Title: Discovery of Guanidine Derivatives from Buthus martensii Karsch with Metal-Binding and Cholinesterase Inhibition Properties Liu YM, Fan JJ, Wang LN Ref: Molecules, 26:, 2021 : PubMed
Two rare guanidine-type alkaloids, Buthutin A (1) and Buthutin B (2), along with two other compounds (3, 4), were isolated from Buthus martensii Karsch, and determined using extensive spectroscopic data analysis and high resolution-mass spectrometry. Compound 1 showed the most potent inhibition on AChE and BChE with IC(50) values of 7.83 +/- 0.06 and 47.44 +/- 0.95 microM, respectively. Kinetic characterization of compound 1 confirmed a mixed-type of AChE inhibition mechanism in accordance with the docking results, which shows its interaction with both catalytic active (CAS) and peripheral anionic (PAS) sites. The specific binding of compound 1 to PAS domain of AChE was also confirmed experimentally. Moreover, compounds 1 and 3 exhibited satisfactory biometal binding abilities toward Cu(2+), Fe(2+), Zn(2+) and Al(3+) ions. These results provide a new evidence for further development and utilization of B. martensii in health and pharmaceutical products.
        
Related information
Citations formats
Liu YM, Fan JJ, Wang LN (2021) Discovery of Guanidine Derivatives from Buthus martensii Karsch with Metal-Binding and Cholinesterase Inhibition Properties Molecules26: