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OBJECTIVE: To prepare Usnic acid self-microemulsion, prescription optimization and evaluate its quality. METHODS: Usnic acid self-microemulsion was prepared by emulsification method using medium chain triglycerides-single linoleic acid glyceride (1:1, m/m) as oil phase, polyoxyethylene hydrogenated castor oil as emulsifier, diethylene glycol monoethyl ether as co-emulsifier. Based on the solubility test and pseudotemary phase diagram, using self-emulsifying time (t), light transmittance (T), drug equilibrium solubility (S), accumulative dissolution rate at 5 min and 60 min (Q5 min, Q60 min) as evaluation indexes, central composite design-response surface methodology was utilized to optimize oil phase ratio and ratio of emulsifier to co-emulsifier (Km) in microemulsion formulation. At the same time, the optimal formulation was verified, the morphology, particle size, drug-loading amount and dissolution of Usnic acid self-microemulsion were investigated. RESULTS: The optimal formulation was as follows as oil phase ratio of 25％, Km of 2. 0; ratio of mixed oil phase, emulsifier, co-emulsifier in the formulation was 25％, 50％, 25％. t, T, S, Q5 min and Q60 min of Usnic acid self-microemulsion prepared by optimal formulation were 1. 96 min, 87. 67％, 5. 67 mg/g, 66. 58％, 76. 73％ (all RSD<3％, n = 3),respectively. The relative errors of them to predicted values were all less than 4％ (n = 3). Usnic acid self-microemulsion was spherical droplet in shape after diluted with water. The average particle size was 39. 4 nm, average drug-loading amount was 4. 55 mg/g. Q90 min of Usnic acid self-microemulsion reached 99. 58％ in pH 6. 8 phosphate buffer (n = 3). CONCLUSIONS: Prepared Usnic acid self-microemulsion is in line with quality requirements.
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OBJECTIVE:To virtually screen lignanoid compounds with inhibitory effect of histone deacetylase(HDAC)by vir-tual screening method. METHODS:Using“lignanoid”as keyword,requiring CNKI,VIP,PubMed and other database,lignanoid compounds were collected as ligand to establish ligand base, histone deacetylase receptor HDAC2 (PDB code:4LXZ) and HDAC8 (PDB code:1T69) were selected from PDB database,and then ligands and 3D active site of receptors were docked by SYBYL-X 2.0 software. The affinity of receptors to ligand was reflected by total score. RESULTS:345 lignanoid compounds, 4LXZ and 1T69 primary ligand were used to establish ligand base which included 347 ligands. Ligands No.275,271,110,200, 056,258,181,129,037,270,187 were demonstrated good affinity with receptors HDAC2 and HDAC8. Ligands and receptors residue were docked via hydrogen bond. CONCLUSIONS:Lignanoid compounds have inhibitory effect on HDAC;virtual screen-ing method is effective in natural product activity prediction,which can provide quick access to and theoretical guidance for new pharmacological studies of lignanoid compounds.
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Objective To study the relationship between polymorphism of NAT2 gene and the susceptibility of osteosarcoma. Methods Using serum samples of patients with osteosarcoma , NAT2 gene polymorphism was determined by PCR-RFLP to observe M1, M2 and M3 mutant genes, NAT2 genotype and allele distribution. Slow acetylation and rapid acetylation genotype between groups in the distribution were also detected. Moreover , the relationship between the clinical characteristics of osteosarcoma and NAT2 genetic polymorphism were analyzed. Results From January 2010 to September 2015, 126 patients with osteosarcoma were enrolled as a case group, and 119 healthy persons in the same period were as the control group. In the control group, the frequency of NAT2 genotype (homozygous wild type (wt/wt and miscellaneous synthetic mutant WT/ MX, homozygous mutant MX/MX) were 30.95%, 50.79% and 18.25% respectively; In the experimental group were 47.06%, 46.22% and 6.72% respectively. The frequency of the two groups was statistically significant (P <0.05). Rapid NAT2 acetylator genotype of suffering from the risk of osteosarcoma 1.782 times slow acetylation genotype (P < 0.05). Compared to rapid acetylation genotype patients with osteosarcoma, slow acetylation genotype patients has smaller tumor volume (P = 0.008),lower differentiation degree of tumor (P = 0.011) and less occurrence of distant metastasis (P = 0.001). Conclusion The rapid acetylation genotype of NAT2 gene may be a risk factor for osteosarcoma.
