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Comparative study of microtubule inhibitors--estramustine and natural podophyllotoxin conjugated PAMAM dendrimer on glioma cell proliferation.

Abstract：

:The synthetic estramustine (EM) and natural podophyllotoxin (PODO) anti-mitotic agents that inhibit tubulin polymerization are known anticancer agents. As low bioavailability limits their anticancer properties, we investigated whether conjugation with PAMAM dendrimer (D) could enhance the activity of D-EM and D-PODO by altering their release pattern. Release kinetics indicated synthesized conjugates to be stable against hydrolytic cleavage and showed sustained release characteristics. However, release of D-EM was slow compared to D-PODO conjugate. Antitumor effect of these conjugates on glioma cells revealed (i) increased cell death and cell cycle arrest (ii) decreased migration and (iii) increased tubulin depolymerization as compared to free drug. Importantly, the effects of natural PODO conjugate on glioma cell survival and migration is more pronounced than D-EM.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Sk UH,Dixit D,Sen E

doi

10.1016/j.ejmech.2013.07.007

subject

Has Abstract

pub_date

2013-10-01 00:00:00

pages

47-57

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00455-8

journal_volume

68

pub_type

杂志文章

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