• YAKHAK HOEJI
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• v.49 no.1
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• pp.68-73
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• 2005

Epi-xanthatin analogs containing hydrophilic substituents such as carboxylic acid, alcohol, morpholine, amino acid, and glucose derivatives were synthesized and their in vitro cytotoxicity and in vivo antitumor activity were evaluated. The target compounds were generally cytotoxic against tumor cell lines of human origin with $ED_{50}$ values of $0.1{\sim}30{\mu}g/ml$, except the highly hydrophilic analog 6 containing aspartic acid. Contrary to the potent cytotoxicity weakly hydrophilic analogs 2 and 8 were not active in vivo, or even toxic to the test animals. As a result, hydrophilic analog of epi-xanthatin did not show in vitro cytotoxicity and hydrophobic analogs did not show in vivo antitumor activity, thus it is presumed that amphiphilic analogs or those with medium hydrophilicity would exhibit the antitumor potency in vivo.

• Korean Journal of Pharmacognosy
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• v.31 no.1
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• pp.16-22
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• 2000

These studies were designed to determine the potential cytotoxic activity of MeOH extracts of 65 crude drugs against leukemia L1210 and $P388D_1$, cell line in vitro, of which 25 samples were selected. The n-BuOH extracts of 25 samples were measured using the same method and nine were selected. These samples were measured for the potential antitumor activity against $P388D_1$, for life span in vivo, and against sarcoma 180 for tumor weight. On the basis of results, Notoginseng Radix, Anemarrhenae Rhizoma, Albizziae Cortex, Portulacae Herba, Bupleuri Radix were evaluated the effective plant on the antitumor activity. In addition, the mixture of Notoginseng Radix and Albizziae Cortex was evaluated to enhance the antitumor activity in vivo.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.3
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• pp.1163-1169
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• 2014

Astragalus, a commonly used traditional Chinese medicine, has exhibited antitumor actions in patients. In this study, in vitro and in vivo antitumor effects of astragalus and synergistic antitumor efficacy in combination with pterostilbene were investigated. Melanoma cells were treated with pterostilbene (Pt), graduated doses of astragalus injection (AI), or these in combination. Cell viability was measured using a MTT assay. Released nucleosomes and caspase activity were measured using enzyme-linked immunosorbent assay. Growth inhibition in vitro and in vivo was also assessed. Analysis of variance and t tests were used for statistical analysis. Significant reduction (p<0.05) in cellular proliferation were observed with AI and AI-Pt in a time- and concentration-dependent manner. Apoptosis and caspase-3/7 activity were significantly increased by AI and AI-Pt treatment (p<0.05). In vivo, AI inhibited melanoma tumor growth, with inhibition rates ranging from 36.5 to 62.3%, by inducing apoptosis via up-regulation Bax expression and the Bax/Bcl-2 ratio and down-regulating Bcl-2 expression. AI significantly inhibits the growth of melanoma in vitro and in vivo by inducing apoptosis. These data suggest that combined treatment of astragalus with pterostilbene enhances antitumor efficacy.

• Journal of Nutrition and Health
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• v.26 no.4
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• pp.379-389
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• 1993

Several studies have shown that extracts from yellow-green vegetables reveal antitumor activities. In the present study we investigated the effect of phytol in order to elucidate the immunological mechanism of antitumor activity of this substance. The results obtained from the experiment as follows: 1) Phytol showed cytotoxic effect on sarcoma 180 cells in vitro. 2) When phytol was injected into the peritoneal cavity of mice transplanted with sarcoma 180 cells, the average survival time (24.0 days) tended to increase as compared with the nontreated control (19.2 days). 3) When sarcoma 180 cells were injected subcutaneously into the right groin of mice, and then phytol was injected into the peritoneal cavity, the tumor inhibition ratio was 33%. 4) The natural killer(NK) cell activity was significantly augmented by phytol in vitro and in vivo. Similar augmentations of NK cell activity were obtained with culture supernatants of phytol exposed spleen cells and peripheral blood mononuiclear cells. 5) Phytol on the macrophage from peritoneal cavity showed a higher effectiveness in vivo than in vitro. These results indicate that phytol shows the inhibitory effect for growth of sarcoma 180 cells in vitro, also it can augment macrophage and NK cell activities in vivo.

