1. Diterpenoids from Acanthopanacis Cortex and their anti-inflammatory activity studies.
- Author
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Yang HD, Hou BL, Yang YG, Tang ZS, and Xu HB
- Subjects
- Molecular Structure, Phytochemicals pharmacology, Phytochemicals isolation & purification, Cyclooxygenase 1 metabolism, Acanthaceae chemistry, Humans, Cyclooxygenase 2 Inhibitors pharmacology, Cyclooxygenase 2 Inhibitors isolation & purification, China, Diterpenes pharmacology, Diterpenes isolation & purification, Diterpenes chemistry, Anti-Inflammatory Agents pharmacology, Anti-Inflammatory Agents isolation & purification, Anti-Inflammatory Agents chemistry, Cyclooxygenase 2 metabolism, Leukocyte Elastase antagonists & inhibitors
- Abstract
Acanthopanacis Cortex (A.-C) with a long history of more than1000 years, has been used to treat rheumatism effectively. Nineteen diterpenoids have been isolated from A.-C, including six new compounds (1-6). Among them, compounds 7, 9-11, 13, and 17 were discovered from A.-C for the first time. The structures of 1-6 were determined by analyzing their NMR data and comparing their experimental and calculated electronic circular dichroism spectra. Moreover, the single-crystal X-ray diffraction data of 1, 2, 8, and 14 were provided. The anti-inflammatory activity of 1-5 and 7-18 on neutrophil elastase, cyclooxygenase-1 (COX-1), and cyclooxygenase-2 (COX-2) has been studied in vitro, and the results showed that 15 had almost no inhibitory effects on COX-1 at 200 μM but a significant activity against COX-2 with an IC
50 of 0.73 ± 0.006 μΜ. It indicated that compound 15 can provide valuable information for the design of selective COX-2 inhibitors., Competing Interests: Declaration of competing interest The authors declare no conflicts of interest., (Copyright © 2024 Elsevier B.V. All rights reserved.)- Published
- 2024
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