首页> 外国专利> APPLICATION OF TETRAHYDROPALMATINE IN PREPARATION OF DRUGS AGAINST OXALIPLATIN-INDUCED PERIPHERAL NEUROTOXICITY

APPLICATION OF TETRAHYDROPALMATINE IN PREPARATION OF DRUGS AGAINST OXALIPLATIN-INDUCED PERIPHERAL NEUROTOXICITY

机译:四氢丙氨酸在氧化铂诱导的外周神经毒性制备药物中的应用

摘要

An application of tetrahydropalmatine in the preparation of drugs against oxaliplatin-induced peripheral neurotoxicity. Tetrahydropalmatine has an inhibitory effect on transporters OCTN1, OCTN2 and OCT2 that mediate the uptake of OXA by DRG neurons, but has no significant inhibitory effect on an MRP2 transporter that mediates OXA efflux. The tetrahydropalmatine can reduce the accumulation of the OXA in primary cultured DRG neurons and reduce the DRG neurotoxicity induced by the OXA. The tetrahydropalmatine significantly reduces the concentration of the OXA in DRG of mice and rats, and significantly reduces the peripheral neurotoxicity in mice and rats induced by the OXA. The tetrahydropalmatine does not reduce the concentration of the OXA in tumor tissues in tumor-bearing nude mice and the antitumor activity of the OXA. Therefore, the tetrahydropalmatine can reduce the peripheral neurotoxicity of the OXA, but does not weaken the antitumor efficacy thereof.
机译:四氢丙氨酸在氧化素诱导的外周神经毒性制备药物中的应用。 四氢丙氨酸对转运蛋白OctN1,Octn2和Oct2具有抑制作用,DRG神经元介导OXA的摄取,但对MRP2转运蛋白没有显着的抑制作用,介导OXA流出。 四氢丙氨酸可以减少原发性培养的DRG神经元中的氧气积聚,并减少了由OXA诱导的DRG神经毒性。 四氢丙氨酸显着降低了小鼠和大鼠DRG中的OXA的浓度,并显着降低了OXA诱导的小鼠的周围神经毒性。 四氢丙氨酸不会降低肿瘤组织中肿瘤组织中的氧气浓度和氧气的抗肿瘤活性。 因此,四氢丙氨酸可以减少氧气的周围神经毒性,但不会削弱其抗肿瘤功效。

著录项

  • 公开/公告号WO2021169194A1

    专利类型

  • 公开/公告日2021-09-02

    原文格式PDF

  • 申请/专利权人 ZHEJIANG UNIVERSITY;

    申请/专利号WO2020CN109411

  • 申请日2020-08-16

  • 分类号A61K31/4375;A61K31/55;A61P25/02;A61P39/02;

  • 国家 CN

  • 入库时间 2022-08-24 22:26:11

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