Objective: To investigate the lignans compounds constituents of Lavandula angustifolia. Methods: The chemical constituents were isolated and purified by TLC, silica gel, MCI-gel, and RP-HPLC, and their structures were identified by analysis of spectroscopic evidences and physicochemical properties. Results: A total of 11 constituents were isolated from L. angustifolia and elucidated as pinoresinol (1), syringaresinol (2), fraxiresinol-4'-O-β-D-glucopyranoside (3), syringaresinol-4'-O-β-D-glucopyranoside (4), 8-hydroxypinoresinol-4-O-β-D-glucopyranoside (5), rel-(2α,3β)-7-O-methylcedrusin (6), lariciresinol-4'-O-β-D-glucoside (7), (2S,3R)-2,3-dihydro-2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxybenzofuran-5-(trans) propen-1-ol-3-O-β-glucoside (8), (7S,8R)-dihydrodehydrodiconiferyl alcohol-9-β-D-glucopyranoside (9), (7R,8R)-7,8-dihydro-9'-hydroxyl-3'-methoxyl-8- hydroxymethyl-7-(4-hydroxy-3-methoxyphenyl)-1'-benzofuranpropanol-9'-O-β-D-glucopyranoside (10), and (E)-3-((2S,3S)-2-(4- hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-2,3-dihydrobenzofuran-5-yl) allyl-2-hydroxyacetate (11). Conclusion: The 11 compounds are isolated from this plant for first time.

AIMTo explore the causes of the difference in spermatogenic suppression between responders and non-responders in Chinese men treated with levonorgestrel (LNG) implants plus testosterone undecanoate (TU) injectable.

METHODSThe 16 Chinese volunteers treated were divided into two groups in regard to the sperm count during the treatment period, 7 men in the responder group (Group R), including 6 azoospermia and one severe oligozoospermia, and the remaining 9 in the non-responder group (Group N), including 4 oligozoospermia and 5 with sperm counts greater than 20 x 10(6)/mL. The differences in serum profiles of FSH, LH, T, LNG and T/LH ratio were compared between the two groups and the correlation between the seminal fluid parameters and serum reproductive hormones was analyzed.

RESULTSThe serum FSH level was lower in Group R than that in Group N (P<0.05), while the serum LH and LNG levels were higher in Group R than those in Group N (P<0.05). The sperm density (P<0.01, r=0.235), motility(P<0.01, r=0.326) and vitality (P<0.01, r=0.219) showed significantly positive correlation with the serum FSH level.

CONCLUSIONThe blood LNG and T levels, the degree of FSH inhibition and/or the sensitivity of the pituitary-testis axis to exogenous steroids, as well as the individual spermatogenetic potential and the functional status of the Leydig cells may be factors bringing about individual differences in spermatogenic suppression in Chinese men treated with LNG and TU.

Adult ; Contraceptive Agents, Male ; administration & dosage ; Drug Implants ; Follicle Stimulating Hormone ; blood ; Humans ; Injections ; Levonorgestrel ; administration & dosage ; pharmacokinetics ; Leydig Cells ; physiology ; Luteinizing Hormone ; blood ; Male ; Sperm Count ; Spermatogenesis ; drug effects ; Testosterone ; administration & dosage ; analogs & derivatives ; blood

Aged ; Coal Mining ; Electrocardiography ; Heart Rate ; Humans ; Male ; Middle Aged ; Pneumoconiosis ; complications ; physiopathology ; Tachycardia ; etiology

