通过天然的异硫酸酸盐抑制可溶性环氧化酶
Fawzy Elbarbry1, Michael J Espiritu1, Kaylen Soo1
1School of Pharmacy, Pacific University, 222 SE 8th Ave, Ste. 451, Hillsboro, OR, 97123, USA.
Biochemical and biophysical research communications
|June 19, 2024
概括
六种天然异硫酸盐 (ITC) 被评估为可溶性环氧化酶 (sEH) 抑制剂. 硫福拉和异酸显示出强大的SEH抑制作用,对其他酶具有选择性.
科学领域:
- 药理学 药理学是指药理学的学科.
- 生物化学 生化学
- 药用化学 医学化学
背景情况:
- 溶性环氧化酶 (sEH) 是开发治疗药物的关键目标.
- 自然化合物为新药候选人提供了一个有希望的来源.
- 异硫酸酸盐 (ITC) 是一种具有潜在生物活性的自然化合物.
研究的目的:
- 评估六种天然异硫酸盐 (ITC) 作为可溶性环氧化酶 (sEH) 抑制剂的效力和选择性.
- 研究ITC作为安全有效的sEH抑制剂的潜力,用于治疗开发.
主要方法:
- 分子对接被用来预测配体-受体相互作用.
- 在体外对sEH的抑制活性通过基于光的测试来确定.
- 使用LC-MS/MS和HPLC-UV测定,对微体环氧化酶 (mEH) 和人肝细胞染色体P450 (CYP) 酶进行选择性评估.
主要成果:
- 分子对接表明ITC与sEH催化残留的特定结合相互作用.
- 硫黄 (SFN) 和异硫酸 (PITC) 呈现出最高的强度,IC50值分别为3.65微米和7.5微米.
- 没有观察到mEH的显著抑制,并且埃鲁辛和伊贝林对测试的CYP酶没有抑制,表明具有良好的选择性.
结论:
- 自然的ITC显示出作为sEH的强大和选择性抑制剂的潜力.
- 这些发现支持自然ITCs作为针对sEH的安全治疗剂的发展.
- 对ITC的进一步研究可能会导致通过sEH活动调节的各种疾病的新疗法.
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