ABSTRACT
A novel macrocyclic lactone (1) was isolated from the fermentation broth of Streptomycesmicroflavus neau3, and the structure was elucidated by extensive spectroscopic analysis. Compound 1 showed high acaricidal activity against adult mites (IC(50)=11.1 µg mL(-1)), and nematocidal activity against Caenorhabditis elegans (IC(50)=17.4 µg mL(-1)), especially the acaricidal activity against mite eggs with an IC(50) of 37.1 µg mL(-1), which was relative higher than that of the commercial acaricide and nematocide milbemycins A(3)/A(4).
Subject(s)
Acaricides/pharmacology , Antinematodal Agents/pharmacology , Caenorhabditis elegans/drug effects , Lactones/pharmacology , Macrocyclic Compounds/pharmacology , Mites/drug effects , Acaricides/chemistry , Acaricides/isolation & purification , Animals , Antinematodal Agents/chemistry , Antinematodal Agents/isolation & purification , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Fermentation , Insecticides/chemistry , Insecticides/isolation & purification , Insecticides/pharmacology , Lactones/chemistry , Lactones/isolation & purification , Macrocyclic Compounds/chemistry , Macrocyclic Compounds/isolation & purification , Molecular Conformation , Stereoisomerism , Streptomyces/chemistry , Streptomyces/metabolism , Structure-Activity RelationshipSubject(s)
Adenocarcinoma/drug therapy , Lung Neoplasms/drug therapy , Phenyl Ethers/pharmacology , Streptomyces/metabolism , Adenocarcinoma/pathology , Antineoplastic Agents/chemistry , Antineoplastic Agents/isolation & purification , Antineoplastic Agents/pharmacology , Cell Line, Tumor , China , Colorimetry , Dose-Response Relationship, Drug , Humans , Inhibitory Concentration 50 , Lung Neoplasms/pathology , Phenyl Ethers/chemistry , Phenyl Ethers/isolation & purificationABSTRACT
A new quinoline derivative, methyl 8-(3-methoxy-3-methylbutyl)-2-methylquinoline-4-carboxylate (1), was isolated from the endophytic strain Streptomyces sp. neau50, and the structure was elucidated by extensive spectroscopic analysis. Compound 1 showed cytotoxicity against human lung adenocarcinoma cell line A549 with an IC(50) value of 29.3 µg mL(-1).
