• Archives of Pharmacal Research
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• 제25권4호
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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.

• Macromolecular Research
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• 제16권6호
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• pp.510-516
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• 2008

New antitumor active polymers, poly(methacryloyl-2-oxy-1,2,3-propanetricarboxylic acid-co-exo-3,6-epoxy-l,2,3,6-tetrahydrophthalic acid) [poly(MTCA-co-ETAc)], poly(methacryloyl-2-oxy-l,2,3-propanetricarboxylic acid-co-hydrogen ethyl-exo-3,6-epoxy-l,2,3,6-tetrahydrophthalate) [poly(MTCA-co-HEET)], and poly(methacryloyl-2-oxy-l,2,3-propanetricarboxylic acid-co-a-ethoxy-exo-3,6-epoxy-1,2,3,6-tetrahydrophthaloyl-5-fluorouracil) [poly(MTCA-co-EETFU)] were synthesized and characterized. Their antitumor activity, inhibition of DNA replication and antiangiogenesis were examined. The structures of the polymers were identified by FT-IR, $^1H$ and $^{13}C$-NMR spectroscopy. The number average molecular weights of the fractionated polymers determined by GPC ranged from 9,400 to 14,900, and polydispersity indices were less than 1.7. The in vitro cytotoxicity of these polymers was determined and their antitumor activity was evaluated. The $IC_{50}$ values (the drug concentration at inhibition of 50% tumor growth) indicated that the synthesized polymers were much better inhibitors of cancer cells and showed lower cytotoxicity than the free 5-FU. The in vivo antitumor activity of the conjugates was examined using mice bearing the sarcoma 180 tumor cell line. The life spans (TIC) of the mice treated with the conjugates were higher than those treated with the free 5-FU. In addition, the synthesized conjugates showed excellent antiangiogenic activity based on an embryo chorioallantoic membrane assay.

• 대한수의학회지
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• 제33권4호
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• pp.701-710
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• 1993

The pine needles, Pinus densiflow Sieb. et Zucc., which is a feed for goats showing a low incidence rate of cancer were evaluated to confirm the potent anticancer effects, with or without several conventional anticancer drugs. The pine needles collected from Mt. Buk-Han located near Seoul were extracted with 95% methanol and methand and concentrated. From the methanol extract, SOM-A, was extracted dichlormethane and SOM-B was extracted with ethyl acetate. SOM-C was extracted with distilled water. These extracts were tested for their antitumor activities in vitro and in vivo. Among them, SOM-A and SOM-C exhibited potent antitumor activities described as belows. 1. The cytotoxic effects of SOM-A and SOM-C were examined against in vitro cultured murine and humman tumor cells. SOM-A showed strong cytotoxicity against human tumor cell lines and SOM-C showed strong cytotoxicity against murine tumor cell lines tested. 2. The antitumor effects of SOM-A and SOM-C were examined against P388 and L1210 of mouse ascitic tumors. The highest mean survival time(MST) ration was 151%(P388) for SOM-C(90mg/kg). 3. To compare the antitumor effects of SOM-A, SOM-B, and SOM-C against solid tumors, S-180 and Ehrlich carcinoma were implanted subcutaneously to mice on Day O. The drugs were given intraperitoneally to mice once a day on Days 1-20, and the tumor weights were measured on Day 21. SOM-A showed inhibition of tumor growth more than 50% in the experiment on S-180 and Ehrlich, and SOM-C also markedly inhibited tumor growth. However, SOM-B had no effect. 4. SOM-C combined with ${\alpha}$-interferon and SOM-C combined with Mitomycin-C enhanced the antitumor activities against murine ascitic tumors P388 leukemia.

• Toxicological Research
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• 제19권2호
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• pp.147-152
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• 2003

We investigated antitumor activities of the ethanol extract from mushroom Phellinus linteus and Phellinus baumii on mulberry, oak and elm. in vitro test, the ethanol extract of mushroom cultivated on oak of Phellinus linteus showed highest activities about SK-OV-3, HCT15, XF498, SK-MEL-2 and A549. SK-OV-3 cell line showed 100% cytotoxicity in 100 $\mu\textrm{g}$/ml and HCT15 (98.39%), XF498 (89.62%), SK-MEL-2 (84.07%) and A549 (79.92%) cytotoxicity respectively. Also $IC_{50}$ showed 3.99 $\mu\textrm{g}$/ml to SK-OV-3 cell line and HCT15 (4.37 $\mu\textrm{g}$/ml), A549 (5.48 $\mu\textrm{g}$/ml), SK-MEL-2 (6.72 $\mu\textrm{g}$/ml), XF 498 (6.88 $\mu\textrm{g}$/ml). As those results, cultivated oak of Phellinus linteus showed a very low $IC_{50}$ value against SK-OV-3, HCT15, XF498, SK-MEL-2 and A549 cancer cell lines.

• Archives of Pharmacal Research
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• 제29권12호
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• pp.1091-1095
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• 2006

For the development of novel antitumor agents, we designed and synthesized terpyridines, and their biological activities were evaluated. Although most of the newly prepared terpyridines showed strong cytotoxicity against several human cancer cell lines, [2,2';6',2"]-terpyridine displayed the most significant cytotoxicity.

