The inhibitory effect of gossypol acetic acid on the activity of (Na++K+)-ATPase partially purified from the outer medulla of rabbit kidney was examined, the IC50 is 6.5 μM. The enzyme kinetic studies show that gossypol is noncompetitive with ATP, Mg2+, Na+ and K+ with apparent Ki of 15, 13, 14.0 and 4.4 μM respectively. These data suggest that gossypol inhibition of (Na++K+)-ATPase is due to direct catalytic action at the subunit level, it may prevent proper positioning of the catalytic center or decrease the amount of active enzyme.
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Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, BrazilUniv Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, Brazil
Silva, IV
Caruso-Neves, C
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Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, BrazilUniv Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, Brazil
Caruso-Neves, C
Azeredo, IM
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Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, BrazilUniv Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, Brazil
Azeredo, IM
Carvalho, TLG
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Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, BrazilUniv Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, Brazil
Carvalho, TLG
Lara, LS
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Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, BrazilUniv Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, Brazil
Lara, LS
de Mello, MC
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Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, BrazilUniv Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, Brazil
de Mello, MC
Lopes, AG
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Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, BrazilUniv Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, CCS, BR-219900 Rio De Janeiro, Brazil