Oleanolic acid inhibits proliferation of HUVECs, and inhibits migration and tube formation via VEGF pathway / 药学学报

To investigate the effects of oleanolic acid (OA) on the proliferation, migration and the formation of tube-like structure in human vascular endothelial cells (HUVECs). MTT assay, flat plate scarification, Transwell plates and matrigel-induced tube formation assay were performed to detect the effects of OA on proliferation, migration and tube formation. MTT assay showed that the inhibition rates of HUVECs treated with 60 and 100 microg x mL(-1) of OA for 24 h were 19% and 83% respectively. Treatment of HUVECs significantly inhibited the cell migration in a dose-dependent manner. The vascular indexes of HUVECs treated with 40 and 60 microg x mL(-1) OA were 33% and 20% respectively. Western blotting analysis showed that treatment of the cells with OA significantly attenuated the expression and secretion of VEGF. Additionally, VEGF could in part reverse the effects of OA on migration and tube formation of HUVECs. In conclusion, OA inhibits the proliferation, and VEGF plays an important role in OA induced decreased migration and tube formation of HUVECs.

PTP1B inhibitory activities of bromophenol derivatives from algae / 中国中药杂志

<p><b>OBJECTIVE</b>To study the protein tyrosine phosphatase-1B (PTP1B) inhibitory activity of natural products from algae aiming at searching for new way for the treatment of type 2 diabetes mellitus (T2DM) and obesity.</p><p><b>METHOD</b>Bromophenols derivatives from algae were screened against the PTP1B by the colorimetric assay with GST/PTP1B fusion protein. The Me2SO was distributed as the full enzyme activity, and Na3VO4 (IC50 2 micromol L(-1)) was distributed as the positive control. Inhibition rate was assayed and IC50 were calculated by LOGIT method.</p><p><b>RESULT</b>Three bromophenols from Rhodomela confervoides and Leathesia nana, 3, 4-dibromo-5-(methoxymethyl)-1, 2-benzenediol (1), 2-methyl-3-(2, 3-dibromo4, 5-dihydroxy)-propylaldehyde (2) and 3-(2, 3-dibromo-4, 5-dihydroxy-phenyl)-4-bromo-5, 6-dihydroxy-1, 3-dihydroiso-benzofuran (3) showed significant inhibitory activity against PTP1B. IC50 values were 3.4 +/- micromol L(-1), 4.5 micromol L(-1) and 2.8 micromol L(-1), respectively.</p><p><b>CONCLUSION</b>The results prove that three bromophenol derivatives from algae with significant inhibitory activity against PTP1B were potential and effective therapeutic agents for treatment of T2DM and obesity.</p>

Studies on chemical constitutes of Acantophora spicifera / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constitutes of Acantophora spicifera.</p><p><b>METHOD</b>Compounds were isolated by normal phase silica gel and Sephadex LH-20 gel column chromatography, and reverse-phase HPLC, as well as recrystallization. Their structures were elucidated by spectroscopic methods.</p><p><b>RESULT</b>Seven compounds were isolated from A. spicifera and their structures were identified as aplysin (1), loloilide (2), (R)-(-)-dehydrovomifoliol (3), uracil (4), thymine (5), 1-methoxy-4-(1-propenyl) benzene (6).</p><p><b>CONCLUSION</b>The compounds were obtained from this genus for the first time. Compound 6 was firstly obtained from marine organisms.</p>

Studies on chemical constituents of Laurencia tristicha ( II ) / 中国中药杂志

<p><b>OBJECTIVE</b>To search for chemical constituents with structural diversity from Laurencia tristicha to supply for biological assay.</p><p><b>METHOD</b>Compounds were isolated by means of column chromatography over normal phase silica gel and Sephadex LH-20, recrystallization and HPLC. Structures were identified by spectroscopic methods including 1D NMR, IR and MS. Cytotoxicities of the purified compounds were evaluated by MTT method.</p><p><b>RESULT</b>Seven compounds were isolated from L. tristicha. Their structures were elucidated as cholesterol (1), cholesta- 5-en-3beta, 7alpha-diol (2), beta-stigmasterol (3), phytol (4), zeaxanthin (5), 4 -hydroxybenzaldehyde (6), indolyl-3-carbaldehyde (7). In the cytotoxic assay compound 2 was active against human cancer cell lines HCT-8, Bel-7402, BGc-823, A549 and HELA with IC50 values of 1.90, 2.02, 1.99, 6.52 and 1.20 microg x mL(-1), respectively. Compound 4 showed cytotoxicity against HCT-8 and HELA with IC50 value of 3.51 and 2.04 microg x mL(-1), and other compounds were inactive ( IC50 > 10 microg x mL(-1)).</p><p><b>CONCLUSION</b>Compounds 1-7 were isolated from L. tristicha for the first time. In additon, compounds 2 and 4 were cytotoxic against several human cancer cell lines.</p>

