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RISS 인기검색어
- 검색키워드
- 저자 : Sirichai Adisakwattana (검색결과 4 건)
- 무료
- 기관 내 무료
- 유료
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Synthesis of N-phenylphthalimide Derivatives as ${\alpha}-Glucosidase$ Inhibitors
Pluempanupat, Wanchai,Adisakwattana, Sirichai,Yibchok-Anun, Sirintorn,Chavasiri, Warinthorn 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12
Sixteen N-phenylphthalimide derivatives were synthesized and their ability to inhibit ${\alpha}-glucosidase$ was investigated. N-(2,4-dinitrophenyl)phthalimide was a potent inhibitor of yeast ${\alpha}-glucosidase\;(IC_{50};\;0.158{\pm}0.005mM)\;and\;maltase\;(IC_{50};\;0.051{\pm}0.008mM)$, whereas it did not inhibit sucrase. From a Lineweaver-Burk plot of ${\alpha}-glucosidase$ kinetics, N-(2,4-dichlorophenyl)phthalimide was found to be a competitive inhibitor of yeast ${\alpha}-glucosidase$. These results indicate that N-(2,4-dinitrophenyl)phthalimide could be a representative of a new group of ${\alpha}-glucosidase$ inhibitors.
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Synthesis of N-phenylphthalimide Derivatives as α-Glucosidase Inhibitors
Wanchai Pluempanupat,Sirichai Adisakwattana,Sirintorn Yibchok-Anun,Warinthorn Chavasiri 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12
Sixteen N-phenylphthalimide derivatives were synthesized and their ability to inhibit α-glucosidase was investigated. N-(2,4-dinitrophenyl)phthalimide was a potent inhibitor of yeast α-glucosidase (IC50; 0.158 ± 0.005 mM) and maltase (IC50; 0.051 ± 0.008 mM), whereas it did not inhibit sucrase. From a Lineweaver-Burk plot of α-glucosidase kinetics, N-(2,4-dichlorophenyl) phthalimide was found to be a competitive inhibitor of yeast α-glucosidase. These results indicate that N-(2,4-dinitrophenyl)phthalimide could be a representative of a new group of α- glucosidase inhibitors.
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Pasukamonset, Porntip,Kwon, Oran,Adisakwattana, Sirichai Elsevier 2016 Food hydrocolloids Vol.61 No.-
<P><B>Abstract</B></P> <P>Microencapsulation of phenolic extracts of <I>Clitoria ternatea</I> (CT) petal flower extract through extrusion method of alginate with calcium chloride (CaCl<SUB>2</SUB>) was studied. Encapsulation efficiency varied in the range from 74.17 ± 0.83% to 84.87 ± 0.29% depending on the percentage of CT (5–20%), alginate (1–2%), and CaCl<SUB>2</SUB> (1.5–5%). The results showed that the optimized condition of CT-loaded alginate beads (CT beads) was as follows: 10% CT, 1.5% alginate, and 3% CaCl<SUB>2</SUB> (w/v). Under this condition, the maximal antioxidant capacity of 11.76 ± 0.07 mg gallic acid equivalent/g<SUB>beads</SUB> and the encapsulation efficiency of 84.83 ± 0.40% were obtained. The microencapsulation was found to have smooth surface shape with a particle size distribution of 985 ± 0.53 μm and improve the thermal stability with 188 °C. There was the absence of chemical interactions between CT and alginate as verified by using FT-IR. The microencapsulation of CT significantly retains higher amount of polyphenols and improves antioxidant capacity, pancreatic α-amylase inhibitory activity, and bile acid binding after the gastrointestinal digestion. This study provides a novel food-grade encapsulation formulation to improve the stability as well as the biological activity of plant polyphenols.</P> <P><B>Highlights</B></P> <P> <UL> <LI> CT was encapsulated in calcium alginate beads. </LI> <LI> Encapsulated CT retained polyphenols and antioxidant activity. </LI> <LI> Encapsulating CT increased pancreatic α-amylase inhibitory activity after digestion. </LI> <LI> Encapsulating CT increased bile acid binding after digestion. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
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Park, Soo-yeon,Jin, Bora,Shin, Jae-Ho,Adisakwattana, Sirichai,Kwon, Oran EDITIONS SCIENTIFIQUES ELSEVIER 2017 BIOMEDICINE AND PHARMACOTHERAPY Vol.92 No.-
<P><B>Abstract</B></P> <P>Abnormalities in the hyperbolic relationship between insulin sensitivity and insulin secretion may cause oxidative stress and non-enzymatic glycation, resulting in an increased risk of type 2 diabetes. Here, we performed a 14-week study to investigate the effects of ethanolic extract of <I>Mori ramulus</I> (MRE; 0, 800, and 1600mg/kg body weight) and its signature component oxyresveratrol (OXY; 800mg/kg body weight) on β-cell dysfunction and insulin resistance in C57BLKS/J db/db mice fed with a high-fat diet. Compared with the diabetic control group, the high-dose MRE group showed a significant decrease in fasting blood glucose (<I>p</I> =0.0024); a significant increase in insulin secretion as measured by insulin (<I>p</I> =0.0012) and C-peptide (<I>p</I> =0.0103) levels in plasma and insulin content (<I>p</I> =0.0440) and homeobox factor-1 protein expression (<I>p</I> =0.0148) in the pancreas; and a significant increase in insulin sensitivity as measured by insulin receptor mRNA expression in the liver (<I>p</I> =0.0179) and adipose tissue (<I>p</I> =0.0491). In addition, improvements in the reactive oxygen species level and inflammatory pancreatic and hepatic tissue damage were also observed in the MRE group as assessed by histological findings. A similar but weaker effect was found in the OXY group. Furthermore, we observed a potentiating effect of MRE and OXY on insulin secretion in INS-1 cells in the presence of 27mM glucose, together with an anti-glycation effect as indicated by methylglyoxal-trapping capacity and inhibition of advanced glycation end-product formation. Taken together, these data suggest that MRE could ameliorate β-cell dysfunction and insulin resistance by reducing oxidative damage and advanced glycation end-product (Wagenknecht et al., 2003) formation and that these effects are due, at least in part, to OXY.</P>
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