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Authors = Chartchalerm Isarankura-Na-Ayudhya

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13 pages, 2157 KiB  
Article
Annexin A2 Improves the Osteogenic Differentiation of Mesenchymal Stem Cells Exposed to High-Glucose Conditions through Lessening the Senescence
by Parin Klabklai, Jitrada Phetfong, Rattanawan Tangporncharoen, Chartchalerm Isarankura-Na-Ayudhya, Tulyapruek Tawonsawatruk and Aungkura Supokawej
Int. J. Mol. Sci. 2022, 23(20), 12521; https://doi.org/10.3390/ijms232012521 - 19 Oct 2022
Cited by 13 | Viewed by 3038
Abstract
Osteoporosis is frequently found in chronic diabetic patients, and it results in an increased risk of bone fractures occurring. The underlying mechanism of osteoporosis in diabetic patients is still largely unknown. Annexin A2 (ANXA2), a family of calcium-binding proteins, has been reported to [...] Read more.
Osteoporosis is frequently found in chronic diabetic patients, and it results in an increased risk of bone fractures occurring. The underlying mechanism of osteoporosis in diabetic patients is still largely unknown. Annexin A2 (ANXA2), a family of calcium-binding proteins, has been reported to be involved in many biological process including bone remodeling. This study aimed to investigate the role of ANXA2 in mesenchymal stem cells (MSCs) during in vitro osteoinduction under high-glucose concentrations. Osteogenic gene expression, calcium deposition, and cellular senescence were determined. The high-glucose conditions reduced the osteogenic differentiation potential of the MSCs along with the lower expression of ANXA2. Moreover, the high-glucose conditions increased the cellular senescence of the MSCs as determined by senescence-associated β-galactosidase staining and the expression of p16, p21, and p53 genes. The addition of recombinant ANXA2 could recover the glucose-induced deterioration of the osteogenic differentiation of the MSCs and ameliorate the glucose-induced cellular senescence of the MSCs. A Western blot analysis revealed an increase in p53 and phosphorylated p53 (Ser 15), which was decreased by recombinant ANXA2 in MSC osteoblastic differentiation under high-glucose conditions. Our study suggested that the alteration of ANXA2 in high-glucose conditions may be one of the plausible factors in the deterioration of bones in diabetic patients by triggering cellular senescence. Full article
(This article belongs to the Special Issue Secondary Osteoporosis in Adults 3.0)
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14 pages, 278 KiB  
Article
Boiling, Blanching, and Stir-Frying Markedly Reduce Pesticide Residues in Vegetables
by Kamonrat Phopin, Sompon Wanwimolruk, Chosita Norkaew, Jaruwat Buddhaprom and Chartchalerm Isarankura-Na-Ayudhya
Foods 2022, 11(10), 1463; https://doi.org/10.3390/foods11101463 - 18 May 2022
Cited by 19 | Viewed by 3733
Abstract
Nowadays, a lot of produce (fruits and vegetables) sold in many countries are contaminated with pesticide residues, which cause severe effects on consumer health, such as cancer and neurological disorders. Therefore, this study aims to determine whether cooking processes can reduce the pesticide [...] Read more.
Nowadays, a lot of produce (fruits and vegetables) sold in many countries are contaminated with pesticide residues, which cause severe effects on consumer health, such as cancer and neurological disorders. Therefore, this study aims to determine whether cooking processes can reduce the pesticide residues in commonly consumed vegetables (Chinese kale and yard long beans) in Thailand. For cooking experiments, the two vegetables were cooked using three different processes: boiling, blanching, and stir-frying. After the treatments, all cooked and control samples were subjected to extraction and GC-MS/MS analysis for 88 pesticides. The results demonstrated that pesticide residues were reduced by 18–71% after boiling, 36–100% after blanching, and 25–60% after stir-frying for Chinese kale. For yard long beans, pesticide residues were reduced by 38–100% after boiling, 27–28% after blanching, and 35–63% after stir-frying. Therefore, cooking vegetables are proven to protect consumers from ingesting pesticide residues. Full article
(This article belongs to the Section Food Quality and Safety)
20 pages, 6461 KiB  
Article
Production and Characterization of Recombinant Wild Type Uricase from Indonesian Coelacanth (L. menadoensis) and Improvement of Its Thermostability by In Silico Rational Design and Disulphide Bridges Engineering
by Sakda Yainoy, Thanawat Phuadraksa, Sineewanlaya Wichit, Maprang Sompoppokakul, Napat Songtawee, Virapong Prachayasittikul and Chartchalerm Isarankura-Na-Ayudhya
Int. J. Mol. Sci. 2019, 20(6), 1269; https://doi.org/10.3390/ijms20061269 - 13 Mar 2019
Cited by 18 | Viewed by 6097
Abstract
The ideal therapeutic uricase (UOX) is expected to have the following properties; high expression level, high activity, high thermostability, high solubility and low immunogenicity. The latter property is believed to depend largely on sequence identity to the deduced human UOX (dH-UOX). Herein, we [...] Read more.
