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1
Beta-endorphin is a potent inhibitor of thymidine incorporation into DNA via mu- and kappa-opioid receptors in fetal rat brain cell aggregates in culture.β-内啡肽是一种强效抑制剂，可通过μ-和κ-阿片受体抑制胸腺嘧啶核苷掺入培养的胎鼠脑细胞聚集体中的DNA。
J Neurochem. 1993 Feb;60(2):765-7. doi: 10.1111/j.1471-4159.1993.tb03214.x.
2
The tail-flick inhibition induced by beta-endorphin administered intrathecally is mediated by activation of kappa- and mu-opioid receptors in the mouse.鞘内注射β-内啡肽诱导的甩尾抑制是由小鼠体内κ-和μ-阿片受体的激活介导的。
Eur J Pharmacol. 1992 Apr 7;214(1):59-65. doi: 10.1016/0014-2999(92)90096-m.
3
Spinal delta 2-, but not delta 1-, mu-, or kappa-opioid receptors are involved in the tail-flick inhibition induced by beta-endorphin from nucleus raphe obscurus in the pentobarbital-anesthetized rat.在戊巴比妥麻醉的大鼠中，脊髓δ2阿片受体而非δ1、μ或κ阿片受体参与中缝隐核β-内啡肽诱导的甩尾抑制。
Eur J Pharmacol. 1995 Apr 24;277(2-3):251-6. doi: 10.1016/0014-2999(95)00084-x.
4
Comparison of [125I]beta-endorphin binding to rat brain and NG108-15 cells using a monoclonal antibody directed against the opioid receptor.使用针对阿片受体的单克隆抗体比较[125I]β-内啡肽与大鼠脑和NG108-15细胞的结合。
Mol Pharmacol. 1988 Feb;33(2):170-7.
5
Beta-endorphin: a highly selective endogenous opioid agonist for presynaptic mu opioid receptors.β-内啡肽：一种对突触前μ阿片受体具有高度选择性的内源性阿片激动剂。
J Pharmacol Exp Ther. 1991 Jul 1;258(1):237-42.
6
Opioid receptor selectivity of beta-endorphin in vitro and in vivo: mu, delta and epsilon receptors.β-内啡肽在体外和体内对阿片受体的选择性：μ、δ和ε受体
J Pharmacol Exp Ther. 1988 Sep;246(3):1018-25.
7
Different types of opioid receptors mediating analgesia induced by morphine, DAMGO, DPDPE, DADLE and beta-endorphin in mice.不同类型的阿片受体介导吗啡、DAMGO、DPDPE、DADLE和β-内啡肽在小鼠中诱导的镇痛作用。
Naunyn Schmiedebergs Arch Pharmacol. 1990 Jul;342(1):67-71. doi: 10.1007/BF00178974.
8
Evidence for the implication of phosphoinositol signal transduction in mu-opioid inhibition of DNA synthesis.磷酸肌醇信号转导参与μ-阿片受体对DNA合成抑制作用的证据。
J Neurochem. 1992 Sep;59(3):1145-52. doi: 10.1111/j.1471-4159.1992.tb08357.x.
9
Dynorphins modulate DNA synthesis in fetal brain cell aggregates.强啡肽调节胎儿脑细胞聚集体中的DNA合成。
J Neurochem. 1995 Oct;65(4):1481-6. doi: 10.1046/j.1471-4159.1995.65041481.x.
10
Opioid receptor selectivity of peptide models of beta-endorphin.β-内啡肽肽模型的阿片受体选择性
Int J Pept Protein Res. 1989 Jul;34(1):75-80.

