Displaying publications 1 - 20 of 28 in total

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  1. Fulltext Synthesis, structural and antioxidant studies of some novel N-ethyl phthalimide esters
    Chidan Kumar CS, Loh WS, Chandraju S, Win YF, Tan WK, Quah CK, et al.
    PLoS One, 2015;10(3):e0119440.
    PMID: 25742494 DOI: 10.1371/journal.pone.0119440
    A series of N-ethyl phthalimide esters 4(a-n) were synthesized and characterized by spectroscopic studies. Further, the molecular structure of majority of compounds were analysed by single crystal X-ray diffraction studies. The X-ray analysis revealed the importance of substituents on the crystal stability and molecular packing. All the synthesized compounds were tested for in vitro antioxidant activity by DPPH radical scavenging, FRAP and CUPRAC methods. Few of them have shown good antioxidant activity.
    Matched MeSH terms: Antioxidants/chemical synthesis*
  2. Fulltext A convenient method for the synthesis of (prop-2-ynyloxy)benzene derivatives via reaction with propargyl bromide, their optimization, scope and biological evaluation
    Batool T, Rasool N, Gull Y, Noreen M, Nasim FU, Yaqoob A, et al.
    PLoS One, 2014;9(12):e115457.
    PMID: 25545159 DOI: 10.1371/journal.pone.0115457
    A highly convenient method has been developed for the synthesis of (prop-2-ynyloxy) benzene and its derivatives. Differently substituted phenol and aniline derivatives were allowed to react with propargyl bromide in the presence of K2CO3 base and acetone as solvent. The compounds were synthesized in good yields (53-85%). Low cost, high yields and easy availability of compounds helped in the synthesis. Electron withdrawing groups favor the formation of stable phenoxide ion thus in turn favors the formation of product while electron donating groups do not favor the reaction. Phenol derivatives gave good yields as compared to that of aniline. As aprotic polar solvents favor SN2 type reactions so acetone provided best solvation for the reactions. K2CO3 was proved to be good for the synthesis. Antibacterial, Antiurease and NO scavenging activity of synthesized compounds were also examined. 4-bromo-2-chloro-1-(prop-2-ynyloxy)benzene 2a was found most active compound against urease enzyme with a percentage inhibition of 82.00±0.09 at 100 µg/mL with IC50 value of 60.2. 2-bromo-4-methyl-1-(prop-2-ynyloxy)benzene 2d was found potent antibacterial against Bacillus subtillus showing excellent inhibitory action with percentage inhibition of 55.67±0.26 at 100 µg/ml wih IC50 value of 79.9. Based on results, it can be concluded that some of the synthesized compounds may have potential antiurease and antibacterial effects against several harmful substances.
    Matched MeSH terms: Antioxidants/chemical synthesis*
  3. Fulltext Gastroprotective activity of ethyl-4-[(3,5-di-tert-butyl-2-hydroxybenzylidene) amino]benzoate against ethanol-induced gastric mucosal ulcer in rats
    Halabi MF, Shakir RM, Bardi DA, Al-Wajeeh NS, Ablat A, Hassandarvish P, et al.
    PLoS One, 2014;9(5):e95908.
    PMID: 24800807 DOI: 10.1371/journal.pone.0095908
    BACKGROUND: The study was carried out to determine the cytotoxic, antioxidant and gastro-protective effect of ethyl-4-[(3,5-di-tert-butyl-2-hydroxybenzylid ene)amino] benzoate (ETHAB) in rats.

    METHODOLOGY/PRINCIPAL FINDINGS: The cytotoxic effect of ETHAB was assessed using a MTT cleavage assay on a WRL68 cell line, while its antioxidant activity was evaluated in vitro. In the anti-ulcer study, rats were divided into six groups. Group 1 and group 2 received 10% Tween 20 (vehicle). Group 3 received 20 mg/kg Omeprazole. Groups 4, 5 and 6 received ETHAB at doses of 5, 10, and 20 mg/kg, respectively. After an hour, group 1 received the vehicle. Groups 2-6 received absolute ethanol to induce gastric mucosal lesions. In the WRL68 cell line, an IC50 of more than 100 µg/mL was observed. ETHAB results showed antioxidant activity in the DPPH, FRAP, nitric oxide and metal chelating assays. There was no acute toxicity even at the highest dosage (1000 mg/kg). Microscopy showed that rats pretreated with ETHAB revealed protection of gastric mucosa as ascertained by significant increases in superoxide dismutase (SOD), pH level, mucus secretion, reduced gastric lesions, malondialdehyde (MDA) level and remarkable flattened gastric mucosa. Histologically, pretreatment with ETHAB resulted in comparatively better gastric protection, due to reduction of submucosal edema with leucocyte infiltration. PAS staining showed increased intensity in uptake of Alcian blue. In terms of immunohistochemistry, ETHAB showed down-expression of Bax proteins and over-expression of Hsp70 proteins.

