scholarly journals Serenoa repens extracts: In vitro study of the 5α-reductase activity in a co-culture model for Benign Prostatic Hyperplasia

2018 ◽  
Vol 90 (3) ◽  
pp. 199-202 ◽  
Author(s):  
Daniela Buonocore ◽  
Manuela Verri ◽  
Laura Cattaneo ◽  
Sara Arnica ◽  
Michele Ghitti ◽  
...  
Keyword(s):  
Benign Prostatic Hyperplasia ◽  
Reductase Activity ◽  
Ethanol Extract ◽  
Prostatic Hyperplasia ◽  
Type I ◽  
Serenoa Repens ◽  
Culture Model ◽  
Hexane Extracts ◽  
Ethanol Extracts

Objectives. Benign Prostatic Hyperplasia (BPH) is a form of benign tumor that occurs in humans mainly with ageing. It affects more than 50% of over 50 years old males and it is characterized by an increased synthesis of dihydrotestosterone (DHT), due to the 5α-reductase activity. The BPH therapeutic approach mainly uses 5α-reductase inhibitors, such as the active compounds present in the extracts deriving from species Serenoa repens. Many lipidosterolic extracts are available on the market, which are obtained with different solvents, among them ethanol is recognized as non-toxic and has less handling risks than hexane. The purpose of the present experimental study was to investigate in-vitro the potency of an ethanol extract of S. repens comparing it with an n-hexane one. Materials and methods. Two different lipido-sterolic extracts of S. repens have been tested: ethanol extract and n-hexane extract, two batches for each one. The inhibitory action of the extract was evaluated estimating in-vitro the activity of enzyme 5α-reductase type I (5α-RI), which was mainly active under the experimental condition of pH 7.5. DHT amount, synthesized from testosterone (1 μM), was evaluated in a co-culture model of epithelial cells and fibroblasts resulting from prostatic biopsy of a patient with BPH.Results. The analysis of the resulting dose-response curves showed that the entire S. repens extracts inhibited the 5α-RI showing no difference between the two kinds of extract or between the batches. The resulting IC50 values were the following: 8.809 (95% CI = 5.133-15.56) and 9.464 (95% CI = 5.094- 18.27) for ethanol extracts; 11.08 (95% CI = 6.389-19.98) and 12.72 (95% CI = 7.758-21.53) for n-hexane extracts. Conclusions. The potency of ethanol extracts of S. repens was comparable with the one of n-hexane extracts.

Effect of Pregnenolone Derivatives on the Selective Inhibition of 5α-Reductase 2 Activity

2020 ◽  
Vol 15 (3) ◽  
pp. 179-189
Author(s):  
Marisa Cabeza ◽  
Lucero Bautista ◽  
Eugene Bratoeff ◽  
Juan Soriano ◽  
Yvonne Heuze
Keyword(s):  
Biological Activity ◽  
Benign Prostatic Hyperplasia ◽  
Animal Studies ◽  
Reductase Activity ◽  
Selective Inhibition ◽  
Causative Factor ◽  
Prostatic Hyperplasia ◽  
Hamster Model ◽  
Ic50 Values

Background: Benign prostatic hyperplasia and prostate cancer are androgen-dependent diseases, and dihydrotestosterone (DHT), a 5α-reduced metabolite of testosterone (T), has been implicated as a causative factor in the progression of these diseases. The 5α-reductase enzyme (5α-R) converts T to DHT, which is responsible for increasing cell proliferation, and hence inhibition of this enzyme could lead to potential treatments for these afflictions. Objective: This study focused on evaluating the biological activity of three series of pregnenolone derivatives as inhibitors of 5α-R and as antiandrogens on androgen-dependent glands. Method: To determine the biological activity of these compounds, we evaluated the effect of each one on suppressing the activity of both types of isozymes of 5α-R (1 and 2) by 50% (IC50). Using animal studies, we assessed the effect of these derivatives on the weight of the prostate, seminal vesicles, and diameter of the flank organs of castrated hamsters previously dosed with 1 mg/Kg T. Results: In vitro experiments showed that derivatives 1f, 2b, and 3d were very effective inhibitors of the activity of 5α-R2, showing IC50 values of 21.8, 20, and 15 nM, respectively. Derivatives 2b and 3b showed a lower inhibition effect on 5α-R1. : The data also indicated that derivatives 2b, 1f, 3b, and 3d were very active in reducing prostate weight in the hamster model of benign prostatic hyperplasia. Discussion: Pharmacological experiments showed that pregnenolone derivatives possess an antiandrogenic effect because of the inhibition of DHT production in androgen-dependent glands. Conclusion: The pregnenolone derivatives studied suppressed type 2 5α-reductase activity and because of this, the weight and dimension of androgen-dependent organs were decreased.

