Abstract Natural compound tetrandrine was reported to inhibit the proliferation of T cells by inhibiting activation of NF-κB. Chemically, isotetrandrine differs from tetrandrine only in the stereochemistry at the chiral centers. The present study aimed to compare their anti-proliferation effects on human T cells with a focus on NF-κB. The IC50 values of tetrandrine against MOLT-4 cells, MOLT-4/DNR cells, and concanavalin A-activated peripheral blood mononuclear cells of healthy subjects and dialysis patients were 4.43 ± 0.22, 3.62 ± 0.22, 1.91 ± 0.22 and 3.03 ± 0.28 μM, respectively. Whereas, the IC50 values of isotetrandrine against the above immune cells were 2.19 ± 0.27, 2.28 ± 0.33, 1.29 ± 0.14 and 1.55 ± 0.26 μM, respectively. The inhibitory effect of isotetrandrine against the proliferation of T cells was stronger than that of tetrandrine significantly (p < 0.05). Molecular mechanism investigation showed that 10 μM of isotetrandrine largely decreased the expression of p-NF-κB and NF-κB in both MOLT-4 and MOLT-4/DNR T cells (p < 0.05), whereas 10 μM of tetrandrine slightly inhibited the phosphorylation of p-NF-κB with little influence on the expression of NF-κB. Taken together, absolute configurations of tetrandrine and isotetrandrine are suggested to influence on their anti-proliferation effects in human T cells via different regulation of NF-κB.

中文翻译：

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粉防己碱和异粉防己碱的绝对构型通过对 NF-κB 的不同调节影响其在人 T 细胞中的抗增殖作用

摘要 据报道，天然复合粉防己碱通过抑制 NF-κB 的活化来抑制 T 细胞的增殖。在化学上，异粉防己碱与粉防己碱的不同之处仅在于手性中心的立体化学。本研究旨在比较它们对人 T 细胞的抗增殖作用，重点是 NF-κB。粉防己碱对健康受试者和透析患者的MOLT-4细胞、MOLT-4/DNR细胞和刀豆球蛋白A激活的外周血单个核细胞的IC50值为4.43±0.22、3.62±0.22、1.91±0.22和3.03±0.28μM。 ， 分别。而异粉防己碱对上述免疫细胞的 IC50 值分别为 2.19 ± 0.27、2.28 ± 0.33、1.29 ± 0.14 和 1.55 ± 0.26 μM。异粉防己碱对T细胞增殖的抑制作用明显强于粉防己碱(p < 0.05)。分子机制研究表明，10 μM 异粉防己碱大大降低了 MOLT-4 和 MOLT-4/DNR T 细胞中 p-NF-κB 和 NF-κB 的表达（p < 0.05），而 10 μM 的粉防己碱略微抑制了p-NF-κB 的磷酸化对 NF-κB 的表达影响不大。总之，粉防己碱和异粉防己碱的绝对构型被认为通过对 NF-κB 的不同调节影响它们在人 T 细胞中的抗增殖作用。而 10 μM 的粉防己碱轻微抑制 p-NF-κB 的磷酸化，对 NF-κB 的表达几乎没有影响。总之，粉防己碱和异粉防己碱的绝对构型被认为通过对 NF-κB 的不同调节影响它们在人 T 细胞中的抗增殖作用。而 10 μM 的粉防己碱轻微抑制 p-NF-κB 的磷酸化，对 NF-κB 的表达几乎没有影响。总之，粉防己碱和异粉防己碱的绝对构型被认为通过对 NF-κB 的不同调节影响它们在人 T 细胞中的抗增殖作用。