AIM To study the protective effects of Jingqi Capsules (Cordycps Militaris,Rehmanniae Radix Praeparata,Lycii Fructus,) on the damage to rat reproductive system induced by cyclophosphamide.METHODS After low and high dose groups of Jingqi Capsules and positive group were administered for two weeks in advance,cyclophosphamide [25 mg/(kg · d)] modeling was conducted consecutively by intraperitoneal injection for five days except the normal group,while the treatment groups were administered consecutively.All the rats were executed the day after the end of the modeling.Serum testosterone content was measured by radioimmunoassay;body weight,testis,epididymis and prostate of rats were weighed and organ coefficient was calculated;morphology of testis was observed by HE;sperm count and sperm motility were detected by CASA;apoptosis of cells was observed by TUNEL.RESULTS Compared with the model group,each dose group of Jingqi Capsules increased in the level of serum testosterone and organ coefficient of testis,epididymis and prostate.The damage to seminiferous epithelium relieved and the number of all spermatogenic cells increased.Sperm count and sperm motility increased.Decrease in apoptosis of cells was demonstrated by TUNEL.CONCLUSION Jingqi Capsules has protective effects on damage to rat reproductive system induced by cyclophosphamide.

OBJECTIVETo study the molecular mechanism of Yangjing Zhongyu Decoction (YZD) n-butanol extracts (ZDC) and ethyl acetate extracts (YSYZ) in reducing androgen in porcine granulose cells by mitogen-activated protein kinase (MAPK) pathway.

METHODSPorcine granulose cells were isolated and cultured. They were inoculated by MAPK inhibitor PD98059 at different concentrations, and then they were divided into the blank control group (0), 1, 3, 10, and 25 micromol/L groups. After 24-h culture the cytochrome P450c17a (CYP17) mRNA expression level was detected using Real-time fluorescent quantitative PCR. Contents of androgen (testosterone) in the supernate were detected using RIA and optimal PD98059 concentration screened. After intervened by 10 micromol/L PD98059 for 24 h, the culture solution was intervened by effective ingredients of with or without YZD or YSYZ at various concentrations (0, 1 , 5, 25, 50 mg/mL) at various time points (3, 6, 18, 24 h). Expression levels of p-ERK1/2, c-Fos and CYP17 were detected by Western blot. Testosterone content in the supernate was determined by radioimmunoassay (RIA).

RESULTSTen pLmol/L PD98059 could obviously decrease p-ERK1/2 protein expression and increase CYP17 mRMA expression, and elevate testosterone content in the supernate (P < 0.05). ZDC and YSYZ at 25 ng/mL could increase p-ERK1/2 protein expression and c-Fos levels, and reduce CYP17 protein expression, and lower testosterone content in the supernate after 6-h intervention (P < 0.01).

CONCLUSIONEffective ingredients of YZD could reduce androgen production in porcine granulose cells through increasing activities of MAPK.

Androgens ; Animals ; Drugs, Chinese Herbal ; pharmacology ; Female ; Flavonoids ; Granulosa Cells ; metabolism ; Mitogen-Activated Protein Kinase 3 ; metabolism ; Mitogen-Activated Protein Kinases ; metabolism ; RNA, Messenger ; Swine

OBJECTIVETo compare the intervention effects of four traditional Chinese medicines (TCMs) with typical cold or hot property on body temperature and temperature-sensitive transient receptor potential ion channel proteins (TRPs) of rats with yeast-induced fever.

METHODThe pyrexia model was induced by injecting yeast suspension subcutaneously. Totally 108 male SD rats were randomly divided into the normal group, the model group, the Rhei Radix et Rhizoma treated group, the Coptidis Rhizoma treated group, the Euodiae Fructus treated group, and the Alpiniae Officinarum Rhizoma treated group, with 18 rats in each group. At the 4 h, 8 h and 12 h after injection of yeast, the rats were sacrificed to collect their hypothalamus and dorsal root ganglion. The expressions of TRPV1 and TRPM8 were detected by immunohistochemistry and Western blot method.

