In vitro and in silico PTP-1B inhibition and in vivo antidiabetic activity of semisynthetic moronic acid derivatives

2016 ◽  
Vol 26 (8) ◽  
pp. 2018-2022 ◽  
Author(s):  
Litzia Cerón-Romero ◽  
Paolo Paoli ◽  
Guido Camici ◽  
Virginia Flores-Morales ◽  
María Yolanda Rios ◽  
...  
Keyword(s):  
In Silico ◽  
Antidiabetic Activity ◽  
Ptp 1B

scholarly journals Antidiabetic activity of some pentacyclic acid triterpenoids, role of PTP–1B: In vitro, in silico, and in vivo approaches

2011 ◽  
Vol 46 (6) ◽  
pp. 2243-2251 ◽  
Author(s):  
Juan José Ramírez-Espinosa ◽  
Maria Yolanda Rios ◽  
Sugey López-Martínez ◽  
Fabian López-Vallejo ◽  
José L. Medina-Franco ◽  
...  
Keyword(s):  
In Silico ◽  
Antidiabetic Activity ◽  
Ptp 1B

scholarly journals In vitro and in vivo antidiabetic activity, isolation of flavonoids, and in silico molecular docking of stem extract of Merremia tridentata (L.)

2022 ◽  
Vol 146 ◽  
pp. 112611
Author(s):  
Lenh Vo Van ◽  
Em Canh Pham ◽  
Cuong Viet Nguyen ◽  
Ngoc Thoi Nguyen Duong ◽  
Tuong Vi Le Thi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
In Silico ◽  
Antidiabetic Activity ◽  
Stem Extract ◽  
In Silico Molecular Docking

Mechanism-based antidiabetic activity of Fructo- and isomalto-oligosaccharides: Validation by in vivo, in silico and in vitro interaction potential

2015 ◽  
Vol 50 (2) ◽  
pp. 317-327 ◽  
Author(s):  
Sudhanshu Kumar Bharti ◽  
Supriya Krishnan ◽  
Amit Kumar ◽  
Ashok Kumar Gupta ◽  
Asish Kumar Ghosh ◽  
...  
Keyword(s):  
Interaction Potential ◽  
In Silico ◽  
Antidiabetic Activity ◽  
In Vitro Interaction

scholarly journals Antidiabetic Activity ofRuellia tuberosaL., Role ofα-Amylase Inhibitor:In Silico,In Vitro, andIn VivoApproaches

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Dyah Ratna Wulan ◽  
Edi Priyo Utomo ◽  
Chanif Mahdi
Keyword(s):  
Single Dose ◽  
In Silico ◽  
Amylase Activity ◽  
Alternative Therapy ◽  
Antidiabetic Activity ◽  
Diabetic Rat ◽  
Control Group ◽  
Folk Remedy

Ruellia tuberosaL. is a folk remedy in the treatment of diabetes mellitus. However, its hypoglycemic activity has not been investigated so far. In the present study, the antidiabetic mechanism of the n-hexane fraction of methanolic extract (HFME) of this plant was investigatedin silico,in vitro, andin vivo.In silicostudy was performed using AutoDock4.2 software.In vitro  α-amylase inhibitory activity was investigated by starch-iodine method. A single dose of 450 mg/kg HFME for 14 days was subjected to an antidiabetic screeningin vivoby a multiple low dose streptozotocin (MLD-STZ) induced rats. Molecular modeling results show that Betulin exhibited noncompetitiveα-amylase inhibitory activities. The effect of HFME elicited significant reductions of diabetic rat blood glucose. A single dose administration of HFME inhibitedα-amylase activityin vivo(P<0.01) compared to a diabetic control group. Moreover, this extract strongly inhibited theα-amylase activityin vitro(IC500.14 ± 0.005 mg/mL). It is concluded that HFME exerted an antidiabetic effect viaα-amylase inhibitor. Our findings provide a possible hypoglycemic action ofR. tuberosaL. as an alternative therapy in the management of diabetes.

scholarly journals Antidiabetic Activity of Ficusonolide, a Triterpene Lactone from Ficus foveolata (Wall. ex Miq.): In Vitro, In Vivo, and In Silico Approaches

ACS Omega ◽  
2021 ◽  
Author(s):  
Ala Ud Din ◽  
Maria Khan ◽  
Muhammad Zahir Shah ◽  
Abdur Rauf ◽  
Umer Rashid ◽  
...  
Keyword(s):  
In Silico ◽  
Antidiabetic Activity

Synthesis of oleanolic acid derivatives: In vitro, in vivo and in silico studies for PTP-1B inhibition

2014 ◽  
Vol 87 ◽  
pp. 316-327 ◽  
Author(s):  
Juan José Ramírez-Espinosa ◽  
Maria Yolanda Rios ◽  
Paolo Paoli ◽  
Virginia Flores-Morales ◽  
Guido Camici ◽  
...  
Keyword(s):  
Oleanolic Acid ◽  
In Silico ◽  
In Silico Studies ◽  
Ptp 1B

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.

Recent In Vitro and In Silico Advances in the Understanding of Intranasal Drug Delivery

2020 ◽  
Vol 26 ◽  
Author(s):  
John Chen ◽  
Andrew Martin ◽  
Warren H. Finlay
Keyword(s):  
Drug Delivery ◽  
In Silico ◽  
Local Drug Delivery ◽  
In Vivo Studies ◽  
Intranasal Drug Delivery ◽  
Nasal Sprays ◽  
In Silico Studies ◽  
Drug Delivery Devices

Background: Many drugs are delivered intranasally for local or systemic effect, typically in the form of droplets or aerosols. Because of the high cost of in vivo studies, drug developers and researchers often turn to in vitro or in silico testing when first evaluating the behavior and properties of intranasal drug delivery devices and formulations. Recent advances in manufacturing and computer technologies have allowed for increasingly realistic and sophisticated in vitro and in silico reconstructions of the human nasal airways. Objective: To perform a summary of advances in understanding of intranasal drug delivery based on recent in vitro and in silico studies. Conclusion: The turbinates are a common target for local drug delivery applications, and while nasal sprays are able to reach this region, there is currently no broad consensus across the in vitro and in silico literature concerning optimal parameters for device design, formulation properties and patient technique which would maximize turbinate deposition. Nebulizers are able to more easily target the turbinates, but come with the disadvantage of significant lung deposition. Targeting of the olfactory region of the nasal cavity has been explored for potential treatment of central nervous system conditions. Conventional intranasal devices, such as nasal sprays and nebulizers, deliver very little dose to the olfactory region. Recent progress in our understanding of intranasal delivery will be useful in the development of the next generation of intranasal drug delivery devices.

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.

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