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Curcumin in a model skin lotion formulation

Suhaimi H, Ahmad FB, Friberg SE

J Pharm Sci, 1995 Mar;84(3):376-80.
PMID: 7616381

A lamellar liquid crystalline region was identified in a typical skin lotion formulation system composed of a mixture of isostearic acid and triethanolamine (TEA) at 65:35 (w/w), decane, and water (the temperature was controlled at 30 degrees C). The interlayer spacings were determined by a small-angle X-ray diffraction technique. Incorporation of a natural dye, curcumin, resulted in lower interlayer spacings and higher penetration of water into the layered structure. However, the higher penetration of water was not apparent at all compositions of isostearic acid:TEA, decane, and water.

Matched MeSH terms: Ethanolamines/chemistry*
Fulltext Multivariate optimization in the biosynthesis of a triethanolamine (TEA)-based esterquat cationic surfactant using an artificial neural network

Masoumi HR, Kassim A, Basri M, Abdullah DK, Haron MJ

Molecules, 2011 Jun 29;16(7):5538-49.
PMID: 21716175 DOI: 10.3390/molecules16075538

An Artificial Neural Network (ANN) based on the Quick Propagation (QP) algorithm was used in conjunction with an experimental design to optimize the lipase-catalyzed reaction conditions for the preparation of a triethanolamine (TEA)-based esterquat cationic surfactant. Using the best performing ANN, the optimum conditions predicted were an enzyme amount of 4.77 w/w%, reaction time of 24 h, reaction temperature of 61.9 °C, substrate (oleic acid: triethanolamine) molar ratio of 1:1 mole and agitation speed of 480 r.p.m. The relative deviation percentage under these conditions was less than 4%. The optimized method was successfully applied to the synthesis of the TEA-based esterquat cationic surfactant at a 2,000 mL scale. This method represents a more flexible and convenient means for optimizing enzymatic reaction using ANN than has been previously reported by conventional methods.

Matched MeSH terms: Ethanolamines/chemistry*
Fulltext Synthesis and characterization of a narrow size distribution of zinc oxide nanoparticles

Zak AK, Razali R, Majid WH, Darroudi M

Int J Nanomedicine, 2011;6:1399-403.
PMID: 21796242 DOI: 10.2147/IJN.S19693

Zinc oxide nanoparticles (ZnO-NPs) were synthesized via a solvothermal method in triethanolamine (TEA) media. TEA was utilized as a polymer agent to terminate the growth of ZnO-NPs. The ZnO-NPs were characterized by a number of techniques, including X-ray diffraction analysis, transition electron microscopy, and field emission electron microscopy. The ZnO-NPs prepared by the solvothermal process at 150°C for 18 hours exhibited a hexagonal (wurtzite) structure, with a crystalline size of 33 ± 2 nm, and particle size of 48 ± 7 nm. The results confirm that TEA is a suitable polymer agent to prepare homogenous ZnO-NPs.

Matched MeSH terms: Ethanolamines/chemistry
Diethanolamine-modified pectin based core-shell composites as dual working gastroretentive drug-cargo

Bera H, Kumar S

Int J Biol Macromol, 2018 Mar;108:1053-1062.
PMID: 29122714 DOI: 10.1016/j.ijbiomac.2017.11.019

The current study aimed at developing diethonolamine-modified high-methoxyl pectin (DMP)-alginate (ALG) based core-shell composites for controlled intragastric delivery of metformin HCl (MFM) by combined approach of floating and bioadhesion. DMP with degree of amidation of 48.72% was initially accomplished and characterized by FTIR, DSC and XRD analyses. MFM-loaded core matrices were then fabricated by ionotropic gelation technique employing zinc acetate as cross-linker. The core matrices were further coated by fenugreek gum (FG)-ALG gel membrane via diffusion-controlled interfacial complexation method. Various formulations demonstrated excellent drug encapsulation efficiency (DEE, 51-70%) and sustained drug eluting behavior (Q8h, 72-96%), which were extremely influenced by polymer-blend (ALG:DMP) ratios, low density additives (olive oil/magnesium stearate) and FG-ALG coating inclusion. The drug release profile of the core-shell matrices (F-7) was best fitted in zero-order kinetic model with case-II transport driven mechanism. It also portrayed outstanding gastroretentive characteristics. Moreover, the composites were analyzed for surface morphology, drug-excipients compatibility, thermal behavior and drug crystallinity. Thus, the developed composites are appropriate for controlled stomach-specific delivery of MFM for type 2 diabetes management.