    CONCLUSION/SIGNIFICANCE: The gastroprotective effect of ETHAB may be attributed to antioxidant activity, increased gastric wall mucus, pH level of gastric contents, SOD activity, decrease in MDA level, ulcer area, flattening of gastric mucosa, reduction of edema and leucocyte infiltration of the submucosal layer, increased PAS staining, up-regulation of Hsp70 protein and suppressed expression of Bax.

    Matched MeSH terms: Antioxidants/chemical synthesis
  4. Fulltext Antioxidant Properties and Gastroprotective Effects of 2-(Ethylthio)Benzohydrazones on Ethanol-Induced Acute Gastric Mucosal Lesions in Rats
    Nazarbahjat N, Kadir FA, Ariffin A, Abdulla MA, Abdullah Z, Yehye WA
    PLoS One, 2016;11(6):e0156022.
    PMID: 27272221 DOI: 10.1371/journal.pone.0156022
    A series of new 2-(ethylthio)benzohydrazone derivatives (1-6) were prepared and characterised by IR, 1H NMR, and 13C NMR spectroscopy and mass spectrometry. The newly prepared compounds were screened for their in vitro antioxidant activities using free radical scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) assays. Among them, most powerful antioxidant, compound 1 has been selected in order to illustrate anti-ulcer effect on ethanol-induced gastric mucosal lesions in rats. Four groups of Sprague Dawley rats were respectively treated with 10% Tween 20 as ulcer control group, 20 mg/kg omeprazole as reference group, 50 mg/kg and 100 mg/kg compound 1 as experimental animals. Macroscopically, ulcer control group showed extensive hemorrhagic lesions of gastric mucosa compared with omeprazole or compound 1. Rats pre-treated with compound 1 showed increased in gastric pH and gastric mucus. Histologically, ulcer control group showed severe damage to gastric mucosa with edema and leucocytes infiltration of submucosal layer. In immunohistochemical analysis, rats which were pre-treated with compound 1 showed up-regulation of HSP70 and down-regulation of Bax proteins. In conclusion, the gastroprotective effect of compound 1 may be due to its antioxidant activity, and/or due to up-regulation of HSP70 and down-regulation of Bax protein in stained tissue section.
    Matched MeSH terms: Antioxidants/chemical synthesis
  5. Fulltext New thiosemicarbazides and 1,2,4-triazolethiones derived from 2-(ethylsulfanyl) benzohydrazide as potent antioxidants
    Nazarbahjat N, Nordin N, Abdullah Z, Abdulla MA, Yehye WA, Halim SN, et al.
    Molecules, 2014;19(8):11520-37.
    PMID: 25093989 DOI: 10.3390/molecules190811520
    New thiosemicarbazide derivatives 2-6 were synthesised by reacting 2-(ethylsulfanyl)benzohydrazide with various aryl isothiocyanates. The cyclisation of compounds 2-6 under reflux conditions in a basic medium (aqueous NaOH, 4 N) yielded compounds 7-11 that contain a 1,2,4-triazole ring. All of the synthesised compounds were screened for their antioxidant activities. Compounds 2, 3, and 7 showed better radical scavenging in a 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, with IC50 values of 1.08, 0.22, and 0.74 µg/mL, respectively, compared to gallic acid (IC50, 1.2 µg/mL). Compound 3 also showed superior results in a ferric reducing antioxidant power (FRAP) assay (3054 µM/100 g) compared to those of ascorbic acid (1207 µM/100 g).
    Matched MeSH terms: Antioxidants/chemical synthesis*
  6. Fulltext Synthesis of new 2,5-di-substituted 1,3,4-oxadiazoles bearing 2,6-di-tert-butylphenol moieties and evaluation of their antioxidant activity
    Shakir RM, Ariffin A, Abdulla MA
    Molecules, 2014;19(3):3436-49.
