[Bioactivity of the metabolites from endophytic actinomycete Fq24 against Tetranychus cinnabarinus].

An endophytic actinomycete strain Fq24 was isolated from healthy tomato plants. The acaricidal substances in the metabolites from Fq24 were collected and identified by the methods of extraction, column chromatography, and gas chromatography-mass spectrometry (GC-MS), and their bioactivities against Tetranychus cinnabarinus were measured with slide-dip and leaf-residue methods. Among the extracts, petroleum ether extract had high bioactivity in contact toxicity and oviposition deterrent against T. cinnabarinus. Its lethal concentration of 50% (LC50) was 52.57 mg x L(-1), and its oviposition deterrent concentration of 50% (ODC50) was 43.18 mg x L(-1). The identification with GC-MS showed that the main chemical component of fraction S11 was methyl hexadecanoate, whose molecular formula was C17H34O2, being one of the substances with acaricidal activity in the metabolites from Fq24. The 24 h corrected mortality rate of female mite at 5 mg x mL(-1) of methyl hexadecanoate was 78.3%, and the oviposition deterrent rate was 81.6%.

Martentoxin, a novel K+-channel-blocking peptide: purification, cDNA and genomic cloning, and electrophysiological and pharmacological characterization.

Martentoxin, a novel K+-channel-specific peptide has been purified and characterized from the venom of the East-Asian scorpion (Buthus martensi Karsch). The whole cDNA precursor sequence suggested that martentoxin was composed of 37 residues with a unique sequence compared with other scorpion neurotoxins. The genomic DNA of martentoxin showed an additional intron situated unexpectedly in the 5' UTR region, besides one located close to the C-terminal of the signal peptide. The patch-clamp recording found that martentoxin at the applied dose of 100 nm could strongly block large-conductance Ca2+-activated K+ (BKCa) currents in adrenal medulla chromaffin cells, and BKCa currents blocked by martentoxin could be fully recovered within 30 seconds after washing, which is at least 10 times faster than recovery after charybdotoxin. Meanwhile, a biosensor binding assay showed a fast association rate and a slow dissociation rate of martentoxin binding on rat brain synaptosomes. The binding of martentoxin on rat brain synaptosomes could be inhibited regularly by charybdotoxin, and gradually by toosendanin in a concentration-dependent manner, but not by either apamin or P03 from Buthus martensi. The results thus indicate that martentoxin is a new member in the family of K+-channel-blocking ligands.