Hao-Dong Yang , Yuan-Gui Yang , Zhi-Shu Tang , Kang Ma , Hong-Bo Xu
{"title":"从 Acanthopanacis 皮质提取物中鉴定木酚素作为选择性环氧化酶-2 抑制剂。","authors":"Hao-Dong Yang , Yuan-Gui Yang , Zhi-Shu Tang , Kang Ma , Hong-Bo Xu","doi":"10.1016/j.phytochem.2024.114208","DOIUrl":null,"url":null,"abstract":"<div><p><em>Acanthopanacis</em> cortex (the dried root bark of <em>Acanthopanax gracilistylus</em> W. W. Smith) has been used for the treatment of rheumatic diseases in China for over 2000 years. Four previously undescribed lignans (<strong>1</strong>–<strong>4</strong>) and 12 known lignans (<strong>5</strong>–<strong>16</strong>) were isolated from <em>Acanthopanacis</em> cortex. In this study, the inhibitory activities of compounds <strong>1</strong>–<strong>16</strong> against neutrophil elastase (NE), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) are reported. The results show that compounds <strong>1</strong>–<strong>16</strong> exhibit weak inhibitory activities against NE and COX-1. However, compounds <strong>2</strong>, <strong>6</strong>–<strong>8</strong> and <strong>13</strong>–<strong>16</strong> demonstrate better COX-2 inhibitory effects with IC<sub>50</sub> values from 0.75 to 8.17 <em>μ</em>Μ. These findings provide useful information for the search for natural selective COX-2 inhibitors.</p></div>","PeriodicalId":20170,"journal":{"name":"Phytochemistry","volume":null,"pages":null},"PeriodicalIF":3.2000,"publicationDate":"2024-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Identification of lignans as selective cyclooxygenase-2 inhibitors from the extract of Acanthopanacis cortex\",\"authors\":\"Hao-Dong Yang , Yuan-Gui Yang , Zhi-Shu Tang , Kang Ma , Hong-Bo Xu\",\"doi\":\"10.1016/j.phytochem.2024.114208\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p><em>Acanthopanacis</em> cortex (the dried root bark of <em>Acanthopanax gracilistylus</em> W. W. Smith) has been used for the treatment of rheumatic diseases in China for over 2000 years. Four previously undescribed lignans (<strong>1</strong>–<strong>4</strong>) and 12 known lignans (<strong>5</strong>–<strong>16</strong>) were isolated from <em>Acanthopanacis</em> cortex. In this study, the inhibitory activities of compounds <strong>1</strong>–<strong>16</strong> against neutrophil elastase (NE), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) are reported. The results show that compounds <strong>1</strong>–<strong>16</strong> exhibit weak inhibitory activities against NE and COX-1. However, compounds <strong>2</strong>, <strong>6</strong>–<strong>8</strong> and <strong>13</strong>–<strong>16</strong> demonstrate better COX-2 inhibitory effects with IC<sub>50</sub> values from 0.75 to 8.17 <em>μ</em>Μ. These findings provide useful information for the search for natural selective COX-2 inhibitors.</p></div>\",\"PeriodicalId\":20170,\"journal\":{\"name\":\"Phytochemistry\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":3.2000,\"publicationDate\":\"2024-07-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Phytochemistry\",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0031942224002450\",\"RegionNum\":2,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Phytochemistry","FirstCategoryId":"99","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0031942224002450","RegionNum":2,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
摘要
Acanthopanacis cortex(Acanthopanax gracilistylus W. W. Smith 的干燥根皮)在中国用于治疗风湿病已有 2000 多年的历史。从刺五加皮中分离出了 4 种以前未曾描述过的木脂素(1-4)和 12 种已知的木脂素(5-16)。本研究报告了 1-16 号化合物对中性粒细胞弹性蛋白酶(NE)、环氧化酶-1(COX-1)和环氧化酶-2(COX-2)的抑制活性。结果表明,化合物 1-16 对 NE 和 COX-1 具有微弱的抑制活性。然而,化合物 2、6∼8 和 13∼16 对 COX-2 具有较好的抑制作用,其 IC50 值在 0.75 至 8.17 μΜ 之间。这些发现为寻找天然选择性 COX-2 抑制剂提供了有用的信息。
Identification of lignans as selective cyclooxygenase-2 inhibitors from the extract of Acanthopanacis cortex
Acanthopanacis cortex (the dried root bark of Acanthopanax gracilistylus W. W. Smith) has been used for the treatment of rheumatic diseases in China for over 2000 years. Four previously undescribed lignans (1–4) and 12 known lignans (5–16) were isolated from Acanthopanacis cortex. In this study, the inhibitory activities of compounds 1–16 against neutrophil elastase (NE), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) are reported. The results show that compounds 1–16 exhibit weak inhibitory activities against NE and COX-1. However, compounds 2, 6–8 and 13–16 demonstrate better COX-2 inhibitory effects with IC50 values from 0.75 to 8.17 μΜ. These findings provide useful information for the search for natural selective COX-2 inhibitors.
期刊介绍:
Phytochemistry is a leading international journal publishing studies of plant chemistry, biochemistry, molecular biology and genetics, structure and bioactivities of phytochemicals, including ''-omics'' and bioinformatics/computational biology approaches. Phytochemistry is a primary source for papers dealing with phytochemicals, especially reports concerning their biosynthesis, regulation, and biological properties both in planta and as bioactive principles. Articles are published online as soon as possible as Articles-in-Press and in 12 volumes per year. Occasional topic-focussed special issues are published composed of papers from invited authors.