3. UPLC-MS/MS-based pharmacokinetics of self-microemulsion containing total flavonoids from Sophora flavescens in rats
Chinese Traditional and Herbal Drugs 2019;50(20):5018-5025
Objective: To establish a UPLC-MS/MS method for simultaneous determination of sophoraflavanone G (SFG), kurarinone (Kur), and isoxanthohumol (Iso) in rat plasma using rutin as the internal standard (IS), and to study the pharmacokinetic parameters of total flavonoids (TF) from Sophora flavescens and TF self-microemulsion drug delivery system (TF-SMEDDS) in rats. Methods: Analysis was carried out on an ACQUITY UPLC® HSS T3 C18 column using acetonitrile-0.1% formic acid in water as the mobile phase at a flow rate of 0.2 mL/min. The plasma samples were prepared by liquid-liquid extraction with ethyl acetate. The detection was performed on a triple quadrupole tandem mass spectrometer by multiple reaction monitoring with an electro-spray ionization source in negative ionization mode. All statistical analysis was performed using DAS 2.0 software package. Results: The calibration curves of Kur, SFG, and Iso exhibited good linearity (r2 > 0.995 9) over the range of (0.02-1 600.00), (0.015-1 200.000), and (0.01-800.00) ng/mL, respectively. Precision, accuracy, average extraction recovery, and matrix effects were all in line with biological sample analysis requirements. The pharmacokinetic parameters of Kur, SFG, and Iso from TF were as follows: t1/2z (7.04 ±2.46), (4.54 ± 2.13), (4.73 ± 1.67) h, and AUC0-∞ (3 469.57 ± 555.37), (2 524.48 ± 425.83), (1 006.47 ± 85.46) ng∙h/mL. The pharmacokinetic parameters of Kur, SFG, and Iso from TF-SMEDDS were as follows: t1/2z (13.10 ± 2.67), (11.47 ± 4.17), and (12.67 ± 4.97) h, and AUC0-∞ (13 002.49 ± 2 498.09), (8 070.80 ± 2 264.62), (3 918.85 ± 429.76) ng∙h/mL. The relative bioavailabilities of Kur, SFG, and Iso in TF-SMEDDS were approximately 374.76%, 319.70%, and 389.37%, respectively. Conclusion: The UPLC-MS/MS method can be used to study the pharmacokinetics of three components in S. flavescens in rats. The bioavailability of TF-SMEDDS in rats was significantly increased.
4.Effect of injection with hepatocyte growth factor on angiogenesis in myocardium of dogs with myocardial ischemia
Qiaoying YUAN ; Jing HUANG ; Xuejun LI ; Liangyi SI
Journal of Third Military Medical University 2003;0(13):-
Objective To study the molecular mechanism of injection with hepatocyte growth factor (HGF) at different doses on angiogenesis in myocardium of dogs with acute myocardial infarction (MI).Methods Sixteen 1.5-year-old male hybrid dogs,weighing 11-13 kg,were divided into 500 ?g HGF treatment group,1 000 ?g HGF treatment group,sham operation group,and no MI interference group,4 dogs in each group.Expressions of VEGF,HGF,CD31,and platelet factor Ⅷ in myocardium of dogs with MI were detected,the number of micro blood vessels was calculated,and correlation between angiogenesis and expression of HGF and VEGF was analyzed in 28 d after the model was established.Results HGF gene therapy could up-regulate the expression of CD31 and VEGF.The expression of CD31 and VEGF mRNA was 0.82 and 0.39 respectively in 1 000 ?g HGF group,and 0.47 and 0.21 respectively in 500 ?g HGF group.The expression of VEGF mRNA was 0.09 and no expression of CD31 mRNA was found in MI group.HGF could increase the angiogenesis in infracted myocardium.The microvascular density was 126.4?10.6,79.8?6.0,and 21.7?2.5/mm2,respectively,in 1 000 ?g HGF group,500 ?g HGF group,and MI group (P
5.Effect of simvastatin on RhoA expression and cardiac remodeling with in acute myocardiac infarction rats
Qiaoying YUAN ; Shu QIN ; Liangyi SI ; Xuejun LI
Journal of Third Military Medical University 2002;0(12):-
Objective To investigate the effects of simvastatin on the abatement of the mRNA,protein expression of RhoA and the improvement of the cardiac remodeling and cardiac disfunction after the myocardiac infarction in rats.Methods Rats were divided into 3 groups: the control group,the myocardiac infarction group and Simvastatin intervened group.After 8 weeks,cardiac weight index and hemodynamics were observed,mRNA and protein expression of RhoA in cardiac muscles was measured. Results Compared with the control group,the cardiac weight index and the mRNA and protein expression were increased in rats with myocardiac infarction and the hemodynamics was worsened(P
6.Meta-analysis of bifocal lenses for retarding myopia progression in school-aged myopic children
Shi-ming, LI ; Shan-shan, WU ; Si-yan, ZHAN ; Bo, WANG ; Si-yuan, LI ; Feng-ju, ZHANG ; Ning-li, WANG
Chinese Journal of Experimental Ophthalmology 2011;29(6):549-554
