Impact of drying processes on Bryophyllum pinnatum phenolic constituents and its anti-inflammatory and antioxidative activities in human erythrocytes.

The effect of drying on the phytoconstituents, antioxidative, and anti-inflammatory properties of Bryophyllum pinnatum leaves was investigated. The phenolic constituents were characterized using HPLC-DAD. The aqueous extraction was done and various assays (Inhibition of membrane stabilization, albumin Denaturation and heat-induced hemolysis, malondialdehyde (MDA), and reduced glutathione (GSH) contents, as well as superoxide dismutase (SOD) activity), were carried out on human erythrocytes. The fresh portion (89.12 µg/ml) exhibited the highest potential to inhibit heat-induced hemolysis compared to the standard drug-Diclofenac (91.51 µg/ml). Freeze-dried sample showed the highest inhibitory potential on albumin denaturation ([Freeze-dried-330.72 µg/ml], [Diclofenac-318.63 µg/ml]) and membrane destabilization ([Freeze-dried-331.93 µg/ml], [Diclofenac-289.57 µg/ml]) when compared with Diclofenac. Similarly, the freeze-dried sample showed the highest GSH and SOD level and lowest MDA level when human erythrocytes challenged with tertiary butyl hydroperoxide (tBHP) were treated with the extract. This study confirms the retention of a considerable quantity of bioactive constituents of plants when freeze-dried. PRACTICAL APPLICATIONS: The ideal method of drying Bryophyllum pinnatum and possible anti-inflammatory potential was investigated. This work may apply to the development of anti-inflammatory agents from a natural source with little or no side effect in managing inflammation.

Alkaloid extracts from Bitter leaf (Vernonia amygdalina) and Black nightshade (Solanum nigrum) inhibit phosphodiesterase-5, arginase activities and oxidative stress in rats penile tissue.

The erectogenic potential of alkaloids extracted from Bitter leaf (Vernonia amygdalina) and Black nightshade (Solanum nigrum) was investigated in this study. Fresh leaves obtained from Bitter leaf and Black night shade were air-dried, pulverized, and extracted for alkaloids. The inhibitory potential of the alkaloid extracts on arginase and phosphodiesterase-5 (PDE-5) activities in rats penile tissue was determined in vitro. The antioxidant properties were also evaluated and the constituent alkaloids quantified using GC-MS. The alkaloid extracts inhibited arginase (0-30.51 µg/ml) and PDE-5 (0-133.69 µg/ml) activities in a concentration-dependent pattern. Similarly, the alkaloid extracts inhibited Fe2+ -induced lipid peroxidation in rats penile tissues, scavenged DPPH, OH, and NO radicals as a function of concentration. GC-MS characterization revealed over 20 alkaloid compounds. The inhibition of PDE-5-, arginase-, pro-oxidant-induced lipid peroxidative-, and free radicals-scavenging activities by the alkaloids is suggestive of putative mechanisms underlying their therapeutic use for managing erectile dysfunction in folklore medicine. PRACTICAL APPLICATIONS: Alkaloids extracted from Black nightshade (Solanum nigrum) and Bitter leaf (Vernonia amygdalina) were characterized and investigated by standard procedures for inhibitory action against key erectile dysfunction-linked enzymes and antioxidant activity. The alkaloids inhibited erectile dysfunction-linked enzymes (arginase and PDE-5) and showed considerable antioxidant activity in a concentration-dependent manner. In view of this, we suggest the application of these results in the development of erectile dysfunction drugs in the pharmaceutical industry, with probable minimal or no adverse effect.

Effect of dietary supplementation of Padauk (Pterocarpus soyauxii) leaf on high fat diet/streptozotocin induced diabetes in rats' brain and platelets.

