To evaluate the estrogenic activities of several chemicals such as 17 beta-estradiol (E2), rho-nonylphenol, bisphenol A, butylparaben, and combinations of these chemicals, we used recombinant yeasts containing the human estrogen receptor [Saccharomyces cerevisiae ER + LYS 8127]. We evaluated E2 was most active in the recombinant yeast assay, followed by rho-nonylphenol, bisphenol A, butylparaben. The combinations of some concentrations of 17-estradiol as a strong estrogen and bisphenol A or butylparaben as a weak estrogen showed additive estrogenic effects. Also, the combinations of some concentrations of nonlyphenol and butylparaben and combination of butylparaben and bisphenol A showed additive effects in the estrogenic activity. Therefore, the estrogenic activities of the combinations of two chemicals were additive, not synergistic.
Cloning, Molecular ; Estradiol/pharmacology ; Estrogens/classification/*pharmacology ; Estrogens, Non-Steroidal/*pharmacology ; Humans ; Kinetics ; Parabens/pharmacology ; Phenols/pharmacology ; Receptors, Estrogen/drug effects/*physiology ; Recombinant Proteins/drug effects/metabolism ; Saccharomyces cerevisiae/genetics

OBJECTIVETo investigate the chemical constituents of the brown alga D. divaricata, and to test cytotoxicities of the purified compounds.

METHODCompounds were isolated by normal phase silica gel, Sephadex LH-20 chromatography and reverse phase HPLC techniques. Their structures were elucidated by spectroscopic methods including IR, MS and NMR. Cytotoxicities were tested by MTT method.

RESULTEight compounds were isolated from ethanolic extract of the brown alga D. divaricata and their structures were identified as (-)-torreyol (I), 4beta, 5alpha-dihydroxycubenol (II), 3-farnesyl-p-hydroxybenzioc acid (III), chromazonarol (IV), fucosterol (V), phenyl acetylamine (VI), 4-hydroxybenzoic acid (VII) and n-hexadecanoic acid (VIII).

CONCLUSIONCompound II and IV were obtained from this alga for the first time. The others were isolated from the Dictyotaceae algae for the first time. All compounds were inactive (IC50 > 10 microg x mL(-1)) against human tumor cell lines KB, Bel-7402, PC-3M, Ketr 3 and MCF-7.

Cell Line, Tumor ; drug effects ; Humans ; Parabens ; chemistry ; isolation & purification ; pharmacology ; Phaeophyta ; chemistry ; Stigmasterol ; analogs & derivatives ; chemistry ; isolation & purification ; pharmacology ; Terpenes ; chemistry ; isolation & purification ; pharmacology ; Xanthenes ; chemistry ; isolation & purification ; pharmacology

OBJECTIVETo study the chemical constituents possessing cytotoxicity activity from Elaeagnus pungens.

METHODThe constituents were separated through repeated chromatographic methods and their structures were elucidated by spectral analysis.

RESULTFive compounds were isolated from the ethyl acetate ether extract of leaves of E. pungens. Their structures were elucidated as 4-hydroxybenzoic acid (1), 3, 3'-dimethoxyquercetin (2), caffeic acid methyl ester (3), methyl 3, 4-dihydroxybenzoate (4), spingic acid (5), 4-methoxylbenzoic acid (6), 3-methylkaempferol (7), kaempferol-3-O-beta-D-glucoside (8), dausosterol (9).

CONCLUSIONCompounds 1-8 were isolated from this plant for the first time.

Caffeic Acids ; chemistry ; isolation & purification ; pharmacology ; Cell Proliferation ; drug effects ; Elaeagnaceae ; chemistry ; HeLa Cells ; cytology ; Humans ; Kaempferols ; chemistry ; isolation & purification ; pharmacology ; Parabens ; chemistry ; isolation & purification ; pharmacology ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Quercetin ; analogs & derivatives ; chemistry ; isolation & purification ; pharmacology

