• Archives of Pharmacal Research
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• 제23권2호
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• pp.167-171
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• 2000

We have investigated the in vitro cytotoxic effect of liposome-encapsulated N-(phospho-nacetyl)-L-aspartic acid (PALA) against C-26 murine colon cancer cells, and have compared it in this regard to free PALA. Three different PALA-containing liposomal formulations using distearoylphosphatidylcholine (DSPC), distearoylphosphatidylglycerol (DSPG), and polyethyle-neglycol-derivatized distearoylphosphatidylethanolamine (PEG-DSPE) were made and their cytotoxicity was measured. In 72 hr continuous exposure experiment with C-26 cells, the 50% growth inhibitory concentration ($IC_50$) of DSPG-PALA liposome formulation was $0.09\mu\$, which showed about 65-fold more potent than unencapsulated free PALA ($5.1\mu\$). Similar degree of increase in cytotoxicity was also observed in 1 hr exposure experiment. However the $IC_50$ of PEG-DSPE-PALA liposome and DSPC-PALA liposome were $10.7\mu\$and $11.8\mu\$respectively, which showed slightly less potent than unencapsulated free PALA. Physical characteristics of PALA-liposomes, such as the size and drug:lipid ratio were also determined. In conclusion, negatively-charged DSPG-PALA liposome showed the highest cytotoxic effect among tested on the C-26 cells in vitro.

• Maxillofacial Plastic and Reconstructive Surgery
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• 제18권2호
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• pp.316-322
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• 1996

불소의 유전물질에 대한 독성효과는 현재까지 논란의 대상이되고 있으며, 서로 상반된 연구 결과들이 보고되고 있다. 저자는 불소의 세포 유전학적 효과를 규명하고자 실험실 내에서 배양된 편평상피암 세포주에 염화불소를 처리하여 세포독성 검사와 염색체이상 검사를 시행하여 다음과 같은 결론을 얻었다. 1. 염화불소의 농도와 처리시간에 비례하여 세포성장이 현저히 감소하므로 염화불소는 편평상피암 세포주에 독성을 가진다. 2. 염화불소의 농도가 증가할수록 염색체이상 발현빈도가 현저히 높게 나타나므로 염화불소는 편평상피암 세포주에서 DNA 손상을 야기할 수 있다. 염색체 이상의 형태는 chromatid break가 가장 많이 나타났다.

• 약학회지
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• 제38권6호
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• pp.627-636
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• 1994

Several Pt(II) and Pt(IV) complexes of N,N'-bis(2-hydroxyethyl)ethylenediamine(2-HEen) and N,N'-bis(2-chloroethyl) ethylenediamine(2-CEen) as carrier ligand were prepared. Water soluble Pt complexes were also synthesized by modification of leaving groups. The cytotoxicity of these compounds against leukemia L1210 and P388 cell in vitro were examined. The Pt complexes containing 2-CEen showed more effective cytotoxicity than those containing 2-HEen. Through the nephrotoxicity tests on the primary cultured proximal tubular cells of rabbit kidney and human kidney cells in vitro, Pt complexes with 2-CEen showed higher than those with 2-HEen which were consistent with cytotoxicity but showed very low nephrotoxicity compared with cisplatin. Also the values of BUN and creatinine in serum of Pt complexes were reduced remarkably compared with cisplatin, therefore it can be concluded that new Pt complexes seems to have much lower nephrotoxicity than cisplatin.

• 혜화의학회지
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• 제5권2호
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• pp.503-507
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• 1997

The cytotoxicity-guided fractionation of the roots of Sophora flavescens (Leguminosae) extracts led to the isolation of fifteen active principles 1~15, responsible for the cytotoxicity against five kinds of cultured human tumor cell lines, i.e., A549(non small cell lung), SK-OV-3(ovary), SK-MEL-2(skin), XF498(central nerve system) and HCT-15(colon), evaluated by SRB method in vitro. Compounds 2~14 were classified as unusual flavonoid occurred exclusively in this species and the proliferation of each examined tumor cells were significantly inhibited during the continuous exposure to compounds 1~15 for 48 hours, respectively.

• 약학회지
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• 제39권6호
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• pp.681-688
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• 1995

An n-hexane extract of the roots of Aralia cordata Thunb. (Araliaceae) was found to show significant in vitro cytotoxic activity against P388D$_{1}$ lymphocytic leukemia cell in culture. Bioactivity-directed fractionation of this extract led to the isolation of four polyacetylenes, falcarindiol (1), dehydrofalcarindiol (2), falcarindiol-8-acetate (3) and dehydrofalcarindiol-8-acetate (4). Cytotoxicity of compounds 1 and 3 was found to be better than that of compounds 2 and 4 when these compounds were tested against eight in vitro tumor cell lines, namely, A549, HCT15, DLD1, MCF7, SKOV3, HL60, K562 and P388D$_{1}$. The fact that the cytotoxicity of compounds 1 and 3 against series of tumor cell lines was much stronger than that of compounds 2 and 4 suggested that the saturated carbon chain at the termial and the hydroxyl group at the C-3 are important for the activities. The requirement for the activity was further confirmed by synthesizing and assaying the acetate derivatives of compounds 1 and 2.

