scholarly journals PHYTOCHEMICAL SCREENING AND IN VITRO ANTIOXIDANT AND ANTI-DIABETIC POTENTIALS OF PERSEA AMERICANA MILL. (LAURACEAE) FRUIT EXTRACT

2018 ◽  
Author(s):  
Mahadeva Rao US
Keyword(s):  
Therapeutic Potential ◽  
Kinetic Studies ◽  
Inhibitory Effect ◽  
Persea Americana ◽  
Phytochemical Screening ◽  
Fruit Extract ◽  
Avocado Fruit ◽  
Percentage Yield ◽  
Hydrolyzing Enzymes

Diabetes mellitus (DM) is a metabolic disorder characterized by insulin resistance and pancreatic β-cell dysfunction and the management of blood glucose level is an important strategy in the control of the disease and complications associated with it. Therefore, components that cause uptake of glucose from the bloodstream and inhibitors of carbohydrate hydrolyzing enzymes can be useful in treatment of DM and medicinal plants are often used to achieve this aim. Avocado fruit is rich in phytochemicals necessary for treatment of DM. The purpose of this study was to investigate the inhibitory effect of Persea americana fruit extracts on α-amylase and α-glucosidase enzymes. The percentage yield, phytochemical screening (both qualitative and quantitative), in vitro antioxidant and anti-diabeticassays, and kinetic studies were performed with different solvent extracts of Avocado fruit pulp. Results: Avocado hadgreat and promising potential as pharmaceutical agent, particularly to be developed as anti-diabetic through the inhibition of α-glucosidase and α- amylase enzymes.  In vitro studies of the antioxidant activity of the fruit extract gaveanevidence and strong biochemical rationale of their therapeutic potential. The fruit extract of P. americana may play an important role in the development of nutraceuticals and also in the management of oxidative stress induced DM.

scholarly journals Phytochemical Constituents and In Vitro Anti-Diabetic Properties of Ziziphus jujubа (Rhamnaceae) Fruits

2017 ◽  
Vol 9 (2) ◽  
Author(s):  
Stoilova I ◽  
Trifonova D. ◽  
Marchev A. ◽  
Stanchev V. ◽  
Angelova G. ◽  
...  
Keyword(s):  
Phenolic Acids ◽  
Ethanol Extract ◽  
Kinetic Studies ◽  
Inhibitory Effect ◽  
Total Phenolic ◽  
Fruit Extract ◽  
Quercetin Glycosides ◽  
Dried Extract ◽  
High Inhibition

In the current study the phytochemical profile of 70% ethanol extract of Ziziphus jujubа (Rhamnaceae), cultivated in Bulgaria has been investigated. The fruit extract contained numerous phytochemicals, such as triterpenes, phenolic acids and flavonoids. Five triterpenes, 11 phenolic acids and 5 flavonoids have been identified. The fruit extract had a total phenolic content of 21.62 ± 0.0265 mg/g and total flavonoid content 1.34 ± 0.017 mg/g dried extract. Among the triterpenes with the highest concentration was the betulinic acid 20943.17±527.06 µg/g dried extract, rosmarinic acid (1174.26±29.55 µg/g) among the phenolic acids, followed by myricetin (214.61±5.40 µg/g) as a representative of flavonoids and rutin 3 046.89±76.68 among the quercetin glycosides. The inhibitory effect of Z. jujubа fruit extract has been investigated on the key enzymes linked to diabetes – α-glucosidase and α-amylase. In order to evaluate the type of inhibition a Lineweaver-Burk plot was produced. The results obtained from the enzyme kinetic studies exhibited a mixed noncompetitive-uncompetitive type of inhibition on α-glucosidase and mixed competitive-non-competitive type of inhibition on α-amylase. Besides that the obtained results proved high inhibition of α-glucosidase (79.46% at 1.33 mg.ml-1 extract) and moderate inhibition of α-amylase (39.10% at 0.666 mg.ml-1 extract concentration). These results suggest the possible use of fruits of Z. jujubа in the management of diabetes mellitus.

