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1.
Article in Chinese | WPRIM | ID: wpr-924033

ABSTRACT

Objective To analyze the effect of HIV/AIDS patients receiving antiretroviral therapy (ART) for the first time in Jiangyin, and to provide a reference for further improvement of Jiangyin's AIDS antiretroviral treatment. Methods The historical cards and related information in the treatment management database of Jiangyin City's cases who received ART for the first time from 2005 to 2019 were collected and statistically analyzed. The changes in viral load and CD4+ T lymphocytes (CD4 cells) before and after treatment were compared. Results Among 652 patients receiving ART, 507 cases (77.76%) were successful in virological treatment. The median natural change rate of annual average CD4 cell count was 90.8 cells/μL/year (χ2=37.915, P2=10.713, P<0.05; H =10.394, P<0.05) and different baseline CD4 count layers. The results showed that age and baseline CD4 value were the influencing factors of treatment effect. Conclusion Age and baseline CD4 value can affect the effect of ART treatment. The older the age and the lower the baseline CD4 value, the worse the virological efficacy and the recovery effect of CD4 cells. It is suggested that the infected patients should be involved in ART in time, which is conducive to shorten the time of initial treatment and further improve the effect of antiviral treatment.

2.
Article in Chinese | WPRIM | ID: wpr-921694

ABSTRACT

Phenylpropanoids are one of the major chemical constituents in Zanthoxylum species. They include simple phenylpropanoids, coumarins, and lignans and possess anti-tumor, anti-inflammatory, anti-platelet aggregation, anti-bacterial, anti-viral, insecticidal, and antifeedant activities. This review summarizes the chemical constituents and pharmacological activities from the Zanthoxylum plants in hopes of providing reference for the research and application of phenylpropanoids from this genus.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Coumarins/pharmacology , Lignans , Plant Extracts , Zanthoxylum
3.
China Pharmacy ; (12): 320-327, 2021.
Article in Chinese | WPRIM | ID: wpr-872684

ABSTRACT

OBJECTIVE:To prepare Liguatrazine opthalmic liposome therm osensitive gel ,and to investigate its in vivo and in vitro characteristics. METHODS :The ammonium sulfate gradient method was used to prepare Liguatrazine liposomes. The preparation technology was optimized by using orthogonal test. Using poloxamer P 407 as gel matrix ,Liguatrazine liposomes were prepared into thermosensitive gel. A membraneless model was used to study the dissolution and in vitro drug release of the gel. The modified Franz diffusion cell was used to investigate corneal permeability and further determine corneal hydration value. The effects of the gel on the proliferation of human corneal epithelial cell HCE-T. HE staining and Draize test were used to investigate the stimulatory effects of the gel on corneal cells of the rabbit ,and the histological changes of the eyes were observed. RESULTS :The optimal preparation technology of Liguatrazine liposome was drug-lipid ratio of 1 ∶ 10(m/m),the ammonium sulfate concentration of 0.2 mol/L,phospholipid-cholesterol ratio of 4∶1(m/m),incubation temperature of 45 ℃. Then ligustrazine opthalmic liposome thermosensitive gel was prepared with 23% poloxamer P 407 as gel matrix. The gel had good gelatinization temperature. The in vitro drug release and dissolution showed zero-order kinetic characteristics ,and in vitro drug release of the gel was mainly related to dissolution (R2=0.993 4). The cumulative transcorneal permeability of the gel was 43.3% within 6 hours and corneal hydration value was 72.98%. Low and medium concentrations (1,5 mg/L)of Ligustrazine opthalmic liposome thermosensitive gel had no obvious proliferation toxicity to HCE-T cells ,but it showed cytotoxicity at high concentration (10 mg/L). The mean Draize eyeirritation score of the gel on rabbit cornea was within non-stimulation,and there was no abnormal change in rabbit (No.2018001) corneal histology. CONCLUSIONS : Prepared Ligustrazine opthalmic liposome thermosensitive gel has a suitable phase transition temperature ,good corneal permeability ,and low corneal irrit ation.

4.
Acta Pharmaceutica Sinica ; (12): 3252-3260, 2021.
Article in Chinese | WPRIM | ID: wpr-906843

ABSTRACT

Drug combination can effectively enhance the anti-tumor effect, reduce the drug dose, and improve medication safety. The use of nano-carrier for drug co-delivery can effectively avoid the differences in drug delivery behavior in vivo. Triptolide and celastrol are the main anti-tumor active components of Tripterygium wilfordii Hook f. Modern studies have shown that the combination of triptolide and celastrol can significantly enhance the antitumor effect, but they are limited by poor water solubility and low tumor tissue delivery rate. In this study, a biomimetic erythrocyte membrane liposome co-loaded with triptolide and celastrol was prepared to characterize the morphology, particle size, potential, drug release, serum stability, and other properties. The immunogenicity, uptake behavior, and anti-cell proliferation ability of the biomimetic liposome was compared. All the animal experiments were carried out in accordance with protocol evaluated and approved by the Ethics Committee of Chengdu University of Traditional Chinese Medicine (Chengdu, China). The results showed that the biomimetic erythrocyte membrane liposome co-loaded with triptolide and celastrol (C+T/RBCm@Lip) in this study had an average particle size of 119.12 ± 2.78 nm and a spherical "core-shell" structure. The zeta potential value was -16.9 ± 1.2 mV, and the drug release behavior in vitro was slow. In addition, the process of coating the cell membrane maintained the characteristics of erythrocyte membrane protein, had good stability in serum, and could effectively avoid the recognition and clearance of macrophages, without causing immunogenicity in vivo. The uptake effect of co-loaded biomimetic liposomes on HepG2 hepatocellular carcinoma cells was enhanced compared with that of uncoated cell membrane liposomes, and the inhibitory effect on proliferation of HepG2 cells was enhanced. In conclusion, the biomimetic liposomes coated with erythrocyte membrane prepared in this study is beneficial to the anti-tumor delivery of triptolide and celastrol, and could enhance the inhibitory effect on the growth of HepG2 liver cancer cells, providing a new idea for the anti-tumor application of Tripterygium wilfordii Hook f.

5.
Article in Chinese | WPRIM | ID: wpr-906258

ABSTRACT

The pathogenesis of metabolic syndrome (MS) includes insulin resistance (IR), central obesity, chronic low-grade inflammation, oxidative stress, endoplasmic reticulum stress, elevated free fatty acid levels, intestinal flora imbalance, renin angiotensin system abnormality, and autophagy activity deficiency, etc. Most researchers believe that IR plays a central role in the pathogenesis of MS, and abdominal obesity is an important initial factor of MS. According to the incidence and clinical characteristics, MS is classified as "obesity" "pidan" " abdominal fullness " and other diseases. It is said that the pathogenesis of MS is related to the deficiency of spleen and kidney, the formation of phlegm, turbidity, blood stasis and other pathological products, which damage the body's functions of qi, blood, yin and yang. Traditional Chinese medicine (TCM) has unique advantages in treating MS based on the holistic view and syndrome differentiation concept. It has multi-level, multi-target and multi-channel treatment characteristics. It can intervene insulin signal transduction, regulate adipocyte factor secretion level, relieve oxidative stress and endoplasmic reticulum stress response, regulate intestinal flora and renin angiotensin system, reduce free fatty acid level and regulation Autophagy and other ways to improve chronic low-grade inflammation and IR status, and then comprehensive prevention and treatment of MS and its complications. However, the following problems still exist:lack of high-quality randomized controlled clinical research and large sample real-world research, clinical unified diagnosis and treatment standard has not yet formed, lack of genetic animal model in basic research, relatively single signal pathway and target of experimental research, and difficulty in timely formation of clinical transformation of scientific research achievements. Therefore, we should make full use of modern scientific and technological means to carry out systematic and standardized multicenter, large sample, high-quality randomized controlled trials or real-world research, we should prepare perfect animal models, focus on the crosstalk relationship between multiple related cell signaling pathways, and actively explore the potential relationship between signaling pathways and prescription compatibility, so as to actively promote basic scientific research achievements Clinical practice may be the key research direction in the prevention and treatment of MS in TCM.

6.
Article in Chinese | WPRIM | ID: wpr-886503

ABSTRACT

@#Objective    To analyze the correlation between the gray value of epicardial fat and the prognosis of patients with atrial fibrillation (AF) treated by thoracoscopic radiofrequency ablation. Methods    The clinical data of 97 patients, including 75 males and 22 females with an average age of 57.8±9.4 years, who underwent thoracoscopic radiofrequency ablation in Fuwai Hospital from 2017 to 2018 were analyzed retrospectively. The left atrial fat volume and average gray scale were calculated by left atrial enhanced CT. According to the average gray scale of left atrial fat tissue, the patients were divided into three groups: a high gray scale group, a medium gray scale group and a low gray scale group. The patients were followed up at 3, 6 and 12 months after operation. The end point of follow-up was the recovery rate of sinus rhythm. Survival analysis was used to analyze the correlation between CT features of epicardial fat enhancement and prognosis. Results    After adjustment of body mass index, body surface area, gender and left atrial end diastolic diameter, regression analysis showed that the fat gray of left atrial enhanced CT was correlated with the type of AF (OR=0.30, 95%CI 0.12-0.79, P=0.014). Cox regression analysis showed that the fat gray value of left atrial CT predicted the recurrence of AF after thoracoscopic radiofrequency ablation (OR=0.92, 95%CI 0.85-0.99). The Kaplan-Meier curve showed significant difference in the long-term recurrence rate of AF among the three groups (P=0.011). The lower left atrial fat enhanced CT gray scale was, the higher long-term recurrence rate of AF was. Conclusion    The gray value of left atrial fat enhanced CT can effectively predict the recurrence of AF after radiofrequency ablation in thoracoscopic surgery.

