| In order to find new substances with anticancer bioactivities from metabolites of marine microorganisms, microorganism strains were collected and isolated from sea area around china. With morphological changes of Pyricularia oryzae and Alternaria solani as bioassays, 5 microorganism strains with better activities were selected to be researched. The chemical constituents of the fermentation and/or mycelia of these six strains were studied on by all kinds of chromatographical techniques (such as silica gel chromatography, sephadex LH-20, PTLC and HPLC etc.). 48 compounds were obtained and their structures were determined by means of physicochemical evidence and spectral analysis.11 compounds were isolated from the strain Bacillus sp. ZV-80 and identified as pyrrolopiperazine-1,4-dione (1), urea (2), 3-benzyl-2,5-piperazinedione (3), 3-isobutyl-6-methyl-piperazine-2,5-dione (4), 3-methylpiperazine-2,5-dione (5), 3-isobutyl-piperazine-2,5-dione (6), 3-isobutyl-8-hydroxy-pyrrolo piperazine-1,4-dione (7), thymine (8), 1,2-benzenedicarboxylic acid-dibutyl ester (9), hexadecylicacid (10), uracil (11). 11 compounds were isolated from the strain Gliocladium sp. YUP-08 and identified as diketopiperazine JA7-9 (12), diketopiperazine DCB-2 (13), diketopiperazine DCB-1 (14), diketopiperazine GA-9 (15), diketopiperazine GA-10 (16), 3-(hydroxymethyl)phenol (17), 4-methyl-1,2-benzenediol (18). 4-(2-hydroxyethyl) phenol (19), 2-hydroxy-6-methylbenzoic acid (20), ergosta-5,7,22E-triene-3p-ol (21), 23-methylergosta-5,7,22E-triene-3β-ol (22). 12 compounds were isolated from the strain Monoscus purpureus 41-06 and identified as cycloarthropsone (23), 6-methoxy-7-hydroxycoumarin (24), 3-benzyl-7-hydroxyhexahydropyrrolo [1,2-a]pyrazine-1,4-dione (25), 3-methyl-7-hydroxyhexahydropyrrolo[1,2-a]pyrazine-1,4-dione (26), 5-(hydroxymethyl) furan-2-carbaldehyde (27), formononetin (28), diisobutyl phthalate (29), 4-hydroxybenzoic acid (30), 2-hydroxybenzoic acid (31), succinic acid (32), mannose (33), mannitol (34). 7 compounds were isolated from the strain Trichothecium sp.37-04 and identified as trichodimerol (35), sorbicillin (36), ergosta-8(9),22E-diene-3β,5a,6β, 7a-tetraol (37), 5a,8a-epidioxyergosta-6,22E-dien-3β-ol (38), 5a,8a-epidioxyergosta-6,9(11), 22E-trien-3β-ol (39), 3,5,9-trihydroxyergosta-7,22-diene-6-one (40), ergosta-5,7,22E-triene-3β-ol (41). 7 compounds were isolated from the strain Penicillium sp.35-04 and identified as 3-benzyl-6-isopropylpiperazine-2,5-dione (42), 3-benzyl-6-isobutyl-piperazine-2,5-dione (43), 3-benzyl-6-sec-butyl-piperazine-2,5-dione (44), 3,6-dibenzylpiperazine-2,5-dione (45), 3-isobutyl-6-isopropylpiperazine-2,5-dione (46), 3-sec-buty1-6-isobutyl piperazine-2,5-dione (47), 3-sec-buty1-6-isopropyl-piperazine-2,5-dione (48).5 compounds (12-16) among the obtained compounds are new compounds. All of them are new diketopiperazines with geranyl group, which is a rare group in diketopiperazine.The cytotoxicity in vitro against three cancer cells were measured. Diketopiperazines 12-16 showed strong activities against the cancer cells selected. The known compound 36 exhibited a moderate cytotoxic activity and strong apoptotic activity against cancer cell HL-60. A discussion about the relationship between structure and cytotoxicity of diketopiperazines was carried out on the basis of the results of compounds 12-16.On the basis of the literatures, the study advance of diketopiperazines from natural resource and synthesis methods was reviewed.
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