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Three homoisoflavonoids, 6-aldehydo-3-ophiopogonanone A, methyl ophiopogonanone A and ophiopogonanone A from Ophiopogon japonicus were analyzed simultaneously by HPLC with acetonitrile-water containing 0.5% H3 PO4 (58:42) as the mobile phase, and the detection wavelength was set at 296 nm (0-14 min) and 275 nm (14-22 min). The mean recoveries of three homoisoflavonoids were 99.41%-99.86% (RSD 0.82%-1.05%). The linear response ranges of. 6-aldehydo-3-ophiopogonanone A, methyl ophiopogonanone A and ophiopogonanone A were 0.165-0.990 microg (r = 0.999 9), 0.153-0.918 microg (r = 0.999 9), and 0.270-1.620 microg (r = 0.999 9), respectively. This method was certified to be accurate and reliable and can be used for quality control of O. japonicus.
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Cromatografia Líquida de Alta Pressão , Métodos , Medicamentos de Ervas Chinesas , Isoflavonas , Ophiopogon , QuímicaRESUMO
<p><b>OBJECTIVE</b>To determine the contents of twelve ginsenosides in the root of Panax ginseng by HPLC.</p><p><b>METHOD</b>The analysis is carried out at room temperature on a Luna NH2 column (4.6 mm x 150 mm, 5 microm) eluted with acetonitrile and water as the mobile phases in a gradient elution. The flow-rate was 1.0 mL x min(-1), the detection wavelength was 203 nm.</p><p><b>RESULT</b>Twelve ginsenosides (Rh2, Rh1, Rg2, Rg3, Rg1, Rf, Re, Rd, Re, Rb2, Rb3, Rb1) were separated at baseline within 60 min with good linearity (r > or = 0.999 5). The recovery rates were 98.1%, 95.3%, 96.1%, 95.6%, 97.3%, 98.6%, 98.0%, 96.4%, 96.1%, 97.6%, 96.8%, 96.9% (RSD < or = 3.0%).</p><p><b>CONCLUSION</b>The method was simple,fast and could control the quality of P. ginseng effectively.</p>
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Cromatografia Líquida de Alta Pressão , Métodos , Ginsenosídeos , Panax , Química , Extratos Vegetais , Raízes de Plantas , Química , Controle de QualidadeRESUMO
Objective To analyze the correlation of preoperative serum vascular endothelial growth factor(VEGF)level with serum CA125 level in patients with epithelial ovarian cancer(EOC),and to evaluate the prognostic value of preoperative serum VEGF in these patients.Methods Forty-one patients with EOC were included as study group,while 20 healthy women were selected as control group.Enzymelinked immunosorbent assay(ELISA)and chemiluminescence assay were used to measure serum VEGF and CA125 level respectively.The correlations of serum VEGF with CA125 level,postoperative recurrence rate and survival time were analyzed retrospectively.Resuits Serum VEGF levels in patients with EOC were higher than those in healthy women,with the median of 415 and 165 ng/L,range 110-2120 and 100-735 ng/L respectively(P＜0.01).No correlation was found between preoperative serum VEGF and CA125 level (Spearman test,P=0.989).High preoperative serum VEGF was positively correlated with postoperative recurrence.Serum VEGF level in patients with postoperative recurrence was higher than that in patients without recurrence,with the median of 490 and 315 ng/L respectively(P=0.035).Univariate analysis showed that higher serum level was reversely correlated with shorter survival.Median overall survival time in patients with higher serum VEGF level and lower serum VEGF level was 18 months and＞35 months respectively(P=0.010).Multivariate Cox model analysis showed that high VEGF level was an independentfactor for the prognosis of EOC(P=0.042).Conclusion Preoperative serum VEGF level is not correlated with CA125 concentration in patients with EOC,and it is an independent risk factor for prognosis.
