• Natural Product Sciences
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• 제25권4호
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• pp.311-316
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• 2019

Artocarpus heterophyllus has been used as traditional medicine. This plant is one of the sources of flavonoid. Flavonoid compounds possessed a wide range of biological properties including anticancer. This study was performed to investigate the cytotoxic effect of flavonoids from A. heterophyllus on H460 and MCF-7 cell lines. The interaction of flavonoids and cisplatin against tested cancer cells was also evaluated. MTT assay was used to determine the cytotoxic effect of flavonoid. Isobologram analysis was selected to evaluate the synergistic effect between flavonoid and cisplatin, their interaction was then confirmed using AO/PI staining method. Amongst of flavonoid compounds, artocarpin exhibited strong cytotoxic effect on both MCF-7 and H460 cell lines with IC₅₀ values of 12.53 ㎍/mL (28.73 μM) and 9.77 ㎍/mL (22.40 μM), respectively. This compound enhanced anticancer activity of cisplatin against H460 and MCF-7. The combination produced a synergistic effect on H460 and MCF-7 cell lines with a combination index (CI) values of 0.2 and 0.18, respectively. The AO/PI stained demonstrated that the combination of artocarpin and cisplatin caused morphological changes that indicated apoptosis. Moreover, artocarpanone also significantly increased cytotoxic effect of cisplatin compared to its single concentration with CI below than 1. This result suggested the potency of flavonoid named artocarpin to enhance the anticancer activity of cisplatin on H460 and MCF-7 cell lines.

• 한국식품영양과학회지
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• 제35권7호
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• pp.823-827
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• 2006

신선한 미더덕을 동결건조하여 분말로 만들어 water, MeOH, EtOH 및 acetone의 용매로 추출하여 항암활성을 조사하였다. 대장암 세포주 HT-29에 대한 미더덕 추출물의 암세포증식 억제효과는 ethanol 추출물이 $500\;{\mu}g/mL$ 농도에서 45.0%로 가장 높은 활성을 보였으며, 대조구와 다른 추출물에 비교하여 크게 세포의 응축과 세포수의 감소를 형태학적으로 관찰할 수 있다. 용매별 추출물 중 가장 강력한 항암활성을 가지는 ethanol 추출물을 이용하여 정제수율을 높여 암세포 성장억제효과를 확인하기 위하여 n-hexane, diethyl ether, ethyl acetate 및 water 순으로 극성을 높여 분획한 결과 diethyl ether 분획물에서 가장 높은 항암활성을 나타내었다. 그리고 diethyl ether 분획물을 인간대장암 유래의 세포주 SW620, 자궁경부암 세포 HeLa 및 유방암 세포 MCF-7에 처리하였을 때 농도 의존적으로 높은 항암활성이 나타났으며, 가장 높은 농도 $500\;{\mu}g/mL$ 처리 시 모두 10%이하의 세포 생존율을 나타내었다. 지금까지는 한약재를 비롯한 농산물 유래의 추출물이 항암효과를 보이는 연구가 보고된바 있으나 해양생물 유래의 추출물에서 항암효과를 보이는 결과에 대하여 구체적으로 보고된 바가 없는 실정이다. 따라서 이번 연구결과는 생리활성 물질을 탐색함에 있어서 해양생물이 중요한 천연자원이 될 수 있다는 가능성을 확인할 수 있었다.

• Natural Product Sciences
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• 제24권2호
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• pp.93-98
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• 2018

Medicinal plants are potential sources of anticancer agents screening. A large number of phytochemicals, including triterpenoids, have been reported to have significant cytotoxic effects on cancer cells. From the fruits of Ligustrum japonicum Thunb., thirteen triterpenoids (1 - 13) were isolated and evaluated for their cytotoxic activity against Hela and HL-60 cells. As results, 8 (oleanolic acid) showed significant effects on Hela with $IC_{50}$ values of $5.5{\mu}M$, and moderate effects on HL-60 cells with $IC_{50}$ values of $55.9{\mu}M$. Meanwhile, 10 (oleanderic acid) and 11 ($3{\beta}$-acetoxy-urs-12-en-28-oic acid) exhibited moderate inhibitory effects on Hela with $IC_{50}$ value of 55.0 and $68.8{\mu}M$, respectively. Moreover, 10 showed cytotoxic effect on HL-60 cell line with $IC_{50}$ value of $63.9{\mu}M$. To our knowledge, this is the first report that oleanderic acid was isolated from L. japonicum and investigated in cytotoxic effects on Hela and HL-60 cells.

