ABSTRACT
This study was done to identify the content compounds of Achillea wilhelmsii (A. wilhelmsii) and to evaluate its hypoglycemic and anti-hypercholesterolemic activity and effect on inflammatory mediators. The extracts and fractions of A. wilhelmsii were thoroughly analyzed using high performance liquid chromatography (HPLC), and the total content of phenols and flavonoids was determined. The hypoglycemic activity was evaluated in vivo using alloxan-induced diabetic mice. The effect upon inflammatory mediators was evaluated in vitro using the human monocytic leukemia cell line (THP-1). The anti-hypercholesterolemic activity was evaluated in vitro using the 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase assay kit. The water extract (WE)-treated group showed the highest reduction in the fasting blood glucose levels (FBGL). The chloroform fraction (CF) and ethyl acetate fraction (EAF) both showed a significant ability to reduce the secretion of tumor necrosis factor alpha (TNF-α). The EAF, however, also attenuated the levels of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9). The CF showed the most significant 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibition activity. The five main compounds in the CF were isolated and identified. Out of the five compounds in the CF, 1ß,10ß-epoxydesacetoxymatricarin (CP1) and leucodin (CP2) showed the highest anti-hypercholesterolemic potential. A molecular docking study provided corresponding results.
Subject(s)
Antioxidants/administration & dosage , Diabetes Mellitus, Experimental/drug therapy , Inflammation/drug therapy , Plant Extracts/administration & dosage , Achillea/chemistry , Acyl Coenzyme A/chemistry , Animals , Antioxidants/chemistry , Cell Line , Chromatography, High Pressure Liquid , Flavonoids/administration & dosage , Flavonoids/chemistry , Flavonoids/isolation & purification , Humans , Hypercholesterolemia/drug therapy , Hyperglycemia/drug therapy , Inflammation Mediators/chemistry , Mice , Mice, Inbred NOD , Molecular Docking Simulation , Phenols/administration & dosage , Phenols/chemistry , Phenols/isolation & purification , Plant Extracts/chemistry , Risk FactorsABSTRACT
The antiurease activity of the aqueous extracts of 42 plants growing in the Czech Republic was investigated. A phenol-hypochlorite reaction was used for the determination of ammonia produced by urease. The inhibitory activity of the extracts at a concentration of 0.2 mg/mL varied from 17.8% to 80.0%. Extracts from six Potentilla species expressed inhibitory activity against jack bean urease. They were further investigated for their phenolic constituents and the major compounds were subjected to molecular docking. The results revealed that both jack bean urease and Helicobacter pylori urease were inhibited by quercetin-3-O-ß-D-galactopyranoside-6â³-gallate (1), myricetin-3-O-ß-D-glucuronide (2), tiliroside (3) and B-type procyanidin (4). The antiurease activity of the investigated Potentilla species is probably due to the presence of complex phenolic constituents such as flavonoid glycosides and catechin dimers.
Subject(s)
Flavonoids/isolation & purification , Flavonoids/pharmacology , Galactosides/isolation & purification , Galactosides/pharmacology , Helicobacter pylori/drug effects , Phenols/isolation & purification , Phenols/pharmacology , Plants, Medicinal/chemistry , Potentilla/chemistry , Urease/antagonists & inhibitors , Algorithms , Canavalia/enzymology , Czech Republic , Flavonoids/chemistry , Galactosides/chemistry , Helicobacter Infections/drug therapy , Phenols/chemistry , Quercetin/analogs & derivativesABSTRACT
UNLABELLED: In this review, an overview of the available literature on urease is presented. Urease is an enzyme which catalyzes the hydrolysis of urea. The occurrence of ureases and their functions are discussed thoroughly. The relationship of urease to ureolytic bacteria is examined, and the currently available urease inhibitors, both inorganic and natural, are presented. Finally, the importance of urease and current and future applications of new inhibitors and explored. KEYWORDS: bacteria inhibitor urease.
