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Poly medicine tolerance restrainers and revelation inhibiter

机译:多元药物耐受性限制和启示抑制剂

摘要

PURPOSE: To obtain a multidrug resistance inhibitor, capable of inhibiting the multidrug resistance and maintaining anticancer action essentially possessed by an anticancer agent without exhibiting any toxicity as in the case of Ca2+ antagonistic agents which have hitherto been used as the multidrug resistance inhibitor. ;CONSTITUTION: A multidrug resistance inhibitor containing a flavonoid or its pharmaceutically permissible salt, especially quercetin as an active ingredient in an amount of 0.01-99wt.%, preferably 0.1-80wt.%. Since the above-mentioned active ingredient is capable of inhibiting and suppressing the action of substances for inducing or enhancing the transcription and expression of a multidrug resistance gene (MDR1), the anticancer action essentially possessed by an anticancer agent can be maintained or enhanced. Since the above-mentioned gene MDR1 expressed in tumorous cells having the multidrug resistance is inhibited at a transcription level, the inhibitor has no toxicity as in the case of Ca2+ antagonistic agents. Furthermore, the dose of the multidrug resistance inhibitor is normally about 1-500mg per adult expressed as the amount of the quercetin and orally or parenterally administered in about 1-4 divided portions a day.;COPYRIGHT: (C)1993,JPO&Japio
机译:用途:获得一种多药耐药抑制剂,该药能够抑制多药耐药性并保持抗癌剂基本具有的抗癌作用,而不会像迄今为止一直使用的Ca 2 + 拮抗剂那样具有任何毒性。用作多药耐药性抑制剂。组成:一种多药耐药性抑制剂,其含有黄酮类化合物或其药学上允许的盐,尤其是槲皮素作为活性成分,含量为0.01-99wt。%,优选为0.1-80wt。%。由于上述活性成分能够抑制和抑制用于诱导或增强多药抗性基因(MDR1)的转录和表达的物质的作用,因此可以维持或增强抗癌剂基本具有的抗癌作用。由于在具有多药耐药性的肿瘤细胞中表达的上述基因MDR1在转录水平上被抑制,因此该抑制剂不像Ca 2 + 拮抗剂那样具有毒性。此外,多药耐药性抑制剂的剂量通常为每个成年人约1-500mg,以槲皮素的量表示,每天口服或胃肠外给药约1-4次。(COPYRIGHT:(C)1993,JPO&Japio

著录项

  • 公开/公告号JP2514500B2

    专利类型

  • 公开/公告日1996-07-10

    原文格式PDF

  • 申请/专利权人 KUREHA CHEMICAL IND CO LTD;

    申请/专利号JP19910263234

  • 发明设计人 KOMANO TOORU;NAGATA KAZUHIRO;

    申请日1991-09-14

  • 分类号A61K31/35;

  • 国家 JP

  • 入库时间 2022-08-22 03:56:51

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