Background Whether the wearing of bifocal lenses can delay the development of myopia in school childhood is in controversy.To assess the effect of bifocal lenses using evidence-based medicine method is of important significance.Objective Present study was to compare the effect of bifocal lenses with single vision lenses in retarding myopia progression in school-aged myopic children.Methods This was a evidence-based medicine study.The systematical literature search was performed from MEDLINE(1966 to October 2010),EMBASE(1974 to October 2010),Cochrane Library,Chinese Biomedical Database(1978 to October 2010),and Chinese Clinical Trial Registry combined with hand searching of related bibliographies of journals and books were applied to collect the randomized-controlled clinical trial about bifocal lenses.Screening,evaluation and data extraction of the retrieved literature were performed by two investigators independently.Mata-analysis was used to assess the progression of refraction and axial length among included randomized clinical trials.Results Three high-quality randomized-controlled clinical trials meeting the inclusion criterion were included in this meta-analysis.The results showed that the weighted mean difference in progression of refraction was 0.22D between bifocal lenses and single vision lenses(95% CI:-0.24-0.67),and the difference was statistical insignificance(P=0.35).The weighted mean difference in progression of refraction during the follow-up durations of 6,12,18,24 and >30 months were 0.15(95% CI:-0.09-0.38),0.17(95% CI:-0.05-0.39),0.42(95% CI:-0.14-0.98),0.23(95% CI:-0.21-0.66) and 0.03(95% CI:-0.40-0.46),respectively without statistical significance.The weighted mean difference in elongation of axial length between two interventions was -0.17mm(95% CI:-0.26-0.08) with a statistically significance(P=0.000).Conclusion Based on currently available studies,bifocal lenses could not significantly slow the progression of myopia in myopic school-aged children in comparison with single vision lenses.Because only few high-quality studies are currently available,this conclusion need to be supported by more large-sample-size clinical trials.
7.Biofeedback therapy for chronic prostatitis: Application and consideration.
Si-da CHEN ; Jing LI ; Shen-qing LI ; Li-huan QIAN ; Yuan HE ; Bu-ping LIU
National Journal of Andrology 2016;22(1):57-62
Studies of biological feedback (BF) for the treatment of chronic prostatitis (CP) are occasionally reported have exhibited some related problems. This article presents an evaluation of the published literature on the BF treatment of CP at home and abroad in the aspects of instrument, method, application, effect, function, and mechanism. UROSTYMTM and MyoTrac are often employed and their operating paths are basically the same. NIH prostate symptom scores, urinary function, pain, sexual function, immune function, prostate fluid, and other indicators are generally used for the analysis of the effects of BF alone or in combination with other therapies on CP and its related symptoms. Either BF alone or BF combined with other therapies can promote urination, reduce pain, improve the quality of life, attenuate inflammation, improve sexual function, adjust immunity, and lessen physical and chemical stimulation. However, the relevant literature is of low quantity and quality, the reported studies are not standardized, and exploration of the action mechanisms is neglected.
Biofeedback, Psychology
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Humans
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Male
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Prostatitis
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therapy
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Quality of Life
8.Study on quantitative methods of cleistocalycis operculati cortex.
Li-Si CHEN ; Jia-Ju OU ; Shu-Yuan LI ; Song-Gui LU
China Journal of Chinese Materia Medica 2014;39(16):3128-3130
Cleistocalycis Operculati Cortex is the dry bark of Cleistocalyx operculatus. It is the raw material of Compound Hibiscuse which is external sterilization antipruritic drugs. The quality standard of Cleistocalycis Operculati Cortex in Guangdong Province "standard for the traditional Chinese medicine" (second volumes) only contains TLC identification. It is unable to effectively monitor and control the quality of Cleistocalycis Operculati Cortex. A reversed-phase HPLC method was established for the determination of 3, 3'-O-dimethylellagic acid from Cleistocalycis Operculati Cortex and the content was calculated by external standard method for the first time. Under the selected chromatographic conditions, the target components between peaks to achieve effective separation. 3,3'-O- dimethylellagic acid standard solution at the concentration of 1.00 - 25.0 mg x L(-1) showed a good linear relationship. The standard curve was Y = 77.33X + 7.904, r = 0.999 5. The average recovery was 101.0%, RSD was 1.3%. The HPLC method for the determination of 3,3'-O-dimethylellagic acid in Cleistocalycis Operculati Cortex is accurate and reliable. It can provide a strong technical support for monitoring the quality of Cleistocalycis Operculati Cortex.