Matched MeSH terms: Ethanolamines/chemistry*
Triethanolamine - solution for rapid hydrothermal synthesis of titanate nanotubes

An'amt M, Huang N, Radiman S, Lim H, Muhamad M

Sains Malaysiana, 2014;43:137-144.

Titanate nanotubes were prepared by a rapid hydrothermal method in the presence of triethanolamine (TEA) using TiO2 nanoparticles as a precursor. The addition of TEA significantly reduced the formation time of the titanate nanotubes from 24 to 6 h. The crystalline structure of the titanate nanotubes was revealed to be H2Ti2O5 through the X-ray diffraction (xRD) measurement. The morphology of the titanate nanotubes was confirmed using transmission electron microscopy (TEM) while the surface area was characterized using Brunauer-Emmett-Teller (BET) surface area analysis. The titanate nanotubes produced were several hundred nanometers in length and had an average outer diameter of - 11.5 nm, inner diameter of -5.0 nm, interlayer spacing of 0.93 nm and surface area of >250 m2Ig. The photocatalytic activity of the titanate nanotubes was studied using methylene blue as a model dye; the titanate nanotubes showed better photocatalytic performance as compared to TiO2 nanoparticles.

Matched MeSH terms: Ethanolamines
Fulltext Statistical optimization of process parameters for lipase-catalyzed synthesis of triethanolamine-based esterquats using response surface methodology in 2-liter bioreactor

Masoumi HR, Basri M, Kassim A, Abdullah DK, Abdollahi Y, Abd Gani SS, et al.

ScientificWorldJournal, 2013;2013:962083.
PMID: 24324389 DOI: 10.1155/2013/962083

Lipase-catalyzed production of triethanolamine-based esterquat by esterification of oleic acid (OA) with triethanolamine (TEA) in n-hexane was performed in 2 L stirred-tank reactor. A set of experiments was designed by central composite design to process modeling and statistically evaluate the findings. Five independent process variables, including enzyme amount, reaction time, reaction temperature, substrates molar ratio of OA to TEA, and agitation speed, were studied under the given conditions designed by Design Expert software. Experimental data were examined for normality test before data processing stage and skewness and kurtosis indices were determined. The mathematical model developed was found to be adequate and statistically accurate to predict the optimum conversion of product. Response surface methodology with central composite design gave the best performance in this study, and the methodology as a whole has been proven to be adequate for the design and optimization of the enzymatic process.

Matched MeSH terms: Ethanolamines/chemical synthesis; Ethanolamines/chemistry*
Determination of a new antimalarial drug, benflumetol, in blood plasma by high-performance liquid chromatography

Mansor SM, Navaratnam V, Yahaya N, Nair NK, Wernsdorfer WH, Degen PH

J Chromatogr B Biomed Appl, 1996 Jul 12;682(2):321-5.
PMID: 8844426

A rapid and selective high-performance liquid chromatographic assay for determination of a new antimalarial drug (benflumetol, BFL) is described. After extraction with hexane-diethyl ether (70:30, v/v) from plasma, BFL was analysed using a C18 Partisil 10 ODS-3 reversed-phase stainless steel column and a mobile phase of acetonitrile-0.1 M ammonium acetate (90:10, v/v) adjusted to pH 4.9 with ultraviolet detection at 335 nm. The mean recovery of BFL over a concentration range of 50-400 ng/ml was 96.8 +/- 5.2%. The within-day and day-to-day coefficients of variation were 1.8-4.0 and 1.8-4.2%, respectively. The minimum detectable concentration in plasma for BFL was 5 ng/ml with a C.V. of less than 10%. This method was found to be suitable for clinical pharmacokinetic studies.

