Displaying publications 61 - 80 of 143 in total

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  1. Green nanoemulsion-laden glyphosate isopropylamine formulation in suppressing creeping foxglove (A. gangetica), slender button weed (D. ocimifolia) and buffalo grass (P. conjugatum)
    Lim CJ, Basri M, Omar D, Abdul Rahman MB, Salleh AB, Raja Abdul Rahman RN
    Pest Manag Sci, 2013 Jan;69(1):104-11.
    PMID: 22865686 DOI: 10.1002/ps.3371
    Pesticides are developed with carriers to improve their physicochemical properties and, accordingly, the bioefficacy of the applied formulation. For foliar-applied herbicide, generally less than 0.1% of the active ingredient reaching the target site could reduce pesticide performance. Recently, a carrier of nanoemulsion consisting of oil, surfactant and water, with a particle size of less than 200 nm, has been shown to enhance drug permeability for skin penetration in pharmaceutical delivery systems. In the present work, the aim was to formulate a water-soluble herbicide, glyphosate isopropylamine (IPA), using a green nanoemulsion system for a biological activity study against the weeds creeping foxglove, slender button weed and buffalo grass.
  2. Fulltext Unlocking the mystery behind the activation phenomenon of T1 lipase: a molecular dynamics simulations approach
    Abdul Rahman MZ, Salleh AB, Abdul Rahman RN, Abdul Rahman MB, Basri M, Leow TC
    Protein Sci, 2012 Aug;21(8):1210-21.
    PMID: 22692819 DOI: 10.1002/pro.2108
    The activation of lipases has been postulated to proceed by interfacial activation, temperature switch activation, or aqueous activation. Recently, based on molecular dynamics (MD) simulation experiments, the T1 lipase activation mechanism was proposed to involve aqueous activation in addition to a double-flap mechanism. Because the open conformation structure is still unavailable, it is difficult to validate the proposed theory unambiguously to understand the behavior of the enzyme. In this study, we try to validate the previous reports and uncover the mystery behind the activation process using structural analysis and MD simulations. To investigate the effects of temperature and environmental conditions on the activation process, MD simulations in different solvent environments (water and water-octane interface) and temperatures (20, 50, 70, 80, and 100°C) were performed. Based on the structural analysis of the lipases in the same family of T1 lipase (I.5 lipase family), we proposed that the lid domain comprises α6 and α7 helices connected by a loop, thus forming a helix-loop-helix motif involved in interfacial activation. Throughout the MD simulations experiments, lid displacements were only observed in the water-octane interface, not in the aqueous environment with respect to the temperature effect, suggesting that the activation process is governed by interfacial activation coupled with temperature switch activation. Examining the activation process in detail revealed that the large structural rearrangement of the lid domain was caused by the interaction between the hydrophobic residues of the lid with octane, a nonpolar solvent, and this conformation was found to be thermodynamically favorable.
  3. Purification and characterisation of an F16L mutant of a thermostable lipase
    Ali MS, Yun CC, Chor AL, Rahman RN, Basri M, Salleh AB
    Protein J, 2012 Mar;31(3):229-37.
    PMID: 22350313 DOI: 10.1007/s10930-012-9395-8
    A mutant of the lipase from Geobacillus sp. strain T1 with a phenylalanine to leucine substitution at position 16 was overexpressed in Escherichia coli strain BL21(De3)pLysS. The crude enzyme was purified by two-step affinity chromatography with a final recovery and specific activity of 47.4 and 6,315.8 U/mg, respectively. The molecular weight of the purified F16L lipase was approximately 43 kDa by 12% SDS-PAGE analysis. The F16L lipase was demonstrated to be a thermophilic enzyme due its optimum temperature at 70 °C and showed stability over a temperature range of 40-60 °C. The enzyme exhibited an optimum pH 7 in phosphate buffer and was relatively stable at an alkaline pH 8-9. Metal ions such as Ca(2+), Mn(2+), Na(+), and K(+) enhanced the lipase activity, but Mg(2+), Zn(2+), and Fe(2+) inhibited the lipase. All surfactants tested, including Tween 20, 40, 60, 80, Triton X-100, and SDS, significantly inhibited the lipolytic action of the lipase. A high hydrolytic rate was observed on long-chain natural oils and triglycerides, with a notable preference for olive oil (C18:1; natural oil) and triolein (C18:1; triglyceride). The F16L lipase was deduced to be a metalloenzyme because it was strongly inhibited by 5 mM EDTA. Moderate inhibition was observed in the presence of PMSF at a similar concentration, indicating that serine residues are involved in its catalytic action. Further, the activity was not impaired by water-miscible solvents, including methanol, ethanol, and acetone.