    PMID: 24658568 DOI: 10.3390/molecules19033436
    Eleven new 2,6-di-tert-butyl-4-(5-aryl-1,3,4-oxadiazol-2-yl)phenols 5a-k were synthesized by reacting aryl hydrazides with 3,5-di-tert butyl 4-hydroxybenzoic acid in the presence of phosphorus oxychloride. The resulting compounds were characterized based on their IR, ¹H-NMR, ¹³C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to test the antioxidant properties of the compounds. Compounds 5f and 5j exhibited significant free-radical scavenging ability in both assays.
    Matched MeSH terms: Antioxidants/chemical synthesis*
  7. Fulltext Heteroaryl chalcones: design, synthesis, X-ray crystal structures and biological evaluation
    Kumar CS, Loh WS, Ooi CW, Quah CK, Fun HK
    Molecules, 2013 Oct 15;18(10):12707-24.
    PMID: 24132195 DOI: 10.3390/molecules181012707
    Chalcone derivatives have attracted increasing attention due to their numerous pharmacological activities. Changes in their structures have displayed high degree of diversity that has proven to result in a broad spectrum of biological activities. The present study highlights the synthesis of some halogen substituted chalcones 3(a-i) containing the 5-chlorothiophene moiety, their X-ray crystal structures and the evaluation of possible biological activities such as antibacterial, antifungal and reducing power abilities. The results indicate the tested compounds show a varied range of inhibition values against all the tested microbial strains. Compound 3c with a p-fluoro substituent on the phenyl ring exhibits elevated antimicrobial activity, whereas the compounds 3e and 3f displayed the least antimicrobial activities. The compounds 3d, 3e, 3f and 3i showed good ferric and cupric reducing abilities, and the compounds 3b and 3c showed the weakest reducing power in the series.
    Matched MeSH terms: Antioxidants/chemical synthesis
  8. Fulltext Antimicrobial and antioxidant activities of new metal complexes derived from 3-aminocoumarin
    Kadhum AA, Mohamad AB, Al-Amiery AA, Takriff MS
    Molecules, 2011 Aug 15;16(8):6969-84.
    PMID: 21844844 DOI: 10.3390/molecules16086969
    3-Aminocoumarin (L) has been synthesized and used as a ligand for the formation of Cr(III), Ni(II), and Cu(II) complexes. The chemical structures were characterized using different spectroscopic methods. The elemental analyses revealed that the complexes where M=Ni(II) and Cu(II) have the general formulae [ML(2)Cl(2)], while the Cr(III) complex has the formula [CrL(2)Cl(2)]Cl. The molar conductance data reveal that all the metal chelates, except the Cr(III) one, are non-electrolytes. From the magnetic and UV-Visible spectra, it is found that these complexes have octahedral structures. The stability for the prepared complexes was studied theoretically using Density Function Theory. The total energy for the complexes was calculated and it was shown that the copper complex is the most stable one. Complexes were tested against selected types of microbial organisms and showed significant activities. The free radical scavenging activity of metal complexes have been determined by measuring their interaction with the stable free radical DPPH and all the compounds have shown encouraging antioxidant activities.
    Matched MeSH terms: Antioxidants/chemical synthesis*
  9. Fulltext Conjugated Oligo-Aromatic Compounds Bearing a 3,4,5-Trimethoxy Moiety: Investigation of Their Antioxidant Activity Correlated with a DFT Study
    Kareem HS, Nordin N, Heidelberg T, Abdul-Aziz A, Ariffin A
    Molecules, 2016 Feb 17;21(2).
    PMID: 26901175 DOI: 10.3390/molecules21020224
    A series of heterocyclic compounds bearing the well-known free radical scavenging 3,4,5-trimethoxybenzyloxy group, was synthesized. The key compound 4-(3,4,5-trimethoxybenzyl-oxy)benzohydrazide was converted into thiosemicarbazide derivatives, which were subsequently cyclized with NaOH to provide 1,2,4-triazole derivatives. Alternative treatment of the acid hydrazide with carbon disulfide in the presence of KOH led to the corresponding 1,3,4-oxadiazole and various alkylated derivatives. The newly synthesized compounds were purified and the structures of the products were elucidated and confirmed on the basis of their analytical and spectral data. Their antioxidant activities were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH(•)) and Ferric Reducing Antioxidant Power (FRAP) assays. The thiosemicarbazide derivatives were highly active in both antioxidant assays with the lowest IC50 value for DPPH radical scavenging. Theoretical calculations based on density functional theory (DFT) were performed to understand the relative importance of NH, SH and CH hydrogens on the radical scavenging activities of these compounds.
