• Archives of Pharmacal Research
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• 제27권9호
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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.

• 약학회지
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• 제43권1호
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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.

• 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.

• Archives of Pharmacal Research
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• 제27권9호
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• pp.893-900
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• 2004

2- or 6-Substituted BZT-N derivatives were synthesized, and their cytotoxic activity against can-cer L1210 and SNU-1 cells was examined. The antitumor action was also assessed in mice bearing S-180 cells in peritoneal cavity. In a comparison, it was found that 6-substituted BZT-N derivatives exhibited higher potencies in both bioactivities than 2-substituted BZT-N derivatives against L1210 cells in in vitro and S-180 in vitro tests exception of compound 36. Interestingly, it was observed that 2-substituted compound 36, which has methyl group at RI position, exhib-ited a better antitumor activity than 6-substituted compounds against L1210 and SNU-1 in vitro. The EDso value of 2-substituted compound 36 against L1210 was found to be comparable to the EDso value of adriamycin and was even better against the solid cancer cell line SNU-1. It was also observed that 2-substituted compound 36 showed better antitumor activity in mice bearing S-180 cells in the peritoneal cavity. The T/C (％) value of 2-substituted compound 36 was simi-lar to that of adriamycin. Quantitative structure-activity relationship (QSAR) tests reveal that the experimental E $D_{50}$ values against SNU-1 closely correlate with both the calculated HOMO ener-gies ( $E_{HOMO}$) and the measured H-NMR chemical shift of 3-H ($\delta$$_{H}$). The results suggests that a compound having higher $E_{HOMO}$ and $\delta$$_{H}$ values usually should have a lower E $D_{50}$ (SNU-1) value.lue.lue.lue.

• Archives of Pharmacal Research
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• 제19권3호
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• pp.228-230
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• 1996

Cannabigerol(3) was synthesized and evaluated for its inhibitory activity against mouse skin melanoma cells. Cannabigerol displayed significant antitumor activity [inhibitory concentration $(IC_{50})=31.31\mug/mL]$ in vitro assay.

• 생약학회지
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• 제31권1호
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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.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 1999년도 The 6th International Symposium on the Development of Anti-Cancer Resource from Plants
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• pp.84-89
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• 1999

The present study has been undertaken to detect edible medicinal plants with antineoplastic property on the basic of a number of traditional Korean medical literatures, besides studies on development of anti-cancer medical wild plants growing in Korea and to prove experimentally their efficacy by in vitro and in vivo tests.235 species from 45 family 79 genus were screened primarily as edible sources of antitumor effect. Among those the crude. extracts of 40 spp. showed considerable cytotoxicity in vitro and especially Pegangkuen(Patrinia scabiosaefolia), Deod-eog(Codonopsis lanceolata), Okssusu(Zea may), and Geureong(Eragrositis ferru-ginea) exhibited significant antitumor activity against sarcoma 180 asites mice. However, additional researches should be mode for the confirmation of their availability as antitumor plants.

• Archives of Pharmacal Research
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• 제20권4호
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• pp.368-371
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• 1997

In an effort to increase of the antitumor activity of 2(S)-$2^{I}$,$5^{I}$-trihydroxy-7, 8-dimethoxyflavanone isolated from Scutellaria indica, we synthesized its analogues, II, III and IV. They showed potent cytotoxicity in vitro against cancer cell lines, L1210, K562 and A549. On the basis of $ED_50$ values against the cancer cell lines, III exhibited about 2-7 times stronger activity than I against various cell lines. We tested the antitumor activity of the analogues against Sarcoma 180 cells in vivo and evaluated the structure-activity relationship. The antitumor activity appeared to be related to the hydrogen bond between carbonyl group at C-4 and hydroxyl group at C-5, in contrast to cytotoxic action.

• Archives of Pharmacal Research
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• 제20권2호
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• pp.138-143
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• 1997

5-Aryl-2,3-dihydroimidazo[2,1-a]isoquinolines were reported to have strong antitumor activity and one of the derivatives such as $5-[4^{l}$ -(piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,1-a] isoquinoline (1, SDZ 62-434) was found to be more effective than the clinical cytostatic agent edelfosine (2) in in vitro and in vivo assays. Currently SDZ 62-434 is in clinical trials in Europe. The structure-activity relationship studies of SDZ 62-434 showed that compounds with substitution on ring A were less active than the lead compound. Ring B in SDZ 62-434 was essential for the activity because compounds without B ring had no antitumor activity. Among the 3-arylisoquinolin-1-one derivatives, $3-[4^{I}$-(piperidinomethyl)phenyl] substituted analog had no antitumor activity but simple phenyl substituted compound, such as 4, showed the most potent antitumor activity in various human tumor cell lines.

• 약학회지
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• 제45권6호
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• pp.617-622
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• 2001

A protein-polysaccharide fraction of a Korean wild mushroom Psathyrella velutina, PVP, was prepared and its antitumor immunomodulatory activity was investigated. When PVP was administered once daily for seven days from day 1 to day 7 into male ICR mice implanted with 1 $\times$ 10$^{5}$ cells of sarcom 180 tumor cells into the peritoneum on day 4, it inhibited the growth of sarcoma 180 cells by 92.8%. In XTT assay, PVP also exhorted in vitro anti-proliferation activity on U-937, a human monoblastoid cell line, as well as sarcoma 180 cells. PVP showed marked stimulatory activity on the immune system in that it induced the accumulation of PEC (the stimulation index, Sl=4.90 at 100 mg/kg), stimulated the BALB/c mouse splenic lymphocytes to form lymphoblasts (Sl=5.75 at 100$\mu\textrm{g}$/ml), and upergulated the expression of CD25 molecules. All these results strongly support that PVP exhorts its antitumor activity through stimulation of the immune system as well as anti-proliferative activity on the tumor cells.