7.
Article in Chinese | WPRIM | ID: wpr-872938

ABSTRACT

Metabolic syndrome (MS) is a pathological condition characterized by central obesity, insulin resistance, hypertension, and hyperlipidemia. With the increase of poor dietary habits and lifestyles in modern society, especially the poor living habits of sedentariness and less movement, the prevalence of MS has increased year by year. According to relevant data, the number of MS patients worldwide will reach about 2.568 billion by 2040, which will seriously endanger human life and health. Huanglian Wendantang, as a famous traditional Chinese medicine prescription for clearing away heat and drying dampness, regulating Qi and resolving phlegm, and benefiting the stomach and gall, has been proved to have significant pharmacological effects in lowering blood fat, reducing blood sugar and resisting inflammation by modern pharmacological studies, and widely used in the treatment of metabolic diseases, cardiovascular diseases and other systemic diseases. In recent years, a large number of studies have proved that Huanglian Wendantang has a significant effect on MS. In terms of clinical efficacy, it could significantly improve the pathological state of obesity, dyslipidemia, abnormal glucose metabolism and hypertension in MS patients. Meanwhile, it could also interfere with the inflammatory state, prethrombotic state, abnormal vascular regulation and other potential risk factors in the body, with a high safety and fewer side effects. In terms of experimental study, it could enhance the insulin sensitivity, and improve the insulin resistance of MS animal models and cell models through interventions in insulin signal transduction, inflammatory response, and antioxidant stress. By retrieving PubMed, CNKI, Weipu, Wanfang and other databases, the author summarized the study reports of Huanglian Wendantang on MS in recent years in three aspects: theoretical study, clinical efficacy study and experimental mechanism study, in the expectation of provide some scientific references for in-depth study of the mechanism of Huanglian Wendantang in treating MS and the development and clinical promotion of the prescription.

8.
Journal of Experimental Hematology ; (6): 1912-1918, 2019.
Article in Chinese | WPRIM | ID: wpr-781519

ABSTRACT

OBJECTIVE@#To explore the effect of the expression regulation of mitotic control protein DIS3 on the proliferation ability of 3 cell Lines of human myeloma.@*METHODS@#Human myeloma cell lines NCI-h929, RPMI 8226 and U266B1 were selected as study objects, and the over-expression vector of DIS3 gene and DIS3-siRNA were designed and constructed, respectively. The cell experiments were divided into 5 groups: control, DIS3 over-expression-empty vector, DIS3-siRNA negative control, DIS3 over-expression and DIS3-siRNA group. After culture for 24 h, 48 h and 72 h, the proliferation capacity of these three cell lines was measured by MTT assay. And cell samples were collected after culture for 72 h, the expression of proliferation cell nuclear antigen (PCNA) was detected by RT-qPCR and Western blot.@*RESULTS@#MTT assay results showed that the proliferation capacity of cells in DIS3 over-expression group was significantly reduced, as compared with the DIS3 over-expression-empty vector group at the same time point (24, 48 or 72 h) (P<0.05, P<0.01). Compared with DIS3-siRNA negative control group at the same time point (24, 48 or 72 h), the proliferation capacity of cells in the DIS3-siRNA group significantly increased (P<0.05, P<0.01). The results of RT-qPCR and Western blot showed that the mRNA and protein expression levels of PCNA in cells of DIS3 over-expression group were significantly reduced, as compared with DIS3 over-expression empty vector group (P<0.01). Compared with the DIS3-siRNA negative control group, the mRNA and protein expression of PCNA in the cells of DIS3-siRNA group very significantly increased (P<0.01).@*CONCLUSION@#Over expression of DIS3 can significantly reduce the proliferation ability of 3 cell lines of human myeloma, which may be closely related with reducing PCNA expression.