scholarly journals Anti-Inflammatory, Antioxidant, and Anthelmintic Activities of Ocimum basilicum (Sweet Basil) Fruits

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Clement Osei Akoto ◽  
Akwasi Acheampong ◽  
Yaw Duah Boakye ◽  
Abdulai A. Naazo ◽  
Derrick H. Adomah
Keyword(s):  
Antioxidant Activities ◽  
Anthelmintic Activity ◽  
Ethanol Extract ◽  
Ocimum Basilicum ◽  
High Concentration ◽  
Hexane Extracts ◽  
Anti Inflammatory ◽  
Ethanol Extracts ◽  
Dpph Scavenging

Basil (Ocimum basilicum Linn.) is a plant that has found use in traditional medicine and household remedy against human ailments. The present study aimed at investigating hexane and ethanol fruit extracts of Ocimum basilicum Linn. for their phytoconstituents and anti-inflammatory, antioxidant, and anthelmintic activities. Phytochemical screenings were performed using standard protocols. Anti-inflammatory activities were assessed using the egg albumin denaturation method, while the antioxidant activities of the extracts were determined using DPPH scavenging, total antioxidant capacity (TAC), and hydrogen peroxide (H2O2) assays. In vitro anthelmintic activity of both extracts was investigated against Eudrilus eugeniae (Earthworms). Column chromatography was employed to separate the least polar fraction A, using hexane as the mobile phase, which was analyzed using FTIR analysis. The preliminary phytochemical screening revealed the presence of alkaloids, phenols, saponins, glycosides, steroids, tannins, terpenoids, and flavonoids. The hexane and ethanol extracts exhibited high concentration-dependent anti-inflammatory activities, with their percentage inhibitions being 34.0 ± 0.01 and 17.6 ± 0.04 μg/mL, respectively. The hexane extract showed a higher concentration-dependent antioxidant activity (IC50 of 14.17 ± 1.15 μg/mL) compared to the ethanol extract (IC50 > 100.0 μg/mL) for the DPPH assay. The IC50 values of ethanol and hexane extracts were 623.5 ± 0.27 and >1000.0 μg/mL, respectively, for the H2O2 scavenging assay. TAC was determined to be 37.48 ± 0.09 and 18.81 ± 0.12 gAAE/100 g for ethanol and hexane extracts, respectively. Both extracts showed a higher concentration-dependent anthelmintic activity. Increasing the concentration increased the helmintic potency of the extracts. The results indicate that both hexane and ethanol extracts of Ocimum basilicum Linn. exhibit anti-inflammatory, antioxidant, and anthelmintic activities and support the traditional usage of this plant.

scholarly journals Serenoa repens and Urtica dioica Fixed Combination: In-Vitro Validation of a Therapy for Benign Prostatic Hyperplasia (BPH)

2020 ◽  
Vol 21 (23) ◽  
pp. 9178
Author(s):  
Miriam Saponaro ◽  
Isabella Giacomini ◽  
Giulia Morandin ◽  
Veronica Cocetta ◽  
Eugenio Ragazzi ◽  
...  
Keyword(s):  
Benign Prostatic Hyperplasia ◽  
Urtica Dioica ◽  
Prostatic Hyperplasia ◽  
Human Model ◽  
Ros Production ◽  
Serenoa Repens ◽  
Prostate Cell ◽  
Age Related ◽  
Anti Inflammatory

Benign prostatic hyperplasia (BPH) is an age-related chronic disorder, characterized by the hyperproliferation of prostatic epithelial and stromal cells, which drives prostate enlargement. Since BPH aetiology and progression have been associated with the persistence of an inflammatory stimulus, induced both by Nuclear Factor-kappa B (NF-κB) activation and reactive oxygen species (ROS) production, the inhibition of these pathways could result in a good tool for its clinical treatment. This study aimed to evaluate the antioxidant and anti-inflammatory activity of a combined formulation of Serenoa repens and Urtica dioica (SR/UD) in an in vitro human model of BPH. The results confirmed both the antioxidant and the anti-inflammatory effects of SR/UD. In fact, SR/UD simultaneously reduced ROS production, NF-κB translocation inside the nucleus, and, consequently, interleukin 6 (IL-6) and interleukin 8 (IL-8) production. Furthermore, the effect of SR/UD was also tested in a human androgen-independent prostate cell model, PC3. SR/UD did not show any significant antioxidant and anti-inflammatory effect, but was able to reduce NF-κB translocation. Taken together, these results suggested a promising role of SR/UD in BPH and BPH-linked disorder prevention.

