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  1. Characterization of polymeric micelles for pulmonary delivery of beclomethasone dipropionate
    Gaber NN, Darwis Y, Peh KK, Tan YT
    J Nanosci Nanotechnol, 2006 10 20;6(9-10):3095-101.
    PMID: 17048523
    The potential of using poly-(ethylene oxide)-block-distearoyl phosphatidyl-ethanolamine (mPEG-DSPE) polymer to prepare BDP-loaded micelles with high entrapment efficiency and mass median aerodynamic diameter of less than 5 microm demonstrating sustained release properties was evaluated. The result showed that lyophilized BDP-loaded polymeric micelles with entrapment efficiency of more than 96% could be achieved. Entrapment efficiency was affected by both the drug to polymer molar ratio and the amount of drug used. Investigation using FTIR and DSC confirmed that there was no chemical or physical interaction and the drug was molecularly dispersed within the micelles. TEM images showed that the drug-loaded polymeric micelles were spherical in shape with multivesicular morphology. Further analysis by photon correlation spectroscopy indicated that the particle size of the BDP-loaded micelles was about 22 nm in size. In vitro drug release showed a promising sustained release profile over six days following the Higuchi model. The mass median aerodynamic diameter and fine particle fraction were suitable for pulmonary delivery. Moreover, the small amount of deposited drug in the induction port (throat deposition) suggested possible reduction in incidence of oropharyngeal candidiasis, a side effect normally associated with inhaled corticosteroids therapy. The high encapsulation efficiency, comparable inhalation properties, sustained release behavior together with biocompatibility nature of the polymer support the potential of BDP-loaded polymeric micelles as a versatile delivery system to be used in the treatment of asthma and chronic obstructive pulmonary disease.
    Matched MeSH terms: Aerosols/chemistry; Beclomethasone/chemistry*; Colloids/chemistry*; Drug Carriers/chemistry*; Nanostructures/chemistry*
  2. A facile approach to prepare regenerated cellulose/graphene nanoplatelets nanocomposite using room-temperature ionic liquid
    Mahmoudian S, Wahit MU, Imran M, Ismail AF, Balakrishnan H
    J Nanosci Nanotechnol, 2012 Jul;12(7):5233-9.
    PMID: 22966551
    This study presents the preparation of regenerated cellulose (RC)/graphene nanoplatelets (GNPs) nanocomposites via room temperature ionic liquid, 1-ethyl-3-methylimidazolium acetate (EMIMAc) using solution casting method. The thermal stability, gas permeability, water absorption and mechanical properties of the films were studied. The synthesized nanocomposite films were characterized by Fourier transform infrared (FTIR), X-ray diffraction (XRD) and scanning electron microscopy (SEM). The T20 decomposition temperature of regenerated cellulose improved with the addition of graphene nanoplatelets up to 5 wt%. The tensile strength and Young's modulus of RC films improved by 34 and 56%, respectively with the addition of 3 wt% GNPs. The nanocomposite films exhibited improved oxygen and carbon dioxide gas barrier properties and water absorption resistance compared to RC. XRD and SEM results showed good interaction between RC and GNPs and well dispersion of graphene nanoplatelets in regenerated cellulose. The FTIR spectra showed that the addition of GNPs in RC did not result in any noticeable change in its chemical structure.
    Matched MeSH terms: Cellulose/chemistry*; Graphite/chemistry*; Macromolecular Substances/chemistry; Nanostructures/chemistry*; Ionic Liquids/chemistry*
  3. Observation of a cubical-like microstructure of strontium iron garnet and yttrium iron garnet prepared via sol-gel technique
    Nasir N, Yahya N, Kashif M, Daud H, Akhtar MN, Zaid HM, et al.
    J Nanosci Nanotechnol, 2011 Mar;11(3):2551-4.
