Adeniyi A. Adebayo

In vitro inhibition of phosphodiesterase-5 and arginase activities from rat penile tissue by two Nigerian herbs (Hunteria umbellata and Anogeissus leiocarpus)

Abstract Background: Anogeissus leiocarpus and Hunteria umbellata have been reportedly used in traditional medicine for the management of erectile dysfunction (ED). However, the scientific basis for their use has not been well established. Therefore, this study was designed to investigate the inhibitory effects of water extractable phytochemicals of H. umbellata and A. leiocarpus on phosphodiesterase-5 (PDE-5) and arginase as well as pro-oxidants induced lipid peroxidation in rat penile tissue. Methods: The effects of the extracts on important enzymes (PDE-5 and arginase) linked with ED and pro-oxidants (Fe2+ and sodium nitroprusside) induced lipid peroxidation were investigated. Also, radicals scavenging and metal chelating abilities were determined. In addition, phenolic contents were determined and characterized using HPLC. Results: The results showed that both extracts inhibited PDE-5 and arginase activities in a dose-dependent manner. Inhibitory property of A. leiocarpus (IC50 – 174.19 μg/mL) was significantly better (p<0.05) than that of H. umbellata (IC50 – 537.72 μg/mL) in PDE-5 assay. The extracts were potent inhibitors of arginase than PDE-5, and these extracts were equally potent in inhibiting arginase. Furthermore, Fe2+ and sodium nitroprusside caused a significant increase in malondialdehyde content; however, both extracts reduced malondialdehyde level in concentration-dependent manner. It is noteworthy that both extracts scavenged radicals (OH* and ABTS*) and chelated Fe2+. HPLC analysis revealed abundance of rutin, chlorogenic acid, gallic acid, caffeic acid, and quercetin, among others. Conclusions: The ability of the extracts to inhibit PDE-5, arginase and pro-oxidant induced lipid peroxidation, and chelate metal might suggest their folkloric use for the management of ED.

Phenolic profile and Enzyme Inhibitory activities of Almond (Terminalia catappa) leaf and Stem bark

ABSTRACT Almond (Terminalia catappa) is a species used in Nigerian folkloric medicine because of its antihypertensive property. In this study, the acetylcholinesterase, arginase, phosphodiesterase-5 and angiotensin-1-converting enzyme inhibition and antioxidant properties of the phenolic-rich extracts from almond leaf and stem bark were determined. The chemical composition was evaluated using high-performance liquid chromatography. The total phenol and flavonoid contents were estimated and the antihypertensive potential was estimated by the determination of acetylcholinesterase, arginase, phosphodiesterase-5 and angiotensin-1-converting enzyme inhibition in vitro. Three assays were used for the evaluation of antioxidant properties of the extracts. Eleven and eight phenolic compounds were detected in leaf and stem bark respectively. The phenolic-rich extracts showed remarkable enzyme inhibition activity in concentration dependent manner, with high antioxidant activities. Almond leaf and stem bark can serve as potential natural source for the development of a novel antihypertensive agent.

Erection-stimulating, anti-diabetic and antioxidant properties of Hunteria umbellata and Cylicodiscus gabunensis water extractable phytochemicals

Abstract Background Herbs have been used as an aphrodisiac since ages. This study was designed to investigate the effects of Hunteria umbellata (HU) seeds and Cylicodiscus gabunensis (CG) stem barks aqueous extracts on key enzymes relevant to erectile dysfunction (phosphodiesterase-5 and arginase) and type-2 diabetes (α-amylase and α-glucosidase). Methods In ascertaining the erectogenic and antidiabetic properties of the extracts, the effects of the extracts on activities of some enzymes relevant to erectile dysfunction (arginase and phosphodiesterase-5) and type-2 diabetes (α-amylase and α-glucosidase) were determined. Antioxidant properties of the extracts were assessed through several antioxidant assays (DPPH˙, OH˙). Furthermore, their phenolic constituents were estimated and quantified using HPLC. Results The results revealed that both extracts inhibited α-amylase and α-glucosidase in a concentration-dependent manner. HU showed higher α-amylase (IC50=221.30 µg/mL) and α-glucosidase (IC50=184.35 µg/mL) inhibition than CG. Also, both extracts inhibited phosphodiesterase-5 and arginase in a dose-dependent manner in vitro; nevertheless, HU showed higher inhibition [phosphodiesterase-5 (IC50=539.72 µg/mL); arginase (41.53 µg/mL)] than CG [phosphodiesterase-5 (IC50=611.35 µg/mL); arginase (47.95 µg/mL)]. In addition, the extracts possess antioxidant properties through radical (DPPH and OH) scavenging and metal (Fe2+) chelating abilities. HPLC analysis of phenolic constituents revealed the abundance of gallic acid, chlorogenic acid, caffeic acid, ellagic acid and quercetin. Conclusions The ability of samples’ extract to inhibit some of key enzymes relevant to erectile dysfunction and type-2 diabetes could render them cheap, natural and alternative therapy with erectogenic and antidiabetic potentials.