    Matched MeSH terms: Antioxidants/chemical synthesis*
  10. Fulltext Coumarins as Potential Antioxidant Agents Complemented with Suggested Mechanisms and Approved by Molecular Modeling Studies
    Al-Majedy YK, Al-Duhaidahawi DL, Al-Azawi KF, Al-Amiery AA, Kadhum AA, Mohamad AB
    Molecules, 2016 Jan 23;21(2):135.
    PMID: 26805811 DOI: 10.3390/molecules21020135
    Syntheses of coumarins, which are a structurally interesting antioxidant activity, was done in this article. The modification of 7-hydroxycoumarin by different reaction steps was done to yield target compounds. Molecular structures were characterized by different spectroscopical techniques (Fourier transformation infrared and nuclear magnetic resonance). Antioxidant activities were performed by using various in vitro spectrophometric assays against 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and hydrogen peroxide (H2O2). All compounds exhibited high efficiency as antioxidants compared to ascorbic acid. The highest efficiency scavenging activity was found for compound 3 (91.0 ± 5.0), followed by compounds 2 and 4 (88.0 ± 2.00; and 87.0 ± 3.00). Ascorbic acid C was used as a standard drug with a percentage inhibition of 91.00 ± 1.5. The mechanism of the synthesized compounds as antioxidants was also studied. Hartree-Fock-based quantum chemical studies have been carried out with the basis set to 3-21G, in order to obtain information about the three-dimensional (3D) geometries, electronic structure, molecular modeling, and electronic levels, namely HOMO (highest occupied molecular orbital) and LUMO (lowest unoccupied molecular orbital), to understand the antioxidant activity for the synthesized compounds.
    Matched MeSH terms: Antioxidants/chemical synthesis*
  11. Fulltext Rational Design and Synthesis of New, High Efficiency, Multipotent Schiff Base-1,2,4-triazole Antioxidants Bearing Butylated Hydroxytoluene Moieties
    Yehye WA, Abdul Rahman N, Saad O, Ariffin A, Abd Hamid SB, Alhadi AA, et al.
    Molecules, 2016 Jun 28;21(7).
    PMID: 27367658 DOI: 10.3390/molecules21070847
    A new series of multipotent antioxidants (MPAOs), namely Schiff base-1,2,4-triazoles attached to the oxygen-derived free radical scavenging moiety butylated hydroxytoluene (BHT) were designed and subsequently synthesized. The structure-activity relationship (SAR) of the designed antioxidants was established alongside the prediction of activity spectra for substances (PASS). The antioxidant activities of the synthesized compounds 4-10 were tested by the DPPH bioassay. The synthesized compounds 4-10 inhibited stable DPPH free radicals at a level that is 10(-4) M more than the well-known standard antioxidant BHT. Compounds 8-10 with para-substituents were less active than compounds 4 and 5 with trimethoxy substituents compared to those with a second BHT moiety (compounds 6 and 7). With an IC50 of 46.13 ± 0.31 µM, compound 6 exhibited the most promising in vitro inhibition at 89%. Therefore, novel MPAOs containing active triazole rings, thioethers, Schiff bases, and BHT moieties are suggested as potential antioxidants for inhibiting oxidative stress processes and scavenging free radicals, hence, this combination of functions is anticipated to play a vital role in repairing cellular damage, preventing various human diseases and in medical therapeutic applications.
    Matched MeSH terms: Antioxidants/chemical synthesis
  12. Fulltext Benzofuranyl Esters: Synthesis, Crystal Structure Determination, Antimicrobial and Antioxidant Activities
    Kumar CS, Then LY, Chia TS, Chandraju S, Win YF, Sulaiman SF, et al.
    Molecules, 2015 Sep 11;20(9):16566-81.
