• Archives of Pharmacal Research
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• 제19권1호
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• pp.6-11
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• 1996

The trichothecenes are sesquiterpenoid mycotoxins characterized by the 12,13-epoxytrichothec-9-ene ring system. We have tested cytotoxicity of several naturally-occurring or synthesized trichothecenes against human solid tumor cell lines. Among them, trichothecin(I) and $4-\beta$-Acetoxy-12,13-epoxytrichothec-9-ene (trichodermin, II) exhibited highly cytotoxic activities. 4-.betha.-Hydroxy-12,13-epoxytrichothec-9-ene (trichodermol, III) and $4-\beta$-Methoxy-12,13-epoxytrichothec-9-ene (IV) had mild cytotoxicities. But 12,13-Epoxytrichothec-9-ene-4-one (V) and $4-\beta$-Hydroxy-12,13-epoxytrichothec-9-ene(VI) had no cytotoxicities up to 10 $\mug/ml$. And in the tested cell lines, HCT15 colon cancer cell line was the most sensitive to all tested trichothecenes.

• 약학회지
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• 제43권5호
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• pp.598-605
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• 1999

The hot water and mathanol extracts of Artemisia argyi showed considerable cytotoxicities against H9(ATCC HTB 176) cancer cell with IC50 values of $48.6{\;}\mu\textrm{g}/ml$ and $51.9{\;}\mu\textrm{g}/ml$, respectively. These cytotoxicities were found to be dependent on the extract concentrations and culture days. CuZnSOD and MnSOD activities were significantly increased in the cytoplasm and mitochondria fractions of cancer cell, and media in the presence of Artemisia argyi. Such enhanced SOD activities were generally in the range of two to threefolds. In contrast to SOD, catalase and glutathione peroxidase activities were not detected at all. These results suggest that Artemisia argyi have generated $O_2^-$ in the mitochondria and cytoplasm of H9 cancer cell with concurrent induction of CuZnSOD and MnSOD in situ, which dismutate $O_2^-{\}to{\;}H_2O_2$. Without coordinated actions of catalase and/or glutathione peroxidase $H_2O_2$ is easily converted to very toxic OH and these reactive oxygen species together might have induced necrosis and/or apoptosis of H9 cell.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2002년도 Current Trends in Toxicological Sciences
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• pp.83-83
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• 2002

To assess the role of 8-oxoguanine glycosylase (OGG1) in the cell defense against radiation injury, the radiation-induced cytotoxicities were compared between the mutant type KG-1 featuring a loss of OGG1 activity due to a homozygous mutation of Arg 229 G1n, and the wild type U937.(omitted)

• Bulletin of the Korean Chemical Society
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• 제22권4호
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• pp.372-374
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• 2001

Three simple carboxamides incorporating the phenethylamine moiety have been isolated from strain XR-NC of a symbiotic bacterium Xenorhabdus nematophilus. Their structures were identified by spectroscopic data and synthesis. The compounds exhibited significant cytotoxicities against human cancer-cell line, viz. the gastric adenocarcinoma, colon adenocarcinoma and lung adenocarcinoma.

• 약학회지
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• 제44권2호
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• pp.175-181
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• 2000

Pedunculagin is an ellagitannin purified from Alnus hirsuta var. microphylla, Betulaceae. The effects of pedunculagin on the immune system have been characterized to induce enhancement of NK (natural killer) cell cytotoxicities against tumor cells. The present study investigated whether pedunculagin can enhance macrophage cytotoxicity against P8l5 tumor cells. Macrophage cultured with pedunculagin enhanced cytotoxicity in a dose dependent manner In addition, the same treatments increased NO production, which plays important roles in the immune system. liken together these results demonstrate that pedunculagin significantly enhances cytolytic activities of macrophage.

• Bulletin of the Korean Chemical Society
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• 제35권9호
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• pp.2809-2812
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• 2014

The 43-residue defensin-like peptide coprisin, which is isolated from dung bettle, Copris tripartitus, is a potent antimicrobial peptide. In our previous work, we determined the tertiary structure of coprisin and found that alpha helical region of coprisin from residue 19 to residue 30 is important for its antimicrobial activities. Here, we designed cop12mer and cop9mer analogs of coprisin based on the tertiary structure of coprisin. To investigate the relationship between hydrophobicity and antimicrobial activities and develop the potent peptide antibiotics, we designed cop9mer-1 with substitution of $His^2$ with Trp in cop9mer. The results showed that cop9mer-1 has higher toxicities as well as improved antimicrobial activities compared to cop9mer. In order to reduce the toxicity of cop9mer-1, we designed cop9mer-2 and cop9mer-3 with substitution of $Cys^3$ with Lys or Ser. Substitution of $Cys^3$ with these hydrophilic amino acids results in lower cytotoxicities compared to cop9mer-1. Cop9mer-2 with substitution of $Cys^3$ with Lys in Cop9mer-1 showed high antibacterial activities against drug resistant bacteria without cytotoxicity. Antibiotic action of cop9mer-1 analog appears to involve permeabilization of the bacterial cell membrane while cop9mer-2 and cop9mer-3 may have different mechanism of action. These results imply that that optimum balance in hydrophobicity and hydrophilicity in these 9-meric peptides plays key roles in their antimicrobial activities as well as cytotoxicities.

