• 제목/요약/키워드: DNA topoisomerase I

검색결과 73건 처리시간 0.053초

활어소종탕이 항종역반응에 미치는 영향 (Study on Antitumor Activity and Immunomodulatory effects of Seoleosojong-tang)

  • 손기정;박양춘
    • 동의생리병리학회지
    • /
    • 제18권1호
    • /
    • pp.137-147
    • /
    • 2004
  • In order to evaluate the antitumor activity and immunomodulatory effects of Seoleosojong-tang(SST), studies were done. We measured the cytotoxic activity for various kinds of cancer cells, inhibitory effect on activity of DNA topoisomerase I, cell adhesion to complex extracellular matrix, survival time in ICR bearing S-180, pulmonary colonization and histological changes of lung in C57BL/6 injected i.v. with B16-F10, CAM assay, expression of CD4/sup +/, CD8/sup +/, B220/sup +/, cytokine gene in spleen cell. The results were obtained as follows: 1. In cytotoxicity against A549, HT1080, 816-F10, NCL-H661 was showed cytotoxicity as compared with control. 2. The inhibitory effect on adhesion of A549, 816-F10 to complex extracellular matrix was over 40% at 100 ㎍/㎖ of SST. 3. In DNA topoisomerase I assay, SST has inhibitory effect. 4. The T/C% was 120.8 in SST treated group in S-180 bearing ICR mice. 5. In pulmonary colonization assay, a number of colonies were decreased significantly and histological changes were showed that infiltration area of cancer cells were inhibited effectively in SST treated group. 6. In CAM Assay, SST has antiangiogenic effect. 7. On the expression of positive cell to CD4/sup +/, CD8/sup +/ and 8220/sup +/ in spleen cells, CD4/sup +/ cells were increased significantly in SST treated group. 8. Effect of SST on IL-1β gene expression in splenic cell was significantly increased as function of whole concentration. 9. The gene expression of IL-4, IL-6, IL-10, IL-12, IFN-γ, TNF-α were increased in SST treated group. From above results SST could be usefully applied for antitumor activity and immunomodulatory effects, but further research of SST should be required.

DNA Topoisomerases I and II Inhibitory Activity and Cytotoxicity of Compounds from the Stems of Parthenocissus tricuspidata

  • Woo, Mi Hee;Zhao, Bing Tian;Tran, Manh Hung;Jeong, Su Yang;Ma, Eun Sook;Min, Byung Sun
    • Bulletin of the Korean Chemical Society
    • /
    • 제34권9호
    • /
    • pp.2675-2679
    • /
    • 2013
  • Activity-directed isolation of the methylene chloride fraction from the stems of Parthenocissus tricuspidata have led to the identification of two new compounds (1-2): 1-(2',3',5'-trihydroxyphenyl)-2-(4"-hydroxyphenyl)-ethane-1,2-(E)-epoxide (1, tricuspidatin A) and erythro-1-(3',5'-dihydroxyphenyl)-2-(4"-hydroxyphenyl)-ethane-1,2-diol (2, tricuspidatin B), together with four known compounds (3-6): ${\beta}$-sitosterol (3), nonacosan-1-ol (4), 3-(4-hydroxy-3-methoxyphenyl)-2-propenoic acid hexacosyl ester (5) and betulinic acid (6). Their chemical structures were elucidated based on spectroscopic (IR, UV, MS, 1D and 2D NMR) and physicochemical analyses. Compounds 1 and 2 showed strong DNA topoisomerase II inhibitory activity at both concentrations of 20 and $100{\mu}M$. In addition, 3 exhibited strong cytotoxic activity against the HT-29 and HepG2 cancer cell lines, and 6 showed strong cytotoxicity against the HT-29 and MCF-7 ones.

Cytotoxicity and DNA Topoisomerase Inhibitory Activity of Constituents Isolated from the Fruits of Evodia officinalis

  • Xu, Ming-Lu;Li, Gao;Moon, Dong-Cheol;Lee, Chong-Soon;Woo, Mi-Hee;Lee, Eung-Seok;Jahng, Yurng-Dong;Chang, Hyeun-Wook;Lee, Seung-Ho;Son, Jong-Keun
    • Archives of Pharmacal Research
    • /
    • 제29권7호
    • /
    • pp.541-547
    • /
    • 2006
  • Four alkaloids (1-4), three quinolone alkaloids (5-7), and three flavanoid glucosides (8-10) were isolated from the fruits of Evodia officinalis Dode, and their structures were determined from chemical and spectral data. Compounds, 3, 8, 9 and 10 were isolated from this plant for the first time. Of these compounds, 1-3 and 5-7 exhibited moderate cytotoxicities against cultured human colon carcinoma (HT-29), human breast carcinoma (MCF-7), and human hepatoblastoma (HepG-2). Compound 8 showed strong inhibitory effects on DNA topoisomerases I and II (70 and 96% inhibition at a concentration of $20\;{\mu}M$, respectively).

