scholarly journals Assessment of antidiabetic potential and phytochemical profiling of Rhazya stricta root extracts

2020 ◽  
Vol 20 (1) ◽  
Author(s):  
Rashid Mahmood ◽  
Waqas Khan Kayani ◽  
Tanveer Ahmed ◽  
Farnaz Malik ◽  
Shahzad Hussain ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Blood Glucose ◽  
In Vivo Studies ◽  
Antidiabetic Activity ◽  
In Vitro Assays ◽  
Root Extracts ◽  
Positive Effects ◽  
Rhazya Stricta ◽  
Dpp Iv

Abstract Background Diabetes mellitus is a chronic disease characterized by hyperglycemia that may occur due to genetic, environmental or lifestyle factors. Natural remedies have been used to treat diabetes since long and many antidiabetic compounds of varied efficacies have been isolated from medicinal plants. Rhazya stricta has been used for decades for the treatment of diabetes mellitus and associated ailments. Considering the folkloric use of R. stricta against diabetes, it was aimed to investigate the effectiveness of its root extracts against diabetes through in vitro assays and in vivo studies using animal model along with phytochemical profiling through GCMS. Methods Various fractions of Rhazya stricta obtained through column chromatography were evaluated for a variety of assays including α-glucosidase, Dipeptidyl peptidase-IV (DPP-IV), β-secretase and Glucagon-like peptide-1 (GLP-1) secretion studies. For the in vivo studies the alloxan-induced diabetic mice were treated with root extracts and blood glucose levels, HbA1C, and other biochemical markers along with the histological study of the liver were done. The phytochemical identification was performed using an Agilent 7890B GC coupled to a 7010 Triple Quadrupole (MS/MS) system. GraphPad Prism software version 5.01 was used for statistical analysis. Results Majority of the extract fractions showed excellent results against diabetes by inhibiting enzymes DPP-IV (Up to 61%) and β-secretase (Up to 83%) with IC50s 979 μg/ml and 169 μg/ml respectively with increase in the GLP1 secretion. The results of in vivo studies indicated a marked reduction in blood glucose and HbA1c levels along with positive effects on other parameters like lipid profile, liver functions and renal functions of extract-treated mice as compared to control. The histological examination of the liver demonstrated hepatoprotective effects against diabetes led changes and various classes of phytochemicals were also identified through GCMS in different fractions. Conclusion The results revealed strong antidiabetic activity of R. stricta root with the potential to protect body organs against diabetic changes. Moreover, a variety of phytochemicals has also been identified through GCMS that might be responsible for the antidiabetic potential of Rhazya stricta root. Graphical abstract

Synthesis, Characterization and Screening of Some Novel 2-Methyl-N'-[(Z)-Substituted-Phenyl ethylidene] Imidazo [1, 2-A] Pyridine-3-Carbohydrazide Derivatives as DPP-IV Inhibitors for the Treatment of Type 2 Diabetes Mellitus

2021 ◽  
Vol 18 ◽  
Author(s):  
Prerana A. Chavan ◽  
Shailaja B. Jadhav
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Blood Glucose ◽  
Antidiabetic Activity ◽  
Antihyperglycemic Activity ◽  
Chronic Hyperglycemia ◽  
Dpp Iv

Background: One of the leading global metabolic diseases marked by insulin resistance and chronic hyperglycemia is type 2 diabetes mellitus (T2DM). Since the last decade, DPP-4 enzyme inhibition has proved to be a successful, safe, and well-established therapy for the treatment of T2DM. Objective: The present work reports the synthesis, characterization, and screening of some novel 2-methyl-N'-[(Z)-substituted-phenyl ethylidene] imidazo [1, 2-a] pyridine-3-carbohydrazide derivatives as DPP-IV inhibitors for the treatment of T2DM. Methods: The molecular docking was performed to study these derivatives' binding mode in the enzyme's allosteric site. All the synthesized compounds were subjected for DPP-IV enzyme assay and in vivo antihyperglycemic activity in STZ-induced diabetic rats. Results: The synthesized derivatives exhibited potent antidiabetic activity as compared to the standard drug Sitagliptin. Out of sixteen compounds, A1, A4, B4, C2, C3, and D4 have shown promising antidiabetic activity against the DPP-IV enzyme. The most promising compound, C2, showed a percentage inhibition of 72.02±0.27 at 50 µM concentration. On the 21st-day compound, C2 showed a significant reduction in serum blood glucose level, i.e., 156.16±4.87 mg/dL, then diabetic control, which was 280.00±13.29 mg/dL whereas, standard Sitagliptin showed 133.50±11.80 mg/dL. In the in vivo antihyperglycemic activity, the compounds have exhibited good hypoglycemic potential in fasting blood glucose in the T2DM animal model. All the docked molecules have exhibited perfect binding affinity towards the active pocket of the enzyme. The synthesized derivatives were screened through Lipinski's rule of five for better optimization, and fortunately, none of them had violated the rule. Conclusion: The above results indicates that compound C2 is a relatively active and selective hit molecule that can be structurally modified to enhance the DPP-IV inhibitor's potency and overall pharmacological profile. From the present work, it has been concluded that substituted pyridine-3-carbohydrazide derivatives possess excellent DPP-IV inhibitory potential and can be better optimized further by generating more in vivo, in vitro models.