    PMID: 21449424
    This is our initial response towards preparation of nano-inductors garnet for high operating frequencies strontium iron garnet (Sr3Fe5O12) denoted as SrIG and yttrium iron garnet (Y3Fe5O12) denoted as YIG. The garnet nano crystals were prepared by novel sol-gel technique. The phase and crystal structure of the prepared samples were identified by using X-ray diffraction analysis. SEM images were done to reveal the surface morphology of the samples. Raman spectra was taken for yttrium iron garnet (Y3Fe5O12). The magnetic properties of the samples namely initial permeability (micro), relative loss factor (RLF) and quality factor (Q-Factor) were done by using LCR meter. From the XRD profile, both of the Y3Fe5O12 and Sr3Fe5O12 samples showed single phase garnet and crystallization had completely occurred at 900 degrees C for the SrIG and 950 degrees C for the YIG samples. The YIG sample showed extremely low RLF value (0.0082) and high density 4.623 g/cm3. Interesting however is the high Q factor (20-60) shown by the Sr3Fe5O12 sample from 20-100 MHz. This high performance magnetic property is attributed to the homogenous and cubical-like microstructure. The YIG particles were used as magnetic feeder for EM transmitter. It was observed that YIG magnetic feeder with the EM transmitter gave 39% higher magnetic field than without YIG magnetic feeder.
    Matched MeSH terms: Iron/chemistry*; Strontium/chemistry*; Yttrium/chemistry*; Macromolecular Substances/chemistry; Nanostructures/chemistry*
  4. Characterization of alcohol/salt aqueous two-phase system for optimal separation of gallic acids
    Ng HS, Kee PE, Yim HS, Tan JS, Chow YH, Lan JC
    J Biosci Bioeng, 2021 May;131(5):537-542.
    PMID: 33674222 DOI: 10.1016/j.jbiosc.2021.01.004
    Gallic acid (GA) is a hydrophilic polyphenol which is noteworthy for strong antioxidant capacity. The drawbacks of conventional extraction approaches such as time-consuming and high processing cost are often viewed as a hurdle to extract GA from plant sources in industrial scale. Aqueous two-phase system (ATPS) is a separation approach which can be employed as an alternative to the conventional approaches. The partition behaviour of GA in an alcohol/salt ATPS was investigated in this study to aid the development of industrial scale ATPS to extract GA from natural sources. The separation of GA was characterized by determining the types of alcohol and salt, phase composition, sample load, pH of the system and addition of adjuvants applied in the alcohol/salt ATPS construction. The hydrophilic GA was targeted to the salt-rich phase of the alcohol/salt ATPS with a partition coefficient (KGA) of 25.00 ± 0.00. The optimum condition of ATPS for the maximum partition of GA was achieved in ATPS comprised of 24% (w/w) 1-propanol and 22% (w/w) phosphate salt at pH 8 with 5% (w/w) of 1 mg/mL sample loading and 2% (w/w) NaCl addition. The findings suggest that ATPS can be applied for separation of GA from various natural sources.
    Matched MeSH terms: Alcohols/chemistry*; Gallic Acid/chemistry; Polyethylene Glycols/chemistry; Salts/chemistry*; Water/chemistry*
  5. Bioseparation of phycocyanin from Phormidium tergestinum using an aqueous two-phase system
    Tan JS, Abbasiliasi S, Lalung J, Tam YJ, Murugan P, Lee CK
    Prep Biochem Biotechnol, 2021;51(3):260-266.
    PMID: 32876520 DOI: 10.1080/10826068.2020.1808793
    This study aimed at purification of phycocyanin (PC) from Phormidium tergestinum using an aqueous two-phase system (ATPS) comprised of polyethylene glycol (PEG) and salts. The partitioning efficiency of PC in ATPS and the effect of phase composition, pH, crude loading, and neutral salts on purification factor and yield were investigated. Results showed that PC was selectively partitioned toward bottom phase of the system containing potassium phosphate. Under optimum conditions of 20% (w/w) PEG 4000, 10% (w/w) potassium phosphate, 20% (v/v) crude load at pH 7, with addition of 0.5% (w/w) NaCl, PC from P. tergestinum was partially purified up to 5.34-fold with a yield of 87.8%. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis showed that the molecular weight of PC was ∼19 kDa. Results from this study demonstrated ATPS could be used as a potential approach for the purification of PC from P. tergestinum.