Synthesis of Benzoquinoxalines

  • Kwon, Nam-Koong;Lee, Hee-Soon
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
    • /
    • pp.351.2-351.2
    • /
    • 2002
  • We have previously reported the synthesis and cytotoxic activities of a series of azaanthraquinone derivatives on the model of doxorubicin(Dox). Dox is known to intercalate into DNA and to inhibit topoisomerase II activity. But in the case of Quinone compounds like Dox. its use is limited because of systemic toxicities. primarily cardiotoxicity and myelosuppression. In this study. we describe the synthesis of benzoquinoxaline derivatives as DACA analogue. DACA has a neutral chromophore and acridine moiety and posions both topoisomerases I and ll with DNA intercalating activity. In order to delineate the SAR of benzoquinoxaline derivatives. an effcient sythetic rout to the target compounds without quinone group. Various attempted removal of quinone from benzoquinoxlinedione was unsuccessful. Diels-Alder rout applied for the synthesis of the target compounds will be discussed.

  • PDF

가미보중익기탕이 항암활성 및 항전이효과에 관한 연구 (Study on Antitumor Activity of Kamibojungikgi-tang)

  • 이병주;김동희;이효정;김성훈
    • 동의생리병리학회지
    • /
    • 제17권3호
    • /
    • pp.765-770
    • /
    • 2003
  • To explore the possible cancer agent from oriental prescriptions, we have examined its antitumor and anti metastatic activities of Kamibojungikgi-tang(KBIT). KBIT extracts exhibited cytotoxicity against P388, A549 and B16-F10 cell lines in a dose-dependent manner and showed antiadhesive effect of A549 cell to complex extracellular matrix at 1 ㎎/㎖ in vitro. In DNA topoisomerase I assay, KBIT extracts showed strong inhibitoty effect in a dose-dependent manner. In pulmonary colonization assay with B16BL6, a number of colonies in the lungs were decreased effectively in KBIT treated group as compared with control group. Moreover, in CAM assay, KBIT extracts significantly inhibited angiogenesis at 15㎍/egg as compared with control. The T/C% was 141% in KBIT treated group in S-180 bearing ICR mice. From the above results it was concluded that KBIT had antitumor and anti metastatic activities. So it is expected to be clinically helpful on the prevention and treatment of cancer, although it is still necessary to study its mechanism on molecular biology and immunology.

구강암 세포주에 대한 CKD-602의 항암 효과 (ANTICANCER EFFECT OF CKD-602(BELOTECAN, CAMTOBELL$^{(R)}$) ON THE ORAL CANCER CELL LINES)

  • 윤필영;옥용주;명훈;이종호;김명진
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
    • /
    • 제31권1호
    • /
    • pp.7-12
    • /
    • 2005
  • Purpose: CKD-602, a newly developed water-soluble campthotecin analogue, is a anticancer agent which act as a DNA topoisomerase I inhibitor. CKD-602 is known as more potent and tolerable agent. The main purposes of this study were to measure the cytotoxic effect of CKD-602 on the oral cancer cell lines and to evaluate the apoptotic aspect of dead cells. Materials and Methods: To determine the cytotoxic effect of CKD-602 on the oral cancer cell lines in comparison with various cell lines, such as lung cancer and colon cancer cell lines, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay was performed. And apoptosis was analyzed using fluorescence-activated cell sorting(FACS) system. Results: CKD-602 decreased the viability of malignant cells in a dose dependent manner and in a time dependent manner. CKD-602 showed excellent cytotoxicity to the oral cancer cell lines. Also, apoptotic portion was increased in a dose dependent manner. Conclusion: These findings indicated that CKD-602 induced apoptotic cell death in the various cell lines including oral cancer cell lines. From the results, it was suggested that CKD-602 would be a potential therapeutic agent for the oral cancer. More successive researches on the anticancer effect of CKD-602 should be performed.

A New Stilbene Glucoside from the Roots of Polygonum multiflorum Thunb.

  • Xu, Ming-Lu;Zheng, Ming Shan;Lee, Yeon-Kyong;Moon, Dong-Cheol;Lee, Chong-Soon;Woo, Mi-Hee;Jeong, Byeong-Seon;Lee, Eung-Seok;Jahng, Yurng-Dong;Chang, Hyeun-Wook;Lee, Seung-Ho;Son, Jong-Keun
    • Archives of Pharmacal Research
    • /
    • 제29권11호
    • /
    • pp.946-951
    • /
    • 2006
  • One new stilbene glucoside (6), along with five known compounds (1-5), were isolated from the roots of Polygonum multiflorum Thumb., and their chemical structures established based on physicochemical and spectroscopic data. Of the compounds, compound 3 showed DNA topoisomerase I and II inhibitory activities.