生物活性 | |||
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描述 | Apocynin is a most widely studied pan-NADPH-oxidase inhibitor and a scavenger of hydrogen peroxide, as well as inhibits rho kinases. Apocynin could eliminate hydrogen peroxid in a dose-dependent manner at concentration ranging in 3-100μM. Intraperitoneal injection with Apocynin at dose of 5mg/kg reduced lung injury and blocked NADPH oxidase activation in lung tissues by carrageenan in mice. The administration of Apocynin significantly reduced ICAM-1, P-selectin induced by carrageenan and attenuated neutrophil infiltration into the lung tissue. Also Apocynin attenuated carrageenan-induced TNF-α and IL-1β, iNOS expression, Fas ligand, apoptosis and Bax expression, as well as prevented carrageenan-induced inhibition of Bcl-2 expression and activation of NF-κB pathway and MAPK pathway at 4h post carrageenan injection. Some study showed that Apocynin may work as an antioxidant more than a NADPH oxidase inhibitor for apocynin failed to inhibit superoxide anion generation in HEK293 cells overexpressing NADPH oxidase isoforms (Nox1, Nox2, or Nox4). | ||
作用机制 | Apocynin is an oxidase assembly inhibitor which can inhibit association of p47phox with membrane-bound heterodimer.[5] |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03376555 | Microvascular Dysfunction | Phase 1 Phase 2 | Recruiting | June 30, 2019 | United States, Pennsylvania ... 展开 >> Pennsylvania State University Recruiting University Park, Pennsylvania, United States, 16802 收起 << |
NCT03680573 | Cardiovascular Diseases ... 展开 >> Cardiovascular Risk Factor Vasoconstriction 收起 << | Phase 1 | Completed | - | United States, Texas ... 展开 >> Engineering Research Building Arlington, Texas, United States, 76019 收起 << |
NCT03680638 | Cardiovascular Diseases ... 展开 >> Cardiovascular Risk Factor Vasodilation 收起 << | Phase 1 | Completed | - | United States, Texas ... 展开 >> Engineering Research Building Arlington, Texas, United States, 76019 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
6.02mL 1.20mL 0.60mL |
30.09mL 6.02mL 3.01mL |
60.18mL 12.04mL 6.02mL |
参考文献 |
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