• Title/Summary/Keyword: Antitumor activities

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Augmentation of Macrophage Cytotoxicity and NO Production by Pedunculagin (Pedunculagin의 Macrophage에 대한 항암활성 및 Nitric Oxide 생성)

  • 이도익;김형근;이민원;최영욱;김하형;김은주
    • YAKHAK HOEJI
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    • v.44 no.2
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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.

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A versatile biomimetic total synthesis of benzo[c]phenanthridine and protobeberine alkaloids using lithiated toluamide-benzonitrile cycloaddition

  • Le, Thanh-Nguyen;Kang, Sung-Kyung;Cho, Won-Jea
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.65.1-65.1
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    • 2003
  • Natural benzo[c]phenanthridine and protoberberine alkaloids which have been attractive to synthetic organic chemists and biochemists over the last 2 decades since such compounds have shown interesting biological properties such as antitumor, antiviral and antimicrobacterial activities. For the systematic research on these alkaloids, several total syntheses of these alkaloids have been reported. However, the bulk of reported benzo[c]phenanthridine synthetic studies to date have involved multistep sequences for assembly of the target molecules as well as lack of generality for synthesizing substituted molecules. (omitted)

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Characterization of Acharan Sulfate Binding Proteins in Murine Lewis Lung Carcinoma Cell

  • Joo, Eun-Ji;Hahn, Bum-Soo;Kim, Yeong-Shik
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.150.2-151
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    • 2003
  • We have focused on various biological activities of acharan sulfate (AS) isolated from the giant African snail Achatina fulica. In a previous study, AS showed antiangiogenic and immunomodulating activity. We also investigated antitumor activity of AS. In vitro AS had no cytotoxicity within 0 to 200 ug/ml in tumor cells such as Lewis lung carcinoma(LLC) , KM1214 (human colon cancer cell) and Caki-1 (human kidney cancer cell) by both MTT and SRB assay. In vivo AS was used to treat C57BL/6 mice bearing LLC by subscutaneous injection. (omitted)

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Stereoselective synthesis of novel 4′$\alpha$-C-methyl branched novel carbocyclic nucleosides

  • Kim, Ji-Hee;Ko, Ok-Hyun;Hong, Joon-Hee
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.345.2-345.2
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    • 2002
  • Recently. 4'${\alpha}$-C homologated furanose nucleosides. especially alkyl branches. are molecules of considerable current interest. One of reasons for this prominence arises from the notable biological activities as antiviral and antitumor agents. as shown in 4'${\alpha}$-C-methyl-2-deoxythymidine (EC$_{50}$ = 7.2$\mu$M against HIV in MT-4 cell), 4'${\alpha}$-C-fluoromethyl-2-deoxycytidine. 4'${\alpha}$-C-hydroxymethylthymidine and 4'${\alpha}$- -C-azidomethyl-thymidine. (omitted)omitted)

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The effects of carbon sources on antitumor and anticomplementary activities of Ganoderan extracted from the mycelium of Ganoderma lucidum IY009 (Ganoderma lucidum IY009 균사체로부터 추출된 ganoderan의 항암 및 항보체 활성에 미치는 탄소원의 영향)

  • Han, Man-Deuk;Lee, June-Woo;Jeong, Hoon;Chung, Sung-Kyun;Lee, Seung-Yong;Yoon, Kyung-Ha
    • The Korean Journal of Mycology
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    • v.23 no.3 s.74
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    • pp.209-225
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    • 1995
  • Ganoderan, antitumor ${\beta}-glucan$ from Ganoderma lucidum was extracted from the mycelium of G.lucidum IY009 which was cultured in various carbon sources. The mycelium was shown to be capable of utilizing various carbon sources, e.g., soluble starch, fructose and glucose, and differs in morphology on carbon sources. In radioisotope assay, about $5.2{\sim}16%$ of glucose was to be incorporated in ganoderan of the mycelium. The monosugars of these ganoderan were mainly consisted of glucose, mannose, galactose. The galactose was not good carbon source for growing the mycelium but the best carbon source for producing the potentialized-ganoderan on the antitumor and anticomplementary activity. The tumor inhibition ratio of ganoderan-GAL, obtained from galactose medium, was 83.6% at the dose of 20 mg/kg/day. This crude polysaccaride was composed of five monosaccharide and the protein contained 16 amino acids. Also, ganoderan-GAL increased the anticomplementary activity than that obtained from any other media. This fact suggests that the structural differences of ganoderan influence the antitumor and anticomplementary activity.

