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Updated: Sep 13, 2026
Facilitating Drug Discovery: An Automated High-content Inflammation Assay in Zebrafish
Published on: July 16, 2012
Discovery of novel anti-inflammatory compounds from Borojó via bioactivity-guided zebrafish phenotyping screening and
Yuan-Ru Zheng1, Li-Fang Zou1, Hu-Hu Zeng2
1School of Traditional Chinese Medicine, Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Guangdong Basic Research Center of Excellence for Integrated Traditional and Western Medicine for Qingzhi Diseases, International Joint Laboratory of Zebrafish Models of Human Diseases and Drug Discovery, Southern Medical University, Guangzhou 510515, PR China.
Abstract:
Five new compounds, (3R,4S)-4-(2-methoxy-2-oxoethyl)cyclopent-1-ene-1,3-dicarboxylic acid (1), (3R,4S)-4-methylcyclopent-2-ene-1,3-dicarboxylic acid (2), (3R,4S)-4-(carboxymethyl)cyclopent-1-ene-1,3-dicarboxylic acid (3), tans-3-oxo-3,3a,6,6a-tetrahydro-1H-cyclopenta[c]furan-4-carboxylic acid (4) and tans-3,3a,4,6a-tetrahydro-2H-cyclopenta[b]furan-5-carboxylic acid (5), along with 4 known secondary metabolites including dihydroxybenzoic acid (6), trans-sinapic acid (7), furan-2-carboxylicacid (8) and 5-hydroxylmethylfuraldehyde (9) were isolated from Borojó (Borojoa patinoi Cuatrecasas). Their structures were established by spectroscopic data (UV, IR, MS, NMR, CD). Anti-inflammatory evaluation in zebrafish models revealed that both the crude extract and all isolates suppressed neutrophil recruitment, with 1 being the most active. Mechanistic studies showed that 1 inhibited LPS-induced inflammation by modulating the STAT3 and the TNF-α/NF-κB p65/IκBα pathways, reducing inflammatory cell infiltration, cytokine expression (IL-6, TNF-α), and nuclear translocation of p-STAT3 (Tyr705) and NF-κB p65. Molecular docking confirmed its binding to STAT3 and TNF-α. The discovery of novel anti-inflammatory compounds in Borojó, with the mechanisms validated, provides a molecular basis for its traditional use and supporting its development as a functional food or therapeutic agent.
