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Larik, Fayaz Ali,Faisal, Muhammad,Saeed, Aamer,Channar, Pervaiz Ali,Korabecny, Jan,Jabeen, Farukh,Mahar, Ihsan Ali,Kazi, Mehar Ali,Abbas, Qamar,Murtaza, Ghulam,Khan, Gul Shahzada,Hassan, Mubashir,Seo, Academic Press 2019 Bioorganic chemistry Vol.86 No.-
<P><B>Abstract</B></P> <P>The increasing resistance of pathogens to common antibiotics, as well as the need to control urease activity to improve the yield of soil nitrogen fertilization in agricultural applications, has stimulated the development of novel classes of molecules that target urease as an enzyme. In this context, the newly developed compounds on the basis of 1-heptanoyl-3-arylthiourea family were evaluated for Jack bean urease enzyme inhibition activity to validate their role as potent inhibitors of this enzyme. 1-Heptanoyl-3-arylthioureas were obtained in excellent yield and characterized through spectral and elemental analysis. All the compounds displayed remarkable potency against urease inhibition as compared to thiourea standard. It was found that novel compounds fulfill the criteria of drug-likeness by obeying Lipinski’s rule of five. Particularly compound <B>4a</B> and <B>4c</B> can serve as lead molecules in 4D (drug designing discovery and development). Kinetic mechanism and molecular docking studies also carried out to delineate the mode of inhibition and binding affinity of the molecules.</P> <P><B>Highlights</B></P> <P> <UL> <LI> A new family of 1-heptanoyl-3-arylthioureas (<B>4a-4j</B>) was synthesized in excellent yield. </LI> <LI> The synthesized 1-heptanoyl-3-arylthiourea family were evaluated for Jack bean urease enzyme inhibition activity. </LI> <LI> Particularly compound <B>4a</B> and <B>4c</B> can serve as lead molecules in 4D (drug designing discovery and development). </LI> <LI> Kinetic mechanism and molecular docking studies also carried out to delineate the mode of inhibition and binding affinity. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Reactive oxygen species-mediated unfolded protein response pathways in preimplantation embryos
Ihsan Ali,Syed Zahid Ali Shah,Yi Jin,Zhong-Shu Li,Obaid Ullah,Nan-Zhu Fang 대한수의학회 2017 Journal of Veterinary Science Vol.18 No.1
Excessive production of reactive oxygen species (ROS) and endoplasmic reticulum (ER) stress-mediated responses are critical to embryonic development in the challenging in vitro environment. ROS production increases during early embryonic development with the increase in protein requirements for cell survival and growth. The ER is a multifunctional cellular organelle responsible for protein folding, modification, and cellular homeostasis. ER stress is activated by a variety of factors including ROS. Such stress leads to activation of the adaptive unfolded protein response (UPR), which restores homeostasis. However, chronic stress can exceed the toleration level of the ER, resulting in cellular apoptosis. In this review, we briefly describe the generation and impact of ROS in preimplantation embryo development, the ROS-mediated activation mechanism of the UPR via the ER, and the subsequent activation of signaling pathways following ER stress in preimplantation embryos.
Ali Ersin Zumrutbas,Ali Ihsan Bozkurt,Okan Alkis,Cihan Toktas,Bulent Cetinel,Zafer Aybek 대한배뇨장애요실금학회 2016 International Neurourology Journal Vol.20 No.4
Purpose: The aims of this study were to assess the prevalence of nocturia and nocturnal polyuria (NP) and to define new cutoff values according to age and sex for both conditions. Methods: Data from a population-based prevalence survey conducted among a random sample of 2,128 adults were analyzed in this study. Participants were requested to fill out a questionnaire including the International Continence Society (ICS) definitions of lower urinary tract symptoms and the International Consultation on Incontinence Questionnaire - Short Form. Additionally, a 1-day bladder diary was given to each individual. The participants were divided into 5 age groups. The prevalence of nocturia was calculated based on definitions of nocturia as ≥1 voiding episodes, ≥2 episodes, and ≥3 episodes. NP was evaluated according to the ICS definition. The mean±standard errors and 95th percentile values were calculated in each group as new cutoff values for NP. Results: The prevalence of nocturia was estimated as 28.4%, 17.6%, and 8.9% for ≥1, ≥2, and ≥3 voiding episodes each night, respectively. When nocturia was defined as 2 or more voiding episodes at night, the prevalence decreased significantly. The mean NP index was 29.4%±15.0% in men and 23.1%±11.8% in women. For the age groups of <50 years, 50–59 years, and ≥60 years, the new cutoff values for the diagnosis of NP were calculated as 48%, 69%, and 59% for men and 41%, 50%, and 42% for women, respectively. Conclusions: We found that the definition of nocturia was still controversial and that waking up once for voiding might be within the normal spectrum of behavior. The definition of NP should be modified, and new cutoff values should be defined using the data presented in our study and in other forthcoming studies.
