第十二章抗肿瘤药物ChapterAntineoplasticDrugs讲解.pptx

第十二章抗肿瘤药物Chapter12AntineoplasticDrugs第四节抗肿瘤植物药有效成分

Section4ActiveIngredientsofAntitumorBotanicals

第四节抗肿瘤植物药有效成分

Section4ActiveIngredientsofAntitumorBotanicals(一)喜树碱和羟基喜树碱Camptothecinandhydroxycamptothecin是从中国特有珙桐科植物喜树中分离得到的两种生物碱，作用于DNA拓扑异构酶I，对肝癌、大肠癌、白血病等有效，但副作用较大。TheyaretwokindsofalkaloidsisolatedfromtheuniqueChinesenyssaceaeplant,camptothecaacuminata.ItactsonDNAtopoisomeraseI,andiseffectiveforlivercancer,colorectalcancer,leukemia,etc.,butthesideeffectsarerelativelylarge.喜树Camptothecaacuminata

(二)长春碱和长春新碱Vincaleukoblastinumandvincristine与微管蛋白结合阻止微管蛋白双微体聚合成为微管；又可诱导微管的解聚，使纺锤体不能形成，细胞停止于分裂中期，从而阻止肿瘤细胞分裂繁殖。Itiscombinedwithtubulintopreventtubulindoublemicrosomesfrompolymerizingintomicrotubules;itcanalsoinducethedepolymerizationofmicrotubules,sothatthespindlebodycannotbeformed,andthecellsstopinthemiddlestageofdivision,therebypreventingtumorcellsfromdividingandmultiplying.——天然的抗肿瘤生物碱，结构中含有吲哚环——Naturalanti-tumoralkaloidwithindoleringinitsstructure

长春碱用于治疗各种实体瘤，长春新碱用于急性及慢性白血病等。对长春碱进行结构改造，合成长春地辛和长春瑞滨。Thevincaleukoblastinumisusedfortreatingvarioussolidtumors,acuteandchronicleukemia.Thestructureofthevincaleukoblastinumismodifiedtosynthesizevindesineandvinorelbine.

(三)鬼臼素及其衍生物Podophyllotoxinanditsderivatives鬼臼素是一种生物碱，具有抗癌活性，由于毒性大不能用于临床，它的半合成衍生物依托泊苷、替尼泊苷用于临床。Podophyllotoxinisanalkaloidwithanti-canceractivity.Itcannotbeusedclinicallyduetohightoxicity,Itssemi-syntheticderivatives,suchasetoposideandteniposidecanbeusedclinicallywith.

(四)紫杉醇Paclitaxel从红豆杉的树皮和树叶中提取的生物碱，为具有紫杉烯环的二萜类化合物，临床用于卵巢癌和乳腺癌的治疗。ThealkaloidsextractedfromthebarkandleavesofTaxuschinensisarediterpenoidcompoundswithataxanering,anditisclinicallyusedfortreatingovariancancerandbreastcancer.Paclitaxel

1.结构特点Structuralcharacteristics具有紫杉烷骨架的二萜类化合物Diterpenoidcompoundwitha