Aqueous extracts of avocado pear (Persea americana Mill.) leaves and seeds exhibit anti-cholinesterases and antioxidant activities in vitro

2016 ◽  
Vol 27 (2) ◽  
Author(s):  
Ganiyu Oboh ◽  
Veronica O. Odubanjo ◽  
Fatai Bello ◽  
Ayokunle O. Ademosun ◽  
Sunday I. Oyeleye ◽  
...  
Keyword(s):  
Leaf Extract ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Seed Extract ◽  
Persea Americana ◽  
Dependent Manner ◽  
Natural Treatment

AbstractAvocado pear (The inhibitory effects of extracts on AChE and BChE activities and antioxidant potentials (inhibition of FeThe extracts inhibited AChE and BChE activities and prooxidant-induced TBARS production in a dose-dependent manner, with the seed extract having the highest inhibitory effect and the leaf extract exhibiting higher phenolic content and radical scavenging abilities, but lower Fe chelation ability compared with that of the seed. The phytochemical screening revealed the presence of saponins, alkaloids, and terpenoids in both extracts, whereas the total alkaloid profile was higher in the seed extract than in the leaf extract, as revealed by GC-FID.The anti-cholinesterase and antioxidant activities of avocado leaf and seed could be linked to their phytoconstituents and might be the possible mechanisms underlying their use as a cheap and natural treatment/management of AD. However, these extracts should be further investigated in vivo.

scholarly journals Garlic Extract: Inhibition of Biochemical and Biophysical Changes in Glycated HSA

2021 ◽  
Vol 11 (22) ◽  
pp. 11028
Author(s):  
Mohd W. A. Khan ◽  
Ahmed A. Otaibi ◽  
Arwa F. M. Alhumaid ◽  
Abdulmohsen K. D. Alsukaibi ◽  
Asma K. Alshamari ◽  
...  
Keyword(s):  
Structural Changes ◽  
Therapeutic Potential ◽  
Inhibitory Effect ◽  
Significant Inhibition ◽  
Garlic Extract ◽  
Diabetic Patients ◽  
Age Related ◽  
Health Complications ◽  
Biophysical Changes

Glycation of various biomolecules contributes to structural changes and formation of several high molecular weight fluorescent and non-fluorescent, advanced glycation end products (AGEs). AGEs and glycation are involved in various health complications. Synthetic medicines, including metformin, have several adverse effects. Natural products and their derivatives are used in the treatment of various diseases due to their significant therapeutic qualities. Allium sativum (garlic) is used in traditional medicines because of its antioxidant, anti-inflammatory, and anti-diabetic properties. This study aimed to determine the anti-glycating and AGEs inhibitory activities of garlic. Biochemical and biophysical analyses were performed for in vitro incubated human serum albumin (HSA) with 0.05 M of glucose for 1, 5, and 10 weeks. Anti-glycating and AGEs inhibitory effect of garlic was investigated in glycated samples. Increased biochemical and biophysical changes were observed in glycated HSA incubated for 10 weeks (G-HSA-10W) as compared to native HSA (N-HSA) as well as glycated HSA incubated for 1 (G-HSA-1W) and 5 weeks (G-HSA-5W). Garlic extract with a concentration of ≥6.25 µg/mL exhibited significant inhibition in biophysical and biochemical changes of G-HSA-10W. Our findings demonstrated that garlic extract has the ability to inhibit biochemical and biophysical changes in HSA that occurred due to glycation. Thus, garlic extract can be used against glycation and AGE-related health complications linked with chronic diseases in diabetic patients due to its broad therapeutic potential.

Phytochemical Screening and Anti-Diabetic Efficacy of O. Sanctum Seed Extract on Streptozotocin Induced Diabetic Rats

2017 ◽  
Vol 54 (3) ◽  
pp. 336
Author(s):  
Kavitha K. ◽  
Ponne S.
Keyword(s):  
Body Weight ◽  
Digestive Enzymes ◽  
Fasting Blood Glucose ◽  
Inhibitory Effect ◽  
Diabetic Rats ◽  
Seed Extract ◽  
Phytochemical Screening ◽  
Weight Changes

The present study was designed to assess the in vitro and in vivo anti-diabetic efficacy of <em>O. sanctum</em> seed and its phytochemical screening. In vitro inhibitory effect on carbohydrate digestive enzymes like α-amylase and α-glucosidase and in vivo parameters such as fasting blood glucose and body weight changes were studied, a potent inhibitory effect was observed on activities of digestive enzymes and a marked decrease in the glucose level in the <em>O. sanctum</em> seed extract treated streptozotocin induced diabetic rats was noted. Further a marked reduction in body weight was also observed.