Modulatory Effects of Alkaloid Extract from Gongronema latifolium (Utazi) and Lasianthera africana (Editan) on Activities of Enzymes Relevant to Neurodegeneration

ABSTRACT Most alkaloids are produced by plants as a defense mechanism against herbivores. Since alkaloids are known to possess pharmacological effects, this study sought to investigate the in vitro modulatory effect of alkaloid obtained from two commonly consumed vegetables in southern Nigeria, Lasianthera africana (editan) and Gongronema latifolium (utazi), on some enzyme activities relevant to neurodegeneration. Effects of the alkaloids on cholinesterases (acetylcholinesterase [AChE] and butyrylcholinesterase [BChE]) and monoamine oxidase (MAO) activities were determined in vitro. In addition, Fe2+ chelating ability as well as radical-scavenging abilities were determined. Alkaloid profile was also determined using gas chromatography coupled with flame ionization detector (GC-FID). The results revealed that the alkaloids inhibited AChE, BChE, and MAO activities in a concentration-dependent manner, such that the alkaloid from G. latifolium showed higher enzyme inhibition (AChE [IC50 = 87.39 µg/ml], BChE [IC50 = 118.65 µg/ml], and MAO [IC50 = 61.37 µg/ml]) than L. africana (AChE = 115.60 µg/ml; BChE = 169.48 µg/ml; MAO = 73.72 µg/ml). In addition, GC-FID analysis revealed abundance of choline in both extracts. Gongronema latifolium and Lasianthera africana alkaloid extracts inhibit enzymes (acetylcholinesterase, butyrylcholinesterase, and monoamine oxidase) implicated in neurodegenerative diseases. Hence, these vegetables could offer dietary supplement in the management of neurodegenerative diseases.

Phenolic-rich extracts of Eurycoma longifolia and Cylicodiscus gabunensis inhibit enzymes responsible for the development of erectile dysfunction and are antioxidants

Abstract Background: Herbs have been used from ages to manage male sexual dysfunction. Hence, this study sought to investigate the effects of Eurycoma longifolia (EL) and Cylicodiscus gabunensis (CG) stem bark extracts on some enzymes implicated in erectile dysfunction in vitro. Methods: The extracts were prepared, and their effects on phosphodiesterase-5 (PDE-5), arginase, and angiotensin-1-converting enzyme (ACE) as well as pro-oxidant-induced lipid peroxidation were assessed. Furthermore, phenolic contents were determined, and their components were characterized and quantified using high-performance liquid chromatography with diode array detector (HPLC-DAD). Results: The results revealed that the extracts inhibited PDE-5, arginase, and ACE in a concentration-dependent manner. However, IC50 values revealed that CG had higher inhibitory potential on PDE-5 (IC50=204.4 μg/mL), arginase (IC50=39.01 μg/mL), and ACE (IC50=48.81 μg/mL) than EL. In addition, the extracts inhibited pro-oxidant-induced lipid peroxidation in penile tissue homogenate. HPLC-DAD analysis showed that CG is richer in phenolic compounds than EL, and this could be responsible for higher biological activities observed in CG than EL. Conclusions: Hence, the observed antioxidant property and inhibitory action of CG and EL on enzymes relevant to erectile dysfunction in vitro could be part of possible mechanisms underlying their involvement in traditional medicine for the management of male sexual dysfunction.

Modulatory effect of some citrus (Citrus limon, Citrus reticulata, Citrus maxima) peels on monoamine oxidase, phosphodiesterase-5 and angiotensin-1 converting enzyme activities in rat heart homogenate

Abstract Background Citrus peels have been reported useful in folk medicine for the management of cardiovascular diseases, but there is dearth of information on the possible mechanisms for their therapeutic action. The aim of this study was to investigate the effect of methanolic extracts from some citrus [lime (Citrus limon), tangerine (Citrus reticulata), shaddock (Citrus maxima)] peels on some enzymes relevant to the management of cardiovascular diseases [monoamine oxidase (MAO), phosphodiesterase-5 (PDE-5) and angiotensin-1-converting enzyme (ACE)]. Methods Effect of methanolic extracts of lime, tangerine and shaddock peels on MAO, PDE-5 and ACE were carried out using standard methods. In addition, the ability of the extracts to prevent oxidative damage in rat heart homogenates was also investigated. Finally, the total polyphenol content of extracts was determined. Results The results revealed that methanolic extracts of lime, tangerine and shaddock peels inhibited MAO, PDE-5, ACE and pro-oxidants induced lipid peroxidation in rat heart homogenate in a concentration-dependent manner. Conclusions Findings in this study revealed citrus peel methanolic extracts as natural inhibitor of enzymes (MAO, PDE-5 and ACE) implicated in cardiovascular diseases. Therefore, citrus peels could help in the management of cardiovascular diseases possibly through inhibition of these enzymes.

Effect of cooking on glycemic index, antioxidant activities, α-amylase, and α-glucosidase inhibitory properties of two rice varieties

Abstract This study was designed to investigate the influence of cooking on the glycemic index (GI), amylose, and amylopectin contents of two rice varieties. Two rice varieties (foreign long rice and ofada) were sourced for, divided into two, one portion cooked and the other used raw. The sugar, starch, amylose, and amylopectin contents as well as glycemic indices, antioxidant properties, and the ability of the rice to inhibit carbohydrate‐hydrolyzing enzymes (α‐amylase and α‐glucosidase) were determined. In addition, polyphenol content was determined. The results revealed that cooking caused a significant increase in starch content of the rice varieties. In the same vein, cooking increases the amylopectin content but has no effect on the amylose content. In addition, cooking shows no effect on polyphenol content but significantly increases radical scavenging ability of rice varieties used in this study. Furthermore, cooking lower the α‐amylase and α‐glucosidase inhibitory properties of two rice varieties except for foreign rice. However, the inhibitory effect of both cooked and raw foreign and ofada rice on α‐amylase and α‐glucosidase coupled with their low GI may explain their important role in controlling blood glucose level.