This study is to investigate the activation effect of butyl-p-hydroxybenzoate (Bpb) on cAMP-dependent cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel gating. A stably transfected Fischer rat thyroid (FRT) epithelial cell lines co-expressing human CFTR and a green fluorescent protein mutant with ultra-high halide sensitivity (EYFP) were used to measure CFTR-mediated iodide influx rates. Bpb was identified as an effective activator of wild-type CFTR chloride channel, it can correct delta F508-CFTR gating defects but not processing defect. Bpb can't potentiate G551D-CFTR channel gating. The activity was reversible and dose-dependent. The study also provided clues that Bpb activates CFTR chloride channel through a direct binding mechanism. Our study identified Bpb as a novel structure CFTR activator. Bpb may be useful for probing CFTR channel gating mechanisms and as a lead compound to develop pharmacological therapy for CFTR-related disease.
Animals ; Cell Line ; Cystic Fibrosis Transmembrane Conductance Regulator ; genetics ; metabolism ; Dose-Response Relationship, Drug ; Epithelial Cells ; metabolism ; Green Fluorescent Proteins ; genetics ; metabolism ; Ion Channel Gating ; drug effects ; Mutation ; Parabens ; administration & dosage ; pharmacology ; Rats ; Rats, Inbred F344 ; Thyroid Gland ; cytology

OBJECTIVETo investigate the chemical constituents of the branches and leaves of Polyalthia nemoralis.

METHODThe compounds were isolated and purified by silica gel, macroporous adsorption resin and Sephadex LH-20 column chromatographic methods. Their chemical structures were elucidated on the basis of physicochemical properties and spectral data.

RESULTFourteen compounds were isolated and identified as syringic acid (1), 3-methoxy-4-hydroxycinnamic acid (2), vanillic acid (3), 4-hydroxybenzoic acid (4), mauritianin (5), (+)-xylopinidine (6), (+)-oblongine(7), (+)-tembetarine (8), eythritol (9), D-mannitol (10), ethyl-beta-D-glucopyranoside (11), (+)-magnoflorine (12), stepharanine (13), (2S, 4R)-4-hydroxy-2-piperidine-carboxylic acid (14), respectively.

CONCLUSIONAll the compounds were isolated from the genus Polyalthia for the first time; compounds 6 and 13 showed inhibitation activities against multi tumor cell lines.

Alkaloids ; chemistry ; isolation & purification ; pharmacology ; Antineoplastic Agents, Phytogenic ; chemistry ; pharmacology ; Aporphines ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Cell Survival ; drug effects ; Chromatography, Agarose ; methods ; Coumaric Acids ; chemistry ; isolation & purification ; pharmacology ; Gallic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; pharmacology ; Humans ; Kaempferols ; chemistry ; isolation & purification ; pharmacology ; Parabens ; chemistry ; isolation & purification ; pharmacology ; Plant Extracts ; chemistry ; isolation & purification ; pharmacology ; Plant Leaves ; chemistry ; Plant Stems ; chemistry ; Polyalthia ; chemistry ; Vanillic Acid ; chemistry ; isolation & purification ; pharmacology

OBJECTIVETo evaluate the influence of an extract of Genista tinctoria L. herba (GT) or methylparaben (MP) on histopathological changes and 2 biomarkers of oxidative stress in rats subchronicly exposed to bisphenol A (BPA).

METHODSAdult female Wistar rats were orally exposed for 90 d to BPA (50 mg/kg), BPA+GT (35 mg isoflavones/kg) or BPA+MP (250 mg/kg). Plasma and tissue samples were taken from liver, kidney, thyroid, uterus, ovary, and mammary gland after 30, 60, and 90 d of exposure respectively. Lipid peroxidation and in vivo hydroxyl radical production were evaluated by histological analysis along with malondialdehyde and 2,3-dihydroxybenzoic acid detection.

RESULTSThe severity of histopathological changes in liver and kidneys was lower after GT treatment than after BPA or BPA+MP treatment. A minimal thyroid receptor antagonist effect was only observed after BPA+MP treatment. The abnormal folliculogenesis increased in a time-dependent manner, and the number of corpus luteum decreased. No significant histological alterations were found in the uterus. The mammary gland displayed specific estrogen stimulation changes at all periods. Both MP and GT revealed antioxidant properties reducing lipid peroxidation and BPA-induced hydroxyl radical generation.

CONCLUSIONGT L. extract ameliorates the toxic effects of BPA and is proved to have antioxidant potential and antitoxic effect. MP has antioxidant properties, but has either no effect or exacerbates the BPA-induced histopathological changes.

Animals ; Benzhydryl Compounds ; toxicity ; Chemical and Drug Induced Liver Injury ; pathology ; prevention & control ; Endocrine Disruptors ; toxicity ; Female ; Genista ; Hydroxyl Radical ; blood ; Lipid Peroxidation ; drug effects ; Liver ; pathology ; Oxidative Stress ; drug effects ; Parabens ; toxicity ; Phenols ; toxicity ; Phytotherapy ; Plant Extracts ; pharmacology ; therapeutic use ; Rats ; Rats, Wistar