Pinocembrin is a flavonoid compound and a competitive histidine decarboxylase (HDC) inhibitor[1]. Pinocembrin has multiple biological activities, such as antibacterial, anti-inflammatory, antioxidant and neuroprotective effects[2, 3].
In vitro, Pinocembrin (25-200µM) treatment of A549 cells for 24-72h reduced cell viability, proliferation, promoted cell apoptosis, and reduced cell autophagy in a dose- and time-dependent manner[4]. Pinocembrin (100µM) treatment of colorectal cancer HT29 and HCT116 cells inhibited cell proliferation, migration, and invasiveness, and inhibited epithelial-mesenchymal transition[5]. Pinocembrin (25-100µM) treatment of ovarian cancer SKOV3 cells for 48h inhibited cell proliferation and migration and promoted cell apoptosis, and downregulated the mRNA levels of N-cadherin and GABAB receptors[6].
In vivo, oral administration of Pinocembrin (50mg/kg) to diabetic encephalopathy (DE) mice for 10 days significantly improved the behavioral and cognitive impairments of DE mice in the open field task and Morris water maze, significantly increased the neuronal survival rate in the frontal cortex and hippocampal CA3 region, inhibited the nuclear translocation of NF-κB in the cerebral cortex and hippocampus of mice, and reduced the expression of DETNF-α[7].
References:
[1] Hanieh H, Islam V I H, Saravanan S, et al. Pinocembrin, a novel histidine decarboxylase inhibitor with anti-allergic potential in in vitro[J]. European Journal of Pharmacology, 2017, 814: 178-186.
[2] Rasul A, Millimouno F M, Ali Eltayb W, et al. Pinocembrin: a novel natural compound with versatile pharmacological and biological activities[J]. BioMed research international, 2013, 2013(1): 379850.
[3] Shen X, Liu Y, Luo X, et al. Advances in biosynthesis, pharmacology, and pharmacokinetics of pinocembrin, a promising natural small-molecule drug[J]. Molecules, 2019, 24(12): 2323.
[4] Gong H. Pinocembrin suppresses proliferation and enhances apoptosis in lung cancer cells in vitro by restraining autophagy[J]. Bioengineered, 2021, 12(1): 6035-6044.
[5] Jiang L, Yang Y, Feng H, et al. Pinocembrin inhibits the proliferation, migration, invasiveness, and epithelial-mesenchymal transition of colorectal cancer cells by regulating LACTB[J]. Cancer Biotherapy & Radiopharmaceuticals, 2022, 37(7): 527-536.
[6] Gao J, Lin S, Gao Y, et al. Pinocembrin inhibits the proliferation and migration and promotes the apoptosis of ovarian cancer cells through down-regulating the mRNA levels of N-cadherin and GABAB receptor[J]. Biomedicine & Pharmacotherapy, 2019, 120: 109505.
[7] Pei B, Sun J. Pinocembrin alleviates cognition deficits by inhibiting inflammation in diabetic mice[J]. Journal of neuroimmunology, 2018, 314: 42-49.
Pinocembrin是一种黄酮类化合物，是竞争性的组氨酸脱羧酶（HDC）抑制剂[1]。Pinocembrin具有多种生物活性，例如抗菌、抗炎、抗氧化和神经保护作用等[2, 3]。
在体外，Pinocembrin（25-200µM）处理A549细胞24-72h，以剂量和时间依赖性方式降低了细胞活力，减少了增殖并促进了细胞的凋亡，减少了细胞的自噬[4]。Pinocembrin（100µM）处理结直肠癌HT29和HCT116细胞，抑制了细胞的增殖、迁移、侵袭性，抑制了上皮-间质转化[5]。Pinocembrin（25-100µM）处理卵巢癌SKOV3细胞48h，抑制了细胞的增殖和迁移并促进细胞凋亡，下调了N-钙粘着蛋白和GABAB受体的mRNA水平[6]。
在体内，Pinocembrin（50mg/kg）通过口服治疗糖尿病脑病（DE）小鼠10天，显著改善了DE小鼠在旷场任务和Morris水迷宫中的行为和认知障碍，显著增加了额叶皮质和海马CA3区域的神经元存活率，抑制了小鼠大脑皮层和海马中的NF-κB的核转位并降低DETNF-α的表达[7]。