• Preventive Nutrition and Food Science
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• 제21권4호
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• pp.384-388
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• 2016

Reactive oxygen species are tumorigenic by their ability to increase cell proliferation, survival, and cellular migration. The purpose of the present study was to compare the antioxidant activity and cytotoxic effects of 3 berry extracts (strawberry, Korean raspberry, and mulberry) in A2780 human ovarian carcinoma cells. Except for raspberry, the ethyl acetate or methylene chloride fractions of berries containing phenolic compounds exerted dose dependent free radical scavenging activities. In the raspberry fractions, the hexane fraction also exhibited potent antioxidant activity. The cytotoxic effects of berries extracts in A2780 human ovarian carcinoma cells were measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Surprisingly, co-treatment with n-butanol (BuOH) fractions of berries showed stronger cytotoxic effects compared to the other fractions. These findings suggest that potent anticancer molecules are found in the BuOH fractions of berries that have stronger cytotoxic activity than antioxidants.

• Journal of Acupuncture Research
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• 제19권5호
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• pp.57-72
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• 2002

Objectives : This study was undertaken to determine the cytotoxic effects of crude bee venom which is widely used for aqua-acupuncture in oriental medical clinic. Methods : We compared the effects of crude bee venom, apamin, melittin and MCD peptide on cellviability by MTT asssay. Results : The obtained results are summarized as follows: 1. Bee venom, apamin, melittin and MCD peptide showed concentration--dependent cytotoxic effect in some human cell lines(human glioma cell line과 neuroblastorna, human mast cell line) for 24 and 48 Hour treatment. 2. Bee venom, apamin, melittin and MCD peptide showed dose-dependent cytotoxic effect in some human cell lines for 24 and 48 Hour treatment. 3. Bee venom treatment for 24 and 48 hour showed higher cytotoxic effects than apamin, melittin and MCD peptide. Conclusions : These results suggest that bee venom, apamin, melittin and MCD peptide have concentration- and dose- dependent cytotoxic effect in some human cell lines. But further study is needed for optimal concentration and dose.

• Biomolecules & Therapeutics
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• 제12권3호
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• pp.189-193
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• 2004

Over the past several years, research efforts have been directed both at economically producing valuable substances from the wood biomass and at producing lignolytic enzymes at a lower cost. In the present study, we found that Phellinus igniarius, the basidiomycetes, secreted lignin peroxidase as a main lignolytic enzyme, which was detected maximum activity at 16th day of culture and showed 37 kDa of molecular mass in identification by activity assay and purification by anion-exchange chromatography. The Phellinus igniarius-derived lignin peroxidase hydrolyzed steam-exploded wood (Quercus mongolica) powder into small molecules showing cytotoxicity against cancer cel1s (HepG2 hepatoma, SK-N-SH neuroblastoma, B16 melanoma, MBT-2 bladder cancer). In addition, the enzyme hydrlysates of lignins (ELg) that were extracted from the steam-exploded oak showed more potent cytotoxic effects on the cancer cells than the enzyme hydrolysates of wood biomass (EWp), indicating that the cytotoxic effect of EWp may be due to the enzyme-degraded products of lignin among the lignocellulosics. Furthermore, the cytotoxic effect of ELg on Chang, normal liver cells, was much less potent than that of ELg on HepG2 and B16 cancer cells, indicating that the cytotoxic effect of ELg may be specific for cancer cells. The present results suggest that Phellinus igniarius may be a useful resource for the large-scale production of lignin peroxidase and that the lignin peroxidase may be applied for the generation of valuable biodegradation products from wood lignocellulosics for medical use.

• 한국식품과학회지
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• 제36권5호
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• pp.812-817
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• 2004

한국 전통약주와 기존에 암세포주에 대한 세포독성이 보고되어 있는 알코올 음료에 대한 항종양 세포독성을 비교하기 위하여 무증자 발효 방법으로 발효시키면서 한약재를 첨가한 전통약주I과 뽕잎, 메밀 등을 첨가한 전통약주II, 비교 시료로 적포도주, 백포도주, 맥주, 일본 청주 등에 대하여 연구하였다. 각 시료에 대하여 10-80배까지 단계적으로 희석하여 DLD-1, HepG2, K562, EMT6, LLC1에 처리하였을 때, 인체유래 대장암 세포주인 DLD-1의 경우 적포도주에서만 강한 세포독성이 확인되었는데, 전통약주I의 경우 그 농축액에서 DLD-1에 대하여 적포도주와 유사한 세포독성을 확인할 수 있었다. 나머지 4종의 암세포주에서는 10-20배 희석배수에서 적포도주, 전통약주I, 전통약주II가 세포독성을 보였으나, 각 암세포주의 종류에 따라서 세포독성은 약간씩 차이를 보였다. HepG2, K562, EMT6의 경우 10배 희석배수에서 모두 비슷한 세포독성을 보인 반면에 마우스 유래 폐암세포주인 LLC1의 경우에는 전통약주I과 전통약주II의 세포독성이 적포도주보다 우수한 것을 확인하였다. 본 연구의 결과에 의하면 이러한 항암효과는 전통약주에 존재하는 미지의 약리성분이 작용하는 것으로 판단되었다.

