scholarly journals α-Glucosidase Inhibitory and Glucose Uptake Stimulatory Effects of Phenolic Compounds From Dendrobium christyanum

2020 ◽  
Vol 15 (3) ◽  
pp. 1934578X2091345 ◽  
Author(s):  
Htoo Tint San ◽  
Panitch Boonsnongcheep ◽  
Waraporn Putalun ◽  
Wanwimon Mekboonsonglarp ◽  
Boonchoo Sritularak ◽  
...  

A methanolic extract from the dried root of Dendrobium christyanum Rchb.f. (Orchidaceae) exhibited α-glucosidase inhibitory activity and glucose uptake stimulatory effect. Chromatographic separation of the extract led to the isolation of 13 phenolic compounds (1-13). Their structures were determined by spectroscopic analysis. The isolates were then evaluated for in vitro α-glucosidase inhibitory and glucose uptake stimulatory activities. Methyl haematommate (1), methyl 2,4-dihydroxy-3,6-dimethylbenzoate (3), n-docosyl 4-hydroxy- trans-cinnamate (4), coniferyl aldehyde (6), 4,5-dihydroxy-2-methoxy-9,10-dihydrophenanthrene (7), gigantol (10), and diorcinolic acid (13) showed higher α-glucosidase inhibitory activity than the drug acarbose. Moreover, n-docosyl 4-hydroxyl- trans-cinnamate (4), vanillin (5), and coniferyl aldehyde (6) could enhance glucose uptake by L6 myotubes. Compounds 4 and 6 appear to be potential hypoglycemic agents since they possess both α-glucosidase inhibitory and glucose uptake stimulatory activities. This study is the first report on the chemical constituents and antidiabetic activity of D. christyanum.

2020 ◽  
Vol 7 (2) ◽  
pp. 50-55
Author(s):  
Anitha T A ◽  
Pakutharivu T ◽  
Nirubama K ◽  
Akshaya V

The traditional herbal medicines are mainly obtained from plants are used in the management of Diabetes mellitus. The main objective of this work was to assess the presence of phytochemical compounds and to evaluate the in vitro antidiabetic activity of isopropanolic extracts of Pimenta racemosa leaves by studying their α-amylase inhibitory activity and glucose transport across yeast cells. Screening of phytochemicals showed positive results for alkaloids, steroids, cardiac glycosides, terpenoids, reducing sugars, anthraquinones, and results of in vitro α-amylase inhibitory studies demonstrated there was a dose-dependent increase in percentage inhibitory activity by the isopropanolic leaf extracts of Pimenta racemosa. At a concentration of 1 mg/ml, the extract showed a percentage inhibition 33.6 and for 5 mg/ml it was 91.2. The glucose uptake study was also studied through yeast cells by analyzing theamount of glucose remaining in the medium after a specific time intervals. It serves as an indicator for the capability of isopropanolic leaf extracts of Pimenta racemosa to transport the glucose into yeast cells. As a result, we found that the isopropanolic leaf extract of Pimenta racemosa have inhibitory activity against αamylase and also, which is efficient in glucose uptake. This therapeutic potentiality of Pimenta racemosa could be exploited in the treatment of Type 2 Diabetes mellitus. Further studies are also required to elucidate whether the plant have antidiabetic potential by in vivo for corroborating the traditional claim of the plant.


2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Abdur Rauf ◽  
Muhammad Saleem ◽  
Ghias Uddin ◽  
Bina S. Siddiqui ◽  
Haroon Khan ◽  
...  

Pistacia integerrimais one of twenty species among the genusPistacia. Long horn-shaped galls that develop on this plant are harvested and used in Ayurveda and Indian traditional medicine to make “karkatshringi”, a herbal medicine used for the treatment of asthma and different disorders of respiratory tract. However, until now, the molecular mechanisms of action of “karkatshringi” and its chemical characterization are partially known. This study deals with the isolation and characterization of the active constituents from the methanolic extract ofP. integerrimagalls and it was also oriented to evaluatein vitroandin silicotheir potential enzymatic inhibitory activity against phosphodiesterase-1 (PDE1), a well-known enzyme involved in airway smooth muscle activity and airway inflammation. Our results showed that the methanolic extract ofP. integerrimagalls and some of its active constituents [naringenin (1) and 3,5,7,4′-tetrahydroxy-flavanone (2)] are ablein vitroto inhibit PDE1 activity (59.20 ± 4.95%, 75.90 ± 5.90%, and 65.25 ± 5.25%, resp.) and demonstratein silicoan interesting interaction with this enzymatic site. Taken together, our results add new knowledge of chemical constituents responsible for the biological activity ofP. integerrimaand contextually legitimate the use of this plant in folk medicine.


