Background: Glycation is a non enzymatic reaction initiated by the primary addition of sugar to the amino groups of proteins.In the early stage of glyction, the synthesis of intermediates leading to formation of Amadori compounds occurs. In the late stage, advanced glycation end product (AGE) are irreversibly formed after a Complex cascade of reaction.Objective: Survey effect of Papaverine on Human Serum Albumin Glycation.Methods: In this study HSA incubate with Glucose and different papaverine concentration for 42 days at 37oC. also HSA incubate alone (control sample), with Glucose (glycated sample) and with different papaverine concentration (without Glucose) respectively under the same conditions. Then samples survey with circular dichroism fluorescence and UV spectroscopy.Results: HSA glycation increase in proportion to papaverine concentration. samples contain Glucose and papaverine show more change in secondary structure, free amino groups and AGE fluorescence in relation to glycated and control samples.Conclusion: In glycatedα helix and b sheet show 5.7% decrease and 3.1% increase in comparison to control respectively. Glycated show 14.2% fluorescence more than control. Free lys number in glycated show 8% less than control sample. All this cases show more change in samples which contain papaverine and Glucose. Seem papaverine change HSA and cause more lys contact with sugar thus papaverine increase glycation.

Introduction: Glycation is a non enzymatic reaction initiated by the primary addition of sugar to the amino groups of proteins. In the early stage of glycation, the synthesis of intermediates leading to formation of Amadori compounds occurs. In the late stage, advanced glycation end product (AGE) is irrevesibly formed after a complex cascade of reactions. Glycation also affect diabetes-related complications physiological aging and neurodegenerative diseases such as alzeimers.Materials & Methodsi In this study, HAS incubation with glucose and different concentration of papaverine for 42 days at 37oC. as well as HSA incubation alone (control sample), with glucose (glycated sample)were treated respectively under the same conditions. After 42 days, the samples by use of circular dichroism, fluorescence and UV spectroscopy were investigated.Findings: HSA glycation increases alon with rising of papaverine concentration. Samples containing papaverine showed more changes in secondary structure, free amino groups and AGE fluorescence in relation to glycated and control samples. Discussion & Conclusion: In glycated helix and sheet a 5.7% decrease and 3.1% increase were seen in comparison to the control respectively. Glycated showed 14.2% fluorescence more than the control. Free lys number in glycated showed 8% less in relation to the control. All this cases showed more changes in samples which contained papaverine. HSA absorb in presence of papaverine showed that papaverine cause more lys contact with sugar and an increase in glycation.

Opium mixture serves as a vital source of alkaloids, including significant medicinal compounds used in the pharmaceutical industry. One such compound is papaverine (6), a benzylisoquinolinic alkaloid found in opium mixture, possessing distinct medicinal properties. This article addresses the limitations associated with extracting substances from natural compounds by focusing on the synthesis of papaverine in four comprehensive steps. The synthetic route employs 2-(4,3-dimethoxyphenyl) acetic acid (1), which undergoes transformation to yield methyl 2-(4,3-dimethoxyphenyl) acetate (2). Through the binding of compound (2) with commercially available 2-(4,3-dimethoxyphenyl) ethane amine (3), amide (4) is obtained. Subsequently, ring closure of compound (4) is efficiently achieved using polyphosphoric acid (PPA) in refluxing toluene, leading to the formation of 1-(4,3-dimethoxy-benzyl)-7,6-dimethoxy-4,3-dihydroisoquinoline (5). The next crucial step involves the hydrogenation of compound (5) with Pd/C in a water-solvent medium, successfully yielding the desired product, papaverine (6), with an impressive efficiency of 58.7%. Characterization of the formed products is carried out using FTIR, 1H NMR, 13C NMR, and Mass spectrometry techniques, confirming their chemical identities. By developing a synthetic approach to produce papaverine, this study offers valuable insights into the efficient synthesis of this important medicinal compound, potentially paving the way for its widespread application in the pharmaceutical industry.