    Matched MeSH terms: Phosphates/chemistry; Phycocyanin/chemistry*; Polyethylene Glycols/chemistry; Water/chemistry; Potassium Compounds/chemistry
  6. Dissipation of acephate, chlorpyrifos, cypermethrin and their metabolites in a humid-tropical vegetable production system
    Chai LK, Mohd-Tahir N, Bruun Hansen HC
    Pest Manag Sci, 2009 Feb;65(2):189-96.
    PMID: 18979521 DOI: 10.1002/ps.1667
    High amounts of insecticides are often used in intensive tropical vegetable production systems. Their persistence and residues in vegetables and soils need to be studied to ensure food safety and environmental stability. The dissipation of acephate, chlorpyrifos, cypermethrin and their metabolites was studied in green mustard [Brassica juncea (L.) Coss.] and soils. Two treatments, Impact 75 (acephate) and Agent 505 (cypermethrin plus chlorpyrifos), were applied 4 times at weekly intervals.
    Matched MeSH terms: Chlorpyrifos/chemistry; Mustard Plant/chemistry*; Organothiophosphorus Compounds/chemistry; Pesticide Residues/chemistry; Pyrethrins/chemistry
  7. Chemical investigation and biological activities of the essential oil of Knema kunstleri Warb. from Malaysia
    Salleh WMNHW, Anuar MZA, Khamis S, Nafiah MA, Sul'ain MD
    Nat Prod Res, 2021 Jul;35(13):2279-2284.
    PMID: 31544509 DOI: 10.1080/14786419.2019.1669027
    The chemical composition of the essential oil of Knema kunstleri Warb. (Myristicaceae) was investigated for the first time. The essential oil was obtained by hydrodistillation and fully characterized by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). In total, 36 components were identified in the essential oil, which made up 91.7% of the total oil. The essential oil is composed mainly of β-caryophyllene (23.2%), bicyclogermacrene (9.6%), δ-cadinene (7.3%), α-humulene (5.7%), and germacrene D (4.3%). The essential oil showed moderate activity towards DPPH free-radical scavenging and lipoxygenase inhibition. To the best of our knowledge, this is the first study of the composition and bioactivities of the essential oil report concerning the genus Knema.
    Matched MeSH terms: Biphenyl Compounds/chemistry; Oils, Volatile/chemistry; Picrates/chemistry; Free Radical Scavengers/chemistry; Myristicaceae/chemistry*
  8. Fulltext Accelerated Solvent Extractions (ASE) of Mitragyna speciosa Korth. (Kratom) Leaves: Evaluation of Its Cytotoxicity and Antinociceptive Activity
    Goh YS, Karunakaran T, Murugaiyah V, Santhanam R, Abu Bakar MH, Ramanathan S
    Molecules, 2021 Jun 17;26(12).
    PMID: 34204457 DOI: 10.3390/molecules26123704
    Mitragyna speciosa Korth (kratom) is known for its psychoactive and analgesic properties. Mitragynine is the primary constituent present in kratom leaves. This study highlights the utilisation of the green accelerated solvent extraction technique to produce a better, non-toxic and antinociceptive active botanical extract of kratom. ASE M. speciosa extract had a dry yield (0.53-2.91 g) and showed a constant mitragynine content (6.53-7.19%) when extracted with organic solvents of different polarities. It only requires a shorter extraction time (5 min) and a reduced amount of solvents (less than 100 mL). A substantial amount of total phenolic (407.83 ± 2.50 GAE mg/g and flavonoids (194.00 ± 5.00 QE mg/g) were found in ASE kratom ethanol extract. The MTT test indicated that the ASE kratom ethanolic leaf extract is non-cytotoxic towards HEK-293 and HeLa Chang liver cells. In mice, ASE kratom ethanolic extract (200 mg/kg) demonstrated a better antinociceptive effect compared to methanol and ethyl acetate leaf extracts. The presence of bioactive indole alkaloids and flavonols such as mitragynine, paynantheine, quercetin, and rutin in ASE kratom ethanolic leaf extract was detected using UHPLC-ESI-QTOF-MS/MS analysis supports its antinociceptive properties. ASE ethanolic leaf extract offers a better, safe, and cost-effective choice of test botanical extract for further preclinical studies.
