文档介绍：苦参碱衍生物的合成及其体内抑制肝癌H22细胞活性研究摘要苦参碱广泛存在于豆科植物苦参、苦豆子、广豆根等中,具有降温, 解热、镇静、镇痛、抗心律失常、保护心肌缺血作用,另外在抗乙型肝炎病毒,诱导肿瘤细胞增殖、分化、凋亡等方面,显示出多种药理活性,在肿瘤、乙型肝炎和其他疾病治疗上面有新的医学发展前景。由于苦参碱存在化学稳定性差、生物利用度较低、对中枢神经系统有毒副作用等缺点, 所以其利用度并不广泛。因此通过化学方法对苦参碱进行结构修饰,以期增强其药理活性、降低毒性,对于苦参碱的开发应用具有重要意义。在参照苦参碱的化学结构以及其具有的药理活性的基础上,设计并合成了28个结构新颖的苦参碱衍生物,并采用1HNMR,MS,II澍他们进行了结构表征,确认为目标化合物。经过体内抗肿瘤活性测试表明:所合成的化合物均具有不同程度的抗肿瘤活性作用。以环磷酰***和苦参碱为阳性对照药,通过对比目标化合物的抑制率发现:、;化合物RW23、RW28的抗肿瘤活性与环磷酰***相当,但优于苦参碱。关键词:苦参碱衍生物合成抗肿瘤 SYNTHESIS 0F M ATRINE DERn陷LTIVES AND ITS EFFECT INVIVo AB STRACT Matrine iswidely found inflavescentsophora,sophora alopecuroides Land radixsophorae modem medical research indicated thatthe ponents ofthesememcines,matrine,has agood effect on lowing temperature,antipyreticeffect,sedation,tramadol,antiarrhythmic,protecting myocardial ischemia,besides,matrine show avariety ofpharmac ological activity on treating chromc hepatitisB,inducing proliferation,differentiation, andapoptosis intumor ithas anew medicinedevelopment prospect in the treatment oftumors,hepatitis Band widespread use of matrine islimitedbecause itspoor chemical stabilityis,lowbioavailability and toxicsideeffects on central nervo US we can use some chemical ways tochange itsstucture SO astoenhancedpharmacological activity and reducedtoxicity. Considering the pharmacological activity and the structure ofmalrine, twenty-eight novel structure ofmatrine derivatives have been designed and pounds wereidentifiedby1HNMR,MS and IR. The resultsof the initialanti-hepatoma invivo tests showed pounds had effect inanti—hepatoma their inhibitionrate,we foundtheactivity ofRW0 1 toRW22,RW24 toRW27 isthe salTle asthereferencesubstances activity ofRW23,RW28 isthe salne asthe reference substances ofcyclophosphamide,higer thancyclophospha mide. KEY WORDS:matrine;derivatives;synthesis;anti-tumor; III 广西大掣啊页士掌位论文