三氟淫羊藿素对慢性炎性痛大鼠的抗炎消肿作用  

Trifluoro-icaritin exerts anti-inflammatory and detumescence effects in CFA rats

作　　者：孙亚兰 贾丹丹 黄诚[2,3] SUN Ya-lan;JIA Dan-dan;HUANG Cheng(Gannan Medical University,Ganzhou,Jiangxi 341000;School of Basic Medicine,Gannan Medical University;Institute of Pain Medicine,Gannan Medical University,Ganzhou,Jiangxi 341000)

机构地区：[1]赣南医学院,江西赣州341000 [2]赣南医学院基础医学院,江西赣州341000 [3]赣南医学院疼痛医学研究所,江西赣州341000

出　　处：《赣南医学院学报》2022年第2期109-113,124,共6页JOURNAL OF GANNAN MEDICAL UNIVERSITY

基　　金：国家自然科学基金项目(31160213);江西省主要学科学术和技术带头人培养计划项目(20142BCBC22008);赣鄱英才555工程领军人才项目;江西省研究生创新项目(YC2019-S421)。

摘　　要：目的:探讨三氟淫羊藿素(Trifluoro-icaritin,ICTF)是否改善完全弗氏佐剂(Complete freund’s adjuvant,CFA)诱发的大鼠足底炎症和肿胀程度。方法:将雄性SD大鼠随机分为3组:Ctrl组、CFA组和CFA+ICTF组。Ctrl组仅在大鼠左侧足底皮下注射100μL生理盐水;CFA组和CFA+ICTF组分别在大鼠左侧足底皮下注射100μL CFA,且CFA+ICTF组大鼠每天腹腔注射1次ICTF(3 mg·kg^(-1)),共持续21 d,在造模前1 d测量基线(Baseline,BL)水平及造模后第1 d、7 d、14 d和21 d分别检测大鼠足趾肿胀程度并采集图像。在第21 d取各组大鼠足底组织,应用HE染色检测炎症细胞浸润情况。应用分子对接技术模拟ICTF与胆碱能抗炎通路关键受体α7n ACh R的相互作用,并对数据进行分析比对。结果:大鼠足趾容积结果显示,与Ctrl组比较,CFA组大鼠足趾肿胀程度上调,与CFA组比较,CFA+ICTF组大鼠足趾肿胀程度在第14 d和21 d下调,差异均有统计学意义(P<0.05)。HE染色结果显示,经ICTF治疗后,CFA大鼠足底组织炎性细胞浸润减少。分子对接结果显示,LOB与α7-ACh BP对接的抑制常数(Ki)为1.68μmol·L^(-1),结合自由能(△G)为-7.88 kcal·mol^(-1),结合能力强,ICTF与α7-ACh BP对接的Ki为5.59μmol·L^(-1),△G为-7.17 kcal·mol^(-1),具有较强的结合能力,且ICTF分子对接空间构象与α7-ACh BP激动剂LOB接近。结论:ICTF可能通过激活胆碱能抗炎通路的α7n ACh R对CFA大鼠发挥抗炎消肿作用。Objective:To investigate whether trifluoro icaritin(ICTF)can improve the degree of plantar inflammation and swelling induced by complete freund’s adjuvant(CFA)in SD rats.Methods:Male SD rats were randomly divided into three groups:Ctrl group,CFA group and CFA+ICTF group.In Ctrl group,rats were injected subcutaneously into the left plantar 100μL normal saline;the CFA group and CFA+ICTF group rats were injected subcutaneously into the left plantar 100μL CFA;Rats in CFA+ICTF group were injected intraperitoneally once daily with ICTF(3 mg·kg^(-1))for21 days.The baseline(BL)level was measured one day before modeling,and the toe swelling degree was detected and images were collected on the first,seventh,fourteenth and twenty-first days after modeling.On the 21st day,the plantar tissues of rats in each group were taken and the infiltration of inflammatory cells was detected by HE staining.Molecular docking technology was used to connect ICTF with the key receptor of cholinergic anti-inflammatory pathwayα7n ACh R,and analyze and compare the data.Results:The results of toe volume showed that compared with the Ctrl group,the degree of toe swelling in CFA group was significantly up-regulated,and compared with CFA group,the degree of toe swelling in CFA+ICTF group was obviously down-regulated on the 14 d and 21 d,with statistical significance(P<0.05).HE results showed that the inflammatory cell infiltration of plantar tissue decreased significantly after ICTF treatment.The results of molecular docking showed that the suppression constant of docking(Ki)of LOB andα7-ACh BP was 1.68μmol·L^(-1),binding energy(△G)was-7.88 kcal·mol^(-1),with strong combination ability;Ki of ICTF andα7-ACh BP docking was5.59μmol·L^(-1),△G was-7.17 kcal·mol^(-1),with strong combination ability,the docking space conformation of ICTF molecule was close toα7-ACHBP agonist LOB.Conclusion:ICTF may activate cholinergic anti-inflammatory pathwayα7n ACh R to exert anti-inflammatory and detumescence effects on CFA rats.

关 键 词：三氟淫羊藿素 慢性炎性痛 分子对接 α7nAChR 

分 类 号：R338[医药卫生—人体生理学]