Effects of Novel Diarylpentanoid Analogues of Curcumin on Secretory Phospholipase A<sub>2</sub>, Cyclooxygenases, Lipo-oxygenase, and Microsomal Prostaglandin E Synthase-1
作者:Waqas Ahmad、Endang Kumolosasi、Ibrahim Jantan、Syed N. A. Bukhari、Malina Jasamai
DOI:10.1111/cbdd.12280
日期:2014.6
diarylpentanoid curcumin analogues 5, 6, 7, and 13 demonstrated higher inhibition of microsomal prostaglandin E synthase‐1 activity with IC50 ranging from 2.41 to 4.48 μm, which was less than that of curcumin. The present results suggest that some of these diarylpentanoid analogues were able to inhibit the activity of these enzymes. This raises the possibility that diarylpentanoid analogues of curcumin might
花生四烯酸及其代谢物由于其在炎症中的重要作用而引起了人们的关注。抑制花生四烯酸代谢中涉及的酶被认为是协同的抗炎作用。合成了一系列新型姜黄素二芳基戊烷类似物,并评估了它们对分泌性磷脂酶A 2,环加氧酶,大豆脂加氧酶以及微粒体前列腺素E合酶-1的抑制作用。之间的姜黄素类似物,化合物3,6,9,12,和17显示出分泌的磷脂酶A的强抑制2活性,以IC 50值范围从5.89到11.02 μ米。七姜黄素类似物1,3,6,7,9,11,和12环氧合酶-2的抑制表现出与IC 50值在46.11至94.86 μ米,这明显高于姜黄素的低。化合物3,6,7,12,和17对脂氧合酶的活性有很强的抑制作用。diarylpentanoid姜黄素类似物对微粒体前列腺素E合酶-1活性的初步筛选表明,4个diarylpentanoid姜黄素类似物5,6,7,和13表现出较高的抑制微粒体前列腺素E合酶-1活性的带IC 50范围从2