• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.212-212
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• 1994

본 연구소에서 분리하여 항암활성을 측정한바 있는 Sesquiterpene lactone계열의 KR-53170이 in vitro에 비해 in vivo에서 상대적으로 낮은 효력을 보이는데 착안 그 유도체들을 합성함으로써 in vivo stability 및 efficacy를 개선하고자 하였다. 합성된 물질의 in vivo activity는 human tumor cell중에서 A549(폐암), SK-OV-3(난소암1, SK-MEL-2(피부암), XF-498(중추신경계암), HCT-15(직장암)의 5개 암세포를 이용하여 ED$_{50}$($\mu\textrm{g}$/ml )를 측정하였으며 대조물질로는 KR-53170과 Cisplatin이 사용되었다. 그 결과 HR-53170의 terminal methyl ketone이 carboxylic acid로 변환된 CW-251001과 이것의 methyl ester인 CW-251002, ethyl ester인 CW-251003, 그리고 morpheline과 수용성으로 N-methylpiperazine, N-methyl-N'-aminopiperazine, 4-Piperidinopiperidine을 결합시켜서 합성한 CW-251011, CW-251012, CW-251013, CW-251014가 in vitro에서 어느 정도 활성을 유지하였다. 특히 이들중 CW-251001, CW-251012, CW-251013, CW-2s1014는 물에 대한 용해도가 상당히 개선되어 in vivo 활성검색을 위한 후보물질로 고려되었다. 하지만 이들중 CW-251001은 in vivo에서 낮은 농도에서는 활성이 거의 없었으며 놓은 농도에서는 독성을 나타내었다.

• Bulletin of Food Technology
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• v.13 no.2
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• pp.98-108
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• 2000

• Proceedings of the Plant Resources Society of Korea Conference
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• 1996.09a
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• pp.16-26
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• 1996

• Microbiology and Biotechnology Letters
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• v.31 no.4
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• pp.362-367
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• 2003

Coriolus versicolor was grown in a defined synthetic liquid medium and citrus extracts, and the culture extracts were examined for antioxidant activity, nitrite scavenging activity, and in vitro anticancer activity against HeLa, PC-3, HepG2, and A-549 cells. Whereas the culture extracts obtained from the synthetic medium and the un-inoculated citrus extract showed 60 and 22％ of the 1,1-diphenyl-2-picrylhydrazyl radical scavenger activity, the culture extracts obtained from the citrus extracts medium exhibited antioxidant activity up to 89％. The nitrite scavenging activity of the culture extracts obtained from the citrus extracts medium and the synthetic liquid medium, and the un-inoculated citrus extract at pH 1.2 were up to 67, 55, and 34％, respectively. The culture extract obtained from the synthetic liquid medium inhibited the growth of HeLa, PC-3, HepG2, and A-549 up to 66, 23, 18, 10％ at 48 h of incubation, respectively; however, the culture extract obtained from the citrus extracts medium inhibited the growth of HeLa, PC-3, HepG2, and A-549 up to 75, 82, 55, and 82％, respectively. As a negative control, the un-inoculated citrus extract was examined in the same way and inhibited the growth of HeLa, PC-3, and HepG2 cells 20, 6, and 15％ at 48 h incubation, respectively; the inhibition of A-549 cell growth was negligible. These results clearly showed that the fermentation of C. versicolor in the citrus extracts rather than in the defined synthetic medium significantly enhanced the anticancer activity, antioxidant activity, and nitrite scavenging activity.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.224-224
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• 1994

N-arylsulfonylimidazolenes를 항암효과가 우수한 화합물로 설정하여 이들 유도체를 합성하고 이들의 세포독성을 측정한바 있다. 그 이유는 2번 위치의 alkoxy기에 의하여 alkylating agent로서 작용할 수 있다는 개념과 생체 반응 후 생성될 것으로 예상되는 N-arylsulfonylimidazolidinone이 sulofenur와 유사한 작용을 갖을 것으로 기대 되었기 때문이다. 이에따라 N-arylsulfonylimidazolidinone 유도체의 항암효과의 측정이 관심의 대상이 됨에 따라 이들 유도체를 합성하고 이들의 세포독성을 관찰함으로써N-arylsulfonylimidazolidinone 유도체들의 구조 활성 상관관계를 관찰하고자 하였다. 합성은 출발물질을 N-arylsulfonyl-2-alkoxyimidazoline에서 시작 몇단계를 거쳐 목적하는 화합물을 합성 하였다.

• The Korean Journal of Food And Nutrition
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• v.26 no.4
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• pp.609-614
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• 2013

This study was carried out in order to investigate the functional properties of methanol extracts from two parts (root and fruit) of Xanthium strumarium by means of measuring the contents of total polyphenols and flavonoid as well as determining $ABTS{\cdot}^+$, DPPH radical scavenging activity, hydroxyl radical scavenging activity (OH${\cdot}$) and anticancer activity. The examination of physiologically active substances in the two parts revealed that the Xanthium strumarium fruit had high total polyphenol, flavonoid contents, $ABTS{\cdot}^+$ DPPH and hydroxyl radical scavenging activity. The Xanthium strumarium fruit has higher activities of anticancer activities on prostate cell lines compared to other cancer cell lines.

• Journal of Life Science
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• v.9 no.1
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• pp.58-62
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• 1999

Several nucleoside 5'-monophosphate analogues and lipophilic nucleoside 5'-(3-pyridinylcarbonyl)monophosphate analogues were synthesized. Antitumor activities of the synthesized nucleoside malogues against P338 mouse leukemia, FM3A murine mammary carcinoma, and U937 human histiocytic lymphoma cells were determined by MTT assay. Antitumor activities of the lipophilic uridine 5'-(3-pyridinylcarbonyl) monophosphate(7) and 2',3'-didehydro-3'-deoxy-thymidine-5'-(3-pyridinylcarbonyl) monophosphate(8) were stronger than those of uridine 5'-monophosphate(1) and 2',3'-didehydro-3'-deoxythymidine-5'-monophosphate(4). This preliminary experimental result suggests that nucleoside 5'-(3-pyridinylcar-bonyl)monophosphate analogues may be new prodrugs to overcome the clinical limit.

• Korean Journal of Medicinal Crop Science
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• v.7 no.3
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• pp.185-192
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• 1999

Four different parts of Hovenia dulcis $T_{HUNB}$; fruit, bark, vessel area, fruit coat were extracted with water and ethanol. The ethanol extracts of bark, fruit coat and fruit were fractionized into diethyl ether, chloroform and aqueous partitions. Ethanol extract of fruit coat increased the activity of cathepsin B up to 55 %, which can enhance the alcohol dehydration in the liver. The ethanol extracts was more effective than water extracts against the growth of Hep3B, MCF7. The ethanol extracts of bark (0.5mg/ml) inhibited 90% the growth of MCF7. Each extracts and fractions (0.5mg/ml) did not show considerable cytotoxicity on HEL299. In overall, most of the fractions had similar effects to ethanol extracts; however, diethyl ether and chloroform fractions had higher bioactivity than ethanol extracts, but aqueous fraction.

• Journal of Korea Entertainment Industry Association
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• v.13 no.2
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• pp.253-259
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• 2019

Prostate cancer(PrCa) is a leading cause of cancer-related death in man. Medicinal plants are exploited for many drugs to treat various ailments. The drugs derived from the plants promote health, augmented the resistance of the body against disease. Pueraia lobata(wild) Ohwi(P. Lobata), kudzu, which is a twining perennial woody herb native to China, Korea, Japan, India, and the United States. Plants such as Moringa oleifera, have hypoglycemic properties and other beneficial properties. The objective of the study was to analyze the effects of kadzu and moringa, natural plant products on antioxidant activity and proliferation of the hormone-sensitive prostate cancer LNCaP cells. MTT assay, flow cytometry analysis were employed to investigate the anticancer mechanism and DPPH assay was determined to the antioxidant activity to scavenge free radicals in extract of these. All two extracts showed significantly antioxidant activity at 10 and 50mg/ml of concentration. kadzu and moringa reduced LNCaP cell viability in a dose dependent manner. Specially moringa extract was more potent cytotoxic than kadzu extract. Statistical analyses revealed kadzu and moringa exhibited significantly higher (P < 0.05) cytotoxicity and antioxidant activity in LNCaP. The finding of this study provides a scientific basis for using kadzu and moringa in future development of chemotherapeutic drugs against hormone-sensitive prostate cancer.

• Journal of Dairy Science and Biotechnology
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• v.26 no.1
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• pp.5-10
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• 2008

This study was conducted to isolate protein components from culture supernatant of Lactobacillus casei. and measure anti-cancer activity. The protein components were isolated A and B on Ultrafiltration membrane(3, 10, 30, 100 KDa). And the protein components A and B were isolated fractions(number $3{\sim}9$) on FPLC. Experimental studies were progressed through the cell cytotoxicity and anti-cancer activities. Cell cytotoxicity test using human kidney normal cell(293) showed cytotoxicity of below 20% by the protein components A and B($100{\mu}g/mL$). The anti-cancer activity was increased up to 70% by the protein components A and B($100{\mu}g/mL$) in AGS(stomach cancer), A549(lung cancer), MCF-7 (breast cancer), SK-OV-3(ovary cancer) and LoVo(colon cancer). Cell cytotoxicity test was showed cytotoxicity of about 50% by the fractions(number 3, 8, 9) isolated FPLC. The others have not the cytotoxicity about the human normal cell. The anti-cancer activity was increased up to 70% by the fraction number 7 in cancer cell line. Therefore the components isolated from culture supernatant of Lactobacillus casei were showed anti-cancer activity.