Keracyanin (chloride) is a potent and selective inhibitor of pancreatic α-amylase activity with IC50 value of 24.4μM [1]. By breaking the O-H bonds connected to the aromatic rings, Keracyanin exhibits excellent antioxidant activity and has a high efficiency in scavenging free radicals[2]. Keracyanin has been widely used to regulate the responses of monocytes and macrophages, and to inhibit the expression of inflammatory factors[3].
In vitro, Keracyanin pretreatment (200μM) for 24 hours significantly reversed the cytotoxicity induced by blue light, reduced the occurrence of oxidative stress and decreased the phosphorylation levels of FAK and MAPK[4]. Treatment with 120μM Keracyanin for 18 hours significantly induced apoptosis in HL-60 cells, accompanied by a significant increase in the activities of caspase-3 and caspase-9[5]. Treatment with 20μg/ml Keracyanin for 24 hours significantly reduced the cytotoxicity of H₂O₂ on RAW264.7 cells, and decreased the intracellular reactive oxygen species levels and DNA damage[6].
In vivo, oral single dose of Keracyanin (300mg/kg) plus maltose resulted in a significant decrease in the postprandial blood glucose level of rats 30 minutes after the loading[7]. In anesthetized rats, intravenous injection of Keracyanin (25μmol/kg) via the femoral artery can reduce the mean arterial pressure (MAP) within 5 seconds[8].
References:
[1] Baş Topcu K S, Sağ V, Genç N, et al. Phytochemical and Biological Evaluation of Cyanus celikhanensis Extract: An in Silico and in Vitro Approach[J]. Chemistry & Biodiversity, 2025, 22(5): e202402247.
[2] Newair E F, Shehata A G, Essam M. Electrochemical oxidation profile of anthocyanin keracyanin on glassy and screen-printed carbon electrodes[J]. Electrochem, 2023, 4(2): 273-281.
[3] Santamarina A B, Pisani L P, Baker E J, et al. Anti-inflammatory effects of oleic acid and the anthocyanin keracyanin alone and in combination: Effects on monocyte and macrophage responses and the NF-κB pathway[J]. Food & Function, 2021, 12(17): 7909-7922.
[4] Lee H Y, Kim J S. Cherry fruit anthocyanins cyanidin-3-O-glucoside and cyanidin-3-O-rutinoside protect against blue light-induced cytotoxicity in HaCaT cells[J]. Applied Biological Chemistry, 2023, 66(1): 3.
[5] Feng R, Ni H M, Wang S Y, et al. Cyanidin-3-rutinoside, a natural polyphenol antioxidant, selectively kills leukemic cells by induction of oxidative stress[J]. Journal of Biological Chemistry, 2007, 282(18): 13468-13476.
[6] Jung H, Kwak H K, Hwang K T. Antioxidant and antiinflammatory activities of cyanidin-3-glucoside and cyanidin-3-rutinoside in hydrogen peroxide and lipopolysaccharide-treated RAW264. 7 cells[J]. Food Science and Biotechnology, 2014, 23(6): 2053-2062.
[7] Adisakwattana S, Yibchok-Anun S, Charoenlertkul P, et al. Cyanidin-3-rutinoside alleviates postprandial hyperglycemia and its synergism with acarbose by inhibition of intestinal α-glucosidase[J]. Journal of Clinical Biochemistry and Nutrition, 2011, 49(1): 36-41.
[8] Thilavech T, Abeywardena M Y, Adams M, et al. Naturally occurring anthocyanin cyanidin-3-rutinoside possesses inherent vasorelaxant actions and prevents methylglyoxal-induced vascular dysfunction in rat aorta and mesenteric arterial bed[J]. Biomedicine & Pharmacotherapy, 2017, 95: 1251-1259.
Keracyanin (chloride)是一种强效、选择性的胰腺α-淀粉酶活性抑制剂，IC50值为24.4μM[1]。通过破坏与芳香环连接的O-H键，Keracyanin表现出优异的抗氧化活性，并具有高效的自由基清除能力[2]。Keracyanin已广泛应用于调节单核细胞和巨噬细胞的反应，并抑制炎症因子的表达[3]。
在体外，Keracyanin预处理（200μM）24小时显著逆转了蓝光诱导的细胞毒性，减少了氧化应激的发生，并降低了FAK和MAPK的磷酸化水平[4]。用120μM的Keracyanin处理18小时显著诱导了HL-60细胞凋亡，同时伴随着caspase-3和caspase-9活性的显著增加[5]。用20μg/ml的Keracyanin处理24小时显著降低了H2O2对RAW264.7细胞的细胞毒性，并降低了细胞内活性氧水平和DNA损伤 [6]。
在体内，口服单剂量Keracyanin（300mg/kg）加麦芽糖使大鼠在负荷后30分钟的餐后血糖水平显著降低[7]。在麻醉大鼠中，通过股动脉静脉注射Keracyanin（25μmol/kg）可在5秒内降低平均动脉压（MAP）[8]。