中国骨与关节杂志
中國骨與關節雜誌
중국골여관절잡지
Chinese Journal of Bone and Joint
2015年
11期
850-855
,共6页
魏长征%吴祎%宋瑞瑞%蒋丽霞
魏長徵%吳祎%宋瑞瑞%蔣麗霞
위장정%오의%송서서%장려하
透明质酸%自由基%骨关节炎
透明質痠%自由基%骨關節炎
투명질산%자유기%골관절염
Hyaluronic acid%Free radicals%Osteoarthritis
目的:制备一种具有一定清除自由基能力的巯基化透明质酸,为其临床上治疗骨关节炎提供基础理论依据。方法以透明质酸钠为原料,用1-(3-二甲氨基丙基)-3-乙基碳二亚胺( EDC )活化羧基,加入带二硫键的化合物——胱胺二盐酸盐,使其与透明质酸钠的羧基反应交联成带稳定二硫键的透明质酸水凝胶,再用二硫苏糖醇( DTT )还原二硫键成巯基,制得巯基化透明质酸。结果该制备得巯基化透明质酸的巯基含量平均达到24.19%。对其进行还原力、羟自由基清除能力、超氧阴离子自由基清除能力检测表明,该巯基化透明质酸还原力相当于同等浓度维生素 C 的(4.15±0.21)%,对羟自由基的50%清除浓度约为5 mg / ml,对邻苯三酚的自氧化反应也有显著的抑制作用,加入10 mg / ml 的该样品其邻苯三酚的氧化速率仅为原始自氧化速率的20%( P<0.05)。结论注射透明质酸对关节软骨有很好的润滑作用,同时用巯基改性后具备较好的抗氧化性能。巯基化合物作为供氢体,去猝灭自由基,自身被氧化成稳定的二硫键,不会再发生链反应。本实验利用巯基的抗氧化性,改性透明质酸钠,使其具备一定的抗氧化性能,即清除自由基能力,为其临床的进一步应用提供了基础理论依据。
目的:製備一種具有一定清除自由基能力的巰基化透明質痠,為其臨床上治療骨關節炎提供基礎理論依據。方法以透明質痠鈉為原料,用1-(3-二甲氨基丙基)-3-乙基碳二亞胺( EDC )活化羧基,加入帶二硫鍵的化閤物——胱胺二鹽痠鹽,使其與透明質痠鈉的羧基反應交聯成帶穩定二硫鍵的透明質痠水凝膠,再用二硫囌糖醇( DTT )還原二硫鍵成巰基,製得巰基化透明質痠。結果該製備得巰基化透明質痠的巰基含量平均達到24.19%。對其進行還原力、羥自由基清除能力、超氧陰離子自由基清除能力檢測錶明,該巰基化透明質痠還原力相噹于同等濃度維生素 C 的(4.15±0.21)%,對羥自由基的50%清除濃度約為5 mg / ml,對鄰苯三酚的自氧化反應也有顯著的抑製作用,加入10 mg / ml 的該樣品其鄰苯三酚的氧化速率僅為原始自氧化速率的20%( P<0.05)。結論註射透明質痠對關節軟骨有很好的潤滑作用,同時用巰基改性後具備較好的抗氧化性能。巰基化閤物作為供氫體,去猝滅自由基,自身被氧化成穩定的二硫鍵,不會再髮生鏈反應。本實驗利用巰基的抗氧化性,改性透明質痠鈉,使其具備一定的抗氧化性能,即清除自由基能力,為其臨床的進一步應用提供瞭基礎理論依據。
목적:제비일충구유일정청제자유기능력적구기화투명질산,위기림상상치료골관절염제공기출이론의거。방법이투명질산납위원료,용1-(3-이갑안기병기)-3-을기탄이아알( EDC )활화최기,가입대이류건적화합물——광알이염산염,사기여투명질산납적최기반응교련성대은정이류건적투명질산수응효,재용이류소당순( DTT )환원이류건성구기,제득구기화투명질산。결과해제비득구기화투명질산적구기함량평균체도24.19%。대기진행환원력、간자유기청제능력、초양음리자자유기청제능력검측표명,해구기화투명질산환원력상당우동등농도유생소 C 적(4.15±0.21)%,대간자유기적50%청제농도약위5 mg / ml,대린분삼분적자양화반응야유현저적억제작용,가입10 mg / ml 적해양품기린분삼분적양화속솔부위원시자양화속솔적20%( P<0.05)。결론주사투명질산대관절연골유흔호적윤활작용,동시용구기개성후구비교호적항양화성능。구기화합물작위공경체,거졸멸자유기,자신피양화성은정적이류건,불회재발생련반응。본실험이용구기적항양화성,개성투명질산납,사기구비일정적항양화성능,즉청제자유기능력,위기림상적진일보응용제공료기출이론의거。
Objective To synthesize a thiol modiifed hyaluronic acid with a certain ability of scavenging free radicals and to provide theory basis for the clinical treatment of osteoarthritis.Methods Sodium hyaluronic acid ( HA ) as raw material, 1- ( 3-dimethylaminopropyl ) -3- ethylcarbodiimide hydrochloride ( EDC ) was used to activate the carboxyl of HA and cystamin dihydrochloride was introduced to crosslink the HA hydrogel. Subsequently, dithiothreitol ( DTT ) was used to deoxidize the disulifde linkage into thiol and the thiol-HA was achieved.Results The thiol content of thiol-HA was 24.19%. The reducing capacity, the rate of hydroxyl radical scavenging and the rate of superoxide anion clearance were chosen to evaluate the antioxidant activities of the thiol-HA. The experimental results showed that the reducing force of the thiol-modiifed HA was equivalent with ( 4.15±0.21 ) % of vitamin C at the same concentration. Meanwhile, the concentration of the thiol-HA at 50% of the hydroxyl free radical scavenging was about 5 mg / ml. 10 mg / ml of the sample was added, the oxidation rate of pyrogallol was decreased to 20% of its autoxidation rate (P<0.05 ).Conclusions The articular cartilage is well lubricated by the injection of hyaluronic acid. Better oxidation resistance is achieved by the modiifcation of thiol. As a hydrogen donor, free radicals are quenched by thiol compounds which are oxidized to stable disulfide bond without chain reaction. In this research, sodium hyaluronate is modiifed by thiol with its oxidation resistance, therefore a certain antioxidant property is achieved with the ability of scavenging free radicals. And a theory basis is provided for the further clinical application.