| Autor: |
Kim JH; a Radiation Breeding Research Center, Advanced Radiation Technology Institute , Korea Atomic Energy Research Institute , Jeoungeup , Jeollabuk-do , Republic of Korea., Thao NP; b Institute of Marine Biochemistry (IMBC) , Vietnam Academy of Science and Technology (VAST) , Hanoi , Vietnam., Han YK; c College of Pharmacy, Chungnam National University , Daejeon , Republic of Korea., Lee YS; c College of Pharmacy, Chungnam National University , Daejeon , Republic of Korea., Luyen BTT; d Department of Pharmaceutical Industry , Hanoi University of Pharmacy , Hanoi , Vietnam., Oanh HV; d Department of Pharmaceutical Industry , Hanoi University of Pharmacy , Hanoi , Vietnam., Kim YH; c College of Pharmacy, Chungnam National University , Daejeon , Republic of Korea., Yang SY; c College of Pharmacy, Chungnam National University , Daejeon , Republic of Korea. |
| Abstrakt: |
Cholinesterases (ChEs) are enzymes that break down neurotransmitters associated with cognitive function and memory. We isolated cinnamic acids (1 and 2), indolinones (3 and 4), and cycloartane triterpenoid derivatives (5-19) from the roots of Cimicifuga dahurica (Turcz.) Maxim. by chromatography. These compounds were evaluated for their inhibitory activity toward ChEs. Compound 1 was determined to have an IC 50 value of 16.7 ± 1.9 μM, and to act as a competitive inhibitor of acetylcholinesterase (AChE). Compounds 3, 4 and 14 were found to be noncompetitive with IC 50 values of 13.8 ± 1.5 and 6.5 ± 2.5 μM, and competitive with an IC 50 value of 22.6 ± 0.4 μM, respectively, against butyrylcholinesterase (BuChE). Our molecular simulation suggested each key amino acid, Tyr337 of AChE and Asn228 of BuChE, which were corresponded with potential inhibitors 1, and 3 and 4, respectively. Compounds 1 and 4 were revealed to be promising compounds for inhibition of AChEs and BuChEs, respectively. |
