| It is reported that there are about 134 species of sea cucumbers spread in the China seas, of which more than 20 species are edible. A long time ago, Chinese people had known that some species of sea cucumbers could be used as foods, and some species could be used as folk medicine for the treatment of some diseases. In continuing to search for compounds with novel structures and pharmacological activity from the sea cucumbers, we team had done lots of research works before. Our had made researches on Mensamaria intercedens Lampert, Acaudina molpadioides Semper, Philinopsis lineolate, etc, and had found lots of new compounds with new pharmacological activity, some of the researches had been supported by the National High Technology Development Project (863 project). Our main goal was to discover some new leading compounds for development of anticancer drugs.Colochirus anceps is widely distributed in the south sea in Fujian province China. There is no report about the chemical studies performed on this sea cucumbers species, so far. In our research, nine compounds and derivates from Colochirus anceps sea cucumber were separated by various chromatography methods including LPLC, MPLC, HPLC on silica gel and Zobax SB C-18 respectively. The structures of six compounds were elucidated by chemical and spectral analysis (IR, EI-MS, ESI-MS, 1H NMR, 13C NMR, HMQC, TOCSY, DQF-COSY, HMBC, NOESY). Two of the six compounds were triterpene glycosides: 3-O-{[3′′′′-O-methyl-β-D-glucopyranosyl-(1→3)- 6′′′-O-sulfate-β-D-glucopyranosyl-(1→4)]-[β-D-xylopyranosyl-(1→2)]- β-D-quinovopyranosyl-(1→2)-4′-O-sulfate-β-D-xylopyranosyl}-holosta-9(11)-olefin-3β-ol-16-one, which was named as Colochiroside A(CA-1); 3-O-{[3′′′′-O-methyl-β-D-glu-copyranosyl-(1→3)-β-D-glucopyranosyl-(1→4)]-[β-D-xylopyranosyl-(1→2)]-β-D-quinovopyranosyl-(1→2)-β-D-xylopyranosyl}-holosta-9(11)-olefin-3β-ol-16-one, was named as DS-colochiroside A(DS-CA-1). Both of the two triterpene glycosides containing of one carbonyl at C-16 and five monosaccharides in the sugar parts. The other four of the six compounds were cerebrosides: 1-O-β-D-glucopyranosyl-(2S, 3R, 4E, 8E)-2-docosanoylamino-13-methyl-4, 8-hexadecadiene-1, 3-diol, which was named colochiroside B; 1-O-β-D-glucopyranosyl-(2S, 3R, 4E, 8E)-2-[(2R)-2-hydroxy-docosanoylamino]-13-methyl-4, 8-hexadecadiene-1, 3-diol, which was named as Colochiroside C; 1-O-β-D-glucopyranosyl-(2S, 3R, 4E, 8E)-2-[(2R)-2-hydroxytricosa-noylamido]-13-met-hyl-4, 8-hexadecadiene-1, 3-diol, which was named as Colochiroside D; 1-O-β-D-glucopyranosyl-(2S, 3R, 4E, 8E)-2-[(2R)-2-hydroxytetraco-sanoylamino]-13-methyl-4, 8-hexadecadiene-1, 3-diol, which was named as Colochiroside E. All the six compounds are novel.Colochiroside A (CA-1) was a triterpene glycoside and showed inhibiting activity against Pyricularia oryzae. The preliminary cytotoxic assay of CA-1 indicated that this compound exhibited significant cytotoxic activity against cultured tumor cell lines of P388, HL-60, A-549, SPC-A4, MKN-28, SGC-7901, BEL-7402, HO-8910, MDA-MB-435, MDA-MB-468, HMEC, HUVEC, WI-38, A431. In the test of hemolytic activity using 1% suspensions of rabbit erythrocytes, saponin CA-1 was found active with ED50≤20μg/ml.The preliminary antitumor assay of CA-1 indicated that this saponin exhibited high inhibiting activity at a dose of 4mg/Kg against S-180 sarcoma in mouse, with 70% restraining rate. In another anticancer assay, the saponin CA-1 showed significant activity against the H22 live cancer in the mouse, at a dose of 3mg/Kg, with the inhibiting rate of 52.2%.Our study focused on bioactive constituents of colochirus anceps and had provided a valuable leading compound for the development of new antitumor drugs, and established a homebase for further researching of the sea cucumber resources in the China seas.
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