    Matched MeSH terms: Plant Extracts/chemistry*; Solvents/chemistry; Plant Leaves/chemistry; Mitragyna/chemistry*; Secologanin Tryptamine Alkaloids/chemistry
  9. Fulltext Plant-Based Biosynthesis of Copper/Copper Oxide Nanoparticles: An Update on Their Applications in Biomedicine, Mechanisms, and Toxicity
    Letchumanan D, Sok SPM, Ibrahim S, Nagoor NH, Arshad NM
    Biomolecules, 2021 04 12;11(4).
    PMID: 33921379 DOI: 10.3390/biom11040564
    Plants are rich in phytoconstituent biomolecules that served as a good source of medicine. More recently, they have been employed in synthesizing metal/metal oxide nanoparticles (NPs) due to their capping and reducing properties. This green synthesis approach is environmentally friendly and allows the production of the desired NPs in different sizes and shapes by manipulating parameters during the synthesis process. The most commonly used metals and oxides are gold (Au), silver (Ag), and copper (Cu). Among these, Cu is a relatively low-cost metal that is more cost-effective than Au and Ag. In this review, we present an overview and current update of plant-mediated Cu/copper oxide (CuO) NPs, including their synthesis, medicinal applications, and mechanisms. Furthermore, the toxic effects of these NPs and their efficacy compared to commercial NPs are reviewed. This review provides an insight into the potential of developing plant-based Cu/CuO NPs as a therapeutic agent for various diseases in the future.
    Matched MeSH terms: Copper/chemistry*; Metal Nanoparticles/chemistry*; Green Chemistry Technology/methods; Phytochemicals/chemistry
  10. Analytical GC-FID Method for the Determination of Organic Solvents in Radiopharmaceuticals
    Hassan H, Othman MF, Zakaria ZA, Saad FFA, Abdul Razak HR
    Curr Radiopharm, 2021;14(2):131-144.
    PMID: 33115398 DOI: 10.2174/1874471013999201027215704
    BACKGROUND: Organic solvents play an indispensable role in most of the radiopharmaceutical production stages. It is almost impossible to remove them entirely in the final formulation of the product.

    OBJECTIVE: In this presented work, an analytical method by gas chromatography coupled with flame ionization detection (GC-FID) has been developed to determine organic solvents in radiopharmaceutical samples. The effect of injection holding time, temperature variation in the injection port, and the column temperature on the analysis time and resolution (R ≥ 1.5) of ethanol and acetonitrile was studied extensively.

    METHODS: The experimental conditions were optimized with the aid of further statistical analysis; thence, the proposed method was validated following the International Council for Harmonisation (ICH) Q2 (R1) guideline.

    RESULTS: The proposed analytical method surpassed the acceptance criteria including the linearity > 0.990 (correlation coefficient of R2), precision < 2%, LOD, and LOQ, accuracy > 90% for all solvents. The separation between ethanol and acetonitrile was acceptable with a resolution R > 1.5. Further statistical analysis of Oneway ANOVA revealed that the increment in injection holding time and variation of temperature at the injection port did not significantly affect the analysis time. Nevertheless, the variation in injection port temperature substantially influenced the resolution of ethanol and acetonitrile peaks (p < 0.05).

    CONCLUSION: The proposed analytical method has been successfully implemented to determine the organic solvent in the [18F]fluoro-ethyl-tyrosine ([18F]FET), [18F]fluoromisonidazole ([18F]FMISO), and [18F]fluorothymidine ([18F]FLT).

    Matched MeSH terms: Acetonitriles/chemistry; Ethanol/chemistry; Fluorine Radioisotopes/chemistry*; Solvents/chemistry*; Radiopharmaceuticals/chemistry*
  11. Fulltext Optical and Photoacoustic Properties of Laser-Ablated Silver Nanoparticles in a Carbon Dots Solution
    Sadrolhosseini AR, Krishnan G, Shafie S, Abdul Rashid S, Wadi Harun S
    Molecules, 2020 Dec 09;25(24).