The ideal therapeutic uricase (UOX) is expected to have the following properties; high expression level, high activity, high thermostability, high solubility and low immunogenicity. The latter property is believed to depend largely on sequence identity to the deduced human UOX (dH-UOX). Herein, we explored L. menadoensis uricase (LM-UOX) and found that it has 65% sequence identity to dH-UOX, 68% to the therapeutic chimeric porcine-baboon UOX (PBC) and 70% to the resurrected ancient mammal UOX. To study its biochemical properties, recombinant LM-UOX was produced in E. coli and purified to more than 95% homogeneity. The enzyme had specific activity up to 10.45 unit/mg, which was about 2-fold higher than that of the PBC. One-litre culture yielded purified protein up to 132 mg. Based on homology modelling, we successfully engineered I27C/N289C mutant, which was proven to contain inter-subunit disulphide bridges. The mutant had similar specific activity and production yield to that of wild type (WT) but its thermostability was dramatically improved. Up on storage at −20 °C and 4 °C, the mutant retained ~100% activity for at least 60 days. By keeping at 37 °C, the mutant retained ~100% activity for 15 days, which was 120-fold longer than that of the wild type. Thus, the I27C/N289C mutant has potential to be developed for treatment of hyperuricemia. Full article
(This article belongs to the Special Issue Enzymes as Targets for Drug Development)
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21 pages, 2340 KiB  
Article
Molecular Docking of Aromatase Inhibitors
by Naravut Suvannang, Chanin Nantasenamat, Chartchalerm Isarankura-Na-Ayudhya and Virapong Prachayasittikul
Molecules 2011, 16(5), 3597-3617; https://doi.org/10.3390/molecules16053597 - 28 Apr 2011
Cited by 95 | Viewed by 16616
Abstract
Aromatase is an enzyme that plays a critical role in the development of estrogen receptor positive breast cancer. As aromatase catalyzes the aromatization of androstenedione to estrone, a naturally occurring estrogen, it is a promising drug target for therapeutic management. The undesirable effects [...] Read more.
Aromatase is an enzyme that plays a critical role in the development of estrogen receptor positive breast cancer. As aromatase catalyzes the aromatization of androstenedione to estrone, a naturally occurring estrogen, it is a promising drug target for therapeutic management. The undesirable effects found in aromatase inhibitors (AIs) that are in clinical use necessitate the discovery of novel AIs with higher selectivity, less toxicity and improving potency. In this study, we elucidate the binding mode of all three generations of AI drugs to the crystal structure of aromatase by means of molecular docking. It was demonstrated that the docking protocol could reliably reproduce the interaction of aromatase with its substrate with an RMSD of 1.350 Å. The docking study revealed that polar (D309, T310, S478 and M374), aromatic (F134, F221 and W224) and non-polar (A306, A307, V370, L372 and L477) residues were important for interacting with the AIs. The insights gained from the study herein have great potential for the design of novel AIs. Full article
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11 pages, 268 KiB  
Article
Bioactive Azafluorenone Alkaloids from Polyalthia debilis (Pierre) Finet & Gagnep.
by Supaluk Prachayasittikul, Patumporn Manam, Maneekarn Chinworrungsee, Chartchalerm Isarankura-Na-Ayudhya, Somsak Ruchirawat and Virapong Prachayasittikul
Molecules 2009, 14(11), 4414-4424; https://doi.org/10.3390/molecules14114414 - 3 Nov 2009
Cited by 49 | Viewed by 10799
Abstract
This study investigated bioactive extracts of Polyalthia debilis (Annonaceae) with antimicrobial, antimalarial and cytotoxic activities. Extensive chromatographic isolations provided azafluorenone alkaloids; onychine (1) and 7-methoxyonychine (2) together with a mixture of β–sitosterol and stigmasterol. The two alkaloids were isolated from the P. [...] Read more.
