Colorectal cancer, which is the third most common type of cancer diagnosed in both men and women, is the leading cause of cancer-related deaths worldwide. Cowanin is a pure compound extracted from Garcinia cowa Roxb., a tree species present in Thailand, Malaysia and Myanmar. The crude extract has been demonstrated to have antitumor activity, inflammation induction, antibacterial activity, anti-inflammatory activity and antimalarial activity. In the present study, the effects of cowanin on apoptosis induction and on the apoptosis-related and mitogen-activated protein kinase (MAPK) pathways were investigated in the LoVo human colorectal cancer cell line. The cytotoxicity of cowanin in LoVo cells was determined by MTT assay. Hoechst 33342 and JC‑1 staining were used to determine nuclear morphological changes and mitochondrial membrane potential, respectively. The expression levels of BCL2 apoptosis regulator (Bcl‑2) family, MAPK and AKT serine/threonine kinase 1 (Akt) pathway proteins following cowanin treatment were determined by western blot analysis. The results demonstrated that cowanin inhibited cell proliferation and induced cell death via the apoptosis pathway. Cowanin treatment increased BCL2 associated X (Bax) and decreased Bcl‑2 expression. In addition, cowanin activated caspase‑9, -7 and poly-ADP-ribose-polymerase expression. Furthermore, cowanin decreased the levels of phosphorylated extracellular signal-regulated kinase (p‑ERK), p‑Akt, p‑3‑phosphoinositide‑dependent protein kinase‑1, while it increased p‑p38 expression, thus resulting in the induction of apoptosis. In conclusion, cowanin inhibited cell proliferation and induced apoptosis of LoVo cells via the MAPK and Akt signaling pathways. Notably, inhibition of p38 by using a p38 inhibitor (SB203580) prevented the cowanin-induced apoptosis in LoVo cells. These results suggested that cowanin may be a potential candidate for the treatment of colorectal cancer and provided important information on the molecular mechanisms underlying its antitumor activity.
Ionic liquids (ILs) based ultrasonic-assisted extract has been applied for the extraction of essential oil from Persicaria minor leaves. The effects of temperature, sonication time, and particle size of the plant material on the yield of essential oil were investigated. Among the different ILs employed, 1-ethyl-3-methylimidazolium acetate was the most effective, providing a 9.55% yield of the essential oil under optimum conditions (70 ℃, 25 min, IL:hexane ratio of 7:10 (v/v), particle size 60-80 mesh). The performance of 1-ethyl-3-methylimidazolium acetate in the extraction was attributed to its low viscosity and ability to disintegrate the structural matrix of the plant material. The ability of 1-ethyl-3-methylimidazolium acetate was also confirmed using the conductor like-screening model for realistic solvents. This research proves that ILs can be used to extract essential oils from lignocellulosic biomass.
An ionic liquid, 1-n-butyl-3-methylimidazolium chloride (BmimCl) was blended with urea at 1:1 mole ratio to create a BmimCl/Urea mixture. The agarose/talc composite films containing the BmimCl/Urea mixture were then acquired through a gelation method. The weight ratio of agarose and talc was fixed at 4:1, while the content of BmimCl/Urea was varied from 0 to 10 wt % relative to the overall weight of the composite films. The tensile stress and modulus results showed the optimum BmimCl/Urea content in the composite film lies at 8 wt %. The talc particles are embedded in the agarose matrix and there are no pullouts for the composite films containing BmimCl/Urea as demonstrated by SEM micrographs. The addition of BmimCl/Urea increased the glass transition temperature of the composite films, however, the thermal decomposition temperature decreased drastically. FTIR and FT-Raman spectra indicated the existence of interaction between agarose and talc, which improves their interfacial adhesion. As a conclusion, a BmimCl/Urea mixture can be utilized as a coupling agent for agarose/talc composite films.
A preliminary report on the short-term use of Tioconazole for vaginal candidiasis is presented. The cure rate was found to be approximately 90% in mild degrees of the disease, with good patient compliance and minimal side effects. However no conclusion can be drawn for moderate or severe cases of the condition.
