• 약학회지
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• 제40권2호
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• pp.225-229
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• 1996

The cytotoixic effect of Pylorae Herba (Pyrola japonica Klenze) against L1210 and K-562 cells was studied in vitro. The methanolic extract of Pylorae Radix was add ed to the culture of L1210 cells and K-562 cells for the cytotoxic activity and the ED50 values of hexane, ethylacetate, buthanol and water fractions from methanolic extract were determined using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazoliumbromide) assay. The active constituent isolated by bioassay guided fractionation followed by purification gave rise to a yellow needle crystal and was clarified to be chimaphilline by the comparison with the published data. The average life spans with it were not prolonged significantly on tumor growth in hybrid female mouse (BDF1-KIST) inoculated subcutaneously with P388 cells.

• Archives of Pharmacal Research
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• 제23권2호
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• pp.155-158
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• 2000

Bioassay-guided fractionation of Crataegus pinnatifida (Rosaceae) gave two cytotoxic ursane-type triterpenes which were identified as uvaol (1) and ursolic acid (2) by physicochemical and spectroscopic methods. 3-Oxo-ursolic acid (3) was synthesized from ursolic acid (2) by Jones method. The cytotoxic activities of these compounds were tested against murine L1210 and human cancer cell lines (A549, SK-OV-3, SK-MEL-2, XF498, and HCT15) in vitro. Compounds 1 and 2 showed moderate cytotoxicities against L1210, whereas they showed weak activities against human cancer cell lines. However compound 3 exhibited potent cytotoxic activities both in murine and in human cancer cell lines.

• Journal of Ginseng Research
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• 제17권1호
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• pp.52-60
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• 1993

Panax ginseng has been extensively used in the traditional oriental medicine as a restorative, tonic and Prophylactic agent. Recently, several reports regarding to anticancer effects of Panax ginseng has accumulated. These studies emphasized the fact that the anticancer activities might be due to a glycoside group called ginsenoside or pan.u saponin which has a water soluble characteristic. However, the authors and collaborates demonstrated that a highly lipid soluble component in extract of Panax ginseng roots contains a considerable cytotoxic activities against marine leukemic cells (L1210, P388) and human censer cells (HRT-18, HT-29, HCT48). This study was devised to observe the cytotoxic activities of Petroleum-ether extract of Panax giuseng roots (crude GBD and its Partially Purified fraction from silicic acid column chromatography (7 : 3 GX) against sarcoma-180 (5-180) and Walker carcinosar- coma 256 (Walker 256) in vivo, and murine leukemic Lymphocytes (L1210) and human rectal cancer cells (HRT-18) and human colon cancer cells (HT-29 and HCT48) in vitro. Each cell-line was cultured in medium containing serial concentration of the crude GX or 7 : 3 GX in vitro. A highly lipid soluble compound in the extract of Panax ginseng root was cytocidal to murine leukemic cells and human colon and rectal cancer cells in vitro. In the meantime, ginseng saponin derivatives did not have cytotoxic effects at its corresponding concentration. The growth rates of the cancer cells in medium containing ginseng extracts were inhibited gradually to a significant degree roughly in proportion to the increase of the extract concentration. The cytotoxic activity of 7 : 3 GX was about 3 times more potent than that of crude GX, one unit of cytotoxic activity against L1210 cells being equivalent to 2.54 Ug and 058 Ug for the crude GX and 7 : 3 GX, respectively. The Ri value of the active compound on silica- gel thin layer chromatography with petroleum-ether/ethyl ether/acetic acid mixture (90 : 10 : 1, v/v/v) as a developing so lvent was 053. While, the Panaxydol and Panaxynol as active compounds were purified from Petroleum-ether extract of Panax ginseng root by Drs. Ahn and Kim, and author found out that the one unit of cytotoxic activity of the Panaxydol and Panaxynol against L1210 cells being equivalent to 056 Ug and 0.3918 respectively. The survival times of mice inoculated with S-180 cells were extended about 1.5 to 2 times by the 7 : 3 GX treatment compared with their control group. The significantly decreased hemoglobin values of rats after inoculation with Walker 256 were recovered to normal range by oral administration of the crude Gt The synthetic levels of protein, DNA and RNA in human colon and rectal cancer cells were significantly diminished by treatment with the crude GX, which can explain a part of the origin of its anticancer activity.