Ali, Gowhar,Subhan, Fazal,Islam, Nazar Ul,Ullah, Nasir,Shahid, Muhammad,Ullah, Sami,Ullah, Ihsan,Shah, Rehmat,Khan, Ikhtiar,Sewell, Robert D. E.,Abbas, Ghulam 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.7
The aim of the current study was to explore in vivo any relative gastroulcerogenic prospective propensity of newly synthesized nitrogen containing derivatives of salicyl alcohol; compound (I) [1-(2-hydroxybenzyl) piperidinium chloride], compound (II) [4-carbamoyl-1-(2- hydroxybenzyl)piperidinium chloride] and aspirin in albino rats. The experimental groups received the following oral treatments daily for 6 days: group I saline control; group II, standard (aspirin) treatment group [150 mg/kg of body weight]; group III, test (compound I) treatment group [100, 150 mg/kg]; group IV, test (compound II) treatment group [100, 150 mg/kg]. The results showed that in the case of the aspirin treated group and compound (I) [150 mg/kg], there was a significant increase in gastric volume, free acidity, total acidity, ulcer score and a decrease in gastric pH. Furthermore, histopathological examination of gastric mucosa of these treated groups revealed detectable morphological changes. Utilizing the same protocol, synthetic compound (I) [100 mg/kg] and (II) [100, 150 mg/kg] exhibited no statistically significant ulcerogenic or cytotoxic properties. A cyclooxygenase (COX) selectivity test indicated the preferential inhibition of COX-I and COX-II enzymes by compounds (I) and (II). This study therefore indicates that these synthetic compounds may possess reduced ulcerogenic potential and could be a functional substitute to aspirin.
Ullah, Ihsan,Khan, Abdul Latif,Ali, Liaqat,Khan, Abdur Rahim,Waqas, Muhammad,Hussain, Javid,Lee, In-Jung,Shin, Jae-Ho Microbiological Society of Korea 2015 The journal of microbiology Vol.53 No.2
<P>The Photorhabdus temperata M1021 secretes toxic compounds that kill their insect hosts by arresting immune responses. Present study was aimed to purify the insecticidal and antimicrobial compound(s) from the culture extract of P. temperata M1021 through bioassay guided fractionation. An ethyl acetate (EtOAc) extract of the P. temperata M1021 exhibited 100% mortality in Galleria mellonella larvae within 72 h. In addition, EtOAc extract and bioactive compound 1 purified form the extract through to column chromatography, showed phenol oxidase inhibition up to 60% and 80% respectively. The analysis of H-1 and C-13 NMR spectra revealed the identity of pure compound as 'benzaldehyde'. The benzaldehyde showed insecticidal activity against G. mellonella in a dose-dependent manner and 100% insect mortality was observed at 108 h after injection of 8 mM benzaldehyde. In a PO inhibition assay, 4, 6, and 8 mM concentrations of benzaldehyde were found to inhibit PO activity about 15%, 42%, and 80% respectively. In addition, nodule formation was significantly (P < 0.05) inhibited by 4, 6, and 8 mM of benzaldehyde as compare to control. Moreover, benzaldehyde was found to have great antioxidant activity and maximum antioxidant activity was 52.9% at 8 mM benzaldehyde as compare to control. Antimicrobial activity was assessed by MIC values ranged from 6 mM 10 mM for bacterial strains and 8 mM to 10 mM for fungal strains. The results suggest that benzaldehyde could be applicable for developing novel insecticide for agriculture use.</P>
Gowhar Ali,Fazal Subhan,Nazar Ul Islam,Nasir Ullah,Muhammad Shahid,Sami Ullah,Ihsan Ullah,Rehmat Shah,Ikhtiar Khan,Robert D. E. Sewell,Ghulam Abbas 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.7
The aim of the current study was to explorein vivo any relative gastroulcerogenic prospective propensityof newly synthesized nitrogen containing derivativesof salicyl alcohol; compound (I) [1-(2-hydroxybenzyl)piperidinium chloride], compound (II) [4-carbamoyl-1-(2-hydroxybenzyl)piperidinium chloride] and aspirin in albinorats. The experimental groups received the following oraltreatments daily for 6 days: group I saline control; group II,standard (aspirin) treatment group [150 mg/kg of bodyweight]; group III, test (compound I) treatment group [100,150 mg/kg]; group IV, test (compound II) treatment group[100, 150 mg/kg]. The results showed that in the case of theaspirin treated group and compound (I) [150 mg/kg], therewas a significant increase in gastric volume, free acidity,total acidity, ulcer score and a decrease in gastric pH. Furthermore, histopathological examination of gastricmucosa of these treated groups revealed detectable morphologicalchanges. Utilizing the same protocol, syntheticcompound (I) [100 mg/kg] and (II) [100, 150 mg/kg]exhibited no statistically significant ulcerogenic or cytotoxicproperties. A cyclooxygenase (COX) selectivity test indicatedthe preferential inhibition of COX-I and COX-IIenzymes by compounds (I) and (II). This study thereforeindicates that these synthetic compounds may possessreduced ulcerogenic potential and could be a functionalsubstitute to aspirin.
