scholarly journals Phenanthrenes from Eulophia macrobulbon as Novel Phosphodiesterase-5 Inhibitors

2017 ◽  
Vol 12 (1) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Prapapan Temkitthawon ◽  
Kanokwan Changwichit ◽  
Nantaka Khorana ◽  
Jarupa Viyoch ◽  
Khanit Suwanborirux ◽  
...  
Keyword(s):  
Pulmonary Hypertension ◽  
Erectile Dysfunction ◽  
Chemical Constituents ◽  
Pde5 Inhibitor ◽  
Pde5 Inhibitors ◽  
New Class ◽  
Phosphodiesterase 5 Inhibitors ◽  
Phosphodiesterase 5

Phosphodiesterase 5 (PDE5) inhibitors can be used for the treatment of erectile dysfunction and pulmonary hypertension. In order to search for new leads of PDE5 inhibitors, we investigated the chemical constituents of the tubers of Eulophia macrobulbon (E.C. Parish & Rchb. f) Hook. f A new phenanthrene, 9,10-dihydro-4-(4′-hydroxybenzyl)-2,5-dimethoxyphenanthrene-1,7-diol (1) and three known phenanthrenes i.e., 1-(4′-hydroxybenzyl)-4,8-dimethoxyphenanthrene-2,7-diol (2), (9,10-dihydro-2,5-dimethoxyphenanthrene-1,7-diol (3) and 1,5,7-trimethoxyphenanthrene-2,6-diol) (4) were isolated. Among these, 2 was the most potent PDE5 inhibitor (IC50 =1.67±0.54 μM) evaluated by the [3H]cGMP radioassay method, whereas 1 showed mild activity (IC50 = 62.3±3.3 μM). Their inhibitory selectivities against PDE5 over PDE6 were also studied. This study suggests phenanthrenes as a new class of PDE5 inhibitors.

Phosphodiesterase 5 Inhibitors for Erectile Dysfunction

2005 ◽  
Vol 39 (7-8) ◽  
pp. 1286-1295 ◽  
Author(s):  
Stephen M Setter ◽  
Jason L Iltz ◽  
Jack E Fincham ◽  
R Keith Campbell ◽  
Danial E Baker
Keyword(s):  
Clinical Trial ◽  
Erectile Dysfunction ◽  
Data Extraction ◽  
Pde5 Inhibitor ◽  
Clinical Trial Data ◽  
Research Review ◽  
Pde5 Inhibitors ◽  
Search Terms ◽  
Review Articles ◽  
Phosphodiesterase 5

OBJECTIVE To review the pharmacologic and clinical trial data of the Food and Drug Administration–approved phosphodiesterase 5 (PDE5) inhibitors for the treatment of erectile dysfunction (ED). DATA SOURCES Primary research and review articles were identified through a search of ScienceDirect, PubMed/MEDLINE, and International Pharmaceutical Abstracts (1990–August 2004). The following search terms were used in the Medicine Dentistry and Pharmacology, Toxicology, and Pharmaceutical Sciences subcategories: phosphodiesterase 5 inhibitor, PDE5 inhibitor, erectile dysfunction, sildenafil, vardenafil, tadalafil, prostatectomy, and diabetes. Web of Science (1990–August 2004) was used to search for additional abstracts using the same search terms as above. The package inserts for sildenafil, vardenafil, and tadalafil were also consulted. STUDY SELECTION AND DATA EXTRACTION All identified research, review articles, and abstracts were assessed for relevance, and all relevant information was included. Priority was given to the primary medical literature and clinical trial reports. DATA SYNTHESIS ED is a common disorder in males with increased prevalence associated with age and presence of cardiovascular disease, prostatectomy, or diabetes mellitus. Sildenafil, vardenafil, and tadalafil are selective PDE5 inhibitors currently available for treatment of ED. Their pharmacology and pharmacokinetics vary slightly, but with potentially important clinical differences in duration of activity; all have similar clinical efficacy and adverse effect profiles in patients with ED of various causes. CONCLUSIONS Sildenafil, vardenafil, and tadalafil are safe and effective PDE5 inhibitors for the treatment of ED.