Purpose: To analyze the predictive factors causing ischemic priapism following penile doppler ultrasonography (PDU) with intracavernosal papaverine injection Materials and methods: Medical records of 467 patients who underwent PDU examination following intracavernosal papaverine injection for erectile dysfunction (ED) between 2009 and 2017 were retrospectively reviewed. Patients with hematological disease anamnesis, patients taking phosphodiesterase-5 inhibitor, patients with intracavernosal injection therapy anamnesis, and patients who underwent PDU with other intracavernosal vasodilator drugs other than papaverine were excluded from the study. The remaining 268 patients were divided into two groups as priapism (38 patients) and non-priapism (230 patients). The groups were compared in terms of demographic data, American Society of Anesthesiologists (ASA) score, comorbidities, international index of erectile dysfunction (IIEF) score, and PDU results. The significant parameters were analyzed with binary logistic regression analysis. The receiver operating analysis was used to obtain cut-off, sensitivity, and specificity values for the independent predictive factors. Results: The age, ASA score, diabetes mellitus, IIEF score, duration of ED, peak arterial, and peak end diastolic venous flow values in the 20th minute were significantly different in the two groups (p < 0. 001). Binary logistic regression analysis found age, duration of erectile dysfunction, IIEF score, peak arterial flow, and venous flow rate in the 20th minute were predictive variables for the occurrence of priapism. Conclusion: Young patients, patients with good IIEF score, patients with ED for a short time, and patients with normal peak arterial and venous flows are more prone to developing post-papaverine ischemic priapism.

Introduction: Telomere maintenance is essential for the continued proliferation of dividing cells, and is implicated in chromosome stability and cell immortalization. Telomerase activity, that allows cancer cells to maintain their telomeric DNA for an indefinite replicative capacity, is an attractive target against cancer. A well known benzylisoquinoline alkaloid, papaverine, we focused on to evaluate its antiproliferaive effects on breast cancer MCF7 cells.Methods: Cytotoxicity of the commercially available pure compound papaverine HCl (Sigma) was determined by MTT assay. A modified quantitative real-time polymerase chain reaction (PCR) -based telomerase repeat amplification protocol (TRAP) was used to estimate relative telomerase activity in papaverine-treated cells in comparison with the untreated control cells. Relative expression level of the catalytic subunit of telomerase (hTERT) gene was estimated using real time reverse transcription-PCR (RT-PCR).Results: IC50 concentration of papaverine after 48 hours treatment was measured to 120 micromolar At this concentration telomerase activity showed a considerable decrease (almost 70% in comparison with untreated control cells), in a concentration dependent manner. Quantitative real-time RT-PCR experiments indicated a similar reduction in transcription level of hTERT gene under treatment with papaverine.Conclusion: Papaverine is a potent natural compound in suppression of cancer cell immortality most probably by antitelomerase activity. It is a valuable putative compound for further development of promising anti-cancer agents.

Background: Sexual dysfunction in males is characterized by the inability to achieve or maintain an erection sufficient for a satisfactory sexual activity. Erectile dysfunction is a common disorder in males and intracavernosal injection of papaverine followed by color Doppler ultrasonography of the penis is used to diagnose and treat vascular impotence. In this study, we examined the relationship between changes in peak systolic velocity (PSV) and erectile dysfunction with vascular cause after a cavernosal injection of papaverin.Methods: We performed this self-controlled clinical trial in Shahid Hasheminejad Hospital in Tehran, Iran during 2010 and 2011. The study population consisted of 90 patients with erectile dysfunction. The peak systolic velocity (PSV) of cavernosal arteries was evaluated before and after injection of 40-80 mg papaverine and it was compared in the patients with and without response to injection.Results: The mean age of participants was 47.7±13.7 years. Response to papaverine injection was positive in 41 (45.5%) patients. The mean PSV values were 14.68+5.65 and 53.74+18.8 cm/s before and after the injection, respectively (P<0.001). A PSV cut-off point of 10 cm/s was determined for the condition before injection. The sensitivity and specificity of the value for diagnosis of arterial erectile dysfunction were calclulated as 50% and 100%, respectively.Conclusion: A PSV cut-off point of 10 cm/s in flaccid status before papaverine injection has a low sensitivity but high specificity for the diagnosis of arterial erectile dysfunction. Future studies with sufficient cases of arterial erectile dysfunction are necessary for final judgments and suggestion a new cut off point.

We recently have read with great interest an article entitled “Clinical Efficacy of Intravenous Papaverine plus Ketorolac in the Emergency Treatment of Renal Colic: A Randomized, Double-blind Clinical Trial”, by Mohammadreza Pirouzi and colleagues, which was published in your esteemed journal (Vol 49, No. 11, November 2024).

We would like to address the letter critiquing our article entitled “Clinical Efficacy of Intravenous Papaverine Plus Ketorolac in the Emergency Treatment of Renal Colic: A Randomized, Double-blind Clinical Trial”, which was published in your esteemed journal (Vol 49, No. 11, November 2024). We appreciate the thoughtful comments provided in the letter and are grateful for the opportunity to respond to the points raised.