Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy.
Eur J Med Chem. 2011 Feb;46(2):488-96. doi: 10.1016/j.ejmech.2010.11.028. Epub 2010 Nov 24.
As a part of our drug discovery efforts we developed a series of simplified derivatives of bolinaquinone (BLQ), a hydroxyquinone marine metabolite, showing potent anti-inflammatory activity. Thirteen new hydroxyquinone derivatives closely related to BLQ were synthesized and tested on mouse macrophage-like RAW 264.7 cell line in order to investigate their ability to modulate the production of Prostaglandin E2 (PGE2). This optimization process led to the identification of three strictly correlated compounds with comparable and higher inhibitory potency than BLQ on PGE2 production. To evaluate the affinity of BLQ and its analogues for hsPLA2, surface plasmon resonance (SPR) experiments were performed.
在我们的药物发现工作中，我们开发了一系列 bolinaquinone（BLQ）的简化衍生物，BLQ 是一种羟基醌海洋代谢物，具有很强的抗炎活性。为了研究它们调节前列腺素 E2（PGE2）产生的能力，我们合成了 13 种与 BLQ 密切相关的新羟基醌衍生物，并在小鼠巨噬细胞样 RAW 264.7 细胞系上进行了测试。这一优化过程确定了三种具有可比性和更高抑制效力的严格相关化合物，其对 PGE2 的产生比 BLQ 更强。为了评估 BLQ 及其类似物与 hsPLA2 的亲和力，进行了表面等离子体共振（SPR）实验。