BACKGROUND: This study investigated the effects of Padauk leaf on brain malondialdehyde (MDA) content, acetylcholinesterase (AChE) activities, ectonucleotidases and adenosine deaminase (ADA) activities in the platelet of high fat diet and streptozotocin (STZ)-induced diabetic rats. METHODS: The animals were divided into six groups (n=7): normal control rats; diabetic rats+high fat diet (HFD); diabetic rats+HFD+Metformin; diabetic rats+HFD+acarbose; diabetic rats+HFD+10% Padauk leaf; normal rats+basal diet+10% Padauk leaf. After 30days of experiment comprising of acclimatization, dietary manipulation, pre-treatment with STZ and supplementation with Padauk leaf, the animals were sacrificed and the rats' brain and blood were collected for subsequent analysis. RESULTS: The results demonstrated that the elevated MDA content and AChE activity in the diabetic rats were significantly reduced when compared with the control rats. Furthermore, the increased NTPDases, 5'-nucleotidase and ADA activities in the diabetic rats were significantly reduced when compared with the control rats. CONCLUSION: This study demonstrated that Padauk leaf exhibited modulatory effects on purinergic and cholinergic enzymes involved in the prevention of platelet abnormality and consequent vascular complications in diabetic state.

Alterations of Na+/K+-ATPase, cholinergic and antioxidant enzymes activity by protocatechuic acid in cadmium-induced neurotoxicity and oxidative stress in Wistar rats.

BACKGROUND: This study assessed the possible protective mechanisms of protocatechuic acid (PCA) against cadmium (Cd)-induced oxidative stress and neurotoxicity in rats. METHODS: Male wistar strain rats weighing between 150-160g were purchased and acclimatized for two weeks. The rats were divided into seven groups of seven each; NC group received normal saline, CAD group received 6mg/kg of Cd-solution, CAD+PSG group received Cd-solution and prostigmine (5mg/kg), CAD+PCA-10 and CAD+PCA-20 groups received Cd-solution and PCA (10mg/kg and 20mg/kg) respectively, PCA-10 and PCA-20 groups received 10mg/kg and 20mg/kg PCA each. Animals were administered normal saline, Cd and PCA daily by oral gavage for 21days. After which the animals were sacrificed, the brain excised, homogenized and centrifuged. The activities of enzymes (Na+/K+-ATPase, cholinesterases, catalase, glutathione peroxidase, superoxide dismutase) and levels of oxidative stress markers (lipid peroxidation and reduced glutathione) linked to neurodegeneration were subsequently assessed. RESULTS: Significant (p<0.05) alterations in the enzyme activities and levels of oxidative stress markers were observed in CAD group when compared to the NC group. However, the activities of the enzymes were reversed in CAD+PSG and CAD+PCA groups. CONCLUSIONS: PCA may protect against cadmium-induced neurotoxicity by altering the activities of Na+/K+-ATPase, acetylcholinesterase, butyrylcholinesterase and endogenous antioxidant enzymes.

Modulatory Effects of Ferulic Acid on Cadmium-Induced Brain Damage.

Studies have shown the pharmacological relevance of phenolics like ferulic acid (FA) in promoting health. This study sought to investigate the modulatory effects of FA on cadmium-induced brain damage in rats. Brain damage was induced in Wistar strain rats by oral administration of cadmium (5 mg/kg body weight) for 21 days. Assays for malondialdehyde (MDA) content, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), monoamine oxidase (MAO), and Na(+)/K(+)-ATPase activities were carried out. The study revealed significant (P < .05) increases in the MDA content and all enzymes' (AChE, BChE, MAO, and Na(+)/K(+)-ATPase) activity investigated following cadmium administration. However, rats administered FA (10 and 20 mg/kg body weight) alongside cadmium significantly (P < .05) protected the brain by reversing the level of lipid peroxidation as measured by the MDA content as well as the enzymes' activity. This study, therefore, substantiates the neuroprotective potentials of FA especially in the management of cadmium-induced toxicity.

Modulatory effect of protocatechuic acid on cadmium induced nephrotoxicity and hepatoxicity in rats in vivo.

