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View Full Version : Reversal effect and mechanism of lobeline on the multidrug-resistance of human breast


Rich66
09-08-2009, 07:38 PM
<dl class="AbstractPlusReport"><dt class="head">1: Zhong Nan Da Xue Xue Bao Yi Xue Ban. (javascript:AL_get(this,%20'jour',%20'Zhong%20Nan% 20Da%20Xue%20Xue%20Bao%20Yi%20Xue%20Ban.');) 2009 Aug;34(8):738-43.
</dt><dd class="abstract"> [Reversal effect and mechanism of lobeline on the multidrug-resistance of human breast cancer cells MCF-7/ADM.]

[Article in Chinese]


<!--AuthorList-->Chen J (http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=Search&Term=%22Chen%20J%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_DiscoveryPanel.Pubmed_RVAbstractPlus), Shen L (http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=Search&Term=%22Shen%20L%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_DiscoveryPanel.Pubmed_RVAbstractPlus), Zhou R (http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=Search&Term=%22Zhou%20R%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_DiscoveryPanel.Pubmed_RVAbstractPlus), Yao W (http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=Search&Term=%22Yao%20W%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_DiscoveryPanel.Pubmed_RVAbstractPlus), Zhong M (http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=Search&Term=%22Zhong%20M%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_DiscoveryPanel.Pubmed_RVAbstractPlus), Zhu ZH (http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=Search&Term=%22Zhu%20ZH%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_DiscoveryPanel.Pubmed_RVAbstractPlus), Zeng S (http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=Search&Term=%22Zeng%20S%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_DiscoveryPanel.Pubmed_RVAbstractPlus).
Department of Oncology, Xiangya Hospital, Central South University, Changsha 410008, China.
Objective To explore the reversal effect and mechanism of lobeline on the multidrug-resistance (MDR) of human breast cancer cells MCF-7/ADM. Methods In human breast cancer cell line MCF-7/ADM, MTT assay was used to determine the cell growth inhibiting ratio of MCF-7/ADM by ADM and Fu.Fluorospectorphotometer was employed to investigate the intracellular concentration of rhodamine123 to reflect the effect of lobeline on the activity of MDR-related protein P-glycoprotein (P-gp).Taking untreated MCF-7/ADM cells as controls,flow cytometry was applied to detect the intracellular concentration of rhodamine123 in MCF-7/ADM cell intervened with lobeline of 20 mumol/L.Results The sensitivity of MCF-7/ADM to ADM and Fu was significantly increased by lobeline in a dose-dependent manner. The inhibitive concentration 50 (IC(50)) of ADM declined from (44.81+/-0.43) mg/L to (16.72+/-0.75) mg/L with a reversion index of 2.68. The IC(50) of Fu declined from (53.12+/-1.60) mg/L to (38.90+/-1.43) mg/L with a reversion index of 1.37. The fluorescence intensity of lobeline-treated cells was significantly higher than that of the controls, when the concentration of lobeline was more than 10 mumol/L. With fewer side effects, the reversal efficacy of 20 mumol/L lobeline was 71.6% of the classical MDR reversal agent of verapamil at the same concentration. Conclusion Lobeline can reverse the MDR of MCF-7/ADM cells by inhibiting the activity of P-glycoprotein.
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Rich66
09-08-2009, 07:40 PM
http://en.wikipedia.org/wiki/Lobeline
Lobeline has been used as a smoking cessation (http://en.wikipedia.org/wiki/Smoking_cessation) aid,<sup id="cite_ref-0" class="reference">[1] (http://en.wikipedia.org/wiki/Lobeline#cite_note-0)</sup><sup id="cite_ref-1" class="reference">[2] (http://en.wikipedia.org/wiki/Lobeline#cite_note-1)</sup><sup id="cite_ref-2" class="reference">[3] (http://en.wikipedia.org/wiki/Lobeline#cite_note-2)</sup> and may have application in the treatment of other drug addictions such as addiction to amphetamines<sup id="cite_ref-3" class="reference">[4] (http://en.wikipedia.org/wiki/Lobeline#cite_note-3)</sup><sup id="cite_ref-4" class="reference">[5] (http://en.wikipedia.org/wiki/Lobeline#cite_note-4)</sup>, cocaine<sup id="cite_ref-5" class="reference">[6] (http://en.wikipedia.org/wiki/Lobeline#cite_note-5)</sup> or alcohol.<sup id="cite_ref-6" class="reference">[7] (http://en.wikipedia.org/wiki/Lobeline#cite_note-6)</sup>.