scholarly journals Pharmacological Modeling and Study for Antidiabetic Activity of Praecitrullus fistulosus Leaves Extracts

2020 ◽  
Vol 10 (4-s) ◽  
pp. 13-16
Author(s):  
Ashutosh Tiwari ◽  
C.K Tyagi ◽  
Harish Pandey ◽  
Sunil Kumar Shah
Keyword(s):  
Research Work ◽  
Ethanol Extract ◽  
Extraction Methods ◽  
Water Soluble ◽  
Antidiabetic Activity ◽  
In Vivo Models ◽  
Successive Extraction ◽  
Praecitrullus Fistulosus

Phytochemical and pharmacological investigations of leaves of Praecitrullus fistulosus for the antidiabetic activity have been done in our research work encompassed in depth and systematic screening of plant leaves and further extraction, characterization and bioevaluation. The research was envisaged for antidiabetic activity of different extracts procured by successive extraction methods and to find out or isolate the most possible active compounds from the active extracts showing the best activity. The antidiabetic activity of all extracts has been evaluated by STZ induced diabetes. The isolated compounds have been evaluated by in-vitro and in-vivo models. The alcohol soluble extractives values were found to be higher than water soluble extractive value. Alcohol being a moderately non polar solvent, able to extract polar and non-polar components yields higher extractive value. The ethanol extract shows significant enhancement in glucose tolerance in glucose fed hyperglycemic normal rats and produced a marked decrease in blood glucose levels at 200 mg/kg and 400 mg/kg body weight in streptozotocin-diabetic rats after 21 days treatment. Keywords: Praecitrullus fistulosus, Streptozotocin and Glibenclamide, diabetes, Pharmacological Evaluation

scholarly journals Antidiabetic Activity ofPterospermum acerifoliumFlowers and Glucose Uptake Potential of Bioactive Fraction in L6 Muscle Cell Lines with Its HPLC Fingerprint

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Rathinavelusamy Paramaguru ◽  
Papiya Mitra Mazumder ◽  
Dinakar Sasmal ◽  
Venkatesan Jayaprakash
Keyword(s):  
Glucose Uptake ◽  
Fasting Blood Glucose ◽  
Ethanol Extract ◽  
Ethyl Acetate Fraction ◽  
Diabetic Control ◽  
Antidiabetic Activity ◽  
Peripheral Tissues ◽  
Hplc Fingerprint

The present study was designed to estimate the detailed antidiabetic activity ofPterospermum acerifolium(L.) Willd flowers.In vitroalpha amylase inhibition study was carried out on 50% ethanol extract of flowers (PAFEE) and its various fractions. The active ethyl acetate fraction (PAFEF) was subfractionated into three subfractions (PAFE1, PAFE2, and PAFE3) and subjected to acute toxicity studies followed by antidiabetic screeningin vivoby streptozotocin-nicotinamide induced type II diabetes. Diabetic animals treated with PAFE2 (30 mg/kg) reduced the levels of fasting blood glucose, significantly (P<0.001) compared to that of diabetic control animals. Histological studies on drug treated groups did not show remarkable positive changes inβ-cells. PAFE2 showed32.6±1.93% glucose uptake over control and, in the presence of PI3K inhibitor wortmannin, declined to13.7±2.51%. HPLC analysis of PAFE2 reveals the presence of quercetin and apigenin as major constituents and both are inhibiting the glycogen phosphorylase enzyme in molecular modelling studies. The study evidenced strongly that the probable glucose lowering mechanism of action of active subfraction PAFE2 is by increasing the glucose uptake in peripheral tissues and by inhibition of gluconeogenesis.

scholarly journals BIOASSAY-GUIDED EVALUATION OF FICUS SEMICORDATA FOR ANTIDIABETIC ACTIVITY

2017 ◽  
Vol 9 (3) ◽  
pp. 71 ◽  
Author(s):  
Virender Kaur ◽  
Kumud Upadhyaya ◽  
Milind Pande
Keyword(s):  
Diabetes Mellitus ◽  
Early Stage ◽  
Ethanol Extract ◽  
Postprandial Hyperglycemia ◽  
Alpha Amylase ◽  
Antidiabetic Activity ◽  
Biological Studies