This study investigated bioactive extracts of Polyalthia debilis (Annonaceae) with antimicrobial, antimalarial and cytotoxic activities. Extensive chromatographic isolations provided azafluorenone alkaloids; onychine (1) and 7-methoxyonychine (2) together with a mixture of β–sitosterol and stigmasterol. The two alkaloids were isolated from the P. debilis for the first time. Isolated fractions containing a mixture of triterpenoids (C7, C8 and C9) exhibited the most potent antimicrobial activity against many bacterial strains with minimum inhibitory concentration of 64 μg/mL. Fractions with antimalarial and cytotoxic activities were also observed. The findings suggest the potential use of P. debilis in medicinal applications. Full article
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18 pages, 737 KiB  
Article
Synthesis and Theoretical Study of Molecularly Imprinted Nanospheres for Recognition of Tocopherols
by Theeraphon Piacham, Chanin Nantasenamat, Thummaruk Suksrichavalit, Charoenchai Puttipanyalears, Tippawan Pissawong, Supanee Maneewas, Chartchalerm Isarankura-Na-Ayudhya and Virapong Prachayasittikul
Molecules 2009, 14(8), 2985-3002; https://doi.org/10.3390/molecules14082985 - 12 Aug 2009
Cited by 42 | Viewed by 15564
Abstract
Molecular imprinting is a technology that facilitates the production of artificial receptors toward compounds of interest. The molecularly imprinted polymers act as artificial antibodies, artificial receptors, or artificial enzymes with the added benefit over their biological counterparts of being highly durable. In this [...] Read more.
Molecular imprinting is a technology that facilitates the production of artificial receptors toward compounds of interest. The molecularly imprinted polymers act as artificial antibodies, artificial receptors, or artificial enzymes with the added benefit over their biological counterparts of being highly durable. In this study, we prepared molecularly imprinted polymers for the purpose of binding specifically to tocopherol (vitamin E) and its derivative, tocopherol acetate. Binding of the imprinted polymers to the template was found to be two times greater than that of the control, non-imprinted polymers, when using only 10 mg of polymers. Optimization of the rebinding solvent indicated that ethanol-water at a molar ratio of 6:4 (v/v) was the best solvent system as it enhanced the rebinding performance of the imprinted polymers toward both tocopherol and tocopherol acetate with a binding capacity of approximately 2 mg/g of polymer. Furthermore, imprinted nanospheres against tocopherol was successfully prepared by precipitation polymerization with ethanol-water at a molar ratio of 8:2 (v/v) as the optimal rebinding solvent. Computer simulation was also performed to provide mechanistic insights on the binding mode of template-monomer complexes. Such polymers show high potential for industrial and medical applications, particularly for selective separation of tocopherol and derivatives. Full article
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20 pages, 371 KiB  
Article
Modeling the LPS Neutralization Activity of Anti-Endotoxins
by Chadinee Thippakorn, Thummaruk Suksrichavalit, Chanin Nantasenamat, Tanawut Tantimongcolwat, Chartchalerm Isarankura-Na-Ayudhya, Thanakorn Naenna and Virapong Prachayasittikul
Molecules 2009, 14(5), 1869-1888; https://doi.org/10.3390/molecules14051869 - 20 May 2009
Cited by 23 | Viewed by 11899
Abstract
Bacterial lipopolysaccharides (LPS), also known as endotoxins, are major structural components of the outer membrane of Gram-negative bacteria that serve as a barrier and protective shield between them and their surrounding environment. LPS is considered to be a major virulence factor as it [...] Read more.
Bacterial lipopolysaccharides (LPS), also known as endotoxins, are major structural components of the outer membrane of Gram-negative bacteria that serve as a barrier and protective shield between them and their surrounding environment. LPS is considered to be a major virulence factor as it strongly stimulates the secretion of pro-inflammatory cytokines which mediate the host immune response and culminating in septic shock. Quantitative structure-activity relationship studies of the LPS neutralization activities of anti-endotoxins were performed using charge and quantum chemical descriptors. Artificial neural network implementing the back-propagation algorithm was selected for the multivariate analysis. The predicted activities from leave-one-out cross-validation were well correlated with the experimental values as observed from the correlation coefficient and root mean square error of 0.930 and 0.162, respectively. Similarly, the external testing set also yielded good predictivity with correlation coefficient and root mean square error of 0.983 and 0.130. The model holds great potential for the rational design of novel and robust compounds with enhanced neutralization activity. Full article
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21 pages, 277 KiB  
Article
Vasorelaxant and Antioxidant Activities of Spilanthes acmella Murr.
