Screening of Active Ingredients From Ficus tikoua Bur. Against Rheumatoid Arthritis and Their Enrichment Using a β‐Cyclodextrin‐Based Monolith

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Abstract
Ficus tikoua Bur., a perennial creeping woody liana belonging to the genus Ficus (Moraceae), has been traditionally used in combination therapies for rheumatoid arthritis (RA). This study aimed to screen active components from F. tikoua Bur. against RA. Prior to activity testing, compounds with appropriate polarity and size were enriched by a homemade β‐cyclodextrin‐based monolithic material when adjusting the polarity of the enrichment mobile phase. Anti‐inflammatory activity evaluations of different fractions were conducted using Cell Counting Kit‐8 (CCK‐8) assay and enzyme‐linked immunosorbent assay (ELISA). Results showed that the compounds in F. tikoua Bur. had no significant effect on RAW264.7 cell viability while effectively reducing secretion levels of inflammatory cytokines IL‐6 and TNF‐α. When a mixture of methanol and water (30:70, v / v ) was used as the enrichment mobile phase, those components adsorbed on the monolith exhibited optimal inhibition effects on IL‐6 and TNF‐α production. Further separation and LC–MS analysis of the most active fraction, combined with literature data, 4‐hydroxy‐3,5‐bis(3′‐methyl‐2‐butenyl) benzoic acid‐O‐β‐D‐glucopyranoside may be the primary anti‐inflammatory constituent. Optimization of enrichment conditions revealed that the monolithic material achieved an enrichment factor of 15.352 for the screened compound.
Funding Information
  • National Natural Science Foundation of China (21974034)

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