    PMID: 33316885 DOI: 10.3390/molecules25245798
    This study used the carbon dots solution for the laser ablation technique to fabricate silver nanoparticles. The ablation time range was from 5 min to 20 min. Analytical methods, including Fourier transform infrared spectroscopy (FTIR), UV-visible spectroscopy, transmission electron microscopy, and Raman spectroscopy were used to categorize the prepared samples. The UV-visible and z-scan techniques provided optical parameters such as linear and nonlinear refractive indices in the range of 1.56759 to 1.81288 and 7.3769 × 10-10 cm2 W-1 to 9.5269 × 10-10 cm2 W-1 and the nonlinear susceptibility was measured in the range of 5.46 × 10-8 to 6.97 × 10-8 esu. The thermal effusivity of prepared samples, which were measured using the photoacoustic technique, were in the range of 0.0941 W s1/2 cm-2 K-1 to 0.8491 W s1/2 cm-2 K-1. The interaction of the prepared sample with fluoride was investigated using a Raman spectrometer. Consequently, the intensity of the Raman signal decreased with the increasing concentration of fluoride, and the detection limit is about 0.1 ppm.
    Matched MeSH terms: Carbon/chemistry*; Fluorides/chemistry; Silver/chemistry*; Nanocomposites/chemistry*; Metal Nanoparticles/chemistry*
  12. Optimization of Pectin Extraction from Sweet Potato Peels Using Citric Acid and its Emulsifying Properties
    Hamidon NH, Abang Zaidel DN, Mohd Jusoh YM
    Recent Pat Food Nutr Agric, 2020;11(3):202-210.
    PMID: 32031081 DOI: 10.2174/2212798411666200207102051
    BACKGROUND: Pectin is a natural polysaccharide that has been used widely as a stabilizer in food emulsion system.

    OBJECTIVE: This study aimed to optimize the yield of pectin extracted from sweet potato residue and investigate its emulsifying properties.

    METHODS: Response surface methodology (RSM) has been utilized to investigate the pectin extracted from sweet potato peels using citric acid as the extracting solvent. Investigation of the effect of different extraction conditions namely temperature (°C), time (min) and solution pH on pectin yield (%) were conducted. A Box-Benhken design with three levels of variation was used to optimize the extraction conditions.

    RESULTS: The optimal conditions determined were temperature 76°C, time 64 min and pH 1.2 with 65.2% yield of pectin. The degree of esterification (DE) of the sweet potato pectin was determined using Fourier Transform Infrared (FTIR) Spectroscopy. The pectin is high-methoxyl pectin with DE of 58.5%. Emulsifying properties of sweet potato pectin were investigated by measuring the zeta-potential, particle size and creaming index with addition of 0.4 and 1.0 wt % pectin to the emulsion.

    CONCLUSION: Extraction using citric acid could improve the pectin yield. Improved emulsion stability was observed with the addition of the sweet potato pectin.

    Matched MeSH terms: Pectins/chemistry*; Plant Extracts/chemistry*; Citric Acid/chemistry; Ipomoea batatas/chemistry*; Emulsifying Agents/chemistry*
  13. Structural and Biochemical Insights into the Inhibition of Human Acetylcholinesterase by G-Series Nerve Agents and Subsequent Reactivation by HI-6
    McGuire JR, Bester SM, Guelta MA, Cheung J, Langley C, Winemiller MD, et al.
    Chem Res Toxicol, 2021 03 15;34(3):804-816.
    PMID: 33538594 DOI: 10.1021/acs.chemrestox.0c00406
    The recent use of organophosphate nerve agents in Syria, Malaysia, Russia, and the United Kingdom has reinforced the potential threat of their intentional release. These agents act through their ability to inhibit human acetylcholinesterase (hAChE; E.C. 3.1.1.7), an enzyme vital for survival. The toxicity of hAChE inhibition via G-series nerve agents has been demonstrated to vary widely depending on the G-agent used. To gain insight into this issue, the structures of hAChE inhibited by tabun, sarin, cyclosarin, soman, and GP were obtained along with the inhibition kinetics for these agents. Through this information, the role of hAChE active site plasticity in agent selectivity is revealed. With reports indicating that the efficacy of reactivators can vary based on the nerve agent inhibiting hAChE, human recombinatorially expressed hAChE was utilized to define these variations for HI-6 among various G-agents. To identify the structural underpinnings of this phenomenon, the structures of tabun, sarin, and soman-inhibited hAChE in complex with HI-6 were determined. This revealed how the presence of G-agent adducts impacts reactivator access and placement within the active site. These insights will contribute toward a path of next-generation reactivators and an improved understanding of the innate issues with the current reactivators.
