scholarly journals In Vitro Investigation and Evaluation of Novel Drug Based on Polyherbal Extract against Type 2 Diabetes

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Zainab Riaz ◽  
Murtaza Najabat Ali ◽  
Zunaira Qureshi ◽  
Muhammad Mohsin
Keyword(s):  
Type 2 Diabetes ◽  
Digestive Enzyme ◽  
Yeast Cells ◽  
Antidiabetic Activity ◽  
Alcoholic Extract ◽  
Dissolution Profile ◽  
Active Compounds ◽  
Standard Drug ◽  
In Vitro Investigation

Background/Aim. Type 2 diabetes is the most common form of diabetes mellitus. The aim of this study was to develop and standardize the polyhedral formulation (granule) and check its efficacy with regard to type 2 diabetes. Methods. The alcoholic extract of each plant (H. antidysentrica, Prunus dulcis and Cicer arietinum) and oleic acid was mixed and then formulated by wet granulation method. FTIR was done to investigate the presence of active compounds. Physicochemical properties of granules were evaluated and antidiabetic potential was substantiated through inhibition of carbohydrate digestive enzyme (α-amylase and α-glucosidase), glucose uptake activity in yeast cells, and antioxidant activity. Results. IR spectra indicated the presence of active compounds by showing the characteristic peaks of phenols and amines. The FTIR results also showed no interaction between drug and excipients. The prepared granules exhibited excellent flow properties according to USP 30. The dissolution profile of active pharmaceutical ingredient (API) from granules showed 72–80% release in 2 hrs. Granules exhibited better inhibition of α-amylase and α-glucosidase as in comparison with the standard drug and found to be dose-dependent. The enhanced uptake of glucose was observed with a decrease in drug concentration. Moreover, the DPPH scavenging activity was high (98%) at 1 mg/ml. Conclusion. The stabilized formulation (granules) was formed and the presence of active compounds is responsible for better antidiabetic activity by inhibiting carbohydrate-digesting enzymes. Hence, it could lower the postprandial hyperglycemia and has the potential to be used for the treatment of type II diabetes after determining the dose regime.

scholarly journals The Active Role of Leguminous Plant Components in Type 2 Diabetes

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Monika Gętek ◽  
Natalia Czech ◽  
Małgorzata Muc-Wierzgoń ◽  
Elżbieta Grochowska-Niedworok ◽  
Teresa Kokot ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Bioactive Compounds ◽  
International Diabetes Federation ◽  
Noncommunicable Diseases ◽  
Antidiabetic Activity ◽  
Leguminous Plant ◽  
Morbidity Rate ◽  
Diabetes Incidence ◽  
Leguminous Plants

Diabetes appears to be one of the most frequent noncommunicable diseases in the world. A permanent growth in the incidence of diabetes can be observed and according to the International Diabetes Federation (IDF) the year 2030 will mark the increase in the number of diabetics to 439 mln worldwide. Type 2 diabetes accounts for about 90% of all diabetes incidence. Nutrition model modification not only features the basic element in type 2 diabetes treatment but also constitutes the fundamental factor influencing a morbidity rate decrease. Leguminous plants are a key factor in the diabetic diet; plants such as pulses or soybeans are nutritious products valued highly in nutrition. These legumes are high in the content of wholesome protein and contain large amounts of soluble alimentary fiber fractions, polyunsaturated fatty acids, vitamins and minerals, and bioactive substances with antioxidant, anti-inflammatory, and anticancer activity. They are distinguished by the high amount of bioactive compounds that may interfere with the metabolism of glucose. The most significant bioactive compounds displaying antidiabetic activity in leguminous plants are as follows: genistein and daidzein, alpha-amylase inhibitors, and alpha-glucosidase inhibitors.In vitroresearch using leguminous plant extracts has confirmed their antidiabetic properties. Leguminous plants should be employed in the promotion of healthy lifestyles in terms of functional food.

Systematic investigation of the mechanism of Cichorium glandulosum on type 2 diabetes mellitus accompanied with non-alcoholic fatty liver rats

2019 ◽  
Vol 10 (5) ◽  
pp. 2450-2460 ◽  
Author(s):  
Huiyu Qin ◽  
Haijun Chen ◽  
Yang Zou ◽  
Xiaoyi Zhang ◽  
Changqing Wei ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Fatty Liver ◽  
Systematic Investigation ◽  
Systems Pharmacology ◽  
Active Compounds ◽  
Alcoholic Fatty Liver ◽  
Action Mechanisms

Strategy of this systems-pharmacology approach to investigate the active compounds and action mechanisms of CG on T2DM-NAFLD.