The efficacy of a 2.15% imidacloprid gel bait against laboratory strain Periplaneta americana and Blattella germanica
was evaluated under laboratory conditions. The susceptibility trend of both species towards imidacloprid was: adult male
< adult female < nymphs. All stages of both species were dead within 10 days in primary poisoning testing. Periplaneta
americana adult male (LT50 = 0.47 h; LT95 = 5.24 h) died fastest, while nymphs of B. germanica took the longest time to
reach 95% mortality (LT95 = 43.84 h). In indirect exposure via secondary poisoning, only adult males of P. americana (LT50
= 100.63 h) and B. germanica (LT50 = 54.66 h) obtained 50% mortality before the testing ended. No complete mortalities
were achieved in any stages of both species within 10 days of secondary poisoning testing. Therefore, imidacloprid gel
bait used in this study was able to cause complete mortalities within less than 2 days of 10-day primary poisoning testing
but less effective in the 10-day secondary poisoning testing.
Recent progress on highly tough and stretchable polymer networks has highlighted the potential of wearable electronic devices and structural biomaterials such as cartilage. For some given applications, a combination of desirable mechanical properties including stiffness, strength, toughness, damping, fatigue resistance, and self-healing ability is required. However, integrating such a rigorous set of requirements imposes substantial complexity and difficulty in the design and fabrication of these polymer networks, and has rarely been realized. Here, we describe the construction of supramolecular polymer networks through an in situ copolymerization of acrylamide and functional monomers, which are dynamically complexed with the host molecule cucurbit[8]uril (CB[8]). High molecular weight, thus sufficient chain entanglement, combined with a small-amount dynamic CB[8]-mediated non-covalent crosslinking (2.5 mol%), yields extremely stretchable and tough supramolecular polymer networks, exhibiting remarkable self-healing capability at room temperature. These supramolecular polymer networks can be stretched more than 100× their original length and are able to lift objects 2000× their weight. The reversible association/dissociation of the host-guest complexes bestows the networks with remarkable energy dissipation capability, but also facile complete self-healing at room temperature. In addition to their outstanding mechanical properties, the networks are ionically conductive and transparent. The CB[8]-based supramolecular networks are synthetically accessible in large scale and exhibit outstanding mechanical properties. They could readily lead to the promising use as wearable and self-healable electronic devices, sensors and structural biomaterials.
The aim of the present study was to test the hypothesis that the proliferation of a human osteoblast cell line (HOS cells) stimulated with hydroxyapatite (HA) may be regulated by nitric oxide (NO). The cells were cultured on the surface of HA. Medium or cells alone were used as controls. L-arginine, D-arginine, 7-NI (an nNOS inhibitor), L-NIL (an iNOS inhibitor), L-NIO (an eNOS inhibitor) or carboxy PTIO, a NO scavenger, was added in the HA-exposed cell cultures. The cells were also precoated with anti-human integrin alphaV antibody. The levels of nitrite were determined spectrophotometrically. Cell proliferation was assessed by colorimetric assay. The results showed increased nitrite production and cell proliferation by HA-stimulated HOS cells up to day 3 of cultures. Anti-integrin alphaV antibody, L-NIO, or carboxy PTIO suppressed, but L-arginine enhanced, nitrite production and cell proliferation of HA-stimulated HOS cells. The results of the present study suggest, therefore, that interaction between HA and HOS cell surface integrin alphaV molecule may activate eNOS to catalyze NO production which, in turn, may regulate the cell proliferation in an autocrine fashion.
The aim of the present study was to determine the effect of nitric oxide (NO) on the production of cyclic AMP (cAMP) by a human osteoblast cell line (HOS cells) stimulated with hydroxyapatite. Cells were cultured on the HA surfaces with or without the presence of NO donors (SNAP and NAP) for 3 days. The effect of adenylyl cyclase inhibitor (SQ22536), NO scavenger (carboxy PTIO) or endothelial nitric oxide synthase (eNOS) inhibitor (L-NIO), was assessed by adding these to the cultures of HA-stimulated HOS cells with or without the presence of SNAP. Furthermore, HOS cells were pre-treated with anti-human integrin alphaV antibody prior to culturing on HA surfaces with or without the presence of SNAP. The levels of cAMP and cGMP were determined from the 3-day culture supernatants. The results showed that the production of cAMP but not cGMP by HA-stimulated HOS cells was augmented by SNAP. SQ22536 and carboxy PTIO suppressed but L-NIO only partially inhibited the production of cAMP by HA-stimulated HOS cells with or without the presence of exogenous NO. Pre-treatment of the cells with anti-human integrin alphaV antibody suppressed the production of cAMP by HA-stimulated HOS cells with or without the presence of NO. Therefore, the results of the present study suggest that NO may up-regulate the production of cAMP, perhaps, by augmenting adenylyl cyclase activity initiated by the binding between HOS cell-derived integrin alphaV and HA surface.
