文献检索文档翻译深度研究
Suppr Zotero 插件Zotero 插件
邀请有礼套餐&价格历史记录

新学期,新优惠

限时优惠:9月1日-9月22日

30天高级会员仅需29元

1天体验卡首发特惠仅需5.99元

了解详情
不再提醒
插件&应用
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
高级版
套餐订阅购买积分包
AI 工具
文献检索文档翻译深度研究
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2025

局部应用合成三萜 RTA 408 可保护小鼠免受辐射诱导的皮炎。

Topical application of the synthetic triterpenoid RTA 408 protects mice from radiation-induced dermatitis.

机构信息

a  Reata Pharmaceuticals, Inc., Irving, Texas 75063; and.

出版信息

Radiat Res. 2014 May;181(5):512-20. doi: 10.1667/RR13578.1. Epub 2014 Apr 10.


DOI:10.1667/RR13578.1
PMID:24720753
Abstract

Free radicals produced during cancer radiotherapy often leads to dermatitis, with the insult ranging from mild erythema to moist desquamation and ulceration. This toxicity can be dose limiting and promote chronic complications, such as fibrosis and wound recurrence. The purpose of this study was to evaluate if RTA 408, a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor nuclear factor-kappa b (NF-κB), could protect skin from radiation-induced dermatitis. Mice were irradiated (10 Gy/day) on days 0-2 and 5-7, and RTA 408 (0.01%, 0.1% and 1.0%) was topically applied once daily starting on day 5 or up to day 40. Dermatitis severity was evaluated using a scale ranging from 0 (normal) to 5 (frank ulceration), as well as histologically. The mRNA expression of Nrf2 and NF-κB target genes in skin was also evaluated. RTA 408 (0.01%, 0.1% and 1.0%) reduced the percentage of animal-days with scores ≥2 by 11%, 31% and 55% and scores ≥3 by 16%, 60% and 80%, respectively. Dose-dependent improvements in the appearance of skin were also manifestly visible, with RTA 408 at 1.0% eliciting a normal macroscopic appearance by the end of the treatment period on day 40, including substantial hair regrowth. Moreover, 1.0% RTA 408 markedly reduced epidermal and collagen thickening, prevented dermal necrosis and completely alleviated skin ulcers. These improvements were associated with significant increases in Nrf2 target genes and significant decreases in NF-κB target genes. Together, these data indicate that RTA 408 represents a potentially promising new therapy for the treatment of radiation-induced dermatitis.

摘要

自由基在癌症放射治疗过程中产生,往往会导致皮炎,从轻度红斑到湿性脱皮和溃疡不等。这种毒性可能是剂量限制的,并促进慢性并发症,如纤维化和伤口复发。本研究的目的是评估 RTA 408(一种强效激活抗氧化转录因子 Nrf2 并抑制促炎转录因子核因子-κB(NF-κB)的合成三萜)是否可以保护皮肤免受辐射诱导的皮炎。在第 0-2 天和第 5-7 天,用 10 Gy/天照射小鼠,从第 5 天开始,每天一次局部应用 RTA 408(0.01%、0.1%和 1.0%),直至第 40 天。使用 0 至 5 分的量表(0 为正常,5 为严重溃疡)评估皮炎严重程度,以及组织学评估。还评估了皮肤中 Nrf2 和 NF-κB 靶基因的 mRNA 表达。RTA 408(0.01%、0.1%和 1.0%)分别使动物天数的评分≥2 的百分比降低 11%、31%和 55%,评分≥3 的百分比降低 16%、60%和 80%。RTA 408(1.0%)在治疗期结束时(第 40 天)明显改善皮肤外观,表现为正常的宏观外观,包括大量毛发再生。此外,1.0%RTA 408 显著减少表皮和胶原增厚,防止真皮坏死,并完全缓解皮肤溃疡。这些改善与 Nrf2 靶基因的显著增加和 NF-κB 靶基因的显著减少相关。总之,这些数据表明 RTA 408 是一种有潜力的治疗辐射诱导性皮炎的新疗法。

相似文献

[1]
Topical application of the synthetic triterpenoid RTA 408 protects mice from radiation-induced dermatitis.

Radiat Res. 2014-4-10

[2]
Topical application of the synthetic triterpenoid RTA 408 activates Nrf2 and induces cytoprotective genes in rat skin.

Arch Dermatol Res. 2014-7

[3]
A novel Nrf2 activator from microbial transformation inhibits radiation-induced dermatitis in mice.

J Radiat Res. 2016-9

[4]
Topical application of RTA 408 lotion activates Nrf2 in human skin and is well-tolerated by healthy human volunteers.

BMC Dermatol. 2015-7-14

[5]
Topical Application of Phlorotannins from Brown Seaweed Mitigates Radiation Dermatitis in a Mouse Model.

Mar Drugs. 2020-7-22

[6]
The novel triterpenoid RTA 408 protects human retinal pigment epithelial cells against H2O2-induced cell injury via NF-E2-related factor 2 (Nrf2) activation.

Redox Biol. 2016-8

[7]
Targeted Nrf2 activation therapy with RTA 408 enhances regenerative capacity of diabetic wounds.

Diabetes Res Clin Pract. 2018-2-21

[8]
Topical hypochlorite ameliorates NF-κB-mediated skin diseases in mice.

J Clin Invest. 2013-11-15

[9]
RTA 408, A Novel Synthetic Triterpenoid with Broad Anticancer and Anti-Inflammatory Activity.

PLoS One. 2015-4-21

[10]
Mechanisms and therapeutic implications of RTA 408, an activator of Nrf2, in subarachnoid hemorrhage-induced delayed cerebral vasospasm and secondary brain injury.

PLoS One. 2020-10-5

引用本文的文献

[1]
Macrophage derived VEGF regulates macrophage senescence to inhibit radiation-induced dermatitis.

J Transl Med. 2025-9-2

[2]
RTA 408 attenuates TBHP-Induced apoptosis in nucleus pulposus cells via Nrf2/ARE and NF-κB signaling pathways: in vitro and in vivo evidence for mitigating rats' intervertebral disc degeneration.

Arthritis Res Ther. 2025-6-19

[3]
Effectiveness of quality and quantity mononuclear cells for enhancing wound healing in diabetic ischemic limb animal model.

Int Wound J. 2025-4

[4]
Repurposing of a library for high-content screening of inhibitors against Echinococcus granulosus.

Parasit Vectors. 2024-9-3

[5]
Role of ferroptosis in radiation-induced soft tissue injury.

Cell Death Discov. 2024-7-5

[6]
An Overview of Radiation Countermeasure Development in Radiation Research from 1954 to 2024.

Radiat Res. 2024-8-1

[7]
The Role of NRF2 in Trinucleotide Repeat Expansion Disorders.

Antioxidants (Basel). 2024-5-26

[8]
An Experimental Model of Proton-Beam-Induced Radiation Dermatitis In Vivo.

Int J Mol Sci. 2023-11-15

[9]
RTA-408 Regulates p-NF-κB/TSLP/STAT5 Signaling to Ameliorate Nociceptive Hypersensitivity in Chronic Constriction Injury Rats.

Mol Neurobiol. 2024-3

[10]
Autophagy gene Atg7 regulates the development of radiation-induced skin injury and fibrosis of skin.

Skin Res Technol. 2023-6

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

推荐工具

医学文档翻译智能文献检索