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

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

[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.

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 search for chemical constituents with structural diversity from Laurencia tristicha to supply for biological assay.

METHODCompounds were isolated by means of column chromatography over normal phase silica gel and Sephadex LH-20, recrystallization and HPLC. Structures were identified by spectroscopic methods including 1D NMR, IR and MS. Cytotoxicities of the purified compounds were evaluated by MTT method.

RESULTSeven compounds were isolated from L. tristicha. Their structures were elucidated as cholesterol (1), cholesta- 5-en-3beta, 7alpha-diol (2), beta-stigmasterol (3), phytol (4), zeaxanthin (5), 4 -hydroxybenzaldehyde (6), indolyl-3-carbaldehyde (7). In the cytotoxic assay compound 2 was active against human cancer cell lines HCT-8, Bel-7402, BGc-823, A549 and HELA with IC50 values of 1.90, 2.02, 1.99, 6.52 and 1.20 microg x mL(-1), respectively. Compound 4 showed cytotoxicity against HCT-8 and HELA with IC50 value of 3.51 and 2.04 microg x mL(-1), and other compounds were inactive ( IC50 > 10 microg x mL(-1)).

CONCLUSIONCompounds 1-7 were isolated from L. tristicha for the first time. In additon, compounds 2 and 4 were cytotoxic against several human cancer cell lines.

Antineoplastic Agents ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; drug effects ; Cholestenes ; chemistry ; isolation & purification ; pharmacology ; Cholesterol ; chemistry ; isolation & purification ; pharmacology ; Humans ; Inhibitory Concentration 50 ; Laurencia ; chemistry ; Phytol ; chemistry ; isolation & purification ; pharmacology

Objective To investigate the adrenal steroidogenic function in genotype-proven heterozygotes carrying mutations in CYP17A1 gene in vivo. Methods Eight patients and 14 family members from 5 families with 17-hydroxylase/17,20-lyase deficiency (17OHD) were recruited. The mutations of the CYP17A1 gene in these individuals were screened by direct sequencing of PCR products. The hormonal response to ACTH was evaluated in the 14 genotype-proven carriers and 45 age- and sex-matched normal subjects. Results Three mutations were found in 5 unrelated families. 14 carriers with CYP17A1 mutation were identified, including 7 heterozygotes with D487_F489del, 6 with Y329fs, and 1 for H373L. Compared to the normal subjects, the carriers exhibited lower basal and ACTH-stimulated cortisol levels, but higher ACTH-stimulated corticosterone level. The ratios of corticosterone to cortisol in the genotype-proven heterozygotes were higher than those of normal individuals at baseline and following ACTH-stimulation. Similarly, progesterone level and ratios of progesterone to 17-hydroxyprogesterone in the male heterozygotes were also higher than that of normal individuals before and after stimulation. No significant differences were observed in the hormone levels between two genotypes (D487_F489del vs Y329fs). Conclusions Genotype-proven carriers of 17OHD without apparent clinical symptoms exhibit decreased enzyme activity,analogous to mildly impaired adrenal 21-hydroxylase activity in the carriers of CYP21 A2 gene mutation.