scholarly journals Synthesis and In Vitro Screening of Novel Heterocyclic β-d-Gluco- and β-d-Galactoconjugates as Butyrylcholinesterase Inhibitors

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2833
Author(s):  
Krešimir Baumann ◽  
Lorena Kordić ◽  
Marko Močibob ◽  
Goran Šinko ◽  
Srđanka Tomić
Keyword(s):  
Active Site ◽  
Kinetic Studies ◽  
Inhibitory Effect ◽  
In Vitro Screening ◽  
Sugar Moiety ◽  
Brain Barrier Permeability ◽  
The Central Nervous System ◽  
Key Residues ◽  
Micromolar Range

The development of selective butyrylcholinesterase (BChE) inhibitors may improve the treatment of Alzheimer’s disease by increasing lower synaptic levels of the neurotransmitter acetylcholine, which is hydrolysed by acetylcholinesterase, as well as by overexpressed BChE. An increase in the synaptic levels of acetylcholine leads to normal cholinergic neurotransmission and improved cognitive functions. A series of 14 novel heterocyclic β-d-gluco- and β-d-galactoconjugates were designed and screened for inhibitory activity against BChE. In the kinetic studies, 4 out of 14 compounds showed an inhibitory effect towards BChE, with benzimidazolium and 1-benzylbenzimidazolium substituted β-d-gluco- and β-d-galacto-derivatives in a 10–50 micromolar range. The analysis performed by molecular modelling indicated key residues of the BChE active site, which contributed to a higher affinity toward the selected compounds. Sugar moiety in the inhibitor should enable better blood–brain barrier permeability, and thus increase bioavailability in the central nervous system of these compounds.

Vitamin C inhibits the activation of the NLRP3 inflammasome by scavenging mitochondrial ROS

Inflammasome ◽  
2016 ◽  
Vol 2 (1) ◽  
Author(s):  
Xuesong Sang ◽  
Hongbin Wang ◽  
Yihui Chen ◽  
Qiuhong Guo ◽  
Ailing Lu ◽  
...  
Keyword(s):  
Vitamin C ◽  
Nlrp3 Inflammasome ◽  
Therapeutic Potential ◽  
Protein Complexes ◽  
Inhibitory Effect ◽  
Inflammasome Activation ◽  
Mitochondrial Ros ◽  
Regulatory Effects

AbstractInflammasomes are intracellular protein complexes that mediate maturation and secretion of the pro-inflammatory cytokines IL-1β and IL-18. Inflammasomes have been connected with various diseases, therefore the regulation of inflammasome activation is important for the development of novel therapies for many inflammatory syndromes. Vitamin C is an essential nutrient and has regulatory effects on immune cells. Here we report that vitamin C has an inhibitory effect on the activation of the NLRP3 inflammasome in vitro and in vivo. Mechanistically, this inhibition is through scavenging mitochondrial ROS but not through NF-κB inhibition. Moreover, specificity tests show that the AIM2 inflammasome and the NLRC4 inflammasome can also be inhibited by vitamin C. Our results have thus identified a new inflammasome regulator and provide therapeutic potential for inflammasome-associated diseases.

scholarly journals In-vitro Antivenom Potential of Solanum dasyphyllum Methanolic Leaf and Fruit Extracts against Naja nigricollis Venom

2020 ◽  
pp. 38-45
Author(s):  
Adewunmi Rofiat Funmilola ◽  
Gidado Abubakar ◽  
Zanna Hassan
Keyword(s):  
Medicinal Plants ◽  
Leaf Extract ◽  
Inhibitory Effect ◽  
Fruit Extract ◽  
Southwestern Part ◽  
Fruit Extracts ◽  
Snake Envenomation ◽  
The Family ◽  
Inhibitory Potential

Solanum dasyphyllum belongs to the family of plants called Solanaceae, it is commonly called "Africa eggplant" and one of the medicinal plants used in the treatment of snake envenomation in the southwestern part of Nigeria, but investigation concerning its anti-venom activity has not been established. The present study evaluates the in-vitroenzyme inhibition potential of S.dasyphyllum leaf and fruit extracts against Naja nigricollis (Black-necked spitting cobra) venom. The inhibitory potential of S. dasyphyllum leaf and fruit on proteases, acetylcholinesterase, phospholipase A2 and hyaluronidase enzymes present in the snake venom was evaluated. The methanolic leaf and fruit extracts of S. dasyphyllum inhibited the activity of all enzymes evaluated, however, the leaf extract exhibited better enzyme inhibitory effect on N. nigricollis venom when compared with the fruit. This could be due to the presence of various phytochemicals in leaf and fruit extract.  This result substantiates the ethnomedicinal usage of S. dasyphyllum and would help to develop potent antidote therapy against N. nigricollis envenomation.

