• Title/Summary/Keyword: cytotoxic activities

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Cytotoxic Activities of some Geranylated Flavones against L1210 Cell (L1210세포에 대한 제라닐화 후라본의 세포독성)

  • Baik, Kyeong-Up;Ahn, Byung-Zun
    • YAKHAK HOEJI
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    • v.32 no.2
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    • pp.125-128
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    • 1988
  • Geranylation of some synthetic and natural flavones have yielded cytotoxic products against L1210 coll; 5,2´-dihydroxy-6,7,8-trimethoxy-6´-geranyloxyflavone 4$(8.5{\mu}g/ml)$, 5,6-dihydroxy-7-gerenyloxyflavone 9$(2.3{\mu}g/ml)$. 2 has showed the same range of cytotoxicity as the starting material, 5,2´-dihydroxy-6,7,8-trimethoxy-6´-benzyloxyflavone$(17.0{\mu}g/ml)$. The cytotoxicity of 4 was lower than its starting substance, 5,2´,6´-trihydroxy-6,7,8-trimethoxyflavone $(4.5{\mu}g/ml)$. On geranylating 5,6,7-trihydroxyflavone(baicalein, $15.0{\mu}g/ml$) the cytotoxic activity has been strongly potentiated($2.3{\mu}g/ml$ of 9). The presence of at least a free hydroxy group in B-ring of Skullkapflavone II-type flavones. was essential for a high activity. A larger RD-group than methoxy in the B-ring has weakened the activity. The cytotoxicities of baicalein series could not be correlated to their structures.

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Bioactive Constituents of Marine Sponges of the Genus Spongosorites

  • Bao, Baoquan;Hong, Jongki;Lee, Chong-O.;Cho, Hee Young;Jung, Jee H.
    • Journal of Marine Bioscience and Biotechnology
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    • v.1 no.3
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    • pp.144-155
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    • 2006
  • This report reviews the literatures on chemical constituents of marine sponges of the genus Spongosorites and also highlights our own research. Specific biological activities of the metabolites from these sponges include: cytotoxic, antitumor, antibacterial, antifungal, antiviral, anti-inflammatory, and other pharmacological activities.

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Cytotoxic Activities of Amentoflavone against Human Breast and Cervical Cancers are Mediated by Increasing of PTEN Expression Levels due to Peroxisome Proliferator-Activated Receptor γ Activation

  • Lee, Eun-Jung;Shin, So-Young;Lee, Jee-Young;Lee, So-Jung;Kim, Jin-Kyoung;Yoon, Do-Young;Woo, Eun-Rhan;Kim, Yang-Mee
    • Bulletin of the Korean Chemical Society
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    • v.33 no.7
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    • pp.2219-2223
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    • 2012
  • Human peroxisome proliferator-activated receptor gamma ($hPPAR{\gamma}$) has been implicated in numerous pathologies, including obesity, diabetes, and cancer. Previously, we verified that amentoflavone is an activator of $hPPAR{\gamma}$ and probed the molecular basis of its action. In this study, we investigated the mechanism of action of amentoflavone in cancer cells and demonstrated that amentoflavone showed strong cytotoxicity against MCF-7 and HeLa cancer cell lines. We showed that $hPPAR{\gamma}$ expression in MCF-7 and HeLa cells is specifically stimulated by amentoflavone, and suggested that amentoflavone-induced cytotoxic activities are mediated by activation of $hPPAR{\gamma}$ in these two cancer cell lines. Moreover, amentoflavone increased PTEN levels in these two cancer cell lines, indicating that the cytotoxic activities of amentoflavone are mediated by increasing of PTEN expression levels due to $hPPAR{\gamma}$ activation.

Anti-cancer Effects of Kamiboa-tang and some other Traditional Medical Prescriptions (가미보아탕(加味保我湯) 및 수종(數種) 한방처방의 항암효과에 대한 연구)

  • Sung, Hyun-Jea
    • The Journal of Internal Korean Medicine
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    • v.28 no.2
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    • pp.321-332
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    • 2007
  • Objectives : Anticancer and immune-modulating effects of several Korean medical prescriptions including Yukgunja-tang, Bohwa-tang, Sogam-Won, and Kamiboa-tang were investigated. Methods : In vitro anti-cancer effects were measured by cytotoxicity MTT assay using SNU-1 gastric cancer cell lines, In vivo anti-cancer effects were measured by increased life span of S-180 sarcoma-injected ICR mouse. Immune-modulating effects were analyzed by measuring hemagglutinin titer, appearance of rosette forming cells, lymphocyte proliferation, and phagocytic index in methotrexate-pretreated mice. Results : In vitro assay showed that only Sogam-won showed cytotoxic effect with $IC_{50}$ of 87.9 ${\mu}g/ml$. All other prescriptions showed no cytotoxic effects against SNU-1 gastric cancer cell line. However, in vivo assay showed that Sogam-won showed lowest anti-cancer effects in contrast to its highest cytotoxic effects, Kamiboa-tang, which showed no cytotoxic effect, showed the highest in vivo anticancer effects, with increased life span of 140%. Kamiboa-tang showed significant immune-enhancing activities by significantly increasing rosette forming cells, lymphocyte proliferation, and phagocytic index in methotrexate-pretreated mice (P<0.05). Conclusion : The anticancer effect of Kamiboa-tang is not mediated by direct inhibition of cancer cells but is mediated by improving immune reactions against cancer cells.

