a Reata Pharmaceuticals, Inc., Irving, Texas 75063; and.
Radiat Res. 2014 May;181(5):512-20. doi: 10.1667/RR13578.1. Epub 2014 Apr 10.
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.
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。
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