Matched MeSH terms: Ethanolamines/blood*; Ethanolamines/pharmacokinetics
Facile synthesis and characterization of tailor-made pectin-gellan gum-bionanofiller composites as intragastric drug delivery shuttles

Bera H, Kumar S, Maiti S

Int J Biol Macromol, 2018 Oct 15;118(Pt A):149-159.
PMID: 29932998 DOI: 10.1016/j.ijbiomac.2018.06.085

Olive oil-entrapped diethanolamine-modified high-methoxyl pectin (DMP)-gellan gum (GG)-bionanofiller composites were developed for controlled intragastric delivery of metformin HCl (MFM). DMP had a degree of amidation of 48.7% and was characterized further by FTIR, XRD and DSC analyses. MFM-loaded composites were subsequently accomplished by green synthesis via ionotropic gelation technique using zinc acetate as cross-linker. The thermal, X-ray and infrared analyses suggested an environment in the composites compatible with the drug, except certain degree of attenuation in drug's crystallinity. Scanning electron microscopy revealed almost spherical shape of the composites. Depending upon the mass ratios of GG:DMP, types of nanofiller (neusilin/bentonite/Florite) and oil inclusion, the composites exhibited variable drug encapsulation efficiency (DEE, 50-85%) and extended drug release behaviours (Q8h, 69-94%) in acetate buffer (pH 4.5). The optimized oil-entrapped Florite R NF/GG: DMP (1:1) composites eluted MFM via case-II transport mechanism and its drug release data was best fitted in zero-order kinetic model. The optimized formulation demonstrated excellent gastroretentive properties and substantial hypoglycemic effect in streptozotocin-induced diabetic rats. These novel hybrid matrices were thus found suitable for controlled intragastric delivery of MFM for the management of type 2 diabetes.

Matched MeSH terms: Ethanolamines/administration & dosage; Ethanolamines/chemistry
Fulltext Sp1 and Sp3 Are the Transcription Activators of Human ek1 Promoter in TSA-Treated Human Colon Carcinoma Cells

Kuan CS, See Too WC, Few LL

PLoS One, 2016;11(1):e0147886.
PMID: 26807725 DOI: 10.1371/journal.pone.0147886

Ethanolamine kinase (EK) catalyzes the phosphorylation of ethanolamine, the first step in the CDP-ethanolamine pathway for the biosynthesis of phosphatidylethanolamine (PE). Human EK exists as EK1, EK2α and EK2β isoforms, encoded by two separate genes, named ek1 and ek2. EK activity is stimulated by carcinogens and oncogenes, suggesting the involvement of EK in carcinogenesis. Currently, little is known about EK transcriptional regulation by endogenous or exogenous signals, and the ek gene promoter has never been studied.

Matched MeSH terms: Ethanolamines; Phosphatidylethanolamines
Scheduling the blended solution as industrial CO2 absorber in separation process by back-propagation artificial neural networks

Abdollahi Y, Sairi NA, Said SB, Abouzari-lotf E, Zakaria A, Sabri MF, et al.

Spectrochim Acta A Mol Biomol Spectrosc, 2015 Nov 5;150:892-901.
PMID: 26119355 DOI: 10.1016/j.saa.2015.06.036

It is believe that 80% industrial of carbon dioxide can be controlled by separation and storage technologies which use the blended ionic liquids absorber. Among the blended absorbers, the mixture of water, N-methyldiethanolamine (MDEA) and guanidinium trifluoromethane sulfonate (gua) has presented the superior stripping qualities. However, the blended solution has illustrated high viscosity that affects the cost of separation process. In this work, the blended fabrication was scheduled with is the process arranging, controlling and optimizing. Therefore, the blend's components and operating temperature were modeled and optimized as input effective variables to minimize its viscosity as the final output by using back-propagation artificial neural network (ANN). The modeling was carried out by four mathematical algorithms with individual experimental design to obtain the optimum topology using root mean squared error (RMSE), R-squared (R(2)) and absolute average deviation (AAD). As a result, the final model (QP-4-8-1) with minimum RMSE and AAD as well as the highest R(2) was selected to navigate the fabrication of the blended solution. Therefore, the model was applied to obtain the optimum initial level of the input variables which were included temperature 303-323 K, x[gua], 0-0.033, x[MDAE], 0.3-0.4, and x[H2O], 0.7-1.0. Moreover, the model has obtained the relative importance ordered of the variables which included x[gua]>temperature>x[MDEA]>x[H2O]. Therefore, none of the variables was negligible in the fabrication. Furthermore, the model predicted the optimum points of the variables to minimize the viscosity which was validated by further experiments. The validated results confirmed the model schedulability. Accordingly, ANN succeeds to model the initial components of the blended solutions as absorber of CO2 capture in separation technologies that is able to industries scale up.