Norisoprenoids from red alga Gymnogongrus flabelliformis / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents of the red alga Gymnogongrus flabelliformis Harv.</p><p><b>METHOD</b>Compounds were isolated by normal phase silica gel and Sephadex LH - 20 gel column chromatography and reverse phase HPLC. Their structures were elucidated by spectroscopic methods including MS, 1H-NMR, 13C-NMR. Cytotoxicity of the compounds was screened by using standard MIT method.</p><p><b>RESULT</b>Five compounds were isolated from G. flabelliforrmis, their structures were identified as(3S, 6R, 7E)-( + )-3-hydroxyl-4, 7-mega-stigmadien-9-one (1), (3S, 5R, 6S, 7E)-(-)-3-hydroxy-5, 6-epoxy-7-megastigmene-9-one (2), (3S, 5S, 6R, 7E)-(+)3-hydroxy-5, 6-epoxy-7-megastigmene-9-one (3), dehydrovomifoliol (4), (3R)-(-)4-[(2R, 4S)-4-acetoxy-2-hydroxy-2, 6, 6-trimethylcyclohexylidene] -3-buten-2-one (5).</p><p><b>CONCLUSION</b>All of the compounds were obtained from this species for the first time and compound 1 was a new natural product. These compounds were inactive (IC50 > 10 microg x mL(-1)) in the MTT assay against several human cancer cell lines.</p>

Chemical constituents from red alga Corallina pilulifera / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents of red alga Corallina pilulifera.</p><p><b>METHOD</b>Compounds were isolated by normal phase silica gel and Sephadex LH - 20 gel column chromatography, reverse phase HPLC and recrystallization. Their structures were elucidated by spectroscopic methods including MS, 1H-NMR, 13C-NMR, HSQC, HMBC. Cytotoxicity of the compounds was screened by using standard MTT method.</p><p><b>RESULT</b>Seven compounds were isolated from red alga C. pilulifera, their structures were identified as (E) -phytol epoxide (1), phytenal (2), phytol (3), dehydrovomifoliol (4), loliolide (5), 3beta-hydroxy-5alpha, 6alpha-epoxy-7-megastigmene-9-one (6), 4-hydroxybenzaldehyde (7).</p><p><b>CONCLUSION</b>All of the compounds were obtained from this species for the first time. These compounds were inactive (IC50 > 10 microg x mL(-1)) in the MTT assay.</p>

Chemical constituents from marine alga Chaetomorpha basiretorsa / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents of marine alga Chaetomorpha basiretorsa.</p><p><b>METHOD</b>Compounds were isolated by normal phase silica gel and Sephadex LH-20 gel colum chromatography, reverse phase MPLC, reverse phase HPLC and recrystallization. Their structures were elucidated by spectroscopic methods including MS, IR, NMR, and X-ray crystalography. Cytotoxicity of the compounds were screened by using standard MTT method.</p><p><b>RESULT</b>Nine compounds were isolated from C. basiretorsa and their structures were identified as N-phenyl-2-naphthalenamine( I ), dibutyl phthalate( II ), diisobutyl phthalate( III ), 1-phenyl-ethane-1, 2-diol( IV ), 2-hydrox-gamma-benzaldehyde( V ), diethyleneglycol monobenzoate( VI ), uracil( VII ), thymine( VIII ) and thymidine( IX ).</p><p><b>CONCLUSION</b>All these compounds were obtained from this genus for the first time, N-phenyl-2-naphthalenamine and diethyleneglycol monobenzoate were first reported from the marine organisms. Compound I and VII showed moderate activity against KB cell(IC50 10.15 microg x mL(-1) for I and 3.79 microg x mL(-1) for VII ) and MCF-7 cell(IC50 3.24 microg x mL(-1) for VII).</p>

Studies on chemical constitutes of green alga Chaetomorpha basiretorsa and their bioactivity / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Chaetomorpha basiretorsa and screen for bioactive leading compounds.</p><p><b>METHOD</b>Compounds were isolated by normal phase silica gel and Sephadex LH-20 gel column chromatography, reverse phase MPLC and reverse phase HPLC. Their structures were elucidated by spectroscopic methods including MS, IR and 1D, 2D NMR. Cytotoxicity of the compounds was screened by using standard MTT method. The purified compounds' inhibition against proliferation of dog vascular smooth muscle cells was also screened by MTT assay.</p><p><b>RESULT</b>Five compounds were isolated from C. basiretorsa and their structures were identified as euphol (I), loloilide (II), 4-cumylphenol (III), zeaxanthin (IV) and lactucaxanthin (V).</p><p><b>CONCLUSION</b>All these compounds were obtained from this genus for the first time. Compound (III), 4-cumylphenol, was a new nature product. All compounds were inactive (IC50 > 10 microg x mL(-1)) in cytotoxicity screening. In inhibition against proliferation of dog vascular smooth muscle cells test, the cell survival ratio to compound I was (0.32 +/- 0.056)% which indicate its potential anti-atherosclerotic bioactivity.</p>