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Discovery of Guanidine Derivatives from Buthus martensii Karsch with Metal-Binding and Cholinesterase Inhibition Properties.

ABSTRACT: 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 IC50 values of 7.83 ± 0.06 and 47.44 ± 0.95 μM, 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 Cu2+, Fe2+, Zn2+ and Al3+ ions. These results provide a new evidence for further development and utilization of B. martensii in health and pharmaceutical products.

SUBMITTER: Liu YM 

PROVIDER: S-EPMC8588048 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature

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Discovery of Guanidine Derivatives from <i>Buthus martensii</i> Karsch with Metal-Binding and Cholinesterase Inhibition Properties.

Liu Yu-Ming YM   Fan Jing-Jing JJ   Wang Li-Ning LN  

Molecules (Basel, Switzerland) 20211108 21

Two rare guanidine-type alkaloids, Buthutin A (<b>1</b>) and Buthutin B (<b>2</b>), along with two other compounds (<b>3</b>, <b>4</b>), were isolated from <i>Buthus martensii</i> Karsch, and determined using extensive spectroscopic data analysis and high resolution-mass spectrometry. Compound <b>1</b> showed the most potent inhibition on AChE and BChE with IC<sub>50</sub> values of 7.83 ± 0.06 and 47.44 ± 0.95 μM, respectively. Kinetic characterization of compound <b>1</b> confirmed a mixed-typ  ...[more]

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