• Natural Product Sciences
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• v.8 no.4
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• pp.165-169
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• 2002

One-hundred and twenty plant extracts were prepared from 29 Indonesian plants and were primarily tested in vitro cytotoxicity in cultured human lung (A549), colon (Col2), and stomach (SNU-638) cancer cells. As a result, the 23 extracts were found to be active in the criteria of $ED_{50}$<$20\;{\mu}g/ml$. Remarkable cytotoxicity was observed for chloroform and n-butanol extracts of Calotropis gigantea, with $ED_{50}$ values ranging from 0.25 to $0.46\;{\mu}g/ml$. Five extracts derived from Eclipta alba and Excoecaria cochinchinensis displayed potent cell-line selective cytotoxicity, while the rest of 15 extracts showed modest cytotoxic activity against all of three cancer cells. In addition, the cytotoxic potential of subfractions of Zingiber cassumunar against a panel of human cancer cell lines is presented.

• Biomolecules & Therapeutics
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• v.31 no.6
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• pp.692-699
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• 2023

The lack of molecular targets hampers the treatment of triple-negative breast cancer (TNBC). In this study, we determined the cytotoxicity of domperidone, a dopamine D2 receptor (DRD2) antagonist in human TNBC BT-549 and CAL-51 cells. Domperidone inhibited cell growth in a dose- and time-dependent manner. The annexin V/propidium iodide staining showed that domperidone induced apoptosis. The domperidone-induced apoptosis was accompanied by the generation of mitochondrial superoxide and the down-regulation of cyclins and CDKs. The apoptotic effect of domperidone on TNBC cells was prevented by pre-treatment with Mito-TEMPO, a mitochondria-specific antioxidant. The prevention of apoptosis with Mito-TEMPO even at concentrations as low as 100 nM, implies that the generation of mitochondrial ROS mediated the domperidone-induced apoptosis. Immunoblot analysis showed that domperidone-induced apoptosis occurred through the down-regulation of the phosphorylation of JAK2 and STAT3. Moreover, domperidone downregulated the levels of D2-like dopamine receptors including DRD2, regardless of their mRNA levels. Our results support further development of DRD2 antagonists as potential therapeutic strategy treating TNBC.

• Natural Product Sciences
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• v.9 no.2
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• pp.109-111
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• 2003

A bioassay-guided fractionation of the active chloroform extracts of the rhizomes of Zingiber cassumunar Roxb. led to the isolation of a potential cytotoxic principle, curcumin (1), along with two inactive compounds, (E)-4-(3',4'- dimethoxyphenyl)but-3-en-1-ol (2) and (E)-4- (3',4'-dimethoxyphenyl)but-3-en-1- yl acetate (3). Curcumin (1) showed a significant cytotoxicity against several human cancer cell lines $(Col2;\;2.30,\;A549;\;12.30,\;SNU638;\;IC_{50}\;18.80\;{\mu}g/ml)$.

• Archives of Pharmacal Research
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• v.28 no.3
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• pp.290-293
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• 2005

A known monoalkyl glycerol ether, ($\pm$)-1-nonadecyloxy-2,3-propanediol (1) was isolated from the ethyl acetate extract of a soft coral Dendronephthya gigantea as a weakly cytotoxic constituent against four human cancer cell lines, A549, HT-29, HT-1080, and SNU-638. In addition, a known ceramide, (28,3R,4E,8E)-N-hexadecanoyl-2-amino-4,8-octadecadiene-1 ,3-diol (2), was also isolated as an inactive constituent. This is the first report on the isolation of the compounds 1 and 2 from the octocoral, Dendronephthya species.

• Proceedings of the Korean Vacuum Society Conference
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• 2012.02a
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• pp.549-549
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• 2012

