1.Cardioprotection of Shenfu preparata on cardiac myocytes through cytochrome P450 2J3.
Yong XIAO ; Zengchun MA ; Yuguang WANG ; Hongling TAN ; Xiangling TANG ; Qiande LIANG ; Chengrong XIAO ; Yue GAO
Journal of Integrative Medicine 2013;11(5):327-36
To evaluate whether Shenfu injection (SFI) protects against cardiac myocyte injury induced by Fupian injection (FPI) in vitro.
2.Research advances of photosensitizer in photodynamic therapy of glioblastoma
Hong-cheng ZHAO ; Yue-qing WANG ; Qing-yun LI ; Hao DENG ; Xiao TAN ; Xiao-wen LIU
Acta Pharmaceutica Sinica 2022;57(6):1750-1757
Glioblastoma is a malignant tumor in central nervous system, which has strong invasion, poor prognosis and short survival time. At present, the main treatment strategy of glioblastoma is surgical excision, supplemented by radiotherapy and chemotherapy. However, due to incomplete resection and high recurrence rate, it is urgent to find novel therapeutic method for glioblastoma. Photodynamic therapy, as a promising non-surgical treatment, provides a new strategy for postoperative adjuvant therapy of glioblastoma. This review summarizes the mechanism and clinical application of photodynamic therapy mediated by various photosensitizers in glioblastoma, in order to provide help for the treatment of glioblastoma.
3.Circulatory sleep apnea: Preliminary report of clinical observation on sleep apnea in patients with chronic heart failure.
Si-xin XIE ; Xing-guo SUN ; Fu-rong WANG ; Xiao-yue TAN ; Xue-mei ZHANG
Chinese Journal of Applied Physiology 2015;31(4):329-331
OBJECTIVEThe aim of this study is to investigate the occurrence and mechanism of Cheyne-Stokes breathing pattern in patients with heart failure.
METHODSFifty-six patients who performed polusomnography sleep testing at National Center of Cardiovascular Diseases Fuwai Hospital from March to May in 2015. We divided them into chronic heart failure (CHF) group and non-CHF group.
RESULTSThe occurrences of sleep apnea in two groups were high. In CHF group (n = 11) , there were 10 patients with apnea hypopnea index (AHI) > 5; and their AHI was 23.93 ±14.63. In non-CHF group (n = 45), there were 33 patients whose AHI > 5; and their AHI was 16.20 ± 18.76. The ratio of center sleep apnea to all gross sleep apnea ratio in CHF group was higher than that in non-CHF group (80.21% ± 30.55% vs 27.16% ± 35.71%, P < 0.01 ).
CONCLUSIONBased upon the new theory of holistic integrative physiology and medicine, we explain the mechanism of circulatory dysfunction induce the oscillation breathing in patients with CHF. The sleep apnea and C-S respiration in CHF should be called circulatory sleep apnea, rather than central sleep apnea.
Cheyne-Stokes Respiration ; Chronic Disease ; Heart Failure ; physiopathology ; Humans ; Polysomnography ; Sleep Apnea Syndromes ; physiopathology ; Sleep Apnea, Central
4.Investigation of metabolic kinetics and reaction phenotyping of ligustrazin by using liver microsomes and recombinant human enzymes.
Yan TAN ; Xiao-Mei ZHUANG ; Guo-Lin SHEN ; Hua LI ; Yue GAO
Acta Pharmaceutica Sinica 2014;49(3):374-379
The metabolic characteristics of ligustrazin (TMPz) in liver microsomes were investigated in the present study. The reaction phenotyping of TMPz metabolism was also identified by in vitro assessment using recombinant human cytochrome P450 enzymes (CYP) and UDP glucuronosyltransferases (UGT). TMPz was incubated at 37 degrees C with human (HLM) and rat liver microsomes (RLM) in the presence of different co-factors. The metabolic stability and enzyme kinetics of TMPz were studied by determining its remaining concentrations with a LC-MS/MS method. TMPz was only metabolically eliminated in the microsomes with NADPH or NADPH+UDPGA. In the HLM and RLM with NADPH+UDPGA, t1/2, K(m) and V(max) of TMPz were 94.24 +/- 4.53 and 105.07 +/- 9.44 min, 22.74 +/- 1.89 and 33.09 +/- 2.74 micromol x L(-1), 253.50 +/- 10.06 and 190.40 +/- 8.35 nmol x min(-1) x mg(-1) (protein), respectively. TMPz showed a slightly higher metabolic rate in HLM than that in RLM. Its primary oxidative metabolites, 2-hydroxymethyl-3, 5, 6-trimethylpyrazine (HTMP), could undergo glucuronide conjugation. The CYP reaction phenotyping of TMPz metabolism was identified using a panel of recombinant CYP isoforms (rCYP) and specific CYP inhibitors in HLM. CYP1A2, 2C9 and 3A4 were found to be the major CYP isoforms involved in TMPz metabolism. Their individual contributions were assessed b) using the method of the total normalized rate to be 19.32%, 27.79% and 52.90%, respectively. It was observed that these CYP isoforms mediated the formation of HTMP in rCYP incubation. The UGT reaction phenotyping of HTMP glucuronidation was also investigated preliminarily by using a panel of 6 UGT isoforms (rUGT). UGT1A1, 1A4 and 1A6 were the predominant isoforms mediated the HTMP glucuronidation. The results above indicate that the metabolism of TMPz involves multiple enzymes mediated phase I and phase II reactions.