Subject(s)
Cell Line, Tumor , Cell Proliferation , Exosome Multienzyme Ribonuclease Complex , Humans , Multiple Myeloma , RNA, Small Interfering , Transfection
9.
Article in Chinese | WPRIM | ID: wpr-774549

ABSTRACT

Based on the fact that glycyrrhizic acid can form micelles in aqueous solution and play a role in solubilization, the optimal compatibility ratio between puerarin and glycyrrhizic acid was screened to prepare puerarin-glycyrrhizic acid dispersible tablets and investigate the dissolution of puerarin. The particle size, Zate potential and puerarin dissolution were compared among the micellar solutions with mass ratio of 7∶1, 6∶1, 5∶1, 4∶1, 3∶1 and 2∶1(puerarin to glycyrrhizic acid), and it was found that when the mass ratio of puerarin and glycyrrhizic acid was 5∶1, the micelle showed smallest particle size, uniform distribution, and largest puerarin dissolution, so mass ratio of 5∶1 was determined as the optimal condition. The formulation of puerarin-glycyrrhizic acid dispersible tablets was optimized by single factor and orthogonal test: puerarin 100.0 mg, glycyrrhizin 20.0 mg, polyvinylpolypyrrolidone 24.0 mg as disintegrating agent, microcrystalline cellulose 135.0 mg as stuffing bulking agent, hydroxypropyl methyl cellulose 18.0 mg as adhesive agent, magnesium stearate 2.7 mg as lubricant, and tablet weight of 300.0 mg. High-performance liquid chromatography(HPLC) method was used to determine the content of puerarin in dispersible tablets. Puerarin showed a good linear relationship(r=0.999 8) in the range of 15.5-248 g·L~(-1), with high precision(RSD<2.0%) and good repeatability(RSD<2.0%), and the recovery rate was 101.1%, RSD 0.89%. There was no significant difference in the quantity of puerarin in different batches of puerarin-glycyrrhizic acid dispersible tablets. When the artificial gastric juice was used as the dissolution medium, the dissolution of puerarin in puerarin-glycyrrhizic acid dispersible tablets could reach over 85% within 15 min. When phosphate buffer(pH 6.8) was used as the dissolution medium, the dissolution of puerarin in the puerarin-glycyrrhizic acid dispersible tablets had a faster dissolution rate in vitro, 99.8% in 30 min. Therefore, puerarin-glycyrrhizic acid dispersible tablets could improve the dissolution of puerarin in vitro due to the solubilization effect of glycyrrhizic acid.


Subject(s)
Glycyrrhizic Acid , Chemistry , Isoflavones , Chemistry , Solubility , Tablets
10.
China Pharmacy ; (12): 1459-1464, 2019.
Article in Chinese | WPRIM | ID: wpr-816906

ABSTRACT

OBJECTIVE: To prepare puerarin microemulsion with phase Ⅰ metabolic regulation (R-PR-ME) and to study pharmacokinetic characteristics of rats in vivo. METHODS: R-PR-ME and Puerarin microemulsion without metabolic regulation (NR-PR-ME) were prepared by Shah method. Pseudo-ternary phase diagram was used to optimize microemulsion formula using drug loading amount as index. The particle size and PDI of microemulsion were characterized by using a laser particle size analyzer. Rats were used as animal models, and HPLC method was used to determine the blood concentration of puerarin before and 5, 10, 15, 20, 30, 45, 60, 90, 120, 180, 240, 360, 480, 600 min after intragastric administration of R-PR-ME, NR-PR-ME and puerarin suspension (PR-SP) at puerarin dosage of 120 mg/kg. The pharmacokinetic parameters were calculated by using DAS 2.0 software. SPSS 19.0 software was used for statistical analysis. The relative bioavailability of R-PR-ME was calculated with NR-PR-ME as reference preparation. RESULTS: The formula of R-PR-ME included that oleoyl polyoxyl-6 glyserides (oil phase)-polysorbate 20 (emulsifier)-glycerides (co-emulsifier) mass ratio of 2 ∶ 4 ∶ 4; drug-loading amount of 67.50 mg/g, particle size was (22.59±0.53) nm (n=3) and PDI was 0.182±0.017 (n=3). The formula of NR-PR-ME included that soybean oil (oil phase)-polysorbate 80 (emulsifier)- glycerol (co-emulsifier) mass ratio of 1 ∶ 4.5 ∶ 4.5, drug-loading amount of 61.32 mg/g, particle size of (15.45±1.06) nm(n=3) and PDI of 0.156±0.012 (n=3). Pharmacokinetic parameters of R-PR-ME, NR-PR-ME and PR-SP included that AUC0-600 min were (134.187±37.152), (65.145±18.762) and (49.623±12.143) μg·min/mL; cmax were (1.316±0.306), (1.082±0.294) and (0.425±0.106) μg/mL; MRT were (155.068±33.204), (100.264±27.683), (60.524±14.086) min; t1/2β were (365.880±101.250), (283.280±80.940), (80.063±21.189) min (n=6), respectively. Compared with PR-SP, AUC0-600 min, cmax, MRT and t1/2β of R-PR-ME and NR-PR-ME were increased significantly (P<0.05 or P<0.01). Compared with NR-PR-ME, AUC0-600 min, MRT and  t1/2β of R-PR-ME were more higher (P<0.05). The relative bioavailability of of R-PR-ME was 205.98%. CONCLUSIONS: R-PR-ME is prepared successfully with high drug-loading amount, and can significantly increase the bioavailability of puerarin in rats, compared with PR-SP and NR-PR-ME.