• Biomolecules & Therapeutics
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• 제14권3호
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• pp.148-151
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• 2006

We have previously reported that 2.4 kb of L-plastin promoter (LP) could regulate the expression of adenoviral vector (AV) exogenous genes in a tumor cell specific manner. In the present study, we tested if the replication competent AdLPE1A vector results in a direct cytotoxic effect in hepatocelluar carcinoma (HCC) cells. In vitro cytotoxicity tests were carried out with replication-competent (AdLPE1A) and -incompetent (AdLPCD) LP-driven vectors. AdLPE1A is an AV in which LP was inserted 5' to the E1A and E1B genes. The AdLPCD vector contains LP and the E. coli cytosine deaminase (CD) gene in transcription unit. Exposure of cells to AdLPE1A generated a significant cytotoxic effect as compared to the control. Almost 90% of the cell had manifested the characteristic cytopatic effect on day 9 after infection of cells with 10 MOI of AdLPE1A. On the other hand, almost 35% of the cells were left when the cells had been treated with 100 MOI of AdLPCD together with 5-FC on day 9 when compared with the cells which had never been exposed neither 5-FC nor AdLPCD. These results showed that the replication competent AdLPE1A vector could kill the HepG2 cells directly by the oncolytic effect of the virus. The replication competent AV vector carrying viral E1A generated greater cytotoxic effect than the replication incompetent AV, which contains the CD prodrug activation transcription unit without E1A, in HepG2 cells.

• 대한의생명과학회지
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• 제25권1호
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• pp.66-74
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• 2019

Hyperlipidemia is defined as conditions of the accumulation of lipids such as free fatty acids (FFA), triglyceride (TG), cholesterol and/or phospholipid in the bloodstream. Hyperlipidemia can cause lipid accumulation in non-adipose tissue, which is lipid-cytotoxic effects in many tissues and mediates cell dysfunction, inflammation or programmed cell death (PCD). TG is considered to be a major cause of atherosclerosis through inflammatory necrosis of vascular endothelial cells. Recently, TG have also been shown to exhibit lipid-cytotoxicity and induce PCD. Therefore, we investigated the effect of TG on the cytotoxic effect of various cell types. When exposed to TG, the cell viability of U937 monocytes and Jurkat T lymphocytes, as well as the cell viability of MCF-7, a non-immune cell, decreased in time- and dose-dependent manner. In U937 cells and Jurkat cells, caspase-9, an intrinsic apoptotic caspase, and caspase-8, an extrinsic apoptotic caspase, were increased by exposure to TG. However, in TG-treated MCF-7 cells, caspase-8 activity increased only without caspase-9 activity. In addition, the reduction of cell viability by TG was recovered when all three cell lines were treated with pan-caspase inhibitor. These results suggest that activation of apoptotic caspases by TG causes lipotoxic effect and decreases cell viability.

• 대한수의학회지
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• 제63권1호
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• pp.2.1-2.7
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• 2023

Fenbendazole (FBZ) is a benzimidazole anthelmintic widely used to treat parasitic infections. The anticancer effect of FBZ has been recently highlighted leading to its consideration as a potential anticancer agent. Although previous studies have demonstrated the effect of FBZ on cancer cells, there is a paucity of studies on the effect of FBZ on lymphoma cells and normal immune cells. Herein, we investigated the effects of FBZ on a mouse lymphoma cell line, EL-4 cells, and spleen cells, using vincristine as a positive control. The cellular metabolic activity of EL-4 cells was decreased by FBZ, but that of the spleen cells was not decreased. Moreover, FBZ reduced the mitochondrial membrane potential and induced reactive oxygen species production in EL-4 cells, but not in spleen cells. FBZ induced G2/M phase arrest and increased the sub G0/G1 phase ratio, indicating apoptosis. Furthermore, compared to the control cells, the reactivity of spleen cells pretreated with FBZ to lipopolysaccharide was maintained. In summary, FBZ is cytotoxic to EL-4 cells, but not to spleen cells. This study provides experimental evidence that FBZ exerts an anticancer effect, and less cytotoxic effects and functional damage to normal spleen cells.