Two new arthropod toxins purified from the venom of the Mexican scorpion Centruroides nigrescens

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  Two new arthropod toxins purified from the venom of the Mexican scorpion Centruroides nigrescens Abstract The venom of the slender black scorpion Centruroides nigrescens , from the State of Guerrero México, was fractionated by Sephadex G–50 gel filtration, followed by carboxymethyl cellulose ion separation and high–performance liquid chromatography, permitting to obtain two new peptides toxic to arthropods. The estimate LD 50 of the soluble venom for the insect Acheta domesticus was 11.1 μg/g body weight, and for the arthropod Armadillidium vulgare was 61.1 μg body weight . The amino acid sequence of toxin Cnige1 (toxic to A. domesticus and A. vulgare ) contains 65 amino acids, with a molecular mass of 7273.37 mass units, whereas toxin Cnige2, toxic to A. domesticus , contains 68 amino acids, with a molecular mass of 7548.81 units. Both peptides are well packed, containing 8 cysteines, which in the native venoms are forming 4 disulfide bridges each. The amino acid sequences f...

Structural Optimization, Fungicidal Activities Evaluation and Structure-activity Relationship of Guanidine Derivatives from Buthus martensii Karsch

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Structural Optimization, Fungicidal Activities Evaluation and Structure-activity Relationship of Guanidine Derivatives from Buthus martensii Karsch

Abstract

A guanidine compound was isolated and identified from Buthus martensii Karsch. Based on its characteristic structure, we used it as a lead compound to carry out structural optimization and subsequent fungicidal evaluation. Here 18 guanidine derivatives were designed and synthesized by a facile method, and their structures were characterized by 1H, 13C NMR, and HRMS. Biological assay indicated that most of the title compounds possess potential fungicidal activities against Alternaria altanata, and Penicillium digitatum. Especially, 5a, 5d, and 5i showed inhibition rates (IR) of 41.9, 41.9, and 44.2% respectively against P. digitatum at a concentration of 25 mg/L, whose activities surpassed that of hymexazol. This is the first report on the active derivatives from B. martensii in application of plant protection, providing scientific references for the development and utilization of active ingredients from scorpions.

Zhu, T., Li, K., Huang, D. et al. Structural Optimization, Fungicidal Activities Evaluation and Structure-activity Relationship of Guanidine Derivatives from Buthus martensii Karsch. Russ J Org Chem 59 (Suppl 1), S101–S110 (2023). https://doi.org/10.1134/S1070428023130109