Bufotenine and its derivatives: synthesis, analgesic effects identification and computational target prediction / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
;
(6): 454-463, 2021.
Article
in English
| WPRIM
| ID: wpr-881086
ABSTRACT
Natural product bufotenine (5) which could be isolated from Venenum Bufonis, has been widely used as a tool in central nervous system (CNS) studies. We present here its quaternary ammonium salt (6) which was synthesized with high yields using 5-benzyloxyindole as raw materials, and we firstly discover its analgesic effects in vivo. The analgesic evaluation showed that compounds 5 and 6 had stronger effects on the behavior of formalin induced pain in mice. Moreover, the combination of compound 6 and morphine has a synergistic effect. We intended to explain the molecular mechanism of this effect. Therefore, 36 analgesic-related targets (including 15 G protein-coupled receptors, 6 enzymes, 13 ion channels, and 2 others) were systemically evaluated using reverse docking. The results indicate that bufotenine and its derivatives are closely related to acetyl cholinesterase (AChE) or α
Full text:
Available
Index:
WPRIM (Western Pacific)
Type of study:
Diagnostic study
/
Prognostic study
Language:
English
Journal:
Chinese Journal of Natural Medicines (English Ed.)
Year:
2021
Type:
Article
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