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[ $\beta$ ]-Secretase (BACE1) Inhibitors from Pomegranate (Punica granatum) Husk
Kwak Hye-Min,Jeon So-Young,Sohng Bang-Ho,Kim Jong-Guk,Lee Jin-Man,Lee Kyung-Bok,Jeong HyunHee,Hur Jong-Moon,Kang Young-Hwa,Song Kyung-Sik The Pharmaceutical Society of Korea 2005 Archives of Pharmacal Research Vol.28 No.12
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 $IC_{50}$ values of 3.9 $\times$$10^{-6}$ and 4.1$\times$$10^{-7}$ M and Ki values of 2.4$\times$$10^{-5}$and 5.9$\times$$10^{-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.
β-Secretase (BACE1) Inhibitors from Pomegranate (Punica granatum) Husk
Hye-Min Kwak,So-Young Jeon,Bang-Ho Sohng,Jong-Guk Kim,Jin-Man Lee,이경복,Hyun-Hee Jeong,Jong-Moon Hur,강영화,송경식 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.12
In the course of screening for anti-dementia agents from natural products, two β-secretase (BACE1) inhibitors were isolated from the husk of pomegranate (Punica granatum) by activityguided purification. They were identified as ellagic acid and punicalagin with IC50 values of 3.9 ×10-6 and 4.1×10-7 M and Ki values of 2.4×10-5 and 5.9×10-7 M, respectively. The compounds were non-competitive inhibitors with a substrate in the Dixon plot. Ellagic acid and punicalagin were less inhibitory to α-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, thus indicating that they were relatively specific inhibitors of BACE1.