Antidiabetic Activity of Ergosterol from Pleurotus Ostreatus in KK-Ay Mice with Spontaneous Type 2 Diabetes Mellitus

2018 ◽  
Vol 62 (3) ◽  
pp. 1700444 ◽  
Author(s):  
Mingrui Xiong ◽  
Yun Huang ◽  
Yajing Liu ◽  
Mi Huang ◽  
Guanjun Song ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Pleurotus Ostreatus ◽  
Antidiabetic Activity ◽  
Ay Mice

scholarly journals Recent Advances in In-Vitro Assays for Type 2 Diabetes Mellitus: An Overview

2020 ◽  
Vol 16 (1) ◽  
pp. 13-23
Author(s):  
Nazmina Vhora ◽  
Ujjal Naskar ◽  
Aishwarya Hiray ◽  
Abhijeet S. Kate ◽  
Alok Jain
Keyword(s):  
Type 2 Diabetes ◽  
Drug Discovery ◽  
High Throughput ◽  
High Throughput Screening ◽  
Antidiabetic Activity ◽  
Screening Methods ◽  
Selection Of

BACKGROUND: A higher rate of attenuation of molecules in drug discovery has enabled pharmaceutical companies to enhance the efficiency of their hit identification and lead optimization. Selection and development of appropriate in-vitro and in-vivo strategies may improve this process as primary and secondary screening utilize both strategies. In-vivo approaches are too relentless and expensive for assessing hits. Therefore, it has become indispensable to develop and implement suitable in-vitro screening methods to execute the required activities and meet the respective targets. However, the selection of an appropriate in-vitro assay for specific evaluation of cellular activity is no trivial task. It requires thorough investigation of the various parameters involved. AIM: In this review, we aim to discuss in-vitro assays for type 2 diabetes (T2D), which have been utilized extensively by researchers over the last five years, including target-based, non-target based, low-throughput, and high-throughput screening assays. METHODS: The literature search was conducted using databases including Scifinder, PubMed, ScienceDirect, and Google Scholar to find the significant published articles. DISCUSSION and CONCLUSION: The accuracy and relevance of in-vitro assays have a significant impact on the drug discovery process for T2D, especially in assessing the antidiabetic activity of compounds and identifying the site of effect in high-throughput screening. The report reviews the advantages, limitations, quality parameters, and applications of the probed invitro assays, and compares them with one another to enable the selection of the optimal method for any purpose. The information on these assays will accelerate numerous procedures in the drug development process with consistent quality and accuracy.

scholarly journals The Mechanism of Jinqi Jiangtang Tablet in Treatment of Type 2 Diabetes Mellitus Based on Network Pharmacology

2020 ◽  
Author(s):  
Mingjun Yang ◽  
Boni Song ◽  
Zhitong Bing ◽  
Juxiang Liu ◽  
Rui Li ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Drug Targets ◽  
Kegg Pathway ◽  
Enrichment Analysis ◽  
Network Pharmacology ◽  
Active Compounds ◽  
Online Tool

Abstract Background: Type 2 Diabetes Mellitus(T2DM) is an endocrine disease that caused mainly by insulin resistance (IR) and β cell dysfunction. The incidence of T2DM is quite high in the worldwide. To explore the molecular mechanism of Jinqi Jiangtang Tablet(JJT) in treating of T2DM based on Network Pharmacology. Methods: The active compounds, targets of three Traditional Chinese medicines in JJT were obtained by the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform（TCMSP） database and Uniprot database; The targets of T2DM were screened through the Drugbank database; The compound-target network was constructed via the Cytoscape 3.7.2 software and used the built-in Network analyzer to analyze and select the key active compounds; The overlapping targets of drug and disease targets were gained by the VENNY online tool and the targets were built by STRING website to select the key genes; Gene Ontology(GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway were performed on the potential targets using DAVID6.8 online tool to study the mechanism of overlapping targets. Via Systems Dock platform to validate the interaction between compound and targets Results: Twenty-five active compounds of JJT were screened, 101 drug targets, 142 disease targets and twenty-one overlapping targets. GO enrichment analysis showed that the biological processes (BP)mainly included the blood circulation ,etc. Cell composition(CC) mainly affected the integral component of plasma membrane, etc. Molecular functions(MF) mainly involved alpha-adrenergic receptor activity, etc. KEGG pathway analysis showed that there were twelve pathways related to T2DM, among which PPAR signaling pathway was related to T2DM mostly. RXRA is one of key targets of JJT and berberine performed well. Conclusions: This study revealed the mechanism of JJT in treatment of T2DM preliminarily and supplied a further foundation for studying its mechanism.

