Objectives: To study the effects of CPU 86017, a berberine derivative, and its four enantiomers on thyrotoxicosis-induced oxidative stress and the excessive endothelin-1 system in rat testes.
Methods: Adult male SD rats were given high-dose L-thyroxin (0.2 mg/kg subcutaneously) once daily for 10 days to develop thyrotoxicosis. Subsets of the rats were treated with CPU 86017 or its four enantiomers (SR, SS, RS, and RR) once daily from day 6 to day 10. The alterations of redox, nitric oxide synthase, and endothelin-1 system in testes were examined by spectrophotometry and reverse transcriptase-polymerase chain reaction assay.
Results: After 10 days of high-dose L-thyroxin administration, increased mRNA expression of prepro-endothelin-1 and endothelin-converting enzyme was observed in the rat testes, accompanied by an elevated inducible nitric oxide synthase activity and oxidative stress. CPU 86017 and its enantiomer SR significantly improved these abnormalities.
Conclusions: High-dose L-thyroxin results in an overactive endothelin-1 system and oxidative stress in adult rat testis. CPU 86017 and its enantiomer SR suppressed the excessive ET-1 system by improving oxidative stress, and SR exhibited more potent efficacy than CPU 86017 and other enantiomers.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.urology.2006.03.068 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Apocynin and raisanberine alleviate intermittent hypoxia induced abnormal StAR and 3β-HSD and low testosterone by suppressing endoplasmic reticulum stress and activated p66Shc in rat testes.
Reprod Toxicol
April 2013
College of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
We hypothesized that hypoxia induced testicular damage is mediated by an activated NADPH oxidase (NOX), therefore, APO (apocynin) an inhibitor of NOX and raisanberine (RS), a calcium influx inhibitor were tested if they could attenuate hypoxic toxicity to the testis. Male Sprague-Dawley rats were exposed to hypoxia (10±0.5% O₂) for 17d and intervened with APO and RS in the last 6d.
View Article and Find Full Text PDFRaisanberine protected pulmonary arterial rings and cardiac myocytes of rats against hypoxia injury by suppressing NADPH oxidase and calcium influx.
Acta Pharmacol Sin
May 2012
Research Division of Pharmacology, China Pharmaceutical University, Nanjing, China.
Aim: To investigate the protection of pulmonary arterial rings and cardiac myocytes of rats by raisanberine (RS), a derivative of berberine, against hypoxia injury and to elucidate the action mechanisms.
Methods: Adult SD rats were exposed to intermittent hypoxia for 17 d or 28 d. The pulmonary arterial rings were isolated and vascular activity was measured using a transducer and computer-aided system.
CPU86017-RS attenuate hypoxia-induced testicular dysfunction in mice by normalizing androgen biosynthesis genes and pro-inflammatory cytokines.
Acta Pharmacol Sin
April 2012
Faculty of Pharmacy, China Pharmaceutical University, Nanjing, China.
Aim: Downregulation of androgen biosynthesis genes StAR (steroidogenic acute regulatory) and 3β-HSD (3β-hydroxysteroid dehydrogenase) contributes to low testosterone levels in hypoxic mice and is possibly related to increased expression of pro-inflammatory cytokines in the testis. The aim of this study is to investigate the effects of CPU86017-RS that block Ca(2+) influx on hypoxia-induced testis insult in mice.
Methods: Male ICR mice were divided into 5 groups: control group, hypoxia group, hypoxia group treated with nifedipine (10 mg/kg), hypoxia groups treated with CPU86017-RS (60 or 80 mg/kg).
Endoplasmic reticulum stress mediating downregulated StAR and 3-beta-HSD and low plasma testosterone caused by hypoxia is attenuated by CPU86017-RS and nifedipine.
J Biomed Sci
January 2012
Faculty of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Background: Hypoxia exposure initiates low serum testosterone levels that could be attributed to downregulated androgen biosynthesizing genes such as StAR (steroidogenic acute regulatory protein) and 3-beta-HSD (3-beta-hydroxysteroid dehydrogenase) in the testis. It was hypothesized that these abnormalities in the testis by hypoxia are associated with oxidative stress and an increase in chaperones of endoplasmic reticulum stress (ER stress) and ER stress could be modulated by a reduction in calcium influx. Therefore, we verify that if an application of CPU86017-RS (simplified as RS, a derivative to berberine) could alleviate the ER stress and depressed gene expressions of StAR and 3-beta-HSD, and low plasma testosterone in hypoxic rats, these were compared with those of nifedipine.
View Article and Find Full Text PDFAim: To investigate whether CPU86017, a berberine derivative, attenuates heart failure by blocking calcium influx and exerting its antioxidant activity.
Methods: Myocardial infarction was induced in male Sprague-Dawley rats for 17 d followed by isoproterenol (ISO) (5 mg/kg, sc) treatment for 5 d to reduce cardiac function. The rats were divided into 5 groups: sham operation, myocardial infarction (MI), MI plus ISO, and co-treated (in mg/kg, po) with either propranolol (PRO, 10) or CPU86017 (80).
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!