Research Papers:

Chemopreventive activity of celastrol in drug–resistant human colon carcinoma cell cultures

Helena Moreira _, Anna Szyjka and Kazimierz Gąsiorowski

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Oncotarget. 2018; 9:21211-21223. https://doi.org/10.18632/oncotarget.25014

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Helena Moreira1, Anna Szyjka1 and Kazimierz Gąsiorowski1

1Department of Basic Medical Sciences, Wroclaw Medical University, Borowska 211, 50-556 Wrocław, Poland

Correspondence to:

Helena Moreira, email: [email protected]

Keywords: celastrol; colon cancer; multidrug resistance; cancer stem cells

Received: September 13, 2017     Accepted: March 09, 2018     Published: April 20, 2018


Celastrol (tripterine) a pentacyclic triterpenoid extracted from the roots of Tripterygium wilfordii Hook f., exhibits potent antioxidant and anti-inflammatory activity and also exerts important anti-cancer effects, as induction of apoptosis and lowering the level of drug resistance of several cancers.

Increased level of cellular resistance to cytostatic drugs is typical for colorectal cancers, and largely determines the failure of chemotherapy for this tumor.

The purpose of our research was to evaluate the chemopreventive effect of celastrol on cultures of colon cancer cells resistant to doxorubicin (LOVO/DX). With the use of flow cytometry we have shown that celastrol reduces the cell size of the SP (side population; subpopulation of cancer cells enriched with cancer stem cells), increases frequency of apoptosis and binds to Pgp protein in cell membranes inhibiting its transport function. The inhibition of the Pgp transport function has been shown to increase the accumulation of rhodamine-123 and standard cytostatic- doxorubicin in LOVO/DX cells.

Our results prove that celastrol exhibits significant chemopreventive and chemosensitizing activities on drug resistant colon cancer cells. Celastrol appears to be a good candidate for adjuvant medicine that can improve the effectiveness of standard cytostatic therapy in humans.

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