Antidepressant potential of Uncaria rhynchophylla and its active flavanol, catechin, targeting melatonin receptors
Geng, Chang-An1,2; Yang, Tong-Hua1,2; Huang, Xiao-Yan1,2; Ma, Yun-Bao1,2; Zhang, Xue-Mei1,2; Chen, Ji-Jun1,2,3
Corresponding AuthorChen, Ji-Jun(chenjj@mail.kib.ac.cn)
2019-03-25
Source PublicationJOURNAL OF ETHNOPHARMACOLOGY
ISSN0378-8741
Volume232Pages:39-46
AbstractEthnopharmacological relevance: Traditional Chinese medicines (TCMs) are fascinating sources for natural drug candidates. Uncaria rhynchophylla (Gouteng) is a famous TCM used for alleviating central nervous system (CNS) disorders, while its antidepressant constituents are still disputed. Aim of the study: The present study was designed to assess the antidepressant property of U. rhynchophylla and characterize the active constituents targeting melatonin receptors which are closely related to CNS diseases. Materials and methods: The total extract and each fraction of U. rhynchophylla were extensively assessed for their agonistic activity on melatonin receptors in vitro. The following bioassay-guided fractionation yielded the active constituents, whose activity was confirmed by dose-dependent bioassay and antagonistic experiment on HEK293 cells. Their antidepressant effects were evaluated on forced swimming test (FST), tail suspension test (TST) and open-field test (OFT) mice models in vivo. Their metabolic profiles in mice plasma were analyzed by LCMS-IT-TOF. Results: The stems and hooks of U. rhynchophylla were revealed with agonistic activity on melatonin receptors (MT1 and MT2). Under the guidance of bioassay, two flavanols, catechin and epicatechin were obtained and showed obviously activity agitating MT1 (EC50 = 25.8 and 156.1 mu M) and MT2 (EC50 = 47.3 and 208.8 mu M) receptors. The agonistic activity of catechin on melatonin receptors can be antagonized by luzindole at the concentrations of 1.57-100 mu M. Catechin could significantly reduce the immobility time in both FST and TST mice models at doses of 80 and 40 mg/kg, without obvious effect on locomotor activity in OFT mice model. Five phase II (M1-M5) and one phase I (M6) metabolites of catechin were detected in mice plasma after intragastric (i.g.) administration. Conclusion: Catechin is a potent antidepressant candidate from U. rhynchophylla by targeting melatonin receptors. The main metabolic pathways of catechin in mice plasma are glucuronidation (M3) and methylated glucuronidation (M4 and M5). This study provides valuable information for understanding the antidepressant potency of Gouteng and its active constituents.
KeywordUncaria rhynchophylla Catechin Melatonin receptors Metabolites Antidepressant activity
DOI10.1016/j.jep.2018.12.013
Indexed BySCI
Language英语
WOS Research AreaPlant Sciences ; Pharmacology & Pharmacy ; Integrative & Complementary Medicine
WOS SubjectPlant Sciences ; Chemistry, Medicinal ; Integrative & Complementary Medicine ; Pharmacology & Pharmacy
WOS IDWOS:000467003000005
Citation statistics
Cited Times:6[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/66864
Collection植物化学与西部植物资源持续利用国家重点实验室
Corresponding AuthorChen, Ji-Jun
Affiliation1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, 132 Lanhei Rd, Kunming 650201, Yunnan, Peoples R China
2.Yunnan Key Lab Nat Med Chem, Kunming 650201, Yunnan, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
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GB/T 7714
Geng, Chang-An,Yang, Tong-Hua,Huang, Xiao-Yan,et al. Antidepressant potential of Uncaria rhynchophylla and its active flavanol, catechin, targeting melatonin receptors[J]. JOURNAL OF ETHNOPHARMACOLOGY,2019,232:39-46.
APA Geng, Chang-An,Yang, Tong-Hua,Huang, Xiao-Yan,Ma, Yun-Bao,Zhang, Xue-Mei,&Chen, Ji-Jun.(2019).Antidepressant potential of Uncaria rhynchophylla and its active flavanol, catechin, targeting melatonin receptors.JOURNAL OF ETHNOPHARMACOLOGY,232,39-46.
MLA Geng, Chang-An,et al."Antidepressant potential of Uncaria rhynchophylla and its active flavanol, catechin, targeting melatonin receptors".JOURNAL OF ETHNOPHARMACOLOGY 232(2019):39-46.
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