A GPC1-targeted and gemcitabine-loaded biocompatible nanoplatform for pancreatic cancer multimodal imaging and therapy

Nanomedicine ◽  
2019 ◽  
Vol 14 (17) ◽  
pp. 2339-2353 ◽  
Author(s):  
Wenli Qiu ◽  
Huifeng Zhang ◽  
Xiao Chen ◽  
Lina Song ◽  
Wenjing Cui ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Cancer Detection ◽  
Multimodal Imaging ◽  
Near Infrared ◽  
Therapeutic Potential ◽  
Inhibitory Effect ◽  
In Vivo Studies ◽  
Blood Biochemical

Aim: Biomarker-targeted nanocarrier holds promise for early diagnosis and effective therapy of cancer. Materials & methods: This work successfully designs and evaluates GPC1-targeted, gemcitabine (GEM)-loaded multifunctional gold nanocarrier for near-infrared fluorescence (NIRF)/MRI and targeted chemotherapy against pancreatic cancer in vitro and in vivo. Results: Blood biochemical and histological analyses show that the in vivo toxicity of GPC1-GEM-nanoparticles (NPs) was negligible. Both in vitro and in vivo studies demonstrate that GPC1-GEM-NPs can be used as NIRF/MR contrast agent for pancreatic cancer detection. Treatment of xenografted mice with GPC1-GEM-NPs shows a higher tumor inhibitory effect compared with controls. Conclusion: This novel theranostic nanoplatform provides early diagnostic and effective therapeutic potential for pancreatic cancer.

scholarly journals Inhibitory Effect onIn VitroLDL Oxidation and HMG Co-A Reductase Activity of the Liquid-Liquid Partitioned Fractions ofHericium erinaceus(Bull.) Persoon (Lion’s Mane Mushroom)

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Mohammad Azizur Rahman ◽  
Noorlidah Abdullah ◽  
Norhaniza Aminudin
Keyword(s):  
Therapeutic Potential ◽  
Reductase Activity ◽  
Antioxidant Properties ◽  
Density Lipoprotein ◽  
Thiobarbituric Acid ◽  
Inhibitory Effect ◽  
Hexane Fraction ◽  
Ldl Oxidation ◽  
Hericium Erinaceus

Oxidation of low-density lipoprotein (LDL) has been strongly suggested as the key factor in the pathogenesis of atherosclerosis. Mushrooms have been implicated in having preventive effects against chronic diseases due especially to their antioxidant properties. In this study,in vitroinhibitory effect ofHericium erinaceuson LDL oxidation and the activity of the cholesterol biosynthetic key enzyme, 3-hydroxy-3-methyl glutaryl coenzyme A (HMG Co-A) reductase, was evaluated using five liquid-liquid solvent fractions consisting of methanol : dichloromethane (M : DCM), hexane (HEX), dichloromethane (DCM), ethyl acetate (EA), and aqueous residue (AQ). The hexane fraction showed the highest inhibition of oxidation of human LDL as reflected by the increased lag time (100 mins) for the formation of conjugated diene (CD) at 1 µg/mL and decreased production (68.28%, IC500.73 mg/mL) of thiobarbituric acid reactive substances (TBARS) at 1 mg/mL. It also mostly inhibited (59.91%) the activity of the HMG Co-A reductase at 10 mg/mL. The GC-MS profiling of the hexane fraction identified the presence of myconutrients:inter alia, ergosterol and linoleic acid. Thus, hexane fraction ofHericium erinaceuswas found to be the most potentin vitroinhibitor of both LDL oxidation and HMG Co-A reductase activity having therapeutic potential for the prevention of oxidative stress-mediated vascular diseases.

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