Drug Resistance ; Hormones ; pharmacology ; Humans ; Membrane Proteins ; genetics ; Nephrotic Syndrome ; genetics

This study was designed to validate the correlation between integrated pharmacokinetic and therapeutic effects of alkaloids using bile processed Rhizoma Coptidis (BRC). Rats were divided into three groups: normal, disease model, model+BRC. Rats were induced to have an excessive heat syndrome. Rectal temperatures were collected at 0, 3, 6 and 9 h after single oral administration of the drugs. The plasma concentrations of three alkaloids were quantified at different times by UPLC-MS/MS after the administration of BRC. An approach of self-defined weighting coefficiency was created to the holistic pharmacokinetic profiles of alkaloids in BRC. The classified and integrated synthetic concentrations were obtained, and then the pharmacokinetic parameters of alkaloids were calculated from non-compartmental model analysis. The potential relationship between the integrated mean concentration of alkaloids and the antifebrile efficacy was investigated. The holistic t(max) of alkaloids was 1.11 h, the antifebrile effect of BRC at 3 h was improved over the model group. Double peaking appeared in the integrated blood concentration-time curve, the second t(max) of alkaloids was 4.82 h. The antifebrile effects of BRC at 3-6 h were significant, and the antifebrile effects at 6-9 h was decreased significantly. Dynamic variation of alkaloids of BRC in the body exhibited the similarity to the pattern of its antifebrile effect.
Administration, Oral ; Alkaloids ; pharmacokinetics ; Animals ; Bile ; Coptis ; chemistry ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Rhizome ; chemistry ; Tandem Mass Spectrometry

Objective To study the preventive effect of small-dose fluconazol adiministered in low frequency on nosocomial fungal infectoin.Methods The condition of nosocomial fungal infection among 200 patients in pediatric intensive care unit (PICU)were observed,who were suffered with serious infection or basic diseases and underwent broad-spectrum or ultra-broad spectrum antibiotic and steroid hormones treatment.These patients were divided imto treatment and control group.And the patients in treatment group received fluconazol[5 mg/(kg?time)once every 2 days,total 3 times,after that,twice 1 week till improved] to prevent fungal infection .The control group were treated with fluconazol [6-10 mg/(kg?time),once everyday for 10-14 days] after fungal infection.Results The incidence rate of nosocomial fungal infectoin of control group was 58.3%(56 out of 96 cases,which were 44 cases of mouth,5 cases of respiratory tract ,5 cases of digestive tract and 2 cases of urethra ) and that of treatment group was 1.9%(2 out of 104 cases, which were 2 cases of mouth).In control group,37 cases were cured,17 cases improved and 2 cases were not effective.Mouth fungal infection in treatment group was gently and cured with 1 or 2 times of local treatment .The treatment group didn′t occured liver function damage or aggravation.Conclusion For PICU patients, adiministration of small-dose flucomazol in low frequency is an effective and relatively safety method to prevent against nosocomial fungal infectoin.

Humans ; Kidney Diseases ; genetics ; Mutation ; WT1 Proteins ; genetics

Objective To establish the preparation techniques for preparing the reference substance of platycodin-D.Methods Raw material of platycodi radix was extracted with 70 %MeOH.The concentrated extract passed through D101 macroporous resin column,then the 40 %alcohol eluate was separated by silica gel column chromatography with chloroform-methanol gradient elution.The fractions contained platycodin-D were collected and purified by HPLC.Results HPLC analysis and normalization of peak areas showed the purity of the platycodin-D was 98.8 %.Conclusions The preparation techniques are simple and high yield,can be used for preparing the reference substance of platycodin-D.

