• 한국식품과학회지
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• 제35권3호
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• pp.479-482
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• 2003

동과자 열수 추출물의 in vitro 항암효과는 2 mg/mL의 농도에서 가장 높게 나타났으며 in vivo 상에서의 0.1 g/kg, 0.01 g/kg의 경구 투여시 각각 21%, 17%의 생명연장율(increased life span, ILS)을 나타내었다. SK-OV-3에 대한 SRB assay를 이용한 열수 추출물(2 mg/mL)의 방사선(5 Gy) 병용 투여에 있어서 86%의 저해효과를 나타내었다.

• 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.

• Food Science and Biotechnology
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• 제15권3호
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• pp.369-373
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• 2006

Water extracts obtained from cultured mountain ginseng (CMG) were evaluated for their ability to stimulate immune cells and inhibit cancer cell proliferation. The lymphocyte subpopulation in mouse splenocytes in vivo was significantly increased by the administration of the CMG extract (27.4 mg/mouse). Interleukin-2 and ${\gamma}$-interferon in the mice serum increased up to 30% in CMG extract-treated mice. At a concentration of 1.37 mg/mL, nitric oxide increased up to 400% in the macrophage cell line treated with CMG extract. The CMG extract significantly retarded the proliferation of human acute promyelocytic (HL60), human histiocytic (U937), and mouse lymphocytic (L1210) leukemia cell lines in vitro at concentrations over 2.74-13.7 mg/mL. In addition, CMG extract treatments (1.37 mg/mL and 2.74 mg/mL) lead to the increased expression of the p53 gene and protein in cultured U937 leukemia cell lines. These results indicate that water extracts of CMG are capable of both immune cell stimulation and cancer cell growth inhibition.

• Archives of Pharmacal Research
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• 제21권2호
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• pp.198-206
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• 1998

Fourty eight derivatives of 2-(1-oxyalkyl)-1,4-dioxy-9,10-anthraquinone were synthesized, and their antitumor activity was evaluated. On the whole, 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinones (DHAQ=1,4-dihydroxy-9,10-anthraquinone) showed stronger cytotoxic activity against L1210 cells than 2-(l-hydroxyalkyl)-1,4-dimethoxy-9,10-anthraquinones(DMAQ =1,4-dimethoxy-9,10-anthraquinone), implying that free hydroxy groups at C-1 and C-4 of the anthraquinone structure are necessary for the cytotoxic activity. The bioactivity of 2-(lhydroxyalkyl)-DHAQ derivatives differed according to the size of alkyl group at C-1;while the elongation of alkyl group over 7 carbon atoms failed to enhance the bioactivity, the derivatives possessing alkyl moiety of 1-6 carbon atoms showed an increase in the cytotoxicity and the antitumor activity in Sarcoma-180; 2-hydroxymethyl-DHAQ ($ED_{50}$, $15\mu\textrm{g}$/ml; T/C, 125%), 2-(1 -hydroxyethyl)-DHAQ($1.9{\mu}g/ml;139.2%)$;, 2-(1-hydroxypropyl)-DHAQ ($7.2{\mu}g$/ml; 135.1%), 2-(1-hydroxybutyl)-DHAQ ($10.2{\mu}g/ml; 125.3%)$, 2-(1-hydroxypentyl)-DHAQ ($23.7{\mu}g/ml; 110.1%$). and 2-(1-hydroxyhexyl)-DHAQ ($58{\mu}g/ml;108%$). Next, 2-(1-Hydroxyalkyl)-DHAQ derivatives were acetylated to produce 2-(1-acetoxyalkyl)-DHAQ analogues. Although the acetylation somewhat enhanced the cytotoxicity, but not the antitumor action. In addition, the presence of phenyl group at $C-1^{l}$ enhanced the cytotoxicity and the T/C value, compared to alkyl groups of same size; 2-(1-hydroxy-1-phenyl)-DHAQ ($ED_{50}$, $5.6{\mu}g$, T/C, 137%).

• 한국식품영양과학회지
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• 제28권2호
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• pp.458-463
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• 1999

Methanol extract and its fraction of traditional fermented soybean paste(doenjang) from Soonchang area were studied for growth suppression on the various tumor cells and suppression components, by using HPLC and GC were analysed. Hexane fraction of methanol extract was indicated 79%, 76%, 67%, 66%, 78% of growth suppression on L1210, P338D1, HepG2, WiDr and SNU 1 tumor cells, respectively. Ethylacetate fraction of methanol extract also showed 81%, 75%, 75%, 76% and 82% of growth suppression on the same tumor cells, respectively. Peak 8 obtained from HPLC of ethylacetate fraction indicated 81%, 77%, 77%, 75% and 79% of growth suppression on the same tumor cells and identified as a genistein, by comparing with standard one by HPLC analysis. Hexane fraction of methanol extract contained oleic acid, linoleic acid and palmitic acid.

