Phase 2 enzyme inducer sulphoraphane blocks prostaglandin and nitric oxide synthesis in human articular chondrocytes and inhibits cartilage matrix degradation.

Objective: We explored the inhibitory effect of sulphoraphane (SFN), a potent inducer of Phase 2 enzymes, on cytokine-induced prostaglandin E(2) (PGE2) and nitric oxide (NO) production and cartilage degradation in articular chondrocytes. The regulatory mechanism of SFN on nuclear factor (NF)-κB was investigated.

Methods: Chondrocytes were obtained from patients with knee OA.

In vitro antioxidant and anti-inflammatory activities of Angelica decursiva.

Mounting evidences continue to support the involvement of oxidative/nitrosative stress and inflammation in the pathogenesis of many diseases. Plant constituents having antioxidant activities together with anti-inflammatory activities may provide better opportunities to develop anti-inflammatory agents. In view of this, we evaluated the antioxidant and antiinflammatory activities of methanolic extract of whole plants of Angelica decursiva, and its solvent soluble fractions via in vitro activities against lipopolysaccharide-induced nitric oxide (NO) production in RAW 264.

Anti-tumorigenic activity of sophoflavescenol against Lewis lung carcinoma in vitro and in vivo.

This study examined the in vitro cytotoxic activity and in vivo antitumor activity as well as intracellular apoptotic capacities of a prenylated flavonol, sophoflavescenol from Sophora flavescens, to evaluate prospective anti-tumorigenic drugs, and antitumor potential. In addition, the in vitro antioxidant and anti-inflammatory capacities were evaluated. Despite the small effect on human breast adenocarcinoma (MCF-7), sophoflavescenol showed cytotoxicity against human leukaemia (HL-60), Lewis lung carcinoma (LLC), and human lung adenocarcinoma epithelial (A549) cells.

Protective effects of luteolin against apoptotic liver damage induced by D-galactosamine/lipopolysaccharide in mice.

In this study, the protective effects of luteolin (1, a major component of Cirsium japonicum) were examined against d-galactosamine (GalN)/lipopolysaccharide (LPS)-induced fulminant hepatic failure. Mice received an intraperitoneal injection of 1 (25, 50, 100, and 200 mg·kg(-1)) 1 h before treatment with GalN (700 mg·kg(-1))/LPS (10 μg·kg(-1)). Treatment with GalN/LPS resulted in increased mortality and serum aminotransferase activity.

Lymphopenia is an important prognostic factor in peripheral T-cell lymphoma (NOS) treated with anthracycline-containing chemotherapy.

Background: Peripheral T-cell lymphoma, not otherwise specified (PTCL-NOS) is a heterogeneous group of aggressive T-cell lymphomas with poor treatment outcomes. The aim of this study was to evaluate whether lymphopenia at diagnosis would have an adverse effect on survival in patients with PTCL-NOS treated with anthracycline-containing chemotherapy.

Methods: A total of 118 patients with PTCL-NOS treated with anthracycline-containing chemotherapy from 4 Korean institutions were included.

Protein tyrosine phosphatase 1B and α-glucosidase inhibitory Phlorotannins from edible brown algae, Ecklonia stolonifera and Eisenia bicyclis.

The present work investigates protein tyrosine phosphatase 1B (PTP1B) and the α-glucosidase inhibitory activities of two edible brown algae, Ecklonia stolonifera and Eisenia bicyclis, as well as in their isolated phlorotannins. Since the individual extracts and fractions showed significant inhibitory activities, column chromatography was performed to isolate six phlorotannins, phloroglucinol (1), dioxinodehydroeckol (2), eckol (3), phlorofurofucoeckol-A (4), dieckol (5), and 7-phloroeckol (6). Phlorotannins 3-6 were potent and noncompetitive PTP1B inhibitors with IC(50) values ranging from 0.

Inhibitory effects of kaurenoic acid from Aralia continentalis on LPS-induced inflammatory response in RAW264.7 macrophages.

