title: The Chemical Composition of Achillea wilhelmsii C. Koch and Its Desirable Effects on Hyperglycemia, Inflammatory Mediators and Hypercholesterolemia as Risk Factors for Cardiometabolic Disease.
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, 1β,10β-epoxydesacetoxymatricarin (CP1) and leucodin (CP2) showed the highest anti-hypercholesterolemic potential. A molecular docking study provided corresponding results.
authors.affiliation: Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. eliankhazneh@gmail.com.
authors.forename: Elian
authors.initials: E
authors.lastname: Khazneh
authors.affiliation: Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. cerfpatolog@gmail.com.
authors.forename: Petra
authors.initials: P
authors.lastname: Hřibová
authors.affiliation: Department of Molecular Biology and Pharmaceutical Biotechnology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. hhosek@gmail.com.
authors.forename: Jan
authors.initials: J
authors.lastname: Hošek
authors.affiliation: Department of Human Pharmacology and Toxicology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. suchypa@vfu.cz.
authors.forename: Pavel
authors.initials: P
authors.lastname: Suchý
authors.affiliation: Department of Human Pharmacology and Toxicology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. kollarp@vfu.cz.
authors.forename: Peter
authors.initials: P
authors.lastname: Kollár
authors.affiliation: Department of Human Pharmacology and Toxicology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. prazanovag@vfu.cz.
authors.forename: Gabriela
authors.initials: G
authors.lastname: Pražanová
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého 1-3, Brno 61242, Czech Republic. muselikj@vfu.cz.
authors.forename: Jan
authors.initials: J
authors.lastname: Muselík
authors.affiliation: Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. hanakovaz@vfu.cz.
authors.forename: Zuzana
authors.initials: Z
authors.lastname: Hanaková
authors.affiliation: Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. vaclavikj@vfu.cz.
authors.forename: Jiří
authors.initials: J
authors.lastname: Václavík
authors.affiliation: Department of Biotechnology and Bioinformatics, Faculty of Chemistry, Rzeszów University of Technology, Powstańców Warszawy 6, Rzeszów 35-959, Poland. mkkmilek@gmail.com.
authors.forename: Michał
authors.initials: M
authors.lastname: Miłek
authors.affiliation: Department of Biotechnology and Bioinformatics, Faculty of Chemistry, Rzeszów University of Technology, Powstańców Warszawy 6, Rzeszów 35-959, Poland. Jaroslav.Legath@uvlf.sk.|Department of Pharmacology and Toxicology, The University of Veterinary Medicine and Pharmacy in Košice, Komenského 73, Košice 04181, Slovakia. Jaroslav.Legath@uvlf.sk.
authors.forename: Jaroslav
authors.initials: J
authors.lastname: Legáth
authors.affiliation: Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. karel.mejkal@post.cz.|Department of Molecular Biology and Pharmaceutical Biotechnology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic. karel.mejkal@post.cz.
authors.forename: Karel
authors.initials: K
authors.lastname: Šmejkal
mesh_terms: D031162:Achillea / Q000737:chemistry; D000214:Acyl Coenzyme A / Q000737:chemistry; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000737:chemistry; D002460:Cell Line; D002851:Chromatography, High Pressure Liquid; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D005419:Flavonoids / Q000008:administration & dosage / Q000737:chemistry / Q000302:isolation & purification; D006801:Humans; D006937:Hypercholesterolemia / Q000188:drug therapy; D006943:Hyperglycemia / Q000188:drug therapy; D007249:Inflammation / Q000188:drug therapy*; D018836:Inflammation Mediators / Q000737:chemistry; D051379:Mice; D016688:Mice, Inbred NOD; D062105:Molecular Docking Simulation; D010636:Phenols / Q000008:administration & dosage / Q000737:chemistry / Q000302:isolation & purification; D010936:Plant Extracts / Q000008:administration & dosage* / Q000737:chemistry; D012307:Risk Factors
chemical_list: D000214:Acyl Coenzyme A; D000975:Antioxidants; D005419:Flavonoids; D018836:Inflammation Mediators; D010636:Phenols; D010936:Plant Extracts; C008047:3-hydroxy-3-methylglutaryl-coenzyme A
keywords: 3-hydroxy-3-methylglutaryl-CoA reductase; Achillea wilhelmsii; anti-hypercholesterolemic; cardiometabolic disease; docking; flavonoids; hypoglycemic; inflammation