title: Chemical Constituents from the Roots and Rhizomes of Asarum heterotropoides var. mandshuricum and the In Vitro Anti-Inflammatory Activity.
abstract: Anti-inflammatory compounds were investigated from the ethanol extract of the roots and rhizomes ofAsarum heterotropoidesvar.mandshuricum, a traditional Chinese medicine called Xixin and used for pain and inflammatory. Nine new compounds were isolated, including six new lignans, neoasarinin A-C (1-3), neoasarininoside A and B (4and5), and asarinin B (7), and one new monoterpene, asarincin A (8), two new amides, asaramid II and III (10and11), and one new natural monoterpene, asaricin B (9), along with 37 known compounds (6,12-47). 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 (6). The 8-O-4' neolignans (1-5) were reported in the genusAsarumfor the first time. The 15 compounds17,19,22-25,28,31,36,40,42,43,45-47were isolated from the genusAsarum, and compounds16,32,33,37and39were isolated fromA. heterotropoidesvar.mandshuricumfor 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 compounds1,4,7,8,14,17-19,22,24,25,29,30,32,33,40-43,45, and46showed potent anti-inflammatory activities in vitro, with 27.9%-72.6% inhibitions at 10-5mol/L. The results of anti-inflammatory assay suggested that lignans obtained from the CHCl₃ extract might be the main active components of Xixin.
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Beijing 100191, China. jing_jy@126.com.|Tonghua Gold-Horse Pharmaceutical Group Co., Ltd., Beijing 100025, China. jing_jy@126.com.
authors.forename: Yu
authors.initials: Y
authors.lastname: Jing
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Beijing 100191, China. zhangyifan@bjmu.edu.cn.
authors.forename: Yi-Fan
authors.initials: YF
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Beijing 100191, China. myshang@bjmu.edu.cn.
authors.forename: Ming-Ying
authors.initials: MY
authors.lastname: Shang
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Beijing 100191, China. guangxl@bjmu.edu.cn.
authors.forename: Guang-Xue
authors.initials: GX
authors.lastname: Liu
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Beijing 100191, China. 13466759800@163.com.
authors.forename: Yao-Li
authors.initials: YL
authors.lastname: Li
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Beijing 100191, China. xuanwang6818@bjmu.edu.cn.
authors.forename: Xuan
authors.initials: X
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, No. 38, Xueyuan Road, Beijing 100191, China. sqcai@bjmu.edu.cn.
authors.forename: Shao-Qing
authors.initials: SQ
authors.lastname: Cai
mesh_terms: D043203:1-Alkyl-2-acetylglycerophosphocholine Esterase / Q000037:antagonists & inhibitors / Q000494:pharmacology; D000577:Amides / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D030023:Asarum / Q000737:chemistry*; D002725:Chloroform; D004365:Drugs, Chinese Herbal / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D000431:Ethanol; D005966:Glucuronidase / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D017705:Lignans / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D015394:Molecular Structure; D039821:Monoterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D009504:Neutrophils / Q000166:cytology / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry; D018517:Plant Roots / Q000737:chemistry; D061251:Primary Cell Culture; D051381:Rats; D027343:Rhizome / Q000737:chemistry; D012997:Solvents / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000893:Anti-Inflammatory Agents; D004365:Drugs, Chinese Herbal; D017705:Lignans; D039821:Monoterpenes; D010936:Plant Extracts; D012997:Solvents; D000431:Ethanol; D002725:Chloroform; D043203:1-Alkyl-2-acetylglycerophosphocholine Esterase; D005966:Glucuronidase
keywords: 8-O-4′ neolignan; Aristolochiaceae; Asarum heterotropoides var. mandshuricum; amide; anti-inflammatory; lignans; monoterpene