Inhibition of human platelet aggregation by Choisyaternatine isolated from Choisya ternata (Rutaceae)

I. Wahab, N. Wong, Maria Jose Santoz-Martinez, F. Boylan
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Abstract

A newly reported alkaloid was isolated from the hexane extract of Choisya ternata Kunth. (Rutaceae) leaves, identified as 6,8-Dimethoxy-7-(3-methylbut-2-enyloxy)quinolin-2-ol (choisyaternatine) (A), together with the known compounds skimmianine (B), lup-20(29)-en-3?-ol (lupeol) (C) and tecleamaniensine A (D). Compounds C and D are reported for the first time in this species. The structures of isolated compounds were elucidated by extensive spectroscopic analyses and comparison with previously reported spectroscopic data. The structure of choisyaternatine was further confirmed based on X-ray data analysis. Anti-platelet activity of hexane extract, choisyaternatine and skimmianine was also evaluated. The extract was able to significantly inhibit collagen-induced platelet aggregation at all concentrations tested (25, 50 and 100 µg/ml). The new compound, choisyaternatine, has shown a significant inhibition of collagen-induced platelet aggregation demonstrated in a concentration dependent manner from 250 µM. The concentrations which inhibit 50% of platelet aggregation (IC50) were found to be 564 µM for skimmianine and 698 µM for choisyaternatine. This is also the first report for the antiplatelet activity for this plant and these alkaloids using human platelets.
鸢尾草水鼠碱对人血小板聚集的抑制作用
从菊苣的己烷提取液中分离得到一种新生物碱。(芸香科)叶片,鉴定为6,8-二甲氧基-7-(3-甲基-2-乙氧基)喹啉-2-醇(选择水杨酸)(A),以及已知化合物skimmianine (B), lup20 (29)-en-3?-ol (lupeol) (C)和tecleamanienine A (D).化合物C和D为首次在该种中报道。通过广泛的光谱分析和与先前报道的光谱数据的比较,阐明了分离化合物的结构。通过x射线数据分析进一步证实了选择性水杨碱的结构。并对己烷提取物、选择性水杨酸钠和脱脂蜜氨酸的抗血小板活性进行了评价。在所有测试浓度(25、50和100µg/ml)下,提取物都能显著抑制胶原诱导的血小板聚集。新化合物选择性水杨酸钠(choisyaternatine)对胶原诱导的血小板聚集具有明显的抑制作用,从250µM开始呈浓度依赖性。对50%的血小板聚集有抑制作用的浓度分别为564µM和698µM。这也是该植物及其生物碱利用人血小板抗血小板活性的首次报道。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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