by Orapin Wongsawatkul, Supaluk Prachayasittikul, Chartchalerm Isarankura-Na-Ayudhya, Jutamaad Satayavivad, Somsak Ruchirawat and Virapong Prachayasittikul
Int. J. Mol. Sci. 2008, 9(12), 2724-2744; https://doi.org/10.3390/ijms9122724 - 18 Dec 2008
Cited by 84 | Viewed by 15987
Abstract
This study reports the effect of Spilanthes acmella Murr. extracts on phenylephrine-induced contraction of rat thoracic aorta as well as their antioxidant activity. Results show that the extracts exert maximal vasorelaxations in a dose-dependent manner, but their effects are less than acetylcholine-induced nitric [...] Read more.
This study reports the effect of Spilanthes acmella Murr. extracts on phenylephrine-induced contraction of rat thoracic aorta as well as their antioxidant activity. Results show that the extracts exert maximal vasorelaxations in a dose-dependent manner, but their effects are less than acetylcholine-induced nitric oxide (NO) vasorelaxation. Significant reduction of vasorelaxations is observed in both NG-nitro-L-arginine methyl ester (L-NAME) and indomethacin (INDO). In the presence of L-NAME plus INDO, synergistic effects are observed, leading to loss of vasorelaxation of both acetylcholine and the extracts. Similarly, the vasorelaxations of the extracts are completely abolished upon the removal of endothelial cells. This demonstrates that the extracts exhibit vasorelaxation via partially endothelium-induced NO and prostacyclin in a dose-dependent manner. Significantly, the ethyl acetate extract exerts immediate vasorelaxation (ED50 76.1 ng/mL) and is the most potent antioxidant (DPPH assay). The chloroform extract shows the highest vasorelaxation and antioxidation (SOD assay). These reveal a potential source of vasodilators and antioxidants. Full article
(This article belongs to the Section Biochemistry)
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15 pages, 356 KiB  
Article
Computational Insights on Sulfonamide Imprinted Polymers
by Chartchalerm Isarankura-Na-Ayudhya, Chanin Nantasenamat, Prasit Buraparuangsang, Theeraphon Piacham, Lei Ye, Leif Bülow and Virapong Prachayasittikul
Molecules 2008, 13(12), 3077-3091; https://doi.org/10.3390/molecules13123077 - 10 Dec 2008
Cited by 33 | Viewed by 16323
Abstract
Molecular imprinting is one of the most efficient methods for preparing synthetic receptors that possess user defined recognition properties. Despite general success of non-covalent imprinting for a large variety of templates, some groups of compounds remain difficult to tackle due to their structural [...] Read more.
Molecular imprinting is one of the most efficient methods for preparing synthetic receptors that possess user defined recognition properties. Despite general success of non-covalent imprinting for a large variety of templates, some groups of compounds remain difficult to tackle due to their structural complexity. In this study we investigate preparation of molecularly imprinted polymers that can bind sulfonamide compounds, which represent important drug candidates. Compared to the biological system that utilizes metal coordinated interaction, the imprinted polymer provided pronounced selectivity when hydrogen bond interaction was employed in an organic solvent. Computer simulation of the interaction between the sulfonamide template and functional monomers pointed out that although methacrylic acid had strong interaction energy with the template, it also possessed high non-specific interaction with the solvent molecules of tetrahydrofuran as well as being prone to self-complexation. On the other hand, 1-vinyl-imidazole was suitable for imprinting sulfonamides as it did not cross-react with the solvent molecules or engage in self-complexation structures. Full article
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17 pages, 578 KiB  
Article
Copper Complexes of Nicotinic-Aromatic Carboxylic Acids as Superoxide Dismutase Mimetics
by Thummaruk Suksrichavalit, Supaluk Prachayasittikul, Theeraphon Piacham, Chartchalerm Isarankura-Na-Ayudhya, Chanin Nantasenamat and Virapong Prachayasittikul
Molecules 2008, 13(12), 3040-3056; https://doi.org/10.3390/molecules13123040 - 8 Dec 2008
Cited by 92 | Viewed by 19662
Abstract
Nicotinic acid (also known as vitamin B3) is a dietary element essential for physiological and antihyperlipidemic functions. This study reports the synthesis of novel mixed ligand complexes of copper with nicotinic and other select carboxylic acids (phthalic, salicylic and anthranilic acids). The tested [...] Read more.
