| Evaluation of cucurbitane-type triterpenoids from Momordica balsamina on P-glycoprotein (ABCB1) by flow cytometry and real-time fluorometry. | |
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MedLine Citation:
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PMID: 19846941 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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BACKGROUND: Cancer cells become refractory to chemotherapy as a consequence of their overexpressing ABC transporters that extrude not only the therapeutic agent but other unrelated compounds such as chemotoxins and biocides before they can reach their intended targets. A compound that can inhibit the activity of these transporters may find use as an adjunct to chemotherapy that had been rendered ineffective. MATERIALS AND METHODS: Four curcubitane-type triterpenes isolated from Momordica balsamina Linn. (Cucurbitaceae), a plant from Mozambique were evaluated for their inhibition of the ABC transporter P-glycoprotein coded by the human ABCB1 gene transfected into mouse lymphoma cells. The evaluation was conducted by flow cytometry using rhodamine 123 and real-time fluorometry assessing accumulation of ethidium bromide (EB) on a real-time basis. RESULTS: Among the compounds isolated, the most active was 7-methoxycucurbita-5,24-diene-3beta,23(R)-diol, which inhibited the efflux of ethidium bromide (EB) and rhodamine 123 from the ABCB1-transfected mouse lymphoma cell. CONCLUSION: Real-time fluorometry replicated the flow cytometric results with significant advantages for the evaluation of efflux pump inhibitors. The substitution of side groups on the cucurbitane skeleton appears to be significant in the inhibition of ABCB1 activity. |
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Authors:
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Gabriella Spengler; Cátia Ramalhete; Marta Martins; Ana Martins; Julianna Serly; Miguel Viveiros; Joseph Molnár; Noélia Duarte; Silva Mulhovo; Maria-José U Ferreira; Leonard Amaral |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Anticancer research Volume: 29 ISSN: 1791-7530 ISO Abbreviation: Anticancer Res. Publication Date: 2009 Oct |
Date Detail:
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Created Date: 2009-10-22 Completed Date: 2009-11-30 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8102988 Medline TA: Anticancer Res Country: Greece |
Other Details:
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Languages: eng Pagination: 3989-93 Citation Subset: IM |
Affiliation:
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Unit of Mycobacteriology, Instituto de Higiene e Medicina Tropical, Universidade Nova de Lisboa, Rua da Junqueira 96, 1349-008 Lisboa, Portugal. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Cell Line, Tumor Flow Cytometry Fluorometry Glycosides / chemistry, pharmacology* Lymphoma, T-Cell / drug therapy, genetics, metabolism Mice Momordica / chemistry* P-Glycoprotein / antagonists & inhibitors*, biosynthesis, genetics Terpenes / chemistry, pharmacology* Transfection Triterpenes / chemistry, pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Glycosides; 0/P-Glycoprotein; 0/Terpenes; 0/Triterpenes; 0/cucurbitane |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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