• BMB Reports
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• v.49 no.5
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• pp.282-287
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• 2016

Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) is a homo-trimeric cytotoxic ligand. Several studies have demonstrated that incorporation of artificial trimerization motifs into the TRAIL protein leads to the enhancement of biological activity. Here, we show that linkage of the isoleucine zipper hexamerization motif to the N-terminus of TRAIL, referred as ILz(6):TRAIL, leads to multimerization of its trimeric form, which has higher cytotoxic activity compared to its native state. Size exclusion chromatography of ILz(6):TRAIL revealed possible existence of various forms such as trimeric, hexameric, and multimeric (possibly containing one-, two-, and multi-units of trimeric TRAIL, respectively). Increased number of multimerized ILz(6):TRAIL units corresponded with enhanced cytotoxic activity. Further, a high degree of ILz(6):TRAIL multimerization triggered rapid signaling events such as activation of caspases, tBid generation, and chromatin condensation. Taken together, these results indicate that multimerization of TRAIL significantly enhances its cytotoxic activity.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.215.2-216
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• 2003

Velutin and betulinic acid were isolated as a cytotoxic principle from the dichloromethane extract of Korean mistletoe (Viscum album var. coloratum) by repeated silicagel chromatography and recrystallization. In in vitro analysis of cytotoxic activity using NIH-3T3 cells, dichloromethane extract of Korean mistletoe was shown to be highly cytotoxic against tumor cells. And we obtained active compound (reffered to VD-2 and VD-6) from the dichloromethane extract. (omitted)

• Archives of Pharmacal Research
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• v.25 no.3
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• pp.240-249
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• 2002

Dibenzyl-g-butyrolactone and 1,2,3,4-tetrahydro-2-naphthoic acid $\gamma$-lactone (TNL) derivatives were synthesized and evaluated for cytotoxic activity against some cancer cell lines. It was found that TNL derivatives with a shorter distance between C-4 in ring A and C'-2 in ring C were more cytotoxic, while dibenzyl-${\gamma}$-butyrolactones with a longer one were nearly inactive. In TNL series, presence of 3,4-dioxy group in ring A and 2-methoxy group in ring C was essential for the enhancement of the activity.

• Natural Product Sciences
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• v.13 no.2
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• pp.110-113
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• 2007

Five flavonoid derivatives, pinostrobin (1), pinocembrin (2), alpinetin (3), cardamonin (4) and boesenbergin A (5) were isolated from the rhizomes of Boesenbergia pandurata. All compounds were elucidated based on its spectroscopic data and by the comparison with the previous works. 2D NMR technique was used for the structure elucidation of boesenbergin A to complement the data reported previously. The extracts and pure compounds were screened for cytotoxic activity against HL-60 cancer cell lines (human promyelocytic leukemia). Cytotoxic screening showed most of the extracts and pure compounds isolated from the rhizomes of Boesenbergia pandurata were active against HL-60 cancer cell line. The chloroform extract and boesenbergin A showed the most potent cytotoxic activity.

• Advances in Traditional Medicine
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• v.4 no.3
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• pp.179-185
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• 2004

The ethanol extract of Indigofera cordifolia was studied for in vivo gastroprotective activity, cytotoxic activity against oral tumor and normal cells, multidrug resistance (MDR) reversal activity, anti-human immunodeficiency virus (HIV) activity and radical scavenging activity. The extract of I. cordifolia showed potent gastric mucosal protective activity against stomach injury induced by HCl/EtOH solution. However, the gastroprotective activity could not be related to the radical mechanism, because the extract weakly scavenged both OH radical and $O_2*^-$. The extract also showed promising levels of MDR-reversing activity. This study demonstrates the tumor-specific cytotoxic action of the plant extract. However, the extract had no anti-HIV activity. From above results, the study suggests the medicinal importance of I. cordiforia extract.

• The Journal of Korean Medicine
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• v.23 no.2
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• pp.211-224
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• 2002

