The anti-diabetic effects of ethanol extract from two variants of Artemisia princeps Pampanini in C57BL/KsJ-db/db mice.

The anti-diabetic effects of two variants of Artemisia princeps Pampanini, sajabalssuk (SB) and sajuarissuk (SS), were investigated in type 2 diabetic animal using their ethanol extracts. Male C57BL/KsJ-db/db (db/db) mice were divided into control, SB ethanol extract (SBE), SS ethanol extract (SSE), or rosiglitazone (RG) groups and their age-matched littermates (db/+) were used. Supplementation of the SBE (0.

Characterizing the wave aberration in eyes with keratoconus or penetrating keratoplasty using a high-dynamic range wavefront sensor.

Purpose: The purpose of this study was to characterize aberrations in 2 populations of eyes, namely those with keratoconus (KC) and those having undergone penetrating keratoplasty (PK), using a large-dynamic range Shack-Hartmann wavefront sensor.

Design: Prospective comparative case series.

Participants: Twenty-one people with ocular pathologic features (either KC or PK) were recruited for this study.

2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship.

Designed and synthesized were a series of pyridines substituted at 2, 4, and 6 positions with various 5- or 6-memberd heteroaromatics as antitumor agents. They were evaluated their topoisomerase I and II inhibitory activities along with cytotoxicities against several human cancer cell lines. Among the prepared compounds, 10-20 showed significant topoisomerase I or II inhibitory activities, and 21-26 showed considerable cytotoxicities against several human cancer cell lines.

Lignans from the fruits of Cornus kousa Burg. and their cytotoxic effects on human cancer cell lines.

The fruits of Cornus kousa Burg. were extracted with 80% aqueous MeOH, and the concentrated extract partitioned with EtOAc, n-BuOH and H2O. Six lignans were isolated from the EtOAc fraction through repeated silica gel, ODS and Sephadex LH-20 column chromatographies.

Metabolism of FPP-3, an anti-inflammatory propenone compound, in rat by liquid chromatography-electrospray ionization tandem mass spectrometry.

1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) is an anti-inflammatory agent with a propenone moiety. Following a single intravenous injection of male Sprague-Dawley rats with 4 mg/kg of FPP-3, three different metabolites of FPP-3 were identified as M1 (1-furan-2-yl-3-pyridin-2-yl-propan-1-one), M2 (1-furan-2-yl-3-pyridin-2-yl-propan-1-ol) and M3 (a glucuronide conjugate of M2) in rat urine by a liquid chromatography-electrospray tandem mass spectrometry. The structures of M1 and M2 were the same as observed previously following the incubation of rat liver microsomes with FPP-3 in the presence of NADPH.

Linoleoyl lysophosphatidic acid and linoleoyl lysophosphatidylcholine are efficient substrates for mammalian lipoxygenases.

Oxygenation of two lysophospholipids, 1-linoleoyl lysophosphatidylcholine (linoleoyl-lysoPC) and 1-linoleoyl lysophosphatidic acid (linoleoyl-lysoPA), by reticulocyte lipoxygenase (LOX) or porcine leukocyte LOX was measured by monitoring the formation of conjugated dienes. Consistent with the above, the formation of linoleoyl-lysophospholipid hydroperoxide as oxygenation product was confirmed by LC/MS analyses. In further study, the oxygenation products of linoleoyl-lysoPC or linoleoyl-lysoPA were found to contain hydroperoxide group predominantly at C-13 with the S enantiomer as a major one, in a good agreement with the positional-specificity and stereo-selectivity of reticulocyte LOX or leukocyte LOX in oxygenation of linoleic acid.

Application of umbilical cord serum eyedrops for the treatment of neurotrophic keratitis.

Purpose: To investigate the efficacy of umbilical cord serum eyedrops for the treatment of neurotrophic keratitis.

Design: Prospective noncomparative case series.

Participants: Twenty-eight eyes of 28 patients with neurotrophic keratitis who were refractory to conventional treatment.

Vision improvement by correcting higher-order aberrations with customized soft contact lenses in keratoconic eyes.

Higher-order aberration correction in abnormal eyes can result in significant vision improvement, especially in eyes with abnormal corneas. Customized optics such as phase plates and customized contact lenses are one of the most practical, nonsurgical ways to correct these ocular higher-order aberrations. We demonstrate the feasibility of correcting higher-order aberrations and improving visual performance with customized soft contact lenses in keratoconic eyes while compensating for the static decentration and rotation of the lens.

Eugenol inhibit 7,12-dimethylbenz[a]anthracene-induced genotoxicity in MCF-7 cells: Bifunctional effects on CYP1 and NAD(P)H:quinone oxidoreductase.

Typically, chemopreventive agents either inhibit the cytochrome P450s (CYPs) that are essential for the metabolism of carcinogens or induce phase II detoxifying enzymes. This study examined the chemopreventive effect of eugenol on 7,12-dimethylbenz[a]anthracene (DMBA)-induced DNA damage in MCF-7 cells. Eugenol inhibited the formation of the DMBA-DNA adduct in a dose dependent manner.