Objective Color doppler ultrasonography of chronic Keshan disease (CKD) was evaluated to provide evidences for clinic diagnosis of the disease. Methods From September to Novermber 2009, according to "Diagnostic criteria of Keshan disease" (GB 17021-1997), 64 cases of CKD were randomly sampled from five Keshan diseased districts in Shandong province, Zoucheng, Sishui, Yishui, Wulian, Jvxian, and Pingyi as patient group. Thirty four healthy volunteers being checked up by Shandong Institute for Endemic Diseases Control and Research were put in control group. All the subjects were examined with Color doppler ultrasonography. The indexes of cardiac structure, left ventricular (LV) systolic function and LV diastolic function were measured.Results Left atrial internal diameter, LV end-diastolic internal diameter, LV end-systolic internal diameter, right ventricular diameter, aorta diameter, right atrial transverse diameter, right atrial long diameter and left ventricle mass of the patient group[(35.38 ± 6.89), (61.57 ± 8.61), (45.39 ± 10.29), (17.22 ± 3.79), (28.69 ± 2.81),(38.00 ± 6.05), (42.68 ± 8.65)mm, (283.22 ± 103.12)g] were higher than that of control group[(26.70 ± 3.27),(45.41 ± 4.93), (26.91 ± 4.35), (13.76 ± 2.27), (24.09 ± 2.89), (31.50 ± 3.32), (35.82 ± 3.14) mm, (156.03 ±39.86)g, t = 6.93, 10.09, 9.98, 4.87, 7.64, 5.81, 4.46, 6.90, all P＜ 0.05]. The LV ejection fraction and fractional shortening of the left ventricular of the patient group[(49.25 ± 14.33)%, (26.11 ± 9.17)%] were lower than that of control group[(73.88 ± 4.04)%, (42.88 ± 3.62)%, t = - 9.79, - 10.22, all P＜ 0.05]. Diffuse hypokinetic motion of the left ventricle reduced in 95% (61/64) of CKD patients, and 5% (3/64) of CKD patients had segmental LV dyskinesia. Seventy five per sent(48/64) of the patients accompanied with mitral regurgitation, and 39% (26/64) of these cases accompanied with tricuspid regurgitation. Meaningful Mitral or tricuspid regurgitation was not found out in control group. Conclusions The CKD patients' bore of atrio-ventricular cavity and LV mass are enlarged, and their motion of ventricle is reduced or partly reduced. They have poor heart function. Mitral regurgitation are more than tricuspid regurgitation. Color doppler Ultrasonography is important in diagnosis of chronic Keshan discase.

Adult ; Diagnostic Errors ; Female ; Humans ; Laryngitis ; diagnosis ; microbiology ; Male ; Middle Aged ; Mycoses ; diagnosis ; Pharyngitis ; diagnosis ; microbiology

Objective: To identificate the bioactive natural products, and study the chemical constituents in the flower buds of Rosa rugosa. Methods: The chemical constituents in the flower buds of R. rugosa were isolated by silica gel, MCI-gel resin, Sephadex LH-20 column chromatography, and high performance liquid chromatography (HPLC) methods. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Results: Nine flavonoids were isolated from the flower buds of R. rugosa, and identified as 8-acetyl-4',7-dimethoxy-6-methyl-flavone (1), kaempferol (2), kaempferol-3-O-β-D-glucopyranoside (3), kaempferol-3-O-β-D-rutinside (4), quercetin (5), quercetin-3-O-β-D-glucopyranoside (6), rutin (7), luteolin (8), and luteolin-7-O-β-D-glucopyranoside (9). Conclusion: Compound 1 is a new compound and it displays the cytotoxicity against NB4, SH-SY5Y, PC3, A549, and MCF7 cells with IC50 values of 6.8, 5.6, 2.2, 1.8, and 7.4 μmol/L, respectively. Compound 9 is isolated from R. rugosa for the first time.

