UCE6, a New Antitumor Antibiotic with Topoisomerase I-mediated DNA Cleavage Activity Produced by Actinomycetes: Producing Organism,Fermentation, Isolation and Biological Activity.

Two novel oxovanadium(IV) complexes ([VO(hntdtsc)(BPIP)] and [VO(hntdtsc)(MOPIP)] (hntdtsc = 2-hydroxy-1-naphthaldehydethiosemicarbazone, BPIP = 2-(4-bromophenyl)-imidazo[4,5- f]-1,10-phenanthroline, MOPIP = 2-(4-methoxyphenyl)-imidazo[4,5- f]1,10-phenanthroline), are synthesized and characterized. Subsequently, the Methyl Thiazolyl Tetrazolium (MTT) assay is used to investigate the antitumor activity of the ligand and two complexes in vitro.The results indicate that both complexes could significantly inhibit selected tumor cells (SH-SY5Y, MCF-7, and SK-N-SH). In addition, the antibacterial activity of VO(hntdtsc)(BPIP) against Staphylococcus aureus is further investigated. Interestingly, VO(hntdtsc)(BPIP) can efficiently attenuate S. aureus growth and abrogate α-hemolysin secretion and biofilm formation. The plasmid DNA cleavage activity of both complexes is also investigated. The results suggest that supercoiled plasmid DNA is efficiently cleaved after treatment with each complex, which might contribute to the biological activity of these oxovanadium(IV) complexes.

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UCT4B, a new antitumor antibiotic with topoisomerase II mediated DNA cleavage activity.

The Journal of Antibiotics ◽

10.7164/antibiotics.46.235 ◽

1993 ◽

Vol 46 (2) ◽

pp. 235-240 ◽

Cited By ~ 10

Author(s):

YOUICHI UOSAKI ◽

SHO-ZOU KAWADA ◽

HIROFUMI NAKANO ◽

YUTAKA SAITOH ◽

HIROSHI SANO

Keyword(s):

Dna Cleavage ◽

Topoisomerase Ii ◽

Antitumor Antibiotic ◽

Cleavage Activity ◽

Dna Cleavage Activity

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Saintopin, a new antitumor antibiotic with topoisomerase II dependent DNA cleavage activity, from Paecilomyces.

The Journal of Antibiotics ◽

10.7164/antibiotics.43.1344 ◽

1990 ◽

Vol 43 (10) ◽

pp. 1344-1346 ◽

Cited By ~ 25

Author(s):

YOSHINORI YAMASHITA ◽

YUTAKA SAITOH ◽

KATSUHIKO ANDO ◽

KEIICHI TAKAHASHI ◽

HIROE OHNO ◽

...

Keyword(s):

Dna Cleavage ◽

Topoisomerase Ii ◽

Antitumor Antibiotic ◽

Cleavage Activity ◽

Dna Cleavage Activity

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Synthesis and Characterisation of RuII Polypyridyl Complexes: DNA-Binding, Photocleavage, and Topoisomerase I and II Inhibitory Activity

Australian Journal of Chemistry ◽

10.1071/ch13329 ◽

2013 ◽

Vol 66 (11) ◽

pp. 1406 ◽

Cited By ~ 3

Author(s):

Xiaojun He ◽

Guang Yang ◽

Xiaonan Sun ◽

Lingjun Xie ◽

Lifeng Tan

Keyword(s):

Dna Binding ◽

Dna Cleavage ◽

Topoisomerase I ◽

Mixed Ligand ◽

Dual Inhibitor ◽

Cleavage Activity ◽

Dna Cleavage Activity ◽

Pbr322 Dna ◽

Dna Strand ◽

Strand Passage

Two mixed-ligand ruthenium(ii) complexes [Ru(phen)2(cptcp)]2+ (Ru1; phen = 1,10-phenanthroline, cptcp = 2-(4-carbazol-9-yl-phenyl)-1H-1,3,7,8-tetraaza-cyclopenta-[l]-phenanthrene) and [Ru(phen)2(btcpc)]2+ (Ru2; btcpc = 9-butyl-6-(1H-1,3,7,8-tetraaza-cyclo-cyclopenta-[l]-phenanthren-2-yl)-9H-carbazole-3-carbaldehyde) have been synthesised and characterised. The DNA-binding behaviours of the two complexes have been investigated by using spectroscopic and viscosity measurements. Results suggest that the two complexes bind to DNA by intercalation. The photocleavage of plasmid pBR322 DNA indicates that Ru1 exhibits more effective DNA cleavage activity in comparison to that exhibited by Ru2 under the same conditions, and different cleavage mechanisms are determined. Topoisomerase inhibition and DNA strand passage assay confirm that Ru1 may act as an efficient dual inhibitor of topoisomerases I and II, whereas Ru2 may only act as a single inhibitor of topoisomerases II.

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