Jing Yu, Zhang Yi-Fan, Shang Ming-Ying, Liu Guang-Xue, Li Yao-Li, Wang Xuan, Cai Shao-Qing
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.
Molecules. 2017 Jan 13;22(1):125. doi: 10.3390/molecules22010125.
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.
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。