1.Effects of high density lipoprotein and apolipoprotein A-Ⅰ mimetic peptide on the expression of adiponectin in 3T3-L1 adipocytes
Xiangzhu XIE ; Shuiping ZHAO ; Bilian YU ; Qiaoqing ZHONG
Chinese Pharmacological Bulletin 2003;0(08):-
Aim To explore the effect of high density lipoprotein and apolipoprotein A-I mimetic peptide on the secretion and the expression of adiponectin in fully differentiated 3T3-L1 adipocytes in inflammatory status and the possible mechanism.Methods Fully differentiated 3T3-L1 adipocytes were incubated in the medium containing various concentrations of high density lipoprotein(10~100 mg?L-1) and apolipoprotein A-I mimetic peptide(1~50 mg?L-1)with 100 ?g?L-1 lipopolysaccharide(n=3).Evaluate the levels of adiponectin in supernatant,the mRNA expression of adiponectin and PPAR?,and the activity of NF-?B.Results During LPS stimulation adiponectin concentrations in supernatant decreased from 0.25?0.03 ?g?L-1 to 0.14?0.02 ?g?L-1(P
2.Effect of high-density lipoprotein on interleukin-8 secretion in 3T3-L1 adipocytes
Qiaoqing ZHONG ; Shuiping ZHAO ; Xing WANG ; Bilian YU ; Jing DONG ; Xiangzhu XIE ; Zhihong WU
Chinese Journal of Endocrinology and Metabolism 2010;26(10):888-890
3T3-L1 adipocytes were cultured with various concentrations of high-density lipoprotein ( HDL, 0, 10, 50, and 100 μg/ml ) for 16 h and with lipopolysaccharide ( LPS, 100 ng/ml ) for another 6 h. Interleukin-8 in the medium was determined by ELISA, and PPAR-γ mRNA expression by reverse transacription polymerase chain reaction (RT-PCR). Interleukin-8 levels were increased in LPS-treated cells ( P<0.05 ), but decreased in HDL-treated cells in the dose-dependent manner. PPARγ mRNA expressions were increased in HDL-treated groups than those treated only with LPS. These results suggested HDL may decrease interleukin-8 secretion via up-regulating PPARγ expression in adipocytes.
3.Pharmacokinetics of sugammadex in reversal of rocuronium-induced muscle relaxant residual in infants and young children undergoing daytime surgery
Hao LUO ; Yao LIU ; Junxiang HUANG ; Yanping GUAN ; Cheng FAN ; Guoping ZHONG ; Xingrong SONG ; Bilian LI
Chinese Journal of Anesthesiology 2023;43(8):966-971
Objective:To investigate the pharmacokinetics of sugammadex in reversal of rocuronium-induced muscle relaxant residual in infants and young children undergoing daytime surgery.Methods:One hundred and four pediatric patients of either sex, aged 3-36 months, of American Society of Anesthesiologists Physical Status classification Ⅱ, with body mass index of 18.5-28.0 kg/m 2, diagnosed with oblique inguinal hernia and/or hydrocele, scheduled for laparoscopic high ligation of hernia sac and/or high ligation of sphingoid surgery, were included in the study. Intraoperative neuromuscle relaxation was assessed by transdermal stimulation of the ulnar nerve in the wrist using a TOF Guard monitor. Rocuronium 0.9 mg/kg, propofol 3 mg/kg, and sufentanyl 0.5 μg/kg were intravenously injected for anesthesia induction, and propofol 6-8 mg·kg -1·h -1 was intravenously infused to maintain anesthesia. The pediatric patients were divided into Ⅰgroup and Ⅱ group according to the degree of postoperative neuromuscular block. In group Ⅰ, sugammadex 2 mg/kg was intravenously injected when TOF returned to T 2 recurrence. In group Ⅱ, sugammadex 4 mg/kg was intravenously injected when the single stimulation count was 1 or 2 after tetanic stimulation. At 2 and 10 min after rocuronium administration, at the end of operation, 2 and 10 min after sugammadex administration, and when the children met the standard of leaving the resuscitation room, venous blood samples were collected for determination of plasma concentrations of rocuronium and sugammadex using ultra-high performance liquid chromatography-mass spectrometry. Pharmacokinetic parameters were determined using the Pheonix WinNonlin software. The onset of rocuronium and time for recovery of TOF ratio to 90% were recorded. Results:The pharmacokinetics of sugammadex was fitted to the nonlinear mixed-effect satrioventricular model.There was no significant difference in the peak concentration, area under the drug concentration-time curve, elimination half-life, apparent clearance, apparent volume of distribution, mean retention time, and time for TOF ratio returning to 90% between the two groups ( P> 0.05). Conclusions:The pharmacokinetics of sugammadex in reversal of rocuronium-induced muscle relaxant residual is fitted to a nonlinear mixed-effect satrioventricular model, and sugammadex 2 and 4 mg/kg have similar pharmacokinetics in infants and young children undergoing daytime surgery.
4.Exploration of the Pharmacological Substance Basis and Action Characteristics of Wenxing Jingjintong Gel Patch in the Treatment of Rheumatoid Arthritis Based on System Pharmacology and LC-MS/MS Technology
Anyu SU ; Weibin HUANG ; Jingyuan MO ; Zixuan ZHANG ; Xun XIE ; Xiaobing HUANG ; Bilian ZHONG ; Yongping ZHANG ; Lisheng WANG ; Chunyi WANG
Traditional Chinese Drug Research & Clinical Pharmacology 2024;35(5):706-718
Objective To explore the key active ingredients and action characteristics of Wenxing Jingjintong Gel Patch in the treatment of rheumatoid arthritis(RA)based on the systematic pharmacology and LC-MS/MS technology.Methods The information of active ingredient from Wenxing Jingjintong Gel Patch was established through LC-MS/MS analysis and literature retrieval.The targets of the active ingredients were predicted using Swiss Target Prediction platform and then mapped with the RA-related targets obtained from GeneCards,DrugBank,and OMIM databases to identify the intersecting targets.The"active ingredients-effective targets"network was constructed through the Cytoscape software.The shared targets were imported into STRING database to construct a protein-protein interaction network.GO function and KEGG pathway enrichment analysis were performed using the Metascape database.Molecular docking studies were conducted using AutoDock software to investigate the interactions between key ingredients and target proteins.Results A total of 142 active ingredients were identified in Wenxing Jingjintong Gel Patch by wsing LC-MS/MS,which were further supplemented to 174 through literature retrieval.There were 175 shared targets between the active ingredients and RA.It was anticipated that Wenxing Jingjintong Gel Patch exerted immune regulation and anti-inflammatory and analgesic effects through the interaction between key active ingredients such as berberine,neobavaisoflavone,and palmatine chloride with key targets,including TNF,IL6,and AKT1 to regulate PI3K/Akt1,JAK/STAT,and MAPK signaling pathways.In 1 152 molecular docking validation,94%of them had binding energies less than-5.0 kcal·mol-1,while 51%of them had binding energies less than-7.0 kcal·mol-1.It was indicated that there was a good binding affinity between the potential active ingredients and core targets.Conclusion This study predicted the active ingredients and action characteristics of Wenxing Jingjintong Gel Patch in the treatment of RA,which provided a theoretical basis for further clinical application and quality control.