    PMID: 26378514 DOI: 10.3390/molecules200916566
    A series of five new 2-(1-benzofuran-2-yl)-2-oxoethyl 4-(un/substituted)benzoates 4(a-e), with the general formula of C₈H₅O(C=O)CH₂O(C=O)C₆H₄X, X = H, Cl, CH₃, OCH₃ or NO₂, was synthesized in high purity and good yield under mild conditions. The synthesized products 4(a-e) were characterized by FTIR, ¹H-, (13)C- and ¹H-(13)C HMQC NMR spectroscopic analysis and their 3D structures were confirmed by single-crystal X-ray diffraction studies. These compounds were screened for their antimicrobial and antioxidant activities. The tested compounds showed antimicrobial ability in the order of 4b < 4a < 4c < 4d < 4e and the highest potency with minimum inhibition concentration (MIC) value of 125 µg/mL was observed for 4e. The results of antioxidant activities revealed the highest activity for compound 4e (32.62% ± 1.34%) in diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, 4d (31.01% ± 4.35%) in ferric reducing antioxidant power (FRAP) assay and 4a (27.11% ± 1.06%) in metal chelating (MC) activity.
    Matched MeSH terms: Antioxidants/chemical synthesis*
  13. Manganese disulfide-silicon dioxide nano-material: Synthesis, characterization, photocatalytic, antioxidant and antimicrobial studies
    Ashraf MA, Peng WX, Fakhri A, Hosseini M, Kamyab H, Chelliapan S
    J. Photochem. Photobiol. B, Biol., 2019 Sep;198:111579.
    PMID: 31401316 DOI: 10.1016/j.jphotobiol.2019.111579
    The sol-gel/ultrasonically rout produced the novel MnS2-SiO2 nano-hetero-photocatalysts with the various ratio of MnS2. Prepared nano-catalyst were investigated in the photo-degradation of methylene blue under UV light illumination. Structural and optical attributes of as-prepared nano-catalysts were evaluated by X-ray diffraction and photoelectron spectroscopy. The morphological were studied by scanning electron microscopy-EDS, and dynamic light scattering. The diffuse reflectance spectroscopy was applied to examine the band gap energy. The Eg values of SiO2, MnS2-SiO2-0, MnS2-SiO2-1, and MnS2-SiO2-2 nanocomposites are 6.51, 3.85, 3.17, and 2.67 eV, respectively. The particle size of the SiO2 and MnS2-SiO2-1 nanocomposites were 100.0, and 65.0 nm, respectively. The crystallite size values of MnS2-SiO2-1 were 52.21 nm, and 2.9 eV, respectively. MnS2-SiO2 nano-photocatalyst was recognized as the optimum sample by degrading 96.1% of methylene blue from water. Moreover, the influence of pH of the solution, and contact time as decisive factors on the photo-degradation activity were investigated in this project. The optimum data for pH and time were found 9 and 60 min, respectively. The photo-degradation capacity of MnS2-SiO2-2 is improved (96.1%) due to the low band gap was found from UV-vis DRS. The antimicrobial data of MnS2-SiO2 were studied and demonstrated that the MnS2-SiO2 has fungicidal and bactericidal attributes.
    Matched MeSH terms: Antioxidants/chemical synthesis
  14. Fulltext The antioxidant activity of new coumarin derivatives
    Kadhum AA, Al-Amiery AA, Musa AY, Mohamad AB
    Int J Mol Sci, 2011;12(9):5747-61.
    PMID: 22016624 DOI: 10.3390/ijms12095747
    The antioxidant activity of two synthesized coumarins namely, N-(4,7-dioxo-2- phenyl-1,3-oxazepin-3(2H,4H,7H)-yl)-2-(2-oxo-2H-chromen-4-yloxy)acetamide 5 and N-(4-oxo-2-phenylthiazolidin-3-yl)-2-(2-oxo-2H-chromen-4-yloxy)acetamide 6 were studied with the DPPH, hydrogen peroxide and nitric oxide radical methods and compared with the known antioxidant ascorbic acid. Compounds 5 and 6 were synthesized in a good yield from the addition reaction of maleic anhydride or mercaptoacetic acid to compound 4, namely N'-benzylidene-2-(2-oxo-2H-chromen-4-yloxy)acetohydrazide. Compound 4 was synthesized by the condensation of compound 3, namely 2-(2-oxo-2H-chromen-4-yloxy) acetohydrazide, with benzaldehyde. Compound 3, however, was synthesized from the addition of hydrazine to compound 2, namely ethyl 2-(2-oxo-2H-chromen-4-yloxy)acetate, which was synthesized from the reaction of ethyl bromoacetate with 4-hydroxycoumarin 1. Structures for the synthesized coumarins 2-6 are proposed on the basis of spectroscopic evidence.
    Matched MeSH terms: Antioxidants/chemical synthesis*
  15. Fulltext In vitro antioxidant and in vivo antidepressant activity of green synthesized azomethine derivatives of cinnamaldehyde
    Chigurupati S, Shaikh SA, Mohammad JI, Selvarajan KK, Nemala AR, Khaw CH, et al.
