Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
8527041 | Chinese Journal of Natural Medicines | 2017 | 6 Pages |
Abstract
Two new dimeric naphthoquinones, 5â²,8â²-dihydroxy-6,6â²-dimethyl-7,3â²-binaphthyl-1,4,1â²,4â²-tetraone (1; Di-naphthodiospyrol D) and 5â²,8â²-dihydroxy-5,8-dimethoxy-6,6â²-dimethyl-7,3â²-binaphthyl-1,4,1â²,4â²-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 1â4 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 IC50 values of 1 and 2 were 260.4 ± 6.37 and 381.4 ± 4.80 µmol·Lâ1, respectively, using thiourea (IC50 = 21 ± 0.11 µmol·Lâ1) as the standard inhibitor. This was the first report demonstrating that the naphthoquinones class showed urease inhibition.
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Authors
Abdur Rauf, Ghias Uddin, Bina S. Siddiqui, Ajmal Khan, Umar Farooq, Farhan A. Khan, Syed Majid Bukhari, Sher Bahadar Khan,