Adedayo O. Ademiluyi

Comparative Study on the Inhibitory Effect of Caffeic and Chlorogenic Acids on Key Enzymes Linked to Alzheimer’s Disease and Some Pro-oxidant Induced Oxidative Stress in Rats’ Brain-In Vitro

This study sought to investigate and compare the interaction of caffeic acid and chlorogenic acid on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and some pro-oxidants (FeSO4, sodium nitroprusside and quinolinic acid) induced oxidative stress in rat brain in vitro. The result revealed that caffeic acid and chlorogenic acid inhibited AChE and BChE activities in dose-dependent manner; however, caffeic acid had a higher inhibitory effect on AChE and BChE activities than chlorogenic acid. Combination of the phenolic acids inhibited AChE and BChE activities antagonistically. Furthermore, pro-oxidants such as, FeSO4, sodium nitroprusside and quinolinic acid caused increase in the malondialdehyde (MDA) contents of the brain which was significantly decreased dose-dependently by the phenolic acids. Inhibition of AChE and BChE activities slows down acetylcholine and butyrylcholine breakdown in the brain. Therefore, one possible mechanism through which the phenolic acids exert their neuroprotective properties is by inhibiting AChE and BChE activities as well as preventing oxidative stress-induced neurodegeneration. However, esterification of caffeic acid with quinic acid producing chlorogenic acid affects these neuroprotective properties.

Soybean phenolic-rich extracts inhibit key-enzymes linked to type 2 diabetes (α-amylase and α-glucosidase) and hypertension (angiotensin I converting enzyme) in vitro.

This study sought to assess the inhibitory activities of phenolic-rich extracts from soybean on α-amylase, α-glucosidase and angiotensin I converting enzyme (ACE) activities in vitro. The free phenolic extract of the soybean was obtained by extraction with 80% acetone, while that of the bound phenolic extract was done by extracting the alkaline and acid hydrolyzed residue with ethyl acetate. The inhibitory action of these extracts on the enzymes activity as well as their antioxidant properties was assessed. Both phenolic-rich extracts inhibited α-amylase, α-glucosidase and ACE enzyme activities in a dose dependent pattern. However, the bound phenolic extract exhibited significantly (P < 0.05) higher α-amylase and ACE inhibition while the free phenolic extract had significantly (P < 0.05) higher α-glucosidase inhibitory activity. Nevertheless, the free phenolic extract had higher α-glucosidase inhibitory activity when compared to that of α-amylase; this property confer an advantage on soybean phenolic-rich extracts over commercial antidiabetic drugs with little or no side effect. And inhibition of ACE suggests the antihypertension potential of soybean phenolic-rich extracts. Furthermore, the enzyme inhibitory activities of the phenolic-rich extracts were not associated with their phenolic content. Therefore, phenolic-rich extracts of soybean could inhibit key-enzyme linked to type 2 diabetes (α-amylase and α-glucosidase) and hypertension (ACE) and thus could explain in part the mechanism by which soybean renders these health promoting effect.

Caffeic and chlorogenic acids inhibit key enzymes linked to type 2 diabetes (in vitro): a comparative study

Abstract Background: Chlorogenic acid is a major phenolic compound that forms a substantial part of plant foods and is an ester of caffeic acid and quinic acid. However, the effect of the structures of both chlorogenic and caffeic acids on their antioxidant and antidiabetic potentials have not been fully understood. Thus, this study sought to investigate and compare the interaction of caffeic acid and chlorogenic acid with α-amylase and α-glucosidase (key enzymes linked to type 2 diabetes) activities in vitro. Methods: The inhibitory effect of the phenolic acids on α-amylase and α-glucosidase activities was evaluated. Thereafter, their antioxidant activities as typified by their 1,1-diphenyl-2 picrylhydrazyl radical scavenging ability and ferric reducing antioxidant properties were determined. Results: The results revealed that both phenolic acids inhibited α-amylase and α-glucosidase activities in a dose-dependent manner (2–8 μg/mL). However, caffeic acid had a significantly (p<0.05) higher inhibitory effect on α-amylase [IC50 (concentration of sample causing 50% enzyme inhibition)=3.68 μg/mL] and α-glucosidase (IC50=4.98 μg/mL) activities than chlorogenic acid (α-amylase IC50=9.10 μg/mL and α-glucosidase IC50=9.24 μg/mL). Furthermore, both phenolic acids exhibited high antioxidant properties, with caffeic acid showing higher effects. Conclusions: The esterification of caffeic acid with quinic acid, producing chlorogenic acid, reduces their ability to inhibit α-amylase and α-glucosidase activities. Thus, the inhibition of α-amylase and α-glucosidase activities by the phenolic acids could be part of the possible mechanism by which the phenolic acids exert their antidiabetic effects.