Herein we propose an alternative way to distinguish ionic liquids from Coulombic-dominated salts, based not on their upper limit melting temperature (100 °C), but on the trend of their phase-forming abilities to create aqueous biphasic systems as a function of temperature, in which a wider plethora of interactions can be appraised.
Microtubule Targeting Agents (MTAs) including paclitaxel, colchicine and vinca alkaloids are widely used in the treatment of various cancers. As with most chemotherapeutic agents, adverse effects and drug resistance are commonly associated with the clinical use of these agents. Methyl 2-(5-fluoro-2-hydroxyphenyl)-1H- benzo[d]imidazole-5-carboxylate (MBIC), a benzimidazole derivative displays greater toxicity against various cancer compared to normal human cell lines. The present study, focused on the cytotoxic effects of MBIC against HeLa cervical cancer cells and possible actions on the microtubule assembly.
Three novel ruthenium(II) complexes of the general formula [Ru(II)(bpy)2
L]2+ were synthesized, where L =
1,10-phenanthroline derivatives of position 2 imidazole having 3,4-didecyloxy-phenyl (ddip), 3,4-ditetradecyloxy-phenyl
(dtip) and 3,4-dihexadecyloxy-phenyl (dhip). All complexes were characterized by elemental analysis, 1
H-NMR and ESI-MS.
Their photophysical properties have also been studied by UV-visible spectroscopy and fluorescence spectroscopy. The
complexes exhibit Ru(II) metal centered emission at approximately 610 nm in acetonitrile solution at room temperature. DNA
binding studies were carried out by UV-visible titration, luminescence titration and viscosity studies. The results indicated
that [Ru(bpy)2
(ddip)]2+ binds to CT-DNA by partial intercalation mode, while [Ru(bpy)2
(dtip)]2+ and [Ru(bpy)2
(dhip)]2+
bind intercalatively via extended ligands.
Imidazolinones are a family of herbicides that are used to control a broad range of weeds. Their high persistence and leaching potential make them probable risk to the ecosystems. In this study, biochar, the biomass-derived solid material, was produced from oil palm empty fruit bunches (EFB) and rice husk (RH) through pyrolysis process. Feedstock and pyrolysis variables can control biochar sorption capacity. Therefore, the present study attempts to evaluate effects of three pyrolysis variables (temperature, heating rate and retention time) on abilities of biochars for removal of imazapic and imazapyr herbicides from soil. Response surface methodology (RSM) was used for optimizing the variables to achieve maximum sorption performance of the biochars. Experimental data were interpreted accurately by quadratic models. Based on the results, sorption capacities of both biochars raised when temperature decreased to 300 °C, mainly because of increased biochars effective functionality in sorption of polar molecules. Heating rate of 3°C/min provided optimum conditions to maximize the sorption capacities of both biochars. Retention time of about 1 h and 3 h were found to be the best for EFB and RH biochars, respectively. EFB biochar was more efficient in removal of the herbicides, especially imazapyr due to its chemical composition and higher polarity index (0.42) rather than RH biochar (0.39). Besides, higher cation exchange capacity (CEC) values of EFB biochar (83.90 cmolc/kg) in comparison with RH biochar (70.73 cmolc/kg) represented its higher surface polarity effective in sorption of the polar herbicides.