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Purification and Structural Analysis of Antitumor Polysaccharides Obtained from Ganoderma lucidum IY 009 (Ganoderma lucidum IY 009로 부터 분리된 항암성 다당류의 정제 및 구조분석)

  • Lee, Kweon-Haeng;Jeong, Hoon;Lee, June-Woo;Han, Man-Deuk;Choi, Kyoung-Sook;Oh, Doo-Hwan
    • Microbiology and Biotechnology Letters
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    • v.22 no.2
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    • pp.190-196
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    • 1994
  • Alkali soluble(AS) fraction, revealed the highest antitumor activity of the alkali extracted fractions of G. lucidum IY 009, was loaded on DEAE cellulose(OH$^{-}$ form) column. AS-1, AS-2, AS-3, AS-4 and AS-5 were obtained by stepwise elution with H$_{2}$O, 0.1 M NaHCO$_{3}$, 0.3 M NaHCO$_{3}$, 0.5 M NaHCO$_{3}$ and 0.5 N NaOH respectively, and their antitumor activities(I.R. %) against the sarcoma 180 were 97.5%, 68.0%, 73.0%, 81.0% and 66.0% respectively. AS-1 observed highest antitumor activity was appeared as single peak on the Sepharose CL-4B column chromatography, and their molecular weight was about 580,000 dalton. The carbohydrate content of AS-1 was 98.9%, their monosaccharide consisted of 67.5% of mannose, 22.5% of xylose, 5.8% of glucose, 1.8% of galactose and 2.0% of ribose. AS-1 was assumed $\alpha $linkaged xylomannan having infrared absorption at 864.3 cm$^{-1}$. The main alditol acetates of AS-1 were identified as 1,5-Di-O-acetyl1-2,3,4-Tri-O-methylxylitol, 1,4,5-Tro-O-acety1-2,3,6-Tri-O-methylmannitol and 1,3,4,5-Tetra-O-acety1-2,6-Di-O-methylmannitol by methylation analysis, and their molar ratio was 1 : 2 : 1. The core portion of AS-1 might be $\alpha $-(1$\longrightarrow $ 4)mannopyranosyl unit branched with side chain, C1 of xylopyranosyl residue linked to C3 of every 3 mannopyranosyl units, and the degree of polymerization of structural unit in AS-1 was about 835.

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Antitumor Effect of Young Radish Kimchi Prepared with Young Radish Cultivated in the Soil Containing Sulfur on Sarcoma-180 Tumor Cells Transplanted Mice (유황처리 열무로 제조한 열무김치의 Sarcoma-180 암세포에 대한 고형암 성장 억제효과)

  • Kong, Chang-Suk;Bak, Soon-Sun;Rhee, Sook-Hee;Kil, Jeung-Ha;Rho, Chi-Woong;Hwang, Hae-Jun;Kim, Nak-Ku;Park, Kun-Young
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.34 no.10
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    • pp.1520-1524
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    • 2005
  • Young radishes (YR, yeolmu in Korean) were cultivated in the soil with and without sulfur. Young radish kimchi-general (YR kimchi-G) was prepared with YR commonly cultivated in the soil without sulfur. Young radish kimchl-sulfur (YR kimchi-S) and young radish kimchi-sulfur with lime mortar (YR kimchi-SL) were prepared with the YR cultivated in the soil with sulfur an4 sulfur added lime mortar on it respectively. Antitumor effects of methanol extracts from the YR kimchis were investigated in sarcoma-180 tumor cell transplanted mice. The solid tumor growth was significantly inhibited by the YR kimchi-SL prepared with YR grown in the soil with sulfur (p < 0.05). The treatment of the methanol extracts from YR kimchi-S and -SL increased the glutathione S-transferase activities and glutathione contents in the livers, compared to thlose of YR kimchi-G and the control. One of the antitumor effects by the YR kimchis was due to the increased the glutathione levels and the glutathione S-transferase activity which is phase 2 enzyme. These results also suggested that the antitumor effects of YR kimchi can be enhanced by using YR cultivated differently in the presence of sulfur that can help to produce sulfur-containing compounds in YR.

Antitumor Activity of 7-[2-(N-Isopropylamino)ethyl]-(20s)-camptothecin, CKD602, as a Potent DNA Topoisomerase I Inhibitor