• 약학회지
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• 제30권4호
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• pp.193-197
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• 1986

A strongly cytotoxic fraction (Fc-2, ED50=0.0003$\mu\textrm{g}$/ml) against L1210 cell was obtained from the root, seed and fruit of Trichosanthes kirilowii. Administration of Fc-2 prolonged the life span of the BDF1 mice bearing L1210 and the ICR mice bearing S-180 by 135%, and 130%, respectively. The Fc-2 affected L1210 cells were enlarged in their diameters two or three times in comparison with the untreated ones. When 20mg/kg of Fc-2 was administered, intraperitoneally, all the mice were killed.

• Archives of Pharmacal Research
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• 제25권5호
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• pp.652-654
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• 2002

Brine shrimp assay-guided fractionation and isolation of the EtOAc soluble fraction of Phryma leptostachya L. (Phrymacaceae) gave two active compounds, phrymarolin II (1) and ursolic acid (2), which were identified by physicochemical and spectroscopic methods. Compound 1 exhibited potent lethality with $LD_{50}$ value of 0.0013 $\mu\textrm{g}$/ml, whereas 2 showed moderate lethality with $LD_{50}$ value of 27.0 $\mu\textrm{g}$/ml against brine shrimp. The cytotoxic activities of 1 and 2 were also evaluated against one murine and five human cancer cell lines employing the sulforhodamin B (SRB) method. Compound 2 exhibited cytotoxic activity against L1210 and SK-MEL-2 cells with $ED_{50}$ values of 3.70 and 9.27 mg/ml, respectively, whereas 1 was devoid of any cytotoxic activity against all cancer cells tested.

• Archives of Pharmacal Research
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• 제20권2호
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• pp.110-114
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• 1997

This research was performed to screen the cytotoxic activities of some pharmaceutical insect relatives. Cytotoxic activities of total extract and fractions of hexane, ethyl acetate, methanol, water and boiling water were extracted from four pharmaceutical insect relatives: the Chinese gall, the cicada slough, the hornet nest and the batryticated silkworm. These extracts were investigated against the cancer cell lines of L1210, P388 and SNU-1 in vitro tests. Results showed that, ED, , against the cancer cell lines of L1210, P388 and SNU-1 were 0.55, 0.50, and $0.83{\mu}g/ml$ in the ethyl acetate fraction from the Chinese gall; 1.07, 2.19, and $2.24{\mu}g/ml$in the ethyl acetate fraction, 1.51, 1.26, and $1.45{\mu}g/ml$ in the water fraction and 1.48, 2.29, and $1.29{\mu}g/ml$in the boiling water fraction from the cicada slough; 3.31, 2.00, and $6.61\mug/ml$ in the water fraction from the hornet nest and 13.80, 19.95, and $31.62{\mu}g/ml$in the hexane fraction and 33.88, 21.88, and $25.12{\mu}g/ml$in the ethyl acetate fraction from the batryticated silkworm, respectively. All of the fractions mentioned above showed high cytotoxic activities and could be suggested for further studies in vivo tests.

• Archives of Pharmacal Research
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• 제19권5호
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• pp.416-422
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• 1996

Twenty one phenylacetylshikonin analogues were synthesized from various subsitituted phenyl acetic acids and their cytotoxicity values against A549, K562 and L1210 cell lines and antitumor action in mice bearing S-180 cells were measured. All of phenylacetylshikonin analogues expressed a potent cytotoxicity $(ED_{50}, 0.1-1.80{\mu}g/ml)$ against L1210 and K562 cells. L1210 cells were the most sensitive to shikonin analogues among these cells. Except 4-methosyphenylacetylshikonin $(0.098 {\mu}g/ml)$, and a-acetoxyphenylacetylshikonin $(0.10 {\mu}g/ml)$, all other shikonin derivatives sshowed higher $ED_{50}$ values than phenylacetylshikonin $(0.13{\mu}g/ml)$, in L1210. In K562 cell, a-substitution of phenylacetylshikonin $(0.1{\mu}g/ml)$, while other subsitutions increased it slightly; 4-methoxyphenylacetylshikonin $(0.033{\mu}g/ml)$ showed a exceptionally good cytotoxicity against K562 cell. 4-Halogenation tended to decrease the cytotoxic effect on L1210 cells, while it enhanced the effect on K562; 4-bromophenylacetyl $$[ED_{50};(L1210)=1.76{\mu}g/ml, ;ED_{50};(K 562)=0.32 {\mu}g/ml]$$ and 4-chlorophenylacetyl shikonin $$[ED_{50};(L1210)=1.64 {\mu}g/ml, ;ED_{50};(K562)=0.32 {\mu}g/ml]$$. In contrast, A549 cells were much less sensitive to these shikonin analogues which showed $ED_{50}$ values of$1.5-1.35 {\mu}g/ml)$.Most of phenylacetylshikonin derivatives showed good antitumor activity in mice bearing S-180 cells. a-A-cetoxyphenylacetylshikonin and 4-dimethylaminophenylacetylshikonin showed highest T/C value (192-195%), implying that introduction of a-acetyl or of 4-dimethylamino group enhanced the antitumor activity as shown for 4-dimethylaminophenylacetylshikonin (T/C, 192%). It might be due to improvement of water solubility by dimethylamino group in the molecule.

