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1.
Chinese Pharmacological Bulletin ; (12): 481-487, 2022.
Article in Chinese | WPRIM | ID: wpr-1014106

ABSTRACT

Organophosphorus pesticides ( OPP) and organophosphorus nerve agents ( OPNAs) are both toxic organophosphorus compounds, which mainly exert toxic effects through irreversible inhibition of acetylcholinesterase ( AChE).This paper takes protein adducts as the research objective, studying the covalent adducts formed by OPP/OPNAs and different target proteins:endogenous scavengers ( butyrylcholinesterase, albumin, transfer-rin) and low-dose toxicity related proteins ( Cytoskeleton pro- tein, neuropathic target esterase, ubiquitin ) .The formation mechanism of protein adducts and the structural characteristics of active sites are reviewed for providing new ideas to confirm the exposure, trace, and accurate treatment and reasonable prevention of OP poisons in the future.

2.
Acta Pharmaceutica Sinica ; (12): 873-878, 2009.
Article in Chinese | WPRIM | ID: wpr-344026

ABSTRACT

To explore new biflavones, 7-hydroxy-8-hydroxymethyl-4'-methoxyisoflavone (1), (5, 7-dihydroxyflavone-8-yl)-(7'-hydroxy-4"-methoxyisoflavone-8'-yl)methane (2), bis(7-hydroxy-4'-methoxyflavone-8-yl) methane (3), bis(3', 5'-diisopropyl-7, 4'-dihydroxy-isoflavone-8-yl)methane (4), and bis(7-hydroxy-isoflavone-8-yl) methane (5) were designed and synthesized from chrysin, formononetin, 7, 4'-dihydroxy-3', 5'-diisopropyl-isoflavone and 7-hydroxy-isoflavone. Their structures were identified with IR, 1H NMR, 13C NMR and elemental analysis. The binding of 1-5 with DNA was studied with fluorescent spectroscopy. Compounds 2-5 showed higher binding affinity with DNA than 1. According to the Stern-Volmer equation, the binding constants of 2, 3 were determined at 35 degrees C and 25 degrees C respectively, they were Kq2 (25 degrees C) = 1.95 x 10(4) Lx mol(-1) and Kq2 (35 degrees C) = 1.67 x 10(4) L x mol(-1); Kq3 (25 degrees C) = 1.89 x 10(4) L x mol(-1) and Kq3 (35 degrees C) = 1.58 x 10(4) L x mol(-1). The quenching mechanism of 2, 3 was suggested as static quenching.


Subject(s)
Biflavonoids , Chemistry , DNA , Chemistry , Flavonoids , Chemistry , Molecular Structure
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