Molecular signalling of a novel curcumin derivative versus Tadalafil in erectile dysfunction

Abstract

The efficacy of a novel curcumin derivative (NCD) versus tadalafil in erectile signalling was assessed. Ten control male rats and 50 diabetic male rats were used and divided into the following: diabetic (DM), curcumin (CURC), NCD, tadalafil and NCD combined with tadalafil rat groups. Cavernous tissue gene expression of heme oxygenase-1 (HO-1), Nrf2, NF-B and p38, enzyme activities of heme oxygenase (HO) and nitric oxide synthase (NOS), cGMP and intracavernosal pressure (ICP)/mean arterial pressure (MAP) were assessed. Results showed that 12 weeks after induction of diabetes, erectile dysfunction (ED) was confirmed by the significant decrease in ICP/MAP, a significant decrease in cGMP, NOS, HO enzyme activities, a significant decrease in HO-1 gene and a significant increase in NF-Ҡβ, p38 genes. Administration of all therapeutic interventions led to a significant increase in ICP/MAP, cGMP levels, a significant increase in HO-1 and NOS enzymes, a significant increase in HO-1, and Nrf2 gene expression, and a significant decrease in NF-Ҡβ, p38 gene expression. NCD or its combination with tadalafil showed significant superiority and more prolonged duration of action. In conclusion, a tendency was observed that CURC and NCD have high efficacy and more prolonged duration of action in enhancing erectile function.

Efficacy and safety of an herbal formula (KBMSI-2) in the treatment of erectile dysfunction: A preliminary clinical study

“…Curcumin may also be involved in the upregulation of gene expression of eNOS, nNOS, and nuclear transcription factor-erythroid 2, and the downregulation of NF-κβ, p38, and inducible NOS gene expression [2526]. In a clinical study using a novel curcumin derivative, in combination with tadalafil or sildenafil, EF was significantly enhanced and a prolonged duration of action was observed [2728]. Allantoin is contained in D. tenuipes as a major active compound.…”

Nanotechnology as a tool to advance research and treatment of non-oncologic urogenital diseases

“…62 Several studies in animal models have demonstrated the potential of oral administration of curcumin (a naturally occurring compound, which has anti-inflammatory, anti-oxidative stress, and anti-catabolic activity) to treat ED associated with diabetes. 63–66 However, clinical translation of curcumin-based therapies has been limited because of its low oral bioavailability, poor aqueous solubility, and rapid degradation. Some of these shortcomings could be mitigated when curcumin is encapsulated into a silane-hydrogel nanoparticle (curcumin-nanoparticle) which allows slow and sustained transdermal delivery of curcumin, thereby avoiding first-pass metabolism.…”

Advances in Nanoparticle Delivery System for Erectile Dysfunction: An Updated Review

“… 70 , 73 , 74 , 77 To improve the efficiency of curcumin, water-soluble curcumin derivatives have been developed. 76 , 78 Abdel Aziz et.al 76 investigated a novel water-soluble curcumin derivative. In their study, oral administration of synthesized water long-acting CURC derivative (10 mg/kg) resulted in a significant improvement in the activity of cavernous tissue heme oxygenase enzyme-1 (HO- 1) and cGMP, and prolonged duration of action compared to sildenafil (4 mg/kg), pure CURC (10 mg/kg), and water-soluble long-acting CURC derivative (2 mg/kg).…”

“…Intake of water-soluble curcumin derivatives resulted in improvement of erectile function was confirmed by a significant increase in ICP. Another research by Abdel Aziz et al 78 compared the efficacy of novel curcumin derivative (NCD) with that of natural curcumin (CURC) and tadalafil (Cialis) in an animal diabetic model of ED. The study involved 60 adult male albino rats, of which 10 were used for control and 50 were diabetic rats caused by a single intraperitoneal injection of streptozotocin (65 mg/kg body weight).…”

“…The study concluded that novel curcumin derivative is more effective than pure curcumin and tadalafil. 78 However, there are no published clinical studies to support the efficacy and safety of curcumin derivatives in the mitigation of ED. Therefore, clinical trials are essential in the development of effective and safe medication.…”