Chemical characterization and biological activity in young sesame leaves (Sesamum indicum L.) and changes in iridoid and polyphenol content at different growth stages.

Three iridoids (lamalbid (I1), sesamoside (I2) and shanzhiside methyl ester (I3)) and seven polyphenols (cistanoside F (P1), chlorogenic acid (P2), pedalitin-6-O-laminaribioside (P3), pedaliin (P4), isoacteoside (P6), pedalitin (P7) and martynoside (P8)) were identified in young sesame leaves (Sesamum indicum L.) other than the acteoside (P5) reported previously. P3 was a new compound, and I1, I3, P2 and P8 were found in a species of Sesamum for the first time.

β-carotene reverses the IL-1β-mediated reduction in paraoxonase-1 expression via induction of the CaMKKII pathway in human endothelial cells.

Interleukin-1 beta (IL-1β) induces endothelial dysfunction and reduces nitric oxide (NO) production. IL-1β also enhances adhesion molecule expression and induces arteriosclerosis. Conversely, high-density lipoprotein (HDL) induces endothelial NO synthase (eNOS), paraoxonase-1 (PON-1) activity, and maintains vascular health.

Interaction of heliquinomycin with single-stranded DNA inhibits MCM4/6/7 helicase.

The antibiotic heliquinomycin inhibited cellular DNA replication at IC(50) of 2.5 µM without affecting level of chromatin-bound MCM4 and without activating the DNA replication stress checkpoint system, suggesting that heliquinomycin perturbs DNA replication mainly by inhibiting the activity of replicative DNA helicase that unwinds DNA duplex at replication forks. Among the DNA helicases involved in DNA replication, DNA helicase B was inhibited by heliquinomycin at IC(50) of 4.

Dietary apigenin regulates high glucose and hypoxic reoxygenation-induced reductions in apelin expression in human endothelial cells.

The early stages of vascular endothelial dysfunction enhance angiogenic stimulation and strongly influence vascular rearrangement. The aim of this study was to determine whether a short period of high glucose (HG, 30 mM glucose) plus tumor necrosis factor alpha (TNFα) treatment or reoxygenation after hypoxia (H/R) alters the expression levels of apelin in human endothelial cells. In addition, we also examined the effects of the dietary flavonoid apigenin on apelin expression.

Minichromosome Maintenance Protein 7 is a potential therapeutic target in human cancer and a novel prognostic marker of non-small cell lung cancer.

Background: The research emphasis in anti-cancer drug discovery has always been to search for a drug with the greatest antitumor potential but fewest side effects. This can only be achieved if the drug used is against a specific target located in the tumor cells. In this study, we evaluated Minichromosome Maintenance Protein 7 (MCM7) as a novel therapeutic target in cancer.

Apigenin inhibits tumor necrosis factor alpha plus high glucose-induced LOX-1 expression in human endothelial cells.

Although hyperglycemia can induce diabetic vascular disorders, the mechanisms responsible for the early stages of this process are unknown. To determine the factor(s) that initially stimulate hyperglycemia and the preventive effects of polyphenols, we examined the effects of high glucose (HG) conditions and several dietary polyphenols on human endothelial cells (EC). The purpose of the present study was to investigate the augmentation of the expression of angiotensin II type I receptor (AT1R), cyclooxygenase-2 (COX-2), lectin-like oxidized LDL receptor-1 (LOX-1), prostacyclin/prostaglandin I 2 synthase (PGIS), and thromboxane A2 synthase (TXA2S) by tumor necrosis factor-alpha (TNFα) in HG conditions (30mM) in human EC over a short period, and we also investigated the regulatory effects of 10 dietary flavonoids.

Stroke status evoked adhesion molecule genetic alterations in astrocytes isolated from stroke-prone spontaneously hypertensive rats and the apigenin inhibition of their expression.

We examined the possibility that the expression of adhesion molecules is regulated differently in cultured astrocytes from stroke-prone spontaneously hypertensive rats (SHRSP/IZM) rats than in those from Wistar Kyoto rats (WKY/IZM) by tumor necrosis factor-alpha (TNF-alpha) or hypoxia and reoxygenation (H/R) and the inhibitory effects of apigenin. It was found that the expression of vascular cell adhesion molecule-1 (VCAM-1) by TNF-alpha in astrocytes isolated from SHRSP/IZM was increased compared with that in WKY/IZM. The expression of monocyte chemotactic protein-1 (MCP-1) mRNA induced by H/R in SHRSP/IZM astrocytes was increased compared with that in normal oxygen concentrations.

Effect of heliquinomycin on the activity of human minichromosome maintenance 4/6/7 helicase.

The antibiotic heliquinomycin, which inhibits cellular DNA replication at a half-maximal inhibitory concentration (IC(50)) of 1.4-4 microM, was found to inhibit the DNA helicase activity of the human minichromosome maintenance (MCM) 4/6/7 complex at an IC(50) value of 2.4 microM.

