期刊
JOURNAL OF NATURAL PRODUCTS
卷 82, 期 12, 页码 3302-3310出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.9b00532
关键词
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资金
- National Natural Science Foundation of China [81703679, 81622047, 81930112]
- Liaoning BaiQianWan Talents Program
- Liaoning Revitalization Talents Program
- National Key R&D Program of China [2018YFC1705900]
- Liaoning Provincial Key RD Program [2019JH2/10300022]
- Open Research Fund of the State Key Laboratory of Cognitive Neuroscience and Learning [CNLZD1801]
Nine new monoterpenoid indole alkaloids, uncarialins A-I (1-9), were isolated from Uncaria rhynchophylla as well as 14 known analogues (10-23). Their structures were determined by HRESIMS, 1D and 2D NMR, and experimental and calculated electronic circular dichroism data. Compounds 5, 7, 15, and 22 displayed significant agonistic effects against the 5-HT1A receptor with EC50 values of 2.2 +/- 0.1, 0.1 +/- 0.1, 1.6 +/- 0.3, and 2.0 +/- 0.5 mu M, respectively. The mechanisms of action of these four compounds with the 5-HT1A receptor were investigated by molecular docking, and the results suggested that amino acid residues Asp116, Thr196, Asn386, and Tyr390 played critical roles in the observed activity of the above -mentioned compounds.
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