Early detection of cancer biomarkers in the blood is of vital importance for reducing the mortality and morbidity in a number of cancers. From this point of view, immunosensors based on nanowire (NW) and carbon nanotube (CNT) field-effect transistors (FETs) that allow the ultra-sensitive, highly specific, and label-free electrical detection of biomarkers received much attention. Nevertheless 1D nano-FET biosensors showed high performance, several challenges remain to be resolved for the uncomplicated, reproducible, low-cost and high-throughput nanofabrication. Recently, two-dimensional (2D) graphene and reduced GO (RGO) nanosheets or films find widespread applications such as clean energy storage and conversion devices, optical detector, field-effect transistors, electromechanical resonators, and chemical & biological sensors. In particular, the graphene- and RGO-FETs devices are very promising for sensing applications because of advantages including large detection area, low noise level in solution, ease of fabrication, and the high sensitivity to ions and biomolecules comparable to 1D nano-FETs. Even though a limited number of biosensor applications including chemical vapor deposition (CVD) grown graphene film for DNA detection, single-layer graphene for protein detection and single-layer graphene or solution-processed RGO film for cell monitoring have been reported, development of facile fabrication methods and full understanding of sensing mechanism are still lacking. Furthermore, there have been no reports on demonstration of ultrasensitive electrical detection of a cancer biomarker using the graphene- or RGO-FET. Here we describe scalable and facile fabrication of reduced graphene oxide FET (RGO-FET) with the capability of label-free, ultrasensitive electrical detection of a cancer biomarker, prostate specific antigen/${\alpha}$ 1-antichymotrypsin (PSA-ACT) complex, in which the ultrathin RGO channel was formed by a uniform self-assembly of two-dimensional RGO nanosheets, and also we will discuss about the immunosensing mechanism.

• Archives of Pharmacal Research
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• v.15 no.4
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• pp.356-359
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• 1992

The activity-oriented fractionation of Psoralea corylifolia led to an isolation of a (+) bakuchio 1 as an activ eprinciple of its antitumoral property in vitro 1 was observed to exhibit a mild cytotoxicity against five kinds of cultured human cancer cell lines, i. e. the A549, SK-OV-3, SK-MEL-2, XF-498 and HCT15. The synthesized 2, 3-epoxide of (+)-bakuchiol 3 showed the similar activity as the (+) bakuchiol 1, whereas the other oxidation derivatives 4 and 5 including the acetyl (+) bakuchiol 2 showed a decreased activity.

• Proceedings of the Korean Society of Toxicology Conference
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• 2002.11b
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• pp.133-133
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• 2002

Platycodi Radix, the root of Platycodon grandiflorum, commonly known as Doraji, is used as a traditional oriental medicine. Extracts from the roots of P. grandiflorum have been reported to have wide ranging health benefits. In Korea, the root of P. grandiflorum is used as a food and employed as a folk remedy for adult diseases.(omitted)

• Archives of Pharmacal Research
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• v.24 no.6
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• pp.518-521
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• 2001

Six bioactive alkaloids, aristolactam B(1), poperolactam A(2), aristolactam A(3), norcepharadione B(4), cepharadione B(5) and splendidine(6) were isolated by bioactivity-guided fractionalton of a methanolic extract of the aerial part of Houttuynia cordata. Several of them exhibited significant cytotoxicity against five human tumor cell lines (A-549,SK-OV-3,SK-MEL-2, XF-498 and HCT-15) in vitro.

• Archives of Pharmacal Research
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• v.22 no.2
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• pp.225-227
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• 1999

A new acylcic deterpene (1) and a known acyclic diterpene 12(S)-hydroxygeranyleraniol (2) were isolated form the aerial parts of Carpesium divaricatum. The structure of 1 was determined to be (2E, 10E)-1, 12-dihydroxy-18-acetoxy-3,7,15-trimethylhexadeca-2,10,14-triene (1) on the basis of spectroscopic studies. Compounds 1 and 2 exhibited cytotoxicity against cultured human tumor cell lines, A549, SK-OV-3, SK-MEL-2, XF498, and $HCT_{15}$, with $ED_{50}$ values ranging from 4.3-10.2 ${\mu}g/ml$ and 4.1-8.3 ${\mu}g/ml$, respectively.

• BMB Reports
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• v.51 no.12
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• pp.642-647
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• 2018

Ubiquitin-conjugating enzyme E2S (UBE2S), a family of E2 protein in the ubiquitination process, is involved in development of various cancers. However, its role in lung adenocarcinoma, has not been well elucidated. In this report, we attempted to investigate expression and function of UBE2S in lung adenocarcinoma. Up-regulation of UBE2S at mRNA, and protein level, was observed in human cancer tissues and lung adenocarcinoma cells. Higher UBE2S expression correlated with poorer prognosis of lung adenocarcinoma patients. UBE2S expression was efficiently suppressed by lentivirus-mediated shRNA strategy in A549 cells, and UBE2S silencing led to reduced cell proliferation, colony formation, and enhanced apoptosis. Inverse results were observed, in UBE2S over-expressed H1299 cells. Microarray analysis indicated that a large number of genes were regulated by UBE2S, and p53 signaling pathway may be critical, to the role of UBE2S in cancer development. Together, UBE2S could be a potential target for lung adenocarcinoma.