• Animal cells and systems
• /
• v.16 no.4
• /
• pp.289-294
• /
• 2012

Histone methylation has diverse functions including transcriptional regulation via its lysine or arginine residue methylation. Studies indicate that deregulation of histone methylation is linked to human cancers including leukemia. Histone H3K27 methyltrnasferase response element II binding protein (RE-IIBP), as a transcriptional repressor to target gene IL-5, interacts with HDAC and is over-expressed in leukemia patient samples. In this study, we have identified that hematopoiesis-related genes GATA1 and HOXA9 are down-regulated by RE-IIBP in K562 and 293T cells. Transient reporter analysis revealed that GATA1 transcription was repressed by RE-IIBP. On the other hand, HOXA9 and PBX-related homeobox gene MEIS1 was up-regulated by RE-IIBP. These results suggest that RE-IIBP might have a role in hematopoiesis or leukemogenesis by regulating the transcription of target genes, possibly via its H3K27 methyltransferase activity.

• Archives of Pharmacal Research
• /
• v.23 no.4
• /
• pp.288-301
• /
• 2000

A series of 2-alkyl, 2-aryl, and 2-piperazinyl benzimidazole-4,7-dione derivatives (7a-h) and 16m-o) were prepared, and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia cell line P388, and human gastric carcinoma cell lines SNU-1 and SNU-16). These compounds showed potent cytotoxicity against all of three cell lines tested, and especially SNU-16 was sensitive to them. 2-Aryl (7g,h) and 2-piperazinyl benzimidazole-4,7-dione derivative (I6 m) were more potent than mitomycin C against P388 and SNU-16. Among benzimidazole-4,7-dione derivatives with alkyl group at position 2, 7a had the most potent cytotoxicity against all of the cell lines tested.

• Natural Product Sciences
• /
• v.19 no.1
• /
• pp.66-70
• /
• 2013

Ten compounds (1 - 10), palmitic acid (1), 10-nonacosanol (2), pentacosan-1-ol (3), phytol (4), ${\beta}$-sitosterol (5), ${\beta}$-sitosterol-3-O-${\beta}$-D-glucopyranoside (6), 2,4-dihydroxycinnamic acid (7), hyperoside (8), uridine (9) and adenosine (10), were isolated from the n-hexane and EtOAc-soluble fractions of the aerial parts of A. dioicus var. kamtschaticus (Rosaceae). The structures of these compounds were elucidated on the basis of spectroscopic evidence. All compounds (1 - 10) were isolated for the first time from this plant. Cytotoxicity of 1 - 10 against Jurkat T (T-lymphocytic leukemia cells), HeLa (Human cervical epitheloid carcinoma cells), MCF-7 (Human breast cancer cells), and HL-60 (Human promyelocytic leukemia cells) cell lines was measured. Compound 6 showed good cytotoxicity against HL-60 cell line with $IC_{50}$ value of 8.13 ${\mu}g/mL$. In addition, compounds 7 and 8 exhibited antioxidant activity with $IC_{50}$ values of 16.30 and 12.42 ${\mu}g/mL$, respectively.

• Journal of the Korean Magnetic Resonance Society
• /
• v.10 no.1
• /
• pp.89-95
• /
• 2006

The methanolic extract of the marine sponge Raspilia hirsute collected from Keomun Island resulted in three types of sterols: a mixture of (24S)-Poriferasta-5, 25-diene-$3\beta$, 24-diol and (24R)-Stigmasta-5, 25-diene-$3\beta$, 24 -diol (1), 25,26,27-Trinorcholest-5-en-$3\beta$,24-diol (2), and Pregn-5-en-20-on-$3\beta$-ol (3). The isolation and structural determination of these sterols are reported here. Compound 1 showed moderate cytotoxicity against human Leukemia cell line K562.