Author(s):  
S. Sowmya ◽  
A. Jayaprakash

This study investigated the in-vitro antioxidant activity and antidiabetic effect of Muntingia calabura fruit extract by in-vitro α-amylase and α-glucosidase inhibitory activity. Muntingia calabura fruit was extracted with aqueous methanol by soxhlet extraction. The total phenols and total flavonoids contents were estimated and evaluated for antioxidant activities (DPPH, ABTS) and in-vitro antidiabetic activity by measuring their inhibitory activity on α-amylase and α-glucosidase levels. The findings showed that the fruit extract had high content of total phenol and exhibited moderate free radical scavenging activity. The fruit extract showed inhibitory effect on α-amylase [IC50Value =61.43 μg/mL] and α-glucosidase [IC50 Value=140.33 μg/mL] compared to standard acarbose. The fruit extract can be used as a potential source for the development of new hypoglycemic agents may be due to the presence of high phenol content.


2020 ◽  
Vol 19 (5) ◽  
pp. 1081-1086
Author(s):  
Htoo Tint San ◽  
Panitch Boonsnongchee ◽  
Waraporn Putalun ◽  
Boonchoo Sritularak ◽  
Kittisak Likhitwitayawuid

Purpose: To examine the glucose uptake stimulatory activity of the root extract of Cissus javana DC. (Vitaceae) in Lδ myotubes of rat, and also to identify the extract’s active principles.Methods: The methanol extract was prepared from Cissus javana tuberous roots and evaluated for glucose uptake stimulatory effects on Lδ rat muscle cells and inhibitory activity against α-glucosidase. The chemical components were isolated using several chromatographic techniques, and their structures characterized by spectroscopic methods. Each isolate was then assayed for glucose uptake stimulatory and α-glucosidase inhibitory activities.Results: The extract (100 μg/ml) exhibited glucose uptake stimulatory effect (70.9 % enhancement) and α-glucosidase enzyme inhibitory activity (100 % inhibition). Through chromatographic separation, bergenin, stigmast-4-en-3-one and β-sitosterol were isolated and identified. Bergenin, at 100 μg/ml (0.3046 mM), increased glucose uptake by Lδ myotubes by 50.5 % without toxicity. At the same concentration, bergenin showed no inhibition on α-glucosidase enzyme, while stigmast-4-en-3-one and β-sitosterol exhibited 98.6 and 40.6 %, inhibition, respectively.Conclusion: This study is the first report on the chemical constituents, and the glucose uptake stimulatory and α-glucosidase inhibitory activities of Cissus javana DC. roots. The findings reveal the antidiabetic potential of the plant and the glucose-uptake enhancing activity of bergenin. Keywords: Cissus javana, α-Glucosidase, Antidiabetes, Rat skeletal muscle cells, Bergenin


Author(s):  
Singaravelu Anand ◽  
Munichetty Arasakumari ◽  
Panneervelu Prabu ◽  
Arul Joseph Amalraj

<p><strong>Objective: </strong>The objective of the present study was to determine the cellular level effect on glucose uptake and aldose reductase inhibitory activity of different extracts of traditional medicinal plant <em>Psidium guajava</em>.</p><p><strong>Methods: </strong><em>Psidium guajava</em> was selected and subjected for successive extraction from non-polar to polar solvents and subjected to glucose uptake and aldose reductase inhibition assay.</p><p><strong>Results: </strong>Based on the results <em>Psidium guajava</em><em> </em>methanolic extract (PGME) showed an enhancement in the glucose uptake and also up-regulates the gene and protein level expression of IRβ, IRS-1, PI3K and GLUT4. Wortmannin, a specific PI3K inhibitor confirms that the active PGME recruits glucose uptake through a PI3K dependent pathway. In the assay of aldose reductase inhibitory activity, the results suggested that PGME possesses a significant inhibitory effect.</p><p><strong>Conclusion: </strong>The result obtained in the present study focuses on the anti-diabetic effect of PGME by studying cellular level glucose uptake in L6 myotubes and aldose reductase inhibitory activity.<strong></strong></p>


2020 ◽  
Vol 98 (12) ◽  
pp. 764-770
Author(s):  
Juan L. Monribot-Villanueva ◽  
Jonathan S. Rodríguez-Fuentes ◽  
Cristina Landa-Cansigno ◽  
Dennis A. Infante-Rodríguez ◽  
Juan P. Díaz-Abad ◽  
...  

Juniperus plant species are rich sources of bioactive secondary metabolites and are traditionally used for the treatment of several illnesses, including those related to hyperglycemia and diabetes. The major bioactive compounds identified in certain species of this genus are terpenes and phenolics. Juniperus deppeana Steud. is mainly used as a wood resource and its chemical composition has been partially established. Our goal was to perform a comprehensive profiling of a methanolic extract of leaves of J. deppeana and determine its potential as a source of α-amylase and α-glucosidase inhibitors. Terpene and phenolic compounds were putatively identified based on their accurate mass spectrometric data. Regarding terpenes, we found mainly diterpenes, specifically dehydroabietic acid-like, hinokiol-like, agathic acid-like, and dihydroxyabietatrienoic acid-like compounds. Isopimaric acid was also identified and its identity was confirmed by coelution with an authentic standard via comparing retention time, mass spectrum, and collisional cross section values. For phenolic compounds, we identified mainly compounds with a chemical structure similar to the biflavonoids amentoflavone and bilobetin. Besides, the methanolic extract of J. deppeana leaves show inhibition of α-amylase (IC50 = 85.11 ± 11.91 μg mL−1) and α-glucosidase (IC50 = 32.50 ± 3.40 μg mL−1) enzymes, demonstrating a potential alternative for the search of antidiabetic natural products.


