Identification of mangiferin as a potential Glucokinase activator by structure-based virtual ligand screening

Min, Qiuxia; Cai, Xinpei; Sun, Wenping; Gao, Fei; Li, Zhimei; Zhang, Qian; Wan, Luo-Sheng; Li, Hua; Chen, Jiachun

doi:10.1038/srep44681

Cited by 33 publications

(15 citation statements)

References 33 publications

(41 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…A more recent work by Min et al [120], using structure-based virtual ligand screening identified mangiferin as a potential glucokinase activator. In the same study, using an in vitro cell-based assay, mangiferin was shown to effectively improve postprandial blood glucose levels by promoting a remarkable enhancement of glucose consumption in HepG2 and C2C12 cells.…”

Section: South African Herbal Tisanesmentioning

confidence: 99%

The Potential of South African Herbal Tisanes, Rooibos and Honeybush in the Management of Type 2 Diabetes Mellitus

2018

View full text Add to dashboard Cite

Diabetes mellitus is a metabolic disease that can lead to high morbidity, mortality and long-term complications. Available treatment strategies, which are mainly based on treating hyperglycemia, with insulin and other pharmacological agents are not completely efficient and can even lead to development of unwanted side effects. Scientific evidence suggests that bioactive compounds from teas and other plant-based foods, which are known source of natural antioxidants, could be an attractive strategy to preferentially treat and manage type 2 diabetes mellitus (T2DM) and thus, have significant therapeutic implications. In this review, we attempt an in-depth analysis and discussion of the current progress in our understanding of the antidiabetic potential of two commercialized South Africa herbal tisanes—Rooibos and Honeybush and their polyphenols.

show abstract

Section: South African Herbal Tisanesmentioning

confidence: 99%

The Potential of South African Herbal Tisanes, Rooibos and Honeybush in the Management of Type 2 Diabetes Mellitus

2018

View full text Add to dashboard Cite

show abstract

“…For example, in the discovery of GK activator, the half maximal effective concentration (EC 50 ) of synthesized activator TMG-123 was <1 µM, 129 while to our knowledge, the best EC 50 of the natural product, mangiferin (a xanthone glucoside from the leaves of Mangifera indica and the root of Anemarrhena asphodeloides ), was more than 100 µM. 130 In addition to GK activation activity, mangiferin has various other functions via diverse targets, such as antioxidant, antimicrobial, antidiabetic, antiallergic and anticancer, 131 which exhibits its nonselective characteristic feature.…”

Section: Discussionmentioning

confidence: 80%

Natural products, an important resource for discovery of <br />multitarget drugs and functional food for regulation of hepatic glucose metabolism

Li¹,

Yu²,

Wang³

et al. 2018

DDDT

View full text Add to dashboard Cite

Imbalanced hepatic glucose homeostasis is one of the critical pathologic events in the development of metabolic syndromes (MSs). Therefore, regulation of imbalanced hepatic glucose homeostasis is important in drug development for MS treatment. In this review, we discuss the major targets that regulate hepatic glucose homeostasis in human physiologic and pathophysiologic processes, involving hepatic glucose uptake, glycolysis and glycogen synthesis, and summarize their changes in MSs. Recent literature suggests the necessity of multitarget drugs in the management of MS disorder for regulation of imbalanced glucose homeostasis in both experimental models and MS patients. Here, we highlight the potential bioactive compounds from natural products with medicinal or health care values, and focus on polypharmacologic and multitarget natural products with effects on various signaling pathways in hepatic glucose metabolism. This review shows the advantage and feasibility of discovering multicompound–multitarget drugs from natural products, and providing a new perspective of ways on drug and functional food development for MSs.

show abstract

“…Test compounds that are high in order formed π-π bonds, hydrophobic bonds and H-bonds with GK and AR, while metformin and miglitol showed only H-bonding. Moreover all ligands interact with allosteric binding site of GK (Matschinsky et al, 2006 ; Min et al, 2017 ) and AR (Antony and Vijayan, 2015 ). The ligands order of affinity against AA was found as; DPAA > DPC1 > DMC1 > DOC1 > CPAA > PFA > miglitol.…”

Section: Discussionmentioning

confidence: 99%

Computational and Pharmacological Evaluation of Ferrocene-Based Acyl Ureas and Homoleptic Cadmium Carboxylate Derivatives for Anti-diabetic Potential

et al. 2018

View full text Add to dashboard Cite

We investigated possible anti-diabetic effect of ferrocene-based acyl ureas: 4-ferrocenyl aniline (PFA), 1-(4-chlorobenzoyl)-3-(4-ferrocenylphenyl) urea (DPC1), 1-(3-chlorobenzoyl)-3-(4-ferrocenylphenyl) urea (DMC1), 1-(2-chlorobenzoyl)-3-(4-ferrocenylphenyl) urea (DOC1) and homoleptic cadmium carboxylates: bis (diphenylacetato) cadmium (II) (DPAA), bis (4-chlorophenylacetato) cadmium (II) (CPAA), using in silico and in vivo techniques. PFA, DPC1, DMC1, DOC1, DPAA and CPAA exhibited high binding affinities (ACE ≥ −350 Kcal/mol) against targets: aldose reductase, peroxisome proliferator-activated receptor γ, 11β-hydroxysteroid dehydrogenase-1, C-alpha glucosidase and glucokinase, while showed moderate affinities (ACE ≥ −250 Kcal/mol) against N-alpha glucosidase, dipeptidyl peptidase-IV, phosphorylated-Akt, glycogen synthase kinase-3β, fructose-1,6-bisphosphatase and phosphoenolpyruvate carboxykinase, whereas revealed lower affinities (ACE < −250 Kcal/mol) vs. alpha amylase, protein tyrosine phosphatases 1B, glycogen phosphorylase and phosphatidylinositol 3 kinase. In alloxan (300 mg/Kg)-induced diabetic mice, DPAA and DPC1 (1–10 mg/Kg) at day 1, 5, 10, 15, and 20th decreased blood glucose levels, compared to diabetic control group and improved the treated animals body weight. DPAA (10 mg/Kg) and DPC1 (5 mg/Kg) in time-dependent manner (30–120 min.) enhanced tolerance of oral glucose overload in mice. DPAA and DPCI dose-dependently at 1, 5, and 10 mg/Kg decreased glycosylated hemoglobin levels in diabetic animals, as caused by metformin. These results indicate that aforementioned derivatives of ferrocene and cadmium possess anti-diabetic potential.

show abstract

Identification of mangiferin as a potential Glucokinase activator by structure-based virtual ligand screening

Cited by 33 publications

References 33 publications

The Potential of South African Herbal Tisanes, Rooibos and Honeybush in the Management of Type 2 Diabetes Mellitus

The Potential of South African Herbal Tisanes, Rooibos and Honeybush in the Management of Type 2 Diabetes Mellitus

Natural products, an important resource for discovery of <br />multitarget drugs and functional food for regulation of hepatic glucose metabolism

Computational and Pharmacological Evaluation of Ferrocene-Based Acyl Ureas and Homoleptic Cadmium Carboxylate Derivatives for Anti-diabetic Potential

Contact Info

Product

Resources

About