Biofilms

A series of isoindoline derivatives were designed, synthesized, and evaluated for their double inhibitory activities. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological tests showed that all compounds exhibited 5-HT or NE reuptake inhibition activity. Among the tested compounds, compound I-3 exhibited potent inhibitory activity against 5-HT and NE reuptake in vitro, and exhibited potent antidepressant activity in vivo. These compounds designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
Antidepressive Agents ; chemical synthesis ; chemistry ; Biological Transport ; Drug Design ; Isoindoles ; chemical synthesis ; chemistry ; Serotonin Uptake Inhibitors ; chemical synthesis ; chemistry ; Structure-Activity Relationship

OBJECTIVETo discuss the changes in Wnt pathway inhibiting factors in esophageal precancerosis lesions induced by methyl benzyl nitrosamine (MBNA) and the effect of Gexia Zhuyu decoction.

METHODWistar rats were subcutaneously injected with MBNA (3.5 mg x kg(-1) for twice per week to establish the model. Since the 1st day after the model establishment, they were orally administered with Gexia Zhuyu decoction (16, 8 mg x kg(-1)). At the 10th week, esophageal tissues were collected to observe the pathological changes of esophageal mucosa, detect SFRP1, sFRP4, Axin1, Axin2 and GSK-3β mRNA levels.by fluorescent quantitation PCR analysis and β-catenin protein level by Western blotting.

RESULTBeing induced by MBNA, rats in the model group showed slight atypical hyperplasia in the histopathological examination. Compared with the normal group, Gexia Zhuyu decoction dose high and low groups showed no significant pathomorphological and histological changes. The model group showed lower gene transcription levels of esophageal tissues sFRP1, sFRP4, Axin1 and Axin2 (P < 0.05 or P < 0.01) and higher β-catenin protein expression level (P < 0.01) than the normal control group. The Gexia Zhuyu decoction low dose group showed higher gene transcription levels of esophageal tissues sFRP1, sFRP4, Axin1 and Axin2 (P < 0.05 or P < 0.01) and lower β-catenin protein expression level (P < 0.01) than the normal control group.

CONCLUSIONUp-regulated β-catenin protein level and down-regulated Wnt pathway could enhance Wnt pathway activity of MBNA-induced esophageal precancerous lesions. Gexia Zhuyu decoction could down-regulate the β-catenin protein level and up-regulate the transcription level of Wnt pathway inhibiting factors, but could not block MBNA-induced esophageal precancerosis lesions.

Animals ; Axin Protein ; genetics ; metabolism ; Drugs, Chinese Herbal ; administration & dosage ; Esophageal Diseases ; drug therapy ; genetics ; metabolism ; pathology ; Glycogen Synthase Kinase 3 ; genetics ; metabolism ; Glycogen Synthase Kinase 3 beta ; Humans ; Male ; Necrosis ; Nitrosamines ; adverse effects ; Proteins ; genetics ; metabolism ; Rats ; Rats, Wistar ; Wnt Proteins ; genetics ; metabolism ; Wnt Signaling Pathway ; drug effects

Child ; Child, Preschool ; Female ; Flow Cytometry ; methods ; Humans ; Infant ; Male ; Thrombasthenia ; classification ; diagnosis

Ten glycosidic compounds were isolated from an ethanol extract of Machilus wangchiana by a combination of various chromatographic techniques including column chromatography over silica gel and Sephadex LH-20 and reversed-phase flash chromatography and HPLC. Their structures were identified by spectroscopic data analysis (IR, MS, and NMR) as icariside B1 (1), boscialin-3-O-β-D-glucopyranoside (2), pisumionoside (3), isolariciresinol-9'-O-β-D-xylopyranoside (4), 5'-methoxyisolariciresinol-9'-O-β-D-xylopyranoside (5), lyoniresinol-9'-O-β-D-xylopyranoside (6), (E) -4-hydroxyphenylprop-7-ene 4-O-β-D-glucopyranoside (7), (E) - 4-hydroxy-3-methoxyphenylprop-7-ene 4-O-α-L-rhamnopyranosyl-(1 --> 6) -β-D-glucopyranoside (8), 4-hydroxy-3-methoxyphenylprop-8-ene 4-O-β-D-xylopyraosyl-(1 --> 6) -β-D-glucopyranoside (9), and 4-hydroxy-3,5-dimethoxyphenylprop-8-ene 4-O-α-L-rhamnpyranosyl-(1 --> 6)-β-D- glucopyranoside (10), respectively.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Glycosides ; chemistry ; isolation & purification ; Lauraceae ; chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization

Human body is inhabited by large number of microbial organisms that form complex ecosystems. Oral cavity is one of the major sites for microbial colonization. Oral microbial diversity is huge as the compositions vary among different oral cavities, different locations within the same oral cavity, or same location at different time points. The differences in compositions and varieties determine the balance of human oral microbial ecosystem, which is directly associated with oral disease or health. This review focuses on the history and new progress of the studies on human oral microbial communities.
Ecosystem ; Humans ; Mouth ; microbiology

Twelve flavonoids were isolated from an ethanol extract of Machilus wangchiana by a combination of various chromatographic techniques including column chromatography over silica gel and Sephadex LH-20 and reversed-phase flash chromatography and HPLC. Their structures were identified by spectroscopic data analysis (IR, MS, and NMR) as (+)-catechin (1), (-)-epicatechin (2), 3'-O-methyl-(+)-catechin (3), 3'-O-methyl-(-)-epicatechin (4), 3, 5, 7, 2', 5'-pentahydroxy flavan (5), (-)-naringenin (6), (-)-eriodictyol (7), (-)-liquiritigenin (8), (2R,3R)-(+)-dihydrokaempferol (9), (2R,3S)-(-)-dihydro- kaempferol (10), (2R, 3R)-(+)-taxifolin (11), and quercetin (12). Compounds 1-10 are isolated from the genus Machilus for the first time.
Drugs, Chinese Herbal ; chemistry ; Flavonoids ; chemistry ; Lauraceae ; chemistry ; Mass Spectrometry ; Molecular Structure ; Plant Roots ; chemistry

Apoptosis ; Colonic Neoplasms ; metabolism ; pathology ; HT29 Cells ; Humans ; Insulin-Like Growth Factor Binding Proteins ; metabolism

From an ethanol extract of Euphorbia micractina roots, seven steroids fifteen aromatic derivatives were isolated by a combination of various chromatographic techniques, including column chromatography over macroporous resin, silica gel, and Sephadex LH-20 and reversed-phase HPLC. Their structures were elucidated by spectroscopic data analysis as stigamast-5-ene-3beta, 7alpha-diol(1), stigamast-5-ene-3beta,7beta-diol(2), stigmast-5-en-3beta-ol-7-one(3), stigmast-4-en-6beta-ol-3-one(4), stigmast-1, 4-dien-3-one(5), stigmast-3,6-dione(6), beta-sitosterol(7), scopoletin(8), aesculetin(9), 6-hydroxy-5,7-dimethoxycoumarin(10), quercetin(11), 3,3', 4'-tri-O-methylellagic acid(12), p-hydroxyphenylethyl anisate(13), m-hydroxyphenylethyl alcohol(14), (E)-cinnamic acid(15), (E)-ferulic acid(16), 3,4-dihydroxybenzoic acid(17), vanillic acid(18), p-hydroxybenzoic acid(19), ethyl 3,4-dihydroxybenzoate (20), ethyl gallate(21), and methyl gallate(22). These compounds were obtained from this plant for the first time.
Drugs, Chinese Herbal ; chemistry ; Euphorbia ; chemistry ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Steroids ; chemistry

Dental plaque is structurally a kind of biofilm which contains a variety of micro-organisms. The interreaction of oral micro-organisms may affect the nature, forms, and toxicity of the dental plaque biofilm, as well as the localization and field planting of bacteria inside the biofilm. The signal transduction existed between the bacterium has an important effect on the formation and virulence of bacterial biofilm. This reviewing paper focuses on the latest research progress of human oral microbial community and dental plaque biofilm.
Bacteria ; Bacterial Adhesion ; Biofilms ; Dental Plaque ; Humans