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替勃龙作为激素治疗和神经保护剂。

Tibolone as Hormonal Therapy and Neuroprotective Agent.

机构信息

Reproductive Health Research Institute, Santiago, Chile; Translational Psychiatry Laboratory, Clínica Psiquiátrica Universitaria, Hospital Clínico, Universidad de Chile, Santiago, Chile; Millennium Nucleus to Improve the Mental Health of Adolescents and Youths (Imhay), Santiago, Chile.

Tallahassee Community College, Tallahassee, FL, USA.

出版信息

Trends Endocrinol Metab. 2020 Oct;31(10):742-759. doi: 10.1016/j.tem.2020.04.007. Epub 2020 Jun 5.

DOI:10.1016/j.tem.2020.04.007
PMID:32507541
Abstract

Tibolone (TIB), a selective tissue estrogenic activity regulator (STEAR) in clinical use by postmenopausal women, activates hormonal receptors in a tissue-specific manner. Estrogenic activity is present mostly in the brain, vagina, and bone, while the inactive forms predominate in the endometrium and breast. Conflicting literature on TIB's actions has been observed. While it has benefits for vasomotor symptoms, bone demineralization, and sexual health, a higher relative risk of hormone-sensitive cancer has been reported. In the brain, TIB can improve mood and cognition, neuroinflammation, and reactive gliosis. This review aims to discuss the systemic effects of TIB on peri- and post-menopausal women and its role in the brain. We suggest that TIB is a hormonal therapy with promising neuroprotective properties.

摘要

替勃龙(TIB)是一种临床用于绝经后妇女的选择性组织雌激素活性调节剂(STEAR),以组织特异性方式激活激素受体。雌激素活性主要存在于大脑、阴道和骨骼中,而无活性形式则主要存在于子宫内膜和乳房中。关于 TIB 的作用存在相互矛盾的文献。虽然它对血管舒缩症状、骨矿物质流失和性健康有好处,但报告称激素敏感型癌症的相对风险更高。在大脑中,TIB 可以改善情绪和认知、神经炎症和反应性神经胶质增生。本综述旨在讨论 TIB 对绝经前和绝经后妇女的全身作用及其在大脑中的作用。我们认为 TIB 是一种具有有前景的神经保护特性的激素治疗药物。

相似文献

1
Tibolone as Hormonal Therapy and Neuroprotective Agent.替勃龙作为激素治疗和神经保护剂。
Trends Endocrinol Metab. 2020 Oct;31(10):742-759. doi: 10.1016/j.tem.2020.04.007. Epub 2020 Jun 5.
2
Cardiovascular effects of tibolone: a selective tissue estrogenic activity regulator.替勃龙的心血管效应:一种选择性组织雌激素活性调节剂。
Cardiovasc Drug Rev. 2007 Summer;25(2):132-45. doi: 10.1111/j.1527-3466.2007.00007.x.
3
Tibolone: the way to beat many a postmenopausal ailments.替勃龙:战胜多种绝经后疾病的方法。
Expert Opin Pharmacother. 2008 Apr;9(6):1039-47. doi: 10.1517/14656566.9.6.1039.
4
Tibolone protects T98G cells from glucose deprivation.替勃龙可保护T98G细胞免受葡萄糖剥夺(的影响)。
J Steroid Biochem Mol Biol. 2014 Oct;144 Pt B:294-303. doi: 10.1016/j.jsbmb.2014.07.009. Epub 2014 Jul 31.
5
The effects of tibolone on mood and libido.替勃龙对情绪和性欲的影响。
Menopause. 2002 May-Jun;9(3):162-70. doi: 10.1097/00042192-200205000-00004.
6
Tibolone: a unique version of hormone replacement therapy.替勃龙:激素替代疗法的一种独特形式。
Ann Pharmacother. 2004 May;38(5):874-81. doi: 10.1345/aph.1D462. Epub 2004 Mar 16.
7
Tibolone: clinical recommendations and practical guidelines. A report of the International Tibolone Consensus Group.替勃龙:临床建议与实用指南。国际替勃龙共识小组报告。
Maturitas. 2005 May 16;51(1):21-8. doi: 10.1016/j.maturitas.2005.02.011.
8
Effects of tibolone on the breast of postmenopausal women.替勃龙对绝经后女性乳房的影响。
Taiwan J Obstet Gynecol. 2007 Jun;46(2):121-6. doi: 10.1016/S1028-4559(07)60005-9.
9
Tibolone regulates systemic metabolism and the expression of sex hormone receptors in the central nervous system of ovariectomised rats fed with high-fat and high-fructose diet.替勃龙可调节高脂高糖饮食喂养的去卵巢大鼠的全身代谢及中枢神经系统中性激素受体的表达。
Brain Res. 2020 Dec 1;1748:147096. doi: 10.1016/j.brainres.2020.147096. Epub 2020 Sep 6.
10
[Clinical aspects of Livial in postmenopausal replacement therapy].[利维爱用于绝经后替代疗法的临床应用]
Ginekol Pol. 2002 Mar;73(3):213-20.

