12. Therapy for Urolithiasis by Urease Inhibitor Hydroxamic Acid

2015 ◽  
pp. 104-110
Author(s):  
K. Kobashi ◽  
K. Munakata ◽  
S. Takebe ◽  
J. Hase ◽  
H. Takeuchi ◽  
...  
Keyword(s):  
Hydroxamic Acid ◽  
Urease Inhibitor

Increasing nitrogen conservation by adding urease inhibitor NBPT to chicken compost manure

2010 ◽  
Vol 18 (3) ◽  
pp. 643-648
Author(s):  
Fa-Bao ZHANG ◽  
Wen-Jie GU ◽  
Pei-Zhi XU ◽  
Kai-Zhi XIE ◽  
Shuan-Hu TANG ◽  
...  
Keyword(s):  
Urease Inhibitor ◽  
Nitrogen Conservation ◽  
Compost Manure

A Structural Insight into Hydroxamic Acid Based Histone Deacetylase Inhibitors for the Presence of Anticancer Activity

2013 ◽  
Vol 21 (23) ◽  
pp. 2642-2664 ◽  
Author(s):  
H. Rajak ◽  
A. Singh ◽  
K. Raghuwanshi ◽  
R. Kumar ◽  
P.K. Dewangan ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Histone Deacetylase ◽  
Hydroxamic Acid ◽  
Histone Deacetylase Inhibitors ◽  
Structural Insight ◽  
Insight Into

Synthesis and Investigation of Therapeutic Potential of Isoform-Specific HDAC8 Inhibitors for the Treatment of Cutaneous T Cell Lymphoma

2019 ◽  
Vol 19 (7) ◽  
pp. 916-934 ◽  
Author(s):  
Appavoo Umamaheswari ◽  
Ayarivan Puratchikody ◽  
Natarajan Hari
Keyword(s):  
Side Effects ◽  
Inhibitory Activity ◽  
Hydroxamic Acid ◽  
Histone Deacetylase Inhibitors ◽  
Therapeutic Potential ◽  
In Vitro Assays ◽  
Normal Cells ◽  
Standard Drug ◽  
In Silico Studies ◽  
Hdac8 Inhibitors

Background:The available treatment option for any type of cancer including CTCL is chemotherapy and radiation therapy which indiscriminately persuade on the normal cells. One way out for selective destruction of CTCL cells without damaging normal cells is the use of histone deacetylase inhibitors (HDACi). Despite promising results in the treatment of CTCL, these HDACi have shown a broadband inhibition profile, moderately selective for one HDAC class but not for a particular isotype. The prevalence of drug-induced side effects leaves open a narrow window of speculation that the decreased therapeutic efficacy and observed side effects may be most likely due to non specific HDAC isoform inhibition. The aim of this paper is to synthesis and evaluates HDAC8 isoform specific inhibitors.Methods:Based on the preliminary report on the design and in silico studies of 52 hydroxamic acid derivatives bearing multi-substituent heteroaromatic rings with chiral amine linker, five compounds were shortlisted and synthesized by microwave assisted approach and high yielding synthetic protocol. A series of in vitro assays in addition to HDAC8 inhibitory activity was used to evaluate the synthesised compounds.Results:Inhibitors 1e, 2e, 3e, 4e and 5e exerted the anti-proliferative activities against CTCL cell lines at 20- 100 µM concentrations. Both the pyrimidine- and pyridine-based probes exhibited μM inhibitory activity against HDAC8. The pyrimidine-based probe 1e displayed remarkable HDAC8 selectivity superior to that of the standard drug, SAHA with an IC50 at 0.1µM.Conclusion:Our study demonstrated that simple modifications at different portions of pharmacophore in the hydroxamic acid analogues are effective for improving both HDAC8 inhibitory activity and isoform selectivity. Potent and highly isoform-selective HDAC8 inhibitors were identified. These findings would be expedient for further development of HDAC8-selective inhibitors.

scholarly journals Biochar and urease inhibitor mitigate NH3 and N2O emissions and improve wheat yield in a urea fertilized alkaline soil

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Khadim Dawar ◽  
Shah Fahad ◽  
M. M. R. Jahangir ◽  
Iqbal Munir ◽  
Syed Sartaj Alam ◽  
...  
Keyword(s):  
Nitrous Oxide ◽  
Grain Yield ◽  
Block Design ◽  
N Uptake ◽  
Nitrous Oxide Emissions ◽  
N2o Emissions ◽  
Urease Inhibitor ◽  
Alkaline Soil ◽  
Total N ◽  
N Assimilation

AbstractIn this study, we explored the role of biochar (BC) and/or urease inhibitor (UI) in mitigating ammonia (NH3) and nitrous oxide (N2O) discharge from urea fertilized wheat cultivated fields in Pakistan (34.01°N, 71.71°E). The experiment included five treatments [control, urea (150 kg N ha−1), BC (10 Mg ha−1), urea + BC and urea + BC + UI (1 L ton−1)], which were all repeated four times and were carried out in a randomized complete block design. Urea supplementation along with BC and BC + UI reduced soil NH3 emissions by 27% and 69%, respectively, compared to sole urea application. Nitrous oxide emissions from urea fertilized plots were also reduced by 24% and 53% applying BC and BC + UI, respectively, compared to urea alone. Application of BC with urea improved the grain yield, shoot biomass, and total N uptake of wheat by 13%, 24%, and 12%, respectively, compared to urea alone. Moreover, UI further promoted biomass and grain yield, and N assimilation in wheat by 38%, 22% and 27%, respectively, over sole urea application. In conclusion, application of BC and/or UI can mitigate NH3 and N2O emissions from urea fertilized soil, improve N use efficiency (NUE) and overall crop productivity.

