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| 1 | Bioassay-guided isolation of novel and selective urease inhibitors from Diospyros lotus显示文摘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_(50) values of 1 and 2 were 260.4 ± 6.37 and 381.4 ± 4.80 μmol·L-1, respectively, using thiourea(IC_(50) = 21 ± 0.11 μmol·L^(-1)) as the standard inhibitor. This was the first report demonstrating that the naphthoquinones class showed urease inhibition. | Abdur Rauf Ghias Uddin Bina S. Siddiqui Ajmal Khan Umar Farooq Farhan A. Khan Syed Majid Bukhari Sher Bahadar Khan | 2017 | Chinese Journal of Natural Medicines2017，15，11： | 2 |
| 2 | Anti-nociceptive, anti-inflammatory and sedative activities of the extracts and chemical constituents of Diospyros lotus L.显示文摘 | Ghias Uddin Abdur Rauf Bina S. Siddiqui Naveed Muhammad Ajmal Khan Syed Uzair Ali Shah | 2014 | Phytomedicine2014，，： | 1 |
| 3 | In vivo sedative and muscle relaxants activity of Diospyros lotus L显示文摘Objective: To evaluate the sedative effect of Diospyros lotus L(D. lotus) extract in mice using the open field and Rota rod tests.Methods: For the sedative and muscle relaxants activities of extract/fractions of the plant, invivo open field and phenobarbitone-induced sleeping time were used, while the Roda rod test was employed in animals for the assessment of muscle relaxant activity.Results: Results from this investigation revealed that the extracts of D. lotus have exhibited significant sedative effect in mice(45.98%) at 100 mg/kg i.p. When the extract was partitioned with different solvents, the n-hexane fraction was inactive whereas the chloroform fraction was the most active with 82.67% sedative effect at 50 and 100 mg/kg i.p. On the other hand,the ethyl acetate and n-butanol fractions displayed significant sedative effects(55.65% and40.87%, respectively) at 100 mg/kg i.p. Among the tested extract/fractions, only chloroform and ethyl acetate fractions showed significant(P < 0.05) muscle relaxant activity in the Rota rod test.Conclusions: In short, our study provided scientific background to the traditional uses of D.lotus as sedative. | Abdur Rauf Ghias Uddin Bina Shaheen Siddiqui Haroon Khan | 2015 | Asian Pacific Journal of Tropical Biomedicine2015，5，4： | 1 |
| 4 | Reversal of multidrug resistance and antitumor promoting activity of 3-oxo-6β-hydroxy-β-amyrin isolated from Pistacia integerrima显示文摘The bioactive triterpenoid 3-oxo-6-β-hydroxy-β-amyrin(1)has been isolated from multiple plant sources.In this study,chloroform fraction of Pistacia integerrima extract was processed for the isolation of the compound.The compound identity was confirmed by advanced spectroscopy technique.X-ray crystallography was applied for molecular structure confirmation.In addition,compound 1 was screen for its activity on reversal of MDR(multidrug resistance)mediated by P-gp(P-glycoprotein).This was accomplished by using rhodamine123 exclusion on multidrug-resistant human ABCB1 gene transfected mouse T-lymphoma cell line.Outcomes revealed that MDR reversing effect was comparable to verapamil as positive control in vitro.Treatment of TPA-induced tumor promotion with 3-oxo-6β-hydroxy-β-amyrin led to reduction in the applied anti-tumor promotion experiment.The chemo-preventive effect of 3-oxo-6β-hydroxy-β-amyrin was comparable to curcumin as positive control based on the reduction of immediate early tumor antigen expression.Molecular docking by applying Autodock Vina 1 and i-GEMDOCK v 2.1 tools indicated that compound 1 gives good docking results,as determined by their fitness score and specificity.Moreover,results showed that compound 1 isolated from Pistacia integerrima precisely attached to a region where co-crystallized ligand for receptor previously existed.Our findings may explain the use of Pistacia integerrima plant extracts as an anticancer agent in folk medicine. | ABDUR RAUF SAUD BAWAZEER MUSLIM RAZA EMAN EL-SHARKAWY MD.HABIBUR RAHMAN MOHAMED A.EL-ESAWI GHIAS UDDIN BINA SSIDDIQUI ANEES AHMED KHALIL JOSEPH MOLNAR AKOS CSONKA DIÁNA SZABÓ HAROON KHAN MOHAMMAD SMUBARAK TAIBI BEN HADDA MUDYAWATI KAMARUDDIN SEEMA PATEL | 2021 | BIOCELL2021，45，1： | 0 |
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