Objective: The early stage of diabetes mellitus type 2 is associated with postprandial hyperglycemia. The therapeutic approach involved in the treatment of type 2 diabetes mellitus is the use of agents that can decrease postprandial hyperglycemia by inhibiting carbohydrate digesting enzymes. In an effort of identifying herbal drugs which may become useful in the prevention or mitigation of diabetes, the antidiabetic activity of Ficus semicordata (FS) and its constituents were studied. The present study was undertaken in part to identify the potent antihyperglycemic fraction from the ethanol extract of the plant, using bioassay guided evaluation.Methods: The ethanol extract of Ficus semicordata were fractionated to obtain chloroform, ethyl acetate, n-butanol and ethanol extracts which were tested for alpha-amylase, alpha-glucosidase inhibitory, properties. Further fractionation of the more active ethanol fraction yielded isolates FS-1 and FS-2 which were tested for in vivo antidiabetic activity using Streptozotocin (STZ)-induced diabetic rats.Results: Ethanol extract from leaves of the plant showed notable alpha-amylase (IC50 = 3.352µg/ml and alpha-glycosidase inhibitory activity (IC50= 3.448µg/ml) as compared to standard acarbose (IC50 = 3.175µg/ml. Subfraction FS-1 and FS-2 which were tested for in vivo antidiabetic activity using acute STZ-induced diabetic rats significantly (*p<0.05, **p<0.01, *** p<0.001) reduced blood glucose level.Conclusion: The Ficus semicordata plant extracts and the fractionated components could be used as a natural antidiabetic after comprehensive in vitro and in vivo biological studies.

scholarly journals Protective effects of orally applied fullerenol nano particles in rats after a single dose of doxorubicin

2011 ◽  
Vol 65 (3) ◽  
pp. 329-337 ◽  
Author(s):  
Ivana Icevic ◽  
Aleksandar Vukmirovic ◽  
Branislava Srdjenovic ◽  
Jan Sudji ◽  
Aleksandar Djordjevic ◽  
...  
Keyword(s):  
Biological Activity ◽  
Single Dose ◽  
Antioxidant Properties ◽  
Water Soluble ◽  
Nano Particles ◽  
Protective Effects ◽  
In Vivo Models ◽  
Nephroprotective Effect

Polyhydroxylated, water soluble, fullerenol C60(OH)24 nano particles (FNP) in vitro and in vivo models, showed an expressive biological activity. The goal of this work was to investigate the potential protective effects of orally applied FNP on rats after a single dose of doxorubicin (DOX) (8 mg/kg (i.p.)) 6 h after the last application of FNP. After the last drug administration, the rats were sacrificed, and the blood and tissues were taken for the analysis. Biochemical and pathological results obtained in this study indicate that fullerenol (FNP), in H2O:DMSO (80:20, w/w) solution given orally in final doses of 10, 14.4, and 21.2 mg/kg three days successively, has the protective (hepatoprotective and nephroprotective) effect against doxorubicin-induced cytotoxicity via its antioxidant properties.

scholarly journals Exploration of Antidiabetic Activity of Stephania japonica Leaf Extract in Alloxan-Induced Swiss Albino Diabetic Mice

2019 ◽  
pp. 1-12
Author(s):  
Md. Dobirul Islam ◽  
Syeda Farida Akter ◽  
Md. Amirul Islam ◽  
Md. Salim Uddin
Keyword(s):  
Gallic Acid ◽  
Ethanol Extract ◽  
Antidiabetic Activity ◽  
Diabetic Mice ◽  
Mice Model ◽  
Leaf Extracts ◽  
Alternative Source ◽  
Dry Extract