11.
Basic & Clinical Medicine ; (12): 361-369, 2018.
Article in Chinese | WPRIM | ID: wpr-693903

ABSTRACT

Objective To study the protective effect of the sodium selenite and benazepril on renal interstitial fibro-sis(RIF) in rat model of unilateral ureteral obstruction(UUO) and its mechanism. Methods The male SD of clean grade rats were randomly divided into sham-operation group,UUO group(UUO model was established by li-gating unilateral ureter), UUO+ sodium selenite group group(sodium selenite 0.2 mg/kg·d gavage), UUO+benazepril group(benazepril 10 mg/kg·d gavage),with 18 in each group.At day 7,14 and 21 after thetreatment, 6 rats selected randomly from each group were killed.The extent of RIF was evaluated by HE and Masson staining of the renal tissue. The expression of connective tissue growth factor(CTGF),transforming growth factor-β1(TGF-β1), alpha smooth muscle actin(α-SMA) andⅢ collagen(ColⅢ) were detected by immunohistochemical method.The protein expression of CTGF and TGF-β1 were detected by Western blot. Chemical colorimetric method was used to detecte the contents of supper oxide dismutase (SOD),malondialdehyde (MDA) and glutathione peroxidase (GSH-px) in renal cortex. Results The extent of RIF and the expression of CTGF,TGF-β1,α-SMA and ColⅢin renal cortex were significantly lower in sodium selenite group and benazepril group at day 7,14 and 21 after the op-eration compared with that in UUO group(P<0.05 or P<0.01). In sodium selenite group and benazepril group,the contents of SOD and GSH-px in renal cortex were higher significantly than those in UUO group at day 7,14 and 21 after the operation respectively(P<0.05),but the MDA in renal cortex was significantly decreased(P<0.05).There were no significant differences in the indexes between the two groups of sodium selenite and benazepril. The expres-sion of CTGF,TGF-β1,α-SMA,ColⅢand the extent of RIF were positively correlated to the level of MDA in UUO group(P<0.05,respectively),and negatively correlated to the level of SOD and GSH-Px(P<0.05,respectively). The expression of CTGF was positively correlated to the expression of α-SMA and ColⅢin UUO group(P<0.05).The expres-sion of CTGF,α-SMA and ColⅢwere positively correlated to RIF in UUO group(P<0.05).Conclusions Sodium sele-nite and benazepril can reduce the extent of RIF in rat model with unilateral ureteral obstruction.

12.
National Journal of Andrology ; (12): 199-205, 2018.
Article in Chinese | WPRIM | ID: wpr-689777

ABSTRACT

<p><b>Objective</b>To explore the inhibitory effect of polyphyllin Ⅰ (PPⅠ) on the proliferation of castration-resistant prostate cancer PC3 cells and its molecular mechanism.</p><p><b>METHODS</b>We cultured human prostate cancer PC3 cells in vitro and treated them with PPⅠ at the concentrations of 0 (blank group), 0.4, 0.8, 1.2, 1.6, 2.0, and 2.4 μmol/L for 24, 48, and 72 hours, respectively. Then we detected the proliferation of the cells by MTT assay, measured their apoptosis by flow cytometry, and determined the expressions of p-ERK1/2, ERK1/2, NF-κB/p65 and DNMT1 proteins as well as the level of NF-κB/p65 in the cells additionally treated with the ERK1/2 inhibitor SP600125 by Western blot.</p><p><b>RESULTS</b>Compared with the blank control group, the PPⅠ-treated PC3 cells showed a concentration- and time-dependent reduction of the survival rate (1.00 ± 0.00 vs 0.85 ± 0.05, P < 0.01) at 0.4 μmol/L after 48 hours of intervention, concentration-dependent early apoptosis at 0.8 μmol/L (4.83 ± 0.95 vs 13.83 ± 2.97, P < 0.01), time-dependent increase of the expressions of p-ERK1/2 (1.00 ± 0.00 vs 1.73 ± 0.17, P < 0.01) and ERK1/2 (1.00 ± 0.00 vs 1.36 ± 0.12, P < 0.01) at 2 hours, and concentration-dependent decrease of the expressions of NF-κB/p65 and DNMT1 at 1.2 μmol/L (1.00 ± 0.00 vs 0.78 ± 0.10 and 0.63 ± 0.06, P < 0.01) and 1.6 μmol/L (1.00 ± 0.00 vs 0.67 ± 0.11 and 0.52 ± 0.09, P<0.01). Inhibition of ERK1/2 phosphorylation with PD98059 markedly reversed PPⅠ-induced decrease of the NF-κB/p65 expression as compared with that in the PPⅠ group (0.86 ± 0.18 vs 0.43 ± 0.09, P < 0.05).</p><p><b>CONCLUSIONS</b>PPⅠ induces the early apoptosis and suppresses the proliferation of PC3 cells, probably by activating the ERK1/2 pathway and inhibiting the expressions of the NF-κB/p65 and DNMT1 proteins.</p>