引用本文的文献

1
Tibolone Improves Motor Recovery and Regulates Neuroinflammation and Gliosis in a Model of Traumatic Spinal Cord Injury.替勃龙可改善创伤性脊髓损伤模型中的运动恢复,并调节神经炎症和胶质细胞增生。
Int J Mol Sci. 2025 Aug 27;26(17):8327. doi: 10.3390/ijms26178327.
2
Analysis of Menopausal Hormone Therapy to Chinese Patients with Menopausal Syndrome: A Real-World Retrospective Study from Chinese Hospitals.中国绝经综合征患者的绝经激素治疗分析:一项来自中国医院的真实世界回顾性研究
Drug Des Devel Ther. 2025 Jun 4;19:4861-4873. doi: 10.2147/DDDT.S517420. eCollection 2025.
3
Using estrogen and progesterone to treat premenstrual dysphoric disorder, postnatal depression and menopausal depression.
使用雌激素和孕激素治疗经前烦躁障碍、产后抑郁症和更年期抑郁症。
Front Pharmacol. 2025 Feb 20;16:1528544. doi: 10.3389/fphar.2025.1528544. eCollection 2025.
4
Targeting Mitochondrial Dysfunction in Cerebral Ischemia: Advances in Pharmacological Interventions.针对脑缺血中线粒体功能障碍:药理学干预进展
Antioxidants (Basel). 2025 Jan 18;14(1):108. doi: 10.3390/antiox14010108.
5
Effects of tibolone combined with zoledronic acid on bone density, bone metabolism, and pain in postmenopausal patients with osteoporosis.替勃龙联合唑来膦酸对绝经后骨质疏松症患者骨密度、骨代谢及疼痛的影响
Am J Transl Res. 2024 Jul 15;16(7):3395-3404. doi: 10.62347/YDKM2312. eCollection 2024.
6
Sex differences in Huntington's disease from a neuroinflammation perspective.从神经炎症角度看亨廷顿病中的性别差异。
Front Neurol. 2024 Jun 10;15:1384480. doi: 10.3389/fneur.2024.1384480. eCollection 2024.
7
Tibolone and Breast Cancer.替勃龙与乳腺癌
J Menopausal Med. 2023 Dec;29(3):92-96. doi: 10.6118/jmm.23032.
8
Tibolone Improves Locomotor Function in a Rat Model of Spinal Cord Injury by Modulating Apoptosis and Autophagy.替勃龙通过调节细胞凋亡和自噬改善脊髓损伤大鼠的运动功能。
Int J Mol Sci. 2023 Oct 18;24(20):15285. doi: 10.3390/ijms242015285.
9
Menopausal hormone therapy and risk of dementia: health insurance database in South Korea-based retrospective cohort study.更年期激素治疗与痴呆症风险:基于韩国健康保险数据库的回顾性队列研究
Front Aging Neurosci. 2023 Sep 7;15:1213481. doi: 10.3389/fnagi.2023.1213481. eCollection 2023.
10
Repurposing of Tibolone in Alzheimer's Disease.他莫昔芬在阿尔茨海默病中的再利用。
Biomolecules. 2023 Jul 13;13(7):1115. doi: 10.3390/biom13071115.