Table 1.

IC₅₀ values of the inhibition by chalcone and flavonoid derivatives against LPS-primed ATP-induced pro-caspase-1 processing in differentiated THP-1 cells.

	Chalcones			Flavonoids		Quercetin
	A ring				B ring
Chalcones	−R1	−R2	−R3	−R4	−R1	−R2	−R3	IC50 (μM)
11Cha1	−OH	−H	−OCH3	−OCH3	−H	−H	−COOH	1.5
11Cha2	−OH	−H	−OMOM a	−OMOM a	−H	−H	−COOH	1.7
11Cha3	−H	−H	−OCH3	−H	−H	−Br	−OH	1.9
11Cha4	−H	−H	−OCH3	−H	−H	−H	−I	>30
11Cha5	−H	−H	−OH	−H	−H	−H	−OCH2COOCH3	3.8
11Cha6	−OMOM a	−OCH3	−OMOM a	−OH	−H	−H	−OBn b	>30
11Cha7	−H	−H	−OBn b	−H	−H	−H	−OH	2.3
11Cha8	−H	−H	−H	−H	−OCH2COOCH2CH3	−H	−H	2.4
11Cha9	−OBn b	−I	−OMOM a	−OH	−H	−H	−OBn b	>30
11Cha10	−OBn b	−OCH3	−OH	−OH	−H	−H	−OBn b	>30
11Cha11	−OBn b	−OCD3	−OH	−OH	−H	−H	−OBn b	>30
Flavonoids	−R1	−R2	−R3	−R1	−R2	−R3	Release (%)	IC50 (μM)
Control							100±0
Apigenin	−OH	−H	−OH	−H	−H	−OH	89.5±18.1c	>30
Luteolin	−OH	−H	−OH	−H	−OH	−OH	94.2±12.4 c	>30
(±)−Hesperetin	−OH	−H	−OH	−H	−OH	−OCH3	58.1±11.6 c	>30
Naringenin	−OH	−H	−OH	−H	−H	−OH	59.0±9.3 c	>30
Hispidulin	−OH	−OCH3	−OH	−H	−H	−OH	79.6±19.1c	>30
Quercetin							81.3±15.6 c	>30

^a −OCH₂OCH₃, ^b −OCH₂C₆H₅, ^c Caspase-1 p20 release (%) in the presence of 30 μM flavonoid.