Insecticidal and cytotoxic effects of natural and hemisynthetic destruxins.
The insecticidal and cytotoxic effects of 13 natural and hemisynthetic destruxins have been studied. DE shows insecticidal effects similar to those of DA, while DE and DA are more active than all the other natural compounds and analogues tested. Brominated destruxin is a relatively active analogue displaying particular modalities of cytotoxic effects which reflect a certain originality of its mode of action. The linear molecule resulting from the opening of the DA cycle is not toxic. The most hydrophilic destruxins showing e.g. charged radicals (COO-) appear the least toxic probably because they do not penetrate easily the cellular membranes.
Dumas
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Station de Recherches de Pathologie Comparée INRA-CNRS, Saint-Christol lez Alès, France.
Robert
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P
Pais
M
M
Vey
A
A
Quiot
J M
JM
D000284:Administration, Oral; D000595:Amino Acid Sequence; D000818:Animals; D012831:Bombyx / Q000166:cytology / Q000187:drug effects; D002460:Cell Line; D002851:Chromatography, High Pressure Liquid; D003593:Cytoplasm / Q000187:drug effects / Q000648:ultrastructure; D003603:Cytotoxins / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity*; D047630:Depsipeptides; D004847:Epithelial Cells; D004848:Epithelium / Q000187:drug effects / Q000648:ultrastructure; D005656:Fungal Proteins; D007313:Insecta / Q000187:drug effects / Q000648:ultrastructure; D007306:Insecticides / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity*; D007814:Larva / Q000187:drug effects / Q000648:ultrastructure; D009682:Magnetic Resonance Spectroscopy; D008317:Malpighian Tubules / Q000187:drug effects / Q000648:ultrastructure; D008854:Microscopy, Electron; D008858:Microscopy, Phase-Contrast; D008969:Molecular Sequence Data; D009183:Mycotoxins / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity*; D010456:Peptides, Cyclic / Q000737:chemistry / Q000633:toxicity; D013329:Structure-Activity Relationship
D003603:Cytotoxins; D047630:Depsipeptides; D005656:Fungal Proteins; D007306:Insecticides; D009183:Mycotoxins; D010456:Peptides, Cyclic; C040423:destruxin A; C040425:destruxin E