    Indian J Pharmacol, 2017 10 17;49(3):229-235.
    PMID: 29033482 DOI: 10.4103/ijp.IJP_293_16
    OBJECTIVES: In this study, three (CS-1 to CS-3) azomethine derivatives of cinnamaldehyde were green synthesized, characterized, and their antioxidant and antidepressant activities were explored.

    MATERIALS AND METHODS: The antioxidant effect of these compounds was initially performed in vitro using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay methods before subjecting them to in vivo experiments. Compounds showing potent antioxidant activity (CS-1 and CS-2) were investigated further for their antidepressant activity using the forced swim test (FST) and tail suspension test (TST). Ascorbic acid (AA) and fluoxetine (20 mg/kg, p.o) were used as reference drugs for comparison in the antioxidant and antidepressant experiments, respectively.

    RESULTS: It was observed that CS-2 and CS-3 exhibited highest DPPH (half maximal inhibitory concentration [IC50]: 16.22 and 25.18 μg/mL) and ABTS (IC50: 17.2 and 28.86 μg/mL) radical scavenging activity, respectively, compared to AA (IC50: 15.73 and 16.79 μg/mL) and therefore, both CS-2 and CS-3 were tested for their antidepressant effect using FST and TST as experimental models. Pretreatment of CS-2 and CS-3 (20 mg/kg) for 10 days considerably decreased the immobility time in both the FST and TST models.

    CONCLUSION: The antioxidant and antidepressant effect of CS-2 and CS-3 may be attributed to the presence of azomethine linkage in the molecule.

    Matched MeSH terms: Antioxidants/chemical synthesis*
  16. Fulltext Autoclave-assisted synthesis of AgNPs in Z. officinale extract and assessment of their cytotoxicity, antibacterial and antioxidant activities
    Kalantari K, Afifi AM, Moniri M, Moghaddam AB, Kalantari A, Izadiyan Z
    IET Nanobiotechnol, 2019 May;13(3):262-268.
    PMID: 31053688 DOI: 10.1049/iet-nbt.2018.5066
    In this study, the authors synthesised silver nanoparticles (AgNPs) using autoclave as a simple, unique and eco-friendly approach. The effect of Zingiber officinale extract was evaluated as a reducing and stabiliser agent. According to transmission electron microscopy results, the AgNPs were in the spherical shape with a particle size of ∼17 nm. The biomedical properties of AgNPs as antibacterial agents and free radical scavenging activity were estimated. Synthesised AgNPs showed significant 1,1-diphenyl-2-picryl-hydrazyl free radical scavenging. Strong bactericidal activity was shown by the AgNPs on Gram-positive and Gram-negative bacteria. A maximum inhibition zone of ∼14 mm was obtained for epidermidis at a concentration of 60 μg/ml for sample fabricated at 24 h. The AgNPs also showed a significant cytotoxic effect against MCF-7 breast cancer cell lines with an half maximal inhibitory concentration value of 62 μg/ml in 24 h by the MTT assay. It could be concluded that Z. officinale extract can be used effectively in the production of potential antioxidant and antimicrobial AgNPs for commercial application.
    Matched MeSH terms: Antioxidants/chemical synthesis*
  17. An overview of structure-activity relationship studies of curcumin analogs as antioxidant and anti-inflammatory agents
    Arshad L, Haque MA, Abbas Bukhari SN, Jantan I
    Future Med Chem, 2017 04;9(6):605-626.
    PMID: 28394628 DOI: 10.4155/fmc-2016-0223
    Curcumin, extracted mainly from Curcuma longa rhizomes, has been reported to possess potent anti-inflammatory and anti-oxidant activities. Although safe at higher doses and exhibiting multiple biological activities, curcumin still has the problem of poor bioavailability which has been an attractive area of research over the last few years. A number of efforts have been made by modifying structural features of curcumin. This review highlights the structurally modified and more stable newly synthesized curcumin analogs that have been screened against antioxidant and anti-inflammatory activities. Also the structure-activity relationship to gain insight into future guidelines for scheming new compounds has been discussed, and further these analogs being more stable may serve as promising agents for use in different pathological conditions.