scholarly journals Foliar Urea with N-(n-butyl) Thiophosphoric Triamide for Sustainable Yield and Quality of Pineapple in a Controlled Environment

2021 ◽  
Vol 13 (12) ◽  
pp. 6880
Author(s):  
Mohammad Amdadul Haque ◽  
Siti Zaharah Sakimin ◽  
Phebe Ding ◽  
Noraini Md. Jaafar ◽  
Mohd Khanif Yusop ◽  
...  
Keyword(s):  
Nitrogen Loss ◽  
Growth Yield ◽  
Fruit Weight ◽  
Soluble Solids ◽  
Urea Solution ◽  
Urease Inhibitor ◽  
N Losses ◽  
N Accumulation ◽  
Yield And Quality

In agricultural production, nitrogen loss leads to economic loss and is a high environmental risk affecting plant growth, yield, and quality. Use of the N fertilizer with a urease inhibitor is thus necessary to minimize N losses and increase the efficiency of N. This study aimed to evaluate the effects of N-(n-butyl) Thiophosphoric Triamide (NBPT) on the growth, yield, and quality of pineapple. The experiment involved two foliar fertilizer treatments: 1% (w/v) urea solution with NBPT (2.25 mL kg−1 urea) was treated as NLU (NBPT Liquid Urea), and the same concentration of urea without NBPT served as the control. Both were applied 12 times, starting 1 month after planting (MAP) and continuing once a month for 12 months. The application of urea with NBPT notably increased the above-ground dry biomass per plant (20% and 10% at 8 and 12 MAP, respectively), leaf area per plant (23% and 15% at 8 and 12 MAP, respectively), N accumulation per plant (10%), PFPN (Partial Factor Productivity) (13%), and average fruit weight (15%) compared to the treatment with urea alone (control). The analysis of quality parameters indicated that urea with NBPT improves TSS (Total Soluble Solids) (19%), ascorbic acid (10%), and sucrose (14%) but reduces the total organic acid content (21%) in pineapple. When using urea with a urease inhibitor (NBPT), there was a significant improvement in growth, yield, quality, and nitrogen use efficiency, with the additional benefit of reduced nitrogen losses, in combination with easy handling. Hence, urea with a urease inhibitor can be used as a viable alternative for increasing pineapple yield by boosting growth with better fruit quality.

ChemInform Abstract: QUINAZOLINES AND 1,4-BENZODIAZEPINES. 80. 1-HYDROXY-1,3-DIHYDRO-2H-1,4-BENZODIAZEPIN-2-ONE, A HYDROXAMIC ACID VIA AN AMIDINE N-OXIDE

1978 ◽  
Vol 9 (2) ◽  
Author(s):  
R. Y. NING ◽  
R. I. FRYER ◽  
B. C. SLUBOSKI
Keyword(s):  
Hydroxamic Acid

scholarly journals Suberoylanilide hydroxamic acid enhances the radiosensitivity of lung cancer cells through acetylated wild-type and mutant p53-dependent modulation of mitochondrial apoptosis

2021 ◽  
Vol 49 (2) ◽  
pp. 030006052098154
Author(s):  
Kan Wu ◽  
Xueqin Chen ◽  
Xufeng Chen ◽  
Shirong Zhang ◽  
Yasi Xu ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Hydroxamic Acid ◽  
Site Directed Mutagenesis ◽  
Lung Cancer Cells ◽  
Mutant P53 ◽  
Suberoylanilide Hydroxamic Acid ◽  
Mitochondrial Apoptosis ◽  
Wild Type ◽  
Clonogenic Cell

Objective Suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor, has shown potential as a candidate radiosensitizer for many types of cancers. This study aimed to explore the radiosensitization mechanism of SAHA in lung cancer cells. Methods Mutations in p53 were generated by site-directed mutagenesis using polymerase chain reaction. Transfection was performed to generate H1299 cells carrying wild-type or mutant p53. The radiosensitizing enhancement ratio was determined by clonogenic assays. Mitochondrial apoptosis was detected using JC-1 staining and flow cytometry analysis. Results Our results showed that SAHA induced radiosensitization in H1299 cells expressing wild-type p53, p53R175H or p53P223L, but this enhanced clonogenic cell death was not observed in parental H1299 (p53-null) cells or H1299 cells expressing p53 with K120R, A161T and V274R mutations. In SAHA-sensitized cells, mitochondrial apoptosis was induced following exposure to irradiation. Additionally, we observed that a secondary mutation at K120 (K120R) could eliminate p53-mediated radiosensitization and mitochondrial apoptosis. Conclusions The results of this study suggest that wild-type and specific mutant forms of p53 mediate SAHA-induced radiosensitization by regulating mitochondrial apoptosis, and the stabilization of K120 acetylation by SAHA is the molecular basis contributing to radiosensitization in lung cancer cells.

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