OBJECTIVE: To explore the protective effect of amlodipine on the cytotoxicity induced by contrast media (meglumine diatrizoate) in human kidney cells (HKC). METHODS: An HKC line was used. The experiment was divided into 4 groups: a model group (diatrizoate 111g/L), a prevention group (diatrizoate 111g/L+amlodipine 10(-5)mol/L), an amlodipine control group (amlodipine 10(-5)mol/L), and a culture medium control group (simple none blood serum DMEM-F12 medium). Cytotoxicity induced by meglumine diatrizoate was analysed by methyl thiazolyl tetrazolium (MTT) test, lactate dehydrogenase (LDH) assay, Hochest33258 fluorescence stained cytospins, and flow cytometric DNA analysis. The protein expression of Bax was determined by Western blot, and caspase-3 activity was examined by fluorometric method. RESULTS: In the prevention group, the cell viability increased significantly (P<0.05), LDH levels decreased (P<0.05), and the apoptosis was lower than that of the model group (P<0.05) .Bax protein expression and caspase 3 activity decreased (P<0.05). CONCLUSION Amlodipine can inhibit the HKC apoptosis and protect the renal tubule cell from injury induced by meglumine diatrizoate.
Amlodipine ; pharmacology ; Apoptosis ; drug effects ; Caspase 3 ; metabolism ; Cell Line ; Contrast Media ; toxicity ; Diatrizoate Meglumine ; toxicity ; Epithelial Cells ; cytology ; drug effects ; Humans ; Kidney Tubules ; cytology ; drug effects ; Protective Agents ; pharmacology

This study aims to investigate the effects of fibroblast growth factor 21 (FGF-21) on learning and memory abilities and antioxidant capacity of D-galactose-induced aging mice. Kunming mice (37.1 +/- 0.62) g were randomly divided into normal control group, model group and FGF-21 high, medium and low dose groups (n = 8). Each group was injected in cervical part subcutaneously with D-galactose 180 mg x kg(-1) x d(-1) once a day for 8 weeks. At the same time, FGF-21-treated mice were administered with FGF-21 by giving subcutaneous injection in cervical part at the daily doses of 5, 2 and 1 mg x kg(-1) x d(-1). The normal control group was given with normal saline by subcutaneous injection in cervical part. At seventh week of the experiment, the learning and memory abilities of mice were determined by water maze and jumping stand tests. At the end of the experiment, the mice were sacrificed and the cells damage of hippocampus was observed by HE staining in each group. Reactive oxygen species (ROS), malondialdehyde (MDA), superoxide dismutase (SOD), glutathione peroxidase (GPx), catalase (CAT) and total antioxidant capacity (T-AOC) in the brain of mice were determined. The results showed that different doses of FGF-21 could reduce the time reaching the end (P < 0.01 or P < 0.05) and the number of touching blind side (P < 0.01 or P < 0.05) in the water maze comparing with the model group. It could also prolong the latency time (P < 0.05) and decrease the number of errors (P < 0.01 or P < 0.05) in the step down test. The result of HE staining showed that FGF-21 could significantly reduce brain cell damage in the hippocampus. The ROS and MDA levels of three different doses FGF-21 treatment group reduced significantly than that of the model group [(5.58 +/- 1.07), (7.78 +/- 1.92), (9.03 +/- 1.77) vs (12.75 +/- 2.02) pmol (DCF) x min(-1) x mg(-1), P < 0.01 or P < 0.05], [(2.92 +/- 0.71), (4.21 +/- 0.81), (4.41 +/- 0.97) vs (5.62 +/- 0.63) nmol x mg(-1) (protein), P < 0.01]. Comparing with the model group, the activities of SOD, GPx, CAT and T-AOC of the three different doses FGF-21 treatment groups were also improved in a dose-dependent manner. This study demonstrates that FGF-21 can ameliorate learning and memory abilities of D-galactose induced aging mice, improve the antioxidant abilities in brain tissue and delay brain aging. This finding provides a theoretical support for clinical application of FGF-21 as a novel therapeutics for preventing aging.
Aging ; drug effects ; Animals ; Antioxidants ; metabolism ; Brain ; drug effects ; Catalase ; metabolism ; Fibroblast Growth Factors ; pharmacology ; Galactose ; Glutathione Peroxidase ; metabolism ; Hippocampus ; drug effects ; Malondialdehyde ; metabolism ; Maze Learning ; drug effects ; Memory ; drug effects ; Mice ; Superoxide Dismutase ; metabolism