    Matched MeSH terms: Nerve Agents/chemistry; Acetylcholinesterase/chemistry; Cholinesterase Inhibitors/chemistry; Oximes/chemistry; Pyridinium Compounds/chemistry
  14. Fulltext Enhanced polyhydroxybutyrate (PHB) production by newly isolated rare actinomycetes Rhodococcus sp. strain BSRT1-1 using response surface methodology
    Trakunjae C, Boondaeng A, Apiwatanapiwat W, Kosugi A, Arai T, Sudesh K, et al.
    Sci Rep, 2021 01 21;11(1):1896.
    PMID: 33479335 DOI: 10.1038/s41598-021-81386-2
    Poly-β-hydroxybutyrate (PHB) is a biodegradable polymer, synthesized as carbon and energy reserve by bacteria and archaea. To the best of our knowledge, this is the first report on PHB production by a rare actinomycete species, Rhodococcus pyridinivorans BSRT1-1. Response surface methodology (RSM) employing central composite design, was applied to enhance PHB production in a flask scale. A maximum yield of 3.6 ± 0.5 g/L in biomass and 43.1 ± 0.5 wt% of dry cell weight (DCW) of PHB were obtained when using RSM optimized medium, which was improved the production of biomass and PHB content by 2.5 and 2.3-fold, respectively. The optimized medium was applied to upscale PHB production in a 10 L stirred-tank bioreactor, maximum biomass of 5.2 ± 0.5 g/L, and PHB content of 46.8 ± 2 wt% DCW were achieved. Furthermore, the FTIR and 1H NMR results confirmed the polymer as PHB. DSC and TGA analysis results revealed the melting, glass transition, and thermal decomposition temperature of 171.8, 4.03, and 288 °C, respectively. In conclusion, RSM can be a promising technique to improve PHB production by a newly isolated strain of R. pyridinivorans BSRT1-1 and the properties of produced PHB possessed similar properties compared to commercial PHB.
    Matched MeSH terms: Carbon/chemistry; Hydroxybutyrates/chemistry*; Polyesters/chemistry*; Polymers/chemistry*; Rhodococcus/chemistry*
  15. Preparation of methacrylamide-functionalized crosslinked chitosan by free radical polymerization for the removal of lead ions
    Sutirman ZA, Sanagi MM, Abd Karim KJ, Wan Ibrahim WA
    Carbohydr Polym, 2016 Oct 20;151:1091-1099.
    PMID: 27474659 DOI: 10.1016/j.carbpol.2016.06.076
    A new poly(methacrylamide) grafted crosslinked chitosan was prepared for removal of lead, Pb(II) ion from aqueous solution. Crosslinked chitosan, in beads form, was grafted with methacrylamide (MAm) using ammonium persulfate (APS) as free radical initiator. Evidence of grafting was determined by comparing FTIR, TGA, SEM and (13)C NMR analyses of chitosan and graft copolymer. The optimal conditions for grafting reaction were as follow: crosslinked chitosan beads (1g), MAm (17.62×10(-1)M), APS (2.63×10(-1)M), reaction time (3h) and temperature (60°C). The modified chitosan bead was then used in laboratory batch experiments to evaluate the removal of Pb(II) ion from water samples. The Langmuir and Freundlich adsorption models were also applied to describe the equilibrium isotherms. The results revealed that the adsorption of Pb(II) ions onto the beads fitted very well with the Langmuir model with the maximum capacity (qmax) of 250mgg(-1).
