scholarly journals SYNTHESIS AND ANTICANCER ACTIVITY TEST OF 2-HYDROXY-N-PHENYLNICOTINAMIDE

2013 ◽  
Vol 13 (2) ◽  
pp. 166-170 ◽  
Author(s):  
Salahuddin Salahuddin ◽  
Muhammad Hanafi ◽  
Hariyanti Hariyanti
Keyword(s):  
Biologically Active ◽  
Leukemia Cells ◽  
Cytotoxicity Test ◽  
The Novel ◽  
Activity Test ◽  
Ic50 Value ◽  
Amidation Reaction ◽  
One Step ◽  
Ft Ir ◽  
The Uk

The novel compound of 2-hydroxy-N-phenylnicotinamide was synthesized from modification of the UK-3A compound, which was known biologically active to inhibit bacterial and cancer cells growth. Synthesis of this compound was carried out in one-step reaction. Analog UK-3A compound namely 2-hydroxy-N-phenylnicotinamide was synthesized from 2-hydroxynicotinic acid as the starting material using amidation reaction with aniline in presence of DCC/DMAP in pyridine. Analog UK-3A was analyzed and identified using TLC, FT-IR, LC-MS and FT-NMR spectrofotometer. The yield after purification was 42.97%. The IC50 value 85 μg/mL was obtained from cytotoxicity test against P388 Murine Leukemia cells. It indicated that the synthesis products were sufficiently potential for leukemia P388 treatment.

scholarly journals Molecular Docking of Lunacridine from Lunasia amara to DNA : Its Inhibition And Interaction Study Correlated With The Cytotoxic Activity on P388 Murine Leukemia Cells

2010 ◽  
Vol 1 (2) ◽  
pp. 108 ◽  
Author(s):  
M. Sulaiman Zubair ◽  
Subehan Subehan
Keyword(s):  
Molecular Docking ◽  
Binding Energy ◽  
Cytotoxic Activity ◽  
Topoisomerase Ii ◽  
Leukemia Cells ◽  
Active Principle ◽  
Cytotoxicity Test ◽  
Dna Intercalator ◽  
Ic50 Value ◽  
Murine Leukemia

DNA Topoisomerase II inhibitors are a type of anticancer drugs. These drugs perform their biological activity either by forming a DNA-intercalator-topoisomerase II ternary complex or by inhibiting other enzymes and/or transcription factors that act on DNA. The strong interactions with DNA play a crucial role for their pharmacological properties. Lunacridine, the active principle from Lunasia amara, was known as DNA intercalating Topoisomerase II inhibitor. With the aims to explore the affinity and molecular interaction of lunacridine compound isolated from Lunasia amara with DNA, molecular docking study has been carried out with DNA model using Autodock 4.0 software. Cytotoxicity test on P388 murine leukemia cells was done also using 100, 30, 10, 3 and 1 μg/ml series of lunacridine concentration. The docking result shows that Lunacridine itself could to dock intercalatively between base pairs of DNA and the possibility interaction with adenine, thymine and cytosine by dipole-dipole interaction.  The lowest predicted binding  energy of lunacridine is –6,22 kcal/mol, whereas original ligand bis thiazole is -16,37 kcal/mol. Lunacridine compound itself has less cytotoxic activity on P388 murine leukemia cells with the IC50 value of 39,52 μg/ml or 129,41 μM. The binding energy of lunacridine on DNA higher than original ligand show that the interaction of lunacridine with DNA is not stable afford the less cytotoxic activity. However, based on the IC50 value, lunacridine could be depeloved as anticancer.Key words: docking, lunacridine,  Lunasia amara, cytotoxic, P388 murine leukimia cells.

A One-Pot Hydrothermal Synthesis of Eu/BiVO4 Enhanced Visible-Light-Driven Photocatalyst for Degradation of Tetracycline

2020 ◽  
Vol 20 (5) ◽  
pp. 3053-3059 ◽  
Author(s):  
Zhenzhao Pei ◽  
Heng Jia ◽  
Yulong Zhang ◽  
Pei Wang ◽  
Yabao Liu ◽  
...  
Keyword(s):  
Photocatalytic Activity ◽  
Visible Light ◽  
Active Species ◽  
Photocatalytic Process ◽  
One Pot ◽  
Photodegradation Efficiency ◽  
Activity Test ◽  
Visible Light Driven ◽  
One Step ◽  
Ft Ir

Eu/BiVO4 photocatalyst was synthesized by a facile one-step hydrothermal method. The structures and morphologies of Eu/BiVO4 photocatalysts were investigated by XRD, SEM and FT-IR and their photocatalytic activity was evaluated by the degradation of tetracycline hydrochloride (TCH) under the visible light irradiation. From the photocatalytic activity test, 1% Eu/BiVO4 displayed more superior photodegradation efficiency with 91.4% degradation efficiency of TCH in 150 min by contrast with 77.3% degradation rate of pure BiVO4. The mechanism has been explored that h+ is the primary active species, and ·OH is a secondary active substance in the photocatalytic process.

