Design, biological evaluation, and molecular modelling insights of cupressic acid derivatives as promising anti-inflammatory agents

Autor:	Amal F. Soliman, Diaaeldin M. Elimam, Fardous F. El-Senduny, Manal A. Alossaimi, Mubarak Alamri, Fatma M. Abdel Bar
Jazyk:	angličtina
Rok vydání:	2023
Předmět:	Cupressic acid derivatives labdane diterpenoids RAW264.7 cell line COX-2 gene expression anti-inflammatory leads Therapeutics. Pharmacology RM1-950
Zdroj:	Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1 (2023)
Druh dokumentu:	article
ISSN:	14756366 1475-6374 1475-6366
DOI:	10.1080/14756366.2023.2187327
Popis:	The major labdanes in the oleogum resin of Araucaria heterophylla (Salisb.) Franco, 13-epi-cupressic acid (1) and acetyl-13-epi-cupressic acid (2) were used to prepare seven new (3–9), along with one known (10) derivatives. RAW264.7 cells were used to evaluate the anti-inflammatory activity of the derivatives (1–10) via measuring the level of COX-2 expression and IL-6. Pre-treated RAW264.7 cells with 1–10 (except for derivative 7) at 25 µM for 24h exhibited downregulation of COX-2 expression in response to LPS stimulation. Moreover, pre-treatment with compounds 1, 2, or 3 significantly attenuated the LPS-stimulated IL-6 level in RAW264.7 cells (p
Databáze:	Directory of Open Access Journals
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