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新型有机硒化合物6-苯基-7(6H)-异硒唑并[4,3-d]嘧啶酮(ISP)对P388小鼠白血病生长的抗肿瘤作用。

Antitumor effect of a new organic selenium compound, 6-phenyl-7 (6H)-isoselenazolo [4,3-d] pyrimidone (ISP), on the growth of P388 mouse leukemia.

作者信息

Ito H, Wang J Z, Shimura K, Sakakibara J, Ueda T

机构信息

Department of Pharmacology, Mie University School of Medicine, Japan.

出版信息

Anticancer Res. 1990 Jul-Aug;10(4):891-5.

PMID:2382986
Abstract

The organic selenium compound, ISP [6-phenyl-7(6H)-isoselenazolo [4,3-d] pyrimidone] markedly inhibited the growth of P388 mouse leukemia at dose of 100 micrograms/mouse per day x 10 with no sign of toxicity. The antitumor activity of 4,5-dihydro-4-methyl-6-oxo-5-phenyl-6H-pyrazolo [4,5-c] isoselenazole (PIS) was weaker than that of ISP. The total lipid and phospholipid contents in the leukemic cells treated with ISP were significantly decreased. The fatty acid pattern of cholesterol esters, phosphatidyl choline and phosphatidyl ethanolamine from the ISP-treated P388 leukemic cells differed markedly from that of the corresponding lipids from the control leukemic cells. In addition, the synthesis of DNA or RNA was depressed in the ISP-treated leukemic cells. The present results indicate that ISP may open new perspectives in cancer chemotherapy.

摘要

有机硒化合物ISP[6-苯基-7(6H)-异硒唑并[4,3-d]嘧啶酮]在剂量为100微克/小鼠/天×10天时显著抑制P388小鼠白血病的生长,且无毒性迹象。4,5-二氢-4-甲基-6-氧代-5-苯基-6H-吡唑并[4,5-c]异硒唑(PIS)的抗肿瘤活性比ISP弱。用ISP处理的白血病细胞中的总脂质和磷脂含量显著降低。来自经ISP处理的P388白血病细胞的胆固醇酯、磷脂酰胆碱和磷脂酰乙醇胺的脂肪酸模式与对照白血病细胞相应脂质的脂肪酸模式明显不同。此外,经ISP处理的白血病细胞中DNA或RNA的合成受到抑制。目前的结果表明,ISP可能为癌症化疗开辟新的前景。

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