Eriocitrin is a special flavonoid glycoside found in lemons, and its clinical therapeutic potential has been preliminarily confirmed. Studies have shown that its potent antioxidant activity can reduce oxidative stress-related damage and show metabolic regulatory effects on lowering blood lipids and improving insulin sensitivity. In terms of anti-inflammatory, it can alleviate chronic low-grade inflammatory states and has a protective effect on the cardiovascular and liver. In addition, preliminary studies have found that it may have some interventional effect on neurodegenerative diseases and obesity. At present, it is believed that it has application prospects in the field of adjuvant therapy of metabolic syndrome, anti-aging and functional food, but more clinical studies are needed to verify its efficacy and safety.

Pharmacological action

-Hypoglycaemic effect

Eriocitrin, a characteristic bioflavonoid compound, has demonstrated well-defined glycaemic regulatory efficacy by inhibiting the activity of digestive enzymes in the upper gastrointestinal tract responsible for breaking down sucrose and carbohydrates, thereby delaying intestinal absorption of glucose, effectively controlling postprandial blood glucose spikes, and reducing dramatic fluctuations in insulin levels. Studies have shown that the low-dose Eriocitrin group is characterised by a significant decrease in blood glucose concentration and moderate levels of insulin secretion, which can effectively maintain blood glucose homeostasis.

Figure 1 Effects of different doses of Eriocitrin on (A) blood glucose and (B) insulin levels in mice on a high-fat diet.

-Antioxidant

As one of the main flavonoid glycosides in lemon, Eriocitrin has significant antioxidant activity, and a number of studies have confirmed that Eriocitrin's free radical scavenging ability and reducing ability are superior to common antioxidants such as vitamin C. Studies have shown that Eriocitrin can significantly enhance the antioxidant capacity of sepsis model mouse cells, which is manifested by increased catalase (CAT) activity and decreased reactive oxygen species (ROS) level, thereby effectively alleviating the histopathological damage caused by oxidative stress.

Figure 2 Effect of Eriocitrin on antioxidant capacity in sepsis mice. (A) CAT level. (B) Quantitative analysis of ROS fluorescence intensity.

-Anti-inflammatory

The natural flavonoid glycoside eriocitrin can alleviate the pathological response of a variety of inflammatory models, including inhibiting the release of inflammatory factors, relieving tissue oedema, etc., and has an improvement effect on acute and chronic inflammation. Studies have confirmed that Eriocitrin intervention can significantly down-regulate the expression of key inflammatory markers in the colon tissue of mice in a model of acute colitis induced by dextran sodium sulfate (DSS).

Figure 3 Effect of Eriocitrin on the expression of key inflammatory markers in colon cells of mice in an acute colitis model.

-Improve obesity effects

As a natural flavonoid glycoside, eriocitrin can inhibit the abnormal increase of body weight to a certain extent by regulating the body's energy metabolism balance, and at the same time has an ameliorating effect on the accompanying symptoms such as lipid metabolism disorders and insulin resistance that are common in obesity. Studies have shown that eriocitrin was able to significantly improve energy expenditure (EE) and increase muscle weight and brown adipose tissue (BAT) content in mice fed a high-fat diet.

Figure 4 Effects of Eriocitrin on mice fed a high-fat diet. (A) Energy expenditure. (B) Muscle weight. (C) BAT weight.

-Anticancer

Eriocitrin is one of the main active ingredients in limonosides, which can inhibit the proliferation of tumour cells and the growth of some tumour models, improve tumour-related abnormal states, and enhance the anti-tumour effect of chemotherapy drugs, which has a synergistic therapeutic effect. Studies have shown that Eriocitrin significantly inhibits the proliferation of MCF-7 cells in human breast cancer in a concentration-dependent manner.

Figure 5 MCF-7 cells were treated with different concentration gradients of Eriocitrin for 24 hours.

-Other effects

Eriocitrin also has numerous pharmacological effects, including hepatoprotective (reducing chemical liver injury, reducing transaminases, and inhibiting liver fibrosis), cardiovascular protection (improving endothelial function, regulating blood pressure, and preventing atherosclerosis), and neuroprotective effects, as well as improving neurodegenerative lesions, and exhibiting immunomodulatory, antibacterial, and antiviral activities. These broad biological activities make them show good application potential in the field of functional food and drug research and development, but their clinical translation value still needs to be confirmed by further research. 

[1] Ferreira PS, Manthey JA, Nery MS, et al. Low doses of eriocitrin attenuate metabolic impairment of glucose and lipids in ongoing obesogenic diet in mice[J]. J Nutr Sci, 2020, 9: e59.

[2] Wu M, Huang Z, Akuetteh PDP, et al. Eriocitrin prevents Sepsis-induced acute kidney injury through anti-inflammation and anti-oxidation via modulating Nrf2/DRP1/OPA1 signaling pathway[J]. Biochim Biophys Acta Gen Subj. 2024, 1868(7): 130628.

[3] Guo G, Shi W, Shi F, et al. Anti-inflammatory effects of eriocitrin against the dextran sulfate sodium-induced experimental colitis in murine model[J]. J Biochem Mol Toxicol, 2019, 33(11): e22400.

[4] Kwon EY, Choi MS. Eriocitrin Improves Adiposity and Related Metabolic Disorders in High-Fat Diet-Induced Obese Mice[J]. J Med Food, 2020, 23(3): 233-241.

[5] Yuan C, Chen G, Jing C, et al. Eriocitrin, a dietary flavonoid suppressed cell proliferation, induced apoptosis through modulation of JAK2/STAT3 and JNK/p38 MAPKs signaling pathway in MCF-7 cells[J]. J Biochem Mol Toxicol, 2022, 36(1): e22943.