scholarly journals Antidiabetic and hypolipidemic potential of Rhazya stricta Decne extract and its fractions

2015 ◽  
Vol 4 (2) ◽  
pp. 353-361 ◽  
Author(s):  
Asma Ahmed ◽  
Muahammad Javaid Asad ◽  
Muhammad Sheeraz Ahmad ◽  
Rehmatullah Qureshi ◽  
Syed Imam Shah ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Blood Glucose ◽  
Blood Glucose Level ◽  
Ethyl Acetate ◽  
Glucose Level ◽  
Ethyl Acetate Fraction ◽  
Pharmaceutical Journal ◽  
Glycosylated Haemoglobin ◽  
Rhazya Stricta

Diabetes mellitus is the most common human disease and there is growing interest for plant based therapy in managing diabetes mellitus specifically in the developing world. In the present study, Rhazya stricta Decne extract was analysed for its antidiabetic activities. Crude methanolic extracts of different plant parts were tested in vivo on albino mice Balb-C, for the reduction of blood glucose, urea, cholesterol, triacylglycerides and glycosylated haemoglobin. Results obtained showed that leaves of R. stricta have best antidiabetic effect by reducing blood glucose level, Glycosylated haemoglobin, triacylglycerides and Cholesterol in hyperglycaemic mice. The R. stricta leaves extract being most active was further fractionated by solvent extraction using n- Hexane, ethyl acetate, chloroform and water and all fractions were tested for same activities. It was found that ethyl acetate fraction is most effective in the reduction of blood glucose level at fasting and random conditions and blood glucose reduction was comparable to Glucophage, a standard antidiabetic drug. The present study suggests that Rhazya stricta leaves extract and its ethyl acetate fraction has great potential for development of antidiabetic drug.DOI: http://dx.doi.org/10.3329/icpj.v4i2.21484 International Current Pharmaceutical Journal, January 2015, 4(2): 353-361

scholarly journals In-Vitro Antidiabetic Activity of Clinacanthus nutans Extracts

2017 ◽  
Vol 9 (6) ◽  
Author(s):  
Abdullah N. ◽  
Kasim K. F.
Keyword(s):  
Blood Glucose ◽  
Amylase Activity ◽  
Significant Inhibition ◽  
In Vivo Studies ◽  
Antidiabetic Activity ◽  
Inhibition Effect ◽  
Glucose Diffusion ◽  
Clinacanthus Nutans

Diabetes mellitus is a prevalent disease which characterized by hyperglycemia. It is a condition in which blood glucose levels are elevated due to decrease in cellular glucose uptake and metabolism. The management of blood glucose level is critical in the treatment of this disease and this had been offered by α-amylase inhibitors. The present study was designed to determine the in vitro antidiabetic of Clinacanthus nutans extracts. The antidiabetic action was observed by the inhibition effects of the C. nutans extracts on α-amylase activity and glucose diffusion across the dialysis tube. It was found that the antidiabetic action of the C. nutans extracts was not related to glucose diffusion as they did not show any significant glucose entrapment ability. The ethanolic leaves extract of C. nutans exhibited the most significant inhibition effect on α-amylase activity (64.25%) compared to other extracts. However, its inhibitory activity was moderate when compared to the commercial drugs (captopril and acarbose). The ethanolic leaves extract (the best extract) was tested for the presence for flavonoids, saponins and tannin (most reported antidiabetic compounds). Its antidiabetic action might be due to the presence of flavonoids and tannins. However, the absence of saponins might be responsible for its moderate inhibition effect comparable to control. This study suggested the in vivo studies of this plant should be carried out to confirm its antidiabetic mechanism

Preparation and Evaluation of Glipizide Tablets Containing both Enhanced and Sustained Release Solid Dispersions

