• Bulletin of the Korean Chemical Society
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• 제25권10호
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• pp.1559-1563
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• 2004

The topoisomerase II poisoning effect of certain protoberberine alkaloids is associated with anti-cancer activity. Structure-activity relationships of protoberberine analogues substituted on the ring protons reveal that substitution at the C19 position is an important determinant of biological activity. In this study, the effects of substituent modification at the C19 position on the interaction of protoberberines with DNA are determined using UV and NMR spectroscopy. The line broadening effect on aliphatic resonances, chemical shift changes of the imino protons of HP14 upon berberine and berberrubine binding to HP14, and the rate of the exchange process between protoberberine analogs bound indicate that berberrubine binds HP14 more specifically than berberine. In addition, the free HP14 is altered by the substituent at the 19-position. UV spectra of berberrubine have shown a hypochromic effect together with a slight red shift, which are usually regarded as characteristics of DNA intercalation. These results are consistent with our previous report that the berberrubine is partially intercalated with HP14 with molar ratio 1 : 1, whereas a non-specific interaction is predominant between the berberine and HP14.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.256.3-257
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• 2003

The bioactivity-guided fractionation of an active methylene chloride extract of the sclerotium of Poria cocos led to the isolation of compounds 1-5. These compounds were tested in the human colon carcinoma and human breast carcinoma cell lines, compounds 3, 4, and 5 exhibited IC50 values of 10.8, 15.4, and 5.1 $\mu\textrm{g}$/$m\ell$ against human colon carcinoma cell line. In addition, compounds 3, 4 and 5 showed moderate activities as inhibitors of Topoisomerase I and all compounds were inactive in the Topoisomerase II inhibition.

• Bulletin of the Korean Chemical Society
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• 제32권1호
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• pp.303-306
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• 2011

• 한국동물학회:학술대회논문집
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• 한국동물학회 1998년도 한국생물과학협회 학술발표대회
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• pp.315.1-315
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• 1998

No Abstract, See Full Text

• 한국독성학회:학술대회논문집
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• 한국독성학회 2001년도 International Symposium on Signal transduction in Toxicology
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• pp.9-13
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• 2001

Genistein, a natural isoflavonoid phytoestrogen, is a strong inhibitor of protein tyrosine kinase and DNA topoisomerase II activities. Genistein has been shown to have anticancer proliferation, differentiation and chemopreventive effects. In the present study, we have addressed the mechanism of action by which genistein suppressed the proliferation of p53-null human prostate carcinoma cells.(omitted)

• Bulletin of the Korean Chemical Society
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• 제27권8호
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• pp.1231-1234
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• 2006

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.315.1-315.1
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• 2002

DNA topoisomerases I (topo I) and II are essential enzymes that relax DNA supercoiling and relieve torsional strain during DNA processing. including replication. transcription. and repair. Topo I relaxes DNA by cleaving one strand of DNA by attacking a backbone phosphale with a catalytic lyrosine (Tyr723. human topo I). This enzyme has recently been investigated as a new target for antineoplastic drugs. Inhibitors to the enzyme intercalate between the DNA base pairs. interfering religation of cleaved DNA, therefore inhibit the activity of topo I. (omitted)

• 대한의생명과학회지
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• 제12권3호
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• pp.161-170
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• 2006

A new piperazine derivative, 8J-8029, is a synthetic anti-cancer agent which exhibits both microtubule and topoisomerase II inhibiting activities. In this study, we investigated the ability of 8J-8029 for anti-angiogenesis and apoptosis. 8J-8029 decreased the bFGF-induced angiogenesis in the CAM and the mouse Matrigel implants, in vivo. 8J-8029 inhibited the proliferation, migration, invasion, tube fonnation, and expression of MMP-2 in BAECs. In addition, 8J-8029 reduced the cell viability in HepG2 cells, caused the production of fragmented DNA and the morphological changes corresponding to apoptosis. 8J-8029 also elicited the release of cytochrome c and the activation of caspase-3. Taken together, these results suggest 8J-8029 may be a candidate for anti-cancer agent with the ability to inhibit the angiogenesis of endothelial cells and to induce the apoptosis of tumor cells.

• 대한임상검사과학회지
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• 제48권2호
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• pp.74-81
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• 2016

Fluoroquinolone 계 항생제의 광범위한 사용으로 인해 이 약제에 대한 내성 Ureaplasma 종의 분리 비율이 높아지고 있다. Fluoroquinolone 계 항생제 내성은 주로 DNA gyrase와 topoisomerase IV 유전자의 돌연변이로 인해 발생하는 것으로 알려져 있다. DNA gyrase는 A와 B 2개의 소단위로 이루어져 있으며, gyrA와 gyrB 유전자에 의해 암호화되어 있고, Topoisomerase IV는 parC와 parE 유전자에 의해 암호화되어 있다. 본 연구가 진행된 서울의 1개 3차 병원에서 2012년부터 2013년까지 1년동안 Ureaplasma 종의 fluoroquinolone 계 항생제인 OFL과 CIP의 항생제검사 감수성 결과를 분석한 결과 내성과 중등도를 합산할 경우 66.08%, 92.69%로 매우 높은 내성 비율을 보였다. 이에 Ureaplasma 종을 OFL과 CIP에 대한 감수성을 기준으로 4개 그룹으로 분류하여 gyrA, gyrB, parC, parE 유전자의 돌연변이 여부를 검사하여 항생제 내성과의 관련성을 밝히고자 하였다. 그 중 parC 유전자의 돌연변이 빈도가 높아 topoisomerase IV의 돌연변이가 fluoroquinolone 계 약제에 대한 내성과 밀접한 관련이 있음을 확인할 수 있었다. 본 연구를 통해 GyrB의 Asn481Ser, ParC의 Phe149Leu, Asp150Met, Asp151Ile, Ser152Val, ParE의 Pro446Ser, Arg448Lys을 추가로 발견할 수 있었다. 최근 fluoroquinolone 계 항생제의 사용이 증가하고 있기 때문에 추후 Ureaplasma 종의 fluoroquinolone 계 항생제 내성에 대한 지속적인 모니터링이 필수적일 것으로 사료되며, 이와 관련한 유전자의 돌연변이 양상과의 상관관계를 분석하여 기존 배양검사의 단점을 보완할 수 있는 분자 진단학적 검사법의 추가적인 분석이 필요할 것으로 사료된다.

• Bulletin of the Korean Chemical Society
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• 제34권9호
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• pp.2675-2679
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• 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.