Subject(s)
Apoptosis , Cell Proliferation , DNA (Cytosine-5-)-Methyltransferase 1 , Metabolism , Diosgenin , Pharmacology , Flavonoids , Metabolism , Humans , MAP Kinase Signaling System , Male , Mitogen-Activated Protein Kinase 1 , Metabolism , Mitogen-Activated Protein Kinase 3 , Metabolism , NF-kappa B , Metabolism , PC-3 Cells , Phosphorylation , Prostatic Neoplasms, Castration-Resistant , Drug Therapy , Metabolism , Pathology , Signal Transduction , Transcription Factor RelA , Metabolism
13.
Chinese Traditional Patent Medicine ; (12): 1083-1087, 2018.
Article in Chinese | WPRIM | ID: wpr-710273

ABSTRACT

AIM To establish the UPLC fingerprints of Gegen Qinlian Pills (Puerariae lobatae Radix,Scutellariae Radix,Coptidis Rhizoma and Glycyrrhizae Radix et Rhizoma Praeparata cum Melle) and to determine the contents of puerarin,baicalein,palmatine,wogonin,daidzin,daidzein and jateorhizine.METHODS The analysis of 70% methanol extract of this drug was performed on a 30 ℃ thermostatic Waters ACQUITY UPLC(C) BEH C18column,with the mobile phase comprising of methanol-0.1% glacial acetic acid flowing at 0.3 mL/min in a gradient manner,and the detection wavelength was set at 260 nm.RESULTS There were twenty-five common peaks in the fingerprints of ten batches of samples with the similarities of more than 0.98.Seven constituents showed good linear relationships within their own ranges (r > 0.999 0),whose average recoveries were 98.99%-103.6% with the RSDs of 1.13%-2.03%.CONCLUSION This simple,reliable and reproducible method can be used for the quality control of Gegen Qinlian Pills.

14.
China Pharmacy ; (12): 902-905, 2017.
Article in Chinese | WPRIM | ID: wpr-511508

ABSTRACT

OBJECTIVE:To explore the effects of the different compatibility ratios of rutin with quercetin on the pharmacoki-netics of rutin in rats in vivo. METHODS:30 rats were randomly divided into rutin group(rutin-quercetin molar ratio of 4:0,the same below),quercetin group(rutin-quercetin ratio of 0:4),BL1 group(rutin-quercetin ratio of 3:1),BL2 group(rutin-quercetin ratio of 2:2)and BL3 group(rutin-quercetin ratio of 1:3),6 rats in each group,all group was administrated 10 mg/kg(calculat-ed by quercetin core of rutin and quercetin) intragastrically. The blood sample 0.3 mL was respectively taken from tail vein after 0.25,0.5,0.75,1,1.5,2,3,4,6,8,10,12,16,20,24 h of administration,the plasma concentration of quercetin(rutin me-tabolite) was determined by HPLC. DAS 2.0 software was used to calculate the pharmacokinetic parameters. RESULTS:The AUC0-24 h in rutin group,quercetin group,BL1 group,BL2 group and BL3 group were (4.908 ± 0.877),(8.382 ± 3.671), (8.473 ± 0.709),(4.366 ± 2.297),(8.914 ± 2.642)μg·h/L;MRT0-24 h were (9.675 ± 1.359),(3.142 ± 0.489),(3.517 ± 1.128), (3.376 ± 1.046),(4.494 ± 1.653) h;tmax were (5.726 ± 5.645),(1.375 ± 0.703),(1.125 ± 1.438),(1.417 ± 2.300),(1.292 ± 0.954) h;and cmax were (0.609 ± 0.202),(2.341 ± 0.539),(2.425 ± 1.217),(1.464 ± 0.677),(3.325 ± 2.425)μg/L. Compared with rutin group,AUC0-24 h and cmax in quercetin group,BL1 group and BL3 group were significantly increased(P0.05). CONCLUSIONS:Quercetin can inhance the related indexes of rutin in rats in vivo.