Dietary flavonoid apigenin inhibits high glucose and tumor necrosis factor alpha-induced adhesion molecule expression in human endothelial cells.

Diabetes mellitus is associated with increased endothelial dysfunction and development of atherosclerotic vascular diseases. In contrast, an increased intake of dietary flavonoids is associated with a decreased risk of cardiovascular diseases. Here we demonstrate that high glucose (HG) and tumor necrosis factor alpha (TNFalpha) result in the expression of adhesion molecules and junctional molecules on endothelial cells (EC) within a short time.

Adenosine induces expression of glial cell line-derived neurotrophic factor (GDNF) in primary rat astrocytes.

Adenosine, which accumulates rapidly during ischemia due to the breakdown of ATP, has beneficial effects in many tissues. We examined whether adenosine induces the production of glial cell line-derived neurotrophic factor (GDNF) in cultured astrocytes. We evaluated GDNF mRNA expression and GDNF production in astrocytes cultured with adenosine and the adenosine selective receptor agonists 5-(N-ethylcarboxamido) adenosine (NECA), N(6)-cyclopentyladenosine (CPA) and 2-p-(2-carboxyethyl) phenethylamino-5'-N-ethylcarboxamindo-adenosine hydrochloride (CGS 21680).

Stability to light, heat, and hydrogen peroxide at different pH values and DPPH radical scavenging activity of acylated anthocyanins from red radish extract.

The stability of red radish extract to light, heat, and hydrogen peroxide at different pH values (3, 5, and 7) was examined, in which major anthocyanins were pelargonidin glycosides acylated with a combination of p-coumaric, ferulic, or caffeic acids. The light irradiation (fluorescence light, 5000 lx; at 25 degrees C) indicated that the red radish extract was more stable at lower pH than at higher pH. The HPLC analyses revealed that diacylated anthocyanins in the extract were more stable to light at pH 3 than monoacylated anthocyanins.

Effects of paprika pigments on oxidation of linoleic acid stored in the dark or exposed to light.

We examined the antioxidant effects of paprika pigments on oxidation of linoleic acid and on decoloration of the sample when stored at 37 degrees C in the dark or exposed to fluorescent light for 8 h per day. (1)H nuclear magnetic resonance with dioxane as an external proton reference was used to estimate the oxidative deterioration of linoleic acid. Oxidation was estimated by observing the ratio of the divinylmethylene proton signal area in linoleic acid vs the proton signal area in dioxane.

Identification and behavior of reaction products formed by chlorination of ethynylestradiol.

Six products were formed by reaction of ethynylestradiol (EE2) with sodium hypochlorite in buffered solutions. 4-Chloroethynylestradiol (4-ClEE2) and 2,4-dichloroethynylestradiol (2,4-diClEE2) were identified as the two major reaction products, using preparative HPLC, MS, and NMR. When EE2 reacted with chlorine at different pHs (pH 5, 7, and 9) or chlorine concentrations (0.

Identification of reaction products of acylated anthocyanins from red radish with peroxyl radicals.

Red radish anthocyanin extract, which consists of 12 known acylated anthocyanins, was reacted with 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH) to generate peroxyl radicals under acidic pH conditions at 37 degrees C. The reaction products were isolated using preparative HPLC, and their chemical structures were determined to be p-hydroxybenzoic acid (1), 6-O-(E)-p-coumaroyl-2-O-beta-d- glucopyranosyl-alpha-d-glucopyranoside (3), p-coumaric acid (4), 6-O-(E)-feruloyl-2-O-beta-d-glucopyranosyl-alpha-d-glucopyranoside (5), and ferulic acid (6). Some products were not identified.

[Constituent of natural food additive hokosshi extract and an analytical method for the additive in foods].

Hokosshi extract is obtained by ethanol extraction from the seeds of hokosshi (Psoralea corylifolia), which is used as a Chinese medicine. The constituents of hokosshi extract were analyzed. The main constituent was isolated using column chromatography, and identified as bakuchiol by TLC, LC/MS and NMR.

An epidermal growth factor-like toxin and two sodium channel toxins from the sea anemone Stichodactyla gigantea.

Three peptide toxins (gigantoxins I-III) with crab toxicity were isolated from the sea anemone Stichodactyla gigantea by gel filtration on Sephadex G-50 and reverse-phase HPLC on TSKgel ODS-120T and their complete amino acid sequences were determined. Gigantoxins II (44 residues) and III (48 residues) have LD(50) (against crabs) of 70 and 120 microg/kg, respectively, and are analogous to the known type 1 and 2 sea anemone sodium channel toxins, respectively. On the other hand, gigantoxin I (48 residues) is potently paralytic to crabs (ED(50) 215 microg/kg), although its lethality is very weak (LD(50)>1000 microg/kg).