L-Albizziine is an inhibitor of 4-methyleneglutaminase, with an IC50 value of 20mM [1]. L-Albizziine, an inhibitor of glutamate synthase, strongly inhibited the conversion of 2-ketoglutarate in maize leaves[2]. L-Albizziine inhibits asparagine synthetase activity and has been widely used to regulate T-cell activation in different cell models[3].
In vitro, L-Albizziine treatment at 2mM for 72 hours significantly reduced aspartate levels and increased p53 protein expression in HuCCT1 cells[4]. Treatment with 4mM L-Albizziine for 48 hours inhibited p53+/+ and p53−/− HCT116 cell proliferation and reduced cell number[5]. Treatment with 10mM L-Albizziine for 24h impaired vaccinia virus replication in primary human foreskin fibroblasts without affecting cell viability[6].
References:
[1] Ibrahim S A, Lea P J, Fowden L. Purification and properties of 4-methyleneglutaminase from the leaves of peanut (Arachis hypogaea)[J]. Phytochemistry, 1984, 23(8): 1545-1549.
[2] Harel E, Ne'Eman E. Alternative Routes for the Synthesis of 5-Aminolevulinic Acid in Maize Leaves: II. Formation from Glutamate[J]. Plant Physiology, 1983, 72(4): 1062-1067.
[3] Wu J, Li G, Li L, et al. Asparagine enhances LCK signalling to potentiate CD8+ T-cell activation and anti-tumour responses[J]. Nature cell biology, 2021, 23(1): 75-86.
[4] Chu Z, Zhang B, Zhou X, et al. A DNA/RNA heteroduplex oligonucleotide coupling asparagine depletion restricts FGFR2 fusion-driven intrahepatic cholangiocarcinoma[J]. Molecular Therapy Nucleic Acids, 2023, 34.
[5] Deng L, Yao P, Li L, et al. p53-mediated control of aspartate-asparagine homeostasis dictates LKB1 activity and modulates cell survival[J]. Nature communications, 2020, 11(1): 1755.
[6] Pant A, Cao S, Yang Z. Asparagine is a critical limiting metabolite for vaccinia virus protein synthesis during glutamine deprivation[J]. Journal of Virology, 2019, 93(13): 10.1128/jvi. 01834-18.
L-Albizziine是一种4-亚甲基谷氨酰胺酶抑制剂，IC50值为20mM[1]。作为谷氨酸合酶抑制剂，该化合物可强烈抑制玉米叶片中2-酮戊二酸的转化[2]。L-Albizziine通过抑制天冬酰胺合成酶活性，广泛应用于不同细胞模型中调控T细胞活化[3]。
在体外，2mM的L-Albizziine处理HuCCT1细胞72小时可显著降低天冬氨酸水平并增加p53蛋白表达[4]。4mM的L-Albizziine处理p53+/+和p53−/− HCT116细胞48小时能抑制细胞增殖并减少细胞数量[5]。10mM的L-Albizziine处理原代人包皮成纤维细胞24小时可抑制痘苗病毒复制且不影响细胞活力[6]。