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The biological activities of Zelkova leaves and the quality characteristics of Zelkova leaf rice cake according to leaf levels (느티잎의 생리활성 및 느티잎 첨가량에 따른 느티떡의 품질특성)

  • Shon, Jeong-In;Kim, Na-Young;Han, Myung-Joo
    • Korean journal of food and cookery science
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    • v.22 no.4 s.94
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    • pp.468-476
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    • 2006
  • The objectives of this study were to determine the antioxidant and cytotoxic activities of Zelkova leaf extract and the sensory and textural characteristics of Zelkova leaf rice cake. The ethyl acetate layer of Zelkova leaf extract showed the most effective DPPH radical and superoxide anion scavenging activities. The residual layer of Zelkova leaf extract exhibited potent cytotoxicity against the HeLa cell line. In the sensory evaluation, the color and taste of Zelkova leaf rice cakes were not significantly different. Zelkova leaf rice cakes with 20%(5.18), 25%(4.94) and 30%(4.88) added Zelkova leaves showed higher overall acceptability than 0%(4.06) added Zelkova leaves. In the textural analysis, the hardness of the Zelkova leaf rice cake increased slowly with increasing leaf content during 3 day storage. The cohesiveness of 25% and 30% Zelkova leaf rice cakes showed no variation with storage time but that of 0% Zelkova leaf rice cakes decreased with increasing storage period. The 'L' value of Zelkova leaf rice cake decreased with increasing leaf content while the 'a' value of 0% Zelkova leaf rice cake was lower than that of 20%, 25% and 30% Zelkova leaf rice cakes.

Biological Activities and Total Phenolic Content of Ethanol Extracts of White and Flesh-colored Solanum tuberosum L. Potatoes (일반감자와 유색감자 에탄올 추출물의 생리활성 및 폴리페놀 함량)

  • Jang, Hye-Lim;Yoon, Kyung-Young
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.8
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    • pp.1035-1040
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    • 2012
  • This study was aimed to evaluate and compare the biological activities and total phenolic content of ethanol extracts of white (Superior) and colored potatoes (Red, Rose, Haryoung, Blue, Jaseo, and Jasim). Various ethanol extracts (250, 500, 1,000, and $2,000{\mu}g/mL$) were assessed for antioxidant activities of DPPH free radicals and hydroxyl radical scavenging. The cytotoxic activity of the extracts (0, 30, 60, $100{\mu}g/mL$) was also carried out by a human cancer cell lethality bioassay method. Results showed that the DPPH and hydroxyl radical scavenging activities, of all extracts increase in a concentration-dependant manner. All color-fleshed potato extracts, except for Red and Haryoung, showed higher radical scavenging activities than the general white potato extract. Cytotoxicity of the extracts as determined in THP-1 cells showed that Blue and Jasim was highly toxic at most concentrations tested. In addition, the Blue extract had the highest cytotoxic activity on $HepG_2$ cells at the concentration $100{\mu}g/mL$. The contents of total phenolic (TPC) in the extracts significantly varied from 120.0 mg/100 g powder (Superior) to 151.1 mg/100 g powder (Blue), and TPC of all color-fleshed potato extracts was higher than that of white. The greatest positive correlation was found between phenolic contents and hydroxyl radical scavenging activity (r=0.776, p<0.05), and a strong negative correlation was found between hydroxyl radical scavenging activity and cytotoxic activities on $HepG_2$ cells (r=-0.795, p<0.05). The present study demonstrates that color-fleshed potatoes have higher antioxidant and stronger anticancer activities than general potato. These results provide useful and important information for potato breeders and researchers, in order to increase the antioxidant capacity and functional value of colored potatoes for use in the food and pharmaceutical industries.