• Advances in Traditional Medicine
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• 제1권2호
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• pp.45-51
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• 2000

This study was carried out to evaluate cytotoxicity of the methanol extract from Sophora flavescens Ait. against L1210 (lymphocytic leukemia) and $P388D_1$ (lymphoid neoplasma) Cells in vitro. We have determined cytotoxicity by the MTT (3- (4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H- tetrazolium bromide) assay. The order of cytotoxicity of Sophora flavescens Ait. extracts against L1210 and $P388D_1$ cells in vitro is as follows: Fr. 4 > Fr. 3 > Fr. 5 > Fr. 2 > Fr. 1. These results suggest that the fraction 4 of the methanol extracts from Sophora flavescens Ait. may be a valuable choice for the development of antitumor agents. In order to develop an antimicrobial agent, dried Sophora flavescens Ait. was extracted with hot methanol, and then antimicrobial activity (MIC test) was investigated. In this study, the fraction 3 of the methanol extracts from the roots of S. flavescens showed strong growth inhibition activity against gram-positive and gram-negative bacteria (MIC, $3.125\;{\mu}g/ml$) such as S. mutans, S. epidermidis and P. putida. These results indicate that fractions 3 and 4 inhibit tumor cells and bacteria.

• 약학회지
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• 제45권2호
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• pp.133-139
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• 2001

To improve water solubility of 1,4-dihydroxy-9,10-anthraquinone moiety, 23 of 2-(1-aminoacetylalkyl)-1,4-dihydroxy-9,10-anthraquinone derivatives, which contain nitrogen atom, were synthesized. Of the synthesized compounds, 18 compounds were more cytotoxic on L1210 cells than 2-(1-acetyloxyalkyl)-1,4-dihydroxy-9,10-anthraquinone as comparative structure. This result might be due to the increased hydrophilicity of the compounds.

• Archives of Pharmacal Research
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• 제21권6호
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• pp.738-743
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• 1998

Thirty six 5,8-dimethoxy-1,4-naphthoquinone derivatives, which bear unsaturated alkyl side chain with ester bond, were synthesized and tested cytotoxic activity on L1210 cells a nd antitumor activity against ICR mice bearing S-180 cells. It could be recognized that the cytotoxicities of naphthoquinones with R1, being methyl and propyl (IV1~24) were not enhanced by replacing the alkanoyls with alkenoyls. In contrast, the introduction of the alkenoyl moieties on the compounds with $R_1$=hexyl (IV25~36) resulted in the enhancement of their cytotoxicities. Replacement of alkanoyl group with an alkenoyl group generally increased the T/C value of the mice bearing S-180 cells.

• 약학회지
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• 제42권3호
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• pp.275-283
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• 1998

Aclarubicin(ACL)-entrapped freeze dried liposomes were prepared using Microfludizer to attain a sustained release at targeted organs in a prolonged time so that it can reduce th e side effect and maximize the therapeutic effect. The freeze-dried liposomes were evaluated for pharmacokinetics, antitumor activity against Sarcoma 180, cytotoxicity against L1210 and A549 tumor cells, spleen toxicity and myelosuppressive action. The $AUC_{0{\rightarrow}8hr}$ values were $122{\pm}42,\;382{\pm}140,\;419{\pm}171,\;835{\pm}206\;and\;443{\pm}309{\mu}g{\cdot}min/ml$ for free ACL. ACL-liposome formulation I, II, III and IV, respectively. Cytotoidcity of ACL-entrapped liposomes against L1210 and A549 tumor cells was 2-4 times higher than that of free aclarubicin. ACL-liposome formulation I(PC/CHOL/TA) showed the most potent antitumor activity against Sarcoma 180 in mice. The loss of body weight was much smaller with ACL-entrapped liposomes than free ACL after I.p. injection at a dose of 2 mg/kg/day. Compared to free ACL, ACL-entrapped liposomes expressed a lower and delayed spleen toxicity up to 5th day after I.v. administration. Myelosupperssion seemed to be lower with ACL-entrapped liposome of PC/PC-hydrate/CHOL/TA (formulation III) than free aclarubicin.

• 한국식품영양학회지
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• 제16권1호
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• pp.15-21
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• 2003

버섯 균사체로부터 분리한 단백다당체의 Th1 cell 증식효과 및 각종 암세포에 대한 세포독성을 조사하였다. 단백다당체 시료는 영지버섯, 아가리쿠스, 표고버섯, 운지버섯, 그리고 상황버섯을 10$0^{\circ}C$에서 3시간 열수 추출하는 방법으로 조제하였다. Th1 cell의 세포증식을 조사한 결과, 10mg/$m\ell$ 농도에서 모든 시료가 40% 이상 억제하는 효과가 있는 것으로 나타났다. 7 종류의 암세포를 이용한 암세포 생존율을 조사한 결과, 1mg/$m\ell$ 농도에서 P388D1와 L1210에서 아가리쿠스는 2.4%와 39.7%, 표고버섯은 48.4%와 52.5%의 생존율을 보였다. Sarcoma 180으로 복수암을 유발시킨 마우스에게 아가리쿠스와 표고버섯으로부터 추출한 단백다당체를 섭취시킬 경우 생존율이 27~40%까지 유의적으로 증가하는 것으로 나타났다.