Laboratory of Inorganic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15771 Athens, Greece.
Department of Environmental Engineering, School of Engineering, University of Patras, 26504 Patras, Greece.
Molecules. 2023 Feb 16;28(4):1859. doi: 10.3390/molecules28041859.
Metal complexes displaying antiplatelet properties is a promising research area. In our methodology, Platelet-Activating Factor (PAF), the most potent lipid pro-inflammatory mediator, serves as a biological probe. The antiplatelet activity is exerted by the inhibition of the PAF-induced aggregation in washed rabbit platelets (WRPs) and in rabbit plasma rich in platelets (rPRPs). Herein, the synthesis and biological investigation of a series of organometallic tin(II) and tin(IV) complexes, featuring the oxygen tripodal Kläui ligands [(-CR)Co{P(OEt)O}], {R = H, (L); Me (L*)}, are reported. Reaction of NaL () and NaL* () with SnCl, yielded the rare four-coordinate LSnCl () and LSnCl () complexes. Accordingly, LSnPh () and LSnPh () were prepared, starting from PhSnCl. Characterization includes spectroscopy and X-ray diffraction studies for , and . The antiplatelet activity of the lead complexes and (IC = 0.5 μΜ) is superior compared to that of and , while both complexes display a pronounced inhibitory activity against thrombin (IC = 1.8 μM and 0.6 μM). The in vitro cytotoxic activities of and on human Jurkat T lymphoblastic tumor cell line is higher than that of cisplatin.
具有抗血小板特性的金属配合物是一个很有前途的研究领域。在我们的方法中，血小板激活因子（PAF），作为一种最有效的脂质促炎介质，作为生物探针。抗血小板活性是通过抑制血小板激活因子诱导的洗涤兔血小板（WRP）和富含血小板的兔血浆（rPRP）聚集来发挥的。本文报道了一系列具有氧三角架 Kläui 配体[（-CR）Co{P（OEt）O}]的有机锡（II）和锡（IV）配合物的合成和生物学研究，{R = H，（L）；Me（L*）}。NaL（）和 NaL*（）与 SnCl 的反应生成了罕见的四配位 LSnCl（）和 LSnCl（）配合物。相应地，从 PhSnCl 开始制备了 LSnPh（）和 LSnPh（）。表征包括光谱和 X 射线衍射研究。对于 、 和 ，铅配合物 和 （IC = 0.5 μΜ）的抗血小板活性优于 和 ，而这两种配合物对凝血酶均显示出明显的抑制活性（IC = 1.8 μM 和 0.6 μM）。对人 Jurkat T 淋巴母细胞瘤细胞系的 和 的体外细胞毒性活性高于顺铂。
