Studies On The Bioactive Constituents From Holothuria Scabra Jaeger

Holothuria scabra Jaeger distributed abundantly in South China Sea especially in Dongshan Gulf, Fujian province. Up to date, only few chemical works have been performed on these sea cucumbers. Guided by P. oryzae bioassay model, the anticancer and antifungal constituents of Holothuria scabra Jaeger has been investigated by various chromatography methods including LPLC, MPLC, HPLC on resin, silica gel, ODS RP C-18 and Zobax SB C-18 respectively.Six compounds were isolated; all compounds were elucidated by chemical and spectral analysis (IR; EI-MS, HREI-MS, ESI-MS; ¹HNMR, ¹³CNMR, HMQC, TOCSY, ¹H-¹H COSY, DQF-COSY, HMBC, NOESY).Six triterpene glycosides were isolated from the sea cucumber Holothuria scabra Jaeger(from Dongshan Gulf,Fujian province) and elucidated as 3-O-[3^""-O-methyl-β-D-glucopyranosyl(1→3)-β-D-glucopyranosyl(1→4)-β-D-quinovopyranosyl (1→2)-4'-O-sodiumsulfate-β-D-xylopyranosyl]-holosta-9,24-diene-3β,12α,17α-triol,3-O-[β-D-quinovopyranosy 1(1→2)-4'-O-sodiumsulfate-β-D-xylopyranosyl]-holosta-9-en e-3β.12α, 17α-triol,3-O-[3""-O-methyl-β-D-glucopyranosyl(1→3)-β-D-glucopyranosyl (1→4)-β-D-quinovopyranosyl(1→2)-4'-O-sodiurnsulfate-β-D-xylopyranosyl]-holosta-9 -ene-3β, 12α, 17α-triol, 3-O-[β-D-quinovopyranosyl(1→2)-4'-O-sodiumsulfate-β-D-xylopyranosyl]-holosta-22,25-oxido-9-ene-3β,12α, 17α-triol,3-O-[3""-O-methyl-β-D-glucopyranosyl(1→3)-β-D-glucopyranosyl(1→4)-β-D-quinovopyranosyl (1→2)-4'-O-sodiumsulfate-β-D-xylopyranosyl]-holosta-22,25-oxido-9-ene-3β,12α,17α-triol, 3-O-[3""-O-methyl-β-D-glucopyranosyl (1→3)-β-D-glucopyranosyl(1→4)-β-D-quinovopy-ranosyl(1→2)-4'-O-sodiumsulfate-β-D-xylopyranosyl]-16β-acetoxy-holosta-9-ene-3β, 12α.l7α-triol(a new compound), the compound was named by scabraside A.The compounds showed moderate cytotoxity in vitro against many human tumor cell lines such as A549 and P388. Compound 2 showed strongantifungal activity against Candida albicans with MIC 2.1(ug/ml), C. parapsilosis with M IC 1.1(ug/ml), C. neoformans with MIC 4.2(ug/ml), C. tropicalis with MIC 4.2 (ug/ml).Compound 4 and compound 5 showed strong antifungal activity against Candida albicans,C. parapsilosis,C. neoformans,C. tropicalis with MIC from 9.4 (ug/ml) to 125(ug/ml). Compound 6 showed strong antifungal activity against C -andida albicans with MIC 4.2 (ug/ml) too. Compound 7 showed better strong...