ABSTRACT
This study was aimed to compare the pharmacokinetics (PK) of Shengmai injection and Shenmai injection with a single injection administration using a constant speed in subjects with stable angina pectoris.A total of 20 subjects with stable angina pectoris were divided into two groups.Each group was administered with Shengmai and Shenmai injection.The liquid chromatography-mass spectrometry (LC/MS) was adopted to determine concentrations of ginsenosides in plasma at different time points.PK parameters were calculated for comparison.The results showed that after a single intravenous infusion of Shengmai and Shenmai injection,the Cm.of ginsenoside Rg1,ginsenoside Re,ginsenoside Rb1 and ginsenoside Rc in Shenmai group were higher than those of the Shengmai group with statistical significance (P ≤0.05).There were differences on the T1/2 of ginsenoside Rg1,AUC0-144h and CL of ginsenoside Rc,as well as Tmax of ginsenoside Rd (P ≤ 0.05).However,there was no significant difference shown on other PK parameters.It was concluded that after a single Shengmai or Shenmai injection,there were PK differences of ginsenoside Rg1,ginsenoside Re,ginsenoside Rb1 and ginsenoside Rc in the human body.The clinical medication selection should be based on syndrome differentiation and treatment of patients.
ABSTRACT
This study was aimed to establish the pharmacokinetics-pharmacodynamics (PK-PD) model of ginsenoside Rb1 following the intravenous administration of Shengmai injection in subjects with stable angina pectoris.A total of stable angina pectoris were selected and received Shengmai injection for 14 days.Plasma samples were collected at different time points.Plasma concentrations of ginsenoside Rb1 were determined by liquid chromatography-mass spectrometry (LC/MS).The concentration-time curves (AUC) were drawn,and then the PK parameters were calculated.The systolic pressure and diastolic pressure were monitored,and the combined PK-PD model was established based on the theory of effect compartment.The results showed that PK of ginsenoside Rb1 conformed to a mono-compartment model.The effect of Shengmai injection lagged behind the concentrations of ginsenoside Rb1 in plasma.The effect exhibited good correlation with ginsenoside Rb1 in effect compartment.The relationship between effect and plasma concentrations fits the Inhibitory Effect Imax model.It was concluded that the study successfully established the combined PK-PD model of ginsenoside Rb1 in subjects with angina pectoris.The model can efficiently evaluate the effective substance of Shengmai injection.
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OBJECTIVE:To study the pharmacokinetics of the active ingredients of Shenmai injection,including ginsenoside Rg1 and ginsenoside Re,in normal Beagle dogs and those with myocardial ischemia. METHODS:6 Beagle dogs were given isopro-terenol hydrochloride (1.1 mg/kg) sc to establish the model of myocardial ischemia (model group). Another 6 Beagle dogs were given isometric normal saline (2.2 ml/kg) sc as controls group. The two groups of dogs respectively received corresponding drugs sc at 8:00 am and 13:00 pm on day 1 and at 8:00 am on day 2. Each group of dogs were given Shenmai injection(1.6 ml/kg)iv 1 h after administration on day 2,and such intravenous drip lasted for about 1 h. Blood was collected from each group 0,0.25, 0.5,0.75,1(the end of iv),1.5,2,3,4,6,8,12 and 24 h from the start of iv. Liquid chromatography-mass spectrometry was adopted to determine the concentrations of ginsenoside Rg1 and ginsenoside Re in blood,and WinNonlin 6.3 was used to calculate pharmacokinetic parameters for comparison. RESULTS:For ginsenoside Re in the dogs of the model group,t1/2 was(2.69±1.12) h,AUC0-24 h was(2 060.78±812.18)h·μg/L,Vz was(46.16±20.98)ml and CL was(9.02±4.45)ml/h;compared to the normal control group,AUC0-24 h was much greater and Vz and CL were significantly lower,showing a statistically significant difference(P0.05). CON-CLUSIONS:Myocardial ischemia may affect the removal of ginsenoside Re in Beagle dogs,but has no effect on the pharmacoki-netic process of ginsenoside Rg1.
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<p><b>OBJECTIVE</b>To evaluate the inhibitory effect of high mobility group chromosomal protein N2 (HMGN2) on human tongue carcinoma tumor in nude mice.</p><p><b>METHODS</b>A transplantation tumor model in nude mice was constructed by injecting Tca8113 cells. After a week, negative control groups, masculine control groups, and HMGN2 groups were established. Cell culture of the three groups were separately injected with washing buffer II, cis-dichlorodiamineplatinum (DDP), and HMGN2 protein. The tumors were moved after four treatments, and then analyzed by hematoxylin-eosin (HE) staining.</p><p><b>RESULTS</b>A transplanted tumor model was established successfully. The volumes of HMGN2 groups and masculine control groups were smaller than those of the negative groups. Mouse weight did not differ among the three groups. Average tumor weight of the negative group was (0.38 +/- 0.19)g, that of the HMGN2 group was (0.21 +/- 0.15)g, and that of the DDP group was (0.23 +/- 0.16)g. These factors indicated no statistically significant difference among the three groups. The tumor inhibitory rate of HMGN2 group was 45.71%, and that of the positive group was 39.44%. Based on evaluation by naked eye, the tumor in the negative group was larger than that in other groups. In addition, cell necrosis was observed during HE staining.</p><p><b>CONCLUSION</b>HMGN2 could significantly inhibit growth of the transplanted tumor in nude mice.</p>
Subject(s)
Animals , Humans , Mice , Carcinoma , Cell Line, Tumor , High Mobility Group Proteins , Mice, Inbred BALB C , Mice, Nude , Neoplasm Transplantation , Tongue NeoplasmsABSTRACT
<p><b>OBJECTIVE</b>Take human oral squamous cell carcinoma Tca8113 as experimental model, and study the anti oral squamous cell carcinoma activity of high mobility group chromosomal protein N2 (HMGN2) molecule.</p><p><b>METHODS</b>Train a large number of recombinant human HMGN2 expression vector Escherichia coli BL21. HMGN2 was expressed under isopropyl-1-thio-beta-galactopyranoside (IPTG) induction and purified by B-PER GST Fusion Protein Purification Kit. A variety of concentrations HMGN2 were added to cell culture medium, cells were tested by MTT, Hoechst 33342 fluorescence staining, flow cytometry assay and Western-blot.</p><p><b>RESULTS</b>MTT results proved that HMGN2 could significantly inhibit human oral squamous cell carcinoma Tca8113 growth. Hoechst 33342 fluorescence staining, flow cytometry assay test and Western-blot proved HMGN2 could make Tca8113 cells morphological change, make Tca8113 cells block in S period of cell cycle and strongly promote Tca8113 cells to apoptosis.</p><p><b>CONCLUSION</b>HMGN2 can promote apoptosis of oral squamous cell carcinoma cells.</p>