1970 ◽  
Vol 2 (4) ◽  
pp. 714-725
Author(s):  
Adel M. Aly ◽  
Ahmed S. Ali
Keyword(s):  
Blood Glucose ◽  
Blood Glucose Level ◽  
Glucose Level ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
In Vivo Studies ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Tablet Formulations

: Glipizide (GZ) is an oral blood-glucose-lowering drug of the sulfonylurea class characterized by its poor aqueous solubility. Aiming for the production of GZ tablets with rapid onset of action followed by prolonged effect; GZ-Polyethylene glycol (PEG 4000 and 6000) solid dispersions with different ratios, (using melting and solvent evaporation method), as well as, coprecipitate containing GZ with polymethyl-methacrylate (PMMA) were prepared. Four tablet formulations were prepared containing; a) GZ alone, b) GZ: PEG6000, 1:10, c) GZ:PMMA 1:3, and, d)both GZ:PEG6000 1:10 and GZ:PMMA 1:3. The solvent evaporation method showed more enhancement of GZ solubility than the melting one, and this solubilizing effect increased with PEG increment. Generally, PEG6000 showed more enhancement of dissolution than PEG4000 especially at 1:10 drug: polymer ratio (the most enhancing formula). Also, the prepared tablet formulations showed acceptable physical properties according to USP/NF requirements. The dissolution results revealed that tablets containing PEG6000 (1:10) have the most rapid release rate, followed by the formula containing both PEG6000 and PMMA, while that including PMMA alone showed the slowest dissolution rate. Moreover, In-vivo studies for each of the above four formulations, were performed using four mice groups. The most effective formula in decreasing the blood glucose level, through the first 6 hours, was that containing GZ and PEG6000, 1:10. However, formula containing the combination of enhanced and sustained GZ was the most effective in decreasing the blood glucose level through 16 hours. Successful in-vitro in-vivo correlations could be detected between the percent released and the percent decreasing of blood glucose level after 0.5 hours.

Metabolomics of Healthy Berry Fruits

2019 ◽  
Vol 25 (37) ◽  
pp. 4888-4902 ◽  
Author(s):  
Gilda D'Urso ◽  
Sonia Piacente ◽  
Cosimo Pizza ◽  
Paola Montoro
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Bioactive Metabolites ◽  
Active Metabolites ◽  
Positive Effects ◽  
Cell Functions ◽  
Berry Fruits

The consumption of berry-type fruits has become very popular in recent years because of their positive effects on human health. Berries are in fact widely known for their health-promoting benefits, including prevention of chronic disease, cardiovascular disease and cancer. Berries are a rich source of bioactive metabolites, such as vitamins, minerals, and phenolic compounds, mainly anthocyanins. Numerous in vitro and in vivo studies recognized the health effects of berries and their function as bioactive modulators of various cell functions associated with oxidative stress. Plants have one of the largest metabolome databases, with over 1200 papers on plant metabolomics published only in the last decade. Mass spectrometry (MS) and NMR (Nuclear Magnetic Resonance) are the most important analytical technologies on which the emerging ''omics'' approaches are based. They may provide detection and quantization of thousands of biologically active metabolites from a tissue, working in a ''global'' or ''targeted'' manner, down to ultra-trace levels. In the present review, we highlighted the use of MS and NMR-based strategies and Multivariate Data Analysis for the valorization of berries known for their biological activities, important as food and often used in the preparation of nutraceutical formulations.

Novel Phytochemical Constituents and their Potential to Manage Diabetes

2020 ◽  
Vol 26 ◽  
Author(s):  
Shaik Ibrahim Khalivulla ◽  
Arifullah Mohammed ◽  
Kokkanti Mallikarjuna
Keyword(s):  
Natural Products ◽  
Large Population ◽  
World Health ◽  
In Vivo Studies ◽  
Antidiabetic Activity ◽  
Therapeutic Drug ◽  
Pharmacological Activities ◽  
Chemical Structures

