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 genus Morus, and acted by mediating the mGluR₁ pathway.

• Authors: Ya-Nan Wang, Mao-Feng Liu, Wei-Zhen Hou, Rui-Ming Xu, Jie Gao, An-Qi Lu, Mei-Ping Xie, Lan Li, Jian-Jun Zhang, Ying Peng, Li-Li Ma, Xiao-Liang Wang, Jian-Gong Shi, Su-Juan Wang
• Journal: Molecules (Basel, Switzerland) (Molecules) Vol. 22 Issue 2 (Feb 08 2017) ISSN: 1420-3049 [Electronic] Switzerland
• PMID: 28208727 (Publication Type: Journal Article)

Chemical References

• Analgesics
• Benzofurans
• Drugs, Chinese Herbal
• Neuroprotective Agents
• Phytochemicals
• Receptors, Metabotropic Glutamate
• metabotropic glutamate receptor type 1

Topics

• Analgesics (chemistry, pharmacology)
• Benzofurans (chemistry, pharmacology)
• Cell Survival (drug effects)
• Circular Dichroism
• Drugs, Chinese Herbal (chemistry, pharmacology)
• Humans
• Magnetic Resonance Spectroscopy
• Molecular Docking Simulation
• Molecular Dynamics Simulation
• Molecular Structure
• Morus (chemistry)
• Neuroprotective Agents (chemistry, pharmacology)
• Phytochemicals (chemistry)
• Receptors, Metabotropic Glutamate (chemistry, metabolism)