1.Pharmacokinetic studies of scutellarein and glucuronide scutellarin in rats
Yue LIU ; Yong HUANG ; Yongxi DONG ; Yonglin WANG ; Lin ZHENG
Chinese Pharmacological Bulletin 2014;(5):711-714,715
Aims To establish a UPLC-MS/MS meth-od for the determination of plasma concentration of scutellarein and its metabolite and to study their phar-macokinetics in rat plasma. Methods The analysis was achieved by BEH C18 column with a mobile phase composed of 0 . 1 % formic acid in acetonitrile and 0 . 1% aqueous formic acid using step gradient elution. A TQD tandem mass spectrometry equipped with electros-pray ionization source was used as detector and opera-ted by multiple reaction monitoring( MRM) positive ion mode. After intravenous injection of scutellarein, the concentrations of scutellarein and its major metabolite glucuronide scutellarin in rat plasma were determined at different time points. The pharmacokinetic parame-ters were calculated by DAS 2. 0 software. Results Good linearity was achieved for scutellarein, the ex-traction recovery was between 80 . 5 % to 90 . 5 %, the precisions and accuracy were good. The result showed the pharmacokinetic profiles of scutellarein and glucu-ronide scutellarin both fit to the two-compartment mod-el. Conclusion The above mentioned method is spe-cific, rapid, sensitive and suitable for the pharmacoki-netic studies of scutellarein and its metabolite.
2.Management of neck open injury in the primary hospital
Shibin TANG ; Luyang WU ; Yongxi LIN ; Yubin LIAO
Chinese Journal of Primary Medicine and Pharmacy 2008;15(9):1431-1433
Objective To explore how to treat open neck trauma in time and with reason in the primary hospital.Methods 57 cases of neck open injury were hospitalized from Aug.1997 to Jan.2()07,and injury cause,mechanism,diagnosis and treatment of them are analyzed retrospectively.Results There were 29 incisal wounds and 23 penetrating wounds and 5 contusing wounds.Among 57 patients there were 12 significant injuries and 55 minor injuries cases.53 patients had been treated with operative exploration and 10 patients had therapeutic exploration.The result of treatment showed that 50 patients were cured,and 4 patients died of head injury,cervical spinal injury and respiratory failure,anoxic encephalopathy from airway obstruction and hemorrhagic shock from combined injuries of common carotid artery and internal jugular vein.Conclusion The mainstay of choice of treatment is the injury mechanism and clinical signs and symptoms of patient.
3.Rapid pharmacokinetic characteristic evaluation of scutellarin derivatives in vitro
Lin ZHENG ; Jie HU ; Xu CAO ; Yong HUANG ; Yongxi DONG ; Yonglin WANG
Chinese Pharmacological Bulletin 2014;(9):1298-1301
Aim To study the pharmacokinetic char-acteristics of serial compounds that took the scutellarin and scutellarein as lead compounds by using the model of in vitro liver microsomes, and to screen compounds whose medicinal properties were superior to scutellarin and scutellarein. Methods The content of candidate compounds at different times by incubation system of rat liver microsome was determined using UPLC-MS/MS method. Candidate compounds that contained opti-mum T1/2 and CLint were screened. Enzyme kinetics and conversions of candidate compounds were com-pared with those of scutellarin and scutellarein. Re-sults The T1/2 and CLint were optimum of W11 com-pared with those of scutellarin and scutellarein; the Vmax, Km and CLint of compound W11 were (10.25 ±2.59 ) μmol · min-1 · g-1 , ( 4.64 ±0.24 ) μmol · L-1 and ( 2.29 ±0.23 ) L · min-1 · g-1; the Vmax , Km and CLint of scutellarin were (45.95±9.50) μmol · min-1 · g-1 , ( 10.19 ± 1.66 ) μmol · L-1 and (4.48±0.20) L·min-1 ·g-1; W11 might be me-tabolized into scutellarin and M1 ( a compound with mo-lecular weight of 577 after demethylating ) . Conclu-sion The pharmacokinetic properties of candidate compound W11 are better than those of scutellarin, and it could release scutellarin.
4.The variance of HSP70 in cardiac cells of SMDS victims
Jiquan YAN ; Hualan JING ; Yijun ZHANG ; Hongquan XU ; Yongxi WEN ; Hong LIN ; Fuxue JIANG ; Tianyu LU ;
Chinese Journal of Forensic Medicine 2009;24(6):394-396,后插1
Objective This article aims to explore the role of HSP70 in the developing mechanism of SMDS(sudden manhood death syndrome,SMDS)and to investigate the value of it in the early diagnosis of SMDS.Methods By way of immunohistochemieal staining of left,right ventricular musles,sino atrial node and atrioventricular node from 30 cases of SMDS group and 20 cases of control group,we observed and measured the expression of HSP70 and its variance of intensity with graphical analysis software.Results Compared with the control group cases,in cardiac conduction system tissue of SMDS victims.we saw an obviously higher expression and intensity of HSP70(P<0.05).Conclusion As a kind of mediator in stress reaction,HSP70 is involved in the process of protecting the heart from impairment in SMDS,and it can be considerated as a reference index to identify the SMDS.
5.The variance of PKC in cardiac cells of SMDS victims
Hongquan XU ; Hualan JING ; Yijun ZHANG ; Jiquan YAN ; Yongxi WEN ; Hong LIN ; Fuxue JIANG
Chinese Journal of Forensic Medicine 2009;24(6):396-397,后插1
Objective This article aims to explore the relationship between PKC and SMDS(sudden manhood death syndrome,SMDS).Methods By way of immunohistochemical staining of left,right ventricular tousles,sino atrial node and atrioventricular node from 30 cases of SMDS group and 20 cases of control group,we observed and measured the expression and the intensity variance of PKC in myocardial ceHs with graphical analysis software.Results The average gray value and total area of PKC in myocardial cells of cases in the SMS group are obviously higher than that of cases in control group(P<0.05).And in the SMDS group,the average gray value of PKC in sino atrial node is higher than that in atrioventricular node.Conclusion As one way of humoral regulation,PKC is involved in the process of protecting the heart from impairment in SMDS.and it can be considerated as a reference index to identify the SMDS.