Effect of Tadalafil Administration on Redox Homeostasis and Polyamine Levels in Healthy Men with High Level of Physical Activity

Guglielmo Duranti, Roberta Ceci, Luigi Di Luigi, Cristina Antinozzi, Ivan Dimauro, Stefania Sabatini, Manuela Cervelli and Paolo Sgrò
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Guglielmo Duranti: Laboratory of Biochemistry and Molecular Biology, Department of Movement, Human and Health Sciences, Università degli studi di Roma “Foro Italico”, 00135 Rome, Italy
Roberta Ceci: Laboratory of Biochemistry and Molecular Biology, Department of Movement, Human and Health Sciences, Università degli studi di Roma “Foro Italico”, 00135 Rome, Italy
Luigi Di Luigi: Unit of Endocrinology, Department of Movement, Human and Health Sciences, Università degli studi di Roma “Foro Italico”, 00135 Rome, Italy
Cristina Antinozzi: Unit of Endocrinology, Department of Movement, Human and Health Sciences, Università degli studi di Roma “Foro Italico”, 00135 Rome, Italy
Ivan Dimauro: Laboratory of Biology and Genetics, Department of Movement, Human and Health Sciences, Università degli studi di Roma “Foro Italico”, 00135 Rome, Italy
Stefania Sabatini: Laboratory of Biochemistry and Molecular Biology, Department of Movement, Human and Health Sciences, Università degli studi di Roma “Foro Italico”, 00135 Rome, Italy
Manuela Cervelli: Department of Science, “Department of Excellence 2018–2022”, University of Rome “Roma Tre”, 00146 Rome, Italy
Paolo Sgrò: Unit of Endocrinology, Department of Movement, Human and Health Sciences, Università degli studi di Roma “Foro Italico”, 00135 Rome, Italy

IJERPH, 2021, vol. 18, issue 19, 1-12

Abstract: Background: The phosphodiesterase type 5 inhibitor (PDE5I) tadalafil, in addition to its therapeutic role, has shown antioxidant effects in different in vivo models. Supplementation with antioxidants has received interest as a suitable tool for preventing or reducing exercise-related oxidative stress, possibly leading to the improvement of sport performance in athletes. However, the use/abuse of these substances must be evaluated not only within the context of amateur sport, but especially in competitions where elite athletes are more exposed to stressful physical practice. To date, very few human studies have addressed the influence of the administration of PDE5Is on redox balance in subjects with a fitness level comparable to elite athletes; therefore, the aim of this study was to investigate for the first time whether acute ingestion of tadalafil could affect plasma markers related to cellular damage, redox homeostasis, and blood polyamines levels in healthy subjects with an elevated cardiorespiratory fitness level. Methods: Healthy male volunteers (n = 12), with a VO 2max range of 40.1–56.0 mL/(kg × min), were administered with a single dose of tadalafil (20 mg). Plasma molecules related to muscle damage and redox-homeostasis, such as creatine kinase (CK), lactate dehydrogenase (LDH), total antioxidant capacity (TAC), reduced/oxidized glutathione ratio (GSH/GSSG), free thiols (FTH), antioxidant enzyme activities (superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx)), as well as thiobarbituric acid reactive substances (TBARs), protein carbonyls (PrCAR), and polyamine levels (spermine (Spm) and spermidine (Spd)) were evaluated immediately before and 2, 6 and 24 hours after the acute tadalafil administration. Results: A single tadalafil administration induced an increase in CK and LDH plasma levels 24 after consumption. No effects were observed on redox homeostasis or antioxidant enzyme activities, and neither were they observed on the oxidation target molecules or polyamines levels. Conclusion: Our results show that in subjects with an elevated fitness level, a single administration of tadalafil induced a significant increase in muscle damage target without affecting plasma antioxidant status.

Keywords: tadalafil; redox homeostasis; polyamines; antioxidant enzyme activities (search for similar items in EconPapers)
JEL-codes: I I1 I3 Q Q5 (search for similar items in EconPapers)
Date: 2021
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