• 생약학회지
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• 제35권4호통권139호
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• pp.293-299
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• 2004

The current investigation was carried out to find out the anticancer activity of the methanol extract from Buplerum falcatum against cancered ICR mouse and cancer cell lines such as J774A.1 and L1210 cells. Extract of Buplerum falcatum displayed the considerable augmentation(134%) of the survival of ICR mouse bearing Sarcoma 180 cancer. In addition, the cytotoxic effects of methanol extract of Buplerum falcatum against J774A.1 cells and L1210 cells were found to show $IC_{50}$ values of $57.3\;{\mu}g/ml$ and $54.6\;{\mu}g/ml$, respectively. In contrast to such cytotoxicity against cancer cells, the extract exerted only meagre toxicity against normal lymphocytes. The increased generation of $O_2^-$ and the considerably increased activities of super-oxide dismutase(SOD) and glutathione peroxidase(GPx) of both J774A.1 cells and L1210 cells in the presence of Buplerum falcatum extract implied that the observed cytotoxicities may have resulted from the detrimental effect of reactive oxygen species(ROS) evoked by Buplerum falcatum extract on the cancer cells.

• Applied Biological Chemistry
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• 제38권3호
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• pp.273-277
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• 1995

60종의 생약의 methanol 추출물을 L1210세포에 대하여 1차스크리닝실험을 수행하여 항암활성물질을 검색하고, 그 중에서 비교적 세포독성이 강하게 나타나는 산국(Chrysanthemum boreale M.)에서 항암활성물질을 분리정제하였다. 산국의 용매분획물의 L1210, K562, A549세포에 대한 세포독성실험에서는 chloroform 분획에서 $ED_{50}$값이 각각 3.98, 4.28, 3.84 (${\mu}g/ml$)로 나타났다. 이 chloroform 분획에서 유효세포독성물질을 정제하여 Compound I과 Compound II를 각각 얻었으며, 이 중에서 Compound I은 L1210, K562, A549세포에 대하여 각각 $ED_{50}$값이 0.55, 0.0003, 0.001 (${\mu}g/ml$)로 강한 세포독성을 나타내었으나, Compound II는 K562에 대해서만 $ED_{50}$ 값이 4.79 (${\mu}g/ml$)의 세포독성을 나타내었다.

• 동의신경정신과학회지
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• 제3권1호
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• pp.84-90
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• 1992

Solvent and TLC-fractionations of the root of Salvia miltiorrhiza have yielded the results as follows ; Solvent fractions Petr. ether Ether Ethy1 acetate Water Control 100uL 0 0.2 35.1 41.9 43.0 50ul 0.7 3.7 37.2 42.0 TLC-fractionation and the Cytotoxic activity Fractions I II III IV V VI Petr. ehter Control 100uL13.0 7.1 16.8 1.2 30.9 23.2 0.5 48.3 50uL 37.1 26.1 30.0 20.1 45.7 27.2 29.7 Among the solvent fractions the petroleum ehter fraction corresponding to the concentration of 20ug/ml has showed the strongest Cytotoxic activity. (no cell survived) A double dilution of the fraction(10ug/ml) still showed strong activity.(0.2 cells survived) The ether fraction contained strong activity. Of the fraction which have veen obtained by a prcparative silicagel TLC I, II, III & IV were cytotoxic, but V and VI were inactive Howevcr, it is worthwhile to note that no one of these has no strong Cytotoxicity as the pertoleum ether fraction itself. This observation says that the active fractions could be additive or synergic to each other. The most active fraction, IV, was scrached out from the TLC and its UV-spectrum taken. The absorption maxima were 207 and 272 nm, indicating the presence of a flavanone strucuture.