Aims: Presently the medicinal world is rapidly turning more on the therapeutic health benefits of natural product and medicinal plants in the management of major crucial disease and their complications. Medicinal plant, Stephania japonica has been studied for exploring antidiabetic potentiality as an alternative source of medicine against the global threat of Diabetes mellitus (DM). Methods: The extraction of S. japonica leaf was carried out by acetone and ethanol. Phytochemical screening and quantitative analysis of S. japonica leaf extracts were evaluated through chemically forming characterized color formation and calibration method respectively, by using standard reference substances (ascorbic acid, gallic acid, and quercetin) to assess the probable compounds present in the extract. Anti-diabetic potentiality of highest phytochemicals containing two extracts were investigated in in vitro as a ⍺-amylase inhibitors and in vivo through alloxan-induced Swiss albino diabetes mice model. Results: Alkaloids, carbohydrates, steroids, flavonoids, resins, saponins, tannins and coumarins were present in the leaf extracts. The estimated amount of total phenolics, flavonoids, flavonols and proanthrocyanidins contents of acetone and ethanol extract were 92.12±0.64 and 56.54±1.05 mg of gallic acid equivalent (GAE)/gm of dry extract, 66.02±1.42 and 46.17±0.54 mg of catechin equivalent (CAE)/gm of dry extract, 7.05±0.108 and 5.26±0.083 mg of quercetin equivalent (QUE)/gm of dry extract, 35.19±0.67 and 9.55±1.11 mg CAE/gm of dry extract, respectively. In 3, 5-dinitrosalicylic acid method, acetone and ethanol extract showed α-amylase inhibition of 51.02% and 46.62%, respectively at the concentration of 1000 µg/mL whereas in starch iodine color assay, acetone and ethanol extract showed inhibition of 57.32% and 52.12%, respectively at the concentration of 800 µg/mL. In contrast, both of the leaf extracts significantly (p<0.05 to p<0.001) improved the lipid profile parameters, blood glucose level and serum hepatic marker proteins in alloxan-induced diabetic mice. Conclusion: The present study strongly concluded that S. japonica leaf extracts process potent antidiabetic potentiality that might be significance for the management of diabetes and its complications.

EXTH-57. EFFICACY OF SOLUBLE PANOBINOSTAT (MTX110) IN PRECLINICAL MODELS OF ADULT GLIOBLASTOMA

2021 ◽  
Vol 23 (Supplement_6) ◽  
pp. vi176-vi176
Author(s):  
Greg Palmer ◽  
Stephen T Keir ◽  
David M Ashley ◽  
Rhian Davies ◽  
Ben Williams ◽  
...  
Keyword(s):  
Cell Viability ◽  
Cell Lines ◽  
Radiation Treatment ◽  
Water Soluble ◽  
Soluble Form ◽  
Cell Viability Assay ◽  
In Vivo Models ◽  
Drug Concentrations

Abstract INTRODUCTION One of the biggest challenges in treating glioblastoma is achieving effective local drug concentrations, and trials using systemic administration of therapeutics have failed in GBM despite compelling pre-clinical evidence. MTX110 (Midatech Pharma PLC) is a water-soluble form of panobinostat currently in clinical development for DIPG and medulloblastoma using direct tumor delivery. We have previously reported a significant positive benefit of MTX110 in a subcutaneous GBM mouse model in an IDH1 mutated cell line. Here we present follow on data on the potential for MTX110 synergy with radiation in pre-clinical in vivo models. We also present data on efficacy of MTX110 in a panel of GBM cell lines. METHODS In vitro: Cell lines were incubated with MTX110 for 72h over a range of concentrations (1nM-10µM). Each concentration was tested in triplicate with the appropriate blank controls included in each plate. After 72 hours, cell viability was measured via luminescence signal (Promega CellTiter-Glo Luminescent Cell Viability Assay kit (Promega-G7573) read via 2104 EnVision Multilabel Reader, PerkinElmer. In vivo: Tumor-bearing mice were stratified to either the vehicle control or treatment group based on median tumor volume and were treated with MTX110 at a dose of 15mg/kg IP, 5 days consecutively for 2 consecutive weeks, following radiation treatment at a dose of 4Gy delivered as a single fraction on day 1. RESULTS In vitro, MTX110 demonstrated cytotoxic activity in 4 GBM cell lines (U87MG, U251MG, U118MG and T98G) with an average IC50 value in the region of 40nM (17-43nM). In vivo MTX110 in combination with radiation treatment showed an enhanced delay in tumor growth of approximately 50% compared to MTX110 or radiation alone. The results are supportive of the planned exploratory trial in GBM with MTX110.

