Inhibitors of secreted phospholipase A2 suppress the release of PGE2 in renal mesangial cells

被引：10
作者：
Vasilakaki, Sofia [1 ]
Barbayianni, Efrosini [1 ]
Magrioti, Victoria [1 ]
Pastukhov, Oleksandr [2 ]
Constantinou-Kokotou, Violetta [3 ]
Huwiler, Andrea [2 ]
Kokotos, George [1 ]
机构：
[1] Univ Athens, Dept Chem, Organ Chem Lab, Athens 15771, Greece
[2] Univ Bern, Inst Pharmacol, CH-3010 Bern, Switzerland
[3] Agr Univ Athens, Chem Labs, GR-11855 Athens, Greece
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2016年 / 24卷 / 13期
关键词：
Inhibitors; Mesangial cells; Phospholipase A(2); Prostaglandin E-2; Secreted phospholipase A(2); GROUP IVA; EMERGING ROLES; CROSS-TALK; DISEASE; ENZYMES; SERIES; INFLAMMATION; SPLA(2); IIA;
D O I：
10.1016/j.bmc.2016.05.017
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The upregulation of PGE(2) by mesangial cells has been observed under chronic inflammation condition. In the present work, renal mesangial cells were stimulated to trigger a huge increase of PGE(2) synthesis and were treated in the absence or presence of known PLA(2) inhibitors. A variety of synthetic inhibitors, mainly developed in our labs, which are known to selectively inhibit each of GIVA cPLA(2), GVIA iPLA(2), and GIIA/GV sPLA(2), were used as tools in this study. Synthetic sPLA(2) inhibitors, such as GK115 (an amide derivative based on the non-natural amino acid (R)-gamma-norleucine) as well as GK126 and GK241 (2-oxoamides based on the natural (S)-alpha-amino acid leucine and valine, respectively) presented an interesting effect on the suppression of PGE(2) formation. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3029 / 3034
页数：6
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