  4. Manipulation of the conformation and enzymatic properties of T1 lipase by site-directed mutagenesis of the protein core
    Wahab RA, Basri M, Rahman RN, Salleh AB, Rahman MB, Chor LT
    Appl Biochem Biotechnol, 2012 Jun;167(3):612-20.
    PMID: 22581079 DOI: 10.1007/s12010-012-9728-2
    In silico and experimental investigations were conducted to explore the effects of substituting hydrophobic residues, Val, Met, Leu, Ile, Trp, and Phe into Gln 114 of T1 lipase. The in silico investigations accurately predicted the enzymatic characteristics of the mutants in the experimental studies and provided rationalization for some of the experimental observations. Substitution with Leu successfully improved the conformational stability and enzymatic characteristics of T1 lipase. However, replacement of Gln114 with Trp negatively affected T1 lipase and resulted in the largest disruption of protein stability, diminished lipase activity and inferior enzymatic characteristics. These results suggested that the substitution of a larger residue in a densely packed area of the protein core can have considerable effects on the structure and function of an enzyme. This is especially true when the residue is next to the catalytic serine as demonstrated with the Phe and Trp mutation.
  5. Locally isolated yeasts from Malaysia: identification, phylogenetic study and characterization
    Oslan SN, Salleh AB, Rahman RN, Basri M, Chor AL
    Acta Biochim. Pol., 2012;59(2):225-9.
    PMID: 22577620
    Yeasts are a convenient platform for many applications. They have been widely used as the expression hosts. There is a need to have a new yeast expression system to contribute the molecular cloning demands. Eight yeast isolates were screened from various environment sources and identified through ribosomal DNA (rDNA) Internal Transcribed Spacer (ITS). Full sequence of the rDNA ITS region for each isolate was BLASTed and phylogenetic study was constructed by using MEGA4. Among the isolates, isolate WB from 'ragi' (used to ferment carbohydrates) could be identified as a new species in order Saccharomycetales according to rDNA ITS region, morphology and biochemical tests. Isolate SO (from spoiled orange), RT (rotten tomato) and RG (different type of 'ragi') were identified as Pichia sp. Isolates R1 and R2, S4 and S5 (from the surrounding of a guava tree) were identified as Issatchenkia sp. and Hanseniaspora sp., respectively. Geneticin, 50 µg/mL, was determined to be the antibiotic marker for all isolates excepted for isolates RT and SO which used 500 µg/mL and 100 µg/mL Zeocin, respectively. Intra-extracellular proteins were screened for lipolytic activity at 30°C and 70°C. Thermostable lipase activity was detected in isolates RT and R1 with 0.6 U/mg and 0.1 U/mg, respectively. In conclusion, a new yeast-vector system for isolate WB can be developed by using phleomycin or geneticin as the drugs resistance marker. Moreover, strains RT and R1 can be investigated as a novel source of a thermostable lipase.
  6. Fulltext Improvement of thermal stability via outer-loop ion pair interaction of mutated T1 lipase from Geobacillus zalihae strain T1
    Ruslan R, Abd Rahman RN, Leow TC, Ali MS, Basri M, Salleh AB
    Int J Mol Sci, 2012;13(1):943-60.
