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Icariin AND sildenafil

Tao-Hua Lan, Xiao-Ling Chen, Yun-Shan Wu, Hui-Liang Qiu, Jun-Zhe Li, Xin-Min Ruan, Dan-Ping Xu, Dong-Qun Lin
Pulmonary arterial hypertension (PAH) is a chronic progressive disease which leads to elevated pulmonary arterial pressure and right heart failure. 3,7-Bis(2-hydroxyethyl)icaritin (ICT), an icariin derivatives, was reported to have potent inhibitory activity on phosphodiesterase type 5 (PDE5) which plays a crucial role in the pathogenesis of PAH. The present study was designed to investigate the effects of ICT on monocrotaline (MCT)-induced PAH rat model and reveal the underlying mechanism. MCT-induced PAH rat models were established with intragastric administration of ICT (10, 20, 40mg/kg/d), Icariin (ICA) (40mg/kg/d) and Sildenafil (25mg/kg/d)...
April 14, 2018: European Journal of Pharmacology
Y Xu, H Xin, Y Wu, R Guan, H Lei, X Fu, Z Xin, Y Yang
The commonly utilized phosphodiesterase type 5 inhibitors do not lead to satisfactory penile erection after radical prostatectomy mainly because of insufficient nitric oxide drive from the damaged cavernous nerves. The aim of this study was to assess the efficacy and mechanisms of icariin in combination with daily sildenafil on neurogenic erectile dysfunction and penile atrophy in a rat model of bilateral cavernous nerves injury. Sixty male Sprague-Dawley rats injected with 5-ethynyl-2-deoxyuridine (50 mg/kg) at postnatal day 1 for the purpose of tracking endogenous stem cells in penis...
May 2017: Andrology
Lizhi Fu, Fenfen Li, Antje Bruckbauer, Qiang Cao, Xin Cui, Rui Wu, Hang Shi, Bingzhong Xue, Michael B Zemel
PURPOSE: Leucine activates SIRT1/AMP-activated protein kinase (AMPK) signaling and markedly potentiates the effects of other sirtuin and AMPK activators on insulin signaling and lipid metabolism. Phosphodiesterase 5 inhibition increases nitric oxide-cGMP signaling, which in turn exhibits a positive feedback loop with both SIRT1 and AMPK, thus amplifying peroxisome proliferator-activated receptor γ co-activator α (PGC1α)-mediated effects. METHODS: We evaluated potential synergy between leucine and PDE5i on insulin sensitivity and lipid metabolism in vitro and in diet-induced obese (DIO) mice...
2015: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy
Véronique Gilard, Stéphane Balayssac, Aurélie Tinaugus, Nathalie Martins, Robert Martino, Myriam Malet-Martino
One hundred and fifty dietary supplements (DS) marketed to increase sexual performance were analyzed. All these formulations were claimed to contain only natural compounds, plant extracts and/or vitamins. (1)H NMR spectroscopy was used for detecting the presence of adulterants and for their identification and quantification. Mass spectrometry was used as a complementary method for confirming the chemical structures. 61% of DS were adulterated with phosphodiesterase-5 inhibitors (PDE-5i) (27% with the PDE-5i medicines sildenafil, tadalafil and vardenafil, and 34% with their structurally modified analogues)...
January 2015: Journal of Pharmaceutical and Biomedical Analysis
Feng Jin, Qi-Hai Gong, Ya-Sha Xu, Li-Na Wang, Hai Jin, Fei Li, Li-Sheng Li, Yue-Ming Ma, Jing-Shan Shi
Phosphodiesterase-5 (PDE5) inhibitors are predominantly used in the treatment of erectile dysfunction, and have been recently shown to have a potential therapeutic effect for the treatment of Alzheimer's disease (AD) through stimulation of nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) signalling by elevating cGMP, which is a secondary messenger involved in processes of neuroplasticity. In the present study, the effects of a PDE5 inhibitor, icarrin (ICA), on learning and memory as well as the pathological features in APP/PS1 transgenic AD mice were investigated...
June 2014: International Journal of Neuropsychopharmacology
Sooyeun Lee, So-young Kang, Dajeong Ji, Seungkyung Baeck, Sangki Lee, Seung Min Oh, Kyu Hyuck Chung
The chemical castration law, which targets child molesters with recidivism, was introduced in Korea in 2011. For this, leuprolide, a gonadotropin-releasing hormone agonist, is used to decrease testosterone production and suppress libido. In order to achieve efficient law enforcement, it is necessary to monitor intentional ingestion of drugs that antagonize the effect of leuprolide. Therefore, an analytical method for the simultaneous detection of mirodenafil, sildenafil, tadalafil, udenafil, vardenafil, icariin, alprostadil, and yohimbine, which are the major impotence treatment drugs, legitimately or otherwise, in Korea, as well as their selected metabolites, in human urine was established and validated using liquid chromatography-tandem mass spectrometry (LC-MS/MS)...
