• Korean Journal of Pharmacognosy
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• v.13 no.2
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• pp.55-61
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• 1982

Thirtyfour species of Korean medicinal plants which have been frequently used in oriental herb prescriptions were evaluated on their cytotoxicity and potential antitumor activities against AC glioma(9 ASK) in vitro. Dose of $100{\mu}g/ml$ of plant extracts appeared to exhibit slight cytotoxicity. Seven plant extracts, Aralia continentalis(Araliaceae), Lycium chinensis(Solanaceae), Epimedium koreanum(Berberidaceae), Platyodon grandiflorium(Campanulaceae), Pleuropterus multiflorus(Polygonaceae), Rheum undulatun(Polygonaceae) and Scutellaria baicalensis(Laminaceae), exhibited significant reversal$(51{\sim}90%)$ of astrocyte formation into original neuroglial cells' morphology through the prescreen tests.

• Korean Journal of Pharmacognosy
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• v.27 no.1
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• pp.42-46
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• 1996

The medicinal formula, Kilkyungtang (KKT) and two modified Kilkyungtangs (KKT-1 and KKT-2), which were supplemented by the additional crude drug, Houttuyniae herba (KKT-1), and Oldenlandiae diffusae herba (KKT-2) to KKT, had been applied widely as decoctions for the treatment of malignant tumors. Cytotoxic activities against two tumor cell lines, A549 and $B16-F_0$ were investigated. However, none of them were found to exhibit significant cytotoxicity upon tested tumor cells below the concentration of $1000{\mu}g/ml$. However, cytotoxic activities of three reputed antitumor agents, i.e., mitomycin C (MMC), cisplatin (CPT) and 5-fluorouracil (5-FU) was significantly potentiated by the combined treatment of them with KKT, KKT-1 and KKT-2 respectively, especially against A549 (human non small cell lung adenocarcinoma), in vitro.

• YAKHAK HOEJI
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• v.34 no.4
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• pp.262-266
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• 1990

Acetylshikonine, isolated from the root of Lithospermum erythrorhizon showed a strong cytotoxic activity ($ED_{50}=0.10\;ug/ml$) against L1210 cell and T/C = 182% in ICR mice bearing S-180 at a dose of 5 mg/kg. Administrations of 10 mg/kg and 15 mg/kg reduced the T/C values to 60 and 77% respectively. Higher doses reveal toxicity. Seven naphthazarin derivatives synthesized showed good cytotoxic activities against L1210 cell. Especially, naphthazarin and hydronaphthazarin have strong activities ($ED_{50}=0.05\;ug/ml$ for both). Naphthazarin showed a severe toxic effect on ICR mice bearing S-180; no significant toxic effect was observed at a dose of 1 mg/kg or 2 mg/kg, but a severe toxicity (T/C = 23%) by administration of 5 mg/kg. Alkylation of C-2 of naphthazarin is necessary for reducing the toxic effect on ICR mice bearing S-180.

• Bulletin of the Korean Chemical Society
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• v.23 no.3
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• pp.391-394
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• 2002

Berberine and berberrubine, which display antitumor activity, have also demonstrated distinct enzyme-poisoning activities by stabilizing topoisomerase Ⅱ-DNA cleavable complexes. The protoberberine berberrubine differs in chemical structure with berberine at only one position, however, it shows a prominent activity difference from berberine. Solution structures of berberine and berberrubine determined by NMR spectroscopy are similar, however, the minor structural rearrangement has been observed near 19 methoxy or hydroxyl group. We suggest that the DNA cleavage activities of topoisomerase Ⅱ poisons could be correlated with both chemical environments and minor structural change together with hydrophobicity of interacting side chains of drugs with DNA molecule.