• Archives of Pharmacal Research
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• 제25권5호
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• pp.600-607
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• 2002

Two series of 2,3-diarylcyclopent-2-ene-1-ones including 2-aryl-3-(2,5-dihydroxyphenyl)cyclopent-2-ene-1-ones (2a∼2f) and 3-aryl-2-(3',4',5'-trimethoxyphenyl)cyclopent-2-ene-1-one (3a∼3j) were synthesized and evaluated for the cytotoxicity against three tumor cell lines; B16F10, HCT116 and A431. It was found that the 3,4,5-trimethoxy substituent was optimal for the bioactivity of compounds in series 2. Meanwhile, compounds in series 3 exhibited the most potent cytotoxicity with 3-aryl ring being 4-methoxyphenyl (compound 3f), (3-hydroxy-4-methoxy)phenyl (compound 3e), or (3-amino-4-methoxy)phenyl (compound 3j).

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.347.3-347.3
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• 2002

Recent study indicated that terpyridine and its derivatives displayed highly active antitumor properties. In this presentation. derivatives of terpyridines having three pyridine moieties at 2',4',6'-position of central pyridine skeleton were prepared, and evaluated their cytotoxicity against several human cancer cell lines and topoisomerase I inhibitory activities. Most of the prepared compounds showed strong cytotoxicity compared to doxorubicln. In addition. several compounds displayed better cytotoxicity than that of doxorubicin. In addition, several compounds displayed better cytotoxicity than that of doxorubicin. Structure-activity relationship study was perfomed to be indicated that [2.2':6',2']terpyidine skeleton is important to show strong xytotoxicity. Significant topoxicity. Significant topoisomerase I inhibitory activity was not observed for prepared compounds.

• Archives of Pharmacal Research
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• 제18권6호
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• pp.396-401
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• 1995

As a part of trials to develop the antitumor agent from tannins isolated from plants, the antitumor activity of peduculagin, an ellagitannin, isolated from Alnus hirsuta var. microphylla was examined in vitro and in vivo. In vitro, the cytotoxicity was determined by 0.4% typanblue dye exclusion method. peduculagin showed the dose-dependent cytotoxicity against human chronic myelogenous leukemia (K-562), human promyelocytic leukemia (HL-60), mouse lymphoid neoplasm (P388), mouse lymphocytic leukemia (L1210) and mouse sarcoma 180(S180) cell lines. $ED_{50}\; values\; (ED_{50})$ of each cell line were 5.30, 0.92, 2.78, 9.35 and $1.38 \mug/ml$ respectively. The most sensitive cell line was HL-60. In vivo, pedunculagin was administered to ICR mouse with the doses of 50 and $100{\;}{\mu}g/ml$intraperitoneally once at 20 days before S180 inoculation. peduculagin showed the antitumor activity and its T/C ratio (%) was 120.82% in the group of both concentrations.

• 생약학회지
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• 제30권2호
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• pp.130-136
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• 1999

The cytotoxic and antitumor activity of Herba cratalariae sessiliflorae on cultured NIH 3T3 fibroblast and human oral epitheloid carcinoma cells were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) colorimetric method. The light microscopic study was carried out to observe morphological changes of cultured mouse fibroblast and human oral epitheloid carcinoma cells (KB). These results were obtained as follows; Ethyl acetate, chloroform and hexane extracts showed a significant cytotoxicity in NIH 3T3 fibroblast, but the other extracts did not show. All extracts exhibited a significant antitumor activity in human oral epitheloid carcinoma cells, but ethanol extract did not show a antitumor activity. Hexane extract showed low cytotoxic effect, but exhibited the most antitumor activity. The MTT absorbance in NIH 3T3 fibroblast was significantly decreased by treatment with chloroform, ethyl acetate and hexane extracts respectively. Human oral epitheloid carcinoma cells was significantly decreasd by treatment with all extracts with the exception of ethanol extract. The difference in MTT absorbance in two cell Types was most remarkable when treated with water and hexane extracts. Cholroform and hexane extracts showed the strongest effect in growth inhibition of human oral epitheloid carcinoma cells. These results indicated that water extract possessed no cytotoxicity and a strong antitumor activity.

• 대한한방내과학회지
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• 제21권3호
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• pp.425-432
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• 2000

Objective : It is well known that Gagamsojeokbackchool-san show antitumor effects and its activities are result from enhancement of immune function, we investigated the antitumor effects of Sambonggangyongbaneo-tang and its mechanism. Methods : We measured change of body weight, weight of immune organs (Spleen, Thymus), Liver, Kidney, tumor weight, cytotoxicity for investigation of antitumor effects of Sambonggangyongbaneo-tang. Results : 1. The body weight of mouse has no significant difference between control and sample groups. 2. The weights of immune organs (Spleen and Thymus) decreased significantly in sample groups. The weights of Liver and Kidney have no significant difference. 3. The tumor weights in mouse decreased significantly in sample groups and showed dose-dependent effect. 4. Cell viability of Sarcoma 180 has no significant difference in sample groups. 5. HeLa cell viability has no significant difference in low concentration, but it decreased significantly in high concentration. Conclusions : According to the above results, it could be suggested that Sambonggangyongbaneo-tang has prominant antitumor effects and cytotoxicity.