Animals
;
Cytochrome P-450 CYP1A2
;
metabolism
;
Cytochrome P-450 CYP2C9
;
metabolism
;
Cytochrome P-450 CYP3A
;
metabolism
;
Cytochrome P-450 Enzyme Inhibitors
;
Cytochrome P-450 Enzyme System
;
metabolism
;
Drug Interactions
;
Glucuronosyltransferase
;
metabolism
;
Humans
;
Ligusticum
;
chemistry
;
Microsomes, Liver
;
enzymology
;
NADP
;
metabolism
;
pharmacology
;
Pyrazines
;
metabolism
;
pharmacokinetics
;
Rats
;
Uridine Diphosphate Glucuronic Acid
;
metabolism
;
pharmacology
5.Radioprotective effect of E0703 on AHH-1 cells and the related mechanism
Liqun ZHANG ; Zengchun MA ; Yuguang WANG ; Chengrong XIAO ; Hongling TAN ; Minghui YANG ; Yue GAO
Chinese Journal of Radiological Medicine and Protection 2008;28(3):231-235
Objective E0703 is derived from estradiol and has anti-radiation effects on irradiated mice, the effects of E0703 on cell viability,cell cycle and the related mechanism in irradiated AHH-1 cells were investigated in this study.Methods Cell viability,cell apoptosis and cell cycle were determined by Cell Counting Kit-8.Annexin V-FITC double staining kit and Flow Cytometry,respectively.Level of mRNA and protein were detected by RT-PCR and Western blot,respectively.Results 3.0 Gy 60 Co γ-rays induced significant cell cycle arrest,necrosis,apoptosis and reduction of viability.Pretreatment with E0703 for 12 h before irradiation could increase cell viability and regulate cell cycle.but had no obvious effect on cell necrosis and apoptosis.The expression of cell cycle arrest related molecules Rb and MDM2 were increased after 3.0 Gy irradiation,but decreased significantly with pretreatment of E0703.Moreover.the phosphorylation of Rb was also increased.Conclusions The radioprotective function of E0703 might be exerted through influencing on cell cycle and promoting cell proliferation instead of apoptosis or necrosis.
6.UPLC/Q-TOF-MS-based chemical profiling approach to evaluate the chemical constitution of Radix Aconiti Lateralis Preparata in the process of decoction.
Sisi ZHOU ; Zengchun MA ; Qiande LIANG ; Yuguang WANG ; Hongling TAN ; Chengrong XIAO ; Boli ZHANG ; Yue GAO
Journal of Integrative Medicine 2012;10(8):894-900
An ultra-performance liquid chromatography coupled with time-of-flight mass spectrometry (UPLC/Q-TOF-MS)-based chemical analytic technology was used to evaluate the chemical constitution of Radix Aconiti Lateralis Preparata in the process of decocting, so as to provide a scientific basis for processing Radix Aconiti Lateralis Preparata.
7.The factors influencing the transfer of porcine endogenous retroviruses across the membrane in bioartificial livers
Bing HAN ; Xiaolei SHI ; Xianwen YUAN ; Jiangqiang XIAO ; Yue ZHANG ; Jiajun TAN ; Zhongze GU ; Yitao DING
Chinese Journal of Hepatobiliary Surgery 2012;18(5):368-371
ObjectiveTo identify the factors influencing the transfer of porcine endogenous retroviruses across the membrane of a new bioartificial liver (BAL),which is a necessary caution to consider for BALs carrying porcine hepatocytes.MethodsA novel porcine BAL composed of two circuits was constructed using a plasma filter with membrane pore size of 500 nm and a plasma component separator with membrane pore sizes 10 nm,20 nm,30 nm,and 35 nm.Co-cultured cells of porcine hepatocytes and mesenchymal stem cells or single porcine hepatocytes were incubated in the bioreactors.The BAL was continuously worked for 72 hours during which the supernatant was collected from the internal and external circuits every 12 hours.PERV RNA,reverse transcriptase (RT) activity,and in vitro infectivity from the supernatant were detected.ResultsIn the plasma filter group,the PERV RNAlevels were the same in both circuits,suggesting little to no effect of the plasma filter on the PERV RNA's crossing.With plasma component separators,PERV RNA was found in the external circuits at different times without positive RT activity and HEK293 cell infection,but its level was reduced significantly.The larger the membrane pore size was,the earlier and the more RNA was detected.ConclusionsThe membrane pore size,the treatment time and the viral level in the internal circuit are contributing factors influencing the transfer of PERV RNA across the membrane in a BAL.
8.UPLC-TOF/MS based chemical profiling approach to evaluate toxicity-attenuated chemical composition in combination of ginseng and radix aconiti praeparata.