RESULTCompared with the normal group, after injection of yeast, the temperature of rats in the model group notably increased, and reached the peak at 8 h (P < 0.01). The TRPV1 level in hypothalamus and dorsal root ganglia (DRG) of the model group significantly increased, whereas the TRPM8 level significantly reduced. Compared with the model group, the Rhei Radix et Rhizoma group and the Coptidis Rhizoma group showed significant decrease in the high body temperature of rats caused by yeast, down-regulation in the expression of TRPV1, and up-regulation in the expression of TRPM8 (P < 0.05 or P < 0.01). Euodiae Fructus and Alpiniae Officinarum Rhizoma had no significant effect on either temperature or TRPs of fever rats.

CONCLUSIONRhei Radix et Rhizoma and Coptidis Rhizoma, both are TCMs with cold property, can reduce the temperature of fever rats induced by yeast, which may be related to their effective regulation of TRPV1 and TRPM8 in hypothalamus and DRG, while Euodiae Fructus and Alpiniae Officinarum Rhizoma had no relevant effect.

Animals ; Antipyretics ; administration & dosage ; chemistry ; Body Temperature Regulation ; drug effects ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Fever ; drug therapy ; immunology ; microbiology ; physiopathology ; Gene Expression Regulation ; drug effects ; Humans ; Male ; Rats ; Rats, Sprague-Dawley ; Saccharomyces cerevisiae ; immunology ; TRPM Cation Channels ; genetics ; immunology ; TRPV Cation Channels ; genetics ; immunology

OBJECTIVE Nanotechnology provides a novel strategy for the delivery of anticancer drugs. In this study, titanium dioxide coated gold nanorod (GNR/TiO2) nanostructures were used as the drug carrier for gambogic acid in order to improve its anticancer effect. METHODS Biocompatibility and cellular uptake of GNR/TiO2 nanostructures were studied in human glioblastoma U-87 MG cells. Cell viability was evaluated by ATP assay and calcein AM staining. LysoSensor Green DND-189 and Hoechst 33342 were used to analyze the intracellular location of GNR/TiO2 nanostructures. The in vitro anti-cancer effect of gambogic acid loaded nanoparticles was compared with free drug. RESULTS The results showed that GNR/TiO2 nanostructures are biocompatible, and they are localized at the intracel?lular acidic compartments of endosomes and lysosomes. The intracellular drug content delivered via GNR/TiO2 nanostructures was 6 fold higher than the free form, thus dramatically enhancing the anticancer effect of gambogic acid. Furthermore, mild photothermal therapy also showed synergistic effect with the drug. CONCLUSION Our study suggested that GNR/TiO2 nanostructures can be considered as a promising anticancer drug carrier.

Diabetic rats were induced by intraperitoneal injection of streptozotocin.TUNEL and immunohistochemistry results showed that the renal tubular cell apoptosis index(AI)and Bax protein expression were significantly reduced,and the Bcl-2 protein expression in glomeruli was significantly increased in diabetic rats with stable hyperglycemia treated by benazepril compared with diabetic rats with stable hyperglycemia treated by vehicle(all P

OBJECTIVETo explore the impacts on the life quality and the effect mechanism in the patients of allergic rhinitis (AR) treated with warm acupuncture in winter and summer.

METHODSTwo hundred and forty patients of AR were randomized into a summer and winter acupuncture group, a non-summer and winter acupuncture group and a western medication group, 80 cases in each one. In the two acupuncture groups, Dazhui (GV 14), Fengmen (BL 12), Feishu (BL 13), Pishu (BL 20) and Shenshu (BL 23) were selected. In the summer and winter acupuncture group, the warm acupuncture started at the first day of the three periods of hot season and the first day of the third nine-day period after the winter solstice. The treatment was given once every two days, continuously for 15 times. Totally, 30 treatments were required a year. In the non-summer and winter acupuncture group, the warm acupuncture was applied out of the three periods of the hot season and the third nine-day period after the winter solstice. The treatment was given once every two days and 30 treatments for a year. In the western medication group, cetirizine was taken orally, continuously for 30 days as one session. In the three groups, the treatment for 1 year was taken as one session. The second session started in the next year. Totally, 2 sessions were required. The score of rhinoconjunctivitis quality of life questionnaire (RQLQ) and the level of serum immunoglobulin E (IgE) were compared in the patients' of each group before treatment and in 1 and 2 sessions of treatment.

