A Compound Isolated from Phyllanthus tenellus Demonstrates Metabolic and Vascular Effects In Vitro

Planta Medica ◽  
2019 ◽  
Vol 86 (01) ◽  
pp. 78-84 ◽  
Author(s):  
Omar Estrada ◽  
Camilo Di Giulio ◽  
Radharani Dorta-Ledezma ◽  
Freddy Gonzalez-Mujica ◽  
Norma Motta ◽  
...  
Keyword(s):  
Metabolic Syndrome ◽  
Platelet Aggregation ◽  
High Glucose ◽  
Vascular Reactivity ◽  
Cardiovascular Complications ◽  
Scientific Basis ◽  
Phytochemical Analysis ◽  
Vascular Effects ◽  
Control Blood Glucose

AbstractCommon chronic conditions such as metabolic syndrome and diabetes are increasingly associated to metabolic and cardiovascular complications. Although Phyllanthus tenellus leaves have been used in decoctions as a popular remedy to control blood glucose levels and hypertension, its use needs a scientific basis. This study was therefore undertaken to report a phytochemical analysis of P. tenellus leaves and to test if the main active compound has potential to simultaneously tackle several pathophysiological features of metabolic syndrome and diabetes-related metabolic and vascular disorders such as hyperglycaemia, increased platelet activation, and endothelial dysfunction. We performed a partition of the methanolic extract of P. tenellus leaves among different organic solvents followed by chromatographic separation guided by the rat liver microsomal glucose-6-phosphatase assay. Two known tannins were identified by spectroscopic methods as pinocembrin-7-O-[3″-O-galloyl-4″,6″-(S)-hexahydroxydiphenoyl]-α-D-glucose, named P7OG by us, and gemin D. The structural determination of the isolated compounds was based on spectral data. The ability of the main active component, P7OG, to inhibit human platelet aggregation and to modify vascular reactivity of rat aortic rings incubated with high glucose (D-glucose 55 mM) was then evaluated. P7OG was further able to inhibit platelet aggregation induced by adenosine 5′-diphosphate and collagen, showed vasorelaxant effects in arteries precontracted with phenylephrine, and reverted the endothelium-dependent impairment effect of high glucose in rat aortic rings. In conclusion, one tannin isolated from P. tenellus showed promising metabolic, antiaggregant, and vascular effects, which suggests the potential beneficial use of P. tenellus to tackle complex cardiometabolic diseases.

scholarly journals Phytochemical Screening and in vitro Antioxidant Properties of Methanol and Aqueous Leaf Extracts of Geophila obvallata

2018 ◽  
pp. 1-11
Author(s):  
Iserhienrhien Lucky Osafanme ◽  
Okolie Paulinus Ngozi
Keyword(s):  
Aqueous Extract ◽  
Methanol Extract ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Scientific Basis ◽  
Phytochemical Analysis ◽  
Leaf Extracts ◽  
Reducing Ability

Aim: This study investigated the phytochemical constituents and in vitro antioxidant properties of methanol and aqueous leaf extracts of Geophila obvallata using standard methods. Materials and Methods: The in vitro antioxidant assays carried out were 1, 1‐diphenyl‐2‐picrylhydrazyl (DPPH) radical scavenging ability, Nitric oxide (NO•) radical scavenging activity assay, 2, 2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid) (ABTS•+) radical cation scavenging assay, ferric reducing properties and hydroxyl radical scavenging assays. Results: Phytochemical analysis revealed the presence of alkaloids, flavonoids, phenolic compounds, steroids, saponins, terpernoids and cardiac glycosides in both extracts. Relative to the aqueous extract, the methanol extract contained a higher amount of the secondary metabolites. However, both extracts exhibited appreciable and dose-dependent capacities for quenching DPPH, ABTS•+ and NO• free radicals, and potent ferric reducing ability to levels comparable to those of ascorbic acid. The crude methanol extract showed significantly increased (P<0.05) antioxidant activity than the aqueous extract. Conclusion: It was concluded that the extract possesses strong antioxidant properties due to its content of phytochemicals, and provides scientific basis for its ethno medicinal applications.