To investigate the cell-killing effect and its possible mechanism of rClone30-hDR5 in combination with TRAIL on human hepatic carcinoma (HCC) cell line, first of all, recombinant plasmid pee12.4-hDR5 was introduced into HepG2 cells by liposome transfection. After five rounds of screening by flow cytometry, HepG2 cells expressing high levels of DR5 on cell surface were isolated. The cytotoxicity of TRAIL to selected cells was higher than that of TRAIL to HepG2 cells by MTT method (P < 0.01). The result suggested that the cloned hDR5 gene had biological activity. MTT assay showed that, rClone30- hDR5 in combination with TRAIL more efficiently inhibited the tumor growth of HepG2 cells compared to rClone30-hDR5 or TRAIL in vitro. The results of Annexin V-FITC/PI staining and Quantitative Real-time PCR indicated that rClone30-hDR5 in combination with TRAIL significantly increased the mRNA levels of caspase 3 and caspase 8, and induced the apoptosis of tumor cells. HepG2 cells were infected with rClone30-hDR5 or rClone30 at MOI of 1. The expression of hDR5 on tumor surface increased significantly by rClone30-hDR5 compared to that by rClone30, which contributed to the sensitivity to TRAIL. In conclusion, rClone30-hDR5 in combination with TRAIL has potential application value in cancer treatment.
Apoptosis ; Carcinoma, Hepatocellular ; pathology ; Caspase 3 ; metabolism ; Caspase 8 ; metabolism ; Drug Synergism ; Hep G2 Cells ; Humans ; Liver Neoplasms ; pathology ; Real-Time Polymerase Chain Reaction ; Receptors, TNF-Related Apoptosis-Inducing Ligand ; pharmacology ; TNF-Related Apoptosis-Inducing Ligand ; pharmacology ; Transfection

OBJECTIVETo explore the effect of 18-β glycyrrhetinic acid (GA) on the endoplasmic reticulum of nasal epithelial cells in allergic rhinitis (AR) model rats.

METHODSTotally 96 Wistar rats were randomly divided into the blank group, the AR model group, the loratadine group, the GA group, 24 in each group. AR models were established by peritoneally injecting ovalbumin (OVA). Morphological scoring was performed. GA at 21. 6 mg/kg was intragastrically administered to rats in the GA group. Nasal mucosal tissues were taken for electron microscopic examinations at the second, fourth, sixth, and tenth week after drug intervention.

RESULTSThe overlapping score was 2.10 ± 0.45 in the blank group, 5.10 ± 0.56 in the loratadine group, 5.10 ± 0.56 in the AR model group, 5.20 ± 0.78 in the GA group, showing statistical difference when compared with the blank group (P < 0.01). Results under transmission electron microscope showed that the number of the endoplasmic reticulum increased in the AR model group, with obvious cystic dilatation, a lot of vacuole formation, and degranulation. A large number of free ribosomes could be seen in cytoplasm. With persistent allergen exposure, changes mentioned above was progressively aggravated in the endoplasmic reticulum of nasal mucosal epithelium in the AR model group. But the dilation of endoplasmic reticulum, vacuole formation, and degranulation were relieved in the GA group, and got close to those of the blank group.

CONCLUSION18-β GA could improve the expansion, vacuolization, and degranulation of the endoplasmic reticulum of nasal epithelial cells in AR model rats.

Animals ; Anti-Inflammatory Agents ; pharmacology ; therapeutic use ; Endoplasmic Reticulum ; Epithelial Cells ; drug effects ; Glycyrrhetinic Acid ; pharmacology ; therapeutic use ; Nasal Mucosa ; drug effects ; Rats ; Rats, Wistar ; Rhinitis, Allergic ; drug therapy