Neoeriocitrin is a highly potent inhibitor of lactate dehydrogenase A, with an IC50 value of 11.198 ± 0.90µM [1]. Neoeriocitrin has an inhibition effect on pyruvate kinase isoenzyme M2 at a very low concentration of 0.65mM[2]. Neoeriocitrin has been widely used in enzyme inhibition studies and anti-inflammatory experiments[3].
In vitro, Neoeriocitrin treatment of MC3T3-E1 cells at a concentration of 2μg/ml for 72 hours showed great proliferation and osteogenic differentiation effects, Neoeriocitrin significantly enhanced the alkaline phosphatase (ALP) activity of MC3T3-E1 cells, and up-regulated the expression of Runx2, COLI, and OCN[4]. Treatment of human cartilage explants with Neoeriocitrin at a concentration of 50µg/mL for 120h significantly inhibited IL-1β-induced NO production, inhibited proteolytic enzymes (especially matrix metalloproteinase-13), prevented glycosaminoglycan (GAG) release, and reduced structural and mechanical damage to cartilage[5]. Pretreatment of INS-1E cells with Neoeriocitrin (1µM) for 21 hours increased cell viability and reduced the number of apoptotic cells induced by streptozotocin[6].
References:
[1] Yırtıcı Ü. Natural flavonoids as promising lactate dehydrogenase A inhibitors: Comprehensive in vitro and in silico analysis[J]. Archiv der Pharmazie, 2024, 357(9): 2400455.
[2] Aslan E, Guler C, Adem S. In vitro effects of some flavonoids and phenolic acids on human pyruvate kinase isoenzyme M2[J]. Journal of enzyme inhibition and medicinal chemistry, 2016, 31(2): 314-317.
[3] Ahn, J.S.; Lee, C.H.; Liu, X.-Q.; Hwang, K.W.; Oh, M.H.; Park, S.-Y.; Whang, W.K. Neuroprotective Effects of Phenolic Constituents from Drynariae Rhizoma. Pharmaceuticals 2024, 17, 1061.
[4] Li L, Zeng Z, Cai G. Comparison of neoeriocitrin and naringin on proliferation and osteogenic differentiation in MC3T3-E1[J]. Phytomedicine, 2011, 18(11): 985-989.
[5] Crascì L, Panico A. Protective effects of many citrus flavonoids on cartilage degradation process[J]. Journal of Biomaterials and Nanobiotechnology, 2013, 4(3): 279-283.
[6] Aldemir E E, Selmanoğlu G, Karacaoğlu E. The Potential Protective Role of Neoeriocitrin in a Streptozotocin-Induced Diabetic Model in INS-1E Pancreatic ß-Cells[J]. Brazilian Archives of Biology and Technology, 2022, 66: e23220138.
Neoeriocitrin是一种高效的乳酸脱氢酶A抑制剂，IC50值为11.198±0.90µM[1]。Neoeriocitrin在0.65mM的极低浓度下对丙酮酸激酶同工酶M2表现出抑制作用[2]。Neoeriocitrin已广泛应用于酶活性抑制研究和抗炎实验[3]。
在体外，以2μg/ml浓度的Neoeriocitrin处理MC3T3-E1细胞72小时后，细胞表现出显著的增殖和成骨分化特征，Neoeriocitrin能显著增强MC3T3-E1细胞的碱性磷酸酶（ALP）活性，并上调Runx2、COLI和OCN的表达[4]。在人类软骨外植体实验中，50µg/mL浓度的Neoeriocitrin处理120小时可显著抑制IL-1β诱导的NO生成，抑制蛋白水解酶（特别是基质金属蛋白酶-13）活性，防止糖胺聚糖（GAG）释放，并减轻软骨的结构和机械损伤[5]。用1µM的Neoeriocitrin预处理INS-1E细胞21小时，可提高细胞活力并减少链脲佐菌素诱导的凋亡细胞数量[6]。