Nicotinic acid (also known as vitamin B3) is a dietary element essential for physiological and antihyperlipidemic functions. This study reports the synthesis of novel mixed ligand complexes of copper with nicotinic and other select carboxylic acids (phthalic, salicylic and anthranilic acids). The tested copper complexes exhibited superoxide dismutase (SOD) mimetic activity and antimicrobial activity against Bacillus subtilis ATCC 6633, with a minimum inhibition concentration of 256 μg/mL. Copper complex of nicotinic-phthalic acids (CuNA/Ph) was the most potent with a SOD mimetic activity of IC50 34.42 μM. The SOD activities were observed to correlate well with the theoretical parameters as calculated using density functional theory (DFT) at the B3LYP/LANL2DZ level of theory. Interestingly, the SOD activity of the copper complex CuNA/Ph was positively correlated with the electron affinity (EA) value. The two quantum chemical parameters, highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO), were shown to be appropriate for understanding the mechanism of the metal complexes as their calculated energies show good correlation with the SOD activity. Moreover, copper complex with the highest SOD activity were shown to possess the lowest HOMO energy. These findings demonstrate a great potential for the development of value-added metallovitamin-based therapeutics. Full article
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18 pages, 201 KiB  
Article
Antimicrobial and Antioxidative Activities of Bioactive Constituents from Hydnophytum formicarum Jack.
by Supaluk Prachayasittikul, Prasit Buraparuangsang, Apilak Worachartcheewan, Chartchalerm Isarankura-Na-Ayudhya, Somsak Ruchirawat and Virapong Prachayasittikul
Molecules 2008, 13(4), 904-921; https://doi.org/10.3390/molecules13040904 - 18 Apr 2008
Cited by 136 | Viewed by 15614
Abstract
Hydnophytum formicarum Jack. (Rubiaceae) is a medicinal plant whose tuberspossesses cardiovascular, anti-inflammatory and antiparasitic effects and have been usedfor the treatment of hepatitis, rheumatism and diarrhea. Herein we report the isolation of itsactive constituents and the testing of their antimicrobial activity against 27 [...] Read more.
Hydnophytum formicarum Jack. (Rubiaceae) is a medicinal plant whose tuberspossesses cardiovascular, anti-inflammatory and antiparasitic effects and have been usedfor the treatment of hepatitis, rheumatism and diarrhea. Herein we report the isolation of itsactive constituents and the testing of their antimicrobial activity against 27 strains ofmicroorganisms using an agar dilution method and of their antioxidative activity using theDPPH and SOD assays. The results show that the crude hexane, dichloromethane, ethylacetate and methanol extracts exert such activities. Particularly, the crude ethyl acetateextract exhibits antigrowth activity against many Gram-positive and Gram-negativebacteria with MIC 256 μg/mL. Shewanella putrefaciens ATCC 8671 is completelyinhibited at a lower MIC (128 μg/mL). Interestingly, Corynebacterium diphtheriae NCTC10356 is inhibited by all the tested extracts. Significantly, the ethyl acetate extract is alsothe most potent antioxidant, showing 83.31% radical scavenging activity with IC50 8.40μg/mL in the DPPH assay. The other extracts display weak to moderate antioxidativeMolecules 2008, 13905activities, ranging from 28.60-56.80% radical scavenging. The SOD assay shows thatmethanol extract exhibits the highest activity (74.19% inhibition of superoxide radical).The dichloromethane and ethyl acetate extracts display comparable SOD activity. Thepromising bioactivities of the crude ethyl acetate extract guided the first isolation ofbioactive flavonoid and phenolic compounds: isoliquiritigenin (2), protocatechualdehyde(3), butin (4) and butein (5) from this species. Their structures have been fully establishedby 1D and 2D NMR. In addition, stigmasterol was isolated from the crude hexane anddichloromethane extracts. The antimicrobial and cytotoxic activities of compounds 3-5were evaluated. The tested compounds were inactive against HuCCA-1 and KB cell lines,showing ED50> 10 μg/mL. Protocatechualdehyde (3) completely inhibits the growth ofPlesiomonas shigelloides with MIC ≤60 μg/mL. As a result, we propose that Hydnophytumformicarum Jack. can serve as a new source enriched with potent antioxidative andantimicrobial agents. Full article
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