The Differentially Effect of Some Antilipid Drugs on Activity of the Novel Synthesized Paraoxonase (PON1)-Inorganic Hybrid Nanoflowers

2020 ◽  
Vol 62 ◽  
pp. 59-74
Author(s):  
Hayrunnisa Nadaroglu ◽  
Farzad Ghebleh ◽  
Medine Türkoğlu ◽  
Saltuk Buğrahan Ceyhun
Keyword(s):  
Isobutyric Acid ◽  
Hybrid Structure ◽  
Lipid Lowering ◽  
Pon1 Activity ◽  
Hatching Rate ◽  
Zebrafish Embryos ◽  
The Novel ◽  
Step Procedure ◽  
One Step ◽  
Ft Ir

In the present study, the hybrid nanoflower PON1-Ca2+ (hNF-PON1) structure was synthesized and characterized and some antilipid drugs effects were investigated on hybrid paraoxonase (PON1) activity. Firstly, the hPON1 enzyme was purified 304.5 fold with 76.4% yield from human serum using the triple phase separation technique (TPP). Then, the hNF-PON1 was prepared in a one-step procedure using biomimetic mineralization. The catalytic activity of the hybrid enzyme with an 88.49% binding rate increased by 26.40%. The characterization of hNF-PON1 structure was performed with SEM, TEM, EDX, FT-IR and XRD analyzes. The effects of some lipid-lowering drugs (Valeric acid, phenoxy – isobutyric acid, N-desmethyl rosuvastatin) were also investigated on the activity of hNF-PON1 enzyme. When the re-usability of the enzyme was tested 10 times in succession, the enzyme was determined to protect the activity by 60%. Inhibition kinetics (IC50 and Ki values) of hybrid structure was determined. In the last stage of the study, the potential toxic effect of hNF-PON1 structure was evaluated using zebrafish embryos. To this end, zebrafish embryos were exposed to hNF-PON1 with 50-2000 ppm concentrations and monitored at 24, 48, 72 and 96 hpf. Survival rate, hatching rate and body malformations were evaluated during this period and it was determined that the hNF-PON1 structure did not exhibit any toxicity on zebrafish embryos.

Synthesis, characterization and photochemical properties of metallo porphyrazines substituted with alkyl linked carbazole, benzoazepine and phenothiazine moieties

2017 ◽  
Vol 21 (09) ◽  
pp. 599-610 ◽  
Author(s):  
Remziye Olgaç ◽  
Yasemin Baygu ◽  
Burak Yıldız ◽  
Yaşar Gök ◽  
Baybars Köksoy ◽  
...  
Keyword(s):  
Spectroscopic Methods ◽  
The Novel ◽  
Oxygen Generation ◽  
H Nmr ◽  
Singlet Oxygen Generation ◽  
One Step ◽  
Ft Ir ◽  
Photochemical Properties ◽  
C Nmr

Novel octa-phenotiazine, octa-benzoazepine and octa-carbazole substituted magnesium(II) (MgPz-I-III) and zinc(II) (ZnPz-I-III) porphyrazines were synthesized from 2,3-bis[6-(4a,10a-dihydro-phenothiazin-10-yl)-hexylsulfanyl]-but-2-enedinitrile (5), 2,3-bis [6-(4a,11a-dihydro-dibenzo[b,f]azepin-5-yl)-hexysulfan-yl]-but-2-enedinitrile (8) and 2,3-bis(6-carbazol-9-yl-hexylsulfanyl)-but-2-enedinitrile (10), respectively. These dinitrile derivatives 5, 8 and 10 were also prepared by the reaction of 1,2-dicyano-1,2-ethylenedithiolate di-sodium salt (4) with 10-(6-bromohexyl)-10H-phenothiazine (3), 5-(6-bromohexyl)-5H-diben-zo[b,f]azepine (7) and 9-(6-bromo-hexyl)-9H-carbazole (9), respectively. Porphyrazino-zinc(II) complexes were synthesized by one-step reaction using Zn(BuO)[Formula: see text] as a template agent. All the novel compounds were characterized by elemental analysis and different spectroscopic methods such as [Formula: see text]H NMR, [Formula: see text]C NMR, FT-IR, UV-Vis and mass. The photochemical properties including photodegradation and singlet oxygen generation for magnesium(II) and zinc (II) porphyrazine complexes were studied in dimethylsulfoxide solutions for determination of their photosensitizer behaviors.

