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새로운 Anthraquinone 유도체, DHAQ-97의 항암작용: 아폽토시스에 의한 인체 유방암세포 사멸 유도
허연진(Yeon-Jin Hurh),김정환(Jung-Hwan Kim),장정희(Jung-Hee Jang),안병준(Byung-Zun Ahn),서영준(Young-Joon Surh) 한국환경성돌연변이발암원학회 2000 한국환경성돌연변이·발암원학회지 Vol.20 No.1
DHAQ-97, (2-(3-[p-bis(2-chloroethyl)aminophenyl]-2-formylaminopropanoyloxy)methyl-1,4-dihydroxy-9,10-anthraquinone), is a novel anthraquinone derivative synthesized for use as an anti-neoplastic agent. In the present study, we have evaluated the selective cytotoxicity of DHAQ-97 by comparing its effects on viability and proliferation of human breast cancer cell line (MCF-7) versus normal immortalized breast epithelial cell line (MCF-10A). Thus, DHAQ-97 reduced both viability and proliferation of MCF-7 cells to a much greater extent than did for MCF-10A cells. The growth inhibitory and anti-proliferative properties of DHAQ-97 appear to be attributable to its ability to induce apoptosis as revealed by positive staining after in situ nick-end labeling<br/> (TUNEL), cleavage of poly(ADP-ribose)polymerase, release of mitochondrial cytochrome c into cytoplasm, and increased expression of pro-apoptotic Bax protein. Recent studies have indicated possible involvement of the ubiquitous eukaryotic transcription factor, NF-kappa B (NF-kB) in the regulation of apoptotic cell death. In line with this notion, the NF-kB inhibitor pyrrolidine dithiocarbamate significantly attenuated the DHAQ-97-induced cytotoxicity in cultured MCF-7 cells. Furthermore, mild activation of NF-kB, as determined by its increased DNA binding capability, was observed 30 min after treatment with 10 μM DHAQ-97. Taken together, the above findings suggest that DHAQ-97 exerts selective cytotoxicity towards cancer cells through induction of<br/> apoptosis, which appears to be regulated by NF-kB.
Hurh, Joon,Markus, Josua,Kim, Yeon-Ju,Ahn, Sungeun,Castro-Aceituno, Veronica,Mathiyalagan, Ramya,Kim, Yu Jin,Yang, Deok Chun KLUWER 2017 JOURNAL OF NANOPARTICLE RESEARCH Vol. No.
<P>Gold nanoparticles (GNPs) are forecasted to provide an attractive platform in biomedicine and catalysis with their potentials of combining a variety of biophysicochemical properties into an integrated nanodevice with great therapeutic and optical functions. There are several reports of crude plant extracts mediating the conversion of metal ions into nanoparticles. However, we aimed to investigate the capability of single bioactive compounds, namely ginsenosides compound K (C-K) and Rh2, to accommodate a synergistic chemical reduction of gold salts by one-pot green chemistry. Ginsenosides C-K and Rh2 are unique triterpenoid saponins present in Panax ginseng Meyer, a perennial plant traditionally used as an oriental medicinal herbal with long history. C-K and Rh2 have demonstrated diverse pharmacological properties such as anticancer, anti-inflammation, anti-aging, and neuroprotective properties. The reduction of gold ions by these ginsenosides led to the production of nontoxic GNPs as tested in mousemacrophage (J774A. 1) and human kidney epithelial (HEK-293) in vitro. The kinetics of the bioreduction and the influence of pH were examined by an ultraviolet-visible (UV-Vis) spectrophotometer. GNPs were characterized by field emission transmission electron microscopy (FE-TEM), X-ray diffraction (XRD), dynamic light scattering (DLS), and Fourier transform infrared (FTIR) spectroscopy. Ginsenoside loading efficiency of C-K-GNPs and Rh2-GNPs was determined to be approximately 62.83% and 54.91%, respectively, by thermogravimetric analysis (TGA). These results suggest that onepot synthesis by ginsenosides C-K and Rh2may be useful for producing ginsenoside-loaded gold nanocarriers.</P>