    PMID: 22312296 DOI: 10.3390/ijms13010943
    Mutant D311E and K344R were constructed using site-directed mutagenesis to introduce an additional ion pair at the inter-loop and the intra-loop, respectively, to determine the effect of ion pairs on the stability of T1 lipase isolated from Geobacillus zalihae. A series of purification steps was applied, and the pure lipases of T1, D311E and K344R were obtained. The wild-type and mutant lipases were analyzed using circular dichroism. The T(m) for T1 lipase, D311E lipase and K344R lipase were approximately 68.52 °C, 70.59 °C and 68.54 °C, respectively. Mutation at D311 increases the stability of T1 lipase and exhibited higher T(m) as compared to the wild-type and K344R. Based on the above, D311E lipase was chosen for further study. D311E lipase was successfully crystallized using the sitting drop vapor diffusion method. The crystal was diffracted at 2.1 Å using an in-house X-ray beam and belonged to the monoclinic space group C2 with the unit cell parameters a = 117.32 Å, b = 81.16 Å and c = 100.14 Å. Structural analysis showed the existence of an additional ion pair around E311 in the structure of D311E. The additional ion pair in D311E may regulate the stability of this mutant lipase at high temperatures as predicted in silico and spectroscopically.
  7. Effect of ion pair on thermostability of F1 protease: integration of computational and experimental approaches
    Rahman RN, Muhd Noor ND, Ibrahim NA, Salleh AB, Basri M
    J Microbiol Biotechnol, 2012 Jan;22(1):34-45.
    PMID: 22297217
    A thermophilic Bacillus stearothermophilus F1 produces an extremely thermostable serine protease. The F1 protease sequence was used to predict its three-dimensional (3D) structure to provide better insights into the relationship between the protein structure and biological function and to identify opportunities for protein engineering. The final model was evaluated to ensure its accuracy using three independent methods: Procheck, Verify3D, and Errat. The predicted 3D structure of F1 protease was compared with the crystal structure of serine proteases from mesophilic bacteria and archaea, and led to the identification of features that were related to protein stabilization. Higher thermostability correlated with an increased number of residues that were involved in ion pairs or networks of ion pairs. Therefore, the mutants W200R and D58S were designed using site-directed mutagenesis to investigate F1 protease stability. The effects of addition and disruption of ion pair networks on the activity and various stabilities of mutant F1 proteases were compared with those of the wild-type F1 protease.
  8. Fulltext 3D structure elucidation of thermostable L2 lipase from Thermophilic Bacillus sp. L2
    Abd Rahman RN, Shariff FM, Basri M, Salleh AB
    Int J Mol Sci, 2012;13(7):9207-17.
    PMID: 22942761 DOI: 10.3390/ijms13079207
    The crystallization of proteins makes it possible to determine their structure by X-ray crystallography, and is therefore important for the analysis of protein structure-function relationships. L2 lipase was crystallized by using the J-tube counter diffusion method. A crystallization consisting of 20% PEG 6000, 50 mM MES pH 6.5 and 50 mM NaCl was found to be the best condition to produce crystals with good shape and size (0.5 × 0.1 × 0.2 mm). The protein concentration used for the crystallization was 3 mg/mL. L2 lipase crystal has two crystal forms, Shape 1 and Shape 2. Shape 2 L2 lipase crystal was diffracted at 1.5 Å and the crystal belongs to the orthorhombic space group P2(1)2(1)2(1), with unit-cell parameters a = 72.0, b = 81.8, c = 83.4 Å, α = β = γ = 90°. There is one molecule per asymmetric unit and the solvent content of the crystals is 56.9%, with a Matthew's coefficient of 2.85 Å Da(-1). The 3D structure of L2 lipase revealed topological organization of α/β-hydrolase fold consisting of 11 β-strands and 13 α-helices. Ser-113, His-358 and Asp-317 were assigned as catalytic triad residues. One Ca(2+) and one Zn(2+) were found in the L2 lipase molecule.
  9. Fulltext Molecular Cloning and Optimization for High Level Expression of Cold-Adapted Serine Protease from Antarctic Yeast Glaciozyma antarctica PI12
    Alias N, Ahmad Mazian M, Salleh AB, Basri M, Rahman RN
    Enzyme Res, 2014;2014:197938.