Antioxidant Activity, Inhibition α-Glucosidase of Ethanol Extract of Strychnos nitida G. Don and Identification of Active Compounds

2019 ◽  
Vol 5 (3) ◽  
pp. 11-20
Author(s):  
Stefani Dhale Rale ◽  
Hasim Hasim ◽  
Syamsul Falah
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Ethanol Extract ◽  
Ethyl Acetate Fraction ◽  
Inhibition Activity ◽  
Active Compounds ◽  
Activity Inhibition ◽  
Activity Test ◽  
Ic50 Value ◽  
Treatment Of Diabetes

This study aims to find the treatment of diabetes using natural materials by exploring plants in the province of East Nusa Tenggara. his research was conducted out by extracting the Strychnos nitida G.Don stem using a method of maceration by ethanol 70%. Ethanol extract was then fractionated using n-hexane and ethyl acetate. Simplicia from maceration and fractionation results were then tested for antioxidant activity, α-glucosidase inhibition activity and identification of active compounds. The results showed that ethyl acetate fraction had the lowest IC50 value of 86.83 μg / ml. Results of the α-glucosidase activity test showed that ethyl acetate fraction and n-heksan fraction at 900 ppm had the highest percentage of inhibition of 34.23% and 33.89%. Identification using LCMS/MS method showed that ethyl acetate fraction consist of Benzenemethamine, N, N-dioctyl- as an antioxidantcompound and compound 24-methyl-5-cholestone-hexol as an antidiabetic compound. From the results of this study, we concluded that the extract of kayu ular Strychnos nitida G.Don stem has inhibition activity toward α-glucosidase enzyme.

scholarly journals Cardiorespiratory fitness assessment using risk-stratified exercise testing and dose–response relationships with disease outcomes

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Tomas I. Gonzales ◽  
Kate Westgate ◽  
Tessa Strain ◽  
Stefanie Hollidge ◽  
Justin Jeon ◽  
...  
Keyword(s):  
Cardiorespiratory Fitness ◽  
Maximal Oxygen Consumption ◽  
Estimation Method ◽  
The Novel ◽  
Exercise Tests ◽  
Metabolic Equivalent ◽  
Fitness Assessment ◽  
Disease Outcomes ◽  
All Cause Mortality ◽  
The Uk

AbstractCardiorespiratory fitness (CRF) is associated with mortality and cardiovascular disease, but assessing CRF in the population is challenging. Here we develop and validate a novel framework to estimate CRF (as maximal oxygen consumption, VO2max) from heart rate response to low-risk personalised exercise tests. We apply the method to examine associations between CRF and health outcomes in the UK Biobank study, one of the world’s largest and most inclusive studies of CRF, showing that risk of all-cause mortality is 8% lower (95%CI 5–11%, 2670 deaths among 79,981 participants) and cardiovascular mortality is 9% lower (95%CI 4–14%, 854 deaths) per 1-metabolic equivalent difference in CRF. Associations obtained with the novel validated CRF estimation method are stronger than those obtained using previous methodology, suggesting previous methods may have underestimated the importance of fitness for human health.

scholarly journals Hydrothermal Synthesis of Sodalite-Type N-A-S-H from Fly Ash to Remove Ammonium and Phosphorus from Water

Materials ◽  
2021 ◽  
Vol 14 (11) ◽  
pp. 2741
Author(s):  
Pengcheng Lv ◽  
Ruihong Meng ◽  
Zhongyang Mao ◽  
Min Deng
Keyword(s):  
Fly Ash ◽  
Adsorption Capacity ◽  
Removal Rate ◽  
Kinetic Studies ◽  
Solute Concentration ◽  
Raw Material ◽  
Sodium Aluminosilicate ◽  
Equilibrium Data ◽  
One Step ◽  
Ft Ir