引用本文的文献

1
Opioid receptor signaling throughout ontogeny: Shaping neural and behavioral trajectories.阿片受体信号在整个个体发育过程中的作用：塑造神经和行为轨迹。
Neurosci Biobehav Rev. 2025 Mar;170:106033. doi: 10.1016/j.neubiorev.2025.106033. Epub 2025 Jan 31.
2
Selective vulnerability of cerebellar granule neuroblasts and their progeny to drugs with abuse liability.小脑颗粒神经母细胞及其后代对具有成瘾性药物的选择性易损性。
Cerebellum. 2003;2(3):184-95. doi: 10.1080/14734220310016132.
3
Opioid system diversity in developing neurons, astroglia, and oligodendroglia in the subventricular zone and striatum: impact on gliogenesis in vivo.脑室下区和纹状体中发育中的神经元、星形胶质细胞和少突胶质细胞的阿片类系统多样性：对体内神经胶质生成的影响。
Glia. 2001 Oct;36(1):78-88.
4
Regulation of mouse kappa opioid receptor gene expression by retinoids.视黄酸对小鼠κ阿片受体基因表达的调控
J Neurosci. 2001 Mar 1;21(5):1590-9. doi: 10.1523/JNEUROSCI.21-05-01590.2001.
5
Opioids intrinsically inhibit the genesis of mouse cerebellar granule neuron precursors in vitro: differential impact of mu and delta receptor activation on proliferation and neurite elongation.阿片类药物在体外可内在性抑制小鼠小脑颗粒神经元前体的发生：μ受体和δ受体激活对增殖和神经突伸长的不同影响。
Eur J Neurosci. 2000 Apr;12(4):1281-93. doi: 10.1046/j.1460-9568.2000.01015.x.
6
Mu-opioid agonist inhibition of kappa-opioid receptor-stimulated extracellular signal-regulated kinase phosphorylation is dynamin-dependent in C6 glioma cells.μ-阿片受体激动剂对κ-阿片受体刺激的细胞外信号调节激酶磷酸化的抑制作用在C6胶质瘤细胞中是依赖发动蛋白的。
J Neurochem. 2000 Feb;74(2):574-81. doi: 10.1046/j.1471-4159.2000.740574.x.
7
Evidence for kappa- and mu-opioid receptor expression in C6 glioma cells.C6胶质瘤细胞中κ-阿片受体和μ-阿片受体表达的证据。
J Neurochem. 1998 May;70(5):1819-25. doi: 10.1046/j.1471-4159.1998.70051819.x.
8
Developmental expression of the mu, kappa, and delta opioid receptor mRNAs in mouse.小鼠中μ、κ和δ阿片受体mRNA的发育表达。
J Neurosci. 1998 Apr 1;18(7):2538-49. doi: 10.1523/JNEUROSCI.18-07-02538.1998.
9
Dynorphins modulate DNA synthesis in fetal brain cell aggregates.强啡肽调节胎儿脑细胞聚集体中的DNA合成。
J Neurochem. 1995 Oct;65(4):1481-6. doi: 10.1046/j.1471-4159.1995.65041481.x.

本文引用的文献

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kappa-Opioid agonist modulation of [3H]thymidine incorporation into DNA: evidence for the involvement of pertussis toxin-sensitive G protein-coupled phosphoinositide turnover.κ-阿片受体激动剂对[³H]胸腺嘧啶核苷掺入DNA的调节作用：百日咳毒素敏感的G蛋白偶联磷酸肌醇代谢参与的证据
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Effect of naloxone and D-met2-pro5-enkephalinamide treatment on the DNA synthesis in the developing rat brain.纳洛酮和D-蛋氨酸2-脯氨酸5-脑啡肽酰胺治疗对发育中大鼠脑内DNA合成的影响。
Life Sci. 1982 Jul 12;31(2):119-26. doi: 10.1016/0024-3205(82)90423-4.
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Ontogenesis of opiate binding sites and radioimmunoassayable beta-endorphin and enkephalin in regions of rat brain.大鼠脑区阿片类结合位点、放射免疫法可检测的β-内啡肽和脑啡肽的个体发生
Brain Res. 1982 Nov;281(3):257-61. doi: 10.1016/0165-3806(82)90124-9.
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Opiate binding properties of naturally occurring N- and C-terminus modified beta-endorphins.天然存在的 N 端和 C 端修饰的β-内啡肽的阿片样物质结合特性。
Peptides. 1981 Fall;2(3):289-92. doi: 10.1016/s0196-9781(81)80121-0.
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Effects of morphine on DNA synthesis in neonatal rat brain.吗啡对新生大鼠大脑中DNA合成的影响。
Brain Res. 1987 Jan;428(1):45-52. doi: 10.1016/0165-3806(87)90081-2.
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Endogenous opioid systems regulate cell proliferation in the developing rat brain.内源性阿片系统调节发育中大鼠大脑中的细胞增殖。
Brain Res. 1987 May 26;412(1):68-72. doi: 10.1016/0006-8993(87)91440-5.
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Covalent labeling of opioid receptors with radioiodinated human beta-endorphin. Identification of binding site subunit.用放射性碘标记的人β-内啡肽对阿片受体进行共价标记。结合位点亚基的鉴定。
J Biol Chem. 1985 Sep 5;260(19):10833-9.
8
Control of peripheral glial cell proliferation: enteric neurons exert an inhibitory influence on Schwann cell and enteric glial cell DNA synthesis in culture.外周神经胶质细胞增殖的调控：肠神经元对培养中的施万细胞和肠神经胶质细胞的DNA合成具有抑制作用。
Development. 1989 Sep;107(1):107-12. doi: 10.1242/dev.107.1.107.
9
Expression of the three opioid receptor subtypes mu, delta and kappa in guinea pig and rat brain cell cultures and in vivo.豚鼠和大鼠脑细胞培养物及体内μ、δ和κ三种阿片受体亚型的表达。
Int J Dev Neurosci. 1989;7(2):173-9. doi: 10.1016/0736-5748(89)90067-1.
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Opioid-dependent growth of glial cultures: suppression of astrocyte DNA synthesis by met-enkephalin.
Life Sci. 1990;46(2):91-8. doi: 10.1016/0024-3205(90)90041-o.

