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bioRxiv · 10.1101/2024.10.30.621167

In-silico Targeting Phosphodiesterase 5 and In-vivo Evaluation of the Aphrodisiac Effect of Azanza garckeana Fruit

Ejiofor, I. I.·Ezeanya, J. I.·Ibe, C. I.·Ogbue, O. C.·Emodi, R. C.·Agueze, J. C.·Ani, S. C.
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Abstract

Sexual dysfunction is a persistent problem affecting men, with erectile dysfunction (ED) and premature ejaculation being the most common. The current treatment involving the use of PhPDE5 inhibitors, such as sildenafil, is faced with some serious side effects. In Nigeria, there are claims that Azanza garckeana fruit has positive effects in male sexual dysfunction. This study aims to evaluate this claim of the aphrodisiac effects of Azanza garckeana, using computational and animal models. The 3D structures of the protein target of interest (phosphodiesterase) and 21 phytocompounds already isolated from and identified in the fruit were obtained from the Protein Data Bank and PubChem, respectively. The protein targets and the phytocompounds were prepared for molecular docking simulation using the Autodock tool. The docking was performed using Autodock-vina on the Linux platform. Phytocompounds with high specificity for the protein targets were identified, and their solubility profile was obtained. The fruits were extracted with ethanol using a Soxhlet apparatus at 60{degrees}C and concentrated with a rotary evaporator at 40{degrees}C. Phytochemical tests were conducted on the extract, and acute toxicity was evaluated using OECD 423 guidelines. The aphrodisiac effect was studied in-vivo using a rat model. Parameters such as mount and intromission frequencies, mount and ejaculation latency and testosterone levels were assessed. Three phytocompounds showed better binding affinity for phosphodiesterase 5 than the reference compounds and were also found to be a good target for the proteins of interest. The extract was found to contain steroids, flavonoids, and terpenoids. The results from the in-vivo study demonstrated significant increases (p<0.05) in mean mounting and intromission frequencies and ejaculatory latency following treatment with the extract at 500 mg/kg body weight. The study also demonstrated a significant decrease (p<0.05) in mount latency. Testosterone levels increased significantly (p<0.05) at 500mg/kg body weight. This study affirms the aphrodisiac effect of Azanza garckeana fruit in the albino rat model and suggests that the fruits ethanol extract holds promise as an important phytomedicine for the development of more effective treatments for male sexual dysfunction.

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Ejiofor, I. I., Ezeanya, J. I., Ibe, C. I., Ogbue, O. C., Emodi, R. C., Agueze, J. C., Ani, S. C.. 2024-11-03. In-silico Targeting Phosphodiesterase 5 and In-vivo Evaluation of the Aphrodisiac Effect of Azanza garckeana Fruit. https://doi.org/10.1101/2024.10.30.621167

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