| In the test in vitro for cytotoxic components from marine organisms, We found that the metholic extracts of Philinopsis lineolate and Membraniporidae grandicell Canu et Bassler exhibited significant cytotoxicity against the human cancer cell lineHL-60 (IC5014(g/ml, 3.6(g/ml, respectively), and they can also induce morphological deformation of Pyricularia oryzae with minimum morphological deformation concentration (MMDC) 500(g/ml and 50(g/ml, respectively.The components of Philinopsis lineolate (Zhanjiang, Guangdong province) and Membraniporidae grandicell Canu et Bassler (Nanji Isand, Zhejiang province) have been studied guided by Pyricularia oryzae bioactivity method. Flash chromatography, LPLC, MPLC, HPLC and PTLC were applied. Eighteen compounds were separated, thirteen of which were identified by spectrum analysis (IR,1H-NMR,13C-NMR,HMQC,TOCSY,DQF-COSY,HMBC,NOESY,EI-MS,HREI-MS,ESI-MS) and chemical transformation, including five novel compounds.Seven compounds were isolated from Philinopsis lineolate and five new compounds were identified. They are named as Philinopside A(I), Philinopside B(II),Philinopside C(III),Philinopside D(IV),Philinopside E(V). These compounds show moderate cytotoxity in vitro against P388 and human lung carcinoma A-549. Systemic anticancer activities were studied for Philinopside A(I), the major component of Philinopsis lineolate and found that Philinopside A(I) can inhibit tumor angiogensis. A series of pharmacological test were carried out to investigate the inhibition of tumor angiogenesis.1. Philinopside A(I) significantly inhibit the proliferation of HMEC-1 in an apparent concentration-effect dependant manner (IC501.60(0.48(M(n=2))2. Philinopside A(I) significantly inhibit the formation of vessel of vascular endothelial cell(VEC) in an apparent concentration-effect dependant manner (IC50 0.058(0.018(M (n=2).3. Philinopside A(I) significantly inhibit the movement of VEC in an apparent concentration-effect dependant manner(IC50为0.046(M).4. Philinopside A(I) exhibited inhibition of VEGFR-2,PDGFR-( with IC502.6( 0.1(M (n=2), 4.9(0.3(M (n=2) respectively.5. It was proved that Philinopside A(I) could inhibit the formation of new blood vessels of chick cherioallantotic membrane(CAM), with IC5011nmol/egg.Anti-cancer test in vivo showed Philinopside A(I) against mouse liver cancer H22 at 37.9%(2mg/kg,i.v. p<0.01)and against mouse sarcomas S180 at 54.9%(4mg/kg,i.v. p<0.01).Anti-fungal test showed the compounds above exhibited strong activity. MIC80 16mg/L against Candida albicans, MIC80 64mg/L against C. tropicalis. MIC80 128mg/L against C. parapsilosis. MIC80 64mg/L against Cryptococcus neoformansMembraniporidae grandicell Canu et Bassler is a species of Bryozoa family. The chemical components of it has not been reported ever before. The bioactivity guided seperation employed Pyricularia oryzae was carried out. Eleven compounds were separated of which 8 known compounds were identified as Stearic acid (VIII), Palmitic acid (IX), Cholesterol (X), 5(, 8(-Epidioxycholesta-6-en-3(-ol(XI), 9(Z)-en-octadecyl-(-glycerinether(XII), Uracil(XIII), Thymine (XIV) and Thymidine (XV). The structural elucidation of the rest compounds was unable to finish for their very small amounts.In summary, the new lead compound have been provided for TAI. It is the first time to found triterpene glycoside as tumor angiogenesis inhibitor (TAI). The research has been supported by National High Technology Development Project(863 project). The ocean's uncharted depths swarm with creatures. The diversity of the marinelifes is far beyond the people's imagination. The magnificent and beautiful life in the abyss may posses useful pharmaceutical properties. Scientists believe that the marine is an untapped resource bursting with the potential to yield a medical and technological harvest that could change our lives. More and more nature product chemists are engaging in looking at the anti-cancer, anti-viral, anti-microbial, heart-stimulating, nerve-blocking...
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