The invention relates to the field of algaecide inhibitors, in particular to a diketopiperazine derivative derived from an endophytic fungus of seaweed, and a preparation method and application thereof to inhibition of algae. The specific structural formula is as shown in (I). According to the preparation method of the diketopiperazine derivative, seaweed endophytic fungus Trichoderma asperellum A-YMD-9-2 is inoculated in a fungal culture medium for fermentation culture, and a fermentation product is separated and purified, so that the diketopiperazine derivative represented by the formula (I)is obtained. The diketopiperazine derivative obtained by the invention has a half-inhibitory concentration of the compound against microalgae up to 12 [mu]g/mL by a microalgae activity test.
; 宋银平
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