Synthesis and Anti-Tobacco Mosaic Virus/Fungicidal/Insecticidal/Antitumor Bioactivities of Natural Product Hemigossypol and Its Derivatives.
J Agric Food Chem
; 69(4): 1224-1233, 2021 Feb 03.
Article
em En
| MEDLINE
| ID: mdl-33480687
ABSTRACT
To further study the structure-activity relationship of gossypol, hemigossypol (1) and its derivatives (2-23) were successfully designed via structure simplification and chemically synthesized. The anti-tobacco mosaic virus (TMV), fungicidal, and insecticidal activities of them were tested systematically. Most of these derivatives exhibited excellent anti-TMV activity. Furthermore, these compounds also exhibited broad-spectrum fungicidal activities against 14 kinds of phytopathogenic fungi. In particular, hemigossypol acid lactone (7) was stable in the air. In terms of biological activity, it not only showed anti-TMV activity (inhibitory rates of 70.3, 65.4 and 72.4% at 500 µg/mL for inactivation, curative, and protection activity in vivo, respectively) comparable to ningnanmycin but also exhibited higher insecticidal activity against mosquito larvae (60%/0.25 mg/kg) than the commercial species rotenone. None of hemigossypol and the tested derivatives showed antitumor activities.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Fungicidas Industriais
/
Inseticidas
/
Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
J Agric Food Chem
Ano de publicação:
2021
Tipo de documento:
Article