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Liu X.,Southern Medical University | Wang W.,Guangzhou RiboBio Co. | Samarsky D.,Guangzhou RiboBio Co. | Liu L.,Southern Medical University | And 16 more authors.
Nucleic Acids Research | Year: 2014

RNAi technology is taking strong position among the key therapeutic modalities, with dozens of siRNA-based programs entering and successfully progressing through clinical stages of drug development. To further explore potentials of RNAi technology as therapeutics, we engineered and tested VEGFR2 siRNA molecules specifically targeted to tumors through covalently conjugated cyclo(Arg-Gly-Asp-d-Phe-Lys[PEG-MAL]) (cRGD) peptide, known to bind αvβ3 integrin receptors. cRGD-siRNAs were demonstrated to specifically enter and silence targeted genes in cultured αvβ3 positive human cells (HUVEC). Microinjection of zebrafish blastocysts with VEGFR2 cRGD-siRNA resulted in specific inhibition of blood vessel growth. In tumor-bearing mice, intravenously injected cRGD-siRNA molecules generated no innate immune response and bio-distributed to tumor tissues. Continuous systemic delivery of two different VEGFR2 cRGD-siRNAs resulted in down-regulation of corresponding mRNA (55 and 45%) and protein (65 and 45%) in tumors, as well as in overall reduction of tumor volume (90 and 70%). These findings demonstrate strong potential of cRGD-siRNA molecules as anti-tumor therapy. © 2014 The Author(s).

Zou Y.,CAS Guangzhou Institute of Chemistry | Zou Y.,Guangzhou University | Huang Q.,CAS Guangzhou Institute of Chemistry | Huang Q.,University of Chinese Academy of Sciences | And 8 more authors.
Organic and Biomolecular Chemistry | Year: 2013

A series of trans- or cis-stilbenes have been synthesized in good to excellent yields via a functional group-dependent decarboxylation process from the corresponding 2,3-diaryl acrylic acids in a neutral CuI/1,10-phen/PEG-400 system under microwave conditions. The in situ generation of the recyclable catalytic complex, the use of environmentally benign solvent PEG-400, the operational simplicity, the short reaction times, as well as the functional group-dependent chemo- and stereo-selectivity have made the decarboxylation process a highly efficient and applicable protocol. © 2013 The Royal Society of Chemistry.

Liu S.,Chinese Academy of Sciences | Liu S.,Hainan University | Yang W.,Guangzhou General Pharmaceutical Research Institute | Liu S.-B.,Chinese Academy of Sciences | And 6 more authors.
Natural Product Communications | Year: 2014

One new diterpenoid, 11α,12βH-dolabella-4,8(17)-dien-3α, 7β,18-triol (1) and one new sesquilignan, 9-methoxy-7′,8′-cis- 7″,8″-cis-buddlenol B (2), together with three known compounds, (+)-diasyringaresinol (3), N-methyl-5- hydroxy-Δ3-pyrrolin-2- one (4) and marmin (5), have been isolated from Aglaia odorata var. microphyllina. Their structures were determined using 1D and 2D NMR spectroscopy. Compound 1 exhibited cytotoxic activity against the K562 cell line with an IC50 value of 12.5 μg/mL.

Yang Y.-Y.,Chinese Academy of Sciences | Yang W.,Guangzhou General Pharmaceutical Research Institute | Zuo W.-J.,Chinese Academy of Sciences | Zeng Y.-B.,Chinese Academy of Sciences | And 3 more authors.
Journal of Asian Natural Products Research | Year: 2013

Two new acridone alkaloids, 3-methoxy-1,4,5-trihydroxy-10-methylacridone (1) and 2,3-dimethoxy-1,4,5-trihydroxy-10-methylacridone (2), were isolated from the ethanol extract of the branch of Atalantia buxifolia. Their structures were elucidated by spectroscopic methods including 1D and 2D NMR. Compounds 1 and 2 exhibited significant antibacterial activity against Staphylococcus aureus and weak inhibitory effect on acetylcholinesterase. © 2013 Taylor & Francis Group, LLC.

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