کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5559284 1561568 2017 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Inhibitory effects of serratene-type triterpenoids from Lycopodium complanatum on cholinesterases and β-secretase 1
موضوعات مرتبط
علوم زیستی و بیوفناوری علوم محیط زیست بهداشت، سم شناسی و جهش زایی
پیش نمایش صفحه اول مقاله
Inhibitory effects of serratene-type triterpenoids from Lycopodium complanatum on cholinesterases and β-secretase 1
چکیده انگلیسی


- Two new and eight known serratene-type triterpenoids were isolated from Lycopodium complanatum.
- Isolated compounds exerted as inhibition of cholinesterase (ChEs) and BACE1.
- BACE1 inhibitors (1 and 6) have beneficial therapeutic potential for AD.

Phytochemical investigation of Lycopodium complanatum whole plants led to the isolation of two new serratene-type triterpenoids (1 and 2) along with eight known triterpenoids (3-10). Their structures were established using 1D and 2D NMR spectroscopic techniques and mass spectrometry. These compounds did not inhibit acetylcholinesterases (AChE) and butyrylcholinesterase (BChE), but did inhibit β-secretase 1 (BACE1). Compounds 1 and 6 showed potent BACE1 inhibition with IC50 values of 2.79 ± 0.28 and 2.49 ± 0.12 μM, respectively. The kinetic study of BACE1 inhibition revealed that compound 1 showed competitive inhibition, whereas 6 showed mixed-type inhibition. Furthermore, molecular docking results showed that the tested inhibitors 1 and 6 exhibited good binding affinities toward BACE1, with binding energies of −8.8 and −10.3 kcal/mol, respectively.

167

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Chemico-Biological Interactions - Volume 274, 25 August 2017, Pages 150-157
نویسندگان
, , , , , , ,