    Matched MeSH terms: Acrylamides/chemistry*; Free Radicals/chemistry; Lead/chemistry*; Water Pollutants, Chemical/chemistry*; Chitosan/chemistry*
  16. Gambir, "Gambir Sarawak" and toad venom
    Lim WJ, Yap AT, Mangudi M, Hu CY, Yeo CY, Eyo ZW, et al.
    Drug Test Anal, 2017 Mar;9(3):491-499.
    PMID: 27367276 DOI: 10.1002/dta.2034
    Matched MeSH terms: Amphibian Venoms/chemistry*; Plant Extracts/chemistry*; Plants, Medicinal/chemistry; Street Drugs/chemistry; Uncaria/chemistry*
  17. Fulltext Magnetic Properties of Polyvinyl Alcohol and Doxorubicine Loaded Iron Oxide Nanoparticles for Anticancer Drug Delivery Applications
    Nadeem M, Ahmad M, Akhtar MS, Shaari A, Riaz S, Naseem S, et al.
    PLoS One, 2016;11(6):e0158084.
    PMID: 27348436 DOI: 10.1371/journal.pone.0158084
    The current study emphasizes the synthesis of iron oxide nanoparticles (IONPs) and impact of hydrophilic polymer polyvinyl alcohol (PVA) coating concentration as well as anticancer drug doxorubicin (DOX) loading on saturation magnetization for target drug delivery applications. Iron oxide nanoparticles particles were synthesized by a reformed version of the co-precipitation method. The coating of polyvinyl alcohol along with doxorubicin loading was carried out by the physical immobilization method. X-ray diffraction confirmed the magnetite (Fe3O4) structure of particles that remained unchanged before and after polyvinyl alcohol coating and drug loading. Microstructure and morphological analysis was carried out by transmission electron microscopy revealing the formation of nanoparticles with an average size of 10 nm with slight variation after coating and drug loading. Transmission electron microscopy, energy dispersive, and Fourier transform infrared spectra further confirmed the conjugation of polymer and doxorubicin with iron oxide nanoparticles. The room temperature superparamagnetic behavior of polymer-coated and drug-loaded magnetite nanoparticles were studied by vibrating sample magnetometer. The variation in saturation magnetization after coating evaluated that a sufficient amount of polyvinyl alcohol would be 3 wt. % regarding the externally controlled movement of IONPs in blood under the influence of applied magnetic field for in-vivo target drug delivery.
    Matched MeSH terms: Antibiotics, Antineoplastic/chemistry; Doxorubicin/chemistry; Ferric Compounds/chemistry; Polyvinyl Alcohol/chemistry; Magnetite Nanoparticles/chemistry*
  18. Flavonoids-Rich Orthosiphon stamineus Extract as New Candidate for Angiotensin I-Converting Enzyme Inhibition: A Molecular Docking Study
    Shafaei A, Sultan Khan MS, F A Aisha A, Abdul Majid AM, Hamdan MR, Mordi MN, et al.
    Molecules, 2016 Nov 09;21(11).
    PMID: 27834876
    This study aims to evaluate the in vitro angiotensin-converting enzyme (ACE) inhibition activity of different extracts of Orthosiphon stamineus (OS) leaves and their main flavonoids, namely rosmarinic acid (RA), sinensetin (SIN), eupatorin (EUP) and 3'-hydroxy-5,6,7,4'-tetramethoxyflavone (TMF). Furthermore, to identify possible mechanisms of action based on structure-activity relationships and molecular docking. The in vitro ACE inhibition activity relied on determining hippuric acid (HA) formation from ACE-specific substrate (hippuryl-histidyl-leucine (HHL)) by the action of ACE enzyme. A High Performance Liquid Chromatography method combined with UV detection was developed and validated for measurement the concentration of produced HA. The chelation ability of OS extract and its reference compounds was evaluated by tetramethylmurexide reagent. Furthermore, molecular docking study was performed by LeadIT-FlexX: BioSolveIT's LeadIT program. OS ethanolic extract (OS-E) exhibited highest inhibition and lowest IC50 value (45.77 ± 1.17 µg/mL) against ACE compared to the other extracts. Among the tested reference compounds, EUP with IC50 15.35 ± 4.49 µg/mL had highest inhibition against ACE and binding ability with Zn (II) (56.03% ± 1.26%) compared to RA, TMF and SIN. Molecular docking studies also confirmed that flavonoids inhibit ACE via interaction with the zinc ion and this interaction is stabilized by other interactions with amino acids in the active site. In this study, we have demonstrated that changes in flavonoids active core affect their capacity to inhibit ACE. Moreover, we showed that ACE inhibition activity of flavonoids compounds is directly related to their ability to bind with zinc ion in the active site of ACE enzyme. It was also revealed that OS extract contained high amount of flavonoids other than RA, TMF, SIN and EUP. As such, application of OS extract is useful as inhibitors of ACE.