    PMID: 25093119 DOI: 10.1155/2014/197938
    Psychrophilic basidiomycete yeast, Glaciozyma antarctica strain PI12, was shown to be a protease-producer. Isolation of the PI12 protease gene from genomic and mRNA sequences allowed determination of 19 exons and 18 introns. Full-length cDNA of PI12 protease gene was amplified by rapid amplification of cDNA ends (RACE) strategy with an open reading frame (ORF) of 2892 bp, coded for 963 amino acids. PI12 protease showed low homology with the subtilisin-like protease from fungus Rhodosporidium toruloides (42% identity) and no homology to other psychrophilic proteases. The gene encoding mature PI12 protease was cloned into Pichia pastoris expression vector, pPIC9, and positioned under the induction of methanol-alcohol oxidase (AOX) promoter. The recombinant PI12 protease was efficiently secreted into the culture medium driven by the Saccharomyces cerevisiae α-factor signal sequence. The highest protease production (28.3 U/ml) was obtained from P. pastoris GS115 host (GpPro2) at 20°C after 72 hours of postinduction time with 0.5% (v/v) of methanol inducer. The expressed protein was detected by SDS-PAGE and activity staining with a molecular weight of 99 kDa.
  10. Fulltext Rapid adsorption of heavy metals by Fe3O4/talc nanocomposite and optimization study using response surface methodology
    Kalantari K, Ahmad MB, Masoumi HR, Shameli K, Basri M, Khandanlou R
    Int J Mol Sci, 2014;15(7):12913-27.
    PMID: 25050784 DOI: 10.3390/ijms150712913
    Fe3O4/talc nanocomposite was used for removal of Cu(II), Ni(II), and Pb(II) ions from aqueous solutions. Experiments were designed by response surface methodology (RSM) and a quadratic model was used to predict the variables. The adsorption parameters such as adsorbent dosage, removal time, and initial ion concentration were used as the independent variables and their effects on heavy metal ion removal were investigated. Analysis of variance was incorporated to judge the adequacy of the models. Optimal conditions with initial heavy metal ion concentration of 100, 92 and 270 mg/L, 120 s of removal time and 0.12 g of adsorbent amount resulted in 72.15%, 50.23%, and 91.35% removal efficiency for Cu(II), Ni(II), and Pb(II), respectively. The predictions of the model were in good agreement with experimental results and the Fe3O4/talc nanocomposite was successfully used to remove heavy metals from aqueous solutions.
  11. Fulltext Effects of propylene glycol alginate and sucrose esters on the physicochemical properties of modified starch-stabilized beverage emulsions
    Cheong KW, Mirhosseini H, Hamid NS, Osman A, Basri M, Tan CP
    Molecules, 2014 Jun 24;19(6):8691-706.
    PMID: 24962400 DOI: 10.3390/molecules19068691
    This study was conducted to investigate the effect of main emulsion components namely, modified starch, propylene glycol alginate (PGA), sucrose laurate and sucrose stearate on creaming index, cloudiness, average droplet size and conductivity of soursop beverage emulsions. Generally, the use of different emulsifiers or a mixture of emulsifiers has a significant (p < 0.05) effect on the response variables studied. The addition of PGA had a significant (p < 0.05) effect on the creaming index at 55 °C, while PGA-stabilized (PGA1) emulsions showed low creaming stability at both 25 °C and 55 °C. Conversely, the utilization of PGA either as a mixture or sole emulsifier, showed significantly (p < 0.05) higher cloudiness, as larger average droplet size will affect the refractive index of the oil and aqueous phases. Additionally, the cloudiness was directly proportional to the mean droplet size of the dispersed phase. The inclusion of PGA into the formulation could have disrupted the properties of the interfacial film, thus resulting in larger droplet size. While unadsorbed ionized PGA could have contributed to higher conductivity of emulsions prepared at low pH. Generally, emulsions prepared using sucrose monoesters or as a mixture with modified starch emulsions have significantly (p < 0.05) lower creaming index and conductivity values, but higher cloudiness and average droplet size.
  12. Unscrambling the effect of C-terminal tail deletion on the stability of a cold-adapted, organic solvent stable lipase from Staphylococcus epidermidis AT2
    Kamarudin NH, Rahman RN, Ali MS, Leow TC, Basri M, Salleh AB
    Mol Biotechnol, 2014 Aug;56(8):747-57.