Role of glutathione conjugation in the hepatotoxicity and immunotoxicity induced by 1-bromopropane in female BALB/c mice.

1-Bromopropane (1-BP) is used as a cleaning agent or adhesive solvent in the workplace. In the present study, the hepatotoxic and immunotoxic effects of 1-bromopropane and its conjugation with glutathione (GSH) were investigated in female BALB/c mice. The animals were treated orally with 200, 500 and 1000 mg kg(-1) of 1-BP in corn oil for a dose response study or treated orally with 1000 mg kg(-1) of 1-BP for 6, 12, 24 and 48 h for a time course study.

Synthesis, cytotoxicity and structure-activity relationship study of terpyridines.

For the development of novel antitumor agents, we designed and synthesized terpyridines, and their biological activities were evaluated. Although most of the newly prepared terpyridines showed strong cytotoxicity against several human cancer cell lines, [2,2';6',2"]-terpyridine displayed the most significant cytotoxicity.

Method of reconstructing wavefront aberrations by use of Zernike polynomials in radial shearing interferometers.

A novel method of reconstructing wavefront aberrations by use of Zernike polynomials for radial shearing interferometers is discussed. This method uses matrix formalism to calculate the Zernike coefficients of a wavefront under test and shows the validity of reconstructing an arbitrary wavefront aberration from an interferogram taken by a radial shearing interferometer. We also propose a new interferometer setup to determine the shape and the direction (concave or convex) of wavefront aberration in a single measurement.

Human acyl-CoA: cholesterol acyltransferase inhibitory activities of aliphatic acid amides from Zanthoxylum piperitum DC.

Acyl-CoA: cholesterol acyltransferase (ACAT) plays an important role in the esterification of cholesterol with its substrates, cholesterol and fatty acyl coenzyme A, to facilitate both intracellular storage and intercellular transport. ACAT-1 is more involved in macrophage foam cell formation and ACAT-2 plays a critical role in the cholesterol absorption process in intestinal enterocytes. Three aliphatic acid amides, beta-sanshool (1), gamma-sanshool (2), and hydroxy-beta-sanshool (3), were isolated by bioassay-guided fractionation of the ethanolic extracts of Zanthoxylum piperitum DC.

Hypocholesterolemic and antioxidative effects of naringenin and its two metabolites in high-cholesterol fed rats.

This study was conducted to compare the hypocholesterolemic and antioxidant effects of naringenin (0.02%), and its metabolites, rho-hyproxyphenylpropionic acid (PHPP, 0.012%) and rho-hydroxybenzoic acid (PHB, 0.

Human ACAT inhibitory effects of shikonin derivatives from Lithospermum erythrorhizon.

Three naphthoquinones were isolated by bioassay-guided fractionation from the CHCl(3) extracts of roots of Lithospermum erythrorhizon. They were identified as acetylshikonin (1), isobutyrylshikonin (2), and beta-hydroxyisovalerylshikonin (3) on the basis of their spectroscopic analyses. The compounds 1-3 were tested for their inhibitory activities against human ACAT-1 (hACAT-1) or human ACAT-2 (hACAT-2).

Identification of 1-furan-2-yl-3-pyridin-2-yl-propenone, an antiinflammatory agent, and its metabolites in rat liver subcellular fractions.

1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) has been characterized to have an anti-inflammatory activity through the inhibition of the production of nitric oxide and tumor necrosis factor-alpha. In the present studies, the phase 1 metabolism of FPP-3 was investigated in rat liver microsomes and cytosols. When FPP-3 was incubated with rat liver microsomes and cytosols in the presence of NADPH, 2 major peaks were detected on a liquid chromatography/electrospray ionization-mass spectrometry.

Protective effect of the ethanol extract of the roots of Brassica rapa on cisplatin-induced nephrotoxicity in LLC-PK1 cells and rats.

A study was conducted to determine whether the ethanol extract of the roots of Brassica rapa (EBR) ameliorates cisplatin-induced nephrotoxicity in terms of oxidative stress, as characterized by lipid peroxidation, reactive oxygen species (ROS) production, and glutathione (GSH) depletion in LLC-PK1 cells. Pretreatment of cells with EBR prevented cisplatin-induced decreases in cell viability and cellular GSH content. The effect of EBR was then investigated in rats given EBR for 14 d before cisplatin administration.

3-heptylamino-5-phenylpyridazine derivatives as analogues of Acyl-CoA: cholesterol acyltransferase inhibitors containing the N-heptyl-N'-arylureidic moiety.