This study investigates the anti-inflammatory effects of a diterpenoid, kaurenoic acid, isolated from the root of Aralia continentalis (Araliaceae). To determine its anti-inflammatory effects, LPS-induced RAW264.7 macrophages were treated with different concentrations of kaurenoic acid and carrageenan-induced paw edema mice model was used in vivo.

Extraction and identification of three major aldose reductase inhibitors from Artemisia montana.

Aldose reductase inhibitors (ARIs) provide an important therapeutic and preventive opportunity against hyperglycemia associated diabetic complications. The methanolic extracts of 12 species from the genus Artemisia exhibited significant in vitro rat lens AR (RLAR) inhibitory activities with IC(50) values ranging from 0.51 to 13.

Antidiabetic complications and anti-Alzheimer activities of sophoflavescenol, a prenylated flavonol from Sophora flavescens, and its structure-activity relationship.

It was previously reported that prenylated flavonols from Sophora flavescens are inhibitors of rat lens aldose reductase (RLAR), human recombinant aldose reductase (HRAR), advanced glycation endproducts (AGE), β-secretase (BACE1) and cholinesterases (ChE). Based upon structure-activity relationships, 3,4'-dihydroxy flavonols with a prenyl or lavandulyl group substitution at the C-8 position, and a hydroxy group at the C-5, are important for such inhibition. In our ongoing study to isolate active principles from S.

The effects of daidzin and its aglycon, daidzein, on the scopolamine-induced memory impairment in male mice.

In this study, the effect of daidzin or daidzein isolated from Pueraria lobata on the memory impairments induced by scopolamine was assessed in male mice using the passive avoidance and the Morris water maze tasks. Administration of daidzin (5 mg/kg) or daidzein (5 mg/kg) significantly reversed the scopolamine (1 mg/kg)-induced cognitive impairments in male mice as evidenced by the passive avoidance test (p < 0.05) and on the Morris water maze test (p < 0.

Anticholinesterase and antioxidant constituents from Gloiopeltis furcata.

Activity-directed isolation of the ethyl acetate, methylene chloride and n-hexane fractions of Gloiopeltis furcata resulted in the isolation of 18 compounds. Their structures were elucidated as 2-(3-hydroxy-5-oxotetrahydrofuran-3-yl)acetic acid (1), glutaric acid (2), succinic acid (3), nicotinic acid (4), (E)-4-hydroxyhex-2-enoic acid (5), cholesterol (6), 7-hydroxycholesterol (7), uridine (8), glycerol (9), 5-(hydroxymethyl)-2-methoxybenzene-1,3-diol (10), (5E,7E)-9-oxodeca-5,7-dienoic acid (11), (Z)-3-ethylidene-4-methylpyrrolidine-2,5-dione (12), dehydrovomifoliol (13), loliolide (14), cholesteryl stearate (15), palmitic acid (16), cis-5,8,11,14,17-eicosapentaenoic acid (17) and alpha-linolenic acid (18) on the basis of spectroscopic and chemical evidences. Their anticholinesterase and antioxidant activities were evaluated via inhibitory activities on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) as well as scavenging activities on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and peroxynitrite (ONOO(-)).

Comparative analysis of the anti-inflammatory activity of Huang-lian extracts in lipopolysaccharide-stimulated RAW264.7 murine macrophage-like cells using oligonucleotide microarrays.

In this study, we attempted to determine the anti-inflammatory activity of a medicinal plant huang-lian using gene expression profiles as an index. Huang-line extracts (CEXs) were prepared from seven different plant origins and compared for their chemical composition and biological activity. In order to achieve this, RAW264.

Anti-amnesic activity of neferine with antioxidant and anti-inflammatory capacities, as well as inhibition of ChEs and BACE1.