    PMID: 24771007 DOI: 10.1007/s12033-014-9753-1
    Terminal moieties of most proteins are long known to be disordered and flexible. To unravel the functional role of these regions on the structural stability and biochemical properties of AT2 lipase, four C-terminal end residues, (Ile-Thr-Arg-Lys) which formed a flexible, short tail-like random-coil segment were targeted for mutation. Swapping of the tail-like region had resulted in an improved crystallizability and anti-aggregation property along with a slight shift of the thermostability profile. The lipolytic activity of mutant (M386) retained by 43 % compared to its wild-type with 18 % of the remaining activity at 45 °C. In silico analysis conducted at 25 and 45 °C was found to be in accordance to the experimental findings in which the RMSD values of M386 were more stable throughout the total trajectory in comparison to its wild-type. Terminal moieties were also observed to exhibit large movement and flexibility as denoted by high RMSF values at both dynamics. Variation in organic solvent stability property was detected in M386 where the lipolytic activity was stimulated in the presence of 25 % (v/v) of DMSO, isopropanol, and diethyl ether. This may be worth due to changes in the surface charge residues at the mutation point which probably involve in protein-solvent interaction.
  13. A new cold-adapted, organic solvent stable lipase from mesophilic Staphylococcus epidermidis AT2
    Kamarudin NH, Rahman RN, Ali MS, Leow TC, Basri M, Salleh AB
    Protein J, 2014 Jun;33(3):296-307.
    PMID: 24777627 DOI: 10.1007/s10930-014-9560-3
    The gene encoding a cold-adapted, organic solvent stable lipase from a local soil-isolate, mesophilic Staphylococcus epidermidis AT2 was expressed in a prokaryotic system. A two-step purification of AT2 lipase was achieved using butyl sepharose and DEAE sepharose column chromatography. The final recovery and purification fold were 47.09 % and 3.45, respectively. The molecular mass of the purified lipase was estimated to be 43 kDa. AT2 lipase was found to be optimally active at pH 8 and stable at pH 6-9. Interestingly, this enzyme demonstrated remarkable stability at cold temperature (<30 °C) and exhibited optimal activity at a temperature of 25 °C. A significant enhancement of the lipolytic activity was observed in the presence of Ca(2+), Tween 60 and Tween 80. Phenylmethylsulfonylfluoride, a well known serine inhibitor did not cause complete inhibition of the enzymatic activity. AT2 lipase exhibited excellent preferences towards long chain triglycerides and natural oils. The lipolytic activity was stimulated by dimethylsulfoxide and diethyl ether, while more than 50 % of its activity was retained in methanol, ethanol, acetone, toluene, and n-hexane. Taken together, AT2 lipase revealed highly attractive biochemical properties especially because of its stability at low temperature and in organic solvents.
  14. Fulltext The effect of prime emulsion components as a function of equilibrium headspace concentration of soursop flavor compounds
    Cheong KW, Tan CP, Mirhosseini H, Joanne-Kam WY, Sheikh Abdul Hamid N, Osman A, et al.
    Chem Cent J, 2014;8:23.
    PMID: 24708894 DOI: 10.1186/1752-153X-8-23
    BACKGROUND: Perceptions of food products start when flavor compounds are released from foods, transported and appropriate senses in the oral and nose are triggered. However, the long-term stability of flavor compounds in food product has been a major concern in the food industry due to the complex interactions between key food ingredients (e.g., polysaccharides and proteins). Hence, this study was conducted to formulate emulsion-based beverage using natural food emulsifiers and to understand the interactions between emulsion compositions and flavor compounds.

    RESULTS: The influences of modified starch (x 1 ), whey protein isolate (x 2 ), soursop flavor oil (x 3 ) and deionized water (x 4 ) on the equilibrium headspace concentration of soursop volatile flavor compounds were evaluated using a four-component with constrained extreme vertices mixture design. The results indicated that the equilibrium headspace concentration of soursop flavor compounds were significantly (p 

  15. Fulltext Formulation optimization of a palm-based nanoemulsion system containing levodopa
    Zainol S, Basri M, Basri HB, Shamsuddin AF, Abdul-Gani SS, Karjiban RA, et al.
