Shih Hung-Cheng, Chern Ching-Yuh, Kuo Ping-Chung, Wu You-Cheng, Chan Yu-Yi, Liao Yu-Ren, Teng Che-Ming, Wu Tian-Shung
Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan.
Department of Applied Chemistry, National Chiayi University, Chiayi 600, Taiwan.
Int J Mol Sci. 2014 Mar 4;15(3):3926-51. doi: 10.3390/ijms15033926.
The present study was aimed at discovering novel biologically active compounds based on the skeletons of gingerol and shogaol, the pungent principles from the rhizomes of Zingiber officinale. Therefore, eight groups of analogues were synthesized and examined for their inhibitory activities of platelet aggregation induced by arachidonic acid, collagen, platelet activating factor, and thrombin. Among the tested compounds, [6]-paradol (5b) exhibited the most significant anti-platelet aggregation activity. It was the most potent candidate, which could be used in further investigation to explore new drug leads.
本研究旨在基于姜辣素和姜烯酚的骨架发现新型生物活性化合物，姜辣素和姜烯酚是姜科植物姜根茎中的辛辣成分。因此，合成了八组类似物，并检测了它们对花生四烯酸、胶原蛋白、血小板活化因子和凝血酶诱导的血小板聚集的抑制活性。在测试的化合物中，[6]-对甲酚（5b）表现出最显著的抗血小板聚集活性。它是最有潜力的候选物，可用于进一步研究以探索新的药物先导物。
