Effects of chalcone derivatives on players of the immune system

Figures & data

Figure 1 Chalcone backbone.

Table 1 Effects of chalcone derivatives on immune cells

Types of cells	Chalcone/chalcone derivatives	Effects	Reference
Dendritic cells
Monocyte-derived human dendritic cells	Licochalcone A	↓ IL-6 and TNF-α secretion	^Citation38
Mouse dendritic cells	Xanthohumol	Activates caspase 8 and caspase 3, inducing apoptosis	^Citation39
Granulocytes
Human polymorphonuclear neutrophils	2-methoxy-4,4′-dihydroxy-5-α,α-dimethyl-allylchalcone 2-methoxy-3,4,4′-trihydroxychalcone	↓ LTB4 and LTC4 secretion	^Citation43
	Viscolin	↓ Superoxide anion production ↓ Elastase secretion	^Citation46
	(E)-1-[2-Hydroxy-4-methoxy-3-(morpholinomethyl) phenyl]-3-(pyridin-2-yl)prop-2-en-1-one (E)-1-[4-Ethoxy-2-hydroxy-5-(morpholinomethyl) phenyl]-3-(pyridin-2-yl)prop-2-en-1-one	↓ Superoxide anion production ↓ Elastase secretion	^Citation47
	Phenylsulfonyl uranyl chalcone derivatives	↓ LTB4 synthesis ↓ Superoxide anion production ↓ Elastase and myeloperoxidase release	^Citation48
	1-(2,3,4-trimethoxyphenyl)-3-(3-(2-chloroquinolinyl)-2-propen-1-one	↓ Elastase, superoxide anion, and LTB4 synthesis	^Citation49
	Bratelactone	↓ Superoxide anion generation and elastase release ↓ CD11b expression	^Citation50
Rat neutrophils	Broussochalcone A	↓ PK-C enzymatic activity ↓ Superoxide anion production	^Citation44
	2′,5′-dihydroxy-2-naphthylchalcone	↓ Neutrophil degranulation ↓ Superoxide anion production	^Citation45
	2′,5′-dihydroxy-2-furfurylchalcone (DHFC)	↓ Respiratory burst ↓ PLD activation ↓ ERK phosphorylation	^Citation51
Human basophils	Chalcone	↓ Histamine secretion	^Citation52
Rat basophils	4′-O-β-D-glucopyranosyl-4-hydroxy-3′-methoxychalcone 4′-O-β-D-glucopyranosyl-3′,4′-dimethoxychalcone	↓ Degranulation ↓ Intracellular Ca^2+ elevation Inactivation of NADPH oxidase	^Citation53
	Licochalcone D	↓ Basophilic cells degranulation ↓ Extracellular Ca^2+ influx ↓ Activation of ERK pathway	^Citation54
Innate lymphoid cells
IL-2 stimulated cytotoxic cells (LAK cells)	Xanthohumol	↓ Proliferation of LAK cells	^Citation57
Monocytes/macrophages
RAW 264.7 murine macrophages	(3-Phenyl-1-(2,4,6-tris (methoxymethoxy)phenyl)prop-2-yn-1-one)	↓ Transcriptional activity of AP-1 ↓ iNOS expression ↓ TNF-α secretion	^Citation63
	Trans-1,3-diphenyl-2,3-epoxypropane-1-one (DPEP)	↓ iNOS and COX-2 expression ↓ NO and PGE2 production ↓ TNF-α, IL-1β, and IL-6 secretion ↓ NFκB and MAPK phosphorylation	^Citation10
	2′-hydroxy-4′-methoxychalcone 2′,4-dihydroxy-4′-methoxychalcone 2′,4-dihydroxy-6′-methoxychalcone	↓ NO and TNF-α production ↓ NFκB and AP-1 activation	^Citation64
	(E)-1-[3-Hydroxy-4-(morpholinomethyl)phenyl]-3-(pyridin-4-yl)prop-2-en-1-one (E)-1-[3-Hydroxy-2,4-bis(morpholinomethyl)phenyl]-3-(pyridin-2-yl)prop-2-en-1-one	↓ NO production	^Citation47
