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【Tangeretin】Main Citrus Flavonoids with Antidiabetic Effects

【Tangeretin】Main Citrus Flavonoids with Antidiabetic Effects

Tangeretin is an O-polymethoxylated flavone with methoxy groups at positions 5, 6, 7, 8, and 4’, and is found in tangerines and orange peel. It performs a number of biologically beneficial activities and has antioxidant, anti-inflammatory, antitumor, hepatoprotective, and neuroprotective potential. The properties of this flavonoid with respect to diabetes and its associated comorbidities have also been widely studied. Regarding the antidiabetic effects of tangeretin, in vitro evidence confirmed that it increased glucose uptake in differentiated 3T3-F442 adipocytes, even in the presence of insulin. In addition, results showed that 3T3-F442 adipocyte glucose uptake by the PI3K, Akt, and PKA pathways was increased following treatment with this polymethoxyflavonoid.

Sundaram, Shanthi, and Sachdanandam evaluated the antihyperglycemic potential of tangeretin regarding the activities of key enzymes linked with carbohydrate and glycogen metabolism in diabetic rats. Tangeretin treatment reduced blood glucose to near-normal levels, increased hemoglobin (Hb), and decreased hemoglobin (Hb)A1c levels, besides reversing the obese body weight and liver weight changes induced by diabetes. In addition, tangeretin normalized the activities of key hepatic enzymes and reinstated the levels of glycogen and the activities of glycogen synthase and glycogen phosphorylase. Histopathological analysis showed a significant increase in the regeneration of pancreatic β-cells in the islets of Langerhans in tangeretin-treated diabetic rats compared with those in the non-treated diabetic animals.

Furthermore, Sundaram, Shanthi, and Sachdanandam used a diabetic animal model to gain more therapeutic information on the mechanism of the action regarding the antioxidant, anti-inflammatory, and cardio-protective effectiveness of tangeretin. The oral administration of tangeretin reversed the body weight and heart weight changes by its insulinotropic action. Tangeretin administrated to the diabetic rats attenuated and normalized the lipid profiles in the plasma and cardiac tissues. These effects were mediated through the modification of the activities of key enzymes (LCAT, LPL, and HMG-CoA reductase) of lipid metabolism in the liver and increased GLUT4 expression in the heart tissues of diabetic rats. Moreover, tangeretin administration in diabetic rats decreased the levels of lipid peroxidation by increasing the activities of antioxidant enzymes (SOD, catalase (CAT), glutathione peroxidase (GPx), and glutathione reductase (GR)). It also caused a significant reduction in both inflammatory cytokines (TNF-α and IL-6) and cardiac marker enzymes (aspartate aminotransferase (AST), lactate dehydrogenase (LDH), and creatine phosphokinase (CPK)) in the plasma and heart tissues. Additionally, tangeretin treatment markedly decreased the nuclear translocation of NF-κB and TNF-α according to immunostaining in cardiac tissues. In summary, the results suggest that tangeretin treatment plays a beneficial role in regulating diabetes and its associated cardiovascular risk.

Chen, Ma, Sun, and Zhu elucidated the effects of tangeretin on high glucose-induced oxidative stress and extracellular matrix (ECM) accumulation in human glomerular mesangial cells (HGMCs) and discovered the underlying mechanisms. The important inflammatory factor TGF-β1’s expression induced by high glucose was efficiently suppressed in tangeretin-treated cells. The citrus molecule suppressed reactive oxygen species (ROS) and MDA production, while it increased SOD activity. In addition, high glucose treatment greatly increased the expression of fibronectin and collagen IV in HGMCs, which was then reversed by tangeretin treatment. The extracellular signal-regulated kinase (ERK) pathway plays an important role in the development of diabetic nephropathy, and this study concluded that tangeretin can modulate ERK signaling through preventing the activation of the ERK signaling pathway in high glucose-stimulated mast cells (MCs). These results highlighted tangeretin as a curative agent in the management of diabetic nephropathy, the leading cause of morbidity and mortality resulting in end-stage renal disease.

Therefore, tangeretin has a promising role in research into diabetic therapy, since its effects appear to be consistent and reliable in diabetic preclinical studies. Its major effects include attenuating biochemical parameters related to diabetic conditions, modulating key enzymes of lipid and glycolytic metabolism, attenuating inflammation and oxidative-stress-signaling markers, and exhibiting protective effects on the heart and liver tissues, which are considered to be vital in diabetic metabolic disorders.

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