葛根素-钆抗痛风性关节炎活性与机理初探
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摘要
以葛根素为配体,以金属钆为配位中心,通过控制反应条件,设计合成了葛根素-钆(Gd)配合物,并对葛根素-钆的结构进行红外(IR)表征.采用尿酸钠诱导的急性痛风性关节炎大鼠模型,利用敷线法考察造模后2～48 h大鼠踝关节肿胀率的变化,并对大鼠血清、肝脏及滑膜中PGE2、IL-1β、TNF-α的水平进行检测.结果表明,葛根素与稀土金属钆发生配位,得到葛根素-钆(Gd)配合物.葛根素-钆配合物对大鼠痛风性关节炎肿胀抑制作用比葛根素强,葛根素-钆配合物组大鼠血清、肝脏及滑膜中的PGE2、IL-1β和TNF-α水平均低于葛根素组.综上,说明葛根素-钆配合物抗痛风性关节炎活性优于其配体葛根素,其抗炎机制可能与降低体内PGE2、IL-1β和TNF-α的水平有关.
Puerarin rare earth complexe( Gd) was synthesized with puerarin as ligands and rare earth metal gadolinium as the center by controlling the reaction conditions. The structure of the PUE-Gd was characterized through IR method. The effect of PUE-Gd on ankle swelling rate of rats induced by sodium urate detection during 2 ～ 48 h was studied by wire method,and the levels of PGE2,IL-1β and TNF-α in the serum,liver and synovium were detected to detect its Anti-inflammatory activity and mechanism in rats with gouty rrthritis. The result of IR showed that puerarin is coordinated with rare earth metal through the phenolic oxygen atoms and carbonyl oxygen atoms. The inhibitory effect of puerarin-gadolinium complexe on rat gouty arthritis swelling with in 48 h was more significant than that of puerarin. The levels of PGE2,IL-1β and TNF-α in the serum,liver and synovium of rats fed with puerarin-gadolinium complexe group were lower than that of rats fed with pueraringroup,respectively. To sum up,the anti-inflammatory activity of puerarin-gadoliniumcomplexe was better than that of puerarin in rats with gouty rrthriti and the mechanism of anti-inflammatory activity might be related to reducing levels of PGE2,IL-1 beta and TNF-alpha.
Puerarin rare earth complexe( Gd) was synthesized with puerarin as ligands and rare earth metal gadolinium as the center by controlling the reaction conditions. The structure of the PUE-Gd was characterized through IR method. The effect of PUE-Gd on ankle swelling rate of rats induced by sodium urate detection during 2 ～ 48 h was studied by wire method,and the levels of PGE2,IL-1β and TNF-α in the serum,liver and synovium were detected to detect its Anti-inflammatory activity and mechanism in rats with gouty rrthritis. The result of IR showed that puerarin is coordinated with rare earth metal through the phenolic oxygen atoms and carbonyl oxygen atoms. The inhibitory effect of puerarin-gadolinium complexe on rat gouty arthritis swelling with in 48 h was more significant than that of puerarin. The levels of PGE2,IL-1β and TNF-α in the serum,liver and synovium of rats fed with puerarin-gadolinium complexe group were lower than that of rats fed with pueraringroup,respectively. To sum up,the anti-inflammatory activity of puerarin-gadoliniumcomplexe was better than that of puerarin in rats with gouty rrthriti and the mechanism of anti-inflammatory activity might be related to reducing levels of PGE2,IL-1 beta and TNF-alpha.
引文
[1]吴绍刚.葛根素的药理作用解析及临床合理应用[J].基层医学论坛,2017,25(21):3462.
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[10] CODERRE T J,WALL P D. Ankle joint arthritis in rats provide useful tool for the evaluation of anal gesic and anti-arthritic agents[J]. Pharm Biochem Behav,1988,29(8):461-463.
[11] CODERRE T J,WALL P D. Ankle joint arthritis in rats:an alternative animal model of arthritis to that produced by Freud’s adjuvant[J]. Pain,1987,36(28):379-381.
[12] SABINA E P,RASOOL M. An in vivo and in vitro potential of indian ayurvedic herbal formulation triphala on experimental gouty arthritis in mice[J]. Vascul Pharmacol,2008,48(1):14-20.
[13] MIGUELEZ R,PALACIOS I,NAVARRO F,et al. Anti-inflammatory effect of a PAF receptor antagonist and a new molecule with antiproteinase activity in an experimental model of acute urate crystal arthritis[J]. J Lipid Mediat Cell Signal,1996,13(1):35-49.
[14]王红梅,杨中华,张明,等.急性痛风性关节炎的炎症机制研究进展[J].国外医学:老年医学分册,2005(3):124-127.
[15]万春平,李兆福,徐翔峰,等.急性痛风性关节炎免疫学发病机制研究进展[J].风湿病与关节炎,2012,4(1):52-55.