• 대한동의생리학회:학술대회논문집
• /
• 2005.07a
• /
• pp.13-13
• /
• 2005

• Proceedings of the Zoological Society Korea Conference
• /
• 2003.08a
• /
• pp.174.4-174
• /
• 2003

No Abstract, See Full Text

• Proceedings of the PSK Conference
• /
• 2003.10b
• /
• pp.159.2-159.2
• /
• 2003

Codonopside lc is an active natural compound isolated from the roots of Codonopsis lanceolata (Campanulaceae), a Korean medicinal herb. In the present study, we investigated the in vitro effect of Codonopside 1c on the proliferation and induction of apoptosis in HL-60 human promyelocytic cells. When HL-60 cells were treated with Codonopside 1c, evidence of apoptotic features, including DNA fragmentation, formation of DNA ladder in agarose gel elecrophoresis and increse of annexin V binding, were obtained. (omitted)

• Biomolecules & Therapeutics
• /
• v.9 no.4
• /
• pp.282-284
• /
• 2001

The antiallergic drug, cetirizine, inhibits the histamine release from a rat basophilic leukemia (RBL-2H3) cell line, which is frequently used as a mast cell model. By investigating inhibitory activities of (+)- and (-)-cetirizine in RBL-2H3 cells on the histamine release, we aimed to evaluate the effect of their structual characteristics on the antihistamine activity. The study on RBL-2H3 cell has clearly demonstrated that the (-)-cetirizine is significantly more potent than the (+)- or the racemic cetirizine, although there was no difference in pharmacokinetics between (+)- and (-)-cetirizine in rats.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.24 no.1
• /
• pp.1-9
• /
• 1995

1, 25(OH)2-23ene-D3 is a novel vitamine D3 analog which has a double bond between C-23 and C-24. We describe the effects of this analog on cell differentiation and cell proliferation in vitro using the human histiocytic lymphoma cell line U937, and on calcium metabolism in rats in vivo. In the present investigation 1, 25(OH)2-23ene-D3 was compared to the natural metabolite of vitamin D3, 1$\alpha$, 25-dihydroxycholecalciferol[1, 25(OH)2-23ene-D3 was more potent than 1, 25(OH)2-23ene-D3 for inhibition of proliferation and induction of differentiation of U937 cells. Especially, its effect on induction of differentiation, as measured by superoxide production and nonspecific esterase(NSE) activity, was about 20-fold more potent that 1, 25(OH)2-23ene-D3. This analog morphologically and functionally differentiated U937 cells to monocyte-macrophage phenotype showing a decrease of N/C ratio in Giemsa staining and the increase of adherence ability to surface. Intraperitoneal administration of 1, 25(OH)2-23ene-D3 to rats showed that the compound had at least 50 times less activity than 1, 25(OH)2-23ene-D3 in causing hypercalcemia and hypercalciuria. The strong direct effects of 1, 25(OH)2-23ene-D3 on cell proliferation and cell differentiation, coupled with its decreased activity of calcium metabolism make this compound an interesting candidate for clinical studies including patients with leukemia, as well as several skin disorders, such as psoriasis.

• Biomedical Science Letters
• /
• v.17 no.3
• /
• pp.217-223
• /
• 2011

${\beta}$-sitosterol glucoside exists in a variety of plants and have anti-tumor, anti-microbial, and immunomodulatory activities. Mast cells and eosinophils play important roles in a variety of inflammatory diseases, specifically asthma and atopic dermatitis. In the present study, we used lactose-${\beta}$-sitosterol (L-BS) and investigated the effect of L-BS on inflammatory responses of the human mast cell line, HMC-1 and the human eosinophilic leukemia cell line, EoL-1. In HMC-1 cells, L-BS significantly inhibited cell migration in response to stem cell factor without cytotoxicity. However, the mRNA expression of CC chemokine receptors (CCRs), including CCR1-5, were not altered after L-BS treatment in HMC-1 cells. LPS-induced IL-4 production was also suppressed by L-BS in a dose-dependent manner. In EoL-1 cells, the concentration ranging from 0.1 ${\mu}M$ to 10 ${\mu}M$ of L-BS had no cytotoxicity and had no effect on mRNA expression of major protein-mediators derived from activated eosinophils. However, 100 ${\mu}M$ of L-BS induced the apoptosis of EoL-1 cells in a time-dependent manner. This finding indicates the possibility of L-BS as a potential therapeutic molecule in inflammatory diseases and may contribute to the need to improve current therapeutic drugs.