April 2013: Analytical and Bioanalytical Chemistry
Tao Liu, Xin-cheng Qin, Wei-ren Li, Feng Zhou, Guang-yong Li, Hua Xin, Yan-qing Gong, Zhong-cheng Xin
OBJECTIVE: To investigate the effects of icariin and icariside II on eNOS expression and NOS activity in endothelial cells and possible mechanisms using EGFR over-expressed porcine aorta endothelial (PAE) cell line. METHODS: The EGFR gene was transfected into PAE cells and genetic stable cell line (PAE-EGFR) was selected. 12.5 μmol/L of icariin and of icariside II were used to treat the PAE and PAE-EGFR cells respectively for 48 h, the eNOS expression in each group was observed...
August 18, 2011: Beijing da Xue Xue Bao. Yi Xue Ban, Journal of Peking University. Health Sciences
J Zhang, Y-B Wang, C-G Ma, T Liu, W-R Li, Y-Q Gong, Z-C Xin
The aim of this study was to explore the effects and mechanisms of Icarisid II (ICA-II) on enhancing the cellular cGMP in rat corpus cavernosum tissue (RCCT). Diabetes mellitus Wistar rats were induced by streptozotocin, and diabetic ED rats were selected for the RCCT culture by apomorphine. ICA-II was extracted and purified from Icariin (ICA) by enzymatic method. The RCCT was treated with ICA-II, ICA and Sildenafil at different concentrations. cGMP and nitric oxide synthase (NOS) activities were checked respectively by enzyme immunoassay...
May 2012: Andrologia
Hwa-mi Lee, Bong Jin Lee
The commercial success of synthetic phosphodiesterase-5 (PDE-5) inhibitors (viz. sildenafil, vardenafil and tadalafil) for erectile dysfunction (ED) has led to their widespread use as adulterants in dietary supplements (DSs). Reports on adulteration by ED drugs or their analogues in DSs suggest they may cause a serious threat to human health. The problem is becoming more complex as hidden and structurally modified analogues are continuously being reported. To analyse known drugs and their analogues, three commonly used PDE-5 inhibitors, naturally existing icariin and yohimbin, and their 19 analogues were analyzed in this study...
April 2011: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
Alan W Shindel, Zhong-Chen Xin, Guiting Lin, Thomas M Fandel, Yun-Ching Huang, Lia Banie, Benjamin N Breyer, Maurice M Garcia, Ching-Shwun Lin, Tom F Lue
INTRODUCTION: Epimedium species (aka horny goat weed) have been utilized for the treatment of erectile dysfunction in Traditional Chinese Medicine for many years. Icariin (ICA) is the active moiety of Epimedium species. AIM: To evaluate the penile hemodynamic and tissue effects of ICA in cavernous nerve injured rats. We also studied the in vitro effects of ICA on cultured pelvic ganglia. METHODS: Rats were subjected to cavernous nerve injury and subsequently treated for 4 weeks with daily gavage feedings of a placebo solution of normal saline and Dimethyl sulfoxide (DMSO) vs...
April 2010: Journal of Sexual Medicine
Mario Dell'Agli, Germana V Galli, Esther Dal Cero, Federica Belluti, Riccardo Matera, Elisa Zironi, Giampiero Pagliuca, Enrica Bosisio
Plant extracts traditionally used for male impotence (Tribulus terrestris, Ferula hermonis, Epimedium brevicornum, Cinnamomum cassia), and the individual compounds cinnamaldehyde, ferutinin, and icariin, were screened against phosphodiesterase-5A1 (PDE5A1) activity. Human recombinant PDE5A1 was used as the enzyme source. Only E. brevicornum extract (80% inhibition at 50 microg/mL) and its active principle icariin (1) (IC50 5.9 microM) were active. To improve its inhibitory activity, 1 was subjected to various structural modifications...
September 2008: Journal of Natural Products
Zhaojian Jiang, Benrong Hu, Jialing Wang, Qiang Tang, Yan Tan, Jizhou Xiang, Juyan Liu
To further investigate the mechanisms of action of icariin (ICA), we assessed the effects of ICA on the in vitro formation of cGMP and cAMP in isolated rabbit corpus cavernosum. Isolated segments of rabbit corpus cavernosum were exposed to increasing concentrations of ICA and the dose-dependent accumulation of cGMP and cAMP was determined in the tissues samples by means of 125I radioimmunoassay. Responses of the isolated tissues preparations to ICA were compared with those obtained with the reference compounds sildenafil (Sild)...
2006: Journal of Huazhong University of Science and Technology. Medical Sciences
Long Tian, Zhong-cheng Xin, Yi-ming Yuan, Jie Fu, Wu-jiang Liu, Ling-long Wang
OBJECTIVE: To realize the effect of icariin on erectile function of penis. METHODS: After the cavernous nerve (CN) of rat was isolated unilaterally, the corpora cavernosa (CC) and right carotid artery were exposed. A 26G needle catheter was inserted into the right CC to monitor the intracavernous pressure (ICP), and another 26G needle catheter was inserted into the left CC for drug administration. Another catheter was placed into the carotid artery to monitor mean systematic arterial blood press (MBp)...
January 17, 2004: Zhonghua Yi Xue za Zhi [Chinese medical journal]
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