RESULTSAfter treatment, the scores of 7 domains, named activities, common complaints, practical problems, sleep, ocular symptoms, nasal symptoms and emotions were all improved as compared with those before treatment, in the patients of the three groups (all P < 0.05). After 2 sessions treatment, the results in the summer and winter acupuncture group were better than those in the other two groups (all P < 0.05), and the results in the non-summer and winter acupuncture group were better than those in the western medication group (all P < 0.05). After treatment, serum IgE level was lower averagely than that before treatment in the three groups (all P < 0.05). After 2 sessions treatment, the result in the summer and winter acupuncture group was lower than that in the other two groups (both P < 0.05), and the result in the non-summer and winter acupuncture group was lower than that in the western medication group (P < 0.05). After treatment, the total effective rate was 92.3% (72/78) in the summer and winter acupuncture group, better than 80.5% (62/77) in the non-summer and winter acupuncture group and 69.7% (53/76) in the western medication group (both P < 0.05).

CONCLUSIONThe warm acupuncture in both summer and winter achieves the definite efficacy on AR and the effect mechanism is relevant with reducing serum IgE level.

Acupuncture Points ; Acupuncture Therapy ; instrumentation ; methods ; Adolescent ; Adult ; Female ; Humans ; Male ; Middle Aged ; Quality of Life ; Rhinitis, Allergic ; therapy ; Seasons ; Treatment Outcome ; Young Adult

Many drug candidates identified from natural products are poorly water-soluble. The surfactants used to disperse the hydrophobic anticancer drugs in water may cause a serious of acute hypersensitivity reactions. Nanotech?nology provides an alternative strategy for delivery of anticancer drugs. Drugs can be encapsulated or attached to the nanomaterials such as lipids, polymers and solid-core nanoparticles. In the present study, porous inorganic nanoparti?cles have been utilized for delivery of water-insoluble anticancer drugs. The synthesized nanoparticles were functional?ized with different organic polymers. The porous nanoparticles were readily internalized by human glioblastoma U-87 MG cells, and didn't display cytotoxicity. The internalized nanoparticles were mainly localized in endosomes/lysosomes in cells. With the hydrophobic curcumin and carfilzomib as model drugs, intracellular delivery of hydrophobic anticancer drugs by the porous inorganic nanoparticles was studied. The porous nanoparticle-based encapsulation of hydrophobic drug provides the aqueous dispersion of the drugs. In endosomes/lysosomes mimicking buffers with a pH of 4.5-5.5, pH-dependent drug release was observed from drug loaded nanoparticles. The intracellular drug content and cytotoxicity were significantly higher for drug loaded nanoparticles than free drug. These results suggested porous inorganic nanoparticles might be a promising intracellular carrier for hydrophobic anticancer drugs.

PURPOSE: Ventricular repolarization is assessed using the QT interval corrected by the heart rate (QTc) via an electrocardiogram (ECG). Prolonged QTc is associated with an increased risk of arrhythmias and cardiac mortality. As there have been few reports regarding the effects of hyperthyroidism on ventricular repolarization, we studied the association between serum free thyroxine (free T4 [fT4]) and thyroid stimulating hormone (TSH) levels and the QTc interval. METHODS: Thirty-eight patients with hyperthyroidism (<30 years old) were included, and we used their clinical records and available ECGs (between August 2003 and August 2011) to evaluate the association between their fT4 and TSH levels and their QTc interval. In addition, we studied the ECGs of 72 age-matched patients with no hyperthyroidism (control group) and compared their data with that from the patients group. RESULTS: The QTc duration in patients with hyperthyroidism was significantly prolonged compared to that in the control subjects (P<0.001). In addition, the number of hyperthyroid patients with abnormal prolonged QTc was significantly higher than that in the control group (P<0.001). Among the patients with hyperthyroidism, patients with prolonged QTc and borderline QTc had higher fT4 levels and there was positive correlation between their fT4 levels and their QTc interval (P<0.05). However, no correlation was observed between their TSH levels and their QTc interval. CONCLUSION: We report that hyperthyroidism is associated with QTc prolongation. The correlation between the fT4 levels and the QTc interval suggests that thyroid status is associated with QTc values and the risk of cardiac mortality.
Arrhythmias, Cardiac ; Electrocardiography ; Heart Rate ; Humans ; Hyperthyroidism* ; Long QT Syndrome ; Mortality ; Thyroid Gland* ; Thyrotropin ; Thyroxine

