源自Anacyclus根部天然植物化学物质的N-(4-羟基苯乙基)-(4E)-癸烯酰胺通过PARK7抑制血管生成改善糖尿病视网膜病变
N-(4-Hydroxyphenethyl)-(4E)-decenamide derived from natural phytochemical of Anacyclus root ameliorates diabetic retinopathy by inhibiting angiogenesis via PARK7.
摘要(中文译文)
Anacyclus pyrethrum（L.）DC.是菊科的一种草本植物。该药用植物在传统医学中被广泛用于治疗糖尿病及其相关并发症。N-(4-羟苯乙基)-(4E)-癸烯酰胺（HPD）是从其根部提取的天然N-烷基酰胺的合成衍生物。迄今为止，HPD对糖尿病视网膜病变（DR）的治疗疗效及分子机制尚未完全阐明。本研究旨在探讨HPD对DR的治疗潜力并阐明其分子机制。化学合成了HPD。采用体外和体内实验评估其抗血管生成功效。运用蛋白质组学分析，结合分子对接和表面等离子体共振（SPR），筛选并验证HPD的直接结合靶点。此外，通过siRNA介导的基因敲低阐明所鉴定靶点在DR病理中的功能作用。体外和体内实验表明，HPD显著抑制了糖尿病视网膜病变（DR）模型小鼠的病理性血管生成并恢复了视网膜厚度。蛋白质组学分析结合表面等离子体共振（SPR）验证揭示，HPD直接且特异性地结合PARK7。此外，敲低PARK7加剧了病理性血管生成，而HPD干预显著逆转了这一表型改变。HPD通过直接靶向PARK7，抑制病理性血管生成、保护视网膜结构并维持血视网膜屏障完整性，从而减轻糖尿病视网膜病变。
Abstract
Anacyclus pyrethrum (L.) DC. is a herbaceous species of the Asteraceae family. This medicinal plant has been widely used in traditional medicine to treat diabetes and its associated complications. N-(4-Hydroxyphenethyl)-(4E)-decenamide (HPD) is a synthetic derivative of natural N-alkylamides extracted from its roots. To date, the therapeutic efficacy and molecular mechanisms of HPD against diabetic retinopathy (DR) have not been fully clarified. This study aimed to explore the therapeutic potential of HPD against DR and clarify its molecular mechanisms. HPD was chemically synthesized. Its anti-angiogenic efficacy was evaluated using both in vitro and in vivo assays. Proteomic analysis, combined with molecular docking and surface plasmon resonance (SPR), was employed to screen and validate the direct binding targets of HPD. Additionally, siRNA-mediated gene knockdown was performed to clarify the functional role of the identified target in DR pathology. In vitro and in vivo experiments demonstrated that HPD significantly inhibited pathological angiogenesis and restored retinal thickness in diabetic retinopathy (DR) model mice. Proteomics analysis, coupled with surface plasmon resonance (SPR) validation, revealed that HPD directly and exclusively bound to PARK7. Furthermore, knockdown of PARK7 exacerbated pathological angiogenesis, whereas intervention with HPD markedly reversed this phenotypic alteration. HPD directly targets PARK7 to attenuate diabetic retinopathy by suppressing pathological angiogenesis, preserving retinal structure, and maintaining blood-retinal barrier integrity.
如何引用
AMA
Yan Ma, Huihui Sun, Qingxuan Ji, Hanying Liu, Jiahui Wang, Yonggang Liu, et al. N-(4-Hydroxyphenethyl)-(4E)-decenamide derived from natural phytochemical of Anacyclus root ameliorates diabetic retinopathy by inhibiting angiogenesis via PARK7.. Journal of ethnopharmacology. 2027; doi:10.1016/j.jep.2026.122168.
APA
Yan Ma, Huihui Sun, Qingxuan Ji, Hanying Liu, Jiahui Wang, Yonggang Liu, et al (2027). N-(4-Hydroxyphenethyl)-(4E)-decenamide derived from natural phytochemical of Anacyclus root ameliorates diabetic retinopathy by inhibiting angiogenesis via PARK7.. Journal of ethnopharmacology. https://doi.org/10.1016/j.jep.2026.122168
GB/T 7714
Yan Ma, Huihui Sun, Qingxuan Ji, Hanying Liu, Jiahui Wang, Yonggang Liu, et al. N-(4-Hydroxyphenethyl)-(4E)-decenamide derived from natural phytochemical of Anacyclus root ameliorates diabetic retinopathy by inhibiting angiogenesis via PARK7.[J]. Journal of ethnopharmacology, 2027 doi:10.1016/j.jep.2026.122168.
在 PubMed增强版 阅读全文
翻译全文 · AI 文献问答 · PDF 原文下载 · 引用导出