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As a depsipeptide derivative of dolastoxin, auristatin could inhibit tumor growth through acting on tubulin. The activity of auristatin is higher than that of traditional chemotherapeutic drugs by 1000 times. As a linear depsipeptide natural toxic protein isolated from dolabella auricularia, dolastoxin shows strong antitumor activity by acting on tubulin. In addition to containing abundant hydroxy acids, thiophenols, D-amino acids and α-amino acids, the structure of dolastoxin also contains ethylenic and acetylenic bonds. All these groups improve the biological activity and stability of these kind of compounds.