Discovery of Guanidine Derivatives from <i>Buthus martensii</i> Karsch with Metal-Binding and Cholinesterase Inhibition Properties
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 an...
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| Autores principales: | , , |
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| Formato: | article |
| Lenguaje: | EN |
| Publicado: |
MDPI AG
2021
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| Materias: | |
| Acceso en línea: | https://doaj.org/article/db96771a920a426bb04458520b1c6d77 |
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| Sumario: | 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-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 <b>1</b> to PAS domain of AChE was also confirmed experimentally. Moreover, compounds <b>1</b> and <b>3</b> exhibited satisfactory biometal binding abilities toward Cu<sup>2+</sup>, Fe<sup>2+</sup>, Zn<sup>2+</sup> and Al<sup>3+</sup> ions. These results provide a new evidence for further development and utilization of <i>B. martensii</i> in health and pharmaceutical products. |
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