scholarly journals Quercetin promotes long noncoding RNA lncSHGL expression via estrogen receptor α to suppress type 2 diabetes mellitus in mice

2020 ◽  
Author(s):  
Hanlu Fan ◽  
Haiwen Li ◽  
Huijiao Liu ◽  
Peng Li ◽  
Xiaomeng Jia ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Estrogen Receptor ◽  
Noncoding Rna ◽  
Estrogen Receptor Alpha ◽  
Grape Pomace ◽  
Active Compounds ◽  
Organ Systems

Abstract Background Type 2 diabetes mellitus (T2DM) is the most common type of metabolic disorder involving multiple organ systems. Grape has been reported to improve the symptoms of T2DM, the precise mechanism of its action is unclear. Our study was aimed to determine the effect and mechanism of grape pomace extract in T2DM mice induced by high fat diet (HFD). Materials and methods Ultra-performance liquid chromatography and quadrupole time-of-flight mass spectrometry were used to identify the main active compounds in grape pomace extract to improve T2DM. C57BLK/6J mice induced by HFD supplemented with or without quercetin were used to show the effects of quercetin improving T2DM. By online database research, bioinformatics analysis and molecular biology experiments, Estrogen receptor alpha (ERα)-lncSHGL (lncRNA suppressor of hepatic gluconeogenesis and lipogenesis) pathway was identify as the target for quercetin. Results Quercetin was identified as one of the most active compounds in grape pomace extract to improve T2DM. Quercetin could inhibit HFD-induced T2DM in mice by activing ERα. LncSHGL was identified as the downstream of ERα and inhibited HFD-induced T2DM. Conclusions Quercetin could be beneficial for T2DM by promoting lncSHGL transcription and activating the lncSHGL pathway, and may be used as a drug component to treat T2DM.

Pyrano[3,2-c]quinoline Derivatives as New Class of α-glucosidase Inhibitors to Treat Type 2 Diabetes: Synthesis, in vitro Biological Evaluation and Kinetic Study

2019 ◽  
Vol 15 (1) ◽  
pp. 8-16 ◽  
Author(s):  
Zahra Heydari ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Somaye Imanparast ◽  
Mohammad A. Faramarzi ◽  
Mohammad Mahdavi ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Kinetic Study ◽  
Inhibitory Activity ◽  
Cycloaddition Reaction ◽  
Competitive Inhibitor ◽  
Biological Evaluation ◽  
Quinoline Derivatives ◽  
Standard Drug

Background: Pyrano[3,2-c]quinoline derivatives 6a–n were synthesized via simple two-step reactions and evaluated for their in vitro α-glucosidase inhibitory activity. </P><P> Methods: Pyrano[3,2-c]quinoline derivatives 6a–n derivatives were prepared from a two-step reaction: cycloaddition reaction between 1-naphthyl amine 1 and malonic acid 2 to obtain benzo[h]quinoline-2(1H)-one 3 and reaction of 3 with aryl aldehydes 4 and Meldrum’s acid 5. The anti- α-glucosidase activity and kinetic study of the synthesized compounds were evaluated using α-glucosidase from Saccharomyces cerevisiae and p-nitrophenyl-a-D-glucopyranoside as substrate. The α-glucosidase inhibitory activity of acarbose was evaluated as positive control. Results: All of the synthesized compounds, except compounds 6i and 6n, showed more inhibitory activity than the standard drug acarbose and were also found to be non-cytotoxic. Among the synthesized compounds, 1-(2-bromophenyl)-1H-benzo[h]pyrano[3,2-c]quinoline-3,12(2H,11H)-dione 6e displayed the highest α-glucosidase inhibitory activity (IC50 = 63.7 ± 0.5 µM). Kinetic study of enzyme inhibition indicated that the most potent compound, 6e, is a non-competitive inhibitor of α-glucosidase with a Ki value of 72 µM. Additionally, based on the Lipinski rule of 5, the synthesized compounds were found to be potential orally active drugs. Conclusion: Our results suggest that the synthesized compounds are promising candidates for treating type 2 diabetes.

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