    Int J Mol Sci, 2012;13(10):13049-64.
    PMID: 23202937 DOI: 10.3390/ijms131013049
    Response surface methodology (RSM) was utilized to investigate the influence of the main emulsion composition; mixture of palm and medium-chain triglyceride (MCT) oil (6%-12% w/w), lecithin (1%-3% w/w), and Cremophor EL (0.5%-1.5% w/w) as well as the preparation method; addition rate (2-20 mL/min), on the physicochemical properties of palm-based nanoemulsions. The response variables were the three main emulsion properties; particle size, zeta potential and polydispersity index. Optimization of the four independent variables was carried out to obtain an optimum level palm-based nanoemulsion with desirable characteristics. The response surface analysis showed that the variation in the three responses could be depicted as a quadratic function of the main composition of the emulsion and the preparation method. The experimental data could be fitted sufficiently well into a second-order polynomial model. The optimized formulation was stable for six months at 4 °C.
  16. Fulltext Phase behaviour and formation of fatty acid esters nanoemulsions containing piroxicam
    Mat Hadzir N, Basri M, Abdul Rahman MB, Salleh AB, Raja Abdul Rahman RN, Basri H
    AAPS PharmSciTech, 2013 Mar;14(1):456-63.
    PMID: 23386307 DOI: 10.1208/s12249-013-9929-1
    Fatty acid esters are long-chain esters, produced from the reaction of fatty acids and alcohols. They possess potential applications in cosmetic and pharmaceutical formulations due to their excellent wetting behaviour at interfaces and a non-greasy feeling when applied on the skin surfaces. This preliminary work was carried out to construct pseudo-ternary phase diagrams for oleyl laurate, oleyl stearate and oleyl oleate with surfactants and piroxicam. Then, the preparation and optimization study via 'One-At-A-Time Approach' were carried out to determine the optimum amount of oil, surfactants and stabilizer using low-energy emulsification method. The results revealed that multi-phase region dominated the three pseudo-ternary phase diagrams. A composition was chosen from each multi-phase region for preparing the nanoemulsions systems containing piroxicam by incorporating a hydrocolloid stabilizer. The results showed that the optimum amount (w/w) of oil for oleyl laurate nanoemulsions was 30 and 20 g (w/w) for oleyl stearate nanoemulsions and oleyl oleate nanoemulsions. For each nanoemulsions system, the amount of mixed surfactants and stabilizer needed for the emulsification to take place was found to be 10 and 0.5 g (w/w), respectively. The emulsification process via high-energy emulsification method successfully produced nano-sized range particles. The nanoemulsions systems passed the centrifugation test and freeze-thaw cycle with no phase failures, and stable for 3 months at various storage temperatures (3°C, 25°C and 45°C). The results proved that the prepared nanoemulsions system cannot be formed spontaneously, and thus, energy input was required to produce nano-sized range particles.
  17. Fulltext Effect of compositions in nanostructured lipid carriers (NLC) on skin hydration and occlusion
    Loo Ch, Basri M, Ismail R, Lau H, Tejo B, Kanthimathi M, et al.
    Int J Nanomedicine, 2013;8:13-22.
    PMID: 23293516 DOI: 10.2147/IJN.S35648
    To study the effects of varying lipid concentrations, lipid and oil ratio, and the addition of propylene glycol and lecithin on the long-term physical stability of nanostructured lipid nanocarriers (NLC), skin hydration, and transepidermal water loss.
  18. Preparation of emulsions by rotor-stator homogenizer and ultrasonic cavitation for the cosmeceutical industry
    Han NS, Basri M, Abd Rahman MB, Abd Rahman RN, Salleh AB, Ismail Z
    J Cosmet Sci, 2012 Sep-Oct;63(5):333-44.