Zengchun MA ; Sisi ZHOU ; Qiande LIANG ; Chao HUO ; Yuguang WANG ; Hongling TAN ; Chengrong XIAO ; Yue GAO
Acta Pharmaceutica Sinica 2011;46(12):1488-92
In the present study, an ultra performance liquid chromatography coupled with time-of-fight mass spectrometry (UPLC-TOF/MS) based chemical profiling approach was used to evaluate chemical constitution between co-decoction and mixed decoction of ginseng and Radix Aconiti Praeparata. Two different kinds of decoctions, namely co-decoction of ginseng and Radix Aconiti Praeparata: water extract of mixed two herbs, and mixed decoction of ginseng and Radix Aconiti Praeparata: mixed water extract of each individual herbs, were prepared. Batches of these two kinds of decoction samples were subjected to UPLC-TOF/MS analysis. The datasets of t(R) m/z pairs, ion intensities and sample codes were processed with supervised partial least squared discriminant analysis (OPLS-DA) to holistically compare the difference between these two decoction samples. Significant difference between the two decoction samples was showed in the results of positive ion mode. The contents of hypaconitine and deoxyaconitine decreased, while that of benzoylmesaconine, benzoylhypaconine and dehydrated benzoylmesaconine increased in the samples of co-decoction of ginseng and Radix Aconiti Praeparata. The content of diester-diterpenoid alkaloids decreased, while that of monoester-diterpenoid alkaloids increased, which is probably the basis of toxicity-attenuated action when combined ginseng with Radix Aconiti Praeparata.
9.Cytotoxic effect of veratrine hydrochloride on HepG2 cells and its possible mechanism
Canglong LIU ; Yuguang WANG ; Zengchun MA ; Qiande LIANG ; Chengrong XIAO ; Hongling TAN ; Xianglin TANG ; Yue GAO
Chinese Journal of Pharmacology and Toxicology 2014;(3):391-397
OBJECTIVE Tostudythehepatotoxicityofveratrinehydrochloride(VH)anditsmecha-nismoninductionofapoptosisinvitro.METHODS HepG2cellswereexposedtoVH0.1-0.6g·L-1 for 24 h,cell viability was examined by CCK-8 assay,and the morphologic changes in HepG2 cells were quantified.After the treatment with VH 0.1 -0.5 g·L-1 for 24 h,cell membrane injury was examined by detecting the release rate of lactate dehydrogenase (LDH).The effect on reactive oxygen species (ROS),mitochondrial membrane potential and apoptosis was detected by flow cytometry.The mRNA expression of p53,Bax,cytochrome c,caspase 9,caspase 3 was evaluated by real-time PCR. RESULTS HepG2cellviabilitywassignificantlyreducedfollowingexposuretoVH0.1-0.5g·L-1. The IC50 value was 0.4 g·L-1 .The 95%confidence limit was 0.2558-0.6965 g·L-1 .The LDH release rate,ROS and apoptosis rate of HepG2 cells were significantly increased after exposure to VH 0.1 -0.5 g·L-1 for 24 h (P<0.05,P<0.01 ),and the mitochondrial membrane potential markedly declined (P<0.05,P<0.01 ).The expression of p53,Bax,cytochrome c,caspase 9 and caspase 3 was increased(P<0.05,P<0.01).CONCLUSION VHhascytotoxicpotential.Damagetocell me mbrane and mitochondria and initiation of apoptosis-related genes of caspase 9 and caspase 3 mRNA expression may be the mechanis m of apoptosis.
10.Study on the induction of drug metabolizing enzyme CYP1 A1 activity by Ginsenoside Rc,Re,Rf and Rg1
Han LI ; Yuguang WANG ; Zengchun MA ; Hongling TAN ; Chengrong XIAO ; Xianglin TANG ; Boli ZHANG ; Yue GAO
Chinese Pharmacological Bulletin 2016;32(9):1217-1223
Aim To investigate the induction effect of ginsenoside Rc, Re, Rf and Rg1 on CYP1A1, and further validate the role of aryl hydrocarbon receptor in CYP1A1 expression. Methods Dual luciferase re-porter gene system was performed. Four kinds of gin-senoside were screened for aryl hydrocarbon receptor activation by reporter assays, and TCDD as the positive control. Further with different concentrations of ginsen-oside Rc, Re, Rf and Rg1 treated on LS174T cells, RNA and total protein were extracted to detect the reg-ulating effect of ginsenosides on CYP1 A1 mRNA and protein expression with Real-time PCR and Western blot technology respectively. Results Reporter gene screening showed that the ginsenoside Rc, Re, Rf and Rg1 could activate AhR and had potential effects on the induction of CYP1A1 enzyme. Meanwhile, dose-de-pendent induction of the gene expression were observed in response to ginsenoside Rc, Re, Rf and Rg1 and the levels of CYP1 A1 protein expression were increased by ginsenoside Rc, Re, Rf and Rg1 in varying de-grees. Conclusion Ginsenoside Rc, Re, Rf and Rg1 can up-regulate the gene and protein expression of CYP1 A1 possibly via the AhR-mediated CYP1 A1 path-way.