دورية أكاديمية
Amyrin esters induce cell death by apoptosis in HL-60 leukemia cells.
| العنوان: | Amyrin esters induce cell death by apoptosis in HL-60 leukemia cells. |
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| المؤلفون: | Barros FW; Departament of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, Ceará 60430-270, Brazil., Bandeira PN, Lima DJ, Meira AS, de Farias SS, Albuquerque MR, dos Santos HS, Lemos TL, de Morais MO, Costa-Lotufo LV, Pessoa Cdo Ó |
| المصدر: | Bioorganic & medicinal chemistry [Bioorg Med Chem] 2011 Feb 01; Vol. 19 (3), pp. 1268-76. Date of Electronic Publication: 2010 Dec 09. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Original Publication: Oxford : New York : Pergamon Press, c1993- |
| مواضيع طبية MeSH: | Burseraceae*, Antineoplastic Agents/*chemical synthesis , Antineoplastic Agents/*pharmacology , Apoptosis/*drug effects , Cell Death/*drug effects , Leukocytes, Mononuclear/*drug effects , Oleanolic Acid/*analogs & derivatives , Plant Preparations/*chemical synthesis, Antineoplastic Agents/chemistry ; Caspase 3/metabolism ; Cell Cycle/drug effects ; Cell Line, Tumor ; HL-60 Cells ; Humans ; Molecular Structure ; Oleanolic Acid/chemical synthesis ; Oleanolic Acid/chemistry ; Oleanolic Acid/pharmacology ; Plant Preparations/analogs & derivatives ; Plant Preparations/pharmacology |
| مستخلص: | Four derivatives of an α,β-amyrin mixture were synthesized by acylation with appropriate anhydrides. The structures of the compounds were confirmed by means of IR and (1)H and (13)C NMR. The compounds were screened for cytotoxic activity using four human tumor cell lines (HL-60, MDAMB-435, SF-295 and HCT-8) and normal peripheral blood mononuclear cells (PBMC). 3-O-Carboxymaleinate of α,β-amyrin (3a/3b) were found to be the only active compounds of the series (high cytotoxicity), showing IC(50) values ranging from 1.8 to 3μM. In PBMC, 3a/3b were not toxic, suggesting selectivity for tumor cells. To better understand the mechanism of action involved in the cytotoxicity of 3a/3b, HL-60 cells treated with 3a/3b were examined for morphological changes, DNA fragmentation, cell cycle perturbation, externalization of phosphatidylserine and activation of caspases 3/7, with doxorubicin serving as the positive control. The results indicate that the cytotoxicity of 3a/3b involves the induction of cell death by apoptosis. (Copyright © 2010 Elsevier Ltd. All rights reserved.) |
| المشرفين على المادة: | 0 (Antineoplastic Agents) 0 (Plant Preparations) 6SMK8R7TGJ (Oleanolic Acid) EC 3.4.22.- (Caspase 3) KM8353IPSO (beta-amyrin) |
| تواريخ الأحداث: | Date Created: 20110111 Date Completed: 20110823 Latest Revision: 20191210 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1016/j.bmc.2010.12.016 |
| PMID: | 21216606 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3391 |
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| DOI: | 10.1016/j.bmc.2010.12.016 |