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表皮多胺耗竭对甲基乙二醛双(脒腙)在小鼠皮肤中蓄积的影响。

Effect of epidermal polyamine depletion on the accumulation of methylglyoxal bis(guanylhydrazone) in mouse skin.

作者信息

Käpyaho K, Linnamaa K, Jänne J

出版信息

J Invest Dermatol. 1982 May;78(5):391-4. doi: 10.1111/1523-1747.ep12507519.

DOI:10.1111/1523-1747.ep12507519
PMID:6802903
Abstract

A systemic or topical treatment of mice with alpha-difluoromethylornithine, and irreversible inhibitor of mammalian ornithine decarboxylase, produced a rapid depletion of epidermal putrescine and spermidine. When methylglyoxal bis(guanylhydrazone), another inhibitor of polyamine biosynthesis and a potent antiproliferative agent, was subsequently administered the epidermal concentration of the latter drug rose distinctly higher than without a prior difluoromethyl ornithine treatment. The combined use of these 2 antimetabolites of polyamines also profoundly depressed epidermal DNA synthesis, especially in UV-irradiated skin. A "priming" with difluoromethyl ornithine may therefore offer a means to enhance the epidermal accumulation of otherwise poorly absorbed methylglyoxal bis(guanylhydrazone).

摘要

用α-二氟甲基鸟氨酸(一种哺乳动物鸟氨酸脱羧酶的不可逆抑制剂)对小鼠进行全身或局部治疗,会使表皮腐胺和亚精胺迅速耗竭。随后给予甲基乙二醛双(脒腙)(另一种多胺生物合成抑制剂和强效抗增殖剂)时,后一种药物在表皮中的浓度明显高于未预先用二氟甲基鸟氨酸治疗的情况。这两种多胺抗代谢物联合使用也会显著抑制表皮DNA合成,尤其是在紫外线照射的皮肤中。因此,用二氟甲基鸟氨酸进行“预处理”可能提供一种方法来增强原本吸收不良的甲基乙二醛双(脒腙)在表皮中的蓄积。

相似文献

1
Effect of epidermal polyamine depletion on the accumulation of methylglyoxal bis(guanylhydrazone) in mouse skin.表皮多胺耗竭对甲基乙二醛双(脒腙)在小鼠皮肤中蓄积的影响。
J Invest Dermatol. 1982 May;78(5):391-4. doi: 10.1111/1523-1747.ep12507519.
2
Inhibition of DNA and protein synthesis in UV-irradiated mouse skin by 2-difluoromethylornithine, methylglyoxal bis(guanylhydrazone), and their combination.二氟甲基鸟氨酸、甲基乙二醛双(脒腙)及其组合对紫外线照射的小鼠皮肤中DNA和蛋白质合成的抑制作用
J Invest Dermatol. 1983 Aug;81(2):102-6. doi: 10.1111/1523-1747.ep12542177.
3
Combined topical use of difluoromethyl ornithine and methylglyoxal bis (guanylhydrazone) in UV-irradiated mouse skin.二氟甲基鸟氨酸与甲基乙二醛双(胍腙)联合局部应用于紫外线照射的小鼠皮肤。
Br J Dermatol. 1982 Oct;107(4):415-21. doi: 10.1111/j.1365-2133.1982.tb00384.x.
4
Glyoxal bis(guanylhydrazone) as an inhibitor of polyamine biosynthesis in tumour cells.乙二醛双(脒腙)作为肿瘤细胞中多胺生物合成的抑制剂
Biochem J. 1984 Jul 15;221(2):483-8. doi: 10.1042/bj2210483.
5
Suppression of the formation of polyamines and macromolecules by DL-alpha-difluoromethylornithine and methylglyoxal bis(guanylhydrazone) in phytohaemagglutinin-activated human lymphocytes.DL-α-二氟甲基鸟氨酸和甲基乙二醛双(脒腙)对植物血凝素激活的人淋巴细胞中多胺和大分子形成的抑制作用
Biochem J. 1979 Jan 15;178(1):109-17. doi: 10.1042/bj1780109.
6
Methylglyoxal BIS (guanylhydrazone) and alpha-difluoromethylornithine-induced polyamine deprivation in psoriatic lesions.甲基乙二醛双(胍基腙)和α-二氟甲基鸟氨酸诱导银屑病皮损中的多胺缺乏。
Acta Derm Venereol. 1982;62(3):221-4.
7
Differential effects of 2-difluoromethylornithine and methylglyoxal bis(guanylhydrazone) on the testosterone-induced growth of ventral prostate and seminal vesicles of castrated rats.2-二氟甲基鸟氨酸和甲基乙二醛双(脒腙)对去势大鼠睾酮诱导的前列腺腹侧叶和精囊生长的不同作用。
Biochem J. 1984 May 1;219(3):811-7. doi: 10.1042/bj2190811.
8
Inhibitors of polyamine biosynthesis. 4. Effects of alpha-methyl-(+/-)-ornithine and methylglyoxal bis(guanylhydrazone) on growth and polyamine content of L1210 leukemic cells of mice.多胺生物合成抑制剂。4. α-甲基-(±)-鸟氨酸和甲基乙二醛双(脒腙)对小鼠L1210白血病细胞生长和多胺含量的影响。
J Med Chem. 1977 Feb;20(2):249-53. doi: 10.1021/jm00212a012.
9
Differential effect of alpha-difluoromethylornithine on the in vivo uptake of 14C-labeled polyamines and methylglyoxal bis(guanylhydrazone) by a rat prostate-derived tumor.α-二氟甲基鸟氨酸对大鼠前列腺衍生肿瘤体内摄取14C标记的多胺和甲基乙二醛双(胍腙)的差异作用。
Cancer Res. 1984 Mar;44(3):1034-40.
10
Inhibition of the synthesis of polyamines and DNA in activated lymphocytes by a combination of alpha-methylornithine and methylglyoxal bis(guanylhydrazone).α-甲基鸟氨酸与甲基乙二醛双(脒腙)联合使用对活化淋巴细胞中多胺和DNA合成的抑制作用
Cancer Res. 1977 Sep;37(9):3169-72.

引用本文的文献

1
Regulation of the expression of human ornithine decarboxylase gene and ornithine decarboxylase promoter-driven reporter gene in transgenic mice.转基因小鼠中人类鸟氨酸脱羧酶基因表达及鸟氨酸脱羧酶启动子驱动的报告基因的调控
Biochem J. 1993 Jun 15;292 ( Pt 3)(Pt 3):927-32. doi: 10.1042/bj2920927.
2
Alterations in human circulating and bone marrow mononuclear cell polyamine levels in hematologic malignancies as a consequence of difluoromethylornithine administration.由于给予二氟甲基鸟氨酸导致血液系统恶性肿瘤患者循环和骨髓单个核细胞多胺水平的改变。
Invest New Drugs. 1988 Jun;6(2):125-34. doi: 10.1007/BF00195371.