Eicosapentaenoic Acid (EPA) is an orally active omega-3 (ω-3) long-chain polyunsaturated fatty acid (PUFA) and a precursor to prostaglandin-3, thromboxane-3, and leukotriene-5 eicosanoids[1]. Eicosapentaenoic Acid has anti-inflammatory, anti-cardiovascular disease, and anti-diabetic effects. It is found in large quantities in marine organisms[2, 3].
In vitro, Eicosapentaenoic Acid (100 µM) significantly reduces the level of the inflammatory cytokine IL-8 in MDA-MB-231 and MCF-7 breast cancer cells after 48 hours of treatment [4]. Eicosapentaenoic Acid (0.1 μM, 1 μM, 10 μM) induces apoptosis in a dose-dependent manner and activates caspase-3, -7, -9, and PARP enzymes in TE11 and KYSE180 esophageal cancer cells after 24 hours of treatment [5]. Eicosapentaenoic Acid (25 μM) significantly inhibits the proliferation of HT-29 colon cancer cells and downregulates the PI-3K/Akt/mTOR signaling pathway after 24 hours of treatment [6].
In vivo, Eicosapentaenoic Acid (500 mg/kg) administered orally to type 2 diabetic Goto-Kakizaki rats for 4 weeks, significantly reduces circulating insulin levels by 48%, and increases GLUT4 mRNA content in skeletal muscle and adipose tissue [7].
References:
[1] Mason R P, Libby P, Bhatt D L. Emerging mechanisms of cardiovascular protection for the omega-3 fatty acid eicosapentaenoic acid[J]. Arteriosclerosis, thrombosis, and vascular biology, 2020, 40(5): 1135-1147.
[2] Šimat V, Elabed N, Kulawik P, et al. Recent advances in marine-based nutraceuticals and their health benefits[J]. Marine drugs, 2020, 18(12): 627.
[3] Nobre M E P, Correia A O, de Brito Borges M, et al. Eicosapentaenoic acid and docosahexaenoic acid exert anti-inflammatory and antinociceptive effects in rodents at low doses[J]. Nutrition research, 2013, 33(5): 422-433.
[4] Rasha F, Kahathuduwa C, Ramalingam L, et al. Combined effects of eicosapentaenoic acid and adipocyte renin–angiotensin system inhibition on breast cancer cell inflammation and migration[J]. Cancers, 2020, 12(1): 220.
[5] Mizoguchi K, Ishiguro H, Kimura M, et al. Induction of apoptosis by eicosapentaenoic acid in esophageal squamous cell carcinoma[J]. Anticancer research, 2014, 34(12): 7145-7149.
[6] Tang F Y, Cho H J, Pai M H, et al. Concomitant supplementation of lycopene and eicosapentaenoic acid inhibits the proliferation of human colon cancer cells[J]. The Journal of nutritional biochemistry, 2009, 20(6): 426-434.
[7] Figueras M, Olivan M, Busquets S, et al. Effects of eicosapentaenoic acid (EPA) treatment on insulin sensitivity in an animal model of diabetes: improvement of the inflammatory status[J]. Obesity, 2011, 19(2): 362-369.
Eicosapentaenoic Acid（EPA）二十碳五烯酸是一种具有口服活性的omega-3（ω-3）长链多不饱和脂肪酸（PUFA），是前列腺素3、血栓素3和白三烯5类二十烷酸的前体[1]。Eicosapentaenoic Acid具有抗炎、抗心血管疾病、抗糖尿病等作用，在海洋生物中大量存在[2, 3]。
在体外，Eicosapentaenoic Acid（100 µM）处理乳腺癌MDA-MB-231和MCF-7细胞48h，显著降低了细胞内炎症因子IL-8水平[4]。Eicosapentaenoic Acid（0.1 μM、1 μM、10 μM）处理食管癌TE11和KYSE180细胞24h，以剂量依赖性方式诱导细胞凋亡，激活半胱天冬酶-3、-7、-9和PARP酶[5]。Eicosapentaenoic Acid（25μM）处理结肠癌HT-29细胞24h，显著抑制细胞增殖，下调了PI-3K/Akt/mTOR信号通路[6]。
在体内，Eicosapentaenoic Acid（500 mg/kg）通过口服治疗2型糖尿病Goto-Kakizaki大鼠4周，显著减少了循环胰岛素（48%），还导致骨骼肌和脂肪组织中的GLUT4 mRNA含量增加[7]。