    Matched MeSH terms: Antioxidants/chemical synthesis
  18. Colloidal astaxanthin: preparation, characterisation and bioavailability evaluation
    Anarjan N, Tan CP, Nehdi IA, Ling TC
    Food Chem, 2012 Dec 1;135(3):1303-9.
    PMID: 22953858 DOI: 10.1016/j.foodchem.2012.05.091
    Astaxanthin colloidal particles were produced using solvent-diffusion technique in the presence of different food grade surface active compounds, namely, Polysorbate 20 (PS20), sodium caseinate (SC), gum Arabic (GA) and the optimum combination of them (OPT). Particle size and surface charge characteristics, rheological behaviour, chemical stability, colour, in vitro cellular uptake, in vitro antioxidant activity and residual solvent concentration of prepared colloidal particles were evaluated. The results indicated that in most cases the mixture of surface active compounds lead to production of colloidal particles with more desirable physicochemical and biological properties, as compared to using them individually. The optimum combination of PS20, SC and GA could produce the astaxanthin colloidal particles with small particle size, polydispersity index (PDI), conductivity and higher zeta potential, mobility, cellular uptake, colour intensity and in vitro antioxidant activity. In addition, all prepared astaxanthin colloidal particles had significantly (p<0.05) higher cellular uptake than pure astaxanthin powder.
    Matched MeSH terms: Antioxidants/chemical synthesis
  19. PASS-assisted design, synthesis and antioxidant evaluation of new butylated hydroxytoluene derivatives
    Ariffin A, Rahman NA, Yehye WA, Alhadi AA, Kadir FA
    Eur J Med Chem, 2014 Nov 24;87:564-77.
    PMID: 25299680 DOI: 10.1016/j.ejmech.2014.10.001
    New multipotent antioxidants (MPAOs), namely 1,3,4-thiadiazoles and 1,2,4-triazoles bearing the well-known free radical scavenger butylated hydroxytoluene (BHT), were designed and synthesized using an acid-(base-) catalyzed intramolecular dehydrative cyclization reaction of the corresponding 1-acylthiosemicarbazides. The structure-activity relationship (SAR) of the designed antioxidants was performed along with the prediction of activity spectra for substances (PASS) training set. Experimental studies based on antioxidant activity using DPPH and lipid peroxidation assays verified the predictions obtained by the PASS-assisted design strategy. Compounds 4a-b, 5a-b and 6a-b showed an inhibition of stable DPPH free radicals at a 10(-4) M more than the well-known standard antioxidant BHT. Compounds with p-methoxy substituents (4b, 5b and 6b) were more active than o-methoxy substituents (4a, 5a and 6a). With an IC50 of 2.85 ± 1.09 μM, compound 6b exhibited the most promising in vitro inhibition of lipid peroxidation, inhibiting Fe(2+)-induced lipid peroxidation of essential oils derived from the egg yolk-based lipid-rich medium by 86.4%. The parameters for the drug-likeness of these BHT derivatives were also evaluated according to Lipinski's 'rule-of-five'. All of the BHT derivatives were found to violate one of Lipinski's parameters (Log P ≥ 5) even though they have been found to be soluble in protic solvents. The predictive TPSA and %ABS data allow for the conclusion that these compounds could have a good capacity for penetrating cell membranes. Therefore, these novel MPAOs containing lipophilic and hydrophilic groups can be proposed as potential antioxidants for tackling oxidative stress and lipid peroxidation processes.
    Matched MeSH terms: Antioxidants/chemical synthesis
  20. Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities
    Taha M, Ismail NH, Jamil W, Rashwan H, Kashif SM, Sain AA, et al.
    Eur J Med Chem, 2014 Sep 12;84:731-8.
    PMID: 25069019 DOI: 10.1016/j.ejmech.2014.07.078
    4-Methylbenzimidazole 1-28 novel derivatives were synthesized and evaluated for their antiglycation and antioxidant activities. Compounds 1-7 and 11 showed excellent activities ranged 140-280 μM, better than standard drug rutin (294.46 ± 1.50 μM). Compound 1-28 were also evaluated for DPPH activities. Compounds 1-8 showed excellent activities, ranging 12-29 μM, better than standard drug n-propylgallate (IC50 = 30.30 ± 0.40 μM). For superoxide anion scavenging activity, compounds 1-7 showed better activity than standard n-propylgallate (IC50 = 106.34 ± 1.6 μM), ranged 82-104 μM. These compounds were found to be nontoxic to THP-1 cells.
    Matched MeSH terms: Antioxidants/chemical synthesis*
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