1.Improvement effects and mechanism of Achyranthes bidentata total saponins extract on vascular endothelial dysfunction in spontaneously hypertensive rats
Ruifeng LIANG ; Wenjing GE ; Xiaobo KOU ; Ping TIAN ; Hongzhi AN ; Zheng WEI ; Mingli ZHANG
China Pharmacy 2026;37(3):331-337
OBJECTIVE To investigate the improvement effects and mechanism of Achyranthes bidentata total saponins (ABS) extract on vascular endothelial dysfunction in spontaneously hypertensive rat (SHR) based on cytochrome P450 4A (CYP4A)/20-hydroxyeicosatetetraenoic acid (20-HETE)/G protein-coupled receptor 75 (GPR75) axis. METHODS Ten Wistar- Kyoto rats were taken as the normal control group. Forty SHR were first stratified by systolic blood pressure and then, within each stratum, randomly assigned using a random-number table to the model group (MOD group), captopril positive control group (CAP group, 10 mg/kg), ABS low- and high-dose extract groups (ABS-L group, ABS-H group, 60 and 120 mg/kg), with 10 rats in each group. Animals in each group were given the corresponding drug or equal volume of pure water by gavage, once a day, for 28 consecutive days. After the last administration, systolic blood pressure of rats was measured. The levels of vasoactive substances, inflammatory factors and oxidative stress indicators in serum were measured. The pathological changes of rat thoracic aorta were observed. The level of reactive oxygen species (ROS) in aortic tissue was analyzed. The expressions of endothelial nitric oxide synthase (eNOS), CYP4A, GPR75, nuclear factor-κB p65 (NF-κB p65), phosphorylated NF-κB p65, p22phox, and reduced nicotinamide adenine dinucleotide phosphate oxidase 4(NOX4) in thoracic aorta tissue were detected. RESULTS After 28 d of treatment, compared with MOD group, the systolic blood pressure of rats in the ABS-L and ABS-H groups decreased significantly. The levels of 20-HETE, angiotensin Ⅱ, interleukin-1β, interleukin-6, tumor necrosis factor-α, intercellular cell adhesion molecule-1 and malondialdehyde in serum were significantly reduced (P<0.05 or P<0.01), while the levels of nitric oxide, superoxide dismutase, glutathione peroxidase and catalase were significantly increased (P<0.05 or P<0.01). Intimal damage of thoracic aorta was reduced, and endothelial cell morphology was improved. The expressions of ROS, CYP4A, GPR75, p22phox, NOX4 and the phosphorylation level of NF-κB p65 protein in thoracic aorta were down-regulated or reduced (P<0.05 or P<0.01), while the expression of eNOS was up-regulated (P<0.05 or P<0.01). CONCLUSIONS ABS extract may alleviate the inflammatory response and oxidative stress in SHR effectively by down-regulating the expression of CYP4A, reducing the production of 20-HETE, inhibiting the activation of GPR75, and subsequently suppressing the activation of downstream NF-κB and NOX4, thereby improving hypertension-related vascular endothelial dysfunction.
2.Discussion on Syndrome and Treatment Rules of Set Prescription Preparation Containing Platycodon grandiflorum-Glycyrrhiza uralensis Based on Data Mining
Jianjun LYU ; Ruichun HAO ; Jiuzhang MEN ; Xiaobo LI ; Yongfeng KOU
China Pharmacy 2018;29(20):2813-2816
OBJECTIVE:To provide reference for clinical application and related new drug R&D of the couplet medicines of Platycodon grandiflorum-Glycyrrhiza uralensis. METHODS:All set prescription preparations containing P. grandiflorum-G. uralensis in Ministry of Public Health Drug Standard·TCM Set Prescription Preparation were collected;data mining and analysis for the syndrome and treatment rules of these prescriptions were performed by using TCM Inheritance System V 2.5. RESULTS:There were a total of 315 set prescription preparations containing couplet medicine of P. grandiflorum-G. uralensis , 89 main syndromes and 88 main diseases. Among of them,high frequency major syndrome were exterior syndrome attacked by wind-heat and exterior syndrome tightened by wind-cold,and dominating medicine combination were respectively Yinqiao powder and Xingsu powder. High frequency main diseases were common cold and cough. Core medicine combination in the treatment of common cold included Yinqiao powder, Xingsu powder,Huoxiang zhengqi powder and Chaihu zhijie decoction,etc. Core medicine combination in the treatment of cough included Xingsu powder,Zhisou powder,Tongxuan lifei pills and Qingjin huatan decoction,etc. CONCLUSIONS:The study confirms the syndrome and treatment rules of set prescription preparations containing couplet medicines of P. grandiflorum-G. uralensis , and could provide evidence for clinical application of the couplet medicines of P. grandiflorum-G. uralensis and new drug R&D.
3.Efficacy of 150 mg clopidogrel and triple antiplatelet in patients with acute anterior myocardial infarction undergoing PCI
Cong WANG ; Xiaobo ZHOU ; Shuangqing KOU
Chinese Journal of Biochemical Pharmaceutics 2015;37(7):73-75
Objective To observe the efficacy and safety of 150 mg clopidogrel and triple antiplatelet in acute anterior myocardial infarction ( AMI) patients undergoing percutaneous coronary intervention ( PCI).Methods Totally 50 patients who had been diagnosed as acute anterior myocardial infarction and prepared to PCI treatment were randomly divided into two groups:150 mg clopidogrel group ( asprin 100 mg/d qd+clopidogrel 150 mg/d qd) and triple antiplatelet group ( cilostazol 100 mg bid+asprin 100 mg/d qd+clopidogrel 75 mg/d qd).The coronary lession through CAG, incidence of major cardiovascular events and safety in 6 months were observed and assessed.ResuIts There was no significant difference in level of target lesion diameter between two groups after PCI instantly (2.75 ±0.29 mm vs.2.69 ±0.31 mm).There were no significant differences of late lumen loss (LLL) and target lesion revascularization (TLR) between triple antiplatelet group and 150 mg clopidogrel group (0.22 ±0.46 mm vs.0.38 ±0.65 mm; 8%vs.24%) , but the two indexes were improved in a certain extent.There were no significant differences in hemorrhage and major adverse cardiovascular events ( MACE) between two groups.ConcIusion The triple antiplatelet therapy could reduce the late lumen loss and target lesion revascularization, and not increase hemorrhage and adverse cardiovascular events.

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