Neoeriocitrin
(Synonyms: 新北美圣草苷) 目录号 : GC40847
Neoeriocitrin是一种高效的乳酸脱氢酶A抑制剂,IC50值为11.198±0.90µM。
Cas No.:13241-32-2
Sample solution is provided at 25 µL, 10mM.
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]。
Cell experiment [1]: | |
Cell lines | MC3T3-E1 cells |
Preparation Method | The MC3T3-E1 cells were cultured inα-Modified minimal essential medium (α-MEM) supplemented with 10% fetal bovine serum (FBS), 100U/ml penicillin, and 100μg/ml streptomycin at 37°C with 5%CO2. The medium was changed twice a week. MC3T3-E1 cells were harvested by trypsin treatment and suspended in culture medium, and seeded into 96-well dishes at a density of 5×104cells /ml. After 24 hours, the medium was replaced with a new medium containing 5% FBS and osteogenic supplement (OS): consisting of 10μg/ml ascorbic acid and 10mmol/L β-glycerophosphoric acid. Differentiation was induced by Neoeriocitrin at different concentrations (0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20μg/ml). After 72h of incubation, cell proliferation was measured by MTT assay. The assay is based on the ability of living cells to convert soluble 3-(4, 5-dimethyl-thiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) into insoluble dark blue methylene dye reaction products. MTT was dissolved in PBS at a concentration of 5g/L and passed through a 0.22mm filter to remove bacteria. The MTT stock solution was added to the culture medium at a volume ratio of 1:10, incubated at 37°C for 4h, and then DMSO was added to mix to dissolve the dark blue crystals, which were left at room temperature for 10 min before reading with a microplate reader at a wavelength of 492nm. |
Reaction Conditions | 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20μg/ml; 72h |
Applications | Neoeriocitrin at the concentration of 2μg/ml showed an excellent effect in promoting proliferation and bone differentiation. |
References: |
Cas No. | 13241-32-2 | SDF | |
别名 | 新北美圣草苷 | ||
Canonical SMILES | O[C@H]1[C@H](O)[C@@H](CO)O[C@@H](OC2=CC(O)=C(C(C[C@@H](C3=CC=C(O)C(O)=C3)O4)=O)C4=C2)[C@@H]1O[C@@]5([H])[C@H](O)[C@H](O)[C@@H](O)[C@H](C)O5 | ||
分子式 | C27H32O15 | 分子量 | 596.5 |
溶解度 | DMF: 15 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg.ml,Ethanol: 1 mg/ml | 储存条件 | Store at -20°C,protect from light |
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1 mg | 5 mg | 10 mg |
1 mM | 1.6764 mL | 8.3822 mL | 16.7645 mL |
5 mM | 0.3353 mL | 1.6764 mL | 3.3529 mL |
10 mM | 0.1676 mL | 0.8382 mL | 1.6764 mL |
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2.
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