Flavonoids: Prospective Drug Candidates

Cazarolli, Luisa Helena; Zanatta, Leïla; Alberton, Elga Heloísa; Figueiredo, Mariana Sarto; Folador, Poliane; Damazio, Rosangela Guollo; Pizzolatti, Moacir Geraldo; Silva, Fátima Regina Mena Barreto

doi:10.2174/138955708786369564

Cited by 352 publications

(209 citation statements)

References 153 publications

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“…24) Sakuranetin, one of the flavonoids from I. viscosa, had been revealed to significantly increase insulinstimulated glucose uptake (1.5-fold at 100 mM in differentiated 3T3-L1 adipocytes), compared with control group. 15) In our study, the activity of 7-O-MA on 2-NBDG uptake was assessed in HepG2 cells and 3T3-L1 adipocytes by flow cytometry.…”

Section: Discussionmentioning

confidence: 99%

7-O-Methylaromadendrin Stimulates Glucose Uptake and Improves Insulin Resistance in Vitro

Zhang

Lee

Kim

et al. 2010

Biological & Pharmaceutical Bulletin

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The much more common condition of diabetes mellitus (DM) is type 2 DM, which represents 90 to 95% of all diagnosed cases of diabetes.1) Insulin resistance, a specific feature of type 2 DM, is the condition whereby major organs such as muscle and liver become resistant to the action of the hormone, leading to increased glucose output from the liver and reduced uptake and metabolism of glucose by other organs. 2)Studies on the molecular basis of insulin resistance have focused on the peroxisome proliferator-activated receptor g (PPARg). PPARg plays an important role in the regulation of genes involved in adipocyte differentiation, lipid storage, glucose metabolism 3) and insulin signal transduction. 4) In this regard, PPARg is a target for the treatment of insulin resistance as rosiglitazone, an anti-diabetic drug, does.Insulin binding to its receptor induces activation of a complex network of downstream molecules, including phosphatidylinositol 3-kinase (PI3K) and the serine/threonine kinase PI3K-linked protein kinase B (Akt/PKB).5,6) Activation of Akt/PKB stimulates membrane translocation of the glucose transporter, GLUT4, 7) leading to enhanced glucose uptake. Thus, Akt/PKB activation is a prerequisite for glucose uptake.Adenosine 5Ј-monophosphate-activated protein kinase (AMPK) acts as an intracellular energy sensor. Increased recruitment of the AMPK signaling system may be effective in correcting insulin resistance. 8) Activation of AMPK acutely stimulates glucose uptake via both GLUT1 and GLUT4, and enhances the long-term expression of GLUT4. 9) Thus, AMPK is responsible for mediating the stimulation of glucose uptake.The whole plant of Inula viscosa L. was traditionally used in folk medicine for treating DM.10-12) Previous investigations revealed the presence of a series of flavonoids in the whole plant including quercetin, apigenin, naringenin, sakuranetin, and aromadendrin. 13,14) Some of the flavonoids were reported to either improve or inhibit insulin-stimulated glucose uptake in adipocytes. [15][16][17] For instance, sakuranetin was revealed to enhance insulin-stimulated glucose uptake in adipocytes, 15) while apigenin suppressed. 17) Quercetin was reported with somewhat conflict in regulating insulin-stimulated glucose uptake.17,18) 7-O-Methylaromadendrin (7-O-MA) is also one of flavonoids isolated from I. viscosa. The preliminary data using our screening system indicated that 7-O-MA showed significant activities on stimulating insulininduced glucose uptake into both HepG2 cells and differentiated 3T3-L1 adipocytes. Therefore, the specific aim of this study was to investigate the ability of 7-O-MA to improve diabetic conditions and the possible molecular basis. Our results observed that 7-O-MA increased expression of PPARg2 and adipocyte-specific fatty acid binding protein The stimulation of glucose uptake into peripheral tissues is an important mechanism for the removal of glucose in blood and for the management of diabetes mellitus ( Key words 7-O-methylaromadendrin; glucose uptake; AMP-activated pr...

