title: Bioactive Benzofuran Derivatives from Cortex Mori Radicis, and Their Neuroprotective and Analgesic Activities Mediated by mGluR₁.
abstract: Four new benzofuran-type stilbene glycosides and 14 known compounds including 8 benzofuran-type stilbenes and 6 flavonoids were isolated from the traditional Chinese medicine, Cortex Mori Radicis. The new compounds were identified as (9R)-moracin P 3'-O-α-l-arabinopyranoside (1), (9R)-moracin P 9-O-β-d-glucopyranoside (2), (9R)-moracin P 3'-O-β-d-glucopyranoside (3), and (9R)-moracin O 10-O-β-d-glucopyranoside (4) based on the spectroscopic interpretation and chemical analysis. Three benzofuran-type stilbenes, moracin O (5), R (7), and P (8) showed significant neuroprotective activity against glutamate-induced cell death in SK-N-SH cells. In addition, moracin O (5) and P (8) also demonstrated a remarkable inhibition of the acetic acid-induced pain. The molecular docking with metabotropic glutamate receptor 1 (mGluR₁) results indicated that these neuroprotective benzofuran-type stilbenes might be the active analgesic components of the genusMorus, and acted by mediating the mGluR₁ pathway.
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. wangyanan@imm.ac.cn.
authors.forename: Ya-Nan
authors.initials: YN
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. 13241468601@163.com.
authors.forename: Mao-Feng
authors.initials: MF
authors.lastname: Liu
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. houweizhen@imm.ac.cn.
authors.forename: Wei-Zhen
authors.initials: WZ
authors.lastname: Hou
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. rmxu@imm.ac.cn.
authors.forename: Rui-Ming
authors.initials: RM
authors.lastname: Xu
authors.affiliation: GRU Cancer Center, Augusta University, Augusta, GA 30912, USA. jgao@augusta.edu.
authors.forename: Jie
authors.initials: J
authors.lastname: Gao
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. angellu@imm.ac.cn.
authors.forename: An-Qi
authors.initials: AQ
authors.lastname: Lu
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. xiemeiping2016@sina.com.
authors.forename: Mei-Ping
authors.initials: MP
authors.lastname: Xie
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. lilan@imm.ac.cn.
authors.forename: Lan
authors.initials: L
authors.lastname: Li
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. jjzhang@imm.ac.cn.
authors.forename: Jian-Jun
authors.initials: JJ
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. ypeng@imm.ac.cn.
authors.forename: Ying
authors.initials: Y
authors.lastname: Peng
authors.affiliation: Editorial Department, Shenyang Pharmaceutical University, Shenyang 110016, China. malili022406@sina.com.
authors.forename: Li-Li
authors.initials: LL
authors.lastname: Ma
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. wangxl@imm.ac.cn.
authors.forename: Xiao-Liang
authors.initials: XL
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. shijg@imm.ac.cn.
authors.forename: Jian-Gong
authors.initials: JG
authors.lastname: Shi
authors.affiliation: State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. sujuanwang@imm.ac.cn.
authors.forename: Su-Juan
authors.initials: SJ
authors.lastname: Wang
mesh_terms: D000700:Analgesics / Q000737:chemistry* / Q000494:pharmacology*; D001572:Benzofurans / Q000737:chemistry* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D002942:Circular Dichroism; D004365:Drugs, Chinese Herbal / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D062105:Molecular Docking Simulation; D056004:Molecular Dynamics Simulation; D015394:Molecular Structure; D031625:Morus / Q000737:chemistry; D018696:Neuroprotective Agents / Q000737:chemistry* / Q000494:pharmacology*; D064209:Phytochemicals / Q000737:chemistry; D018094:Receptors, Metabotropic Glutamate / Q000737:chemistry / Q000378:metabolism*
chemical_list: D000700:Analgesics; D001572:Benzofurans; D004365:Drugs, Chinese Herbal; D018696:Neuroprotective Agents; D064209:Phytochemicals; D018094:Receptors, Metabotropic Glutamate; C104077:metabotropic glutamate receptor type 1
keywords: Cortex Mori Radicis; analgesia; benzofuran-type stilbenes; neuroprotection