A series of novel Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors 8a-f was synthesized; the substances were characterized by the presence of a 2,5-dimethylpyrazin-3-yl moiety at one end and a 3-heptylamino-5-phenylpyridazine system at the other one, linked through linear alkyl spacers of different length. The new derivatives were designed based on the hypothesis that the 3-amino-5-phenylpyridazine moiety could mimic the aryl substituted urea, which was present in a number of ACAT inhibitors previously described. The choice of the 2,5-dimethylpyrazin-3-yl substituent was supported by a preliminary investigation, which indicated that this moiety is the most powerful in conferring ACAT inhibitory properties to the new series.

DA-9601 inhibits activation of the human mast cell line HMC-1 through inhibition of NF-kappaB.

Mast cell-mediated allergic inflammation is involved in many diseases such as asthma, sinusitis, and rheumatoid arthritis. Mast cells induce synthesis and production of pro-inflammatory cytokines including tumor necrosis factor (TNF)-alpha, interleukin (IL)-1beta and IL-6 with immune regulatory properties. The formulated ethanol extract of Artemisia asiatica Nakai (DA-9601) has been reported to have antioxidative and anti-inflammatory activities.

Anti-atherosclerotic effect of a new synthetic functional oil containing mono- and diacylglycerol from corn oil.

Synthetic oil containing diacylglycerol and monoacylglycerol, called 'functional oil' (FO), was newly produced and evaluated for its putative anti-atherosclerotic potential by in vitro assays and in vivo test using hypercholesterolemic mice (C57BL/6). The FO revealed good inhibitory activities against both liver acyl-CoA:cholesterol acyltransferase and serum lipoprotein-associated phospholipase A2. The FO showed enhanced activities on lipoprotein interaction such as HDL particle rearrangement to produce different sizes of HDL species.

Gigantol isolated from the whole plants of Cymbidium goeringii inhibits the LPS-induced iNOS and COX-2 expression via NF-kappaB inactivation in RAW 264.7 macrophages cells.

During our efforts to find bioactive natural products with anti-inflammatory activity, we isolated gigantol from the whole plants of Cymbidium goeringii (Orchidaceae) by activity-guided chromatographic fractionation. Gigantol was found to have potent inhibitory effects on LPS-induced nitric oxide (NO) and prostaglandin E (2) (PGE (2)) production in RAW 264.7 cells.

Anti-atherosclerotic and anti-inflammatory activities of catecholic xanthones and flavonoids isolated from Cudrania tricuspidata.

The catecholic xanthones and flavonoids 1-13 were isolated from the root bark of Cudrania tricuspidata. Compounds 1 and 3-8 exhibited significant antioxidant activity against low-density lipoprotein (LDL) oxidation in the thiobarbituric acid-reactive substance (TBARS) assay. Among them, prenylated flavonoids 10-12 showed an inhibitory effect on the NO production and iNOS expression in RAW264.

Potent inhibitors of lipoprotein-associated phospholipase A(2): benzaldehyde O-heterocycle-4-carbonyloxime.

A series of multi-substituted oximes were prepared and their potencies for inhibiting lipoprotein-associated phospholipase A(2) (Lp-PLA(2)) activity were evaluated in vitro. Among them, compounds 3a, 3b, and 3m were identified to display a micromolar potency for inhibiting Lp-PLA(2) in whole human plasma and isolated human LDL. Based on these results, structure-activity relationship was studied on modification of three parts of R(1), R(2), and R(3) to identify a potent pharmacophore for Lp-PLA(2).

Antioxidant and anti-inflammatory activities of N-acetyldopamine dimers from Periostracum Cicadae.

A known N-acetyldopamine dimer, (2R,3S)-2-(3',4'-dihydroxyphenyl)-3-acetylamino-7-(N-acetyl-2''-aminoethyl)-1,4-benzodioxane (1) and a new N-acetyldopamine dimer, (2R,3S)-2-(3',4'-dihydroxyphenyl)-3-acetylamino-7-(N-acetyl-2''-aminoethylene)-1,4-benzodioxane (2) were isolated from the methanolic extracts of Periostracum Cicadae. Compounds 1 and 2 inhibited the Cu2+ -mediated, 2,2'-azobis(2-amidinopropane) hydrochloride (AAPH)-mediated, and 3-morpholinosydnonimine (SIN)-1-mediated LDL oxidation in the thiobarbituric acid-reactive substances (TBARS) assay. The antioxidant activities of 1 and 2 were tested with respect to other parameters, such as lag time of conjugated diene formation, relative electrophoretic mobility (REM), and apoB-100 fragmentation on copper-mediated LDL-oxidation.

A preventive approach to oral self-mutilation in Lesch-Nyhan syndrome: a case report.

Lesch-Nyhan syndrome is a rare X-linked recessive disorder of purine metabolism, caused by complete absence of the enzyme hypoxanthine-guanine phosphoribosyl transferase. Persons affected with this incurable disease are developmentally and physically delayed, and suffer from self-injurious behavior. The most typical feature results in partial or total destruction of perioral tissues.