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beta-Secretase (BACE1) inhibitors from pomegranate (Punica granatum) husk.
Arch Pharm Res. 2005 Dec; 28(12):1328-32.AP

Abstract

In the course of screening for anti-dementia agents from natural products, two beta-secretase (BACE1) inhibitors were isolated from the husk of pomegranate (Punica granatum) by activity-guided purification. They were identified as ellagic acid and punicalagin with IC50 values of 3.9 x10(-6) and 4.1x10(-7) M and Ki values of 2.4x10(-5) and 5.9x10(-7) M, respectively. The compounds were non-competitive inhibitors with a substrate in the Dixon plot. Ellagic acid and punicalagin were less inhibitory to alpha-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, thus indicating that they were relatively specific inhibitors of BACE1.

Authors+Show Affiliations

Kwak HM
School of Applied Biosciences, College of Agriculture and Life Sciences, Kyungpook National University, Daegu, Korea.
Jeon SY
No affiliation info available
Sohng BH
No affiliation info available
Kim JG
No affiliation info available
Lee JM
No affiliation info available
Lee KB
No affiliation info available
Jeong HH
No affiliation info available
Hur JM
No affiliation info available
Kang YH
No affiliation info available
Song KS
No affiliation info available

MeSH

AcetatesAmyloid Precursor Protein SecretasesAspartic Acid EndopeptidasesButanolsCatechinDose-Response Relationship, DrugEllagic AcidEndopeptidasesEnzyme InhibitorsFruitHumansHydrolyzable TanninsLythraceaePlant ExtractsPlants, MedicinalSubstrate Specificity

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

16392663

Citation

Kwak, Hye-Min, et al. "Beta-Secretase (BACE1) Inhibitors From Pomegranate (Punica Granatum) Husk." Archives of Pharmacal Research, vol. 28, no. 12, 2005, pp. 1328-32.
Kwak HM, Jeon SY, Sohng BH, et al. Beta-Secretase (BACE1) inhibitors from pomegranate (Punica granatum) husk. Arch Pharm Res. 2005;28(12):1328-32.
Kwak, H. M., Jeon, S. Y., Sohng, B. H., Kim, J. G., Lee, J. M., Lee, K. B., Jeong, H. H., Hur, J. M., Kang, Y. H., & Song, K. S. (2005). Beta-Secretase (BACE1) inhibitors from pomegranate (Punica granatum) husk. Archives of Pharmacal Research, 28(12), 1328-32.
Kwak HM, et al. Beta-Secretase (BACE1) Inhibitors From Pomegranate (Punica Granatum) Husk. Arch Pharm Res. 2005;28(12):1328-32. PubMed PMID: 16392663.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - beta-Secretase (BACE1) inhibitors from pomegranate (Punica granatum) husk. AU - Kwak,Hye-Min, AU - Jeon,So-Young, AU - Sohng,Bang-Ho, AU - Kim,Jong-Guk, AU - Lee,Jin-Man, AU - Lee,Kyung-Bok, AU - Jeong,Hyun-Hee, AU - Hur,Jong-Moon, AU - Kang,Young-Hwa, AU - Song,Kyung-Sik, PY - 2006/1/6/pubmed PY - 2006/2/8/medline PY - 2006/1/6/entrez SP - 1328 EP - 32 JF - Archives of pharmacal research JO - Arch Pharm Res VL - 28 IS - 12 N2 - In the course of screening for anti-dementia agents from natural products, two beta-secretase (BACE1) inhibitors were isolated from the husk of pomegranate (Punica granatum) by activity-guided purification. They were identified as ellagic acid and punicalagin with IC50 values of 3.9 x10(-6) and 4.1x10(-7) M and Ki values of 2.4x10(-5) and 5.9x10(-7) M, respectively. The compounds were non-competitive inhibitors with a substrate in the Dixon plot. Ellagic acid and punicalagin were less inhibitory to alpha-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, thus indicating that they were relatively specific inhibitors of BACE1. SN - 0253-6269 UR - https://www.unboundmedicine.com/medline/citation/16392663/beta_Secretase__BACE1__inhibitors_from_pomegranate__Punica_granatum__husk_ DB - PRIME DP - Unbound Medicine ER -