To evaluate in vitro release and transdermal behaviors of Huoxue Zhitong gel, modified Franz diffusion cell methods was applied to investigate in vitro transdermal absorption of Huoxue Zhitong gel and the content of paeonolan in receptor fluid composed of PEG400%-95% ethanol-water (l:3:6)were determined by HPLC. The results were processed and different equations were fitted. The release law were in accordance with Weibull equation and the fitting equation was In[-1/(1 - Q)] = -0.790 51nt - 1.7012 (r = 0.9809). In 8 hours, cumulative release of paeonol was 85. 18% and the release rate was 2.827 µg . cm-2 h-1. Transdermal actions were consistent with zero-level model fit and the fitting equation was Q(t) = 1.7579t + 0. 7213 (r = 0.9991). In 8 hours, cumulative transdermal rate and transmission rate of paeonol was 54. 85%, 1. 820 µg . cm-2 h-1. So the Huoxue Zhitong gel had a good release and transdermal properties.
Acetophenones ; administration & dosage ; pharmacokinetics ; Administration, Cutaneous ; Animals ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Gels ; Mice ; Skin Absorption

Histiocytosis, Langerhans-Cell ; Humans

Syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid are three main bioactive ingredients in herbs of Saussurea involucrata with various pharmacological properties, while their contents are very low. In this study, the biosynthesis of syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid in the cell suspension cultures of S. involucrata were regulated by feeding carbon sources and precursors, which resulted in a great increase of the contents and yields of the above three bioactive ingredients. After 16 days of fermentation, the yields of syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid reached 339.0, 225.3, 512.7 mg x L(-1), respectively. Meanwhile, their contents increased up to 67.9, 1.9, 10.6 times of wild medicinal material, respectively. The results provided a solid basis for further studies on application of cell suspension cultures of S. involucrata for large-scale production of bioactive compounds syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid.
Cell Culture Techniques ; Cells, Cultured ; Chlorogenic Acid ; analysis ; metabolism ; Cinnamates ; analysis ; metabolism ; Glucosides ; analysis ; biosynthesis ; Phenylpropionates ; analysis ; Saussurea ; chemistry ; growth & development ; metabolism

Objective:To evaluate the anti-HIV-1 activity of two new nonnucleoside reverse transcriptase inhibitors (NNRTIs), JB25 and JB26, in combination with 3 approved drugs (AZT, EFV, SQV)in vitro.Methods:The serially diluted 10 concentrations of JB25 and JB26 were combined with 7 serially diluted AZT, EFV and SQV respectively.The combination was added to 384 cell culture plates and then cocultured with HIV-1 ⅢB infected MT-2 cells for 3 days. Finally, the HIV-1 production was determined by measuring the expression of reporter genes of TZM bl cells. The data were analyzed by MacSynergy Ⅱ software.Results:The average capacity of synergism/antagonism of JB25 with AZT, EFV and SQV was 244.45/-5.05(nmol/L)~2%, 119.58/-65.93 (nmol/L)~2% and 145.83/-0.32 (nmol/L)~2% respectively;the average capacity of synergism/antagonism of JB26 with AZT, EFV and SQV was 398.90/0(nmol/L)~2%, 103.62/-0.49(nmol/L)~2% and 138.473/-0.27 (nmol/L)~2% respectively. Conclusion:Two new NNRTIs JB25 and JB26 develop synergism when combined with 3 approved drugs, respectively. MacSynergy Ⅱ software could evaluate the anti-HIV-1 activity of drug combination.

Objective To evaluate the intervention effects of low-fluoride brick tea in the population, and to provide data for the prevention and control of the brick-tea type fluorosis. Methods Eighty-six Kazakh families with 5-12 years old children were selected and divided into two groups in the severe brick-tea type fluorosis areas of Akesai County of Gansu Province. Forty-six households were intervened by drinking low-fluoride brick tea as intervention group and another 40 households drank general brick tea as control group. The fluoride content in water, tea and urine was monitored and the total daily fluoride intake of adults and children was calculated by the fluoride content of the tea before and during intervention. The baseline prevalence of dental fluorosis was surveyed in all Kazakh school students aged 5 - 12 years before intervention, dental fluorosis prevalence were surveyed in two groups after the intervention. The fluoride content in water, urine,tea, and brick-tea samples was detected by iron electrode method, and dental fluorosis was diagnosed by Dean's method. Results The fluoride content of water were 0.36,0.50 mg/L respectively before and 42 months after intervention. The total daily fluoride intake of adults and children in the intervention group (being 4.39,5.12,5.38,4.49 mg in adults and 1.90,2.33 in children, 2.33, 1.94 mg for four calculations) were lower than those in control group (8.42,9.07,8.35,7.92 and 3.65,3.93, 3.62,3.43 mg). Except the second batch (530.4 mg/kg), the average fluoride content of the other 3 batches of low-fluoride brick tea(239.3,222.88,154.7 mg/kg) was lower than that of 4 batches of market brick tea(366.9,412.2, 286.0,379.6 mg/kg). The fluoride content of low-fluoride brick tea samples was in accordance with the national standard(< 300 mg/kg) in 16 of 21 samples in 4 the batches, and the qualifying rate was 76.19%(16/21). Only 5 of 21 market brick tea samples in 4 batches was qualified, accounting for 23.80%(5/21), both were significantly different(χ2= 11.52, P < 0.01). In 12, 36, 42 months after intervention, urine fluoride content in the intervention group of adult(1.84,1.23,1.77 mg/L) and children(1.55,0.65,1.10 mg/L) was less than that of the control group (adults: 3.37,3.68,3.02 mg/L, children: 2.64,1.64,2.62 mg/L), both being statistically significant (t value were 2.94,2.43,3.91,3.29,2.31,4.42, P < 0.01 or 0.05). The detective rate of dental fluorosis was 69.02%(127/184)at baseline among children. After the intervention, it lowered to [44.83% (13/29) in the intervention group, significantly lower than that in the control group[71.88%(23/32), χ2 = 4.60, P < 0.05]. Conclusion Low-fluoride brick tea can reduce the fluoride intake of the residents who drink brick tea, and alleviate excessive fluoride and the damage of high-fluoride.