• YAKHAK HOEJI
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• v.15 no.1
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• pp.16-23
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• 1971

Seven organic arsine compounds are synthesized as potential anti-tumor agents are subjected to the screening test of activity against SN-36 Leukemia, Sarcoma 180 and Ehrlich ascites carcinoma. Three compounds, namely N-(5-Nitrofroyl)-p-arsanilic acid, N-(2, 4-Dihydroxybenzoethyl)-p-arsanilic acid and N-$\alpha$(p-arsanilido) acetyl thiourea of the all synthesized compounds showed comparatively potential activities against experimental ascitic tumors both through cytological findings and survival duration.

• Journal of Microbiology and Biotechnology
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• v.21 no.10
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• pp.1043-1048
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• 2011

A methanol extract of Cassia tora seeds was successively partitioned with diethyl ether, chloroform, ethyl acetate, and water, and the antitumor-promoting activity of the solvent fractions was determined by inhibition of Epstein-Barr virus early antigen (EBV-EA) activation induced by teleocidin B-4 in Raji cells. The diethyl ether (68.7%) and chloroform (91.2%) fractions and the hydrolysate (94.3%) of the ethyl acetate fraction had strong inhibitory activities. The chloroform and ethyl acetate fractions were chromatographed on silica gel and further purified by HPLC. Three active compounds, obtusifolin-2-glucoside (75.0%), chryso-obtusin-6-glucoside (56.8%), and norrubrofusarin-6-glucoside (39.4%), were obtained from the ethyl acetate fraction, and two active compounds, questin (97.9%) and chryso-obtusin (53.8%), were isolated from the chloroform fraction.

• 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.

• Journal of Life Science
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• v.9 no.6
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• pp.677-683
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• 1999

Gamdutang aqua-acupuncture solution (GAS), Gamdutang water-extracted solution (GWS) and Dae-Gamdutang aqua-acupuncture solution (DGAS) were prepared and tested for antitumor activities. It was shown to possess considerable toxicity toward various tumor cell lines. Concentration of 5 $\times$ and 10$\times$ of GAS resulted in more than 70% inhibition of growth in Ehrlich ascites tumor cells (EATC), Hepa1c1c7 and A549. GAS at concentrations of 5$\times$ and 10$\times$ revealed more than 60% inhibition in HeLa. GWS showed more than 50% inhibition of growth with EATC and HeLa at concentrations of 5$\times$ and 10$\times$, respectively. Toxicity assay with GWS in Hepa1c1c7 and A549 revealed that more than 80% inhibition of growth at the concentration of 5$\times$ and 10$\times$. In morphological study, the number of cells were decreased, and the shape of cells was round-form in EATC, Hepa1c1c7, A549, HeLa with GAS.

• Preventive Nutrition and Food Science
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• v.4 no.2
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• pp.117-121
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• 1999

The anititumor and immunologic activities of the glycoproteins extracted from sea cucumber (Stichopus japonicus) on mice bearing sarcoma 180 cells were investigated . Maximum tumor suppression (64%) occurred at the dose of 100mg glycoprotein/kg. The highest prolongation ratio was achieved at the level of 100mg/kg an dincreased by 395 more than that of control. Glycoproteins from sea cucumber exhibited direct cytotoxic effect on the tumor cells. Dose dependent increase of leucocyte, peritoneal exudate cell and weights of immunoorgans revealed the improvement of immunity. When the glycoportein-administered group was compared with the control, a significant difference was not noted in the clinico-chemical values such as S-GOT, S-GPT , alkaline phoshatse activity, total protein, cholesterol, triglyceride, urea nitrogen and glucose levels in blood. These results suggests that the antitumor activity of sea cucumber glycoprotein is associated with activation of cells in the immune system.

• Archives of Pharmacal Research
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• v.21 no.4
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• pp.445-451
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• 1998

A series of 5-hydroxy-4-quinolone (3) and 5-methoxy-4-quinolone (4) derivatives were synthesized as truncated acridone analogues and evaluated for antitumor, antiheroes and antituberculosis activities. Among them 5-hydroxy-8-methoxy-quinolone showed potent antitumor activity ($IC_{50}$=17.7 $\mu\textrm{M}$ for HL60) which was greater than that of acronycine. However, these compounds didn't show any significant antiheroes or antituberculosis activity.