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Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao) Flowers

The use of α-glucosidase inhibitors is considered to be an effective strategy in the treatment of diabetes. Using a bioassay-guided fractionation technique, five Bacillus stearothermophilus α-glucosidase inhibitors were isolated from the flowers of Musa spp. (Baxijiao). Using NMR spectroscopy analys...

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Autores principales: Sheng, Zhanwu, Dai, Haofu, Pan, Siyi, Wang, Hui, Hu, Yingying, Ma, Weihong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271520/
https://www.ncbi.nlm.nih.gov/pubmed/25045894
http://dx.doi.org/10.3390/molecules190710563
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author Sheng, Zhanwu
Dai, Haofu
Pan, Siyi
Wang, Hui
Hu, Yingying
Ma, Weihong
author_facet Sheng, Zhanwu
Dai, Haofu
Pan, Siyi
Wang, Hui
Hu, Yingying
Ma, Weihong
author_sort Sheng, Zhanwu
collection PubMed
description The use of α-glucosidase inhibitors is considered to be an effective strategy in the treatment of diabetes. Using a bioassay-guided fractionation technique, five Bacillus stearothermophilus α-glucosidase inhibitors were isolated from the flowers of Musa spp. (Baxijiao). Using NMR spectroscopy analysis they were identified as vanillic acid (1), ferulic acid (2), β-sitosterol (3), daucosterol (4) and 9-(4′-hydroxyphenyl)-2-methoxyphenalen-1-one (5). The half maximal inhibitory concentration (IC(50)) values of compounds 1–5 were 2004.58, 1258.35, 283.67, 247.35 and 3.86 mg/L, respectively. Compared to a known α-glucosidase inhibitor (acarbose, IC(50) = 999.31 mg/L), compounds 3, 4 and 5 showed a strong α-glucosidase inhibitory effect. A Lineweaver-Burk plot indicated that compound 5 is a mixed-competitive inhibitor, while compounds 3 and 4 are competitive inhibitors. The inhibition constants (K(i)) of compounds 3, 4 and 5 were 20.09, 2.34 and 4.40 mg/L, respectively. Taken together, these data show that the compounds 3, 4 and 5 are potent α-glucosidase inhibitors.
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spelling pubmed-62715202018-12-21 Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao) Flowers Sheng, Zhanwu Dai, Haofu Pan, Siyi Wang, Hui Hu, Yingying Ma, Weihong Molecules Article The use of α-glucosidase inhibitors is considered to be an effective strategy in the treatment of diabetes. Using a bioassay-guided fractionation technique, five Bacillus stearothermophilus α-glucosidase inhibitors were isolated from the flowers of Musa spp. (Baxijiao). Using NMR spectroscopy analysis they were identified as vanillic acid (1), ferulic acid (2), β-sitosterol (3), daucosterol (4) and 9-(4′-hydroxyphenyl)-2-methoxyphenalen-1-one (5). The half maximal inhibitory concentration (IC(50)) values of compounds 1–5 were 2004.58, 1258.35, 283.67, 247.35 and 3.86 mg/L, respectively. Compared to a known α-glucosidase inhibitor (acarbose, IC(50) = 999.31 mg/L), compounds 3, 4 and 5 showed a strong α-glucosidase inhibitory effect. A Lineweaver-Burk plot indicated that compound 5 is a mixed-competitive inhibitor, while compounds 3 and 4 are competitive inhibitors. The inhibition constants (K(i)) of compounds 3, 4 and 5 were 20.09, 2.34 and 4.40 mg/L, respectively. Taken together, these data show that the compounds 3, 4 and 5 are potent α-glucosidase inhibitors. MDPI 2014-07-18 /pmc/articles/PMC6271520/ /pubmed/25045894 http://dx.doi.org/10.3390/molecules190710563 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Sheng, Zhanwu
Dai, Haofu
Pan, Siyi
Wang, Hui
Hu, Yingying
Ma, Weihong
Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao) Flowers
title Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao) Flowers
title_full Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao) Flowers
title_fullStr Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao) Flowers
title_full_unstemmed Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao) Flowers
title_short Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao) Flowers
title_sort isolation and characterization of an α-glucosidase inhibitor from musa spp. (baxijiao) flowers
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271520/
https://www.ncbi.nlm.nih.gov/pubmed/25045894
http://dx.doi.org/10.3390/molecules190710563
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