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Triterpenes as uncompetitive inhibitors of α-glucosidase from flowers of Punica granatum L.
Nat Prod Res. 2014; 28(23):2191-4.NP

Abstract

The α-glucosidase and maltase inhibitory effects of Punica granatum L. flowers (PGF) were investigated. The methanol extract (PGFMe), n-hexane extract (PGFH), chloroform extract (PGFC) and the remaining water fraction (PGFW) were assayed for their α-glucosidase and maltase inhibitory effects. PGFW showed potent α-glucosidase inhibition with IC₅₀ of 0.8 μg/mL followed by PGFMe (IC₅₀ of 4.0 μg/mL) then PGFC (IC₅₀ of 5.21 μg/mL) in comparison to acarbose (0.9 μM). Due to its selectivity towards α-glucosidase, PGFC was subjected to bioactivity-guided isolation of its main active constituents. Five known compounds (1-5) were identified as β-sitosterol (1), oleanolic acid (2), ursolic acid (3), p-coumaric acid (4) and apigenin (5). Ursolic and oleanolic acids showed potent α-glucosidase inhibition (IC₅₀ of 39.0 and 35.0 μM, respectively), while they did not show significant maltase inhibition. Kinetic study using the double Lineweaver-Burk plot revealed that ursolic acid uncompetitively inhibited α-glucosidase in comparison with acarbose as a competitive inhibitor.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Salah El Dine R
a Department of Pharmacognosy , Faculty of Pharmacy, Cairo University , 11562 Cairo , Egypt.
Ma Q
No affiliation info available
Kandil ZA
No affiliation info available
El-Halawany AM
No affiliation info available

MeSH

Coumaric AcidsDose-Response Relationship, DrugFlowersGlycoside Hydrolase InhibitorsHypoglycemic AgentsLythraceaeOleanolic AcidPropionatesSitosterolsTriterpenesalpha-Glucosidases

Pub Type(s)

Journal Article

Language

eng

PubMed ID

24956202

Citation

Salah El Dine, Riham, et al. "Triterpenes as Uncompetitive Inhibitors of Α-glucosidase From Flowers of Punica Granatum L." Natural Product Research, vol. 28, no. 23, 2014, pp. 2191-4.
Salah El Dine R, Ma Q, Kandil ZA, et al. Triterpenes as uncompetitive inhibitors of α-glucosidase from flowers of Punica granatum L. Nat Prod Res. 2014;28(23):2191-4.
Salah El Dine, R., Ma, Q., Kandil, Z. A., & El-Halawany, A. M. (2014). Triterpenes as uncompetitive inhibitors of α-glucosidase from flowers of Punica granatum L. Natural Product Research, 28(23), 2191-4. https://doi.org/10.1080/14786419.2014.928292
Salah El Dine R, et al. Triterpenes as Uncompetitive Inhibitors of Α-glucosidase From Flowers of Punica Granatum L. Nat Prod Res. 2014;28(23):2191-4. PubMed PMID: 24956202.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Triterpenes as uncompetitive inhibitors of α-glucosidase from flowers of Punica granatum L. AU - Salah El Dine,Riham, AU - Ma,Qiong, AU - Kandil,Zeinab A, AU - El-Halawany,Ali M, Y1 - 2014/06/23/ PY - 2014/6/24/entrez PY - 2014/6/24/pubmed PY - 2015/2/27/medline KW - Punica granatum flower; α-glucosidase KW - uncompetitive KW - ursolic acid SP - 2191 EP - 4 JF - Natural product research JO - Nat Prod Res VL - 28 IS - 23 N2 - The α-glucosidase and maltase inhibitory effects of Punica granatum L. flowers (PGF) were investigated. The methanol extract (PGFMe), n-hexane extract (PGFH), chloroform extract (PGFC) and the remaining water fraction (PGFW) were assayed for their α-glucosidase and maltase inhibitory effects. PGFW showed potent α-glucosidase inhibition with IC₅₀ of 0.8 μg/mL followed by PGFMe (IC₅₀ of 4.0 μg/mL) then PGFC (IC₅₀ of 5.21 μg/mL) in comparison to acarbose (0.9 μM). Due to its selectivity towards α-glucosidase, PGFC was subjected to bioactivity-guided isolation of its main active constituents. Five known compounds (1-5) were identified as β-sitosterol (1), oleanolic acid (2), ursolic acid (3), p-coumaric acid (4) and apigenin (5). Ursolic and oleanolic acids showed potent α-glucosidase inhibition (IC₅₀ of 39.0 and 35.0 μM, respectively), while they did not show significant maltase inhibition. Kinetic study using the double Lineweaver-Burk plot revealed that ursolic acid uncompetitively inhibited α-glucosidase in comparison with acarbose as a competitive inhibitor. SN - 1478-6427 UR - https://www.unboundmedicine.com/medline/citation/24956202/Triterpenes_as_uncompetitive_inhibitors_of_α_glucosidase_from_flowers_of_Punica_granatum_L_ DB - PRIME DP - Unbound Medicine ER -