Background: Diabetes is a chronic disease affecting a large population worldwide and stands as one of the major global health challenges to be tackled. According to World Health Organization, about 400 million are having diabetes worldwide and it is the seventh leading cause of deaths in 2016. Plant based natural products had been in use from ancient time as ethnomedicine for the treatment of several diseases including diabetes. As a result of that, there are several reports on plant based natural products displaying antidiabetic activity. In the current review, such antidiabetic potential compounds reported from all plant sources along with their chemical structures are collected, presented and discussed. This kind of reports are essential to pool the available information to one source followed by statistical analysis and screening to check the efficacy of all known compounds in a comparative sense. This kind of analysis can give rise to few numbers of potential compounds from hundreds, whom can further be screened through in vitro and in vivo studies, and human trails leading to the drug development. Methods: Phytochemicals along with their potential antidiabetic property were classified according to their basic chemical skeleton. The chemical structures of all the compounds with antidiabetic activities were elucidated in the present review. In addition to this, the distribution and their other remarkable pharmacological activities of each species is also included. Results: The scrutiny of literature led to identification of 44 plants with antidiabetic compounds (70) and other pharmacological activities. For the sake of information, the distribution of each species in the world is given. Many plant derivatives may exert antidiabetic properties by improving or mimicking the insulin production or action. Different classes of compounds including sulfur compounds (1-4), alkaloids (5-11), phenolic compounds (12-17), tannins (18-23), phenylpropanoids (24-27), xanthanoids (28-31), amino acid (32), stilbenoid (33), benzofuran (34), coumarin (35), flavonoids (36-49) and terpenoids (50-70) were found to be active potential compounds for antidiabetic activity. Of the 70 listed compounds, majorly 17 compounds are from triterpenoids, 13 flavonoids and 7 are from alkaloids. Among all the 44 plant species, maximum number (7) of compounds are reported from Lagerstroemia speciosa followed by Momordica charantia (6) and S. oblonga with 5 compounds. Conclusion: This is the first paper to summarize the established chemical structures of phytochemicals that have been successfully screened for antidiabetic potential and their mechanisms of inhibition. The reported compounds could be considered as potential lead molecules for the treatment of type-2 diabetes. Further, molecular and clinical trials are required to select and establish the therapeutic drug candidates.

In-silico Studies of Isolated Phytoalkaloid Against Lipoxygenase: Study Based on Possible Correlation

2018 ◽  
Vol 21 (3) ◽  
pp. 215-221
Author(s):  
Haroon Khan ◽  
Muhammad Zafar ◽  
Helena Den-Haan ◽  
Horacio Perez-Sanchez ◽  
Mohammad Amjad Kamal
Keyword(s):  
In Silico ◽  
Docking Studies ◽  
In Vivo Studies ◽  
In Vitro Assays ◽  
Chronic Obstructive ◽  
Lipoxygenase Inhibitors ◽  
Lipoxygenase Inhibition ◽  
In Silico Studies

Aim and Objective: Lipoxygenase (LOX) enzymes play an important role in the pathophysiology of several inflammatory and allergic diseases including bronchial asthma, allergic rhinitis, atopic dermatitis, allergic conjunctivitis, rheumatoid arthritis and chronic obstructive pulmonary disease. Inhibitors of the LOX are believed to be an ideal approach in the treatment of diseases caused by its over-expression. In this regard, several synthetic and natural agents are under investigation worldwide. Alkaloids are the most thoroughly investigated class of natural compounds with outstanding past in clinically useful drugs. In this article, we have discussed various alkaloids of plant origin that have already shown lipoxygenase inhibition in-vitro with possible correlation in in silico studies. Materials and Methods: Molecular docking studies were performed using MOE (Molecular Operating Environment) software. Among the ten reported LOX alkaloids inhibitors, derived from plant, compounds 4, 2, 3 and 1 showed excellent docking scores and receptor sensitivity. Result and Conclusion: These compounds already exhibited in vitro lipoxygenase inhibition and the MOE results strongly correlated with the experimental results. On the basis of these in vitro assays and computer aided results, we suggest that these compounds need further detail in vivo studies and clinical trial for the discovery of new more effective and safe lipoxygenase inhibitors. In conclusion, these results might be useful in the design of new and potential lipoxygenase (LOX) inhibitors.

scholarly journals Potential antidiabetic phytochemicals in plant roots: a review of in vivo studies

2021 ◽  
Author(s):  
Hamidreza Ardalani ◽  
Fatemeh Hejazi Amiri ◽  
Amin Hadipanah ◽  
Kenneth T. Kongstad
Keyword(s):  
Stress Reduction ◽  
Natural Compounds ◽  
Plant Roots ◽  
In Vivo Studies ◽  
Antidiabetic Activity ◽  
Scientific Databases ◽  
Plant Parts ◽  
Plant Families ◽  
Promising Source