Matched MeSH terms: Ethanolamines
Effects of Crude Palm Oil and Crude Palm Kernel Oil Upon Wax Inhibition

Ragunathan T, Husin H, Wood CD

ACS Omega, 2020 Aug 11;5(31):19342-19349.
PMID: 32803027 DOI: 10.1021/acsomega.0c00753

The ever-increasing demand for the finite source of oil has led oil production companies to produce and transport the produced crude oil as efficiently and economically as possible. One of the major concerns especially in waters like the South China Sea is the deposition of wax on the walls of the pipeline or wellbore, constricting and hindering the hydrocarbon flow. This is due to the low seabed temperatures, which can be below the wax appearance temperature (WAT), leading to the deposition of wax out of waxy crude oil through the molecular dispersion mechanism. Currently, many prevention and remedy methods are in place to overcome the problem, but most of the additives possess environmental threat, as most of the chemical solutions used are toxic, nonorganic, and costly. Hence, this paper aims to provide some insights into the effect of palm oil derivatives such as crude palm oil (CPO) and crude palm kernel oil (CPKO) on wax inhibition. The effect of aging time (i.e., immersion time) was also evaluated. A comparison was made between paraffin inhibition efficiency results (PIE %) obtained by CPO, CPKO, poly(ethylene-co-vinyl acetate) (EVA), and triethanolamine (TEA). It was observed that the average efficiency of 81.67% was obtained when 1% CPO was added to heavy crude oil. The wax inhibition performance reached a plateau after 1.5 h of aging time for all of the investigated samples.

Matched MeSH terms: Ethanolamines
Fulltext The study of nanosized semiconducting Nb doped Y-ZrO2

Prastomo, Niki, Lockman, Zainovia, Ahmad Fauzi Mohd Noor, Ahmad Nuruddin, Matsuda, Atsunori

Journal of Nuclear and Related Technologies, 2007;2007(1):149-154.
MyJurnal

Tetragonal Y2O3 stabilized Zirconia (t-Y-ZrO2) powders were doped with Nb2O5 to seek a possibility if electronics doping would enhance the electronics conductivity of the insulating oxide. In this work Y2O3 was added as a stabilizer to produce tetragonal ZrO2 whereas Nb2O5 was added for the electronic doping. Several compositions of powders were prepared by thermal decomposition method and were post annealed at different temperatures. Precursor solutions were prepared from the mixture of zirconyl nitrate, yttrium nitrate and niobium tartarate as well as TEA (triethanolamine). The mixed solution were evaporated, pyrolysed and calcined to produce nanosized powders. The phase formation of the as-made powders was investigated by x-ray diffractometer. The additions of 7% Y2O3 were found to stabilize the tetragonal phase of zirconia.
The addition of Nb2O5 did not alter the stability of the tetragonal phase but it was found that the conductivity of the material has changed. The band gap as measured by the UV-Visible Spectrometer gave a value in the range of 2.97 to 5.01 eV. XRD was also used to deduce the crystallite size (by using Scherer’s equation) and transmission electron microcopy was used to view the particle sizes and shapes. The Nb doped t-Y-ZrO2 prepared in this work was to be nanosized crystal with size ranges from 7 nm to 15 nm.

Matched MeSH terms: Ethanolamines
Fulltext Determining optimum conditions for lipase-catalyzed synthesis of triethanolamine (TEA)-based esterquat cationic surfactant by a Taguchi robust design method

Masoumi HR, Kassim A, Basri M, Abdullah DK

Molecules, 2011 Jun 03;16(6):4672-80.
PMID: 21642941 DOI: 10.3390/molecules16064672

A Taguchi robust design method with an L₉ orthogonal array was implemented to optimize experimental conditions for the biosynthesis of triethanolamine (TEA)-based esterquat cationic surfactants using an enzymatic reaction method. The esterification reaction conversion% was considered as the response. Enzyme amount, reaction time, reaction temperature and molar ratio of substrates, [oleic acid: triethanolamine (OA:TEA)] were chosen as main parameters. As a result of the Taguchi analysis in this study, the molar ratio of substrates was found to be the most influential parameter on the esterification reaction conversion%. The amount of enzyme in the reaction had also a significant effect on reaction conversion%.

