title: Urease inhibitory constituents from Daphne retusa.
abstract: The bioassay-guided fractionation of Daphne retusa Hemsl. has led to the isolation of a new aryl tetrahydronaphthalene lignan derivative named as daphnretusic acid (1), along with six new source compounds such as 5,7-dihydroxyflavone (2), 7-hydroxyflavone (3), 6-methoxyflavone (4), (+) pinoresinol (5), (+) sesamin (6), and β-sitosterol-3-O-β-D-glucopyranoside (7). Their structures were elucidated by (1)H NMR, (13)C NMR, 1D, 2D NMR, UV, IR, and EIMS analyses. All the fractions (n-hexane, CHCl3, AcOEt, CH3OH, and water) and pure compounds (1-7) were subjected to the assay of urease and α-chymotrypsin inhibitory activities. Chloroform and methanol soluble fractions showed moderate urease inhibition. Compound 2 exhibited significant urease inhibition with IC50 value 60.4 ± 0.72 μM, whereas compounds 1 and 3-7 remained inactive during urease inhibition and α-chymotrypsin bioassays.
authors.affiliation: a Department of Chemistry , University of Karachi , Karachi , 75270 , Pakistan.
authors.forename: Farrukh
authors.initials: F
authors.lastname: Mansoor
authors.forename: Itrat
authors.initials: I
authors.lastname: Anis
authors.forename: Ajmal
authors.initials: A
authors.lastname: Khan
authors.forename: Bishnu P
authors.initials: BP
authors.lastname: Marasini
authors.forename: Muhammad Iqbal
authors.initials: MI
authors.lastname: Choudhary
authors.forename: Muhammad Raza
authors.initials: MR
authors.lastname: Shah
mesh_terms: D002918:Chymotrypsin / Q000037:antagonists & inhibitors*; D032364:Daphne / Q000737:chemistry*; D005419:Flavonoids / Q000737:chemistry; D005960:Glucosides / Q000737:chemistry / Q000302:isolation & purification; D017705:Lignans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D010154:Pakistan; D012855:Sitosterols / Q000737:chemistry / Q000302:isolation & purification; D013764:Tetrahydronaphthalenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D014510:Urease / Q000037:antagonists & inhibitors*
chemical_list: D005419:Flavonoids; D005960:Glucosides; D017705:Lignans; D012855:Sitosterols; D013764:Tetrahydronaphthalenes; C587155:daphnretusic acid; C472604:sitosterol-3-O-glucopyranoside; D002918:Chymotrypsin; C117608:alpha-chymotrypsin; D014510:Urease; C429845:7-hydroxyflavone