Pelargonidin (chloride) is an anthocyanin with multiple biological activities such as antioxidant, anti-inflammatory, anti-cancer, and neuroprotective activities[1, 2]. Pelargonidin (chloride) can inhibit the activity of cytochrome P450 family 1 subfamily A member 1 (CYP1A1) with an IC50 value of 33µM[3]. Pelargonidin can improve acetaminophen-induced mouse hepatotoxicity by inhibiting ROS-induced inflammatory apoptotic response[4].
In vitro, Pelargonidin (chloride) (10-100μM) treatment of mouse epidermal cells (JB6 P+ cells) for 1-5 days inhibited cell viability in a dose- and time-dependent manner, enhanced the expression of the Nrf2 gene, and promoted the expression of antioxidant enzymes (such as HO-1 and NQO1)[5]. Pelargonidin (chloride) (1-120μM) treated A549 cells for 48h inhibited cell viability in a dose-dependent manner with an IC50 value of 20µM, promoted the production of endogenous ROS, and reduced mitochondrial membrane potential[6].
In vivo, oral administration of Pelargonidin (chloride) (10mg/kg) to Alzheimer's disease (AD) rats for 2 weeks significantly improved Aβ25-35-induced memory deficits, improved rat hippocampal acetylcholinesterase (AChE) activity, and reduced glial fibrillary acidic protein (GFAP) levels[7].
References:
[1] Jeong S, Ku S K, Bae J S. Anti-inflammatory effects of pelargonidin on TGFBIp-induced responses[J]. Canadian Journal of Physiology and Pharmacology, 2017, 95(4): 372-381.
[2] Kooshki L, Fakhri S, Abbaszadeh F, et al. Pelargonidin improves functional recovery and attenuates neuropathic pain following spinal cord injury in rats: relevance to its neuroprotective, antioxidant, and anti-inflammatory effects[J]. Frontiers in Pharmacology, 2025, 16: 1547187.
[3] Kamenickova A, Anzenbacherova E, Pavek P, et al. Pelargonidin activates the AhR and induces CYP1A1 in primary human hepatocytes and human cancer cell lines HepG2 and LS174T[J]. Toxicology letters, 2013, 218(3): 253-259.
[4] Seo M, Kim H, Lee J H, et al. Pelargonidin ameliorates acetaminophen-induced hepatotoxicity in mice by inhibiting the ROS-induced inflammatory apoptotic response[J]. Biochimie, 2020, 168: 10-16.
[5] Li S, Li W, Wang C, et al. Pelargonidin reduces the TPA induced transformation of mouse epidermal cells–potential involvement of Nrf2 promoter demethylation[J]. Chemico-biological interactions, 2019, 309: 108701.
[6] Yue L, Li Y, Luo Y, et al. Pelargonidin inhibits cell growth and promotes oxidative stress‐mediated apoptosis in lung cancer A549 cells[J]. Biotechnology and Applied Biochemistry, 2024, 71(5): 1195-1203.
[7] Sohanaki H, Baluchnejadmojarad T, Nikbakht F, et al. Pelargonidin improves memory deficit in amyloid β25-35 rat model of Alzheimer’s disease by inhibition of glial activation, cholinesterase, and oxidative stress[J]. Biomedicine & pharmacotherapy, 2016, 83: 85-91.
Pelargonidin (chloride)是一种花青素，具有抗氧化、抗炎、抗癌、神经保护等多种生物活性[1, 2]。Pelargonidin (chloride)能够抑制细胞色素P450家族1亚家族A成员1（CYP1A1）活性，IC50值为33µM[3]。Pelargonidin能够通过抑制ROS诱导的炎症性凋亡反应来改善对乙酰氨基酚诱导的小鼠肝毒性[4]。
在体外，Pelargonidin (chloride)（10-100μM）处理小鼠表皮细胞（JB6 P+细胞）1-5天，以剂量和时间依赖性方式抑制了细胞活力，增强了Nrf2基因的表达，促进了抗氧化酶（如HO-1、NQO1）的表达[5]。Pelargonidin (chloride)（1-120μM）处理A549细胞48h，以剂量依赖性方式抑制了细胞活力，IC50值为20µM，促进了内源性ROS的产生，降低了线粒体膜电位[6]。
在体内，Pelargonidin (chloride)（10mg/kg）通过口服治疗阿尔兹海默病（AD）大鼠2周，显著改善了Aβ25-35诱导的记忆缺陷，改善了大鼠海马乙酰胆碱酯酶 （AChE）活性并降低了神经胶质纤维酸性蛋白（GFAP）水平[7]。