Chromatography, High Pressure Liquid
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methods
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Chromatography, Reverse-Phase
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methods
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Drugs, Chinese Herbal
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analysis
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Plant Bark
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chemistry
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Syzygium
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chemistry
9.Development of an LC-MS/MS method for the quantitation of deoxyglycychloxazol in rat plasma and its application in pharmacokinetic study$
Rongshan LI ; Ruixue RAN ; Quansheng LI ; Yurong HUANG ; Yuan GU ; Duanyun SI
Journal of Pharmaceutical Analysis 2016;6(3):184-189
Deoxyglycychloxazol (TY501) is a glycyrrhetinic acid derivative which exhibits high anti-inflammatory activity and reduced pseudoaldosteronism compared to glycyrrhetinic acid. In this study, a sensitive and rapid liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was established for the quantitation of TY501 in rat plasma. Plasma samples were treated by precipitating protein with methanol and supernatants were separated by a Symmetry C8 column with the mobile phase consisting of me-thanol and 10 mM ammonium formate (containing 0.1%of formic acid) (90:10, v/v). The selected reaction monitoring (SRM) transitions were performed at m/z 647.4-191.2 for TY501 and m/z 473.3-143.3 for astragaloside aglycone (IS) in the positive ion mode with atmospheric pressure chemical ionization (APCI) source. Calibration curve was linear over the concentration range of 5–5000 ng/mL. The lower limit of quantification was 5 ng/mL. The mean recovery was over 88%. The intra-and inter-day precisions were lower than 6.0% and 12.8%, respectively, and the accuracy was within 71.3%. TY501 was stable under usual storage conditions and handling procedure. The validated method has been successfully applied to a pharmacokinetic study after oral administration of TY501 to rats at a dosage of 10 mg/kg.
10.Effects of immunostimulatory CpG ODN on experimental allergic conjunctivitis caused by aspergillus fumigatus
Si-yuan, LI ; Ge, ZHAO ; Chang-you, LI ; Ling-ling, YANG ; Hao, CHEN ; Yi-qiang, WANG
Chinese Journal of Experimental Ophthalmology 2011;29(4):308-313
Background Researches demonstrated that CpG ODN,a immunostimulatory sequences,has preventing and treating effect on allergic conjunctivitis caused by protein allergen.However,its effect on allergic conjunctivitis caused by fungal allergen is unclear. Objective This study aimed to investigate into whether the Th1-Th2 switching immunostimulatory CpG ODN could reverse the response in the murine allergic conjunctivitis model caused by aspergillus fumigatus. Methods A mixture of spores and hyphae of aspergillus fumigatus strain was used to induce allergic conjunctivitis in male BALB/C mice aged 6-8 weeks.This experiment was designed into preventive or therapeutical treatment program.Under both settings,allergic conjunctivitis of the animals were treated with CpG ODN,nonstimulatory GpC ODN or PBS.After the last challenge with the allergen,the clinical symptoms of the animals were scored based on the criteria of Magone.The animals were sacrificed and the histopathological examination of conjunctiva was performed.Expression of TLR4 mRNA in conjunctiva was analyzed by real-time PCR assay.The responsiveness and populations of lymphocytes in spleen and draining lymph nodes were analyzed by flow cytometry.The use complied with the Standard of Association for Research in Vision and Ophthalmology. Results In the prevention mode.CpG ODN decreased subconjunctival infiltration compared with GpC ODN and PBS groups with the average neutrophil count index(21.25 ±11.59/section,30.75 ±11.44 section and 69.00±9.90/section,respectively).Expression of TLR4 mRNA was up-regulated significantly by CpG ODN.The clinical scores for CpG ODN group were insignificantly lower than those in GpC ODN group and PBS group(P>0.05).In the therapeutic mode,compared with GpC ODN and PBS groups,the allergic symptom score in CpG ODN group manifested significantly lower(t=4.000.t=2.750,P<0.01)and showed fewer cellular infiltration(t=4.870,t=3.829,P<0.01)and higher expression of TLR4 mRNA(P<0.01).In cultured splenic and draining lymph node cells,increased percentages of CD4+ CD25+ and CD4+ CD25+ CD69+ in CpG ODN group were observed compared with control groups(|P<0.05). Conclusion CpG ODN can relieve aspergillus fumigatus-induced allergic conjunctivitis via either subconjunctival injection or topical application by upregulating expression of TLR4 and activating Treg lymphocytes.