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Role of 13-(di)phenylalkyl berberine derivatives in the modulation of the activity of human topoisomerase IB.

Abstract：

:Topoisomerases IB are anticancer and antimicrobial targets whose inhibition by several natural and non-natural compounds has been documented. The inhibition effect by berberine and some 13-(di)phenylalkyl berberine derivatives has been tested towards human topoisomerase IB. Derivatives belonging to the 13-diphenylalkyl series display an efficient inhibition of the DNA relaxation and cleavage step, that increases upon pre-incubation with the enzyme. The religation step of the enzyme catalytic cycle is not affected by compounds and only slightly upon pre-incubation. The binding of the protein to the DNA substrate occurs also in the presence of the compounds, as monitored by a DNA shift assay, indicating that the compounds are not able to inhibit the formation of the enzyme-DNA complex but that they act as catalytic inhibitors.

journal_name

Int J Biol Macromol

journal_title

International journal of biological macromolecules

authors

Vieira S,Castelli S,Falconi M,Takarada J,Fiorillo G,Buzzetti F,Lombardi P,Desideri A

doi

10.1016/j.ijbiomac.2015.02.051

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

68-75

eissn

0141-8130

issn

1879-0003

pii

S0141-8130(15)00155-5

journal_volume

77

pub_type

杂志文章

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