含有内氧化物,通过向NOS2从Daedaleopsis confragosa衍生而来的类固醇的铁质中介抗癌活性
Eun Jin Heo1,2, Yeojin Kim3, Jae Woong Chang3
1Department of Convergent Biotechnology and Advanced Materials Science, College of Life Sciences, Kyung Hee University, 17104, Yongin, Republic of Korea.
Animal cells and systems
|December 8, 2025
概括
来自Daedaleopsis confragosa的类固醇,特别是具有内氧化物桥梁的类固醇,通过向可诱导氧化合成酶 (NOS2) 诱导铁亡,表现出强烈的抗癌活性. 这些化合物是有希望的抗癌药物候选者.
科学领域:
- 自然产品化学 自然产品化学
- 药用化学 医学化学
- 癌症生物学 癌症生物学
背景情况:
- 属Daedaleopsis的含有生物活性化合物,包括类固醇.
- 果 (Daedaleopsis confragosa) 的化学成分尚未得到广泛研究.
- 类固醇是一种具有多种生物活性的化合物.
研究的目的:
- 为了化学分析Daedaleopsis confragosa果实体的甲醇提取物.
- 识别和评估类固醇化合物的细胞毒性作用.
- 调查分子作用机制,包括目标预测和铁灭诱导.
主要方法:
- 甲醇提取和化学分析的Daedaleopsis confragosa. 的.
- 对人类癌细胞系进行细胞毒性测定 (HCT116,A549,MDA-MB-231,A375SM).
- 计算目标预测,与可诱导的氧化合成酶 (NOS2) 进行分子对接,并分析铁灭菌标记表达.
主要成果:
- 确定了七种类固醇化合物;化合物1,2,3和5表现出强烈的细胞毒性.
- 诱导性氧化合成酶 (NOS2) 被预测为分子标.
- 化合物2及其副产品2 - 1对NOS2具有很高的结合亲和力.
- 化合物1,2,3和5剂量依赖地增加了铁亡标志物 (PTGS2,SLC7A11,CHAC1,HMOX1).
- 这种NOS2倒置模仿了这些化合物诱导铁亡的作用.
结论:
- 来自D.confragosa的含有内氧化物类固醇是铁亡的强有力的诱导剂.
- 该机制涉及向可诱导的氧化合成酶 (NOS2).
- 这些真菌类固醇显示出作为新型抗癌药物候选者的潜力.
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