs) were extracted by ultrasonic disruption and purified using macroporous resin. Optimized extraction conditions resulted in a TPPs yield of 1.59 ± 0.02 mg GAE/g FW, and optimized purification conditions resulted in a purity of 43.86% with NKA-9 resin. TPPs composition was analyzed by UPLC-ESI-QTOF-MS/MS; chlorogenic acid, catechin, and neochlorogenic acid were the most abundant compounds in thinned peaches. Purified TPPs exhibited scavenging activity on DPPH, ABTS, hydroxyl radical, and FRAP. TPPs inhibited α-amylase and α-glucosidase by competitive and noncompetitive reversible inhibition, respectively. TPPs also exhibited a higher binding capacity for bile acids than cholestyramine. In summary, TPPs from thinned peaches are potentially valuable because of their high antioxidant, hypoglycemic, and hypolipidemic capacities, and present a new incentive for the comprehensive utilization of thinned peach fruit.

10 reasons, why to use naproxen – in the light of new scientific reports

Naproxen is a non-steroidal anti-inflammatory drug with a wide range of use, used in patients with various pain syndromes in the musculoskeletal system. It has anti-inflammatory, analgesic and antipyretic properties through non-selective and reversible inhibition of COX-1 and COX-2 isoforms. In Poland, it is registered in the treatment of rheumatic diseases and acute inflammations of the musculoskeletal system. Some naproxen preparations are also approved for the treatment of migraine and fever. The paper presents the characteristic features of the substance.

Computationally Assisted Lead Optimization of Novel Potent and Selective MAO-B Inhibitors

A series of dietary flavonoid acacetin 7-O-methyl ether derivatives were computationally designed aiming to improve the selectivity and potency profiles against monoamine oxidase (MAO) B. The designed compounds were evaluated for their potential to inhibit human MAO-A and -B. Compounds 1c, 2c, 3c, and 4c were the most potent with a Ki of 37 to 68 nM against MAO-B. Compounds 1c–4c displayed more than a thousand-fold selectivity index towards MAO-B compared with MAO-A. Moreover, compounds 1c and 2c showed reversible inhibition of MAO-B. These results provide a basis for further studies on the potential application of these modified flavonoids for the treatment of Parkinson’s Disease and other neurological disorders.

Reversible inhibition of sperm under guidance as an intratubular and reversible contraception in female rats: An experimental study

Background: Reversible inhibition of sperm under guidance (“RISUG®”) is a promising intravasal male contraceptive. Objective: An exploratory study was conducted with a concept of non-invasive, transcervical, single-intervention and reversible contraception using RISUG® in females. Materials and Methods: In this experimental study, 60 adult Wistar albino female rats weighing 150-155 g, 3-4 months old were divided into four groups: group I: sham-operated control; group II: tubal occlusion with RISUG for 90 days; group III: tubal occlusion with RISUG® for 90 days and reversal with dimethyl sulphoxide and group IV: tubal occlusion with RISUG® for 90 days and reversal with 5% NaHCO3. Animals were subjected to bilateral fallopian tube occlusion with RISUG® and reversal with DMSO and NaHCO3. The estrous cycle, fertility and histology of fallopian tube were evaluated. Results: Group I showed 100% fertility during all mating schedules. Animals of experimental groups indicated positive mating, but 0% fertility was evident following 30, 60, and 90 days of tubal occlusion. However, after reversal, fertility steadily increased to normalcy in groups III (50% at 45 days, 80% at 105 days, 100% at 150 and 195 days) and IV (70% at 45 and 105 days, 100% at 150 and 195 days) animals. Group II illustrated disorganized inner cell linings and eosinated RISUG® implant-filled lumen. Reversal groups (III and IV) revealed complete restoration of cellular histo-architecture. Regular estrous cycle was noticed in all experimental groups. Conclusion: RISUG® is suitable for single intervention, intratubular, reversible contraception in female rats. Key words: Contraception, Fallopian tube, Tubal occlusion, RISUG®, Reversible.