Antioxidant and inhibitory effect of red ginger (Zingiber officinale var. Rubra) and white ginger (Zingiber officinale Roscoe) on Fe2+ induced lipid peroxidation in rat brain in vitro

Neurodegerative diseases have been linked to oxidative stress arising from peroxidation of membrane biomolecules and high levels of Fe have been reported to play an important role in neurodegenerative diseases and other brain disorder. Malondialdehyde (MDA) is the end-product of lipid peroxidation and the production of this aldehyde is used as a biomarker to measure the level of oxidative stress in an organism. The present study compares the protective properties of two varieties of ginger [red ginger (Zingiber officinale var. Rubra) and white ginger (Zingiber officinale Roscoe)] on Fe(2+) induced lipid peroxidation in rat brain in vitro. Incubation of the brain tissue homogenate in the presence of Fe caused a significant increase in the malondialdehyde (MDA) contents of the brain. However, the aqueous extract from both varieties of ginger caused a significant decrease in the MDA contents of the brain in a dose-dependent manner. However, the aqueous extract of red ginger had a significantly higher inhibitory effect on both Fe(2+)-induced lipid peroxidation in the rat brain homogenates than that of white ginger. This higher inhibitory effect of red ginger could be attributed to its significantly higher phytochemical content, Fe(2+) chelating ability, OH scavenging ability and reducing power. However, part of the mechanisms through which the extractable phytochemicals in ginger (red and white) protect the brain may be through their antioxidant activity, Fe(2+) chelating and OH scavenging ability. Therefore, oxidative stress in the brain could be potentially managed/prevented by dietary intake of ginger varieties (red ginger and white ginger rhizomes).

Inhibition of acetylcholinesterase activities and some pro-oxidant induced lipid peroxidation in rat brain by two varieties of ginger (Zingiber officinale).

Ginger has been reportedly used for the management or treatment of Alzheimers disease in folklore medicine. Therefore, this study sought to investigate the inhibitory effects of water extractable phytochemicals of red and white ginger on acetylcholinesterase activities, and sodium nitroprusside (SNP) and quinolinic acid (QA)-induced lipid peroxidation in rat brain -in vitro. Both extracts inhibited acetylcholinesterase (AChE) activities in a dose-dependent manner; however, white ginger had higher acetylcholinesterase inhibitory activity than red ginger. Combination of the ginger inhibited acetylcholinesterase activities synergistically. Furthermore, SNP and QA caused a significant increase in the malondialdehyde (MDA) contents of the brain; however, the extracts significantly decrease the SNP and QA elevated brain MDA contents in a dose-dependent manner. Nevertheless, there was no significant difference (P>0.05) in the inhibition of the SNP and QA-induced lipid peroxidation by both extracts. The inhibitory effect of ginger extracts on acetylcholinesterase activities and some prooxidants induced lipid peroxidation in rats brain could be attributed to the presence of phytochemicals such as flavonoids, tannins, alkaloids and terpenoids. Therefore, some possible mechanism by which ginger extracts exert anti-Alzheimer properties could be through the inhibition of acetylcholinesterase activities and prevention of lipid peroxidation in the brain.

Biological Activities of Essential Oils: From Plant Chemoecology to Traditional Healing Systems

Essential oils are complex mixtures of hydrocarbons and their oxygenated derivatives arising from two different isoprenoid pathways. Essential oils are produced by glandular trichomes and other secretory structures, specialized secretory tissues mainly diffused onto the surface of plant organs, particularly flowers and leaves, thus exerting a pivotal ecological role in plant. In addition, essential oils have been used, since ancient times, in many different traditional healing systems all over the world, because of their biological activities. Many preclinical studies have documented antimicrobial, antioxidant, anti-inflammatory and anticancer activities of essential oils in a number of cell and animal models, also elucidating their mechanism of action and pharmacological targets, though the paucity of in human studies limits the potential of essential oils as effective and safe phytotherapeutic agents. More well-designed clinical trials are needed in order to ascertain the real efficacy and safety of these plant products.

Changes in Polyphenols Distribution and Antioxidant Activity during Fermentation of Some Underutilized Legumes

The effect of fermentation on the polyphenol distribution and antioxidant activity of four underutilized legumes [Cajanus cajan L. Millsp (Pigeon pea), Vigna subterranea L. Verdc (Bambara groundnut), Sphenostylis stenocarpa Harms (African yam bean), and Phaseolus vulgaris L. (Kidney bean)] were investigated. The beans were cooked (12 h), soaked in boiled water (12 h), dehulled, and then cooked again (2 h). The cotyledons were drained, wrapped in jute sacks and left to ferment at 37°C (4 days) to produce condiments. The distribution of free and bound phenolic compounds in the fermented and unfermented beans was determined; thereafter the free radical scavenging ability, reducing power, and the ability of the free and bound phenolic compounds of the fermented and unfermented beans to inhibit lipid peroxidation were determined. The results of the study revealed that fermentation caused a significant increase (p<0.05) in the free soluble phenol content of the legumes, while there was a significant decrease (p<0.05) in the bound phenol content of the legumes. Free soluble phenol from both the fermented and unfermented legumes had a significantly (p<0.05) higher reducing power (except C. cajan), free radical scavenging ability (except C. cajan) and inhibition of lipid peroxidation than bound phenolic extract. However, free soluble phenolic compounds from the fermented beans had a significantly higher (p<0.05) reducing power, free radical scavenging ability, and inhibition of lipid peroxidation than free soluble phenols from unfermented beans. Hence, it was concluded that, fermentation could increase the free soluble phenolic content of the underutilized legumes tested and consequently enhance the antioxidant activities of the legumes; fermented V. subterranea was found to be the most promising condiment with antioxidant activity.