Insilico and In Vitro Study: COX-2 Inhibition by Ethanol Extract of Dayak Onion Bulb (Eleutherine americana Merr) as Treatment Innovation of Benign Prostatic Hyperplasia (BPH)

2020 ◽  
Vol 19 ◽  
Author(s):  
Hendra Sutapa ◽  
M Aris Widodo ◽  
Basuki Bambang Purnomo ◽  
Doddy M Soebadi ◽  
Edvin Prawira Negara
Keyword(s):  
Benign Prostatic Hyperplasia ◽  
Experimental Research ◽  
Inhibitory Activity ◽  
Ethanol Extract ◽  
Prostatic Hyperplasia ◽  
Onion Bulb ◽  
Cox 2 ◽  
Eleutherine Americana ◽  
Cox 1

Introduction: Benign Prostatic Hyperplasia (BPH) is benign tumor in male which is histopathologically known with an increase of epithelial cells and prostatic stroma. Androgens, estrogens, stroma-epithelial interactions, growth factors, and chronic inflammation play a role in the occurrence of BPH. Chronic inflammation in BPH is characterized by excessive expression of COX-2 which will trigger the expression of Bcl-2 anti-apoptotic protein. Dayak onion (Eleutherine americana Merr) is a typical Kalimantan plant that is believed as the treatment for prostate disease. This plant contains flavonoids which can inhibit the COX-2 enzyme. Thus, it causes a reduction in the production of prostaglandin E2. Method: this research was an experimental research computationally and in vitro laboratory experimental research to determine COX-2 inhibitory activity by ethanol extracts of dayak onion. Result and Discussion: In insilico flavonoid, it was strongly related to COX-2 receptor on the active side of TYR371. Thus, it had the potential to inhibit COX-2. COX-2 Inhibitor would cause bcl-2 to be inactive so that apoptosis occurred in BPH. In the in vitro research using human whole blood assay, the Dayak Onion bulb ethanol extract had IC50 COX-2 of 40.57 ng/ml and IC50 COX-1 of 364.89 ng/ml. Therefore, the ratio of IC50 COX-2 to IC50 COX-1 was 0.11. Conclusion: ethanol extract of Dayak onion bulb has inhibitory activity against COX-2. Thus, it has potential as innovation of BPH treatment. Patient Summary: male, age 25-35 years old, healthy (history taking, physical and laboratory examination), and not using NSAIDs for the past 2 weeks.

Evaluation of Snake Venom’s PhospholipaseA2 Enzyme Inhibition Activity of Cyphostemma adenocoule

2020 ◽  
Vol 14 (3) ◽  
pp. 196-202
Author(s):  
Atul Kaushik ◽  
Teamrat S. Tesfai ◽  
Daniel K. Barkh ◽  
Furtuna K. Ghebremeskel ◽  
Habtom G. Zerihun ◽  
...  
Keyword(s):  
Enzyme Inhibition ◽  
Snake Venom ◽  
Ethanol Extract ◽  
Egg Yolk ◽  
Chloroform Extract ◽  
Inhibition Activity ◽  
Traditional Use ◽  
Snake Bites ◽  
Ethanol Extracts

Background: A snake bite is fundamentally an injury often resulting in puncture wounds meted out by the animal's fangs and occasionally resulting in envenomation. Rate of snake bites around 5,400,000 bites per year leads to over 2,500,000 envenomings and around 125,000 fatal cases annually. Snake venom enzymes are rich in metalloproteinases, phospholipaseA2, proteinases, acetylcholinesterases and hyaluronidases. Objective: Cyphostemma adenocoule is traditionally being used for the treatment of snake bites in Eritrea. The present research was aimed at evaluating the snake venom enzyme inhibition activity of C. adenocoule against puff adder venom and developing a base for the traditional use of the plant against snakebites in Eritrea. Methods: The anti-venom activity of C. adenocoule was assessed in-vitro through phospholipaseA2 enzyme inhibition assay using egg yolk as a cell. The ethanol and chloroform extracts of C. adenocoule showed in vitro anti phospholipase A2 activity, whereas the water extracts of the plant showed no activity. Results: Among the extracts of C. adenocoule, the highest percentage of inhibition was obtained from chloroform extract (95.55% at 100mg/ml). The extract showed prominent activity at different concentrations (34.7% at10mg/ml, 48.8% at 20mg/ml, 54.8% at 40mg/ml, 60.9% at 60mg/ml, 80.5% at 80mg /ml). The ethanol extract also showed certain activity at various concentrations (25.22% at10mg/ml, 14.78% at 20mg/ml, 2.6% at40mg/ml). The activity of the chloroform extracts increases as concentration increases, whereas the activity of the ethanol extracts decreases as concentration increases. The aqueous extract of C. adenocoule did not show any activity at all concentrations. Conclusion: In this study, the chloroform and ethanol extracts of the plant inhibited the enzyme of interest and thus proved the efficacy of anti-snake venom activity of the plant.