2014 ◽  
Vol 12 (12) ◽  
pp. 895-900
Author(s):  
Puttanarasaiah Mahesh Kumar ◽  
Marikunte V Venkataranganna ◽  
Kirangadur Manjunath ◽  
Gollapalle L Viswanatha ◽  
Godavarthi Ashok

Processes ◽  
2019 ◽  
Vol 8 (1) ◽  
pp. 33 ◽  
Author(s):  
Samuel Odeyemi ◽  
John Dewar

The incidence of diabetes is on the rise and one of the medically active plants used for the treatment of diabetes in South Africa is Lauridia tetragona. The aim of this study is to investigate the antidiabetic property of the polyphenolics (PP) compounds isolated from the methanolic extract of Lauridia tetragona. The α-amylase, α-glucosidase, dipeptidyl peptidase IV (DPPIV), lipase inhibitory activities, and glucose uptake in HepG2 were investigated. The methanolic extract fractions of L. tetragona yielded six fractions (PP1–PP6) all of which showed weak inhibition against DPPIV and lipase compared to the standards. However, PP4 and PP6 showed the best inhibition against α-amylase (IC50 of 359.3 ± 2.11 and 416.82 ± 2.58 μg/mL, respectively) and α-glucosidase (IC50 of 95.93 ± 2.34 and 104.49 ± 2.21 μg/mL, respectively) and only PP4 (173.6%) resulted in enhanced glucose uptake in HepG2 cells compared to berberine (129.89%) and metformin (187.16%) used as positive controls. The previous investigation on PP4 and PP6 showed the presence of polyphenolics such as ferulic acid, coumaric acid, and caffeic acid. The results of this study suggest that L. tetragona could be suitable as an antidiabetic agent and justifies the folkloric use of the plant to treat diabetes.


Author(s):  
Reema Abu Khalaf ◽  
Shorooq Alqazaqi ◽  
Maram Aburezeq ◽  
Dima Sabbah ◽  
Ghadeer Albadawi ◽  
...  

Background: Diabetes mellitus is a chronic metabolic disorder, characterized by hyperglycemia over a prolonged period, disturbance of fat, protein and carbohydrate metabolism, resulting from defective insulin secretion, insulin action or both. Dipeptidyl peptidase-IV (DPP-IV) inhibitors are relatively a new class of oral hypoglycemic agents that reduces the deterioration of gut-derived endogenous incretin hormones that are secreted in response to food ingestion to stimulate the secretion of insulin from beta cells of pancreas. Objective: In this study, synthesis, characterization, and biological assessment of twelve novel phenanthridine sulfonamide derivatives 3a-3l as potential DPP-IV inhibitors was carried out. The target compounds were docked to study the molecular interactions and binding affinities against DPP-IV enzyme. Methods: The synthesized molecules were characterized using 1H-NMR, 13C-NMR, IR, and MS. Quantum-polarized ligand docking (QPLD) was also performed. Results: In vitro biological evaluation of compounds 3a-3l reveals comparable DPP-IV inhibitory activities ranging from 10%-46% at 100 µM concentration, where compound 3d harboring ortho-fluoro moiety exhibited the highest inhibitory activity. QPLD study shows that compounds 3a-3l accommodate DPP-IV binding site and form H-bonding with the R125, E205, E206, S209, F357, R358, K554, W629, S630, Y631, Y662, R669 and Y752 backbones. Conclusion: In conclusion, phenanthridine sulfonamides could serve as potential DPP-IV inhibitors that require further structural optimization in order to enhance their inhibitory activity.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Yarrappagaari Suresh ◽  
Gutha Rajasekar ◽  
Thopireddy Lavanya ◽  
Benne Lakshminarsimhulu ◽  
Kesireddy Sathyavelu Reddy ◽  
...  

Abstract Background Cleome viscosa is considered as an important medicinal plant extensively used in India, China, Bangladesh, and a few countries in Africa. In the present study, in vitro anti-radical and antidiabetic potential of isolated fractions of methanolic extract of C. viscosa whole plant (MeCV) has been investigated. The identification of polyphenols and their related functional groups in the bioactive fraction was categorized by using HPLC and FT-IR. Results The total phenolic and flavonoid contents of F-D were higher than those of F-A, F-B, and F-C. The F-D exhibited superior antioxidant capacity when compared with the remaining three fractions. However, the F-D showed the highest glucose diffusion activity over the 30 min–27 h incubation period and also inhibited both α-glucosidase and α-amylase enzyme activity. HPLC analysis revealed the presence of the two known compounds (protocatechuic acid hexoside, rutin) and six unknown compounds in the F-D. FTIR spectrum confirmed the presence of phenol group. Conclusion The isolated F-D obtained from MeCV displayed superior antioxidant and antidiabetic activity which indicate the presence of polyphenols in the fraction. The data findings of the present study support the traditional uses of the whole plant of C. viscosa as a promising natural source of biological medicines for oxidative stress and diabetes.


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