Gamma-tocotrienol does not compete with mitoxantrone to be effluxed from ABCG2 overexpressing cells

Then Sue-Mian, . and Loh Sandy Hwei San, . and Tan Karl Vern, . and Briggs Deborah, . and Kerr Ian, . Gamma-tocotrienol does not compete with mitoxantrone to be effluxed from ABCG2 overexpressing cells. pp. 630-638. ISSN 1511-2780

The human adenosine (ATP)-binding cassette (ABC) subfamily G2 (ABCG2) half transporter of the G-subfamily that is involved in transportation of an extensive range of substrates including xenobiotics and endogenous compounds. ABCG2 transporter upregulation in many cancerous tissues is often linked to multiple drug resistance (MDR) due to its involvement in efflux of various drugs. Gamma-tocotrienol (T3) is an isoform of vitamin E that possesses promising anti-cancer effects via various mechanisms however transportation of T3 remains unknown and its therapeutic effects might be limited by MDR. This project thus sought to study the anti-cancer effect (i.e. anti-proliferative effect) of T3 in an ABCG2-expressing breast cancer cell line (MCF7-MX) and the possibility of T3 to be transported via ABCG2 transporter. It was demonstrated that after 72 hr treatment with T3 cell proliferation of MCF7-MX cells was inhibited with IC‚‚43 M. The co-administration of T3 with mitoxantrone (MX) a substrate of ABCG2 has shown that T3 is not a competitor for MX transport (p0.05). The data confirms the anti-proliferative role of T3 in ABCG2 expressing cells and suggests that ABCG2 might have a minimal role in T3 transport. This result provides an essential basis for the further study of T3 as an anti-cancer compound.

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Abstract

The human adenosine (ATP)-binding cassette (ABC) subfamily G2 (ABCG2) half transporter of the G-subfamily that is involved in transportation of an extensive range of substrates including xenobiotics and endogenous compounds. ABCG2 transporter upregulation in many cancerous tissues is often linked to multiple drug resistance (MDR) due to its involvement in efflux of various drugs. Gamma-tocotrienol (T3) is an isoform of vitamin E that possesses promising anti-cancer effects via various mechanisms however transportation of T3 remains unknown and its therapeutic effects might be limited by MDR. This project thus sought to study the anti-cancer effect (i.e. anti-proliferative effect) of T3 in an ABCG2-expressing breast cancer cell line (MCF7-MX) and the possibility of T3 to be transported via ABCG2 transporter. It was demonstrated that after 72 hr treatment with T3 cell proliferation of MCF7-MX cells was inhibited with IC‚‚43 M. The co-administration of T3 with mitoxantrone (MX) a substrate of ABCG2 has shown that T3 is not a competitor for MX transport (p0.05). The data confirms the anti-proliferative role of T3 in ABCG2 expressing cells and suggests that ABCG2 might have a minimal role in T3 transport. This result provides an essential basis for the further study of T3 as an anti-cancer compound.

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Item Type:	Article
AGROVOC Term:	Tocotrienols
AGROVOC Term:	Vitamin e
AGROVOC Term:	Drug resistance
AGROVOC Term:	Chemical reagents
AGROVOC Term:	Cancer (disease)
AGROVOC Term:	Cell culture
AGROVOC Term:	Disease treatment
Depositing User:	Mr. AFANDI ABDUL MALEK
Last Modified:	24 Apr 2025 00:55
URI:	http://webagris.upm.edu.my/id/eprint/9501

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