Brown S, Griffiths L A
Xenobiotica. 1983 Nov;13(11):669-82. doi: 10.3109/00498258309052228.
Butein (2',3,4,4'-tetrahydroxychalcone) and 2',3,4-trihydroxychalcone, following administration to bile-duct-cannulated rats, gave rise to the corresponding 3-O-methyl ethers which were excreted in conjugated forms in bile and urine. After parenteral and oral administration of [14C]butein, 53% and 20% of the dose, respectively, was excreted in bile in 24h. After oral administration of [14C]butein, 4-O-methylbutein, or 2',4',4-trihydroxychalcone to non-cannulated rats, 51%, 58% and 40% dose, respectively, was excreted in faeces, and 39%, 37% and 56%, respectively, in urine. Intraperitoneal administration of butein to non-cannulated rats led to excretion of 41% dose in urine and 56% in faeces. 3-O-Methylbutein and 4-O-methylbutein were demethylated in vivo and on incubation with rat-intestinal microflora in vitro, whilst 2',4-dihydroxy-3-methoxychalcone and 2',3-dihydroxy-4-methoxychalcone were not demethylated in vivo or in vitro. Following parenteral and oral administration of 4-O-methylbutein to bile-duct-cannulated rats, 91% and 21% dose, respectively, was excreted in the bile in 24h. After parenteral or oral administration of 2',4',4-trihydroxychalcone to cannulated rats, approx. 100% and 45% dose, respectively, was excreted in the bile in 24h. Trace amounts of 2',4',4-trihydroxychalcone were hydroxylated to give butein.
将布替因（2'，3，4，4'-四羟基查耳酮）和2'，3，4-三羟基查耳酮给予胆管插管大鼠后，会产生相应的3-O-甲基醚，这些醚以结合形式在胆汁和尿液中排泄。经肠胃外和口服给予[14C]布替因后，24小时内分别有53%和20%的剂量经胆汁排泄。给非插管大鼠口服[14C]布替因、4-O-甲基布替因或2'，4'，4-三羟基查耳酮后，分别有51%、58%和40%的剂量经粪便排泄，39%、37%和56%分别经尿液排泄。给非插管大鼠腹腔注射布替因后，41%的剂量经尿液排泄，56%经粪便排泄。3-O-甲基布替因和4-O-甲基布替因在体内以及与大鼠肠道微生物群体外孵育时会发生去甲基化，而2'，4-二羟基-3-甲氧基查耳酮和2'，3-二羟基-4-甲氧基查耳酮在体内或体外均未发生去甲基化。给胆管插管大鼠经肠胃外和口服给予4-O-甲基布替因后，24小时内分别有91%和21%的剂量经胆汁排泄。给插管大鼠经肠胃外或口服给予2'，4'，4-三羟基查耳酮后，24小时内分别约有100%和45%的剂量经胆汁排泄。痕量的2'，4'，4-三羟基查耳酮会被羟基化生成布替因。