Matched MeSH terms: Ethanolamines/chemistry*
Resistance to the "last resort" antibiotic colistin: a single-zinc mechanism for phosphointermediate formation in MCR enzymes

Lythell E, Suardíaz R, Hinchliffe P, Hanpaibool C, Visitsatthawong S, Oliveira ASF, et al.

Chem Commun (Camb), 2020 Jun 23;56(50):6874-6877.
PMID: 32432618 DOI: 10.1039/d0cc02520h

MCR (mobile colistin resistance) enzymes catalyse phosphoethanolamine (PEA) addition to bacterial lipid A, threatening the "last-resort" antibiotic colistin. Molecular dynamics and density functional theory simulations indicate that monozinc MCR supports PEA transfer to the Thr285 acceptor, positioning MCR as a mono- rather than multinuclear member of the alkaline phosphatase superfamily.

Matched MeSH terms: Ethanolamines/chemistry
Unusual metal ion cofactor requirement of Entamoeba histolytica choline and ethanolamine kinase isoforms

Chang CH, Few LL, Lim BH, Yvonne-Tee GB, Chew AL, See Too WC

Parasitol Res, 2023 Jul;122(7):1651-1661.
PMID: 37202563 DOI: 10.1007/s00436-023-07869-5

The de novo biosynthesis of phosphatidylcholine and phosphatidylethanolamine in Entamoeba histolytica is largely dependent on the CDP-choline and CDP-ethanolamine pathways. Although the first enzymes of these pathways, EhCK1 and EhCK2, have been previously characterized, their enzymatic activity was found to be low and undetectable, respectively. This study aimed to identify the unusual characteristics of these enzymes in this deadly parasite. The discovery that EhCKs prefer Mn2+ over the typical Mg2+ as a metal ion cofactor is intriguing for CK/EK family of enzymes. In the presence of Mn2+, the activity of EhCK1 increased by approximately 108-fold compared to that in Mg2+. Specifically, in Mg2+, EhCK1 exhibited a Vmax and K0.5 of 3.5 ± 0.1 U/mg and 13.9 ± 0.2 mM, respectively. However, in Mn2+, it displayed a Vmax of 149.1 ± 2.5 U/mg and a K0.5 of 9.5 ± 0.1 mM. Moreover, when Mg2+ was present at a constant concentration of 12 mM, the K0.5 value for Mn2+ was ~ 2.4-fold lower than that in Mn2+ alone, without affecting its Vmax. Although the enzyme efficiency of EhCK1 was significantly improved by about 25-fold in Mn2+, it is worth noting that its Km for choline and ATP were higher than in equimolar of Mg2+ in a previous study. In contrast, EhCK2 showed specific activity towards ethanolamine in Mn2+, exhibiting Michaelis-Menten kinetic with ethanolamine (Km = 312 ± 27 µM) and cooperativity with ATP (K0.5 = 2.1 ± 0.2 mM). Additionally, we investigated the effect of metal ions on the substrate recognition of human choline and ethanolamine kinase isoforms. Human choline kinase α2 was found to absolutely require Mg2+, while choline kinase β differentially recognized choline and ethanolamine in Mg2+ and Mn2+, respectively. Finally, mutagenesis studies revealed that EhCK1 Tyr129 was critical for Mn2+ binding, while Lys233 was essential for substrate catalysis but not metal ion binding. Overall, these findings provide insight into the unique characteristics of the EhCKs and highlight the potential for new approaches to treating amoebiasis. Amoebiasis is a challenging disease for clinicians to diagnose and treat, as many patients are asymptomatic. However, by studying the enzymes involved in the CDP-choline and CDP-ethanolamine pathways, which are crucial for de novo biosynthesis of phosphatidylcholine and phosphatidylethanolamine in Entamoeba histolytica, there is great potential to discover new therapeutic approaches to combat this disease.