Cutaneous Reaction to Drugs Used for Erectile Dysfunction: Case Report and Review of the Literature

2006 ◽  
Vol 10 (3) ◽  
pp. 128-130 ◽  
Author(s):  
Renee A. Beach ◽  
Frank Murphy ◽  
Ronald B. Vender
Keyword(s):  
Erectile Dysfunction ◽  
Drug Eruption ◽  
Pde5 Inhibitor ◽  
Sexual Performance ◽  
Pde5 Inhibitors ◽  
Fixed Drug Eruption ◽  
The Past ◽  
Fixed Drug ◽  
Performance Satisfaction ◽  
Phosphodiesterase 5

Background: In the past 9 years, drugs for erectile dysfunction (ED) have been increasingly prescribed for men with erectile difficulty. These drugs, phosphodiesterase 5 (PDE5) inhibitors, help men with ED obtain and sustain an erection, improving both sexual function and sexual performance satisfaction. However, these drugs contain side effects. Objectives: A 56-year-old man developed an erythematous, circle-shaped lesion on his penis. The lesion was recurrent, with evidence of desquamation. The aim was to determine the source of the recurrent lesion based on its morphology and the patient's verbal history. Results: A clinical diagnosis of fixed drug eruption owing to use of the PDE5 inhibitor tadalafil (Cialis) was made. He was not rechallenged with the drug. However, he experienced a subsequent recurrence of the eruption on inadvertent rechallenge. Conclusions: We believe this case to be the first report of this type of reaction owing to tadalafil. Therefore, fixed drug eruption is a newly observable side effect of this drug.

Phosphodiesterase 5 inhibitors and erectile dysfunction

2008 ◽  
Vol 18 (1) ◽  
pp. 21-33 ◽  
Author(s):  
Peter Sandner ◽  
Niels Svenstrup ◽  
Hanna Tinel ◽  
Helmut Haning ◽  
Erwin Bischoff
Keyword(s):  
Erectile Dysfunction ◽  
Phosphodiesterase 5 Inhibitors ◽  
Phosphodiesterase 5

scholarly journals Combination of phosphodiesterase‐5‐inhibitors and beta blockers improves experimental portal hypertension and erectile dysfunction

2020 ◽  
Vol 40 (9) ◽  
pp. 2228-2241 ◽  
Author(s):  
Frank E. Uschner ◽  
Kathleen Glückert ◽  
Rafael Paternostro ◽  
Thorsten Gnad ◽  
Robert Schierwagen ◽  
...  
Keyword(s):  
Erectile Dysfunction ◽  
Portal Hypertension ◽  
Beta Blockers ◽  
Phosphodiesterase 5 Inhibitors ◽  
Phosphodiesterase 5

scholarly journals Audiometry Results and TEOAE and DPOAE Amplitudes in Men Taking a Phosphodiesterase Type 5 Inhibitor for Erectile Dysfunction

2017 ◽  
Vol 96 (7) ◽  
pp. E34-E39 ◽  
Author(s):  
Sertan Öntepeli ◽  
Nuray Bayar Muluk ◽  
Devrim Tuğlu ◽  
Timuçin Şipal
Keyword(s):  
Erectile Dysfunction ◽  
Otoacoustic Emissions ◽  
Pde5 Inhibitor ◽  
Post Treatment ◽  
Guanosine Monophosphate ◽  
Pde5 Inhibitors ◽  
Cochlear Blood Flow ◽  
Distortion Product ◽  
Phosphodiesterase Type 5 Inhibitor ◽  
Phosphodiesterase Type

We conducted a prospective study of transient evoked otoacoustic emissions (TEOAEs) and distortion-product otoacoustic emissions (DPOAEs) in men who were taking an oral phosphodiesterase type 5 (PDE5) inhibitor for erectile dysfunction. Our study group was made up of 30 men (60 ears), aged 34 to 60 years (mean: 50.9). They were randomly divided into three groups; 10 men were given sildenafil (Viagra) at 50 mg twice a week, 10 were given tadalafil (Cialis) at 20 mg twice a week, and 10 were given vardenafil (Levitra) at 20 mg twice a week. All patients took their drug for 3 weeks, for a total of 6 tablets for each patient. Audiometric tests and TEOAE and DPOAE measurements were performed before and after treatment. Post-treatment audiometry demonstrated improvement in hearing in all three groups. However, post-treatment TEOAE amplitudes and DPOAE amplitudes differed among the three groups; they were significantly higher in the sildenafil group at 1.0 kHz and the same in the tadalafil group; in the vardenafil group, the DPOAE amplitude was significantly lower at 3.0 kHz while there was no change in the TEOAE amplitude. We speculate that the possible mechanism for these findings is that PDE5 inhibitors block degradation of cyclic guanosine monophosphate (cGMP) and induce dilation of the cochlear microcirculation, resulting in an increase in cochlear blood flow. We also believe that the decrease in DPOAE amplitudes at 3.0 kHz seen in the vardenafil group may be related to an accumulation of nitric oxide/cGMP complex, which is toxic to the cochlea; however, since there was no change in TEOAE amplitude in the vardenafil group, this influence may be minimal. Further studies are needed to obtain a more comprehensive assessment of the effects of PDE5 inhibitors on hearing with the use of higher doses and longer durations of therapy.

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