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

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

Panax ginseng is the king of herbs and plays important roles in the traditional Chinese medicine industry. In this paper, we summarized the development of ginseng cultivation in China and other main countries, analyzed the effects of ecological factors of soil and climate on ginseng distribution, and investigated the characteristic of main cultivation patterns (conversion of forest to cultivate ginseng soils, cultivated ginseng in the farmland and wild nursery). Aimed at the serious issues in the cultivation, research strategies have been provided to guarantee the sustainable development of the ginseng industry. The patterns of cultivated ginseng in the farmland should be strive to develop; pollution-free cultivation and studies of continuous cropping obstacles should be carried out; ginseng varieties suited to ecological environment of farmland should be bred using modern biotechnology.
Agriculture ; methods ; China ; Climate ; Ecosystem ; Panax ; chemistry ; growth & development ; Soil ; chemistry

OBJECTIVETo explore the operation methods and clinical effects of transfer of the medial half of the coracoacromial ligament to reconstruct the coracoclavicular ligament in treating complete acromioclavicular joint dislocation.

METHODSFrom January 2006 to June 2012,26 patients with acute complete acromioclavicular joint dislocation underwent surgery. Transfer of the medial half of the coracoacromial ligament to reconstruct the coracoclavicular ligament, additional clavical hoot plate and Kirschner wires fixation, were performed in all the patients. Among the patients, 18 patients were male and 8 patients were female, with an average age of 36.7 years old (ranged from 25 to 51 years). The duration from injury to operation was from 3 to 12 days with an average of 5 days. According to the Rockwood classification, 4 cases were grade III and 22 cases were grade V . Clinical manifestation included local swelling, tenderness with snapping, limitation of shoulder joint motion. In preoperative bilateral shoulder joint X-rays, the injured coracoclavicular distance was (16.2 ± 5.0) mm which was significantly wider than that of uninjured sides (7.6 ± 1.0) mm. Clinical results were evaluated according to X-rays and Constant-Murley score.

RESULTSAll incisions obtained primary healing after operation without complication of infection, internal fixation breakage, redislocation. All the patients were followed up from 12 to 30 months with an average of 18 months. Kirschner wires and internal fixation plate were removed at 1 month and 8-10 months after operation, respectively. At final follow-up, the motion of shoulder joint recovered to normal and a no pain joint was obtained. According to Constant-Murley score, 24 cases got excellent results and 2 cases good. There was no significant difference after operation between the injured coracoclavicular distance and the uninjured contralateral side [(7.7 ± 1.2) mm vs (7.6 ± 1.0) mm), P > 0.05].

CONCLUSIONTransfer of the medial half of the coracoacromial ligament to reconstruct the coracoclavicular ligament, additional fixation using hook plate and Kirschner wires is the effective surgical method in treating complete acute acromioclavicular joint dislocation.

Acromioclavicular Joint ; injuries ; Adult ; Female ; Humans ; Joint Dislocations ; surgery ; Ligaments, Articular ; surgery ; Male ; Middle Aged ; Reconstructive Surgical Procedures ; methods

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

This study is to investigate the sedative and hypnotic effects of a novel compound H1208. The sedative activity of H1208 was investigated by recording the spontaneous locomotor activity of mice. The hypnotic property was evaluated by the latency and duration of sleep (loss of righting reflex) in mice and the effect of hypnotics on sleep pattern of electroencephalogram were studied in conscious, freely moving mice with chronically implanted electrodes. The brain monoamine neurotransmitters levels in mice were measured by high performance liquid chromatography-electrochemical detection. The spontaneous locomotor activity was decreased by 56.7% and 80.2% in H1208 (5 and 25 mg x kg(-1), ip) treated mice, respectively. The loss of righting reflex was directly induced in mice after H1208 (60 mg x kg(-1), ip) administration. The non-rapid eye movement sleep increased significantly by 131% and 259%, respectively, within 3 hours after H1208 (30 and 60 mg x kg(-1), ip) administration. However, the rapid eye movement sleep decreased significantly. The contents of DA in the striatum and cortex and 5-HT in the cortex decreased significantly. These results demonstrated that H1208 has potent sedative and hypnotic effects, which may be closely related to the decreased contents of DA and 5-HT in mouse brain.
Animals ; Brain ; drug effects ; physiology ; Dopamine ; metabolism ; Electroencephalography ; Hypnotics and Sedatives ; pharmacology ; Mice ; Motor Activity ; drug effects ; Serotonin ; metabolism ; Sleep ; drug effects

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