Abstract Background Medicinal plants are used to treat various disorders, including diabetes, globally in a range of formulations. While attention has mainly been on the aerial plant parts, there are only a few review studies to date that are focused on the natural constituents present in the plant roots with health benefits. Thus, the present study was performed to review in vivo studies investigating the antidiabetic potential of the natural compounds in plant roots. Methods We sorted relevant data in 2001–2019 from scientific databases and search engines, including Web of Knowledge, PubMed, ScienceDirect, Medline, Reaxys, and Google Scholar. The class of phytochemicals, plant families, major compounds, active constituents, effective dosages, type of extracts, time of experiments, and type of diabetic induction were described. Results In our literature review, we found 104 plants with determined antidiabetic activity in their root extracts. The biosynthesis pathways and mechanism of actions of the most frequent class of compounds were also proposed. The results of this review indicated that flavonoids, phenolic compounds, alkaloids, and phytosteroids are the most abundant natural compounds in plant roots with antidiabetic activity. Phytochemicals in plant roots possess different mechanisms of action to control diabetes, including inhibition of α-amylase and α-glucosidase enzymes, oxidative stress reduction, secretion of insulin, improvement of diabetic retinopathy/nephropathy, slow the starch digestion, and contribution against hyperglycemia. Conclusion This review concludes that plant roots are a promising source of bioactive compounds which can be explored to develop against diabetes and diabetes-related complications. Graphical abstract

scholarly journals Immunobiotic Feed Developed with Lactobacillus delbrueckii subsp. delbrueckii TUA4408L and the Soymilk By-Product Okara Improves Health and Growth Performance in Pigs

2021 ◽  
Vol 9 (5) ◽  
pp. 921
Author(s):  
Yoshihito Suda ◽  
Nana Sasaki ◽  
Kyoma Kagawa ◽  
Mariano Elean ◽  
Binghui Zhou ◽  
...  
Keyword(s):  
Growth Performance ◽  
Lactobacillus Delbrueckii ◽  
In Vivo Studies ◽  
Intestinal Immunity ◽  
Positive Effects ◽  
Markers Of Inflammation ◽  
Immune Health ◽  
Tlr4 Activation ◽  
Lactobacillus Delbrueckii Subsp

Lactobacillus delbrueckii subsp. delbrueckii TUA4408L is able to differentially modulate the innate immune response of porcine intestinal epithelial cells triggered by TLR4 activation. This strain also has a remarkable ability to grow on plant substrates. These two immunological and biotechnological characteristics prompted us to evaluate whether the soymilk by-product okara fermented with the TUA4408L strain can serve as an immunobiotic feed with the ability to beneficially modulate the intestinal immunity of piglets after weaning to improve their productivity. Our in vivo studies demonstrated that the administration of immunobiotic TUA4408L-fermented okara feed significantly increased piglet growth performance and meat quality. These positive effects were associated with the ability of the TUA4408L-fermented okara feed to beneficially modulate both intestinal microbiota and immunity in pigs. The immunobiotic feed improved the abundance of the beneficial bacteria Lactobacillus and Lactococcus in the gut of pigs, reduced blood markers of inflammation, and differentially regulated the expression of inflammatory and regulatory cytokines in the intestinal mucosa. These findings indicate that the immunobiotic TUA4408L-fermented okara feed could be an economical and environmentally friendly option to improve the growth performance and immune health of pigs.

scholarly journals TGFβ signalling acts as a molecular brake of myoblast fusion

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Julie Melendez ◽  
Daniel Sieiro ◽  
David Salgado ◽  
Valérie Morin ◽  
Marie-Julie Dejardin ◽  
...  
Keyword(s):  
Dynamic Control ◽  
Muscle Growth ◽  
Myoblast Fusion ◽  
In Vivo Studies ◽  
In Vitro Assays ◽  
Receptor Complex ◽  
Tgfβ Signalling ◽  
Molecular Brake

AbstractFusion of nascent myoblasts to pre-existing myofibres is critical for skeletal muscle growth and repair. The vast majority of molecules known to regulate myoblast fusion are necessary in this process. Here, we uncover, through high-throughput in vitro assays and in vivo studies in the chicken embryo, that TGFβ (SMAD2/3-dependent) signalling acts specifically and uniquely as a molecular brake on muscle fusion. While constitutive activation of the pathway arrests fusion, its inhibition leads to a striking over-fusion phenotype. This dynamic control of TGFβ signalling in the embryonic muscle relies on a receptor complementation mechanism, prompted by the merging of myoblasts with myofibres, each carrying one component of the heterodimer receptor complex. The competence of myofibres to fuse is likely restored through endocytic degradation of activated receptors. Altogether, this study shows that muscle fusion relies on TGFβ signalling to regulate its pace.

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