Abstract：
:Cytochrome P450 2J2 (CYP2J2) is highly expressed in human tumors and carcinoma cell lines, and has been implicated in the pathogenesis of human cancers. The aim of this study was to identify a compound that could inhibit the activity of CYP2J2, and to examine its anticancer activity. To identify CYP2J2 inhibitors, 10 terpenoids obtained from plants were screened using astemizole as a CYP2J2 probe substrate in human liver microsomes (HLMs). Of these, tanshinone IIA dose-dependently and non-competitively inhibited CYP2J2-mediated astemizole O-demethylation activity. Tanshinone IIA significantly decreased viability of human hepatoma HepG2 cells and SiHa cervical cancer cells; however, it was not cytotoxic against mouse hepatocytes. Furthermore, treatment of cells with tanshinone IIA significantly increased apoptotic cell death rate, as shown by the increase in Annexin V-stained cell populations, Bcl-2 associated X protein (Bax)/B-cell lymphoma 2 (Bcl-2) ratio, and poly (ADP-ribose) polymerase 1 (PARP-1) cleavage in HepG2 cells. Furthermore, the results of this study showed that tanshinone IIA significantly decreased HepG2 cell-based tumor growth in nude mice in a dose-dependent manner. On the other hand, the tanshinone IIA-induced apoptotic cell death rate was significantly attenuated by enhanced up-regulation of CYP2J2 expression. Thus, our data strongly suggest that tanshinone IIA exerts its anticancer effect by inhibiting CYP2J2 activity.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Jeon YJ,Kim JS,Hwang GH,Wu Z,Han HJ,Park SH,Chang W,Kim LK,Lee YM,Liu KH,Lee MYdoi
10.1016/j.ejphar.2015.07.047subject
Has Abstractpub_date
2015-10-05 00:00:00pages
480-488eissn
0014-2999issn
1879-0712pii
S0014-2999(15)30172-2journal_volume
764pub_type
杂志文章abstract：:Sabiporide, a new benzoguanidine, was characterized on fibroblasts stably expressing the Na(+)/H(+) exchanger isoforms NHE-1, NHE-2 and NHE-3. 22Na(+) uptake experiments show that this compound possesses a K(i) of 5+/-1.2 x 10(-8) M for NHE-1, and discriminates efficiently between the NHE-1, -2 and -3 isoforms (K(i) f...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02824-8
更新日期：2003-01-17 00:00:00
abstract：:Specific antagonists of platelet-activating factor (PAF) receptors inhibit platelet aggregation and thromboxane synthesis. These two processes have been implicated in the course of diabetic retinopathy. We assessed the effect of a specific PAF receptor antagonist, WEB 2086-BS (3-(4-(2-chlorophenyl)-9-methyl-6H-thieno(...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00664-5
更新日期：1998-10-30 00:00:00
abstract：:The ability of flunarizine to terminate ouabain-induced ventricular tachycardia was investigated in conscious dogs. These arrhythmias result from triggered activity based on delayed afterdepolarizations. Sustained ventricular tachycardia was induced by ouabain (48 +/- 6 micrograms/kg) and pacing in 13 animals with sur...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90780-2
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abstract：:We have examined the role of protein kinase C in the regulation of foetal-calf serum-stimulated cell proliferation in human prostatic smooth muscle cells. The data showed that the proliferative effect to foetal-calf serum (10%, v/v) was partially inhibited by 12-(2-cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-i...
journal_title：European journal of pharmacology
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doi：10.1016/s0014-2999(98)00683-9
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abstract：:Cannabinoid CB(2) receptor is reported to be expressed in varying amounts in different human immune subpopulations. To examine the expression pattern of CB(2) in the mouse, immune cell subpopulations were purified and studied by semiquantitative Reverse Transcription-Polymerase Chain Reaction (RT-PCR). CB(2) mRNA was ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01122-0
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abstract：:Local anesthetics bind to dopamine transporters and inhibit dopamine uptake in rodent brain. Additionally, local anesthetics are self-administered in rhesus monkeys. The present study determined binding affinities of cocaine and five local anesthetics at dopamine transporters in rhesus monkey brain, and compared bindi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00967-4
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abstract：:In slices of rat occipital cortex preincubated with 3H-noradrenaline, methioine-enkephalin diminished the overflow of tritium evoked by electrical field stimulation or by 20 mM potassium. The effect was not modified by phentolamine, but was antagonized by naloxone. Giver alone, naloxone slightly increased the potassiu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90343-5
更新日期：1976-08-01 00:00:00
abstract：:The human cholecystokinin B (CCKB) receptor has been isolated from a human temporal cortex cDNA library. Transient transfection of the receptor into COS-M6 cells resulted in high specific binding of 125I-sulphated CCK-8 labelled with Bolton and Hunter Reagent (KD = 31 pM). Competition experiments yielded the expected ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90117-1
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abstract：:The effects of a serotonin (5-HT) releasing drug, p-chloroamphetamine, on plasma glucose levels were investigated in rats. p-Chloroamphetamine elicited a significant hyperglycemia. The hyperglycemic effects of p-chloroamphetamine were completely prevented by the 5-HT synthesis inhibitor, p-chlorophenylalanine. Prior a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1998-10-23 00:00:00
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journal_title：European journal of pharmacology
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doi：10.1016/j.ejphar.2004.10.028
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90521-1
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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doi：10.1016/j.ejphar.2006.11.049
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90054-0
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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：10.1016/0922-4106(91)90114-w
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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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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/j.ejphar.2011.01.006
更新日期：2011-03-11 00:00:00
abstract：:Metformin administration has been reported to influence the carotid intima-media thickness (CIMT) in humans. However, since previously conducted studies have yielded inconsistent results, the exact effect of metformin on CIMT remains unclear. Causes that could lead to inconsistency in reported research could be the du...
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90315-4
更新日期：1989-12-19 00:00:00
abstract：:The effect of morphine on the capsaicin-induced cough reflex was studied in mu 1-opioid receptor-deficient CXBK mice. There was no significant difference between the morphine-induced antitussive effect in CXBK mice and C57BL/6 mice, a progenitor strain. Furthermore, the antitussive effects of morphine in both the CXBK...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90553-t
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：2019-11-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90184-4
更新日期：1977-03-07 00:00:00
abstract：:Recent studies suggest that endocannabinoid signaling is modulated by 17β-estradiol (17Eβ) however it is unclear if this applies to the cardiovascular actions of anandamide, a major endocannabinoid. This study examined the in vitro effects of 17Eβ on vasorelaxation to anandamide in myograph-mounted small mesenteric ar...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.01.002
更新日期：2013-02-15 00:00:00