15.
Article in English | WPRIM | ID: wpr-819474

ABSTRACT

OBJECTIVES@#To discuss the association between FGFR4 gene polymorphism rs351855 (Glu388Aly) and the susceptibility and chemotherapeutic effect of cervical cancer infected by high-risk type HPV.@*METHODS@#A total of 162 patients with high-risk HPV cervical cancer and 162 healthy women were collected and the genotypes of the FGFR4 rs351855 locus were detected. The genotype distributions in the two groups were compared. The cervical cancer patients were divided into four groups which namely good therapeutic effect group and bad therapeutic effect, recurrence or metastasis and no recurrence or metastasis group respectively, and the risks of different genotype on the curative effect and prognosis were analyzed by Logistic regression. The survival time of patients with different genotypes was compared.@*RESULTS@#There was no statistic difference in FGFR4 rs351855 genotype distribution between the patients group and control group (P > 0.05), among which the risk of chemotherapy failure on GA + AA patients was 3.257 times as much as that of the GG patients, and the risk of recurrence or metastasis of GA + AA patients was 2.783 times as much as that of the GG patients. For AA patients, the risk of chemotherapy failure and the risk of relapse and metastasis are 3.833 and 3.406 times, respectively, as much as that of the GG patients. The overall survival of GA and AA patients was shorter than that of the GG patients, and significant difference was found (χ = 7.098, P = 0.029). The difference in overall survival between GA + AA patients and GG patients was almost statistically significant (χ = 3.634, P = 0.057).@*CONCLUSIONS@#The FGFR4 rs351855 polymorphism is not associated with the susceptibility of high-risk HPV cervical cancer, but patients with gene A was at higher risk of unfavorable chemotherapy prognosis compared with patients with GG.

16.
China Pharmacy ; (12): 2134-2137, 2017.
Article in Chinese | WPRIM | ID: wpr-614498

ABSTRACT

OBJECTIVE:To establish a method for simultaneous determination of residual methylparaben,ethylparaben,nipa-sol and benzalkonium chloride in marketed eye drops. METHODS:HPLC method was adopted. The determination was performed on Hypersil GOLD C18 column with mobile phase consisted of 0.005 mol/L ammonium acetate(10 mL triehtylamine in 1 L solu-tion,pH adjusted to 5.0±0.5 with glacial acetic acid)-acetonitrile(45:55,V/V)at the flow rate of 1.0 mL/min. The detection wave-length was 262 nm(methylparaben,ethylparaben,nipasol)and 214 nm(benzalkonium chloride),respectively. The column tem-perature was 30 ℃ and sample size was 20 μL. RESULTS:The linear range were 1.2350-15.4380 μg/mL for methylparaben(r=0.9999),1.3170-16.3836 μ g/mL for ethylparaben (r=0.9997),1.2072-15.0894 μ g/mL for nipasol (r=0.9996) and 17.776-222.0 μg/mL for benzalkonium chloride(r=0.9999),respectively. Limits of quantitation were 2.0,2.0,2.0,1.11 μg,re-spectively;limits of determination were 0.375,0.375,0.375,0.333 μg,respectively. RSDs of precision,stability and reproducibili-ty tests were all lower than 2.0%. The average recoveries were 98.14%-102.48%(RSD=1.6%,n=9),98.79%-102.42%(RSD=1.3%,n=9),98.19%-102.49%(RSD=1.5%,n=9)and 98.76%-100.53%(RSD=0.6%,n=9),respectively. CONCLUSIONS:The method is accurate,reproducible,simple and suitable for the determination of residual methylparaben,ethylparaben,nipasol and benzalkonium chloride in marketed eye drops.

17.
Article in Chinese | WPRIM | ID: wpr-320872

ABSTRACT

To prepare ginsenoside-Rh₂ lipid nanoparticles, and investigate the synergistic effect with borneol in resisting tumor activity in vitro. Ginsenoside-Rh₂ lipid nanoparticles were prepared by ultrasonic-assisted solvent evaporation method, and orthogonal design was adopted to optimize formulation process. Its encapsulation efficiency, drug loading ratio, particle size distribution, Zeta potential, morphology and in vitro drug release behavior were characterized, and synergistic effect with borneol in resisting tumor activity were preliminarily studied by MTT. These nanoemulsion particles prepared by the optimized process method were rounding and even in a good shape. Encapsulation efficiency and drug loading ratio of three batches of nanoemulsion particles were (77.3±2.5)% and (7.2±0.2)%, respectively. Nanoemulsion particles showed an obvious sustained release characteristics, with 52.42% cumulative release within 96 h. The killing effect of nanoemulsion particles on glioma cells was dose-dependent, with IC₅₀ of 22.33 μmol•L⁻¹ and 11.46 μmol•L⁻¹ after 24 h and 48 h, respectively. After the combination with borneol, the killing effect of nanoemulsion particles on glioma cells was dose-dependent, with IC₅₀ of 16.36 μmol•L⁻¹ and 8.04 μmol•L⁻¹ after 24 h and 48 h, respectively.