Effect of Combination on the Antioxidant and Inhibitory Properties of Tropical Pepper Varieties Against α-Amylase and α-Glucosidase Activities In Vitro

Pepper used as a spice for food preparations is usually a single type or a combination of several different varieties. This choice is usually based on individual preferences, without consideration of health benefits. Therefore, the present study investigated the health benefits of a combination of 3 pepper varieties commonly consumed in Nigeria. Aqueous extracts (1:100 w/v) of Capsicum annuum var. grossum, C. annuum var. abbreviatum, and C. annuum var. accuminatum and a combination of the 3 varieties (1:1:1) were assayed for phenolic content (total phenol and flavonoid), antioxidant activities (reducing power and 1,1-diphenyl-2-picrylhydrazyl radical-scavenging abilities), inhibitory effect on Fe²⁺-induced lipid peroxidation in rat pancreas in vitro, and the ability of the extracts to inhibit key enzymes linked with type 2 diabetes (α-amylase and α-glucosidase). The combination of peppers showed additive effects in their phenolic content and displayed antioxidant properties. However, the inhibition of pancreatic α-amylase activity showed an additive effect, whereas α-glucosidase inhibitory activity was antagonistic with the combination. C. annuum var. accuminatum contributed most to the activities of the combined peppers. Strong inhibitory activities of the peppers against key enzymes linked to type 2 diabetes and Fe²⁺-induced lipid peroxidation in rat pancreas in vitro, coupled with their antioxidant properties, suggest that pepper could be used in the prevention and management of type 2 diabetes. The pepper combination showed additive tendencies of these properties.

Inhibition of α-amylase and α-glucosidase activities by ethanolic extract of Telfairia occidentalis (fluted pumpkin) leaf

OBJECTIVE To investigate the inhibitory effect of Telfairia occidentalis Hook f. (Curcubitaceae) (T. occidentalis) leaf on key enzyme linked to type-2 diabetes (α - amylase and α - glucosidase) as well as assess the effect of blanching (a commonly practiced food processing technique) of the vegetable on these key enzymes. METHODS Fresh leaves of T. occidentalis were blanched in hot water for 10 minutes, and the extracts of both the fresh and blanched vegetables were prepared and used for subsequent analysis. The inhibitory effect of the extract on α - amylase and α - glucosidase activities as well as some antioxidant parameter was determined in vitro. RESULTS The result revealed that unprocessed T. occidentalis leaf reduce Fe(3+) to Fe(2+) and also inhibited α - amylase and α - glucosidase activities in a dose dependent manner. However, blanching of the leafy vegetables caused a significant (P<0.05) increase in the antioxidant properties but decrease their ability to inhibit α - amylase and α - glucosidase activities. CONCLUSIONS This antioxidant properties and enzyme inhibition could be part of the mechanism by which they are used in the treatment/prevention of type-2 diabetes. However, the blanched vegetable reduces their ability to inhibit both α - amylase and α - glucosidase activity in vitro.

Polyphenolic Composition and Evaluation of Antioxidant Activity, Osmotic Fragility and Cytotoxic Effects of Raphiodon echinus (Nees & Mart.) Schauer

Raphiodon echinus (R. echinus) is used in Brazilian folk medicine for the treatment of inflammation, coughs, and infectious diseases. However, no information is available on the potential antioxidant, cytotoxicity and genotoxicity of this plant. In this study, the polyphenolic constituents, antioxidant capacity and potential toxic effects of aqueous and ethanolic extracts of R. echinus on human erythrocytes and leukocytes were investigated for the first time. R. echinus extracts showed the presence of Gallic, chlorogenic, caffeic and ellagic acids, rutin, quercitrin and quercetin. Aqueous and ethanolic extracts of R. echinus exhibited antioxidant activity in DPPH radical scavenging with IC50 = 111.9 μg/mL (EtOH extract) and IC50 = 227.9 μg/mL (aqueous extract). The extracts inhibited Fe2+ (10 μM) induced thiobarbituric acid reactive substances (TBARS) formation in rat brain and liver homogenates. The extracts (30–480 μg/mL) did not induce genotoxicity, cytotoxicity or osmotic fragility in human blood cells. The findings of this present study therefore suggest that the therapeutic effect of R. echinus may be, in part, related to its antioxidant potential. Nevertheless, further in vitro and in vivo studies are required to ascertain the safety margin of its use in folk medicine.