	2′,4-dihydroxy-6′-isopentyloxychalcone (JSH)	↓ TLR4-mediated NFκB activation ↓ iNOS, COX-2, IL-1β, and IL-6 mRNA expression	^Citation66
	Naringenin chalcone	↓ TNF-α, MCP-1, and NO production	^Citation67
	Sofalcone	↓ NO, TNF-α, and MCP-1 production	^Citation68
	Phenylsulfonyl uranyl chalcone derivatives	↓ PGE2 production	^Citation48
	2′,5′-Dimethoxy-4-hydroxychalcone 3,4-Dichloro-2′,5′-diethoxychalcone	↓ NO production	^Citation69
	3,5-Di-tert-butyl-2′,4,5′-trihydroxychalcone 2′-hydroxy-3,4-dichlorochalcone 2′,5′-dimethoxy-4-hydroxychalcone	↓ NO production	^Citation70
	Cardamonin	↓ iNOS protein expression and NO production	^Citation71
	3-(2-hydroxyphenyl)-1-(5-methyl-furan-2-y-1) propenone (HMP)	↓ NO production Suppression of p38/ATF-2 and AP-1 signaling pathways	^Citation72
	3-(2,3-dimethoxy-phenyl)-1-naphthalene-1-yl-propenone 4-(4-diethylamino-phenyl)-1,1-diphenyl-but-3-en-2-one	↓ IL-6 and TNF-α secretion	^Citation73
	Okanin	↓ NO production and iNOS expression ↑ HO-1 expression	^Citation75
THP-1 monocytes	Cardamonin	↓ TNF-α production	^Citation71
	5-(4-bromo-phenyl)-5-chloro-1-(4-methoxy-phenyl)-penta-2,4-dien-1-one 5-chloro-5-(4-chloro-phenyl)-1-(4-methoxy-phenyl)-1-penta-2,4-dien-1-one	↓ IL-6 and TNF-α secretion	^Citation74
Mouse peritoneal macrophages	4-dimethylamino-3′,4′-dimethoxychalcone	↓ iNOS expression	^Citation65
Microglial cells	2′,5′-Dimethoxy-4-hydroxychalcone 3,4-Dichloro-2′,5′-diethoxychalcone	↓ NO production	^Citation69
	2′-hydroxy-3,4-dichlorochalcone 2′,5′-dimethoxy-4-hydroxychalcone	↓ NO production	^Citation70
Platelets
Rabbit platelets	2′,5′-dihydroxy chalcone 2′,3,4,4′-tetrahydroxyl chalcone	↓ Platelet aggregation	^Citation78
	2′,5′-dihydroxy-4-chlorodihydrochalcone	↓ Platelet aggregation	^Citation79
	(E)-1-[2-Hydroxy-4-methoxy-3-(morpholinomethyl) phenyl]-3-(pyridin-2-yl)prop-2-en-1-one (E)-1-[2-Hydroxy-4-methoxy-5-(morpholinomethyl) phenyl]-3-(pyridin-3-yl)prop-2-en-1-one	↓ Platelet aggregation	^Citation80
T cells
Cytotoxic T cells	Chalcone	↓ Generation and normal function of cytotoxic T cells	^Citation81
	Xanthohumol	↓ Proliferation and development of cells ↓ Production of IL-2, IFN-γ, and TNF-α	^Citation57
	Licochalcone A	↓ Proliferation of T cells ↓ IFN-γ secretion	^Citation84
	Naringenin chalcone	↓ IL-4, IL-5, and IL-13 production	^Citation85
	Naringenin	↓ Proliferation of T cells ↓ IL-2, IFN-γ, and TNF-α mRNA expressions ↑ Expression of apoptosis activators (Akt and Bcl-2) and ↓ apoptosis inhibitors (Bax and Bad)	^Citation86
Mouse EL-4 T cells	Xanthohumol	↑ IL-2 production ↑ NFAT and AP-1 activities	^Citation83

Abbreviations: mRNA, messenger RNA; ↑, increased; ↓, decreased.

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