• BMB Reports
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• 제32권6호
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• pp.585-593
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• 1999

The water and methanol extracts of Artemisia argyi showed significant cytotoxicities against J774A.1 cells but not so much against normal leukocytes. The cytotoxicities were found to be dependent on the extract concentration and the incubation time. The concentration of water and methanol extracts inhibiting 50% of cell proliferation ($IC_{50}$) were estimated to be 44.2 mg/ml and 71.6 mg/ml, respectively. In the presence of Artemisia argyi water extract, total superoxide dismutase (CuZnSOD and MnSOD) activities of media, cytoplasmic and mitochondrial fractions of J774A.1 cells increased in accordance with cytotoxicity. MnSOD was found to be the main component of enhanced total SOD activities, particulary in the mitochondrial fraction. In contrast to SOD, catalase and glutathione peroxidase (GPx) were not found in any instance of the current investigation. In addition, substantial amount of $O_2^-$ appeared to be generated in the mitochondrial fraction under the influence of Artemisia argyi. All data put together, it is postulated that Artemisia argyi extracts seem to stimulate $O_2^-$ generation in mitochondria of J774A.1 cells with concomitant increases of SODs. Since $H_2O_2$, the reaction product of SOD on $O_2^-$, is known to be readily converted to very toxic $OH{\cdot}$ in the absence of catalase and/or GPx cooperation, toxicity derived from ROS such as $O_2^-$, $H_2O_2$, and $OH{\cdot}$ may be the main cause of necrosis and/or apoptosis of J774A.1 cells.

• 동아시아식생활학회지
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• 제19권2호
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• pp.202-209
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• 2009

This study was conducted to gather the basic data on the spread of the domestic kiwifruits, and the development of the manufactured goods and the health functional foods produced using kiwifruits. We determined the chemical compositions of four types of kiwifruits cultivated in Korea, Daeheung, Bidan, Haegeum and Hayward. In addition, we measured the anti-microbial activities and cytotoxicities of these types of kiwifruits. The vitamin C contents of the kiwifruits increased in the order of Bidan (93.82 mg/100 g), Daeheung (85.89 mg/100 g), Haegeum (83.73 mg/100 g) and Hayward (75.28 mg/100 g). The total amino acids contents per 100 g of kiwifruit (dry weight basis) were 483.97 mg (Haegeum), 453.08 mg (Hayward), 437.27 mg (Bidan) and 369.35 mg (Daeheung). The K and Ca contents of the kiwifruits ranged from 14.56~37.12 mg/L and 1.94~8.24 mg/L, respectively; however, the Fe, Mg, Zn and Cr contents all less than 1.83 mg/L. The antimicrobial activities of methanol extracts of kiwifruits against five gram positive bacteria at concentration of 2,000 mg/L in terms of inhibition diameter ranged from 8.8~12.8mm, while raged from 9.2~13.1mm against three gram negative strains of bacteria. The hyperplasia inhibition of lung cancer cells (Calus-6) by 800 mg/L kiwifruits extracts of Bidan, Haegeum, Daeheung and Hayward kiwifruits were 21.2%, 9.5%, 6.7% and 5.0%, respectively. Consequently, it was assumed that kiwifruits was rich in vitamin C, amino acids and K, and that they would therefore be useful in processed goods.

• 임산에너지
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• 제20권2호
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• pp.1-8
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• 2001

8가지 목련과 수목의 수피 및 잔가지를 채집하고 건조하여 MeOH로 열추출하고, 사람의 암세포에 대한 독성을 측정하였다. 이중 일본 목련이 강한 세포독성이 관찰되어 세포독성을 갖는 순수한 물질 즉, magnonol, honokiol, dihydroxybiphenyl ether, linodenine, anonaine, asimilobine에 대한 세포독성을 측정하였다. 그리고 암세포 살해능 및 apoptosis 유도능을 측정한 결과 magnonol, honokiol, dihydroxybiphenyl ether가 초기단계의 apoptosis 유도에 기인함을 밝혔다. 따라서 세포독성이 강한 물질로 판명된 magnolol, honokiol, dihydroxybiphenyl ether에 대한 정량분석을 위해서 MeOH 추출물을 클로로포름, 에틸아세테이트, 수용성 분획으로 나누고, 에틸 아세테이트 분획을 n-Hexane : Acetone(4:1, v/v)용매로 silica gel chromatography를 한 후, 이 들 화합물이 함유된 분획을 만들었다. 이 분획을 HPLC system으로 이들의 함량을 측정한 결과 MeOH 추출물에 대하여 각각 0.9%, 0.3%, 0.24%가 있음을 밝혔다

• 한국식품영양학회지
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• 제30권3호
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• pp.454-463
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• 2017

Ganoderma lucidum has been traditionally used as a medicine for treatment of bronchitis, arthritis, and high blood pressure, and it has been reported to display many biological activities including anticancer and immune activities. Since mushroom mycelium is known to have excellent biological activities together with mushroom fruiting body, studies on biological activities of mushroom mycelium have been actively conducted. Thus, the present study compared the biological activities before and after the cultivation of Ganoderma lucidum mycelium on Atractylodes rhizoma. When the radical scavenging activity was assessed by the DPPH assay, ARGL (ethanol extract of Atractylodes rhizoma mycelium fermented with Ganoderma lucidum) showed radical scavenging activity of 5.58~82.56% at concentrations of $10{\sim}500{\mu}g/assay$, while AR (ethanol extract of Atractylodes rhizoma) showed radical scavenging activity of 5.27~72.08% at the same concentrations. When measured by using the ABTS assay, ARGL showed higher radical scavenging activity than AR, which was consistent with the result obtained by the DPPH assay. In the MTT assay, the cytotoxicity of ARGL against all cell lines was higher than that of AR. In particular, the cytotoxicities of AR and ARGL against Hep3B at a concentration of $400{\mu}g/assay$ were 71.81% and 86.40%, respectively. In addition, the result obtained by the SRB assay was consistent with the result obtained by the MTT assay. According to the results mentioned above, there is a high probability that medicinal herb cultures using mycelium can be used as sources of functional foods since the cytotoxicities against cancer cells and antioxidant activities increased when the mycelium was fermented with Atractylodes rhizoma.