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6,6'-亚甲基双(2,2,4-三甲基-1,2-二氢喹啉)(MTDQ)——一种仲胺型自由基结合抗氧化剂的生物药理学研究

Biopharmacological investigation of 6,6'methylene-bis/2,2,4-trimethyl-1,2-dihydroquinoline (MTDQ) a radical binding antioxidant of secondary amine type.

作者信息

Bär V, Erdélyi V, Foris G, Pollák Z, Eckhardt S

出版信息

Neoplasma. 1977;24(3):253-8.

PMID:895935
Abstract

The evidence of free radicals in tumor tissue and the possibility of their experimental influencing by means of antioxidants justifies the search for new pharmacological groups of tumor inhibiting agents. The authors synthesized a sterically inhibited, heterocyclic, bifunctional, non-toxic radical binding antioxidant of secondary amine type. The structural change is interpreted with the possibility of recombination characteristic for secondary amine groups and the double chain closing effect. The conjugation effect secures mobility of the hydrogen atom. The compound contains 10 to 12 per cent dimer-trimer of higher biological activity than monomers, due to higher molecular weight. An additional pharmacodynamic advantage compared to hitherto known antioxidants consists in its lower vapour volutility and the biradicality.

摘要

肿瘤组织中自由基的证据以及通过抗氧化剂对其进行实验性影响的可能性,为寻找新型肿瘤抑制药物类别提供了依据。作者合成了一种空间位阻型、杂环、双功能、无毒的仲胺型自由基结合抗氧化剂。结构变化被解释为仲胺基团的重组特性和双链封闭效应的可能性。共轭效应确保了氢原子的移动性。由于分子量较高,该化合物含有10%至12%的二聚体-三聚体,其生物活性高于单体。与迄今已知的抗氧化剂相比,其额外的药效学优势在于较低的蒸汽挥发性和双自由基性。

相似文献

1
Biopharmacological investigation of 6,6'methylene-bis/2,2,4-trimethyl-1,2-dihydroquinoline (MTDQ) a radical binding antioxidant of secondary amine type.6,6'-亚甲基双(2,2,4-三甲基-1,2-二氢喹啉)(MTDQ)——一种仲胺型自由基结合抗氧化剂的生物药理学研究
Neoplasma. 1977;24(3):253-8.
2
[Investigation on radiosensitizing and tumor inhibiting actions of the antioxidant MTDQ (6,6'-methylen-bis/2,2,4-trimethyl-1-1,2-dihydroquinolin) (author's transl)].抗氧化剂MTDQ(6,6'-亚甲基双/2,2,4-三甲基-1,2-二氢喹啉)的放射增敏和抑瘤作用研究(作者译)
Arch Geschwulstforsch. 1975;45(5):489-95.
3
Clinical trials with MTDQ /6,6'-methylene-bis (2,2,4-trimethyl-1,2-dihydroquinoline)/ an antioxidant with radiation sensitizing effect.使用MTDQ(6,6'-亚甲基双(2,2,4-三甲基-1,2-二氢喹啉))进行的临床试验,MTDQ是一种具有辐射增敏作用的抗氧化剂。
Strahlentherapie. 1980 Mar;156(3):198-200.
4
Inhibition by an antioxidant of the carcinogenic effect of nitrosomorpholine formed in vivo.一种抗氧化剂对体内形成的亚硝基吗啉致癌作用的抑制。
IARC Sci Publ. 1982(41):659-64.
5
Acute carbon tetrachloride induced lysosomal membrane damage and the membrane protecting effect of a new dihydroquinoline-type antioxidant.急性四氯化碳诱导的溶酶体膜损伤及一种新型二氢喹啉类抗氧化剂的膜保护作用
Int J Tissue React. 1982;4(4):325-30.
6
Cytoprotective effect of free radical scavengers against mucosal damage produced by different antirheumatic drugs.自由基清除剂对不同抗风湿药物所致黏膜损伤的细胞保护作用。
Int J Tissue React. 1986;8(1):35-40.
7
Spin-trapping studies with MTDO, a dihydroquinoline type radical scavenger.使用MTDO(一种二氢喹啉型自由基清除剂)进行自旋捕获研究。
Acta Physiol Hung. 1989;74(3-4):291-4.
8
Liver lipid peroxidation induced by cholesterol and its treatment with a dihydroquinoline type free radical scavenger in rabbits.胆固醇诱导的兔肝脏脂质过氧化及其用二氢喹啉型自由基清除剂的治疗
Acta Physiol Hung. 1984;64(3-4):437-42.
9
[Study of the biochemical and radiochemical effects of the agent MTDQ (author's transl].[药物MTDQ的生化和放射化学效应研究(作者译)]
Strahlentherapie. 1978 Jul;154(7):499-502.
10
Effects of allopurinol, (+)-cyanidanol-3 and dihydroquinoline-type antioxidants on rat hepatic microsomal cytochrome P-450 and monooxygenases.别嘌醇、(+)-儿茶素-3和二氢喹啉型抗氧化剂对大鼠肝微粒体细胞色素P-450和单加氧酶的影响。
Int J Clin Pharmacol Ther Toxicol. 1987 Apr;25(4):201-3.