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OBJECTIVE:To establish an RP-HPLC analysis of Carthamin in mice and to study its pharmacokinetics.METHODS:The serum concentration of Carthamin was determined by RP-HPLC.The blood concentration-time curve was established and the main pharmacokinetic parameters were computed.RESULTS:The linear range of Carthamin was 0.558～55.8 ?g?L-1(r=0.999 2),with the lowest limit of detection at 0.005 ?g?L-1Carthamin in vivo assumed two-compartment model and rapid absorption.CONCLUSION:The proposed method is simple,sensitive and reproducible,and it met the standard for pharmacokinetic study.
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Objective To investigate changes of markers of prethrombotic state(PTS)with heart failure and to explore their clinical significances.Methods Plasma levels of t-PA、PAI-1、Fg、PT、APTT、ET-1、MPV were measured in 52 patients with heart failure and in 38 normal controls.Results Compared with the healthy control group,patients with heart failure had significant increase of plasma PAI-1、Fg and ET-1level.Conclusions PTS is present in heart failure,especially in those with more severe Nyha class.
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Objective To study the action of corn filament beverage (CFB)on falling blood sugar in diabetic rats and mice,provide scientific basis for application of corn filament extraction in falling sugar drug or functional food. Methods 60 rats were randomly divided into control group(pure water),alloxan model group,Kanglishu capsule (0.7 g?kg-1) group,and 7.00,3.50,1.75 mL?kg-1 CFB groups(n=10). the orbital vein blood samples were obtained,the contents of blood sugar were determined;The liver samples were obtained and the contents of liver glycogen were determined. 72 mice were randomly divided into control group(pure water),alloxan model group,Kanglishu capsule (1.0 g?kg-1) group,and 10.0,5.0,0.25 mL?kg-1 CFB groups(n=12),the indexes mentioned above were determined.72 mice were divided into 6 groups same as the method mentioned above,the mice were injected adrenalin hydrochloride through abdominal cavity,blood was extracted by decapitation,and the contents of blood sugar and liver glycogen were determined. Another 72 mice were divided and fed same as the method mentioned above,and the mice were injected glucose through caudal vein,the indexes mentioned above were detected. Results Compared with diabetic model rats,the contents of blood sugar in 7.00 and 3.50 mL?kg-1 CFB groups were reduced obviously(P
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Objective To observe the action of lowering blood fat of corn filament beverage(CFB) on hyperlipemia rats and mice.Methods Sixty rats were randomly divided into control group,alloxan model group,kanglishu capsule 0.70 g?kg-1 group,CFB 7.00,3.50,1.75 mL?kg-1 groups(n=10).Rats in each group were exhibited once a day for 21 d,on the seventh day,fourteenth day,twenty-first day, the contents of serum total cholesterol(TCHO) and triglyceride(TG) were determined,and liver malonaldehyde(MDA) level was measured.Another 60 mice were divided into 6 groups with the method mentioned above,mice in each group were exhibited once a day for 14 d,on the fourteenth day,the serum contents of TCHO and TG were determined,and liver MDA level was determined.Another 72 mice were randomly divided into control group,egg yolk model group,Expellant and Cleanning Fat Capsule 0.4 g?kg1 group,CFB 10.0,5.0,2.5 mL?kg-1 groups(n=12).Mice in each group were exhibited once a day for 10 d.16 h before the last administration,except control group,the mice in other groups were injected with 75% yolk physiological salt solution 0.5mL through the abdominal cavity,and began to starve,1 h after the last administration, the contents of serum TCHO and TG were determined,and liver MDA level was measured.Results Compared with alloxan model group,TCHO and TG in hyperlipemia rats of CFB 7.00 mL?kg-1 all reduced obviously(P
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OBJECTIVE: To establish a HPLC method for the determination of the content of Demethylbellidifolin in different parts of Swertia davidi Franch. METHODS: The analysis was carried out on Hypersil C18 column (150mm?4.6mm,5 ?m) at room temperature with mobile phase consisted of CH3OH-0.5%H3PO4(56∶44) at a flow-rate of 1.0mL?min-1.The detection wavelength was set at 254 nm. RESULTS: The linear range of Demethylbellidifolin was 0.52～2.60?g (r=0.999 4) and the average recovery was 99.77%(RSD=0.95%).CONCLUSION: The method is simple, rapid, reproducible, and suitable for the determination of the content of Demethylbellidifolin in Swertia davidi Franch..
