COX
Cyclooxygenase (COX) is an enzyme (specifically, a family of isozymes) that is responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin. Pharmaceutical inhibition of COX can provide relief from the symptoms of inflammation and pain. Nonsteroidal anti-inflammatory drugs (NSAIDs), such as aspirin and ibuprofen, exert their effects through inhibition of COX. The two isozymes found in human are called COX-1 and COX-2 in the medical literature.
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Phenacetin是非阿片类镇痛化合物,具有抗炎活性。
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Lumiracoxib是一种新型,选择性的COX-2抑制剂,IC50和Ki分别为0.14 μM和0.06 μM,比作用于COX-1选择性高515倍。
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Naproxen sodium是COX抑制剂,对COX-1和COX-2的IC50分别为8.7 μM和5.2 μM。
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Xanthohumol,来自啤酒花的一种异戊烯化查耳酮,抑制COX-1和COX-2活性,并表现出化学预防作用。
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Parthenolide(PTL)能诱导癌细胞凋亡,并杀灭癌症干细胞,还能特异地抑制HDAC1活性而不影响别的I/II类HDAC。
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