Neuroprotective effects of a novel water-soluble poly(ADP-ribose) polymerase-1 inhibitor, MP-124, in in vitro and in vivo models of cerebral ischemia

2011 ◽  
Vol 1389 ◽  
pp. 169-176 ◽  
Author(s):  
Yasuhiro Egi ◽  
Shigeru Matsuura ◽  
Tomoyuki Maruyama ◽  
Masakazu Fujio ◽  
Satoshi Yuki ◽  
...  
Keyword(s):  
Cerebral Ischemia ◽  
Water Soluble ◽  
Neuroprotective Effects ◽  
In Vivo Models ◽  
Soluble Poly

Glycolytic Inhibition and Antidiabetic Activity on Synthesized Flavanone Scaffolds with Computer Aided Drug Designing Tools

2020 ◽  
Vol 17 ◽  
Author(s):  
Natarajan Kiruthiga ◽  
Govindaraj Saravanan ◽  
Chellappa Selvinthanuja ◽  
Kulandaivel Srinivasan ◽  
Thangavel Sivakumar
Keyword(s):  
Diabetes Management ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antidiabetic Activity ◽  
Spectroscopic Techniques ◽  
In Vivo Models ◽  
In Silico Studies ◽  
Ic50 Values

Background:: Diabetes mellitus is a challengeable metabolic disorder that leads to a group of complications when HbA1c level not maintained. Most of the existing drugs available in the market in long-term use may lead to serious adverse effects. Hence, current research focuses on drug development for the management of diabetes by synthesizing natural mimicking flavonoid analogues. Objective:: This study focused on the synthesis of flavanone derivatives imitating natural flavonoid core and investigated for their antidiabetic and antioxidant activity, which can help in the development of drug discovery targeting diabetic management. Methods:: The novel 2-phenyl-2,3-dihydro-chromen-4-ones were synthesized from 1,3-diphenyl-prop-2-en-1-one derivatives and characterized using UV, IR, 1HNMR, 13CNMR and mass spectroscopic techniques. Drug target site was determined using graph theoretical analysis and screened the characterized title compounds for their in-silico studies by analyzing their physiochemical properties, ADMET studies, and molecular docking analysis. Antidiabetic and free radical scavenging effects were investigated both by in-vitro (alpha-amylase inhibitory assay) and in-vivo models. Streptozotocin (STZ) induced rats were used as in-vivo models. Results and Discussion:: The α-amylase inhibitory assay showed flavanones with hydroxyl substitution HFA1-HFA7 had significant IC50 values. The test compounds (HFA3-HFA7) were investigated for their antidiabetic activity on STZ induced rats at 40 mg/kg. The blood glucose level and antioxidant enzymes were significantly restored by title compounds (HFA5, HFA4, and HFA6) with an electron-donating group such as hydroxyl, methoxy and thiophenyl group on ring B compared to glibenclamide. Conclusion:: These results suggest that naturally mimicking synthesized flavanone have antidiabetic and antioxidant properties, which can aid in the development of drug towards diabetes management.

Vitamin C Loaded Chemically Modified Nano Carrier for Human Health Care Application

2020 ◽  
Vol 6 (1) ◽  
pp. 34-40 ◽  
Author(s):  
Monalisha Sengupta ◽  
Md. Adil Shaharyar ◽  
Mahfoozur Rahman ◽  
Kumar Anand ◽  
Anindita Kundu
Keyword(s):  
Vitamin C ◽  
Research Work ◽  
Experimental Studies ◽  
Citrus Fruit ◽  
Human Growth ◽  
The Body ◽  
Water Soluble ◽  
And Storage

