Periplanetols A-F, phenolic compounds from Periplaneta americana with potent COX-2 inhibitory activity
Periplanetols A-F, phenolic compounds from Periplaneta americana with potent COX-2 inhibitory activity
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Periplanetols A–F，来自美洲大蠊的酚类化合物，具有有效的 COX-2 抑制活性
DOI：
10.1016/j.fitote.2020.104589
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发表时间：
2020-06-01
期刊：
影响因子：
3.4
通讯作者：
Cheng, Yong-Xian
中科院分区：
文献类型：
--
作者：
Bai, Hong-Fu;Li, Yan-Peng;Cheng, Yong-Xian
从美洲大蠊（Periplaneta americana）全体的70%乙醇提取物中分离出6种新化合物，即大蠊醇A - F（1 - 4、6和7），一种首次从天然来源分离得到的化合物（5）以及9种已知化合物（8 - 16）。通过综合光谱分析和计算方法明确鉴定了它们的结构，包括绝对构型。对环氧化酶 - 2（COX - 2）抑制的生物学评估显示，化合物1、2和10能够抑制COX - 2活性，其半数抑制浓度（IC50）值分别为768.0 nM、617.7 nM和599.5 nM，表明它们在开发治疗炎症相关疾病的新型药物方面具有潜力。
Six new compounds, periplanetols A - F (1 - 4, 6 and 7), a compound isolated from natural origin for the first time (5), and nine known ones (8 - 16) were isolated from the 70% ethanol extract of the whole bodies of Periplaneta americana. Their structures including absolute configurations were unambiguously identified by comprehensive spectroscopic analyses and computational methods. Biological evaluation toward COX-2 inhibition revealed that compounds 1, 2, and 10 could inhibit COX-2 activity with the IC50 values of 768.0 nM, 617.7 nM, and 599.5 nM respectively, indicating their potential in developping novel agents against inflammation related disorders.