Bioassay-guided isolation of novel and selective urease inhibitors from Diospyros lotus.
10.1016/S1875-5364(18)30021-9
- Author:
Abdur RAUF
1
;
Ghias UDDIN
2
;
Bina S SIDDIQUI
3
;
Ajmal KHAN
4
,
5
;
Umar FAROOQ
6
;
Farhan A KHAN
7
;
Syed Majid BUKHARI
7
;
Sher Bahadar KHAN
8
Author Information
1. Department of Chemistry, University of Swabi, Anbar-23561, Khyber Pakhtunkhwa, Pakistan.
2. Institute of Chemical Sciences, University of Peshawar, Peshawar-25120, Pakistan.
3. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
4. Department of Chemistry, COMSAT Institute of Information Technology, Abbottabad-22060, Pakistan
5. UoN Chair of Oman's Medicinal Plants and Marine Natural Products, University of Nizwa, Birkat Al-Mouz, Nizwa-616, Oman. Electronic address: ajmalkhan@ciit.net.pk.
6. Department of Chemistry, COMSAT Institute of Information Technology, Abbottabad-22060, Pakistan. Electronic address: umarf@ciit.net.pk.
7. Department of Chemistry, COMSAT Institute of Information Technology, Abbottabad-22060, Pakistan.
8. Center of Excellence for Advanced Materials Research (CEAMR), Department of Chemistry, Faculty of Science King Abdulaziz University, Jeddah 21589, Saudi Arabia Kingdom.
- Publication Type:Journal Article
- Keywords:
Carbonic anhydrase-II;
Diospyros lotus;
Naphthoquinones;
Phosphodiesterase-I;
Urease inhibitory activities;
α-Chymotrypsin
- MeSH:
Biological Assay;
Diospyros;
chemistry;
Enzyme Inhibitors;
chemistry;
isolation & purification;
pharmacology;
Molecular Structure;
Naphthoquinones;
chemistry;
isolation & purification;
pharmacology;
Plant Extracts;
chemistry;
pharmacology;
Plant Roots;
Urease;
antagonists & inhibitors
- From:
Chinese Journal of Natural Medicines (English Ed.)
2017;15(11):865-870
- CountryChina
- Language:English
-
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.