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Section: Discussionmentioning

confidence: 99%

7-O-Methylaromadendrin Stimulates Glucose Uptake and Improves Insulin Resistance in Vitro

Zhang

Lee

Kim

et al. 2010

Biological & Pharmaceutical Bulletin

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“…Recent studies have shown that phenolic phytochemicals exert anti-diabetic effect through inhibition of carbohydrate-hydrolyzing enzymes, such as alpha-amylase. In fact, many phenolic compounds and specially flavonoids have been reported as potential antidiabetic agents because they exert a good inhibitory action against α-amylase and could have potential prevention in diabetes mellitus as part of a dietary strategy [49]. These results were confirmed by others studies which showed that all of the tested Citrus flavonoids significantly inhibited amylase-catalyzed starch digestion [50].…”

Section: Inhibition Of α-Amylase Activitymentioning

confidence: 61%

Evaluation of In-vitro Antidiabetic and Hypolipidaemic Activities of Extracts Citrus Lemon Fruit

Basli¹,

Younici²,

Benkerrou³

et al. 2016

JESE-A

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Citrus genus is the most important fruit tree crop in the world and lemon is the third most important Citrus species. The evaluation of the potential inhibitory activity on α-amylase and pancreatic lipase by Citrus lemon fruits of Algerian origin aiming for new applications of the fruits in nutrition and health was carried out. Lemon fruit EtOAc (ethyl acetate) extract showed higher contents of phytochemicals such as total phenolics and flavonoids. Furthermore, lemon fruit showed higher potential for inhibitory effects on α-amylase and pancreatic lipase. It could be concluded that lemon fruits are of great value for nutrition and treatment of diet-related diseases such as obesity and diabetes.

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“…These findings suggest that flavonoids have negligible systemic antioxidant activity, and that the increase in antioxidant capacity of blood seen after consumption of flavonoid-rich foods is not caused directly by flavonoids, but is due to production of uric acid resulting from flavonoid depolymerization and excretion 18 .…”

Section: Resultsmentioning

confidence: 90%

“…Flavonoids present in the all three extracts of this plant can also inhibit the activity of many enzymes such as xanthine oxidase, peroxidase and nitric oxide synthase, which are supposed to be involved in free radical generation, thereby resulting in decreased oxidative damage of macromolecules 18 .Research at the Linus Pauling Institute and the European Food Safety Authority shows that flavonoids are poorly absorbed in the human body (less than 5%), with most of what is absorbed being quickly metabolized and excreted. These findings suggest that flavonoids have negligible systemic antioxidant activity, and that the increase in antioxidant capacity of blood seen after consumption of flavonoid-rich foods is not caused directly by flavonoids, but is due to production of uric acid resulting from flavonoid depolymerization and excretion 18 .…”

Section: Resultsmentioning

confidence: 99%

Qualitative Phytochemical Analysis of Ajwain (Trachyspermum Ammi) From North-West Iran

Mostafavi¹,

Pezhhanfar²

2015

Int. Res. J. Pharm.

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Most spices, owe their individual properties to the pharmacologically active secondary metabolites that they contain. In this study plant Ajwain (Trachyspermum ammi) from North-West Iran was screened for the presence of major phytochemical groups. Three solvent extracts (water, ethanol, ethylacetate) obtained from Ajwain (Trachyspermum ammi) traditionally used in the past and even now for various therapeutic effects including fatigue, diarrhea, bloating, abdominal tumors and especially in local area of Tabriz to cause to heal up the joint pain and loss of appetite. Phytochemical screening of the plant Ajwain (Trachyspermum ammi) showed the presence of carbohydrates, alkaloids, flavonoids, teriterpenoids, steroids, tannins, phenolic compounds, coumarins, resins, saponins, oil and fat, inorganic acids and ascorbic acid as major phytochemical groups. Ajwain (Trachyspermum ammi) tested negative for the presence of glycosides, starch, amino acids, protein, phelobotanin and free antraquinones and organic acids.

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Flavonoids: Prospective Drug Candidates

Cited by 352 publications

References 153 publications

7-O-Methylaromadendrin Stimulates Glucose Uptake and Improves Insulin Resistance in Vitro

7-O-Methylaromadendrin Stimulates Glucose Uptake and Improves Insulin Resistance in Vitro

Evaluation of In-vitro Antidiabetic and Hypolipidaemic Activities of Extracts Citrus Lemon Fruit

Qualitative Phytochemical Analysis of Ajwain (Trachyspermum Ammi) From North-West Iran

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