18.
Article in Chinese | WPRIM | ID: wpr-236089

ABSTRACT

To investigate the effect of Fuke Qianjin tablets on the pharmacokinetics of Azithromycin(AZM) in rats with chronic pelvic inflammation, and evaluate the rationality of the drug combination. The animal models of chronic pelvic inflammatory disease were established by intrauterine injection of mixed bacterial suspension plus mechanic injury in female Sprague-Dawley(SD) rats. The model rats were randomly divided into control group and drug combination group. The rats in control group were given with Azithromycin 10 mg•kg⁻¹•d⁻¹ by intragastric administration, while the rats in drug combination group were given with Fuke Qianjin tablets 1.66 g•kg⁻¹•d⁻¹ by intragastric administration 2 hours after the equivalent dose of azithromycin, once a day, consecutively for 7 days. Plasma samples were collected at different time points and the concentration of AZM in plasma was determined by high performance liquid chromatography coupled with mass spectrometry(HPLC-MS). ADAPT 5.1 software was used to calculate the pharmacokinetic parameters of each group by Inverse Gaussian Function model. SPSS software was used for the statistical analysis of data in each group. The results showed that Fuke Qianjin tablets had no significant effects on the main pharmacokinetic parameters of AZM, including CLt, CLd, MIT and F. The study showed that Fuke Qianjin tablets can be combined with azithromycin for treatment of chronic pelvic inflammation disease.

19.
Article in English | WPRIM | ID: wpr-242832

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of propofol on brain regions at different sedation levels and the association between changes in brain region activity and loss of consciousness using blood oxygen level-dependent functional magnetic resonance imaging (BOLD-fMRI) and bispectral index (BIS) monitoring.</p><p><b>METHODS</b>Forty-eight participants were enrolled at Peking Union Medical College Hospital from October 2011 to March 2012 and randomly assigned to a mild or a deep sedation group using computer- generated random numbers. Preliminary tests were performed a week prior to scanning to determine target effect site concentrations based on BIS and concomitant Observer's Assessment of Alertness/Sedation scores while under propofol. Within one week of the preliminary tests where propofol dose-response was established, BOLD-fMRI was conducted to examine brain activation with the subject awake, and with propofol infusion at the sedation level.</p><p><b>RESULTS</b>Mild propofol sedation inhibited left inferior parietal lobe activation. Deep sedation inhibited activation of the left insula, left superior temporal gyrus, and right middle temporal gyrus. Compared with mild sedation, deep propofol sedation inhibited activation of the left thalamus, precentral gyrus, anterior cingulate, and right basal nuclei.</p><p><b>CONCLUSION</b>Mild and deep propofol sedation are associated with inhibition of different brain regions, possibly explaining differences in the respective loss of consciousness processes.</p>


Subject(s)
Adult , Brain , Consciousness Monitors , Deep Sedation , Dose-Response Relationship, Drug , Humans , Hypnotics and Sedatives , Pharmacology , Male , Propofol , Pharmacology
20.
Article in Chinese | WPRIM | ID: wpr-330254

ABSTRACT

<p><b>OBJECTIVE</b>To study the alkaloids of Macleaya cordata and their anti-tumor activities.</p><p><b>METHOD</b>Alcohol and liquid-liquid extraction were used methods were used to extract the alkaloids constituents, and silica gel, reverse-phase octadecylsilyl (ODS), sephadex LH-20 chromatographic methods and HPLC were applied to isolate and purify compounds. MS, NMR spectroscopic methods were used to determine their structures. Furthermore, the cytotoxicity of these chemical components for MCF-7 and SF-268 cell lines was measured by MTT method.</p><p><b>RESULT</b>Twelve alkaloids were isolated from the fruits of M. cordata, and their structures were identified as: maclekarpine E (1), 6-acetonyldihyrochelerythrine (2), cavidilinine (3), 6-acetonyldihyrosanguinnarine (4), O-methylzanthoxyline (5), 6-methoxy-dihydrosanguinarine (6), spallidamine (7), 6-hydroxyldihydrochelerythrine (8), arnotianamida (9), dihydrosanguinarine (10), protopine (11), and cryptopine (12).</p><p><b>CONCLUSION</b>Compounds 1, 3, 7-9 were isolated from M. cordata for the first time, and compound 5 is a new natural product. The results of cytotoxic assay indicated that compound 6 showed strong cytotoxicity against MCF-7 and SF-268 cell lines with IC50 values of 0.61 μmol · L(-1) and 0.54 μmol · L(-1), respectively.</p>


Subject(s)
Alkaloids , Pharmacology , Antineoplastic Agents, Phytogenic , Cell Line, Tumor , Humans , Papaveraceae , Chemistry
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