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OBJECTIVE:To establish a HPLC method for the determination of quercitrin in Saxifrage.METHODS:The analysis was performed on C18 column(150mm?4.6mm,5?m),the mobile phase was MeOH-0.2%H3PO4 (45∶55)with a flow rate at 1.0ml/min and wavelength at 350nm under room temperature.RESULTS:There was a good linear relationship when the sample size of quercitrin was at a range of 0.40?g～2.00?g(r=0.9 996),the recovery was 95.33%with RSD at 2.80%.CONCLUSION:This method was simple,stable,fast,and reproducible and without the interference of impurity,which can be used for the content determination of quercitrin in Saxifrage.
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BACKGROUND: Craniocerebral injury can cause a series of visceral complications, among which cardiovascular complication is paid special attention.OBJECTIVE: To investigate the effects of craniocerebral injury on changes of circulatory and local angiotensin Ⅱ (Ang Ⅱ ) and local angiotensin Ⅱ receptor 1 (AT1) in the heart.DESIGN: Randomized controlled experiment taking animals as subjects.SETTING: Beijing Tiantan Hospital, and the College of Basic Medicine,Capital University of Medical Sciences.MATERIALS: The experiment was conducted at the Central Laboratory of Capital University of Medical Sciences and the Central Laboratory of Beijing Tiantan Hospital from 2003 to 2004. Totally 40 healthy male Wistar rats were divided randomly into craniocerebral injury group and control group with 20 in each group.METHODS: Rats in craniocerebral injury group were treated with weightdrop method to establish the model of craniocerebral injury, while rats in control group received no impact. Twenty-four hours after hitting, 10 rats in each group were selected to assay their Ang Ⅱ and AT1; the other 10 in each group were selected to observe their myocardial forms.myocardium of rats assayed with light microscope after hematoxylin-eosin staining and transmission electron microscope.It was significantly higher in craniocerebral injury group than in control ity: It was obviously higher in craniocerebral injury group than in control Ⅱ and AT1: The area of positive reactant and gray value in craniocerebral toxylin-eosin staining: Strong acidophil staining was found on myocardial cellular plasma in craniocerebral injury group. The results showed that cytoplasm shrank obviously; muscle fiber broke, decreased or disappeared.Focal hydropic degeneration, lysis or necrosis was observed in myocardium.Ultrastructural pathological observation revealed pathological damage of myocardium.CONCLUSION: Craniocerebral injury in rats can cause myocardial damage, and changes of angiotensin system may be one of the factors.
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Objective: To investigate the short-term effects of ischemic preconditioning (IP) on left ventricular diastolic function in diabetic patients with acute myocardial infarction(AMI). Methods: Totally 188 patients with first AMI were studied. Eighty-one patients without diabetes were divided into group A (with IP) and group B (without IP). The other 107 patients with diabetes were divided into group C (with IP) and group D (without IP).The effect of IP on peak creatine kinase value and left ventricular diastolic function were analyzed separately. Results: The peak creatine kinase value, the peak creatine kinase MB fractions and the incidence of E/A
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Objective To determine serum soluble interleukin 2 receptor level in patients with posthepatitis B liver cirrhosis.Methods Serum sIL 2R was measured using enzyme linked immunosorbent assay.Results Serum sIL 2R was significantly higher in patients with posthepatitis B cirrhosis than that in controls(P