Objective To observe the therapeutic effect of herbal decoction Kugan Yin for cystic hyperplasia of breast.Methods The 131 cases of cystic hyperplasia of breast in phlegm combining qi stagnation syndrome were randomized into treatment group(68 cases)which was treated by Kugan Yin and control group(63 cases)which was treated by Rupixiao Tablets(Tablets for dissolving breast nodules).The changes of symptoms and signs,level of serum sexual hormone and molybdenum target mammography analysis of two groups were observed for comparison.Results The total effective rate of treatment group was obviously better than that of con- trol group(P

AlM:To investigate the effects of pirfenidone ( PFD) on the proliferation and transfomring growth factor-β1 ( TGF-β1 ) expression in vitro culture rat corneal stromal cells.METHODS: Corneal stromal cells from 8 to 10wk SD rats were isolated, cultured and treated with different concentrations of PFD 0mg/mL (control group), 0. 15mg/mL (experimental group▏), 0. 3mg/mL (experimental group‖), 1mg/mL (experimental group Ⅲ) for 48h. CCK-8 assay was performed to assess cell proliferation, while immunocytochemistry and Western Blot were used to detect the expression of ki-67 and TGF-β1 expression, respectively. RESULTS: Compared with control group, PFD significantly inhibited the proliferation in a dose -dependent manner ( all P < 0. 05 ), so was protein expression of ki-67. PFD significantly down-regulated the expression of TGF-β1 in a dose-dependent manner (P<0. 05).CONCLUSlON: Pirfenidone can significantly inhibit the proliferation of rat corneal stromal cell by down regulating TGF-β1 expression, therefore, it has potential prospect in lightening the corneal wound healing reaction.

N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects on acetylcholinesterase activities were tested. N-Acyl-4-phenylthiazole-2-amines were prepared from substituted 2-bromo-1-acetophenones by three steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The results showed that the target compounds had a certain inhibitory activity on AChE in vitro. Among them, 8c was the best, and IC50 of 8c was 0.51 micromol x L(-1), better than that of rivastigmine and Huperzine-A. The inhibitory activities of N-acyl-4-phenylthiazole-2-amines on acetylcholinesterase are worth while to be further studied.
Acetylcholinesterase ; metabolism ; Alkaloids ; pharmacology ; Amines ; chemical synthesis ; pharmacology ; Cholinesterase Inhibitors ; chemical synthesis ; pharmacology ; Drug Design ; Rivastigmine ; pharmacology ; Sesquiterpenes ; pharmacology ; Structure-Activity Relationship ; Thiazoles ; pharmacology

A series of novel 2-amino-4-phenylthiazole derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase were investigated. 2-Amino-4-phenylthiazoles were prepared from alpha-bromoacetophenones by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 8a was the best of them. The IC50 of 8a to AChE is 3.54 micromol x L(-1), and the value was better than that of rivastigmine. 2-Amino-4-phenylthiazole derivatives showed a certain bioactivity in vitro, which were worth further investigation.
Acetylcholinesterase ; metabolism ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Drug Design ; Inhibitory Concentration 50 ; Molecular Structure ; Thiazoles ; chemical synthesis ; chemistry ; pharmacology

[Summary] To investigate the correlation of serum alanine aminotransferase (ALT) level with impaired fasting glucose (IFG) and evaluate the modification effects of body mass index in Chinese adults.The study samples were from a community-based health examination survey in Xuzhou,Jiangsu province of China.A total of 32 433 subjects with biomarkers available were included in the present study.Serum ALT,triglyceride,total cholesterol,high density lipoprotein-cholesterol,low density lipoprotein-cholesterol,and glucose levels were measured.IFG was defined as from 6.1 mmol/L to 7.0 mmol/L.Results are expressed as x±s.The correlation between serum ALT and impaired fasting glucose was assessed using logistic correlation.The correlation of serum ALT and IFG in the group of fasting blood glucose was segnificantly (r=0.07,P＜0.01),while the correlation with the normal blood glucose group fasting blood glucose is weak (r=0.001,P＞0.05).After adjusted for age,sex,and body mass index,there was a strong correlation between the fasting blood glucose (r =0.04,P＜0.01) in ALT and IFG group.After further adjustment for serum lipids,blood pressure,this correlation still exists (r =0.03,P＜0.01).Body mass index influences correlation of ALT and IFG.The present data indicate that the serum ALT is related to the risk of IFG in Chinese adults,and body mass index level may affect the relationship.