• 한국식품과학회지
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• 제36권2호
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• pp.339-344
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• 2004

유자는 성숙할수록 과피와 과육의 총페놀 함량은 많아지고 자유기 소거능이 높아지는 경향을 보였다. 유자로부터 추출한 18가지 용매 추출물의 항산화 활성과 전립선 암세포 DU 145, LN-CaP에 대한 세포독성 실험을 실시한 결과 과피와 과육 모두 미성숙한 유자 보다 성숙한 후 수확한 유자가 그 활성이 높게 나타냈다. 용매별로 살펴보면 과성숙 유자 과피, 과육의 클로로포름, 메탄올 추출물은 전립선 암세포 DU 145에 대하여 60% 이상의 세포사멸 효과를 나타났으며 메탄올 추출물의 효과도 농도에 따라 상당히 높은 것으로 나타났다. 또한 세포 조직을 현미경으로 살펴본 결과 추출물의 처리 농도가 증가할수록 세포 사멸이 쉽게 이루어지는 것을 확인 할 수 있었다. 이런 세포 사멸의 경향은 추출물의 자유기 소거 환성이 높을수록 높게 나타났다.

• 대한한의학방제학회지
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• 제17권2호
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• pp.73-83
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• 2009

Objective : In vitro proapoptotic effect of Hangbaek-Tang (HBT) has been documented by one of us. In the present study, we aimed to demonstrate in vivo effect of HBT on tumor growth. Methods : In vitro selective cytotoxicity of HBT was examined by enumeration of viable cell numbers using BC3A mouse leukemic cells and normal spleen cells. In vivo effect of HBT (25 and 50 mg/mouse) on tumor growth was assayed using BC3A cells innoculated subcutaneously in the flank. Annexin-V apoptosis assay and PI staining was performed to determine the effective serum factor in HBT-treated mice. Leukocyte recruitment into peritoneum were analyzed by microscopy with a stained cytosmear of peritoneal lavage fluid. Results : HBT exhibited in vitro selective cytotoxicity to leukemic cells and did not show any toxicity on immune organs. In vivo i.p. administration of HBT induced significant reduction in tumor growth but not complete regression. Sera obtained from HBT-treated mice strongly inhibited BC3A cell growth in vitro and were revealed to markedly enhance apoptosis and accompanying cell death, when compared to those from PBS-treated mice. Abundant extravasation of leukocytes, especially neutrophils, into peritoneum was observed in HBT-treated mice. Conclusions : HBT causes leukemic, BC3A cell death in vivo via apoptosis as well as in vitro, for which functional involvement of leukocytes is suggested.

• Journal of Microbiology and Biotechnology
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• 제10권1호
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• pp.43-47
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• 2000

In vitro cytotoxicity and antioxidative effects of water extracts prepared from Mustard Leaf Kimchi (MLK) during its fermentation period were investigated. The cytotoxicity against HepG2 (human hepatic cancer) by water extracts from the well fermented Mustard Leaf Kimchi was higher than others (fermented for 0 to 6 days at 18$^{\circ}C$), and IC50 of water extracts at the points of 6, 8, 10, and 14days during fermentation were 213.4, 99.2, 99.9, and 109.8${\mu}{\textrm}{m}$/ml, respectively. Antioxidative activity of water extracts from MLK during various fermentation periods was higher than that of blank distilled water. However, the antioxidative activity of well-fermented water extracts of MLK (fermented for 8-14 days) did not show any difference from that of others (fermented for 2-6 days). Thus, water extracts of well-fermented MLK (fermented during 8-14 days) significantly inhibited the growth of cancer cells in vitro, but little antioxidative activity was influenced by the various fermentation periods.

• Asian Pacific Journal of Cancer Prevention
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• 제16권15호
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• pp.6581-6589
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• 2015

Background: Previously, stingless bee (Trigona spp.) products from East Kalimantan, Indonesia, were successfully screened for in vitro antiproliferative activity against human cancer derived cell lines. It was established that propolis from T. incisa presented the highest in vitro cytotoxicity against the SW620 colon cancer cell line (6% cell survival in $20{\mu}g/mL$). Materials and Methods: Propolis from T. incisa was extracted with methanol and further partitioned with n-hexane, ethyl acetate and methanol. The in vitro cytotoxicity of the extracts was assessed by the MTT assay against human colon (SW620), liver (Hep-G2), gastric (KATO-III), lung (Chago) and breast (BT474) cancer derived cell lines. The active fractions were further enriched by silica gel quick column, absorption and size exclusion chromatography. The purity of each fraction was checked by thin layer chromatography. Cytotoxicity in BT-474 cells induced by cardanol compared to doxorubicin were evaluated by MTT assay, induction of cell cycle arrest and cell death by flow cytometric analysis of propidium iodide and annexin-V stained cells. Results: A cardol isomer was found to be the major compound in one active fraction (F45) of T. incisa propolis, with a cytotoxicity against the SW620 ($IC_{50}$ of $4.51{\pm}0.76{\mu}g/mL$), KATO-III (IC50 of $6.06{\pm}0.39{\mu}g/mL$), Hep-G2 ($IC_{50}$ of $0.71{\pm}0.22{\mu}g/mL$), Chago I ($IC_{50}$ of $0.81{\pm}0.18{\mu}g/mL$) and BT474 (IC50 of $4.28{\pm}0.14{\mu}g/mL$) cell lines. Early apoptosis (programmed cell death) of SW620 cells was induced by the cardol containing F45 fraction at the $IC_{50}$ and $IC_{80}$ concentrations, respectively, within 2-6 h of incubation. In addition, the F45 fraction induced cell cycle arrest at the G1 subphase. Conclusions: Indonesian stingless bee (T. incisa) propolis had moderately potent in vitro anticancer activity on human cancer derived cell lines. Cardol or 5-pentadecyl resorcinol was identified as a major active compound and induced apoptosis in SW620 cells in an early period (${\leq}6h$) and cell cycle arrest at the G1 subphase. Thus, cardol is a potential candidate for cancer chemotherapy.

• Archives of Pharmacal Research
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• 제18권1호
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• pp.60-61
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• 1995