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DW1029M,一种新型植物药候选物,可抑制晚期糖基化终产物形成、大鼠晶状体醛糖还原酶活性和 TGF-β1 信号通路。

DW1029M, a novel botanical drug candidate, inhibits advanced glycation end-product formation, rat lens aldose reductase activity, and TGF-β1 signaling.

机构信息

Department of Research and Development, Dong-Wha Pharmaceutical Company, Giheung Gu, Yong-In City, Republic of Korea; School of Biological Sciences, Seoul National University, Seoul, Republic of Korea; and.

Department of Research and Development, Dong-Wha Pharmaceutical Company, Giheung Gu, Yong-In City, Republic of Korea;

出版信息

Am J Physiol Renal Physiol. 2014 May 15;306(10):F1161-70. doi: 10.1152/ajprenal.00651.2013. Epub 2014 Apr 2.

DOI:10.1152/ajprenal.00651.2013
PMID:24694590
Abstract

DW1029M is a botanical extract consisting of Morus bark and Puerariae radix, produced by Dong-Wha Pharmaceutical, for nephroprotective drug development; it has been in phase II clinical trials in Korea. In our mechanistic investigations, we found that DW1029M inhibits advanced glycation end products (AGEs), rat lens aldose reductase (RLAR), and transforming growth factor (TGF)-β1 signaling, all of which are implicated in diabetic complications such as diabetic nephropathy and diabetic retinopathy. DW1029M inhibits AGE formation via Fe(2+) chelation. The extract contains 13 active constituents that inhibit AGE formation, 8 active constituents that inhibit RLAR activity, and 1 inhibitor of TGF-β1 signaling. Our results suggest DW1029M protects against diabetic nephropathy via blockade of AGE formation, RLAR activity, and TGF-β1 signaling.

摘要

DW1029M 是一种植物提取物,由 Dong-Wha 制药公司生产,用于开发肾保护药物,它已在韩国进行 II 期临床试验。在我们的机制研究中,我们发现 DW1029M 可抑制晚期糖基化终产物 (AGEs)、大鼠晶状体醛糖还原酶 (RLAR) 和转化生长因子 (TGF)-β1 信号通路,这些都与糖尿病并发症有关,如糖尿病肾病和糖尿病视网膜病变。DW1029M 通过螯合 Fe(2+)来抑制 AGE 的形成。该提取物含有 13 种可抑制 AGE 形成的活性成分、8 种可抑制 RLAR 活性的活性成分和 1 种可抑制 TGF-β1 信号通路的抑制剂。我们的研究结果表明,DW1029M 通过阻断 AGE 形成、RLAR 活性和 TGF-β1 信号通路来预防糖尿病肾病。

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