  • Lee, Jun-Hee;Lee, Ju-Mong;Kim, Joon-Kyum;Ahn, Soon-Kil;Lee, Sang-Joon;Kim, Mie-Young;Jew, Sang-Sup;Park, Jae-Gab;Hong, Chung-Il
    • Archives of Pharmacal Research
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    • v.21 no.5
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    • pp.581-590
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    • 1998
  • We developed a novel water-soluble camptothecin analobue, CKD602, and evaluated the inhibition of topoisomerase I and the antitumor activities against mammalian tumor cells and human tumor xenografts. CKD602 was a nanomolar inhibitor of the topoisomerase I enzyme in the cleavable complex assay. CKD602 was found to be 3 times and slightly more potent than topotecan and camptothecin as inhibitors of topoisomerase, respecitively. In tumor cell cytotoxicity, CKD602 was more potent than topotecan in 14 out of 26 human cancer cell lines tested, while it was comparable to camptothecin. CKD602 was tested for the in vivo antitumor activity against the human tumor xenograft models. CKD602 was able to imduce regression of established HT-29, WIDR and CX-1 colon tumors, LX-1 lung tumor, MX-1 breast tumor and SKOV-3 ovarian tumor as much as 80, 94, 76, 67, 87% and 88%, respectively, with comparable body weight changes to those of topotecan. Also the therapeutic margin (R/Emax: maximum tolerance dose/$ED-{58}$) of CKD602 was significantly higher than that of topotecan by 4 times. Efficacy was determined at the maximal tolerated dose levels using schedule dependent i.p. administration in mice bearing L1210 leukemia. On a Q4dx4 (every 4 day for 4 doses) schedule, the maximum tolerated dose (MTD) was 25 mg/kg per administration, which caused great weight loss and lethality in <5% tumor bearing mouse. this schedule brought significant increase in life span (ILS), 212%, with 33% of long-term survivals. The ex vivo antitumor activity of CKD602 was compared with that of topotecan and the mean antitumor index (ATI) values recorded for CKD602 were significantly higher than that noted for topotecan. From these results, CKD602 warrants further clinical investigations as a potent inhibitor of topoisomerase I.

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Antimicrobial activities against oral bacteria and growth inhibition against Actinomyces viscosus using Lentinus edodes various extracts (표고버섯 용매별 추출물의 구강세균에 대한 항균효과 및 Actinomyces viscosus에 대한 생육저해 효과)

  • Han, So-Ra;Lim, Kun-Ok;Oh, Tae-Jin
    • Journal of Korean society of Dental Hygiene
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    • v.15 no.4
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    • pp.735-741
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    • 2015
  • Objectives: Lentinus edodes is an edible mushroom with a variety of beneficial effects such as antitumor, anti-inflammatory, antioxidant, and immune-modulatory activity. This study was carried out to evaluate the antimicrobial activities of Lentinus edodes extracts against oral-related bacteria. Methods: The antimicrobial activities of this extracts were investigated against S. anginosus, S. sobrinus, S. aureus, S. mutans, S. ratti, S. sanguinis, A. viscosus, A. naeslundii, and A. actinomycetemcomitans by the disc diffusion method, minimum inhibitory concentration (MIC), and growth inhibition. Results: Ethanol extracts had no antimicrobial activities, but acetone extracts showed antimicrobial activities against A. viscosus and A. actinomycetemcomitans and ethyl acetate extracts had effects against S. aureus, S. sanguinis, A. viscosus, and A. actinomycetemcomitans. Conclusions: The inhibitory effect of Lentinus edodes extracts was investigated on the growth of A. viscosus. Ethyl acetate and acetone extracts showed 90% and 77% inhibitory effect, respectively, against A. viscosus for 24 hrs. Ethyl acetate extracts had MIC of 25.0 mg/ml and acetone extracts showed MIC of >25.0 mg/ml.

Antitumor and antioxidant activities of Bryonia laciniosa against Ehrlich's Ascites Carcinoma bearing Swiss albino mice

  • Sivakumar, T;Kumar, R Sambath;Perumal, P;Vamsi, MLM;Sivakumar, P;Kanagasabai, R;Baskaran, MV;Karki, Subhas S;Mazumder, UK;Gupta, M
    • Advances in Traditional Medicine
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    • v.5 no.4
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    • pp.322-330
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    • 2005
  • The plant Bryonia laciniosa (Family: Cucurbitaceae) has been indicated for the treatment of various diseases one among which is cancer. The purpose of this study was investigating experimentally the possible anti-tumor effect and antioxidant role of Bryonia laciniosa leaves in animal model. The methanol extract of Bryonia laciniosa (MEBL) administered at the doses of 62.5, 125 and 250 mg/kg in mice for 14 days after 24 h of tumor inoculation. The effect of MEBL on the growth of transplantable murine tumor, life span of EAC bearing mice, hematological profile and liver biochemical parameters (lipid peroxidation, antioxidant enzymes) were estimated. Treatment with MEBL decreased the tumor volume and viable cell count thereby increasing the life span of EAC bearing mice and brought back the hematological parameter more or less normal level. The effect of MEBL also decreases the levels of lipid peroxidation and increased the levels of glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT). The present work indicates that the methanol extract of Bryonia laciniosa exhibited significant antitumor and antioxidant activity in vivo.