Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism

Guangzhou, China

Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism

Guangzhou, China
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Xie G.,Sun Yat Sen University | Xie G.,Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism | Zhu X.,Sun Yat Sen University | Zhu X.,Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism | And 18 more authors.
British Journal of Pharmacology | Year: 2010

Background and purpose: The aims of this study were to investigate the anti-cancer activity of SZ-685C, an anthracycline analogue isolated from marine-derived mangrove endophytic fungi, and to explore the molecular mechanisms underlying such activity. Experimental approach: The effect of SZ-685C on the viability of cancer cell lines was investigated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. SZ-685C-induced apoptosis was assessed by Annexin V-fluorescein isothiocyanate/propidium iodide staining, terminal deoxynucleotidyl transferase-mediated dUTP nick end labelling assay and analysis of caspase activation. The effect of SZ-685C on the Akt/FOXO pathway was studied using Western blotting analysis, and the in vivo anti-tumour efficacy was examined in an MDA-MB-435 breast cancer xenograft model. Key results: SZ-685C suppressed the proliferation of six cancer cell lines derived from human breast cancer, prostate cancer, glioma and hepatoma (IC 50 values ranged from 3.0 to 9.6 μM) and the growth of breast cancer xenografts in mice. SZ-685C had a direct apoptosis-inducing effect through both the extrinsic and intrinsic apoptotic pathways, as shown by activation of caspase-8 and 9 as well as effector caspase-3 and poly (ADP-ribose) polymerase. Phosphorylation of Akt and its downstream effectors, forkhead box protein O1 and forkhead box protein O3a, was down-regulated in SZ-685C-treated cancer cells. Furthermore, the pro-apoptotic protein Bim was up-regulated by SZ-685C treatment consistent with FOXO dephosphorylation. Conclusions and implications: SZ-685C could induce apoptosis through the Akt/FOXO pathway, which consequently leads to the observed anti-tumour effect both in vitro and in vivo. Our data suggest that SZ-685C may be a potentially promising Akt inhibitor and anti-cancer drug candidate. © 2010 The British Pharmacological Society.


Huang C.,Sun Yat Sen University | Huang C.,Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism | Huang C.,Jinan University | Jin H.,Jinan University | And 9 more authors.
Applied Microbiology and Biotechnology | Year: 2012

Alterporriol L, a new bianthraquinone derivative, was isolated from a marine fungus Alternaria sp. ZJ9-6B. The cytotoxic activity and anticancer mechanisms of alterporriol L towards breast cancer cells lines were detected using MTT assay, immunofluorescence, and flow cytometry. Simultaneously, the changes in morphological properties of cells were detected before and after treatment with alterporriol L by atomic force microscope (AFM) at a nanometer scale. MTT assay showed that alterporriol L could effectively inhibit the growth and proliferation, and there was a dose-dependent manner of cell death. Moreover, the alterporriol L could induce cancer cell apoptosis or necrosis. Furthermore, the reactive oxygen species, mitochondrial membrane potential, and cytosolic free calcium level were changed after treatment with alterporriol L, suggesting that alterporriol L played vital roles in breast cancer cells through destroying the mitochondrial. And all these alterations are in accord with changes of morphology detected by AFM, which suggested that the AFM is a useful tool to detect the morphological changes of the cancer cells. © 2011 Springer-Verlag.


Liu F.,Sun Yat Sen University | Cai X.-L.,Sun Yat Sen University | Yang H.,Sun Yat Sen University | Xia X.-K.,Sun Yat Sen University | And 9 more authors.
Planta Medica | Year: 2010

Bioactivity-directed fractionation of the extract of the mangrove endophytic fungus Talaromyces sp. ZH-154, which was isolated from the stem bark of Kandelia candel (L.) Druce, Rhizophoraceae, afforded two new metabolites, 7-epiaustdiol (1) and 8-O-methylepiaustdiol (2), together with the known compounds, stemphyperylenol (3), skyrin (4), secalonic acid A (5), emodin (6), and norlichexanthone (7). Their structures were elucidated on the basis of spectroscopic evidences including CD, MS, and 1D, 2DNMR techniques. The absolute configuration of 1 was unequivocally determined by single-crystal Xray diffraction. All isolated compounds were evaluated for their antimicrobial and in vitro cytotoxic activities. © Georg Thieme Verlag KG Stuttgart New York.


Huang H.-B.,Sun Yat Sen University | Huang H.-B.,CAS South China Sea Institute of Oceanology | Xiao Z.-E.,Sun Yat Sen University | Feng X.-J.,Sun Yat Sen University | And 11 more authors.
Helvetica Chimica Acta | Year: 2011

Four new dimeric naphtho-γ-pyrones, named rubasperone D (1), rubasperone E (2), rubasperone F (3), and its atropisomer rubasperone G (4), together with four known monomeric naphtho-γ-pyrones, TMC 256 A1 (5), rubrofusarin B (6), fonsecin (7), and flavasperone (8), were isolated from the mangrove endophytic fungus Aspergillus tubingensis (GX1-5E) cultivated in solid rice medium. Their structures were elucidated by spectroscopic methods, including IR, 1D- and 2D-NMR, and MS. In the in vitro cytotoxicity assays, 5 displayed inhibitory activities against tumor cell lines of MCF-7, MDA-MB-435, Hep3B, Huh7, SNB19, and U87 MG with IC50 values between 19.92 and 47.98 μM. Compounds 1, 6, and 8 also showed mild cytotoxic activity. Copyright © 2011 Verlag Helvetica Chimica Acta AG, Zürich, Switzerland.


Liu L.,Sun Yat Sen University | Liu L.,Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism | Song Y.-X.,Sun Yat Sen University | Song Y.-X.,Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism | And 8 more authors.
Planta Medica | Year: 2012

Two new lactones, 1 and 2, together with five known compounds, 37, were isolated from the marine mangrove fungus Xylaria sp. BL321. Their structures were determined by comprehensive analysis of their MS and NMR spectroscopic data. The absolute configurations of 1 and 2 were established on the basis of electronic circular dichroism calculations. It was found that the exocyclic double bond of 1 rearranged into a cyclic double bond to form a new crystal compound (1a) in diluted NaOH solution. Compound 3 was isolated for the first time as a natural product; its absolute configuration was determined by single-crystal X-ray crystallography. Compounds 47 displayed cytotoxicity against human breast cancer cell lines MCF-7 and MDA-MB-435, while compounds 13 were inactive (IC 50 >50μM). © Georg Thieme Verlag KG Stuttgart New York.

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