60.下列何者之抗癌作用與金屬螯合(chelation)有關?
(A)doxorubicin
(B)dactinomycin
(C)mitomycin
(D)mitoxantrone
統計: A(4358), B(891), C(1473), D(1085), E(0) #2037522
詳解 (共 10 筆)
還有bleomycin 可與Fe2+螯合
Foye課本上原文:
Anthracycline anticancer agents are also known to interfere with normal ferritin-iron mobilization, resulting in iron accumulation . The anthracyclines chelate strongly with di- and trivalent cations, including intracellular Fe2+, so the generation of cytotoxic hydroxyl radicals after the initial NADPH/CYP450 reductase reduction is essentially guaranteed. Hydroxide anion and Fe3+ are also formed during the production of hydroxyl radicals. Anthracycline–iron complexes (particularlythose involving Fe+3) can also spontaneously generate ROS without the aid of enzymatic catalysis.

另外補充:foye課本查到doxorubicin跟DNA的結合位如下:

(B) dactinomycin是抗生素類的抗癌藥,作用在拓樸異構酶2上面
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72 無法與二價金屬離子螯合(chelation)而形成複合物之抗生素為:
(A) Bleomycin
(B) Doxorubicin
(C) Mitomycin C → 嵌入DNA使之斷裂、烷基化產生cross-link
(D) Oxytetracycline
專技 - 藥理學與藥物化學- 99 年 - 099-2-藥師-藥理學與藥物化學#10002
答案:C
77.Doxorubicin與daunorubicin之結構差異在於前者比後者:
(A)多一個NH2
(B)少一個NH2
(C)多一個OH
(D)少一個OH .
專技 - 藥理學與藥物化學- 103 年 - 103-1-藥師-藥理學與藥物化學#14226
78.長期使用doxorubicin造成心毒性,是由於在體內產生何種代謝物? (103-1)
(A)Epirubicin
(B)Dexrazoxane
(C)Doxorubicinol
(D)Doxorubicin glucuronide
79.下列有關anthracyclines類抗癌藥之敘述,何者錯誤?
(A)Fe2+可螯合在anthracyclinone上之OH及=O間
(B)Anthracyclinone部分可以嵌入DNA中
(C)受NADPH/CYP450 reductase作用,產生 anthracycline hydroquinone
(D)C-7接有D-daunosamine醣基 → L-daunosamine
專技 - 藥理學與藥物化學- 102 年 - 102-1-藥師-藥理學與藥物化學#10014
答案:D
Mitoxantrone
抑制TOP II
SE: 藍綠色尿液
無還原反應,不產生自由基,無心毒性
代謝途徑: N-dealkylation, oxidative deamination, glucuronidation