Aims: the multifunctional potential of neferine derived from the embryo of Nelumbo nucifera seeds for the age-related neurodegenerative disorders, in vivo anti-amnesic activities and in vitro cholinesterases (ChEs)- and β-site APP cleaving enzyme 1 (BACE1)-inhibitory activities, as well as anti-inflammatory and antioxidant activities were investigated.

Main Methods: in vivo anti-amnesic activities were performed via the passive avoidance, Y-maze, and Morris water maze tasks in a scopolamine-induced amnesia model. The cell-free antioxidant capacities were evaluated by in vitro scavenging activities against 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radicals, and peroxynitrite (ONOO(-)), as well as inhibitory activities against nitric oxide (NO), superoxide anion (O(2)(-)), lipid peroxidation, and ONOO(-)-mediated tyrosine nitration.

Identification of anti-inflammatory target genes of Rhizoma coptidis extract in lipopolysaccharide-stimulated RAW264.7 murine macrophage-like cells.

Aim Of The Study: Rhizoma coptidis is used widely in traditional Oriental medicine to treat inflammatory diseases. The aim of this study was to identify the anti-inflammatory target genes of Rhizoma coptidis extract (CEX) in lipopolysaccharide (LPS)-stimulated RAW264.7 murine macrophage-like cells.

Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity.

In our consecutive research on an anti-AD remedy derived from maritime plants, the BACE1 inhibitory activities of Eisenia bicyclis and its isolated phlorotannins were evaluated. The E. bicyclis extract and its fractions exhibited predominant BACE1 inhibition.

Selective inhibition of prenylated flavonoids from Sophora flavescens against BACE1 and cholinesterases.

It was previously reported that certain lavandulylated flavanones from Sophora flavescens are beta-site APP cleaving enzyme 1 (BACE1) inhibitors; however, based upon their levels within the extract, their inhibitory effects should be higher than expected. Moreover, chalcones and flavonols were reported to exert higher bioactivities than flavanones. These findings have led to a further search for other possible constituents potentially contributing to the strong inhibitory activity of the S.

Alaternin attenuates delayed neuronal cell death induced by transient cerebral hypoperfusion in mice.

The aim of this study was to determine whether alaternin exhibits neuroprotective activity after transient cerebral hypoperfusion induced by bilateral common carotid artery occlusion (BCCAO). Mice were subjected to BCCAO, and circulation was restored after 20 min. Alaternin (10 mg/kg, p.

A new abietic acid-type diterpene glucoside from the needles of Pinus densiflora.

From the ethyl acetate fraction of the methanol extract of the needles of Pinus densiflora (Pinaceae), a new diterpenoid glucoside [9alpha,13alpha-epoxy-8beta,14beta-dihydroxy-abietic acid-18-O-beta-D: -glucopyranoside] (1), two flavonoid glucosides [kaempferol 3-O-beta-D: -glucoside (2) and 6-C-methyl kaempferol 3-O-beta-D: -glucoside (3)], and two monoterpenoid glucosides [bornyl 6-O-alpha-Larabinofuranosyl (1-->6)-beta-D: -glucopyranoside (4) and bornyl 6-O-beta-D: -apiofuranosyl (1-->6)-beta-D: -glucopyranoside (5)] were isolated and characterized on the basis of spectral analysis. Of all the compounds, 2 and 3 showed peroxynitrite scavenging activity.

Selective cholinesterase inhibitory activities of a new monoterpene diglycoside and other constituents from Nelumbo nucifera stamens.

A new beta-cyclogeraniol diglycoside (5), along with four known components, cycloartenol (1), p-hydroxybenzoic acid (2), vanilloloside (3), and 5'-O-methyladenosine (4), were first isolated from the n-BuOH fraction of Nelumbo nucifera stamens. The chemical structure of 5 was elucidated as 1-hydroxymethyl-2,6,6-trimethyl-1-cyclohexene 9-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranoside (nuciferoside) on the basis of chemical and spectroscopic evidence, including 1D, 2D NMR, and MS. The anti-Alzheimer effects of 1-5 were evaluated via the acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) inhibition assays.