Are There Standardized Cutoff Values for Neutrophil-Lymphocyte Ratios in Bacteremia or Sepsis?
( Gonul Gurol ),( Ihsan Hakki Ciftci ),( Huseyin Agah Terzi ),( Ali Riza Atasoy ),( Ahmet Ozbek ),( Mehmet Koroglu ) 한국미생물 · 생명공학회 2015 Journal of microbiology and biotechnology Vol.25 No.4
Bacteremia and sepsis are common causes of morbidity and mortality worldwide, with incorrect or delayed diagnoses being associated with increased mortality. New tests or markers that allow a more rapid and less costly detection of bacteremia and sepsis have been investigated. The aim of this study was to clarify the cutoff value of the neutrophillymphocyte ratio (NLR) according to procalcitonin (PCT) level in the decision-making processes for bacteremia and sepsis. In addition, other white blood cell subgroup parameters, which are assessed in all hospitals, for bacteremia and sepsis were explored. This retrospective study included 1,468 patients with suspected bacteremia and sepsis. Patients were grouped according to the following PCT criteria: levels <0.05 ng/ml (healthy group), 0.05-0.5 ng/ml (local infection group), 0.5-2 ng/ml (systemic infection group), 2-10 ng/ml (sepsis group), and >10 ng/ml (sepsis shock group). One important finding of this study, which will serve as a baseline to measure future progress, is the presence of many gaps in the information on pathogens that constitute a major health risk. In addition, clinical decisions are generally not coordinated, compromising the ability to assess and monitor a situation. This report represents the first study to determine the limits of the use of NLR in the diagnosis of infection or sepsis using a cutoff value of <5 when sufficient exclusion criteria are used.
Joham Sarfraz Ali,Ihsan Khan,Muhammad Zia 경희대학교 융합한의과학연구소 2020 Oriental Pharmacy and Experimental Medicine Vol.20 No.1
The present study revolves around two different parts of Monotheca buxifolia extract and their solid phase extraction; and phytochemical and biological evaluation. Polar solvents tended to give maximum extraction yield. The highest phenolic content (69.1 ± 1 µgGAE/mg extract) was observed in the ethyl acetate + methanol (EtOAc + MeOH) fraction of stem. While highest flavonoid content (52.1 ± 0.45 µg QE/mg extract) was observed in MeOH crude extract of leaf. The antioxidant capacity was depicted by the MeOH fraction of leaf and EtOAc + MeOH fraction of stem. MeOH crude extract of leaf and CHCl3 (chloroform) crude extract of stem had notable inhibitory effect against bacterial strains (MIC 11.1 and 23.2 µg/ml, respectively). CHCl3 extract of leaf and n-hexane fraction presented significant antifungal activities (MIC 11.1 ug/ml).Though protein kinase inhibition was not significant but significant antileismanial activity and cytotoxic activity was observed. The study demonstrates potential of M. buxifolia for discovery of significant bioactive compounds through bioactivity guided isolation. Furthermore solid phase extraction is better for partial fractionation of active component.
Heo, Sung Hwan,Ihsan, Aamir,Yoo, Seung Hwa,Ali, Ghafar,Cho, Sung Oh Springer 2010 Nanoscale research letters Vol.5 No.4
<P>Stable carbon nanotube (CNT) field emitters for a vacuum-sealed miniature X-ray tube have been fabricated. The field emitters with a uniform CNT coating are prepared by a simple drop drying of a CNT mixture solution that is composed of chemically modified multi-walled CNTs, silver nanoparticles, and isopropyl alcohol on flat tungsten tips. A highly thermal- and electrical-conductive silver layer strongly attaches CNTs to the tungsten tips. Consequently, the field emitters exhibit good electron emission stability: continuous electron emission of around 100 μA at 2.3 V/μm has stably lasted over 40 h even at non-high vacuum ambient (~10<SUP>−3</SUP> Pa).</P>