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.457-462
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• 2002

Oregonin, a diarylheptanoid derivative from Alnus hirsuta Turcz, Betulaceae, was evaluated for its antitumor activity. Oregonin, known to have an antitumor function, and is a novel immunomodulator, which may augment macrophage activity. MTT assays and NO production tests were performed in order to investigate the cytotoxicity of oregonin in tumor cells and to examine its influence on macrophage in detail. In this study, the tumoricidal activity was also evaluated by a MTT assay. The cytotoxicity measurements in the oregon in-treated group both in vitro and in vivo showed a significant difference from that of the control group. In vivo, oregonin significantly increased NO production in a dose-dependent manner, and in vitro, the thioglycolate-induced inflammatory macrophages increased NO production in a dose-dependent manner after incubation. These results suggest that oregonin reacts with both the inflammatory and non-inflammatory macrophages in a similar way.

• Archives of Pharmacal Research
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• v.24 no.4
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• pp.323-326
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• 2001

Previous studies have demonstrated that CW252053, a quinazoline antifolate, exhibits potent inhibitory activity against thymidylate synthase (TS) as well as cytotoxic activity against tumor cell lines in vitro. In this studys, we evaluated the in vivo antitumor efficacy of CW252053 in the mouse tumor model. Female B6D2F$_1$ mice were injected with LY3.7. 2C TK-/- (thymidine kinase deficient mouse Iymphoma) cells into the gastrocnemius muscle. Then, CW252053 was administered twice daily by intraperitoneal injection for 10 days, and tumor growth was monitored daily by leg diameter measurement. All animals in the vehicle, 5-FU, and low dose (30mgmg/kg CW252053 treated groups died between days 12 and 23 because of the tumor burden. In contrast, dosing with 60 mg/kg of CW252053 produced a cure rat against tumor growth of 37.5% and a survival rate of 50%. Even more significantly, a higher dose of CW252053 (120 mg/kg) elicited both a 100% cure rate and a 100% survival rate at the termination of the study, confirming that this compound has very potent in vivo antitumor activity against tumor growth. During the experimental period of this study no signs of toxicity were observed even at the high CW252053 dosage rate of 120 mg/kg.

• Archives of Pharmacal Research
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• v.27 no.9
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• pp.915-918
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• 2004

By bioassay-guided separation, an already known saponin, Pulsatilla saponin D was isolated from the root of Pulsatilla koreana Nakai as a antitumor component when evaluated by in vivo antitumor activity as well as in vitro cytotoxic activity test. It showed potent inhibition rate of tumor growth (IR, 82％) at the dose of 6.4 mg/kg on the BDF1 mice bearing LLC cells.

• YAKHAK HOEJI
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• v.43 no.1
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• pp.23-27
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• 1999

We previously reported that the extract of unripe cotton ball of Gossypium indicum shows cytotoxic activity and induces an apoptosis in vitro. In present study, its antitumor activity was investigated in vivo. Butanol soluble extract of unripe cotton ball reduced the weight of solid tumor in sarcoma 180 transplanted mouse model. It showed stronger activity than that of Krestin.

• Korean Journal of Pharmacognosy
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• v.35 no.3 s.138
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• pp.199-202
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• 2004

A highly potent antitumor sesquiterpene O-naphthoquionone has been isolated from Ulmus davidiana, which has been traditionally used as the folk medicine. The structure of this compound was established on the basis of spectral data obtained from UV, IR, MS, and NMR spectrometry, and determined as mansonone E. This compound showed potent antitumor activity on in vivo assay, hollow fiber and xenograft assay.

• Natural Product Sciences
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• v.5 no.1
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• pp.1-6
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• 1999

This study was devised to observe the antitumor activity of mugwort (Artemisia princeps Pampan.) against ICR mice inoculated with sarcoma-180 cells. The antitumor compounds were partially purified from petroleum ether extract of mugwort by silicic acid column chromatography. The active fraction used in in vivo test was obtained under the elution with acetone in silicic acid column chromatography. When the acetone fraction was intraperitoneally injected to the mice which had been subcutaneously inoculated on the left groin with sarcoma-180, the growth rate of tumor (sarcoma-180 mass) was inhibited by 30%. In case the acetone fraction was injected to the mice which had been inoculated intraperitoneally with sarcoma-180, the average life span was prolonged by 20%. After the injection of the active fraction, the spleen index and ${\gamma}-globulin$ ratio (%) were increased significantly (p<0.05). The administration of acetone fraction did not cause any abnormality in the body and the homeostasis of mice. Those observations suggest that the acetone fraction of mugwort extract has an antitumor effect in vivo.