Matched MeSH terms: Ethanolamines/metabolism; Phosphatidylethanolamines/metabolism
Identification and Characterization of Entamoeba histolytica Choline Kinase

Chang CH, See Too WC, Lim BH, Few LL

Acta Parasitol, 2024 Mar;69(1):426-438.
PMID: 38172465 DOI: 10.1007/s11686-023-00763-1

PURPOSE: Entamoeba histolytica is one of the death-causing parasites in the world. Study on its lipid composition revealed that it is predominated by phosphatidylcholine and phosphatidylethanolamine. Further study revealed that its phosphorylated metabolites might be produced by the Kennedy pathway. Here, we would like to report on the characterizations of enzymes from this pathway that would provide information for the design of novel inhibitors against these enzymes in future.
METHODOLOGY: E. histolytica HM-1:IMSS genomic DNA was isolated and two putative choline/ethanolamine kinase genes (EhCK1 and EhCK2) were cloned and expressed from Escherichia coli BL21 strain. Enzymatic characterizations were further carried out on the purified enzymes.
RESULTS: EhCK1 and EhCK2 were identified from E. histolytica genome. The deduced amino acid sequences were more identical to its homologues in human (35-48%) than other organisms. The proteins were clustered as ethanolamine kinase in the constructed phylogeny tree. Sequence analysis showed that they possessed all the conserved motifs in choline kinase family: ATP-binding loop, Brenner's phosphotransferase motif, and choline kinase motif. Here, the open reading frames were cloned, expressed, and purified to apparent homogeneity. EhCK1 showed activity with choline but not ethanolamine. The biochemical characterization showed that it had a Vmax of 1.9 ± 0.1 µmol/min/mg. Its Km for choline and ATP was 203 ± 26 µM and 3.1 ± 0.4 mM, respectively. In contrast, EhCK2 enzymatic activity was only detected when Mn2+ was used as the co-factor instead of Mg2+ like other choline/ethanolamine kinases. Highly sensitive and specific antibody against EhCK1 was developed and used to confirm the endogenous EhCK1 expression using immunoblotting.
CONCLUSIONS: With the understanding of EhC/EK importance in phospholipid metabolism and their unique characteristic, EhC/EK could be a potential target for future anti-amoebiasis study.

Matched MeSH terms: Ethanolamines/metabolism
Fulltext Hypothetical Protein BPSL3393 of Burkholderia pseudomallei is Involved in Ethanolamine Catabolism

Luan OG, Yam H, Samian R, Wajidi MFF, Mahadi NM, Mohamad S, et al.

Trop Life Sci Res, 2017 Jul;28(2):57-74.
PMID: 28890761 MyJurnal DOI: 10.21315/tlsr2017.28.2.5

Burkholderia pseudomallei is a soil-dwelling bacterium that causes a globally emerging disease called melioidosis. Approximately one third of the in silico annotated genes in its genome are classified as hypothetical genes. This group of genes is difficult to be functionally characterised partly due to the absence of noticeable phenotypes under conventional laboratory settings. A bioinformatic survey of hypothetical genes revealed a gene designated as BPSL3393 that putatively encodes a small protein of 11 kDA with a CoA binding domain. BPSL3393 is conserved in all the B. pseudomallei genomes as well as various in other species within the genus Burkholderia. Taking into consideration that CoA plays a ubiquitous metabolic role in all life forms, characterisation of BPSL3393 may uncover a previously over-looked metabolic feature of B. pseudomallei. The gene was deleted from the genome using a double homologous recombination approach yielding a null mutant. The BPSL3393 mutant showed no difference in growth rate with the wild type under rich and minimal growth conditions. An extensive metabolic phenotyping test was performed involving 95 metabolic substrates. The deletion mutant of BPSL3393 was severely impaired in its ethanolamine metabolism. The growth rate of the mutant was attenuated when ethanolamine was used as the sole carbon source. A transcriptional analysis of the ethanolamine metabolism genes showed that they were down-regulated in the BPSL3393 mutant. This seemed to suggest that BPSL3393 functions as a positive regulator for ethanolamine metabolism.

