Document Detail


Evaluation of cucurbitane-type triterpenoids from Momordica balsamina on P-glycoprotein (ABCB1) by flow cytometry and real-time fluorometry.
MedLine Citation:
PMID:  19846941     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
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:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Anticancer research     Volume:  29     ISSN:  1791-7530     ISO Abbreviation:  Anticancer Res.     Publication Date:  2009 Oct 
Date Detail:
Created Date:  2009-10-22     Completed Date:  2009-11-30     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8102988     Medline TA:  Anticancer Res     Country:  Greece    
Other Details:
Languages:  eng     Pagination:  3989-93     Citation Subset:  IM    
Affiliation:
Unit of Mycobacteriology, Instituto de Higiene e Medicina Tropical, Universidade Nova de Lisboa, Rua da Junqueira 96, 1349-008 Lisboa, Portugal.
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MeSH Terms
Descriptor/Qualifier:
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:
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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