Bioassay-guided isolation of novel and selective urease inhibitors from Diospyros lotus / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
;
(6): 865-870, 2017.
Artigo
em Inglês
| WPRIM
| ID: wpr-812047
ABSTRACT
Two new dimeric naphthoquinones, 5',8'-dihydroxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (1; Di-naphthodiospyrol D) and 5',8'-dihydroxy-5,8-dimethoxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin (3) and 8-hydroxy diospyrin (4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments. The fractions and compounds 1-4 were evaluated for urease activity and phosphodiesterase-I, carbonic anhydrase-II and α-chymotrypsin enzyme inhibitory activities. Compounds 1 and 2 and their corresponding fractions showed significant and selective inhibitory effects on urease activities. The IC values of 1 and 2 were 260.4 ± 6.37 and 381.4 ± 4.80 µmol·L, respectively, using thiourea (IC = 21 ± 0.11 µmol·L) as the standard inhibitor. This was the first report demonstrating that the naphthoquinones class showed urease inhibition.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Urease
/
Bioensaio
/
Extratos Vegetais
/
Estrutura Molecular
/
Química
/
Naftoquinonas
/
Raízes de Plantas
/
Diospyros
/
Inibidores Enzimáticos
Idioma:
Inglês
Revista:
Chinese Journal of Natural Medicines (English Ed.)
Ano de publicação:
2017
Tipo de documento:
Artigo
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