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β-Secretase (BACE-1) inhibitory effect of biflavonoids
Sasaki H.a, Miki K.b, Kinoshita K.b, Koyama K.b, Juliawaty L.D.c, Achmad S.A.c, Hakim E.H.c, Kaneda M.a, Takahashi K.b
a School of Pharmacy, Shujitsu University, Japan
b Department of Pharmacognosy and Phytochemistry, Meiji Pharmaceutical University, Japan
c Natural Products Research Group, Department of Chemistry, Bandung Institute of Technology, Indonesia
[vc_row][vc_column][vc_row_inner][vc_column_inner][vc_separator css=”.vc_custom_1624529070653{padding-top: 30px !important;padding-bottom: 30px !important;}”][/vc_column_inner][/vc_row_inner][vc_row_inner layout=”boxed”][vc_column_inner width=”3/4″ css=”.vc_custom_1624695412187{border-right-width: 1px !important;border-right-color: #dddddd !important;border-right-style: solid !important;border-radius: 1px !important;}”][vc_empty_space][megatron_heading title=”Abstract” size=”size-sm” text_align=”text-left”][vc_column_text]Here, we describe amentoflavone-type biflavonoids, which were isolated from natural sources and were found to inhibit β-secretase (BACE-1). The structure-activity relationship was studied, and compounds 1-8, 10, 17, and 18 showed BACE-1 inhibitory activity. Among these compounds, 2,3- dihydroamentoflavone 17 and 2,3-dihydro-6-methylginkgetin 18 exhibited potent inhibitory effects with IC 50 values of 0.75 and 0.35 μM, respectively. © 2010 Elsevier Ltd. All rights reserved.[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Author keywords” size=”size-sm” text_align=”text-left”][vc_column_text][/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Indexed keywords” size=”size-sm” text_align=”text-left”][vc_column_text]β-Secretase,2,3-Dihydro-6-methylginkgetin,2,3-Dihydroamentoflavone,Alzheimer,Amentoflavone,BACE-1,Biflavonoid[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Funding details” size=”size-sm” text_align=”text-left”][vc_column_text]This research was partially supported by the Japan Society for the Promotion of Science (JSPS) AA Scientific Platform Program and a Grant from the High-Tech Research Center Project, Ministry of Education, Culture, Sports, Science and Technology (MEXT), Japan ( S0801043 ).[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”DOI” size=”size-sm” text_align=”text-left”][vc_column_text]https://doi.org/10.1016/j.bmcl.2010.06.021[/vc_column_text][/vc_column_inner][vc_column_inner width=”1/4″][vc_column_text]Widget Plumx[/vc_column_text][/vc_column_inner][/vc_row_inner][/vc_column][/vc_row][vc_row][vc_column][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][/vc_column][/vc_row]