OBJECTIVETo investigate the testicular blood flow in patients with testicular microlithiasis (TM) and its correlation with the seminal profile in infertile men.

METHODSWe selected 88 infertile men and examined them by testicular color Doppler and routine seminal tests.

RESULTSTesticular microlithiasis was found in 19 (19.3%) of the patients, classic testicular microlithiasis (CTM) in 7 (8.0%), and limited testicular microlithiasis (LTM) in 10 (11.3%). No significant differences were observed in the age of onset, bilateral testicular volume, resistance index (RI) of bilateral testicular arteries, semen amount and the rate of teratospermia. The bilateral testicular peak systolic velocity (PSV), sperm count and sperm motility were significantly lower in the CTM than in the LTM group (P < 0.05), but showed no statistically significant difference between the LTM and the non-calcification group.

CONCLUSIONTM may be one of the causes of poor sperm function in infertile men.

Adult ; Blood Flow Velocity ; Calcinosis ; complications ; physiopathology ; Humans ; Infertility, Male ; complications ; physiopathology ; Male ; Middle Aged ; Regional Blood Flow ; Semen ; cytology ; Sperm Count ; Sperm Motility ; Testicular Diseases ; complications ; physiopathology ; Testis ; blood supply ; pathology

OBJECTIVETo observe the effect of volatile oil of amomum (VOA) on the expressions of mastocarcinoma-related peptide (PS2) and platelet activating factor (PAF) in helicobacter pyloriassociated gastritis (HPG) and to analyze its potential mechanism.

METHODSEighty patients with HPG were randomly assigned to two groups, 42 patients in the treated group treated with 0.5 mL VOA, thrice per day; and the 38 patients in the control group receiving Western tertiary medicinal treatment. Gastroscopic picture and helicobacter pylori (HP) infection (by quick urease and Warthin-Starry stain) of the gastro-membrane, expressions of PS2 and PAF (by immunohistochemical assay and Western blotting) as well as the contents of aminohexose and phospholipid (by Neuhaus method) in the gastric membrane of all patients were detected before treatment and 4 weeks after treatment. The clinical efficacy in the two groups was compared.

RESULTSThe total effective rate in the treated group was 88.1%, which was significantly higher than that in the control group (78.9%, P<0.05). After treatment, in the treated group, gastric membranous contents of aminohexose and phospholipid was increased, expression of PS2 elevated but that of PAF lowered, all showing significant difference as compared with those in the control group (P<0.01). In the control group, the expressions of PS2 and PAF changed insignificantly. The radical eliminating rate of HP in the treated group and the control group was insignificantly different between them (76.1% vs. 65.8%, P>0.05).

CONCLUSIONThe mechanism of VOA for anti-gastritis might be related with its action in increasing the expression of PS2 and decreasing the expression of PAF, and thus regulating the hydrophobicity of the gastric membrane.

Adult ; Aged ; Amomum ; Blotting, Western ; Chronic Disease ; Female ; Gastric Mucosa ; chemistry ; Gastritis ; drug therapy ; metabolism ; Helicobacter Infections ; drug therapy ; metabolism ; Helicobacter pylori ; Humans ; Immunohistochemistry ; Male ; Middle Aged ; Oils, Volatile ; adverse effects ; therapeutic use ; Peptides ; analysis ; Phospholipids ; analysis ; Platelet Activating Factor ; analysis

OBJECTIVETo compare changes of hypothalamus-pituitary-adrenal axis (HPAA) in different rat models of Gan stagnation (GS), Pi deficiency (PD), Gan stagnation Pi deficiency (GSPD) syndromes, and to observe interventional effect of Chaishu Sijun Decoction (CSD, capable of soothing Gan-qi invigorating Pi) on them.

