ChemInform Abstract: Amphimic Acids, Novel Unsaturated C28 Fatty Acids as DNA Topoisomerase I Inhibitors from an Australian Sponge Amphimedon sp.

ChemInform ◽  
2010 ◽  
Vol 28 (43) ◽  
pp. no-no
Author(s):  
T. NEMOTO ◽  
M. OJIKA ◽  
Y. SAKAGAMI
Keyword(s):  
Fatty Acids ◽  
Topoisomerase I ◽  
Dna Topoisomerase I ◽  
Dna Topoisomerase ◽  
Topoisomerase I Inhibitors

Synthesis and Pharmacological Evaluation of Novel Homocamptothecin-Dihydropyridine Derivative Conjugates as Potent Topoisomerase I Inhibitors

2011 ◽  
Vol 64 (10) ◽  
pp. 1390 ◽  
Author(s):  
Ling-Jian Zhu ◽  
Chun-Lin Zhuang ◽  
Ning Lei ◽  
Chun-Quan Sheng ◽  
Wei Guo ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Antitumour Activity ◽  
Tumour Cell Line ◽  
Dna Topoisomerase I ◽  
Inhibition Activity ◽  
Dna Topoisomerase ◽  
Antitumour Agents ◽  
Topoisomerase I Inhibitors ◽  
Dihydropyridine Derivative ◽  
New Generation

Homocamptothecins (hCPT) represent a new generation of antitumour agents targeting DNA topoisomerase I. The expanded seven-membered lactone E-ring that characterizes hCPT enhances the plasma stability of the drug and reinforces the inhibition of topoisomerase I (Topo I) compared with conventional six-membered CPT. In an attempt to improve the antitumour activity of hCP, a series of novel hCPT derivatives conjugating with dihydropyridine derivates were designed and synthesized based on a synthetic route that couples 7-formylhomocamptothecin with different dihydropyridine derivates. Most of the synthesized compounds exhibited good cytotoxic activity on tumour cell line A549, MDA-MB-435, and HCT116. Furthermore, this class of compounds showed superior Topo I inhibition activity comparable to or higher than CPT.

scholarly journals Inhibition of Escherichia coli DNA topoisomerase I activity by phospholipids

1992 ◽  
Vol 285 (2) ◽  
pp. 503-506 ◽  
Author(s):  
T Mizushima ◽  
S Natori ◽  
K Sekimizu
Keyword(s):  
Escherichia Coli ◽  
Fatty Acids ◽  
Topoisomerase I ◽  
Saturated Fatty Acids ◽  
Egg Yolk ◽  
Inhibitory Effect ◽  
Dna Topoisomerase I ◽  
Dna Topoisomerase ◽  
E Coli ◽  
Dna Relaxation

The DNA relaxation activity of Escherichia coli DNA topoisomerase I in vitro was greatly inhibited by cardiolipin. Inhibition also occurred to some extent with phosphatidylglycerol from egg yolk. Analysis with synthetic phospholipid revealed that phosphatidylglycerol containing unsaturated fatty acids exhibited a strong inhibitory effect, whereas inhibition by phosphatidylglycerol containing saturated fatty acids was weak. Phosphatidylethanolamine showed no inhibitory effect. Chlorpromazine, which interacts with phospholipids, suppressed the inhibitory effect of cardiolipin. Cardiolipin and phosphatidylglycerol with unsaturated fatty acid precipitated topoisomerase I even at low concentrations, whereas phosphatidylglycerol from egg yolk and a synthetic phosphatidylglycerol containing saturated fatty acids precipitated this enzyme only at high concentrations. One-third of the total topoisomerase I in E. coli was found in the membrane fraction. Treatment of E. coli cells with chlorpromazine resulted in relaxation of plasmid DNA. This DNA relaxation was not observed in a topA mutant, suggesting that this relaxation by chlorpromazine in vivo is catalysed by topoisomerase I.

Hypersensitivity of NIH3T3 cells transformed by H-RAS gene to DNA-topoisomerase-I inhibitors

1996 ◽  
Vol 67 (5) ◽  
pp. 702-708 ◽  
Author(s):  
Tatsuo Ohira ◽  
Kazuto Nishio ◽  
Fumihiko Kanzawa ◽  
Tomoyuki Ishida ◽  
Yuichiro Ohe ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Dna Topoisomerase I ◽  
Ras Gene ◽  
Dna Topoisomerase ◽  
Nih3t3 Cells ◽  
Topoisomerase I Inhibitors
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