Background: “Health is wealth” and to maintain it 7 essential nutrients are required. Among these, Vitamin is one that has great importance in very low concentration. As per the solubility, it divides into water-soluble and water-insoluble vitamins. This study concentrates on Vitamin C, a water-soluble vitamin which is essential for human growth due to its activity in the synthesis of carnitine, collagen, and neurotransmitter. It possesses antioxidant, antiatherogenic, and immunomodulatory functions, which may lead to the activity of Vitamin C in many diseases. But humans and some other non-human primates are unable to produce Vitamin C from glucose due to the absence of enzyme gulonolactone oxidase. As a result, humans are dependent on various dietary sources of Vc especially citrus fruit. But these dietary supplies also fail to achieve the required level in the body due to its poor bioavailability and storage. Method: Vitamin C has already proven its activity in cancer therapy. It is also used as a prodrug of H2O2. But due to the poor bioavailability and storage of Vitamin C in the human body, mankind is unable to avail the benefits of Vitamin C. These problems lead to generating different and suitable nanoformulations to incorporate Vitamin C and its derivatives into it. Different research work shows several ways to develop nanoformulations. Amongst all liposomes, microsphere, nanocarriers are of great importance. For Vitamin C incorporation into the nanoformulation, nanocarriers become the most popular choice for researchers. There were several nanocarrier systems developed using Chitosan- Alginate, Silica-Coated-Au Nanoparticles, Chitosan, Mesoporous-silica NCs for suitable incorporation of Vitamin C into these. The performances were assured by performing different in vitro and in vivo tests which will be discussed here. Result: As a result, Vitamin C is now in use for many purposes. It includes not only the above mentioned functions but also other functions too. Due to an antioxidant property, Vitamin C is able to quench reactive oxygen species (ROS) by inhibiting ROS-mediated Nitric Oxide (NO) inactivation. Vitamin C helps to elevate the level of absorption of iron within the cell from dietary iron sources. It also prevents the oxidation of drugs. To achieve all these functions, NCs or nanoformulation plays a great role. Conclusion: It can be concluded that depending on the biocompatibility, loading capacity, protection of the loading molecule, efficiency of cellular uptake, controllable rate of release to achieve the desired effect, and many more factors, the choice of different Nanocarriers (NCs) will be done which ultimately help the human to use it for different purposes. This paper tries to gather some information in one place with respect to different experimental studies.

scholarly journals Synthesis, Characterization and Evaluation of Antidiabetic Activity of Novel Pyrazoline Fused Indole Derivatives

2021 ◽  
pp. 276-292
Author(s):  
Nagesh Vaddiraju ◽  
M. Ajitha ◽  
K. Rajnarayana
Keyword(s):  
Research Work ◽  
Biological Evaluation ◽  
Antidiabetic Activity ◽  
Dimethyl Formamide ◽  
Indole Derivatives ◽  
Standard Drug ◽  
Chemical Structures ◽  
Frame Work

The primary purpose of this research work is to synthesize, characterize and biological evaluation of novel pyrazoline fused indole derivatives lead to creating a new molecular frame work. Methodology: In the present study, the new series of novel pyrazoline fused indole derivatives were synthesized from from indole and substituted acetophenone by the 4 step process. In the first step indole and dimethyl formamide were coupled by using phosphorous oxychloride and NaOH to prepare the compound 1 Indole-3-aldehyde. In the second step compound 1 was condensed with substituted aetophenone to synthesis the compound 2 chalcones (a-h). In the third step chalcones 2(a-h) were coupled with semicarbazide or thiosemicarbazide to synthesis the compound 3(a-p). In the final step compound 3(a-p) were coupled with indole-3-aldehyde to prepare the final product of R-substitutedN-((1H-indol-3-yl)methylene)-5-(1H-indol-3-yl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide and R-substitutedN-((1H-indol-3-yl)methylene)-5-(1H-indol-3-yl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide 4(a-p). Results: The chemical structures of the synthesized compounds were characterized by means of IR, Mass and NMR spectroscopy. The compounds were screened for anti-diabetic activity by In-vitro and In-vivo methods. In In-vivo method 4a, 4m have exhibited moderate anti-diabetic activity as that of standard drug, glibenclamide. In In-vitro method 4a, 4e & 4m have shows moderate anti-diabetic activity as that of reference standard, acarbose. Conclusion: The synthesized novel pyrazoline fused indole derivatives have moderate antidiabetic activity as that of standard drug by In-vitro and In-vivo methods. These compounds can be further exploited to get the potent lead compound.

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