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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Xu, Hong-Bin Xu, Lu-Zhong Mao, Xia-Ping Fu, Jun |
| Description | Author Affiliation: Xu HB ( Department of Clinical Pharmacy, Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai 200072, China. Electronic address: xuhongbin@tongji.edu.cn.); Xu LZ ( Department of Clinical Pharmacy, Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai 200072, China.); Mao XP ( Department of Clinical Pharmacy, Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai 200072, China.); Fu J ( Department of Clinical Pharmacy, Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai 200072, China.) |
| Abstract | The purpose of this study was to investigate the effects of guggulsterone on cyclooxygenase-2 and P-glycoprotein mediated drug resistance in imatinib-resistant K562 cells (K562/IMA). MTT cytotoxicity assay, flow cytometry, western blot analysis, and ELISA were performed to investigate the anti-proliferative effect, the reversal action of drug resistance, and the inhibitory effect on cyclooxygenase-2, P-glycoprotein, BCR/ABL kinase, and PGE2 release in K562/IMA cells by guggulsterone. The results showed that co-administration of guggulsterone resulted in a significant increase in chemo-sensitivity of K562/IMA cells to imatinib, compared with imatinib treatment alone. Rhodamine123 accumulation in K562/IMA cells was significantly enhanced after incubation with guggulsterone (60, 120 µM), compared with untreated K562/IMA cells (p<0.05). When imatinib (1 µM) was combined with guggulsterone (60, 120 µM), the mean apoptotic population of K562/IMA cells was 15.47% and 24.91%. It was increased by 3.82 and 6.79 times, compared with imatinib (1 µM) treatment alone. Furthermore, guggulsterone had significantly inhibitory effects on the levels of cyclooxygenase-2, P-glycoprotein and prostaglandin E2. However, guggulsterone had little inhibitory effect on the activity of BCR/ABL kinase. The present study indicates guggulsterone induces apoptosis by inhibiting cyclooxygenase-2 and down-regulating P-glycoprotein expression in K562/IMA cells. |
| File Format | HTM / HTML |
| ISSN | 09447113 |
| Issue Number | 7 |
| Volume Number | 21 |
| e-ISSN | 1618095X |
| Journal | Phytomedicine |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2014-06-15 |
| Publisher Place | Germany |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Complementary Therapies Benzamides Pharmacology Commiphora Chemistry Cyclooxygenase 2 Inhibitors Drug Resistance, Neoplasm Drug Effects P-glycoprotein Antagonists & Inhibitors Piperazines Pregnenediones Pyrimidines Antineoplastic Agents, Phytogenic Antineoplastic Combined Chemotherapy Protocols Apoptosis Cyclooxygenase 2 Metabolism Dinoprostone Fusion Proteins, Bcr-abl Humans Imatinib Mesylate K562 Cells P-glycoproteins Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Drug Discovery Molecular Medicine Pharmacology Complementary and Alternative Medicine Pharmaceutical Science |
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