Objective To investigate the MRI and echocardiography manifestations of noncompaction of ventricular myocardium(NVM)and assess the role of MRI in the diagnosis of NVM by comparing it with echocardiography.Methods Fourteen cases of NVM diagnosed by echocardiography were examined with MRI,including scanning of black-blood sequences,double inversion recovery fast spin echo (DIRFSE)and triple inversion recovery fast spin echo(TIRFSE),and white blood sequence:fast imaging employ steady state acquisition(FIESTA).Scanning plane includes short axis view,four-chamber view and long axis view.Results Both MRI and echocardiography displayed involvement of left ventricles in thirteen cases and involvement of double ventricles in one case.Apexes of heart and the intermedius are commonly affected.MRI showed 54 segments and echocardiography showed 53 segments affected,and there is no significant difference between the capability of MRI and echocardiography(P=1.000).The affected myocardium consisted of two layers:subendoeardial noncompacted myocardium and epicardial compacted myocardium,and the ratio measurement of N/C by MRI was 3.37?0.89 and it was 3.19?0.82 by echocardiography.Noncompacted myocardium was characterized by prominent and excessive myocardial trabeculations and deep intratrabecular recesses,in which the blood flow was communicated with the ventricle.One case was complicated with ventricular aneurysm,and coronary arteriography was performed with unremarkable findings.One case underwent heart transplantation because of progressive heart failure, Gross findings demonstrated prominent muscular trabeculations with deep intratrabecular recesses,which coincided well with MRI findings.Conclusion The MRI manifestation of NVM is characteristic,and MRI with multiple series and planes is helpful in the diagnose of NVM.Compared with echoeardiography,MRI could display the pathological cardiac muscle more clearly,because of its high soft-tissue resolution and spatial resolution.

Objective To study the personality characteristics of the stagnation of liver-qi syndrome cases with Minnesota Multiphasic Personality Inventory (MMPI).Methods 20 liver-qi stagnation syndrome cases and 20 normal persons whose paired by sex and age were tested by MMPI. The scores of 13 clinical scales and the section plane of MMPI were acquired and analyzed. Results There was a significant difference in 9 clinical scales (F, Pa, D, Pt, Si, Sc, Hs, Hy, Pd) between the liver-qi stagnation syndrome cases and normal persons ( P<0.05～0.001). The scores of Hs, D, Hy, Pd in the liver-qi stagnation syndrome group were higher than the Chinese normal model. The MMPI section plane of liver-qi stagnation group presented the type of 3/1. Conclusion The patients with liver-qi stagnation have some special personality characteristics such as depression, anxiety, loneliness, indifferent and attention.

To make a preliminary study on the mechanism of Coptidis Rhizoma(CR) and Rehmanniae Radix(RR) before and after the combined administration in treating type II diabetes mellitus. The type I diabetes animal model in rats was established by fat emulsion and intraperitoneal injection with streptozotocin, in order to compare the hpyerglycemic and hypolipidemic effects of CR, RR and their combined administration of different ratio. The urinary metabolic profiling in rats of Coptidis Rhizoma and Rehmanniae Radix before and after the combined administration was analyzed by using the gas chromatography-mass spectrometry. The differences among groups in metabolome were analyzed by the principal component analysis (PCA). The biochemical index results indicated that both CR and RR before and after the combined administration could lower high blood glucose, hypertriglyceride and high cholesterol. According to the analytical results of PCA of the rats' urine samples, the CR group was the most close to the normal group, with no significant difference in CR and RR group of different combination ratios. Twelve differentiated metabolites were identified to be related to type II diabetes. Compared with the normal group, the CR-treated group showed significant increase in seven differentiated metabolites. Among CR and RR drugs with different combination ratios, CR played a major role and thus acted as the monarch drug. Whereas RR served as the ministerial drug and assisted CR to show the efficacy. This study laid a foundation for the explanation of the combination mechanism of traditional Chinese medicines.
Animals ; Blood Glucose ; metabolism ; Diabetes Mellitus, Type 2 ; blood ; drug therapy ; urine ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Male ; Rats ; Rats, Wistar ; Rehmannia ; chemistry

OBJECTIVETo observe the effect of Tangke Decoction (TD) on the expression of TGF-beta1/Smad4 of rats with early diabetes and to explore the effect and mechanism of TD against the renal injury induced by diabetes.

