Novel water-soluble curcumin derivative mediating erectile signaling

J Sex Med. 2010 Aug;7(8):2714-22. doi: 10.1111/j.1743-6109.2009.01543.x. Epub 2009 Oct 19.

Abstract

Introduction: Curcumin is an inducer of heme oxygenase enzyme-1 (HO-1) that is involved in erectile signaling via elevating cyclic guanosine monophosphate (cGMP)levels.

Aim: To assess the effect of oral administration of a water-soluble long-acting curcumin derivative on erectile signaling.

Methods: Two hundred and thirty six male white albino rats were divided into four groups; group 1 (N = 20) includes control. Group 2 (N = 72) was equally divided into four subgroups; subgroup 1 received pure curcumin (10 mg/kg), subgroup 2 received the long-acting curcumin derivative (2 mg/kg), subgroup 3 received the long-acting curcumin derivative (10 mg/kg), and subgroup 4 received sildenafil (4 mg/kg). Subgroups were sacrificed after the first, second, and third hour. Group 3 (N = 72) was equally divided into the same four subgroups already mentioned and were sacrificed after 24 hours, 48 hours, and 1 week. Group 4 (N = 72) was subjected to intracavernosal pressure (ICP) measurements 1 hour following oral administration of the same previous doses in the same rat subgroups.

Main outcome measure: Cavernous tissue HO enzyme activity, cGMP, and ICP.

Results: In group 2, there was a significant progressive maintained elevation of HO activity and cGMP tissue levels starting from the first hour in subgroups 3 and 4, whereas, the rise in HO activity and cGMP started from second hour regarding the other rat subgroups. Sildenafil effect decreased after 3 hours. In group 3, there was a significant maintained elevation of HO activity and cGMP tissue levels extended to 1 week as compared to controls for all rat subgroups that received both forms of curcumin. In group 4, long-acting curcumin derivative exhibited more significant potentiation of intracavernosal pressure as compared to control and to the pure curcumin.

Conclusion: Water-soluble long-acting curcumin derivative could mediate erectile function via upregulating cavernous tissue cGMP.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Blood Pressure / drug effects
  • Curcumin / analogs & derivatives*
  • Curcumin / pharmacology*
  • Cyclic GMP / metabolism
  • Delayed-Action Preparations
  • Dose-Response Relationship, Drug
  • Enzyme Induction / drug effects
  • Heme Oxygenase-1 / metabolism*
  • Injections, Intraperitoneal
  • Male
  • Penile Erection / drug effects*
  • Penis / drug effects
  • Phosphodiesterase 5 Inhibitors / pharmacology
  • Phytotherapy*
  • Piperazines / pharmacology
  • Plant Extracts / pharmacology*
  • Purines / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Signal Transduction / drug effects*
  • Sildenafil Citrate
  • Sulfones / pharmacology

Substances

  • Delayed-Action Preparations
  • Phosphodiesterase 5 Inhibitors
  • Piperazines
  • Plant Extracts
  • Purines
  • Sulfones
  • Sildenafil Citrate
  • Heme Oxygenase-1
  • Cyclic GMP
  • Curcumin