OBJECTIVETo investigate the effect of interleukin-2 (IL-2) on myocardial impairment during ischemia/reperfusion or anoxia/reoxygenation.

METHODSChemical anoxia was introduced in the isolated rat ventricular myocytes by Krebs-Henseleit (K-H) solution containing 10(-3) mol/L sodium dithionite. The video-tracking system and spectrofluorometric method were employed to verify the cell contraction and calcium homeostasis of the single myocyte. Radioimmunoassay was used to analyze the IL-2 levels in myocardium.

RESULTSThe levels of IL-2 in myocardium subjected to ischemia/reperfusion were elevated [(14.34+/-5.99 compared with 22.25+/-3.68)ng/g, P<0.01]. During anoxia, cell contraction and the amplitude of electrically induced calcium transient were depressed and the parameters did not return to the pre-anoxia level during reoxygenation. IL-2 at 200 U/L administered during anoxia aggravated the effect of reoxygenation on cell contraction and calcium transient. After perfusion with IL-2, the malondialdehyde content of myocardial mitochondria was elevated.

CONCLUSIONCoexistence of IL-2 during anoxia aggravates the effect of reoxygenation on the cell contraction and calcium homeostasis in the isolated rat ventricular myocytes, in which the mitochondrial lipid peroxidation induced by IL-2 is involved.

Animals ; Calcium ; metabolism ; Interleukin-2 ; physiology ; Lipid Peroxidation ; Male ; Malondialdehyde ; blood ; Mitochondria, Heart ; metabolism ; Myocardial Ischemia ; physiopathology ; Myocardial Reperfusion Injury ; physiopathology ; Rats ; Rats, Sprague-Dawley

AIMTo prepare the compound danshen pH-dependent delayed release pellets and filled them in capsules and then study thier pharmacodynamics.

METHODSThe pH-dependent delayed release pellets were prepared by coating with HPMC, Eudragit L-30D-55 and Eudragit L100-Eudragit S100 (1:6), separately, and mixed in proper proportion to prepare the two pH-dependent delayed release systems T1 and T2. The release of delayed release pellets was determined according to the method of China Pharmacopoeia (2000) in the simulated gastrointestinal pH conditions. The pharmacodynamic,parameters were evaluated by serum pharmacology method.

RESULTSThe compound danshen pH-dependent delayed release pellets were prepared with the characteristics of pH dependent delayed release profile in vitro. In single oral dose, the pharmacodynamic parameters of rapid release tablets R Emax (%) and Tmax (h) were 34.63% and 0.58 h, respectively. Tmax S of delayed-release pellets T1 and T2 were extended to 2.42, 3.17 h and Emax S (%) were declined to 13.57%, 14.52%. The relative bioavailabilities of T1 and T2 were 99.3%, 133.6% , respectively. In multiple oral doses of R the pharmacodynamic parameter of DF was 7.32 and those T1, T2 DF were 3.40, 3.03, respectively.

CONCLUSIONThe compound danshen pH-dependent delayed release capsules have characteristics of pH dependent releasing in vitro and characteristics of delayed release in vivo. In multiple oral (loses the DF of delayed release capsules was lower than that of rapid release tablet at steady state.

Animals ; Area Under Curve ; Biological Availability ; Codonopsis ; chemistry ; Delayed-Action Preparations ; Dogs ; Dose-Response Relationship, Drug ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; pharmacology ; Female ; Guinea Pigs ; Hydrogen-Ion Concentration ; Hypromellose Derivatives ; Male ; Methylcellulose ; analogs & derivatives ; Plants, Medicinal ; chemistry ; Polymethacrylic Acids ; Random Allocation