METHODSSD rats were randomly divided into the normal control group (n = 12), the model group (n = 10), the Chinese herbs prevented group (n =10), the Chinese herbs treated group (n = 10), and the Western medicine control group (n = 10). TD (18 mg/kg) was given by gastrogavage to rats in the Chinese herbs prevented group immediately after successful modeling for 12 weeks, once daily. At the 4th week of successful modeling, rats in the rest 4 groups were administered by gastrogavage. Equal volume of normal saline was given to rats in the model group and the normal control group. Benazepril suspension (1 mg/kg) was administered by gastrogavage to rats in the Western medicine control group for 8 weeks, once daily. TD (18 mg/kg) was given by gastrogavage to rats in the Chinese herbs treated group for 8 weeks, once daily. The body weight, kidney weight, index of kidney weight, fasting blood sugar, 24 h urinary albumin excretion rate were examined after experiment. The pathological changes of the renal tissue were observed by HE staining, Masson staining, and electron microscope. The expression of renal transforming growth factor-beta1, (TGF-beta1) and Smad4 were detected using immunohistochemical assay.

RESULTSCompared with the normal control group, the body weight of rats decreased significantly; the kidney weight, index of kidney weight, blood sugar, 24 h urinary protein excretion, the urinary albumin excretion rate,TGF-beta1 and Smad4 expression increased significantly in the model group (all P < 0.01). Compared with the model group, the aforesaid indices were improved in each treatment group with statistical difference (P < 0.05, P < 0.01). Compared with the Western medicine control group, the kidney weight, index of kidney weight, blood sugar, 24 h urinary protein excretion, and the urinary albumin excretion rate were obviously improved in the Chinese herbs prevented group (P < 0.01). The renal pathological changes were most obvious in the model group significantly, but they were improved in all treatment groups.

CONCLUSIONTD could obviously improve the symptoms of diabetes and down-regulate the expression of renal TGF-beta1 and Smad4 of early diabetic nephropathy rats, which suggested that TD had certain preventive effect on early diabetic nephropathy.

Animals ; Diabetes Mellitus, Experimental ; drug therapy ; metabolism ; Drugs, Chinese Herbal ; therapeutic use ; Kidney ; metabolism ; Male ; Rats ; Rats, Wistar ; Smad4 Protein ; metabolism ; Transforming Growth Factor beta1 ; metabolism

To study the toxicokinetics of bakuchiol, hepatic and renal toxicity in rats after single oral administration of Psoraleae Fructus and combined with Glycyrrhizae Radix et Rhizoma, in order to provide scientific evidences for clinical safe medication use. A total of 35 SD rats were randomly divided into seven groups: vehicle (distilled water) control group, Glycyrrhizae Radix et Rhizoma group, positive control (aristolochic acid A) group, Psoraleae Fructus (40 g x kg(-1)) group( both male and female rats), Psoraleae Fructus and Glycyrrhizae Radix et Rhizoma (40 +20) g x kg(-1) group (both male and female rats). HPLC-UV method was used to determine the concentration of bakuchiol in rat plasma at different time points after single oral administration. Plasma alanine transaminase (ALT), aspartate aminotransferase (AST), blood urea nitrogen (BUN), plasma creatinine (Cr), N-acetyl-β-D-glucosaminidase (NAG) and kidney injury molecule 1 (Kim-1) were measured after administration for 24 h. The main toxicokinetics parameters of bakuchiol in rats exert significantly gender difference. When Psoraleae Fructus combination with Glycyrrhizae Radix et Rhizoma, the total area under the plasma concentration-time curve( AUC), C(max), and plasma clearance (CL) of bakuchiol were increased, respectively; CL, half-life (t½) were decreased, and T(max) were prolonged. The biochemical indicators (including ALT, AST, BUN, Cr and KIM-1 level) in different dose of Psoraleae Fructus groups, were found no statistically significant difference when compared with vehicle control group. The level of NAG in both Psoraleae Fructus and compatibility with Glycyrrhizae Radix et Rhizoma groups were significant increased (P < 0.05). There are obvious effects on toxicokinetics of bakuchiol in rats when Psoraleae Fructus combined with Glycyrrhizae Radix et Rhizoma. Renal toxicity induced by Psoraleae Fructus at high dose was observed after single oral administration and no liver damage in rats was found.
Administration, Oral ; Animals ; Female ; Glycyrrhiza ; toxicity ; Kidney ; drug effects ; Liver ; drug effects ; Male ; Phenols ; pharmacokinetics ; toxicity ; Psoralea ; toxicity ; Rats ; Rats, Sprague-Dawley ; Rhizome ; toxicity ; Toxicokinetics