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辽细辛根及根茎的化学成分与体外抗炎活性

Chemical Constituents from the Roots and Rhizomes of Asarum heterotropoides var. mandshuricum and the In Vitro Anti-Inflammatory Activity.

作者信息

Jing Yu, Zhang Yi-Fan, Shang Ming-Ying, Liu Guang-Xue, Li Yao-Li, Wang Xuan, Cai Shao-Qing

机构信息

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Beijing 100191, China.

Tonghua Gold-Horse Pharmaceutical Group Co., Ltd., Beijing 100025, China.

出版信息

Molecules. 2017 Jan 13;22(1):125. doi: 10.3390/molecules22010125.

DOI:10.3390/molecules22010125
PMID:28098805
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6155747/
Abstract

Anti-inflammatory compounds were investigated from the ethanol extract of the roots and rhizomes of var. , a traditional Chinese medicine called Xixin and used for pain and inflammatory. Nine new compounds were isolated, including six new lignans, neoasarinin A-C (-), neoasarininoside A and B ( and ), and asarinin B (), and one new monoterpene, asarincin A (), two new amides, asaramid II and III ( and ), and one new natural monoterpene, asaricin B (), along with 37 known compounds (, -). Their structures and absolute configurations were elucidated on the basis of spectroscopic methods and chemical analyses. This is the first report of the absolute configuration of asarinin A (). The 8--4' neolignans (-) were reported in the genus for the first time. The 15 compounds , , -, , , , , , , - were isolated from the genus , and compounds , , , and were isolated from var. for the first time. Thirty-seven of the isolates were evaluated for anti-inflammatory activity against the release of β-glucuronidase in polymorphonuclear leukocytes (PMNs) induced by the platelet-activating factor (PAF), and compounds , , , , , -, , , , , , , , -, , and showed potent anti-inflammatory activities in vitro, with 27.9%-72.6% inhibitions at 10 mol/L. The results of anti-inflammatory assay suggested that lignans obtained from the CHCl₃ extract might be the main active components of Xixin.

摘要

从中药细辛(一种传统用于止痛和抗炎的中药材)的根及根茎的乙醇提取物中研究抗炎化合物。分离得到了9个新化合物,包括6个新木脂素,新细辛脂素A - C(-)、新细辛脂苷A和B( 和 )以及细辛脂素B(),1个新单萜,细辛新素A(),2个新酰胺,细辛酰胺II和III( 和 ),1个新天然单萜,细辛新素B(),以及37个已知化合物(, -)。基于光谱方法和化学分析阐明了它们的结构和绝对构型。这是细辛脂素A()绝对构型的首次报道。8 - 4'新木脂素(-)首次在该属中被报道。15个化合物 , , -, , , , , , , , - 从该属中分离得到,化合物 , , , 和 首次从细辛变种中分离得到。对37个分离物针对血小板活化因子(PAF)诱导的多形核白细胞(PMN)中β - 葡萄糖醛酸酶释放的抗炎活性进行了评估,化合物 , , , , , -, , , , , , , , -, , 和 在体外显示出强效抗炎活性,在10 μmol/L时抑制率为27.9% - 72.6%。抗炎试验结果表明,从CHCl₃提取物中获得的木脂素可能是细辛的主要活性成分。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/39ee6a297d8c/molecules-22-00125-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/4785a9c20af2/molecules-22-00125-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/c7289eba318b/molecules-22-00125-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/8c3aa9c1c51e/molecules-22-00125-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/df30e2259b1f/molecules-22-00125-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/f54385841267/molecules-22-00125-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/9c580dc83354/molecules-22-00125-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/39ee6a297d8c/molecules-22-00125-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/4785a9c20af2/molecules-22-00125-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/c7289eba318b/molecules-22-00125-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/8c3aa9c1c51e/molecules-22-00125-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/df30e2259b1f/molecules-22-00125-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/f54385841267/molecules-22-00125-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/9c580dc83354/molecules-22-00125-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3f/6155747/39ee6a297d8c/molecules-22-00125-g007.jpg

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