New Radiolytic Cyclization Products, Phlorocyclin and Isophlorocyclin Exhibit Anti-inflammatory Effects in LPS-stimulated Macrophages
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Phlorocyclin (PC) and isophorocyclin (IPC) are rare benzofuran derivaitves obtained from therepresentive dihydrochalcone glucoside, phloridzin (PZ) and are a type of neolignan backbone with a potential antiglycativeagents. However, research related to the enhancement of biological functionallites to inflammation of thenewly converted products is very limited. This research was directed with the purpose of discovery more effectiveanti-inflammatory agents in macrophages of newly radiolysis products PC and IPC. The anti-inflammatory capacitiesof the characterized products in RAW 264.7 and DH82 macrophages treated with lipopolysaccharide (LPS) to stimulatean inflammation response were examined. The pro-inflammatory factors such as prostaglandin E2 (PGE2), tumornecrosis factor-α (TNF-α), nitric oxide (NO), interleukin-6 (IL-6), and IL-10, without cytotoxicity in LPS-stimulatedmacrophages, were significantly inhibited after treatment with PC and IPC, when compared to PZ. Moreover, PC and IPCdecreased the appearance of cyclooxygenase-2 (COX-2) and inducible NO synthase (iNOS) proteins in macrophages. The cyclization products modified by radiolysis showed the greatest anti-inflammatory effects in macrophage cells,indicating PC and IPC are a potential candidate for use in anti-inflammatory agents.
Abstract
Phlorocyclin (PC) and isophorocyclin (IPC) are rare benzofuran derivaitves obtained from therepresentive dihydrochalcone glucoside, phloridzin (PZ) and are a type of neolignan backbone with a potential antiglycativeagents. However, research related to the enhancement of biological functionallites to inflammation of thenewly converted products is very limited. This research was directed with the purpose of discovery more effectiveanti-inflammatory agents in macrophages of newly radiolysis products PC and IPC. The anti-inflammatory capacitiesof the characterized products in RAW 264.7 and DH82 macrophages treated with lipopolysaccharide (LPS) to stimulatean inflammation response were examined. The pro-inflammatory factors such as prostaglandin E2 (PGE2), tumornecrosis factor-α (TNF-α), nitric oxide (NO), interleukin-6 (IL-6), and IL-10, without cytotoxicity in LPS-stimulatedmacrophages, were significantly inhibited after treatment with PC and IPC, when compared to PZ. Moreover, PC and IPCdecreased the appearance of cyclooxygenase-2 (COX-2) and inducible NO synthase (iNOS) proteins in macrophages. The cyclization products modified by radiolysis showed the greatest anti-inflammatory effects in macrophage cells,indicating PC and IPC are a potential candidate for use in anti-inflammatory agents.
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