Improvement of endothelial function in insulin-resistant carotid arteries treated with pravastatin

2001 ◽  
Vol 95 (3) ◽  
pp. 466-471 ◽  
Author(s):  
Aaron S. Dumont ◽  
M. Eric Hyndman ◽  
Randall J. Dumont ◽  
Paul M. Fedak ◽  
Neal F. Kassell ◽  
...  
Keyword(s):  
Risk Factors ◽  
Endothelial Function ◽  
Vascular Reactivity ◽  
No Production ◽  
Vascular Effects ◽  
Content Type ◽  
Insulin Resistant ◽  
Induced Hypertension ◽  
Fine Print

Object. Insulin resistance and hypertension are independent risk factors for stroke. Endothelial dysfunction in response to risk factors and carotid artery (CA) disease are important in the pathogenesis of stroke. Pravastatin may have cholesterol-independent pleiotropic effects. In the present study the authors examined the effects of short-course pravastatin treatment on endothelial function in CAs obtained in control and insulin-resistant rats with fructose-induced hypertension. Methods. Thirty rats were divided into two experimental groups, in which 14 were fed a regular diet and 16 were fed a fructose-enriched diet for 3 weeks. The rats were then divided into four groups: control, pravastatin-treated control, fructose-fed, and pravastatin-treated fructose-fed. Pravastatin was administered (20 mg/kg/day) for 2 weeks. Excretion of the urinary nitric oxide (NO) metabolite nitrite (NO2−) was also assayed. The CAs from all rats were subsequently removed and assessed for endothelium-dependent and -independent vascular reactivity in vitro. The rats in the fructose-fed group were insulin resistant, hyperinsulinemic, and hypertensive relative to the rats in the control and pravastatin-treated control groups and exhibited diminished endothelium-dependent vasomotion and urinary NO2− excretion (p < 0.05), with preserved endothelium-independent vasomotion. Strikingly, pravastatin treatment restored endothelium-dependent vasomotion and urinary NO2− excretion in rats in the fructose-fed pravastatin-treated relative to the fructose-fed group (p < 0.05). Conclusions. The authors report, for the first time, that pravastatin restores endothelial function in CAs from insulin-resistant rats with fructose-induced hypertension. These beneficial effects were ascribed to direct, cholesterol-independent vascular effects of pravastatin and are likely the result of augmentation of NO production. These data provide impetus for further investigation of nonlipid-lowering indications for pravastatin therapy in the prevention and treatment of CA disease.

scholarly journals Atheroprotective Properties of Costus spicatus (Jacq.) Sw. in Female Rats

Life ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 212
Author(s):  
Bethânia Rosa Lorençone ◽  
Lucas Pires Guarnier ◽  
Rhanany Alan Calloi Palozi ◽  
Paulo Vitor Moreira Romão ◽  
Aline Aparecida Macedo Marques ◽  
...  
Keyword(s):  
Vascular Reactivity ◽  
Density Lipoprotein ◽  
Anatomical Study ◽  
Scientific Basis ◽  
Female Rats ◽  
Prolonged Treatment ◽  
Histopathological Analysis ◽  
Phytochemical Analysis ◽  
Medicinal Species ◽  
Soluble Adhesion Molecules

Background: Costus spicatus (Jacq.) Sw. is a medicinal species frequently prescribed for the treatment of cardiovascular diseases. This study aims to evaluate the effects of this species against the development of atherosclerosis. Methods: First, an anatomical study of the C. spicatus leaves was performed. Then, the extract (ESCS) was obtained and submitted to phytochemical analysis. Female rats were treated with a single dose of ESCS (2000 mg/kg) to assess acute toxicity. Other groups of female rats received an atherogenic diet for 60 days. After 30 days, the animals were treated orally with ESCS (30 and 300 mg/kg), rosuvastatin (5 mg/kg), or vehicle once daily for 30 days. Serum lipids oxidized low-density lipoprotein, soluble adhesion molecules, interleukins 1β and 6, and markers of renal and liver function were measured. Renal function, blood pressure, electrocardiography, and vascular reactivity were also evaluated. Arteries, heart, liver, and kidney were also collected to evaluate the tissue redox state and histopathological analysis. Results: Prolonged treatment with ESCS induces significant hypolipidemic and antioxidant effects, that prevent endothelial dysfunction and modulated the local inflammatory process, reducing the evolution of the atherosclerotic disease. Conclusions: This study provides a scientific basis for the popular use of C. spicatus for the treatment of atherosclerosis.

scholarly journals Thrombocytic activity in patients with arterial hypertension associated with metabolic syndrome

2017 ◽  
Vol 95 (8) ◽  
pp. 719-723
Author(s):  
Il’ya N. Medvedev
Keyword(s):  
Metabolic Syndrome ◽  
Lipid Peroxidation ◽  
Platelet Aggregation ◽  
Arterial Hypertension ◽  
Plasma Lipid ◽  
Platelet Activity ◽  
Aggregation Activity ◽  
Grade Iii

