Inhibition of protein tyrosine phosphatase-1B (PTP1B) has been proposed as a therapy for treatment of type-2 diabetes and obesity. Bioassay-guided fractionation of an EtOAc-soluble extract of the root bark of Erythrina mildbraedii, using an in vitro PTP1B inhibitory assay, resulted in the isolation of three new isoprenylated flavonoids, abyssinone-IV-4'-O-methyl ether (2), 7-hydroxy-4'-methoxy-3'-(3-hydroxy-3-methyl-trans-but-1-enyl)-5'-(3-methylbut-2-enyl)flavanone (3), and abyssinone-VI-4-O-methyl ether (6), along with six known flavonoids, abyssinone-V-4'-O-methyl ether (1), abyssinone-V (4), abyssinone-IV (5), sigmoidin E (7), 4'-hydroxy-5,7-dimethoxyisoflavone (8), and alpinumisoflavone (9). Compounds 1 and 2, 4-7, and 9 inhibited PTP1B activity, with IC50 values ranging from 14.8 +/- 1.1 to 39.7 +/- 2.5 microM. On the basis of the data obtained, flavanones and chalcones with isoprenyl groups may be considered as a new class of PTP1B inhibitors.
The extracts of some propolis samples were analysed by GC-MS and then purified by column chromatography. The latter led to the isolation of a new mono-ether of glycerol, 1'-O-eicosanyl glycerol and a new triterpene, methyl-3β,27-dihydroxycycloart-24-en-26-oate together with known triterpenoids namely betulin, 3β-hydroxylanostan-9,24-dien-21-oic acid, mangiferonic acid, a mixture of ambolic acid and β-sitosterol, 3β-hydroxycycloartan-12,24(25)-diene and 27-hydroxymangiferonic acid. The DPPH radical scavenging potential of some extracts and compounds were measured. The radical scavenging activity varied from Hexane extract of Foumban propolis (IC = 5.6 mg/mL) to Methanol extract of Foumban propolis (IC = 1.07 mg/mL) for the extracts and from 3β-hydroxylanostan-9,24-dien-21-oic acid (IC = 1.22 mg/mL) to 1'-O-eicosanyl glycerol (IC = 0.93 mg/mL) for the compounds. Activities of samples were moderate as they remained closer to those of the standard antioxidants Gallic acid (IC = 0.30 mg/mL) and vitamin C (IC = 0.80 mg/mL), especially 1'-O-eicosanyl glycerol, the most active compound.
Phytochemical study on an EtOAc-soluble extract of the root bark of Erythrina mildbraedii resulted in the isolation of six prenylated flavonoids 1-6. Based on physicochemical and spectroscopic analyses, their structures were determined to be new natural products licoflavanone-4-O-methyl ether (1), 2,7-dihydroxy-4-methoxy-5-(3-methylbut-2-enyl)isoflavone (2), and (3R)-2,7-dihydroxy-3-(3-methylbut-2-enyl)
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.