Interaction between natural compounds and human topoisomerase I

Castelli, Silvia; Coletta, Andrea; D’Annessa, Ilda; Fiorani, Paola; Tesauro, Cinzia; Desideri, Alessandro

doi:10.1515/hsz-2012-0240

Cited by 43 publications

(26 citation statements)

References 67 publications

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“…While most antineoplastic agents inhibit cancer cell proliferation by binding to DNA, CPT antitumor activity is due to inhibition of the nuclear enzyme topoisomerase I [4–5]. In spite of its potential as chemotherapeutic agent, CPT suffers from a reduced in vivo antitumor efficacy owing to its poor water-solubility and chemical instability (Fig.…”

Section: Introductionmentioning

confidence: 99%

PEGylated versus non-PEGylated magnetic nanoparticles as camptothecin delivery system

Castillo¹,

Mata²,

Casula³

et al. 2014

Beilstein J. Nanotechnol.

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SummaryCamptothecin (CPT; (S)-(+)-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-(4H,12H)-dione) is a highly cytotoxic natural alkaloid that has not yet found use as chemotherapeutic agent due to its poor water-solubility and chemical instability and, as a consequence, no effective administration means have been designed. In this work, camptothecin has been successfully loaded into iron oxide superparamagnetic nanoparticles with an average size of 14 nm. It was found that surface modification of the nanoparticles by polyethylene glycol enables loading a large amount of camptothecin. While the unloaded nanoparticles do not induce apoptosis in the H460 lung cancer cell line, the camptothecin-loaded nanoparticle formulations exhibit remarkable pro-apoptotic activity. These results indicate that camptothecin retains its biological activity after loading onto the magnetic nanoparticles. The proposed materials represent novel materials based on naturally occurring bioactive molecules loaded onto nanoparticles to be used as chemotherapeutic formulations. The procedure seems apt to be extended to other active molecules extracted from natural products. In addition, these materials offer the potential of being further implemented for combined imaging and therapeutics, as magnetic nanoparticles are known to be multifunctional tools for biomedicine.

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Section: Introductionmentioning

confidence: 99%

PEGylated versus non-PEGylated magnetic nanoparticles as camptothecin delivery system

Castillo¹,

Mata²,

Casula³

et al. 2014

Beilstein J. Nanotechnol.

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“…Several flavonoids have been shown to interact with Top1 such as quercetin. This compound seems to be able to inhibit the enzyme religation reaction (Castelli et al, 2012).…”

Section: Biological Roles and Effectsmentioning

confidence: 99%

Engineered Escherichia coli as new source of flavonoids and terpenoids

Putignani

Massa

Alisi

2013

Food Research International

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“…The enzyme can be inhibited by natural and nonnatural compounds [10][11][12][13][14][15], that are divided into two classes: class I inhibitors, named poisons, stabilize the enzyme-DNA covalent complex and class II inhibitors, named catalytic inhibitors, interfere with the cleavage or the binding steps of DNA and usually do not stabilize the covalent complex [13]. Camptothecin (CPT) is the best studied poison compound, acting as an interfacial inhibitor that specifically targets the hTopIB, reversibly binding the covalent enzyme-DNA complex [16][17][18][19], slowing down the religation step.…”

Section: Introductionmentioning

confidence: 99%