Cholinesterase and BACE1 inhibitory diterpenoids from Aralia cordata.

Fourteen diterpenes were isolated from the n-hexane fraction of the roots of Aralia cordata (syn. = A. continentalis).

Kaempferol glycosides with antioxidant activity from Brassica juncea.

From the leaves of Brassica juncea, three kaempferol glycosides, kaempferol-3-O-(2-O-sinapoyl)-beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranoside-7-O-beta-D-glucopyranoside (1), kaempferol-3-O-beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranoside-7-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranoside (2), and kaempferol-3-O-(2-O-sinapoyl)-beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranoside-7-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranoside (3) were isolated and the structures elucidated on the basis of spectral and chemical evidences. Antioxidant activities were determined by measuring the scavenging activities on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and peroxynitrite (ONOO(-)). Compounds 1 and 3 showed good antioxidant activities with respective IC(50) values of 28.

Palmatine attenuates D-galactosamine/lipopolysaccharide-induced fulminant hepatic failure in mice.

Palmatine is an isoquinoline alkaloid from Coptis chinensis, an herbal medicine used to treat various inflammatory diseases such as gastritis, edema and dermatitis. The present study examined the cytoprotective properties of palmatine on d(+)-galactosamine (GalN)/lipopolysaccharide (LPS)-induced fulminant hepatic failure. Mice were intraperitoneally given GalN (700 mg/kg)/LPS (10 microg/kg).

Anti-inflammatory activity of the constituents of the roots of Aralia continentalis.

To assess the anti-inflammatory activity of the constituents of the roots of Aralia continentalis, ent-pimara-8(14),15-diene-19-oic acid (continentalic acid, pimaradienoic acid, compound I), 7beta-hydroxy-ent-pimara-8(14),15-diene-19-oic acid (compound II), 7-oxo-ent-pimara-8(14),15-diene-19-oic acid (compound III), 15alpha,16alpha-epoxy-17-hydroxy-ent-kauran-19-oic acid (compound IV) and ent-kaura-16-en-19-oic acid (kaurenoic acid, compound V), their inhibitory effects against cyclooxygenase-2 (COX-2)-catalyzed PGE(2) and inducible nitric oxide synthase (iNOS)-catalyzed NO production by lipopolysaccharide-treated RAW 264.7 cells were examined. Among the compounds tested, compound III and V moderately inhibited NO production.

Quantitative HPLC analysis of two key flavonoids and inhibitory activities against aldose reductase from different parts of the Korean thistle, Cirsium maackii.

Previously, the correlation between antioxidant activity and HPLC profiles of several Korean thistles has been recognized. In our ongoing study of the comparative evaluation of Korean thistles, we chose Cirsiummaackii to assess the antioxidant and aldose reductase (AR) inhibitory activities of its varying parts, including the leaves, roots, stems, and flowers, along with two major components, luteolin 5-O-beta-d-glucopyranoside (1) and the aglycone luteolin (2). In order to determine selective and efficient usage of the individual parts, HPLC quantitative analysis of the two key flavonoids of each C.

Anti-Alzheimer and antioxidant activities of Coptidis Rhizoma alkaloids.

Coptidis Rhizoma and its isolated alkaloids are reported to possess a variety of activities, including neuroprotective and antioxidant effects. Thus, the anti-Alzheimer and antioxidant effects of six protoberberine alkaloids (berberine, palmatine, jateorrhizine, epiberberine, coptisine, and groenlandicine) and one aporphine alkaloid (magnoflorine) from Coptidis Rhizoma were evaluated via beta-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) assays, along with peroxynitrite (ONOO(-)) scavenging and total reactive oxygen species (ROS) inhibitory assays. Six protoberberine alkaloids exhibited predominant cholinesterases (ChEs) inhibitory effects with IC(50) values ranging between 0.