Abstract:
:When the prostate cancer cells become unresponsive to androgen therapy, resistance to chemotherapy becomes imminent, resulting in high mortality. To combat this situation, lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatum spores, was tested against hormone sensitive (LnCaP) and refractory (PC3) prostate cancer cells in vitro. This study aims to check if lycopodine has demonstrable anti-cancer effects and if it has, to find out the possible mechanism of its action. The MTT assay was performed to evaluate the cytotoxic effect. Depolarization of mitochondrial membrane potential, cell cycle, EGF receptor activity and apoptosis were recorded by FACS; profiles of different anti- and pro-apoptotic genes and their products were studied by semi-quantitative RT-PCR, indirect-ELISA, western blotting. Drug-DNA interaction was determined by CD spectroscopy. Administration of lycopodine down-regulated the expression of 5-lipoxygenase and the 5-oxo-ETE receptor (OXE receptor1) and EGF receptor, and caused up-regulation of cytochrome c with depolarization of mitochondrial inner membrane potential, without palpable change in p53 activity, resulting in apoptosis, cell arrest at G0/G1 stage and ultimately reduced proliferation of cancer cells; concomitantly, there was externalization of phosphotidyl serine residues. CD spectroscopic analysis revealed intercalating property of lycopodine with DNA molecule, implicating its ability to block cellular DNA synthesis. The overall results suggest that lycopodine is a promising candidate suitable for therapeutic use as an anti-cancer drug.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Bishayee K,Chakraborty D,Ghosh S,Boujedaini N,Khuda-Bukhsh ARdoi
10.1016/j.ejphar.2012.10.041subject
Has Abstractpub_date
2013-01-05 00:00:00pages
110-21issue
1-3eissn
0014-2999issn
1879-0712pii
S0014-2999(12)00910-7journal_volume
698pub_type
杂志文章abstract::Stimulation of [35S]GTPgammaS binding by serotonin (5-hydroxytryptamine, 5-HT) receptor ligands was characterized in rat hippocampal membranes. The optimized assay contained 30-50 microg protein, 300 microM GDP and 0.1 nM [35S]GTPgammaS, incubated at 37 degrees C for 20 min. At 10 microM, the 5-HT1A receptor agonist R...
journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
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doi:10.1016/s0014-2999(98)00110-1
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00882-1
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(84)90147-x
更新日期:1984-04-06 00:00:00
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journal_title:European journal of pharmacology
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更新日期:1975-05-01 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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abstract::Angiogenesis is critical for re-establishing blood supply to the ischemic myocardium after acute myocardial infarction (AMI). This study aimed to investigate the effects of morroniside on angiogenesis after AMI and explored associated proangiogenic mechanisms. A rat model of AMI was established by ligation of the left...
journal_title:European journal of pharmacology
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更新日期:2020-04-05 00:00:00
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