scholarly journals CINNAMIC ACID AND ITS DERIVATIVES IN THE HERBAL MIXTURES AND THEIR ANTIDIABETIC ACTIVITY

FARMACIA ◽  
2021 ◽  
Vol 69 (3) ◽  
pp. 595-601
Author(s):  
ALONA SAVYCH
2020 ◽  
Vol 17 (3) ◽  
pp. 338-347
Author(s):  
Ajay Chauhan ◽  
Ajmer S. Grewal ◽  
Deepti Pandita ◽  
Viney Lather

Background: Peroxisome proliferator-activated receptor (PPAR) δ is expressed universally in the entire tissues, particularly in those concerned with the lipid metabolism. PPAR δ stimulation alters body’s energy fuel preference to fat from glucose and shows up as an emerging pharmacological target for the treatment of metabolic disorders. Methods: A new series of cinnamic acid derivatives was synthesized and evaluated for the antidiabetic and antiinflammatory activities in the animal models followed by in silico docking studies to determine the binding interactions for the best fit conformations in the binding site of the PPARδ protein. Results: Amongst the synthesized molecules, compound 3 showed higher antidiabetic activity in oral glucose tolerance test and compound 1 showed higher antiinflammatory activity in the carrageenan induced rat paw oedema method. The in vivo study results were supported by the similar in silico molecular docking results. Most of the synthesized derivatives showed drug likeness as depicted via Lipinski’s rule of 5. Conclusion: These molecules can serve as the early hit molecules for the discovery of safe, effective and bioavailable PPARδ agonists for the potential treatment of various metabolic disorders.</P>


Author(s):  
Alona Savych ◽  
Svitlana Marchyshyn ◽  
Roksolana Basaraba ◽  
Liubomyr Kryskiw

The aim of the study was to research the qualitative composition and to investigate the quantitative content of some carboxylic acids in the herbal mixtures with established hypoglycemic, hypolipidemic and antioxidant activity in previous studies in vivo. Materials and methods. Studies of carboxylic acid content in the herbal mixtures were performed by HPLC analysis using Agilent Technologies 1200 liquid chromatograph (USA). Identification and quantitative analysis were performed using standard solutions of carboxylic compounds (tartaric, pyruvic, isocitric, citric, succinic and fumaric acids). Conclusions. HPLC analysis of five samples of the herbal mixture with antidiabetic activity showed the presence of six carboxylic acids. The dominant acid in all samples was isocitric acid. Among the most important for the prevention and treatment of diabetes, high levels of succinic and fumaric acids have been identified and established. The obtained data indicate a correlation between the phytochemical composition of the studied herbal mixtures and their pharmacodynamics, which was previously established


Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
A Brantner ◽  
M Alajlani ◽  
C Autz ◽  
S Benetik ◽  
E Plhak ◽  
...  

2019 ◽  
Vol 3 (3) ◽  
pp. 91-94
Author(s):  
Mudassir Lawal ◽  
◽  
Abdulaziz Suleiman ◽  
Nasiruddin Matazu ◽  
Fatima Dawud ◽  
...  

2020 ◽  
Vol 28 ◽  
Author(s):  
Heba A.S. El-Nashar ◽  
Nada M. Mostafa ◽  
Mohamed El-Shazly ◽  
Omayma A. Eldahshan

Background:: Diabetes mellitus (DM) represents a global health problem characterized by hyperglycemia due to insufficient insulin secretion or failure of insulin activity. There is an imperative need for the discovery of alternative therapeutic agents that overcome the drawbacks of the current synthetic antidiabetic drugs. Objectives:: This review critically summarizes the reports on the known and novel natural compounds including alkaloids, flavonoids, and saponins with a potent antidiabetic activity that were recently published from 2014 to 2019. We discussed the underlying mechanisms of action that put these compounds in the category of effective antidiabetic candidates. Methods: Information was obtained from Google Scholar, Scirus, PubMed, and Science Direct. Discussion and Conclusion:: The reported natural compounds showed promising antidiabetic activity through different mechanisms such as the inhibition of α-amylase, α-glucosidase, insulin-sensitizing effect, direct action on protein tyrosine phosphatase 1B (PTP1B), peroxisome proliferator-activated receptors (PPARs), GLUT4 expression, insulin receptor substrate- 1 (IRS-1) and glycogen synthase kinase-3β (GSK-3β) as well as dipeptidyl peptidase-4 (DPP-4) enzyme. Some compounds inhibited the formation of advanced glycation end products (AGEs). Other compounds prevented the risk of diabetic complications such as cardiovascular diseases, retinopathy, and nephropathy. This review provides a critical overview of the most recent discoveries of antidiabetic agents from natural sources. This overview could help researchers to focus on the most prominent candidates aiming to develop new drug leads.


2020 ◽  
Vol 26 ◽  
Author(s):  
Shaik Ibrahim Khalivulla ◽  
Arifullah Mohammed ◽  
Kokkanti Mallikarjuna

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.


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