[16] IINOKUCHI T,MORIWAKI Y,TSUTSUI H,et al. Plasmainterleukin(IL)-18(interferon-g-inducing factor)andother inflammatory cytokines in patients with gouty arthritis and monosodium urate monohydrate crystal-induced secretion of IL-18[J]. Cytokine,2006,33(1):21-27.
[17] MYTHILYPRIYA R,SACHDANANDAM P S,SACHDANANDAM P. Ameliorating effect of kalpaamruthaa,a siddha preparation in adjuvant induced arthritis in rats with reference to changes in proinflammatory cytokines and acute phase proteins[J].Chem Biol Interact,2009,179(2/3):335-343.
[18] LEE H S,LEE C H,TSAI H C,et al. Inhibition of cyclooxygenase 2 expression by diallyl sulfide on joint inflammation induced by urate crystal and IL-1 beta[J]. Osteoarthritis Cartilage,2009,17(1):91-99.
[19]马誉畅,刑志华,杨鑫,等.葛根素-稀土配合物的抗痛风性关节炎活性研究[J].哈尔滨商业大学学报:自然科学版,2018,34(2):138-142.
[2]夏华玲.葛根素的药理作用研究进展[J].时珍国医国药,2006,17(3):434-435.
[3]曾祥伟,冯倩,张莹莹,等.葛根素对炎症相关疾病研究进展[J].中国药理学通报,2018,34(1):8-11.
[4]马越,吕圭源,陈素红.葛根提取物抗痛风性关节炎作用及机制初探[J].中药新药与临床药理,2011,22(3):241-244.
[5]刘丽娟,张卓.葛根治疗痛风的临床疗效[J].吉林大学学报:医学版,2005,31(5):670.
[6]夏肖萍,费春荣,叶爱青.葛根素对SD大鼠全身炎症反应综合征的治疗作用及其机制研究[J].浙江检验医学,2008,6(2):12-14.
[7]潘见,袁传勋,戴郁青.葛根素配位特性研究[J].天然产物研究与开发,2006,18(4):562-565.
[8]张齐雄,施伦勇,曹蓓,等.黄酮类稀土金属配合物的研究进展[J].中国医药科学,2012,7(2):54-56.
[9]石少明,覃江克,陈振锋,等.具有药用活性的稀土配合物在医药领域中的应用[J].华西药学杂志,2013,28(3):317-320.
[10] CODERRE T J,WALL P D. Ankle joint arthritis in rats provide useful tool for the evaluation of anal gesic and anti-arthritic agents[J]. Pharm Biochem Behav,1988,29(8):461-463.
[11] CODERRE T J,WALL P D. Ankle joint arthritis in rats:an alternative animal model of arthritis to that produced by Freud’s adjuvant[J]. Pain,1987,36(28):379-381.
[12] SABINA E P,RASOOL M. An in vivo and in vitro potential of indian ayurvedic herbal formulation triphala on experimental gouty arthritis in mice[J]. Vascul Pharmacol,2008,48(1):14-20.
[13] MIGUELEZ R,PALACIOS I,NAVARRO F,et al. Anti-inflammatory effect of a PAF receptor antagonist and a new molecule with antiproteinase activity in an experimental model of acute urate crystal arthritis[J]. J Lipid Mediat Cell Signal,1996,13(1):35-49.
[14]王红梅,杨中华,张明,等.急性痛风性关节炎的炎症机制研究进展[J].国外医学:老年医学分册,2005(3):124-127.
[15]万春平,李兆福,徐翔峰,等.急性痛风性关节炎免疫学发病机制研究进展[J].风湿病与关节炎,2012,4(1):52-55.
[16] IINOKUCHI T,MORIWAKI Y,TSUTSUI H,et al. Plasmainterleukin(IL)-18(interferon-g-inducing factor)andother inflammatory cytokines in patients with gouty arthritis and monosodium urate monohydrate crystal-induced secretion of IL-18[J]. Cytokine,2006,33(1):21-27.
[17] MYTHILYPRIYA R,SACHDANANDAM P S,SACHDANANDAM P. Ameliorating effect of kalpaamruthaa,a siddha preparation in adjuvant induced arthritis in rats with reference to changes in proinflammatory cytokines and acute phase proteins[J].Chem Biol Interact,2009,179(2/3):335-343.
[18] LEE H S,LEE C H,TSAI H C,et al. Inhibition of cyclooxygenase 2 expression by diallyl sulfide on joint inflammation induced by urate crystal and IL-1 beta[J]. Osteoarthritis Cartilage,2009,17(1):91-99.
[19]马誉畅,刑志华,杨鑫,等.葛根素-稀土配合物的抗痛风性关节炎活性研究[J].哈尔滨商业大学学报:自然科学版,2018,34(2):138-142.
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