    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors/chemistry*; Flavonoids/chemistry*; Peptidyl-Dipeptidase A/chemistry*; Plant Extracts/chemistry*; Orthosiphon/chemistry*
  19. Selective dual cholinesterase inhibitors from Aconitum laeve
    Ahmad H, Ahmad S, Shah SAA, Khan HU, Khan FA, Ali M, et al.
    J Asian Nat Prod Res, 2018 Feb;20(2):172-181.
    PMID: 28463565 DOI: 10.1080/10286020.2017.1319820
    New lycoctonine-type dual cholinesterase inhibitor, swatinine-C (1), along with three known norditerpenoid alkaloids, hohenackerine (2), aconorine (5) and lappaconitine (6) and two synthetically known but phytochemically new benzene derivatives, methyl 2-acetamidobenzoate (3) and methyl 4-[2-(methoxycarbonyl)anilino]-4-oxobutanoate (4), was isolated from the roots of A. laeve. Structures of new and known compounds (1-6) were established on the basis of latest spectroscopic techniques and by close comparison with the data available in literature. In vitro, compounds (1-6) were tested against AChE and BChE inhibitory activities. Compounds 1 and 2 showed competitive inhibition against AChE (IC50 = 3.7 μM, 4.53 μM) and BChE (IC50 = 12.23 μM, 9.94 μM), respectively. Compounds 5 and 6 showed promising noncompetitive type of inhibitory profile against AChE (IC50 = 2.51 and 6.13 μM) only. Compounds 3 and 4 showed weak inhibitory profile against both AChE and BChE.
    Matched MeSH terms: Aconitine/chemistry; Alkaloids/chemistry; Cholinesterase Inhibitors/chemistry; Plant Roots/chemistry; Aconitum/chemistry*
  20. Near-infrared activatable phthalocyanine-poly-L-glutamic acid conjugate: increased cellular uptake and light-dark toxicity ratio toward an effective photodynamic cancer therapy
    Kiew LV, Cheah HY, Voon SH, Gallon E, Movellan J, Ng KH, et al.
    Nanomedicine, 2017 05;13(4):1447-1458.
    PMID: 28214608 DOI: 10.1016/j.nano.2017.02.002
    In photodynamic therapy (PDT), the low absorptivity of photosensitizers in an aqueous environment reduces singlet oxygen generation efficiency and thereby decreases photosensitizing efficacy in biological conditions. To circumvent this problem, we designed a phthalocyanine-poly-L-glutamic acid conjugate (1-PG) made from a new phthalocyanine (Pc 1) monofunctionalized to allow adequate conjugation to PGA. The resulting 1-PG conjugate retained high absorptivity in the near-infrared (NIR) region at its λmax675nm in an aqueous environment. The 1-PG conjugate demonstrated good singlet oxygen generation efficiency, increased uptake by 4 T1 breast cancer cells via clathrin-mediated endocytosis, and enhanced photocytotoxic efficacy. The conjugate also displayed a high light-dark toxicity ratio, approximately 1.5-fold greater than zinc phthalocyanine at higher concentration (10 μM), an important feature for the reduction of dark toxicity and unwanted side effects. These results suggest that the 1-PG conjugate could be a useful alternative for deep tissue treatment with enhanced anti-cancer (PDT) efficacy.
    Matched MeSH terms: Indoles/chemistry*; Photosensitizing Agents/chemistry*; Glutamic Acid/chemistry*; Singlet Oxygen/chemistry; Nanoconjugates/chemistry*
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