Background and Objective : In order to investigate the effects of Gilgyunglwedok-tang (GRT) on antitumor activity and antimetastatic activity, studies were done experimentally. Materials and Methods : Experimental studies were perfonned for the cytotoxic effect on BALB/c mouse lung fibroblast cells, the proliferating effect of splenic lymphocyte, the expression of CD3e/CD4, CD3e/CD8, and B220 in peripheral blood mononuclear cells (PBMCs), the cytotoxic effect on A549, SK-OV-3, SK-MEL-2, MCF-7 cells, the inhibitory effect on the activity of DNA topoisomerase I, the T/C% in ICR mice bearing S-180, the inhibitory effect of Cell adhesive of A549 Cells and SK-OY-3 Cells to complex extracellular matrix, the inhibitory effect on lung colonies, the change of lung tissue, the antiangiogenic activity, and the effect on MMP-2 and MMP-9 gene expression in the RT1080 cell line. Results and Conclusion : The results were obtained as follows : 1. In the cytotoxic effect on BALB/C mouse lung fibroblast Cell, GHT didn't show the significant cytotoxic effect on BALB/C mouse lung fibroblast cell compared to the control group. 2. In thymidine uptake assay, GHT showed the significant proliferating effect of splenic lymphocyte in proportion to the concentration. 3. In the expression of CD3e/CD4, CD3e/CD8, and B220 in peripheral blood mononuclea cells (PBMCs) of mice, GRT had no significant change to the normal group in CD4. However, GRT showed an increase to the normal group in CD8 and GHT in the only $1\mu\textrm{g}/ml$ category showed an increase to the normal group in B220. 4. In the cytotoxic effect of GRT on A549, SK-OY-3, SK-MEL-2 and MCF-7 cells, there was no significant cytotoxic effect compared to the control group. 5. In the inhibitory effect on the activity of DNA topoisomerase I, GHT in the $10\mu\textrm{g}/ml$ category showed the inhibitory effect on the activity of DNA topoisomerase I in proportion to the concentration. 6. In the T/C% in ICRmice bearing S-180, GHTtreated group showed 123.7% of T/C% compared to the control group. 7. In the inhibitory effect of cell adhesive of A549 Cells and SK-OV-3 Cells to complex extracellular matrix, GRT in the only $100\mu\textrm{g}/ml$ category showed the significant inhibitory effect compared to the control group. 8. In the inhibitory effect on lung colonies, GHT showed the significant inhibitory effect on lung colonies compared to the control group. 9. In the change of lung tissue, GHT showed a significant decrease of lung cancer growth, interalveolar fibrosis and hyaline material compared to the control group. In the development of lymphocyte around lung cancer cells and lung parenchymal, GHT showed the significant inducement efficacy compared to the control group. 10. In CAM assay, the antiangiogenic activity of GHT showed 30%. 11. In the effect on MMP-2 and MMP-9 gene expression in the RT1080 cell line, GHT had no significant inhibitory effect on MMP-2 and MMP-9 gene expression compared to the control group. According to the above results, it could be suggested that GHT has an antitumor activity and antimetastatic activity.

• Archives of Pharmacal Research
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• v.26 no.11
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• pp.912-916
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• 2003

Four known lanostane triterpenoids, schiprolactone A (1), schisanlactone B (2), nigranoic acid (3) and schisandronic acid (4) Were isolated from the stems of Schisandra henryi for the first time. Their structures were characterized by IR, MS and NMR techniques. Compounds 1, 2 and 4 showed moderate cytotoxic activity against Leukemia cells in vitro. Cytotoxic activity of compounds 1-4 showed $IC_{50}$ of 0.0097, 0.01, 0.097 and 0.0099 $\mu$ mol/mL respectively toward Leukemia cells and $IC_{50}$ of 0.097, 0.1, 0.097 and 0.099 $\mu$mol/mL toward Hela cells respectively. It is the first report that these compounds possess cytotoxic activity on Leukemia and Hela cells.

• Archives of Pharmacal Research
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• v.22 no.4
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• pp.380-383
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• 1999

Five 1-azzanthraquinone-3-carboxamides were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines. The most active compound, 7b, exhibited cytotoxic activity comparable to doxorubicin.

• YAKHAK HOEJI
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• v.52 no.4
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• pp.252-258
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• 2008

The cytotoxic effect of benzoic acid and related compounds on the growth of normal cell lines and human oral epithelioid cell line was evaluated by the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and 2,3-bis-[2-methoxy-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-caboxanilide (XTT) methods. 3,4,5-Trihydroxybenzoic acid decreased the cell viability of human oral epithelioid cells and the cell adhesion activity of human oral epithelioid cells. Under the light microscopy, 100 ${\mu}M$ 3,4,5-trihydroxybenzoic acid showed the highest cytotoxic activity. From these results, we can propose that 3,4,5-trihydroxybenzoic acid has a potential anticancer activity.

• Biomolecules & Therapeutics
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• v.9 no.3
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• pp.143-155
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• 2001

Many attention has been focused on developing new chemotherapeutic agents for a treatment of cancer from natural products. From Carpesium divaricatum S. et Z. (Compositae), various monoterpenoid compounds were isolated and exhibited mild antitumor activity against human tumor cell lines. These facts prompted us to explore the structure-activity relationship of these compounds. The synthesis of monoterpenoid compound was accomplished by Fries rearrangement, Grignard reaction, elimination, allylic oxidation, esterification and epoxidation as key steps. The results of in vitro cytotoxicity (A549, SK-OV-3, SK-MEL-2, XF498, HCT15) of the synthesised compounds are as follows: First of all, epoxide moiety is prerequisite for cytotoxic activity in diester compound. Any kind of compounds with olefin or diol moiety instead of epoxide ring exhibited poor or mild cytotoxic activity respectively. Of o-acetoxy and isobutoxy epoxy esters, p-sub-stituted phenylacetate compounds exhibited high cytotoxic activities against SK-MEL-2 and HCT15.