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提高(R)-α-硫辛酸的生物利用度以增强抗氧化活性用于治疗神经性疼痛。

Increasing bioavailability of (R)-alpha-lipoic acid to boost antioxidant activity in the treatment of neuropathic pain.

作者信息

Maglione Emilia, Marrese Cinzia, Migliaro Elisa, Marcuccio Fortuna, Panico Claudia, Salvati Carmine, Citro Giuseppe, Quercio Marco, Roncagliolo Federico, Torello Carlo, Brufani Mario

机构信息

Centro Polidiagnostico "Benedetto Croce" - Giugliano (NA).

出版信息

Acta Biomed. 2015 Dec 14;86(3):226-33.

Abstract

a-lipoic acid (a-LA) is a potent natural antioxidant because it has a broad spectrum of action towards a great many free radical species and boosts the endogenous antioxidant systems.Although it is a multi-functional molecule, its pharmacokinetic characteristics pose restrictions to its use in the treatment of oxidative stress-dependent illnesses. Formulations that increase the bioavailability of a-LA have a better potential efficacy as adjuvants for the treatment of these conditions.This objective was achieved with a liquid formulation for oral use containing only R-aLA, the natural enantiomeric and most active form of a-lipoic acid.For the first time, the effects of this formulation were evaluated on neuropathic pain, a symptom caused by an increase in oxidative stress, regardless of the underlying cause. Neuropathic patients who have used this dietary supplement noticed an improvement in their quality of life and a significant reduction was observed in a number of certain descriptive pain parameters (intensity, burning, unpleasantness, superficial pain).Undoubtedly further, more in-depth, studies need to be conducted; however, this first investigation confirms the role of R-aLA as an anti-oxidant for the aetiological treatment of peripheral neuropathy. Increasing its plasma bioavailability even after a non-invasive administration through the oral route is a good starting point for proposing a valid adjuvant for the treatment of pain symptoms.

摘要

α-硫辛酸(α-LA)是一种强效的天然抗氧化剂,因为它对多种自由基具有广泛的作用,并能增强内源性抗氧化系统。尽管它是一种多功能分子,但其药代动力学特性限制了它在治疗氧化应激相关疾病中的应用。提高α-LA生物利用度的制剂作为这些疾病治疗的佐剂具有更好的潜在疗效。这一目标通过一种仅含有R-αLA(α-硫辛酸的天然对映体且是最具活性的形式)的口服液体制剂得以实现。首次评估了该制剂对神经性疼痛的影响,神经性疼痛是一种由氧化应激增加引起的症状,无论其潜在病因如何。使用这种膳食补充剂的神经病变患者注意到他们的生活质量有所改善,并且在一些特定的描述性疼痛参数(强度、灼痛、不适感、浅表疼痛)方面观察到显著降低。毫无疑问,需要进行进一步更深入的研究;然而,这首次调查证实了R-αLA作为外周神经病变病因治疗抗氧化剂的作用。即使通过口服途径进行非侵入性给药后提高其血浆生物利用度,也是提出一种有效治疗疼痛症状佐剂的良好起点。

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