This work was aimed to elucidate the level of in vitro and in vivo aggregation activity of platelets and the functional significance of individual mechanisms of its regulation in patients with grade III arterial hypertension and metabolic syndrome. The study included 29 adult patients (15 men and 14 women) and 25 clinically healthy subjects of similar age. Biochemical, hematological and statistical methods were used. Marked dyslipidemia was associated with active lipid peroxidation. Plasma thromboxane B2 level was increased by 84,8% while 6-ketoprostaglandin F1α level was decreased by 17,9% and the total amount of NO metabolites by 28,7%. The degree of platelet aggregation and their aggregation with collagen 25,0 and 27,5% lower than the respective control values while the respective indices of their aggregation with ristomycin were 25,7 and 46,4% higher. The degree of platelet aggregation and their aggregation with ADP inducer were 25,7 and 58,4% higher than in control while the platelet-discocyte levels were reduced to 48,6 ± 0,4%. The sum of active platelet forms reached 51,4 ± 0,12% vs 17,9 ± 0,09% in control was, the number of small and large aggregates 18,6 ± 0,08 and 5,4 ± 0,04 per 1000 free platelets respectively vs 2,9 ± 0,06 и 0,2 ± 0,06 in control. Excess platelet activity in the patients was due to their enhanced adhesive and aggregative potential and reduced ability to disaggregate. The most important causs of thrombocytopathy was AH, negative changes in plasma lipid composition, and enhanced lipid peroxidation.

Sirtuin 1 stabilization by HuR represses TNF-α- and glucose-induced E-selectin release and endothelial cell adhesiveness in vitro: relevance to human metabolic syndrome

2014 ◽  
Vol 127 (7) ◽  
pp. 449-461 ◽  
Author(s):  
Giulio Ceolotto ◽  
Saula Vigili De Kreutzenberg ◽  
Arianna Cattelan ◽  
Aline S. C. Fabricio ◽  
Elisa Squarcina ◽  
...  
Keyword(s):  
Metabolic Syndrome ◽  
Cell Adhesion ◽  
Endothelial Cell ◽  
High Glucose ◽  
Protein A ◽  
Sirtuin 1 ◽  
Sirt1 Expression ◽  
The Metabolic Syndrome ◽  
Tnf Α

Overexpression of SIRT1 and of HuR protein, a SIRT1 mRNA stabilizer, prevents TNF-α- and high-glucose-induced E-selectin release and cell adhesion. As a result, SIRT1 stabilization by HuR is reduced, SIRT1 expression is lower, and plasma E-selectins are increased in the patients with the metabolic syndrome.

scholarly journals The Imbalance of Mitochondrial Fusion/Fission Drives High-Glucose-Induced Vascular Injury

Biomolecules ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 1779
Author(s):  
Yunsi Zheng ◽  
Anqi Luo ◽  
Xiaoquan Liu
Keyword(s):  
Vascular Injury ◽  
High Glucose ◽  
Temporal Dynamics ◽  
Early Stage ◽  
Cardiovascular Complications ◽  
Mitochondrial Fusion ◽  
Cellular Apoptosis ◽  
Glucose Exposure

Emerging evidence shows that mitochondria fusion/fission imbalance is related to the occurrence of hyperglycemia-induced vascular injury. To study the temporal dynamics of mitochondrial fusion and fission, we observed the alteration of mitochondrial fusion/fission proteins in a set of different high-glucose exposure durations, especially in the early stage of hyperglycemia. The in vitro results show that persistent cellular apoptosis and endothelial dysfunction can be induced rapidly within 12 hours’ high-glucose pre-incubation. Our results show that mitochondria maintain normal morphology and function within 4 hours’ high-glucose pre-incubation; with the extended high-glucose exposure, there is a transition to progressive fragmentation; once severe mitochondria fusion/fission imbalance occurs, persistent cellular apoptosis will develop. In vitro and in vivo results consistently suggest that mitochondrial fusion/fission homeostasis alterations trigger high-glucose-induced vascular injury. As the guardian of mitochondria, AMPK is suppressed in response to hyperglycemia, resulting in imbalanced mitochondrial fusion/fission, which can be reversed by AMPK stimulation. Our results suggest that mitochondrial fusion/fission’s staged homeostasis may be a predictive factor of diabetic cardiovascular complications.

High Glucose, but Not Testosterone, Increases Platelet Aggregation Mediated by Endothelial Cells

2015 ◽  
Vol 4 (3) ◽  
pp. 205
Author(s):  
Ikhlas Muhammad Jenie ◽  
Budi Mulyono ◽  
Soedjono Aswin ◽  
Sri Kadarsih Soejono
Keyword(s):  
Endothelial Cells ◽  
Platelet Aggregation ◽  
High Glucose ◽  
Platelet Rich Plasma ◽  
Umbilical Vein ◽  
In Vitro Study ◽  
Traditional Risk Factor ◽  
Main Effect ◽  
Effect Of Glucose

