Daptomycin is a new type of lipopeptide antibiotic, which was studied by Lilai company in the 1980s and extracted from the fermentation broth of Streptomyces roseosporus. In phase I and phase II clinical trials, it shows good clinical application value for skin infection caused by Gram-positive bacteria. Its chemical structure and action mechanism are different from all kinds of antibiotics, which means that it can treat multidrug-resistant bacterial infection. However, under high dose, it will cause adverse reactions in skeletal muscle, so Lilai company stopped development. The ownership of daptomycin was purchased by Cubist pharmaceuticals in 1997 and approved by the U.S. Food and Drug Administration in 2003 for the treatment of complex skin infections and structural skin infections caused by Gram-positive bacteria.

Daptomycin is a lipopeptide antibiotic composed of 13 amino acids, of which 10 amino acids are connected from head to tail to form a ring, another 3 amino acids form a side chain, and the end of the side chain is connected with decadecanoic acid. The compound is a semi synthetic antibiotic and an n-decanoyl derivative of a21978c produced by Streptomyces roseus. The structure-activity relationship study showed that the in vitro antibacterial activity of the compound increased with the increase of terminal carbon chains (10 ~ 13), but its in vivo toxicity also increased when the terminal carbon chains were 11 or longer. The aspartic acid residues in the ring of the compound were replaced by other amino acid residues, and the antibacterial activity disappeared. It is shown that the aspartic acid residues are closely related to the antibacterial mechanism of the compound Datormycin binds to bacterial cell membrane protein in the form of non covalent bond, which destroys various functions of bacterial cell membrane, such as disturbing the transport of amino acids by cell membrane, thus hindering the synthesis of bacterial cell wall peptidoglycan; It can also cause bacterial cell death by destroying the bacterial cell membrane and leaking its contents