梅洛西德A通过受体受体调节保护皮肤乳头细胞免受DHT诱导的损伤
Hyun Jun Park1, Bong Geun Song1, Ji Hoon Song1
1R&D Center, Morechem. Co., Ltd., Yongin 16954, Gyeonggi-do, Republic of Korea.
Current issues in molecular biology
|July 23, 2025
概括
Cucumis melo叶提取物 (CLE) 和其化合物Meloside A通过抑制皮肤乳头细胞中二激素 (DHT) 诱导的亡来减少脱发. 梅洛西德A调节雄激素受体 (AR) 活性并减少炎症,为新的脱发疗法提供了潜力.
科学领域:
- 皮肤病学 皮肤病学
- 药理学 药理学 是一个学科.
- 自然产品 化学 化学
背景情况:
- 质性脱毛症 (AGA) 涉及二 (DHT) 诱导人类皮肤乳头细胞 (HDPCs) 通过受体 (AR) 上调调节的亡.
- 目前对AGA的治疗有局限性,需要探索新的治疗药物.
研究的目的:
- 为了研究Cucumis melo* var.的潜力. *makuwa* 叶子提取物 (CLE) 用于抵消HDPC中DHT介导的作用.
- 确定CLE中关键的生物活性化合物,负责这些影响,并阐明它们的作用机制.
主要方法:
- HDPCs接受了CLE和DHT的治疗,以评估细胞亡和AR表达.
- 高性能液体染色学与喷射电离子双重质谱学 (HPLC-ESI-MS) 结合使用用于化合物识别.
- 评估了梅洛A对AR核转位,蛋白质表达,下游基因表达 (IL-6,TGF-β1,DKK-1) 和活性氧物种 (ROS) 生成的影响.
主要成果:
- 在HDPC中,CLE显著降低了DHT诱导的亡,在1000ppm时降低了57.74%.
- 鉴定为主要活性化合物的酸A抑制了DHT刺激的AR核转位,并降低了AR蛋白水平.
- 梅洛西德A降低了IL-6,TGF-β1和DKK-1基因表达,分别降低了16.27%,26.55%和35.38%在100ppm时.
- 在DHT刺激的HDPC中,Melosid A显著抑制了ROS生成,在100ppm时将ROS生成抑制了45.45%.
结论:
- 来自CLE的梅洛西德A显示出显著的抗雄激素脱发效应.
- 该机制涉及调节AR核转位,减少AR表达,抑制炎症基因表达和ROS产生.
- 化物A作为AGA的治疗剂显示出希望,为新的脱发治疗铺平了道路.
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