Discovery of polymethoxyflavones from black ginger (Kaempferia parviflora) as potential β-secretase (BACE1) inhibitors
详细信息 查看全文
- 作者：Kumju Youna ; Jinhyuk Leeb ; c ; Chi-Tang Hod ; Mira Juna ; mjun@dau.ac.kr" class="auth_mail" title="E-mail the corresponding author
- 关键词：Aβ ; β-amyloid peptide ; AD ; Alzheimer's disease ; APP ; Amyloid precursor protein ; BACE1 ; β-site amyloid precursor protein cleaving enzyme 1 ; BBB ; Blood&ndash ; brain barrier ; DMF ; 5 ; 7-dimethoxyflavone ; KP ; Kaempferia parviflora ; PMF ; 3 ; 5 ; 7 ; 3&prime ; 4&prime ; -pentamethoxyflavone ; TACE ; Tumour necrosis factor-α converting enzyme ; TMF ; 5 ; 7 ; 4&prime ; -trimethoxy-flavone
- 刊名：Journal of Functional Foods
- 出版年：2016
- 出版时间：January 2016
- 年：2016
- 卷：20
- 期：Complete
- 页码：567-574
- 全文大小：1429 K
文摘
- •
5,7-DMF, 5,7,4′-TMF, and 3,5,7,3′,4′-PMF were discovered as novel BACE1 specific inhibitors.
- •
DMF, TMF, and PMF suppressed BACE1 activity with IC50 value of 4.95 × 10−5 M, 3.69 × 10−5 M, and 5.98 × 10−5 M, respectively.
- •
DMF, TMF, and PMF were non-competitive inhibitors with a substrate interacted with allosteric sites of BACE1.