Methanolic Extract of Plumbago Zeylanica - A Remarkable Antibacterial Agent Against Many Human and Agricultural Pathogens

  • Singh, Mukesh Kumar;Pandey, Ajit;Sawarkar, Hemant;Gupta, Anshita;Gidwani, Bina;Dhongade, Hemant;Tripathi, Dulal Krishna
    • Journal of Pharmacopuncture
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    • v.20 no.1
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    • pp.18-22
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    • 2017
  • Objectives: The current investigation was carried out to determine the cytotoxic and the antimicrobial activities of methanolic extracts of Plumbago zeylanica. Methods: The stems, leaves, and whole plants were air dried and extracted with methanol by using a Soxhlet extractor for 72 hours at $55-60^{\circ}C$. The antimicrobial activities were determined from the zones of inhibition, which were measured by using the agar well diffusion method, and the cytotoxicity assays were performed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method. Results: The methanolic extracts of the stem and the leaves of Plumbago zeylanica were tested against six bacterial species and nine fungal species, and both extracts showed antimicrobial activity in a dose-dependent manner. The leaf extract of Plumbago zeylanica showed maximum antimicrobial activity against both Staphylococcus aureus sub sp aureus and Fusarium oxysporum. The stem extract was found to be more antimicrobial against the Pseudomonas aeruginosa and the Penicillium expansum species. MTT assays were used to test the cytotoxicity of the whole plant extract in the HCT-116 and the K-562 cell lines, and that extract was shown to have weak cytotoxicity in both cell lines. Conclusion: In the present study, the methanolic stem extracts of Plumbago zeylanica were found to possess remarkable antibacterial activities against many human and agricultural pathogens. The extracts were also found to possess significant antifungal activities, but the antifungal activities were less than the antibacterial activities. Finally, the extracts were found to have weak cytotoxicities in the HCT-116 and the K-562 cell lines.

A Study on Biological Activities of Opuntia humifusa Cladode Extracts (손바닥 선인장 (Opuntia humifusa) 줄기 추출물의 생리활성)

  • Yoon, Min-Sun;Yoo, Jae-Soo;Lee, Keun-Kwang;Kim, Myung-Kon
    • Journal of Applied Biological Chemistry
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    • v.55 no.2
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    • pp.117-121
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    • 2012
  • Biological activities of the hot water and ethanol extracts from Opuntia humifusa cladodes were investigated. 1,1-diphenyl-2-picryl hadrazyl (DPPH) electron donating ability of hot water and ethanol extracts was 79.07 and 82.54%, respectively. Hot water extract generally showed better cytotoxic activity than ethanol extract against each cell line. HeLa and AGS cell lines treated with hot water extract had more than 50% cytotoxic activities. Based on the antimicrobial activities against four microbial strains, both extracts inhibited growth of Staphylococcus aureus KCCM 11593, whereas affected cell growth of three other microorganisms, Escherichia coli (KCCM 11234), Pseudomonas aeruginosa (ATCC 27853), and Salmonella typhimurium (ATCC 11862), in proportion to the concentration of extracts. The inflammatory activities against hot water extract (34.31%) showed higher than that of ethanol extract (25.59%). The effect of extracts on 3T3-L1 preadipocytes differentiation showed that differentiation of treated group with 80 and 100 ${\mu}g/mL$ of hot and ethanol extracts were increased more than treated group with isobutyl methyl xanthine (IBMX) + dexamethasone. These results indicate that the O. humifusa cladodes extracts can be used as a functional material due to their effective biological activities.

Immunlogical Studies on Antitumor Component of Lyophyllum decastes(I) (Lyophyllum decastes의 항암성분의 면역학적 연구(I))

  • 이정옥;최응칠;김병각
    • YAKHAK HOEJI
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    • v.31 no.2
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    • pp.70-81
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    • 1987
  • To elucidate action mechanism of lyophyllan A, an antitumor polysaccharide of Lyophyllum decastes, its immunological activities were examined. Lyophyllan A increased significantly the weights of spleen and liver of mice. Lyophyllan A also restored the decreased thymic weight in tumor-bearing mice. It did not show any direct cytotoxicity against tumor cells, but showed immunopotentiating activities by increasing the number of the plaques in hemolytic plaque assays. Lyophyllan A increased the number of peritoneal exudate cells (PEC) and inhibited the growth of sarcoma 180 mixed with PEC. Moreover the macrophages from lyophyllan A-treated mice exhibited a strong cytotoxic activity towards L5178Y target cells.

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Synthesis of 2,6-Diaromatic Substituted Pyridine Derivatives and Their Antitumor Activities

  • Moon, Yoon-Soo;Lim, Hyun-Tae;Zhao, Long-Xuan;Basnet-Arjun;Lee, Eung-Seok
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.345.1-345.1
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    • 2002
  • ${\alpha}$-terthienyl the first isolated from natural products shows potent antitumor activity, which encouraged us to study terpyridine and its biological properties. Terpyridine has also been reported as having carcinogenicity, and it's erivatives showed high cytotoxic activities against several human cancer cell lines and topoisomerase I inhibitory ctivity. Mannich free base from condensation reaction was allowed to react with pyridinum salts to give activity. (omitted)

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