METHODSSeventy Wistar rats were divided into the normal control group (group 1), the GS group (group 2), the PD group (group 3), the GSPD group (group 4), the GS intervention group (group 5), the PD intervention group (group 6), and the GSPD intervention group (group 7) according to random digit table, 10 in each group. Rats in group 1 received no treatment. Rats in group 2 and 5 were modeled by chronic restraint method. Rats in group 3 and 6 were modeled by excess fatigue plus alimentary abstinence method. Rats in group 4 and 7 were modeled by chronic restraint, excess fatigue, and alimentary abstinence method. At the 2nd weekend of modeling, CSD at 2.86 g/kg was fed to rats in group 5, 6, and 7 by gastrogavage for 2 successive weeks. Equal volume of distilled water was given to rats in the rest 4 groups. On the 29th day, rats were killed, adrenal weight weighed, and adrenal index calculated. Levels of plasma and hypothalamus corticotropin-releasing hormone (CRH), plasma and pituitary adrenocorticotrophic hormone (ACTH), and plasma corticosterone (CORT) were determined using radioimmunity.

RESULTSCompared with group 1, adrenal index significantly decreased in group 2, 3, and 4 (P < 0.05). Of them, plasma and hypothalamus CRH, plasma CORT increased significantly in group 2 and 4 (P < 0.05). Besides, plasma and pituitary ACTH increased in group 4 (P < 0.05). Plasma and pituitary ACTH, as well as plasma CORT decreased significantly in group 3 (P < 0.05). Compared with group 2, 3, and 4, adrenal index increased significantly in group 5, 6, and 7 (P < 0.05). Compared with group 2, plasma CORT, hypothalamus CRH, and pituitary ACTH decreased significantly in group 5 (P < 0.05). Compared with group 3, plasma ACTH and CORT increased significantly in group 6 (P < 0.05). Compared with group 4, plasma CRH, ACTH, CORT, hypothalamus CRH, and pituitary ACTH decreased in group 7 (P < 0.05).

CONCLUSIONSThe function of HPA .axis was damaged to varying degrees in rats of the three models in this experiment. Hyperactivity of HPA axis existed in GS syndrome and GSPD syndrome. Impairment of feedback regulation in hypothalamus and pituitary was accompanied in GSPD syndrome. Hypofunction of HPA axis existed in PDS. CSD, capable of soothing Gan-qi invigorating'Pi, showed improvement on disarranged HPAA, but with optimal effect on GSPD syndrome. CSD had higher correlation with GSPD syndrome.

Adrenocorticotropic Hormone ; metabolism ; Animals ; Corticosterone ; Corticotropin-Releasing Hormone ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Hypothalamo-Hypophyseal System ; metabolism ; Hypothalamus ; metabolism ; Medicine, Chinese Traditional ; Models, Animal ; Pituitary Gland ; metabolism ; Pituitary-Adrenal System ; metabolism ; Rats ; Rats, Wistar

OBJECTIVETo investigate the in vitro effect of HSV-tk/GCV using a hTERT promoter-driven vector system on Skov3 ovarian cancer cells.

METHODSAn expression vector (pBTdel-279-tk) containing tk gene under the hTERT promoter was constructed by molecular biological methods, and then was transfected into Skov3 ovarian cancer cells, normal ovarian epithelial cells (NOEC) and human embryonic lung fibroblast by cationic liposome. Following the transfection with tk, GCV was added, and MTT and flow cytometry methods were applied to investigate its antitumor effect. RT-PCR was used to detect the tk gene in ovarian cancer cells and normal cells after the transfection of pcDNA3-tk or pBTdel-279-tk.

RESULTSpBTdel-279-tk/GCV system induced apoptosis in hTERT-positive ovarian cancer cells, but not in hTERT-negative normal ovarian epithelial cells and fibroblasts. The hTERT promoter system was almost as efficient in inducing cancer cell death as the CMV promoter. tk gene was expressed in Skov3 cells and NOEC after pcDNA3-tk transfection, while positive was only in ovarian cancer cells after pBTdel-279-tk transfection.

CONCLUSIONThe telomerasespecific transfer of the tk gene under the hTERT promoter is a novel targeting approach for the treatment of ovarian cancer and may lead to an effective and specific gene therapy.

Apoptosis ; genetics ; Cystadenocarcinoma, Serous ; genetics ; pathology ; DNA-Binding Proteins ; Female ; Ganciclovir ; pharmacology ; Genetic Therapy ; Humans ; Ovarian Neoplasms ; genetics ; pathology ; Promoter Regions, Genetic ; genetics ; Simplexvirus ; genetics ; Telomerase ; genetics ; Thymidine Kinase ; genetics ; Transfection ; Tumor Cells, Cultured

Adult ; Female ; Heart Diseases ; diagnosis ; Humans ; Mitral Valve Stenosis ; diagnosis ; Postpartum Period ; Pregnancy ; Thrombosis ; diagnosis