In this study, the hydrated sodium aluminosilicate material was synthesized by one-step hydrothermal alkaline desilication using fly ash (FA) as raw material. The synthesized materials were characterized by XRD, XRF, FT-IR and SEM. The characterization results showed that the alkali-soluble desilication successfully had synthesized the sodium aluminosilicate crystalline (N-A-S-H) phase of sodalite-type (SOD), and the modified material had good ionic affinity and adsorption capacity. In order to figure out the suitability of SOD as an adsorbent for the removal of ammonium and phosphorus from wastewater, the effects of material dosing, contact time, ambient pH and initial solute concentration on the simultaneous removal of ammonium and phosphorus are investigated by intermittent adsorption tests. Under the optimal adsorption conditions, the removal rate of ammonium was 73.3%, the removal rate of phosphate was 85.8% and the unit adsorption capacity reached 9.15 mg/L and 2.14 mg/L, respectively. Adsorption kinetic studies showed that the adsorption of ammonium and phosphorus by SOD was consistent with a quasi-secondary kinetic model. The adsorption isotherm analysis showed that the equilibrium data were in good agreement with the Langmuir and Freundlich model. According to thermodynamic calculations, the adsorption of ammonium and phosphorus was found to be a heat-absorbing and spontaneous process. Therefore, the preparation of SOD by modified FA has good adsorption properties as adsorbent and has excellent potential for application in the removal of contaminants from wastewater.

scholarly journals MXene-Ti3C2 assisted one-step synthesis of carbon-supported TiO2/Bi4NbO8Cl heterostructures for enhanced photocatalytic water decontamination

Nanophotonics ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 2077-2088 ◽  
Author(s):  
Daixun Jiang ◽  
Xun Sun ◽  
Xilu Wu ◽  
Shuai Zhang ◽  
Xiaofei Qu ◽  
...  
Keyword(s):  
Charge Separation ◽  
Photocatalytic Performance ◽  
Separation Efficiency ◽  
Salt Flux ◽  
The Novel ◽  
Water Contaminants ◽  
Photocatalytic Removal ◽  
One Step ◽  
Charge Separation Efficiency ◽  
Perovskite Type

AbstractThe strategy to improve the photocatalytic removal efficiencies towards organic pollutants is still a challenge for the novel Sillen–Aurivillius perovskite type Bi4NbO8Cl. Herein, we report carbon-supported TiO2/Bi4NbO8Cl (C-TiO2/Bi4NbO8Cl) heterostructures with enhanced charge separation efficiency, which were fabricated via molten-salt flux process. The carbon-supported TiO2 particles were derived from MXene Ti3C2 precursors, and attached on plate-like Bi4NbO8Cl, acting as electron-traps to achieve supressed recombination of photo-induced charges. The improved charge separation confers C-TiO2/Bi4NbO8Cl heterostructures superior photocatalytic performance with 53% higher than pristine Bi4NbO8Cl, towards rhodamine B removal with the help of photo-induced holes. Moreover, the C-TiO2/Bi4NbO8Cl heterostructures can be expanded to deal with other water contaminants, such as methyl orange, ciprofloxacin and 2,4-dichlorophenol with 44, 25 and 13% promotion, respectively, and thus the study offers a series of efficient photocatalysts for water purification.

scholarly journals Cytocompatibility of stabilized black phosphorus nanosheets tailored by directly conjugated polymeric micelles for human breast cancer therapy

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
M. Biedulska ◽  
P. Jakóbczyk ◽  
M. Sosnowska ◽  
B. Dec ◽  
A. Muchlińska ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Polymeric Micelles ◽  
Black Phosphorus ◽  
Environmental Stability ◽  
Breast Cancer Cell Lines ◽  
The Novel ◽  
Ft Ir ◽  
Dose Dependent ◽  
Aggressive Breast Cancer

AbstractThe novel procedure of few-layer black phosphorus (FLBP) stabilization and functionalisation was here proposed. The cationic polymer PLL and non-ionic PEG have been involved into encapsulation of FLBP to allow sufficient time for further nanofabrication process and overcome environmental degradation. Two different spacer chemistry was designed to bind polymers to tumor-homing peptides. The efficiency of functionalisation was examined by RP-HPLC, microscopic (TEM and SEM) and spectroscopic (FT-IR and Raman) techniques as well supported by ab-initio modelling. The cell and dose dependent cytotoxicity of FLBP and its bioconjugates was evaluated against HB2, MCF-7 and MDA-MB-231 cell lines. Functionalisation allowed not only for improvement of environmental stability, but also enhances therapeutic effect by abolished the cytotoxicity of FLBP against HB2 cell line. Moreover, modification of FLBP with PLL caused increase of selectivity against highly aggressive breast cancer cell lines. Results indicate the future prospect application of black phosphorus nanosheets as nanocarrier, considering its unique features synergistically with conjugated polymeric micelles.

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