A series of novel N-acyl-thiochromenothiazol-2-amine derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase was investigated. N-Acyl-thiochromenothiazol-2-amines were prepared from thiophenol by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 10a was the best in them. The IC50 of 10a to AChE is 7.92 μmol x L(-1), and the value is better than that of rivastigmine. N-Acyl-thiochromenothiazol-2-amine derivatives showed a certain bioactivity in vitro, which were worth further investigation.
Acetylcholinesterase ; metabolism ; Amines ; chemical synthesis ; pharmacology ; Benzopyrans ; chemical synthesis ; pharmacology ; Cholinesterase Inhibitors ; chemical synthesis ; pharmacology ; Rivastigmine ; Structure-Activity Relationship ; Thiazoles ; chemical synthesis ; pharmacology

OBJECTIVETo investigate the effect of ursolic acid (UA) on the alloxan-induced myocardial fibrosis in mice and discuss the possible mechanism.

METHODSDiabetes was produced by a single injection of alloxan (70 mg/kg, i.v.) in mice. The mice were randomly divided into four groups: normal control group, model group, ursolic acid group (UA, 35 mg/kg, p.o.) and benazepril group (5 mg/kg, p. o.), and continuous administrated for 8 weeks. The blood glucose was measured 24 hours after the last administration. Detected the specific biochemical of myocardial tissue: superoxide dismutase (SOD), malondialdehyde (MDA) and hydroxyproline(HYP). Using masson staining to observe the morphology of the myocardial tissue. Immunohistochemistry was employed to determine the protein levels of TGF-beta1.

RESULTSCompared to normal group, the blood glucose, heart index, myocardial tissue MDA, HYP level were increased, and SOD activities were decreased in the diabetic mice, Masson stain showed that myocardial cells disarranged, myocardial collagen fibrosis hyperplasia. Meanwhile, the protein expression of TGF-beta1 was increased in model group. The UA group improved all the above significantly.

CONCLUSIONUA improves the myocardial collagen fibrosis in diabetic mice induced by alloxan, its mechanism may be related to inhibiting the expression of TGF-beta1 and antioxidation.

Animals ; Blood Glucose ; Collagen ; metabolism ; Diabetes Mellitus, Experimental ; metabolism ; pathology ; Fibrosis ; Hydroxyproline ; metabolism ; Male ; Malondialdehyde ; metabolism ; Mice ; Mice, Inbred Strains ; Myocardium ; metabolism ; pathology ; Oxidative Stress ; Superoxide Dismutase ; metabolism ; Transforming Growth Factor beta1 ; metabolism ; Triterpenes ; pharmacology

Colectomy ; Colorectal Neoplasms/surgery* ; Humans ; Laparoscopy ; Treatment Outcome

OBJECTIVETo evaluate the correlation of the single nucleotide polymorphisms (SNPs) of the CYP1A2 gene with the stages and grades of prostate cancer (PCa).

METHODSWe conducted gene sequencing of the rs2069514-3859 (A > G) and rs2069525-1707 (C >T) alleles in the CYP1A2 gene in 253 patients with benign prostatic hyperplasia (BPH) and 206 patients with PCa treated by castration therapy, and statistically analyzed their correlations with the genotypes, stages and grades of prostate cancer.

RESULTSThe incidences of the 2 CYP1A2 SNPs showed no significant difference between the BPH and the castrated PCa patients (P > 0.05), and their genotypes were not correlated with the stages of PCa (P > 0.05). The Gleason scores were mostly <7 in the PCa patients with genotypes containing C in the rs2069525-1707 (C > T) allele (P = 0.030, OR = 4.658, 95% CI: 1.222 - 17.754).

CONCLUSIONSNPs of the CYP1A2 gene may have some correlations with the pathologic stages of PCa, but their mechanisms and clinical significance need to be further confirmed.

Aged ; Aged, 80 and over ; Cytochrome P-450 CYP1A2 ; genetics ; Genotype ; Humans ; Male ; Middle Aged ; Polymorphism, Single Nucleotide ; Prostatic Neoplasms ; genetics ; pathology

OBJECTIVETo study the chemical constitutes of Acantophora spicifera.

METHODCompounds were isolated by normal phase silica gel and Sephadex LH-20 gel column chromatography, and reverse-phase HPLC, as well as recrystallization. Their structures were elucidated by spectroscopic methods.

RESULTSeven compounds were isolated from A. spicifera and their structures were identified as aplysin (1), loloilide (2), (R)-(-)-dehydrovomifoliol (3), uracil (4), thymine (5), 1-methoxy-4-(1-propenyl) benzene (6).

CONCLUSIONThe compounds were obtained from this genus for the first time. Compound 6 was firstly obtained from marine organisms.

Chromatography ; methods ; Chromatography, High Pressure Liquid ; methods ; Rhodophyta ; chemistry ; isolation & purification ; Sesquiterpenes ; chemistry ; isolation & purification ; Styrenes ; chemistry ; isolation & purification ; Thymine ; chemistry ; isolation & purification ; Uracil ; chemistry ; isolation & purification