β-Cyclodextrin-ionic liquid polymer (CD-ILP) was first synthesized by functionalized β-cyclodextrin (CD) with 1-benzylimidazole (BIM) to form monofunctionalized CD (βCD-BIMOTs) and was further polymerized using a toluene diisocyanate (TDI) linker to form insoluble CD-ILP (βCD-BIMOTs-TDI). The βCD-BIMOTs-TDI polymer was characterized using various tools and the results obtained were compared with those derived from the native β-cyclodextrin polymer (βCD-TDI). The SEM result shows that the presence of ionic liquid (IL) increases the pore size, while the thermo gravimetric analysis (TGA) result shows that the presence of IL increases the stability of the polymer. Meanwhile, Brunauer-Emmett-Teller (BET) results show that βCD-BIMOTs-TDI polymer has 1.254 m(2)/g surface areas and the Barret-Joyner-Halenda (BJH) pore size distribution result reveals that the polymer exhibits macropores with a pore size of 77.66 nm. Preliminary sorption experiments were carried out and the βCD-BIMOTs-TDI polymer shows enhanced sorption capacity and high removal towards phenols and As(V).
Several new substituted sulfonamide compounds were synthesized and their structures were confirmed by ¹H-NMR, ¹³C-NMR, FT-IR, and mass spectroscopy. The antibacterial activities of the synthesized compounds were screened against standard strains of six Gram positive and four Gram negative bacteria using the microbroth dilution assay. Most of the compounds studied showed promising activities against both types of bacteria.
Three 1-(2-hydroxyethyl)-3-alkylimidazolium chloride room temperature ionic liquids (ILs) [2OHimC(n)][Cl]; (n=0, 1, 4) have been synthesized from the appropriate imidazole precursors and characterized by IR and NMR spectroscopies and elemental analysis. Their anti-microbial activities were investigated using the well-diffusion method. The viabilities of Escherichia coli, Aeromonas hydrophila, Listeria monocytogenes and Salmonella enterica as a function of IL concentrations were studied. The minimal inhibitory concentrations (MICs) and EC₅₀ values for the present ILs were within the concentration range from 60 to 125 mM and 23 to 73 mM. The anti-microbial potencies of the present ILs were compared to a standard antibiotic, gentamicin. The finding affords additional perspective on the level of ILs toxicity to aquatic lifeforms and yet, this characteristic can be readily harnessed to detect microbial growth and activity.
Five formulated insecticides (lambda-cyhalothrin at 10 mg m⁻², bifenthrin at 50 mg m⁻², fipronil at 10 mg m⁻², fenitrothion at 50 mg m⁻², imidacloprid at 5 mg m⁻²) and one active ingredient (DDT at 500 mg m⁻²) were evaluated using a surface contact method against early and late instars and adults of two strains of the tropical bed bug, Cimex hemipterus (F.). Synergism of lambda-cyhalothrin and fipronil using piperonyl butoxide (PBO) was also assessed.
Unsymmetrically substituted sterically tuned Pd(II)–NHC complexes of the general formula [PdCl2(NHC)2] (NHC = 1-allyl-3-methylimidazolin-2-ylidene, 7; 1-allyl-3-butylimidazol-2-ylidene, 8; 1-benzyl-3-butyl imidazolin-2-ylidene, 9) were prepared through transmetallation from their corresponding Ag(I)–NHC complexes. The Pd complexes were structurally characterized by different spectroscopic and X-ray diffraction methods. Complexes 7 and 9 adopted a trans–anti arrangement of the NHC ligands, whereas complex 8 adopted a cis–syn arrangement. Preliminary antibiogram studies using Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) bacteria showed that Ag(I)–NHC complexes demonstrate higher activity compared with Pd(I)–NHC complexes. Furthermore, Pd(II)–NHC complexes were evaluated for their anticancer potential using the human colorectal cancer cell line. A higher anticancer activity was observed for complexes 8 and 9, with 26.5 and 6.6 mM IC50 values, respectively.
