BACE1 inhibitory effects of lavandulyl flavanones from Sophora flavescens
Abstract
In order to access beta-secretase (BACE1), and enzyme strongly implicated in the cause of Alzheimer's disease, inhibitors must possess sufficient lipophilicity to traverse two lipid bilayers. Current drug candidates, which are almost totally peptide-derived, are thus inefficient because cell permeability presents a serious limiting factor. In this study, lipophilic alkylated (C(10)-C(5)) flavanones from Sophora flavescens were examined for their inhibitory effects against beta-secretase. Lavandulyl flavanones (1, 2, 5, 6, and 8) showed potent beta-secretase inhibitory activities with IC(50)s of 5.2, 3.3, 8.4, 2.6, and 6.7microM, respectively, while no significant activity was observed in the corresponding hydrated lavandulyl flavanones (4 and 7) and prenylated flavanone (3). As we expected, lavandulyl flavanones reduced Abeta secretion dose-dependently in transfected human embryonic kidney (HEK-293) cells. In kinetic studies, all compounds screened were shown to be noncompetitive inhibitor.
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Drug distribution can be affected by herbs inducing or inhibiting plasma or transport protein binding of drugs.
“Drug distribution can also be affected with herbs inducing or inhibiting plasma or transport protein binding of drugs.”
From Phytotherapy: A promising approach for the treatment of Alzheimer's disease (2022) · cites this paper as [95]
At receptor sites, herbs can be antagonistic or supportive of drug-receptor interactions.
“At receptor sites, herbs can be antagonistic or supportive of drug-receptor interactions.”
From Phytotherapy: A promising approach for the treatment of Alzheimer's disease (2022) · cites this paper as [95]
Most herbal preparations share the same metabolic and transport proteins with conventional medications.
“most herbal preparations share the same metabolic and transport proteins with conventional medications”
From Phytotherapy: A promising approach for the treatment of Alzheimer's disease (2022) · cites this paper as [95]
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References 26 · Cited by 53
- Authors
- Hwang, E. M., Ryu, Y. B., Kim, H. Y., Kim, D.-G., Hong, S.-G., Lee, J. H., Curtis-Long, M. J., Jeong, S. H., Park, J.-Y., & Park, K. H.
- Affiliations
- Gyeongsang National University (KR)
- Corresponding author
- Park, Jae-Yong
- Park, Ki Hun
- Venue
- Bioorganic & Medicinal Chemistry
- Publisher
- Elsevier BV
- Published
- 2008-07
- Volume
- 16
- Issue
- 14
- Pages
- 6669-6674
- ISSN
- 0968-0896 (ISSN-L)
- OpenAlex
- W2080796087
- Cited by
- 53
- References
- 26
- Citations by year
- 2025: 1 · 2024: 3 · 2023: 2 · 2022: 2 · 2021: 5 · 2020: 1 · 2019: 1 · 2018: 5 · 2017: 4 · 2016: 3 · 2015: 4 · 2014: 2 · 2013: 2 · 2012: 6
- FWCI
- 1.64
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Bioorganic & Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Korea Science and Engineering Foundation (R13-2005-012-02002-0, R15-2003-012-02001-0)
- Ministry of Science and Technology, Taiwan
- Ministry of Education and Human Resources Development
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Bioactive natural compounds
- Health Sciences › Medicine › Physiology › Alzheimer's disease research and treatments
- Health Sciences › Medicine › Pharmacology › Synthesis of Organic Compounds
- Keywords
- BACE1 inhibition, beta-secretase, Sophora flavescens, Alzheimer's disease, membrane permeability, amyloid-beta secretion, non-competitive inhibition, enzyme kinetics
- MeSH terms
- Alzheimer Disease, Cell Line, Humans, Kinetics, Transfection, Aspartic Acid Endopeptidases, Amyloid beta-Protein Precursor, Inhibitory Concentration 50, Sophora, Flavanones, Amyloid Precursor Protein Secretases
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