(-)-epicatechin gallate is a natural flavanol belonging to the ester-type catechins in tea polyphenols. (-)-epicatechin gallate exerts anti-inflammatory effects by inhibiting cyclooxygenase-1 (COX-1) with an IC₅₀ of 7.5μM[1-2]. (-)-epicatechin gallate is applicable for research in metabolic diseases, bacterial infections, and cancer[3-4].
In vitro, pretreatment of human brain microvascular endothelial cells (HBMVECs) with (-)-epicatechin gallate (2μM) for 1 hour followed by culture under oxygen-glucose deprivation/reoxygenation (OGD/R) conditions, (-)-Epicatechin gallate significantly promoted cell proliferation, migration, and tube formation, inhibited OGD/R-induced apoptosis and autophagy, and reduced ROS, LDH, and MDA levels while increased SOD activity[5]. Pretreatment of vascular smooth muscle cells (VSMCs) with (-)-epicatechin gallate (10–40μM) for 24 hours followed by angiotensin II (Ang II; 1×10⁻⁷μM) induction, (-)-epicatechin gallate significantly inhibited abnormal proliferation and cell cycle progression of VSMCs (increase in G0/G1 phase, decrease in S phase), reduced ROS and TNF-α levels, downregulated gene and protein expression of VEGFA, MMP-9, CASP3, and MMP-2, and inhibited the PI3K/AKT phosphorylation pathway[6].
In vivo, intraperitoneal administration of (-)-epicatechin gallate (100mg/kg/day; single injection 1 hour before hypoxia exposure) to a hypobaric hypoxia-induced high-altitude cerebral edema (HACE) mouse model (C57BL/6J), (-)-epicatechin gallate significantly reduced brain water content and blood-brain barrier permeability, suppressed microglial activation and neuroinflammatory responses, and improved pathological edema injury[7]. Oral administration of (-)-epicatechin gallate (160mg/kg/day) to naturally aged C57BL/6J mice (starting at 54 weeks of age for 8 weeks), (-)-epicatechin gallate significantly increased muscle mass and exercise endurance, promoted skeletal muscle differentiation-related gene expression, and regulated testosterone anabolic pathways to improve sarcopenic phenotypes[8].
References:
[1] Seeram NP, Zhang Y, Nair MG. Inhibition of proliferation of human cancer cells and cyclooxygenase enzymes by anthocyanidins and catechins. Nutr Cancer. 2003;46(1):101-6.
[2] Waffo-Téguo P, Hawthorne ME, Cuendet M, et al. Potential cancer-chemopreventive activities of wine stilbenoids and flavans extracted from grape (Vitis vinifera) cell cultures. Nutr Cancer. 2001;40(2):173-9.
[3] Teng F, Wang L, Wen J, et al. Epicatechin gallate and its analogues interact with sortase A and β-lactamase to suppress Staphylococcus aureus virulence. Front Cell Infect Microbiol. 2025 Mar 25;15:1537564.
[4] Huang D, Su Y, Li M, et al. (-)-Epicatechin gallate ameliorates cyprodinil-induced cardiac developmental defects through inhibiting aryl hydrocarbon receptor in zebrafish. Birth Defects Res. 2024 May;116(5):e2350.
[5] Fu B, Zeng Q, Zhang Z, et al. Epicatechin Gallate Protects HBMVECs from Ischemia/Reperfusion Injury through Ameliorating Apoptosis and Autophagy and Promoting Neovascularization. Oxid Med Cell Longev. 2019 Mar 6;2019:7824684.
[6] Yu J, Song H, Zhou L, et al. (-)-Epicatechin gallate prevented atherosclerosis by reducing abnormal proliferation of VSMCs and oxidative stress of AML 12 cells. Cell Signal. 2024 Sep;121:111276.
[7] Huang Z, Liu M, Zhou Y, et al. Epicatechin Gallate Regulation of Steroid Hormone Levels Improves Sarcopenia in C57BL/6J Mice. Foods. 2025 Jul 16;14(14):2495.
[8] Huang D, Su Y, Li M, et al. (-)-Epicatechin gallate ameliorates cyprodinil-induced cardiac developmental defects through inhibiting aryl hydrocarbon receptor in zebrafish. Birth Defects Res. 2024 May;116(5):e2350.
(-)-epicatechin gallate是一种天然黄烷醇，属于茶多酚中的酯型儿茶素类化合物，(-)-epicatechin gallate通过抑制环加氧酶-1(COX-1)发挥抗炎作用（IC₅₀=7.5μM）[1-2]。(-)-epicatechin gallate可用于代谢性疾病、细菌感染及肿瘤的相关研究[3-4]。
在体外，(-)-epicatechin gallate（2μM）预处理人脑微血管内皮细胞（HBMVECs）1小时，随后在氧糖剥夺/复氧（OGD/R）条件下培养，(-)-epicatechin gallate显著促进细胞增殖、迁移和管状结构形成，并抑制OGD/R诱导的细胞凋亡和自噬，同时降低ROS、LDH和MDA水平并提高SOD活性[5]。(-)-epicatechin gallate（10–40μM）预处理血管平滑肌细胞（VSMCs）24小时，随后在血管紧张素Ⅱ（Ang II；1×10-7μM）诱导条件下培养，(-)-epicatechin gallate显著抑制VSMCs的异常增殖和周期进展（G0/G1期增加、S期减少），降低ROS和TNF-α水平，并下调VEGFA、MMP-9、CASP3和MMP-2的基因和蛋白表达，同时抑制PI3K/AKT磷酸化通路[6]。
在体内，(-)-epicatechin gallate（100mg/kg/day；缺氧暴露前1小时单次注射）腹腔注射处理缺氧诱导的高海拔脑水肿（HACE）模型C57BL/6J小鼠，(-)-epicatechin gallate显著降低脑水含量和血脑屏障通透性，抑制小胶质细胞活化和神经炎症反应，并改善脑水肿病理损伤[7]。(-)-epicatechin gallate（160mg/kg/day）灌胃处理自然衰老的C57BL/6J小鼠（从54周龄开始，持续8周），(-)-epicatechin gallate显著提高肌肉质量和运动耐力，促进骨骼肌分化相关基因表达，并调节睾酮合成代谢途径以改善肌少症表型[8]。