The continuous and sole dependence on imidazolinone (IMI) herbicides for weedy rice control has led to the evolution of herbicide resistance in weedy rice populations across various countries growing IMI herbicide-resistant rice (IMI-rice), including Malaysia. A comprehensive study was conducted to elucidate occurrence, level, and mechanisms endowing resistance to IMI herbicides in putative resistant (R) weedy rice populations collected from three local Malaysian IMI-rice fields. Seed bioassay and whole-plant dose-response experiments were conducted using commercial IMI herbicides. Based on the resistance index (RI) quantification in both experiments, the cross-resistance pattern of R and susceptible (S) weedy rice populations and control rice varieties (IMI-rice variety MR220CL2 and non-IMI-rice variety MR219) to imazapic and imazapyr was determined. A molecular investigation was carried out by comparing the acetohydroxyacid synthase (AHAS) gene sequences of the R and S populations and the MR220CL2 and MR219 varieties. The AHAS gene sequences of R weedy rice were identical to those of MR220CL2, exhibiting a Ser-653-Asn substitution, which was absent in MR219 and S plants. In vitro assays were conducted using analytical grade IMI herbicides of imazapic (99.3%) and imazapyr (99.6%) at seven different concentrations. The results demonstrated that the AHAS enzyme extracted from the R populations and MR220CL2 was less sensitive to IMI herbicides than that from S and MR219, further supporting that IMI herbicide resistance was conferred by target-site mutation. In conclusion, IMI resistance in the selected populations of Malaysian weedy rice could be attributed to a Ser-653-Asn mutation that reduced the sensitivity of the target site to IMI herbicides. To our knowledge, this study is the first to show the resistance mechanism in weedy rice from Malaysian rice fields.
Cyclodextrin-modified micellar electrokinetic chromatography (CD-MEKC) method was developed for simultaneous enantioseparation of three imidazole drugs namely tioconazole, isoconazole and fenticonazole. Three easily available and inexpensive cyclodextrins namely 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), 2-hydroxypropyl-γ-cyclodextrin (HP-γ-CD) and heptakis(2,6-di-O-methyl)-β-cyclodextrin (DM-β-CD) were evaluated to discriminate the six stereoisomers of the drugs. However, none of the three CDs gave a complete enantioseparation of the drugs. Effective enantioseparation of tioconazole, isoconazole and fenticonazole was achieved using a combination of 35 mM HP-γ-CD and 10 mM DM-β-CD as chiral selectors. The best separation using both HP-γ-CD and DM-β-CD (35 mM:10 mM) as chiral selectors were accomplished in background electrolyte (BGE) containing 35 mM phosphate buffer (pH 7.0), 50 mM sodium dodecyl sulfate (SDS) and 15% (v/v) acetonitrile at 27 kV and 30 °C with all peaks resolved in less than 15 min with resolutions, Rs 1.90-27.22 and peak efficiencies, N > 180 000. The developed method was linear over the concentration range of 25-200 mg l(-1) (r(2) > 0.998) and the detection limits (S/N = 3) of the three imidazole drugs were found to be 2.7-7.7 mg l(-1). The CD-MEKC method was successfully applied to the determination of the three imidazole drugs in spiked human urine sample and commercial cream formulation of tioconazole and isoconazole with good recovery (93.6-106.2%) and good RSDs ranging from 2.30-6.8%.
The restoration of mechanical properties is desired for creating the self-healing coatings with no corrosion capabilities. The encapsulation of epoxy resins is limited by various factors in urea and melamine formaldehyde microcapsules. An improved method was developed, where epoxy resin was encapsulated by individual wrapping of poly(melamine-formaldehyde) and poly(urea-formaldehyde) shell around emulsified epoxy droplets via oil-in-water emulsion polymerization method. The synthesized materials were characterized analytically. The curing of the epoxy was achieved by adding the [Ni/Co(2-MI)6].2NO3 as a latent hardener and iron acetylacetonate [Fe(acac)3] as a latent accelerator. Isothermal and non-isothermal differential scanning calorimetric analysis revealed lower curing temperature (Tonset = 116 °C) and lower activation energies (Ea ≈ 69-75 kJ/mol). The addition of microcapsules and complexes did not adversely alter the flexural strength and flexural modulus of the epoxy coatings. The adhesion strength of neat coating decreased from 6310.8 ± 31 to 4720.9 ± 60 kPa and percent healing increased from 50.83 to 67.45% in the presence of acetylacetonate complex at 10 wt% of microcapsules.