1.Impact of retinol binding protein 4 polymorphism on rosiglitazone response in Chinese Type 2 diabetic patients
Fang ZHOU ; Qiong HUANG ; Xingping DAI ; Jiye YIN ; Jing WU ; Honghao ZHOU ; Zhicheng GONG ; Zhaoqian LIU
Journal of Central South University(Medical Sciences) 2011;36(10):949-957
Objective To explore the association between rs3758539G-803A and rs10882283 T-179G polymorphism of retinol binding protein 4 (RBP4) and rosiglitazone response in Chinese type 2 diabetes mellitus (T2DM) patients.Methods A total of 472 Chinese T2DM patients and 198 healthy subjects were enrolled to identify G-803A and T-179G genotypes using a polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP ).assay.Forty-two T2DM patients with different G-803A or T-179G genotypes were selected to undergo a 12-week rosiglitazone treatment (4 mg/d).Serum fasting plasma glucose (FPG),postprandial plasma glucose (PPG),fasting serum insulin (FINS),glycated hemoglobin (HbAlc),postprandial serum insulin ( PINS),triglyceride (TG),low-density lipoprotein-cholesterol ( LDL-c),and high-density lipoprotein-cholesterol (HDL-c) were determined before and after the rosiglitazone treatment.Results T2DM patients with RBP4 G-803A GG genotype showed lower TG and LDL-c concentrations compared with that in the GA +AA genotype subjects.T2DM patients with RBP4 T-179G TT genotype showed lower waist-to-hip ratio (WHR),FPG and FINS values compared with that in the TG + GG genotype individuals.Patients with GG genotype of RBP4 G-803A had an enhanced rosiglitazone efficacy on FPG and FINS compared with that in the GA + AA genotype group.Patients with RBP4 T179G TG + GG genotype showed an enhanced rosiglitazone efficacy on HbAlc level compared with that in the TT genotype group.Conclusion RBP4 G-803A and T-179G polymorphism might be associated with the development of T2DM and affect the therapeutic efficacy of rosignitazone in Chinese T2DM patients.
2. Pharmacokinetics and tissue distribution of tetrahydropalmatine, nobiletin, and costunolide in rats after oral administration of Dalitong extract
Yuanmao ZHANG ; Ran ZHANG ; Ruiwei LIAO ; Xiuxiu MENG ; Chen XU ; Fang-Fang GAO ; Fang-Fang JIYE ; Guangji WANG ; Lin TAO
Chinese Journal of Clinical Pharmacology and Therapeutics 2024;29(1):37-51
AIM: To investigate the pharmacokinetic properties of the main active components of Dalitong extract in SD rats after oral administration using UPLC-MS / MS. METHODS: An UPLC-MS / MS method was established to simultaneously detect tetrahydropalmatine, nobiletin and costunolide in the plasma and tissues of SD rats. The method was applied to investigate the pharmacokinetic characteristics and tissue distribution. RESULTS: After a single oral administration, the three active components were rapidly absorbed into the body, with a peak concentration (Cmax) of (13.73 ± 7.50), (27.01 ± 17.69) and (6.73 ± 29.94) ng / mL for tetrahydropalmatine, nobiletin, and costunolide, respectively. The time to reach the peak concentration (Tmax) was (1.40 ± 0.93), (0.63 ± 0.28) and (2.38 ± 8.81) h, respectively. The area under the curve (AUC) was (80.43±40.03), (41.30±28.69) and (303.90 ± 136.69) ng · h · mL