    PMID: 23089355
    Oil-in-water (O/W) nanoemulsions play an important key role in transporting bioactive compounds into a range of cosmeceutical products to the skin. Small droplet sizes have an inherent stability against creaming, sedimentation, flocculation, and coalescence. O/W emulsions varying in manufacturing process were prepared. The preparation and characterization of O/W nanoemulsions with average diameters of as low as 62.99 nm from palm oil esters were carried out. This was achieved using rotor-stator homogenizer and ultrasonic cavitation. Ultrasonic cell was utilized for the emulsification of palm oil esters and water in the presence of mixed surfactants, Tween 80 and Span 80 emulsions with a mean droplet size of 62.99 nm and zeta potential value at -37.8 mV. Results were comparable with emulsions prepared with rotor-stator homogenizer operated at 6000 rpm for 5 min. The stability of the emulsions was evaluated through rheology measurement properties. This included non-Newtonian viscosity, elastic modulus G', and loss modulus G″. A highly stable emulsion was prepared using ultrasonic cavitation comprising a very small particle size with higher zeta potential value and G' > G″ demonstrating gel-like behavior.
  19. Fulltext Combination of oxyanion Gln114 mutation and medium engineering to influence the enantioselectivity of thermophilic lipase from Geobacillus zalihae
    Wahab RA, Basri M, Rahman MB, Rahman RN, Salleh AB, Leow TC
    Int J Mol Sci, 2012;13(9):11666-80.
    PMID: 23109876 DOI: 10.3390/ijms130911666
    The substitution of the oxyanion Q114 with Met and Leu was carried out to investigate the role of Q114 in imparting enantioselectivity on T1 lipase. The mutation improved enantioselectivity in Q114M over the wild-type, while enantioselectivity in Q114L was reduced. The enantioselectivity of the thermophilic lipases, T1, Q114L and Q114M correlated better with log p as compared to the dielectric constant and dipole moment of the solvents. Enzyme activity was good in solvents with log p < 3.5, with the exception of hexane which deviated substantially. Isooctane was found to be the best solvent for the esterification of (R,S)-ibuprofen with oleyl alcohol for lipases Q114M and Q114L, to afford E values of 53.7 and 12.2, respectively. Selectivity of T1 was highest in tetradecane with E value 49.2. Solvents with low log p reduced overall lipase activity and dimethyl sulfoxide (DMSO) completely inhibited the lipases. Ester conversions, however, were still low. Molecular sieves employed as desiccant were found to adversely affect catalysis in the lipase variants, particularly in Q114M. The higher desiccant loading also increased viscosity in the reaction and further reduced the efficiency of the lipase-catalyzed esterifications.
  20. Carbopol 934, 940 and Ultrez 10 as viscosity modifiers of palm olein esters based nano-scaled emulsion containing ibuprofen
    Abdullah GZ, Abdulkarim MF, Mallikarjun C, Mahdi ES, Basri M, Sattar MA, et al.
    Pak J Pharm Sci, 2013 Jan;26(1):75-83.
    PMID: 23261730
    Micro-emulsions and sometimes nano-emulsions are well known candidates to deliver drugs locally. However, the poor rheological properties are marginally affecting their acceptance pharmaceutically. This work aimed to modify the poor flow properties of a nano-scaled emulsion comprising palm olein esters as the oil phase and ibuprofen as the active ingredient for topical delivery. Three Carbopol ® resins: 934, 940 and Ultrez 10, were utilized in various concentrations to achieve these goals. Moreover, phosphate buffer and triethanolamine solutions pH 7.4 were used as neutralizing agents to assess their effects on the gel-forming and swelling properties of Carbopol ® 940. The addition of these polymers caused the produced nano-scaled emulsion to show a dramatic droplets enlargement of the dispersed globules, increased intrinsic viscosity, consistent zeta potential and transparent-to-opaque change in appearance. These changes were relatively influenced by the type and the concentration of the resin used. Carbopol ® 940 and triethanolamine appeared to be superior in achieving the proposed tasks compared to other materials. The higher the pH of triethanolamine solution, the stronger the flow-modifying properties of Carbopol ® 940. Transmission electron microscopy confirmed the formation of a well-arranged gel network of Carbopol ® 940, which was the major cause for all realized changes. Later in vitro permeation studies showed a significant decrease in the drug penetration, thus further modification using 10% w/w menthol or limonene as permeation promoters was performed. This resulted in in vitro and in vivo pharmacodynamics properties that are comparably higher than the reference chosen for this study.
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