Matched MeSH terms: Ethanolamines
Fulltext Changing paradigms in the treatment of asthma

Loh LC

Family Physician, 2005;13(3):0-0.
MyJurnal

Significant changes have occurred in relation to how chronic asthma is being treated. Emphasis has now shifted from viewing asthma as a condition of smooth muscle dysfunction to one of chronic inflammation. As such, anti-inflammatory therapy forming the cornerstone of treatment represents the first important milestone in the evolution of asthma treatment. For this purpose, inhaled corticosteroid (ICS) is by far the most effective anti-inflammatory therapy. Another important milestone is the recognition of the superiority of adding long-acting β2-agonist (LABA) to ICS over escalating ICS dose alone or other forms of add-on therapies in treating asthmatic patients not responding to regular ICS alone. The effectiveness of adding LABA to ICS in treating asthma logically led to combining the two drugs into one single inhaler (salmeterol/fluticasone and budesonide/formoterol) that has the attractiveness of being user-friendly and ensuring that ICS is not missed out. The unique property of formoterol that allows for repetitive flexible dosing paved way to the concept of using Symbicort for both regular maintenance dosing and as required rescue medication. This revolutionary approach has been recently shown to provide improved asthma outcome, achieved at an overall lower or at least comparable corticosteroid intake, and may represent another evolutionary step in the treatment strategy of chronic asthma.

Matched MeSH terms: Ethanolamines
Synthesis and evaluation of chalcone derivatives as inhibitors of neutrophils' chemotaxis, phagocytosis and production of reactive oxygen species

Bukhari SN, Tajuddin Y, Benedict VJ, Lam KW, Jantan I, Jalil J, et al.

Chem Biol Drug Des, 2014 Feb;83(2):198-206.
PMID: 24433224 DOI: 10.1111/cbdd.12226

Inhibitory effects on neutrophils' chemotaxis, phagocytosis and production of reactive oxygen species (ROS) are among the important targets in developing anti-inflammatory agents and immunosuppressants. Eight series of chalcone derivatives including five newly synthesized series were assessed for their inhibitory effects on chemotaxis, phagocytosis and ROS production in human polymorphonuclear neutrophils (PMNs). Inhibition of PMNs' chemotaxis and phagocytosis abilities were investigated using the Boyden chamber technique and the Phagotest kit, respectively, while ROS production was evaluated using luminol- and lucigenin-based chemiluminescence assay. The new derivatives (4d and 8d), which contain 4-methylaminoethanol functional group were active in all the assays performed. It was also observed that some of the compounds were active in inhibiting chemotaxis while others suppressed phagocytosis and ROS production. The information obtained gave new insight into chalcone derivatives with the potential to be developed as immunomodulators.

Matched MeSH terms: Ethanolamines/chemistry
Fulltext Satisfaction level and asthma control among Malaysian asthma patients on Symbicort Maintenance and Reliever Therapy (SMART) in the primary care setting (SMARTEST study)

Liam CK, Pang YK, Chua KT

Asian Pac J Allergy Immunol, 2014 Jun;32(2):145-52.
PMID: 25003728 DOI: 10.12932/AP0359.32.2.2013

OBJECTIVE: To evaluate Malaysian patients' satisfaction levels and asthma control with Symbicort SMART® in the primary care setting.
METHOD: This is a cross-sectional, multicentre study involving adult patients with persistent asthma who were prescribed only Symbicort SMART in the preceding one month prior to recruitment. Patients' satisfaction with Symbicort SMART and asthma control were evaluated using the self-administered Satisfaction with Asthma Treatment Questionnaire (SATQ) and the Asthma Control Test (ACT).
RESULTS: Asthma was controlled (ACT score >20) in 189 (83%) of 228 patients. The mean overall SATQ score for patients with controlled asthma was 5.65 indicating a high satisfaction level, which was positively correlated with high ACT scores. There were differences in asthma control based on ethnicity, number of unscheduled visits and treatment compliance.
CONCLUSIONS: Symbicort SMART resulted in a high satisfaction level and asthma control among Malaysian patients treated in the primary care setting and it is an effective and appealing treatment for asthmatic patients.
Study site: General practice clinics, Malaysia

Matched MeSH terms: Ethanolamines/administration & dosage*; Ethanolamines/adverse effects

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