β-内啡肽是一种强效抑制剂，可通过μ-和κ-阿片受体抑制胸腺嘧啶核苷掺入培养的胎鼠脑细胞聚集体中的DNA。

Beta-endorphin is a potent inhibitor of thymidine incorporation into DNA via mu- and kappa-opioid receptors in fetal rat brain cell aggregates in culture.

作者信息

Barg J, Belcheva M, McHale R, Levy R, Vogel Z, Coscia C J

机构信息

E. A. Doisy Department of Biochemistry and Molecular Biology, St. Louis University School of Medicine, MO 63104-1079.

出版信息

J Neurochem. 1993 Feb;60(2):765-7. doi: 10.1111/j.1471-4159.1993.tb03214.x.

DOI:10.1111/j.1471-4159.1993.tb03214.x
PMID:8380443
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2571952/
Abstract

Thymidine incorporation into DNA was inhibited dose-dependently by beta-endorphin in rat fetal brain cell aggregate cultures. The inhibition was reversed partially by mu (cyclic D-Phe-Cys-Tyr-D-Trp-Orn-Thr- Pen-Thr amide) or kappa (norbinaltorphimine) antagonists. Complete blockade of the beta-endorphin inhibitory effect was achieved only on concomitant exposure to both antagonists. Eadie-Hofstee analysis revealed that beta-endorphin inhibited thymidine incorporation noncompetitively. In the presence of protease inhibitors, beta-endorphin decreased thymidine incorporation with an IC50 of 0.7 nM. Truncated and N-acetylated beta-endorphin derivatives, which bind with low affinity to opioid receptors, did not affect thymidine incorporation. These findings indicate that beta-endorphin at physiological concentrations can regulate thymidine incorporation in cultured brain cells.

摘要

在大鼠胎儿脑细胞聚集体培养物中，β-内啡肽可剂量依赖性地抑制胸苷掺入DNA。μ（环D-苯丙氨酸-半胱氨酸-酪氨酸-D-色氨酸-鸟氨酸-苏氨酸-苯丙氨酸-苏氨酸酰胺）或κ（诺宾那托啡）拮抗剂可部分逆转这种抑制作用。仅在同时暴露于两种拮抗剂时，才能完全阻断β-内啡肽的抑制作用。伊迪-霍夫斯泰分析表明，β-内啡肽以非竞争性方式抑制胸苷掺入。在蛋白酶抑制剂存在的情况下，β-内啡肽使胸苷掺入减少，IC50为0.7 nM。与阿片受体亲和力低的截短和N-乙酰化β-内啡肽衍生物不影响胸苷掺入。这些发现表明，生理浓度的β-内啡肽可调节培养脑细胞中的胸苷掺入。