Endothelial cells inhibit platelet aggregation by releasing thromboregulators, such as prostacyclin and nitric oxide. Male subject is a traditional risk factor for cardiovascular diseases. Platelet hyperreactivity has been frequently found in patient with diabetes mellitus. To examine whether testosterone and high glucose modify platelet aggregation through endothelial cells, we did an in vitro study using endothelial cells culture from human umbilical vein (HUVEC). Treatments were performed in HUVEC sub culture as either normoglucose (5.6 mM) or high glucose (22.4 mM) medium, with or without testosterone (0, 1, 10, 100 nM), for 24 hours. HUVEC were trypsinized, resuspended, and then incubated with platelet rich plasma from healthy male donors with ratio 1:10<sup>4</sup> for 3 minutes. Platelet aggregation measured by turbidimetry methode. This study showed that testosterone did not significantly influence platelet aggregation through endothelial cells in normoglucose (<em>p </em>= 0.144) or high glucose (<em>p </em>= 0.916) medium. There was no main effect of testosterone (<em>p </em>= 0.73) as well as no interaction between testosterone and glucose (<em>p </em>= 0.69), but there was a main effect of glucose (<em>p </em>= 0.004), to platelet aggregation through endothelial cells. In conclusion, high glucose, but not testosterone, inhibits platelet aggregation mediated by endothelial cells.

Effect of Vaccinium dunalianum Glycoside on Platelet Aggregation in Animals

2013 ◽  
Vol 634-638 ◽  
pp. 1229-1235
Author(s):  
Fei Fei Liu ◽  
Hui Ling Liu ◽  
Jian Xin Cao
Keyword(s):  
Platelet Aggregation ◽  
Vascular Diseases ◽  
Inhibitory Effect ◽  
Scientific Basis ◽  
High Yield ◽  
In Vitro Tests ◽  
High Dose ◽  
Traditional Use ◽  
Experimental Hyperlipidemia

1-O-(p-hydroxyphenyl)-6-O-caffeoyl-β-D-glucoside (PPCG) was isolated in extraordinary high yield from the dried buds of Vaccinium dunalianum. The present study was aimed to investigate the effect of PPCG on platelet aggregation in animals. In in vitro tests, PPCG showed an inhibitory effect on ADP/PAF-induced platelet aggregation. PPCG significantly prolonged the mice bleeding and clotting time. PPCG (100 and 200 mg/kg) dose dependently reduced mortality of ADP-induced acute pulmonary thromboembolism mice to 80% and 70%, respectively, a high dose (200 mg/kg) of that can reduce serum TC and TG levels of the experimental hyperlipidemia animals, but cannot lower blood viscosity. The observations provide a scientific basis for traditional use of this plant for the treatment of articular rheumatism. Furthermore, these results also suggested that PPCG had anti-thromboembolic effects and good prospects for drug development of cardio-cerebral vascular diseases.

scholarly journals Kinetics of α-amylase and α-glucosidase Inhibitory Potential of Hermannia geniculata Eckl. & Zehl root Extracts Used in Basotho Traditional Medicine.

2020 ◽  
Vol 2 (2) ◽  
pp. 105-120
Author(s):  
L. A. Adeniran ◽  
A. O. T. Ashafa
Keyword(s):  
Diabetes Mellitus ◽  
Traditional Medicine ◽  
Competitive Inhibition ◽  
Radical Scavenging ◽  
Ethanol Extract ◽  
Kinetic Studies ◽  
Scientific Basis ◽  
Phytochemical Analysis ◽  
Root Extract

The scientific investigation of the folkloric use of Hermannia geniculata roots in the management of diabetes mellitus was conducted. Phytochemical analyses, in vitro antioxidant and hyperglycaemic studies were carried out on the crude extracts of H. geniculata. Qualitative phytochemical analysis revealed the presence of saponins, phenols, flavonoids, alkaloids, tannins, phytosterols, triterpenes and anthraquinones. The ethanol extract exhibited the highest free radical scavenging capability with the lowest IC values (0.52, 0.38, 0.59, 0.63, 0.39) mg/mL for 50 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2-Azino-bis(3-ethylbenzothiazoline-6-Sulphonic acid (ABTS), hydroxyl radical, superoxide anion radical and metal chelating ability which is significantly different (p<0.05) from the standard (silymarin). In antidiabetic studies, ethanol extract is a potent inhibitor of α-glucosidase (IC : 0.15 mg/mL) which is lower and significantly 50 different (p<0.05) from the standard (acarbose) IC value of (0.52 mg/mL). Ethanol extract 50 exhibited a milder inhibition of α-amylase enzyme with IC (0.57mg/mL) which is higher and 50 significantly different (p<0.05) from acarbose with IC (0.47 mg/mL). Kinetic studies revealed H. 50 geniculata ethanol extract exhibited competitive inhibition of α-amylase and uncompetitive inhibition of α-glucosidase enzymes. All these findings provided the scientific basis which support the use of the root extract of H. geniculata in the management of diabetes mellitus and oxidative stress induced ailments like colitis and ulcers by the Basotho traditional medicine of South Africa.

Sign in / Sign up

Export Citation Format

Share Document