scholarly journals Pharmacological Effects and Potential Clinical Usefulness of Polyphenols in Benign Prostatic Hyperplasia

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 450
Author(s):  
Kensuke Mitsunari ◽  
Yasuyoshi Miyata ◽  
Tomohiro Matsuo ◽  
Yuta Mukae ◽  
Asato Otsubo ◽  
...  
Keyword(s):  
Benign Prostatic Hyperplasia ◽  
Molecular Mechanisms ◽  
Prostatic Hyperplasia ◽  
Pathological Conditions ◽  
Urinary Tract Symptoms ◽  
Anti Inflammatory ◽  
Lower Urinary

Benign prostatic hyperplasia (BPH) is arguably the most common benign disease among men. This disease is often associated with lower urinary tract symptoms (LUTS) in men and significantly decreases the quality of life. Polyphenol consumption reportedly plays an important role in the prevention of many diseases, including BPH. In recent years, in addition to disease prevention, many studies have reported the efficacy and safety of polyphenol treatment against various pathological conditions in vivo and in vitro. Furthermore, numerous studies have also revealed the molecular mechanisms of the antioxidant and anti-inflammatory effects of polyphenols. We believe that an improved understanding of the detailed pharmacological roles of polyphenol-induced activities at a molecular level is important for the prevention and treatment of BPH. Polyphenols are composed of many members, and their biological roles differ. In this review, we first provide information regarding the pathological roles of oxidative stress and inflammation in BPH. Next, the antioxidant and anti-inflammatory effects of polyphenols, including those of flavonoids and non-flavonoids, are discussed. Finally, we talk about the results and limitations of previous clinical trials that have used polyphenols in BPH, with particular focus on their molecular mechanisms of action.

scholarly journals The treatment effects of flaxseed-derived secoisolariciresinol diglycoside and its metabolite enterolactone on benign prostatic hyperplasia involve the G protein-coupled estrogen receptor 1

2016 ◽  
Vol 41 (12) ◽  
pp. 1303-1310 ◽  
Author(s):  
Guan-Yu Ren ◽  
Chun-Yang Chen ◽  
Wei-Guo Chen ◽  
Ya Huang ◽  
Li-Qiang Qin ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Estrogen Receptor ◽  
Benign Prostatic Hyperplasia ◽  
G Protein ◽  
Therapeutic Potential ◽  
Prostatic Hyperplasia ◽  
Docking Simulations ◽  
G Protein Coupled

Secoisolariciresinol diglucoside (SDG), a lignan extracted from flaxseed, has been shown to suppress benign prostatic hyperplasia (BPH). However, little is known about the mechanistic basis for its anti-BPH activity. The present study showed that enterolactone (ENL), the mammalian metabolite of SDG, shared the similar binding site of G1 on a new type of membranous estrogen receptor, G-protein-coupled estrogen eceptor 1 (GPER), by docking simulations method. ENL and G1 (the specific agonist of GPER) inhibited the proliferation of human prostate stromal cell line WPMY-1 as shown by MTT assay and arrested cell cycle at the G0/G1 phase, which was displayed by propidium iodide staining following flow cytometer examination. Silencing GPER by short interfering RNA attenuated the inhibitory effect of ENL on WPMY-1 cells. The therapeutic potential of SDG in the treatment of BPH was confirmed in a testosterone propionate-induced BPH rat model. SDG significantly reduced the enlargement of the rat prostate and the number of papillary projections of prostatic alveolus and thickness of the pseudostratified epithelial and stromal cells when comparing with the model group. Mechanistic studies showed that SDG and ENL increased the expression of GPER both in vitro and in vivo. Furthermore, ENL-induced cell cycle arrest may be mediated by the activation of GPER/ERK pathway and subsequent upregulation of p53 and p21 and downregulation of cyclin D1. This work, in tandem with previous studies, will enhance our knowledge regarding the mechanism(s) of dietary phytochemicals on BPH prevention and ultimately expand the scope of adopting alternative approaches in BPH treatment.

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