INTRODUCTION: This study sought to investigate the effect of protocatechuic acid (PCA); a phenolic compound readily available in most plant foods on cadmium-induced nephrotoxicity and hepatoxicity in rats. CASE DESCRIPTION: Thirty six adult male rats weighing about 150-160 g were acclimatized for 2 weeks and subsequently divided into six groups: Group 1 rats received normal saline (control group), group 2 rats were administered 5 mg Cd/kg body weight in form of solution orally (induced group), groups 3 and 4 received cadmium solution and different doses of PCA (10 and 20 mg/kg body weight) respectively, while groups 5 and 6 were the normal rats administered different doses of PCA (10 and 20 mg/kg) respectively in an experiment that lasted for twenty one days. The animals were sacrificed, the blood was collected and the serum was subsequently prepared. Furthermore, the liver was excised, homogenized and centrifuged to obtain the tissue homogenate used for the analyses. The serum was used for the determination of the total protein, urea, creatinine and uric acid levels while the liver homogenate was used for the estimation of alanine aminotransferase (ALT), aspartate transaminase (AST), and alkaline phosphatase (ALP). DISCUSSION AND EVALUATION: The result revealed that total protein level was reduced in cadmium induced toxicity rat group which was elevated upon treatment with PCA. Conversely, the elevated levels of urea, uric acid and creatinine in cadmium induced toxicity kidney rats were significantly (p < 0.05) reduced in PCA treated groups. Similarly, marked elevation in the ALT, AST and ALP activity were observed in cadmium induced toxicity rat group when compared with the control group. However, significant (p < 0.05) decrease in ALT, AST and ALP activity were noticed in groups administered different doses of PCA. CONCLUSIONS: The results from this study suggest that PCA may protect against cadmium-induced toxicity in the kidney and liver.

Anticholinesterase and Antioxidative Properties of Aqueous Extract of Cola acuminata Seed In Vitro.

Background. Cola acuminata seed, a commonly used stimulant in Nigeria, has been reportedly used for the management of neurodegenerative diseases in folklore without scientific basis. This study sought to investigate the anticholinesterase and antioxidant properties of aqueous extracts from C. acuminata seed in vitro. Methodology. The aqueous extract of C. acuminata seed was prepared (w/v) and its effect on acetylcholinesterase (AChE) and butyrylcholinesterase activities, as well as some prooxidant (FeSO4, sodium nitroprusside (SNP), and quinolinic acid (QA)) induced lipid peroxidation in rat brain in vitro, was investigated. Results. The results revealed that C. acuminata seed extract inhibited AChE (IC50 = 14.6 µg/mL) and BChE (IC50 = 96.2 µg/mL) activities in a dose-dependent manner. Furthermore, incubation of rat's brain homogenates with some prooxidants caused a significant increase P < 0.05 in the brain malondialdehyde (MDA) content and inhibited MDA production dose-dependently and also exhibited further antioxidant properties as typified by their high radicals scavenging and Fe(2+) chelating abilities. Conclusion. Inhibition of AChE and BChE activities has been the primary treatment method for mild Alzheimer's disease (AD). Therefore, one possible mechanism through which the seed exerts its neuroprotective properties is by inhibiting cholinesterase activities as well as preventing oxidative-stress-induced neurodegeneration. However, this is a preliminary study with possible physiological implications.

In Vitro Studies on the Antioxidant Property and Inhibition of α-Amylase, α-Glucosidase, and Angiotensin I-Converting Enzyme by Polyphenol-Rich Extracts from Cocoa (Theobroma cacao) Bean.

Background. This study sought to investigate the antidiabetic and antihypertensive mechanisms of cocoa (Theobroma cacao) bean through inhibition of α-amylase, α-glucosidase, angiotensin-1 converting enzyme, and oxidative stress. Methodology. The total phenol and flavonoid contents of the water extractable phytochemicals from the powdered cocoa bean were determined and the effects of the extract on α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities were investigated in vitro. Furthermore, the radicals [1,1-diphenyl-2 picrylhydrazyl (DPPH), 2,2..-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS), hydroxyl (OH), and nitric oxide (NO)] scavenging ability and ferric reducing antioxidant property of the extract were assessed. Results. The results revealed that the extract inhibited α-amylase (1.81 ± 0.22 mg/mL), α-glucosidase (1.84 ± 0.17 mg/mL), and angiotensin-1 converting enzyme (0.674 ± 0.06 mg/mL [lungs], 1.006 ± 0.08 mg/mL [heart]) activities in a dose-dependent manner and also showed dose-dependent radicals [DPPH (16.94 ± 1.34 mg/mL), NO (6.98 ± 0.886 mg/mL), OH (3.72 ± 0.26 mg/mL), and ABTS (15.7 ± 1.06 mmol/TEAC·g] scavenging ability. Conclusion. The inhibition of α-amylase, α-glucosidase, and angiotensin-1 converting enzyme activities by the cocoa bean extract could be part of the possible mechanism by which the extract could manage and/or prevent type-2 diabetes and hypertension.