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三齿拉雷亚木和特纳草提取物:体外对酪氨酸酶的抑制作用、抗糖化活性以及对参与神经炎症过程的酶和途径的影响。

Trichilia catigua and Turnera diffusa extracts: In vitro inhibition of tyrosinase, antiglycation activity and effects on enzymes and pathways engaged in the neuroinflammatory process.

机构信息

REQUIMTE/LAQV, Laboratório de Farmacognosia, Departamento de Química, Faculdade de Farmácia, Universidade Do Porto, Rua de Jorge Viterbo Ferreira, No. 228, 4050-313, Porto, Portugal.

REQUIMTE/LAQV, Group of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal; Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra (FFUC), Pólo Das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548, Coimbra, Portugal.

出版信息

J Ethnopharmacol. 2021 May 10;271:113865. doi: 10.1016/j.jep.2021.113865. Epub 2021 Jan 21.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Flavonoids interact with multiple targets in Central Nervous System resulting in a broad neuroprotection mediated by complementary processes and synergic interactions. Therefore, flavonoid-based therapies may input positive outcomes in the prevention and early management of neurodegenerative diseases. In Brazilian folk medicine Trichilia catigua is used for its neuroactive properties, such as neurostimulant, antioxidant and anti-neuroinflammatory, while Turnera diffusa is traditionally used as a tonic in neurasthenia. Both species are known to be rich in flavonoids.

AIM OF THE STUDY

To study aqueous extracts of T. catigua and T. diffusa in terms of their antioxidant and antiglycation effects, inhibition of tyrosinase activity, and interaction with enzymes and pathways engaged in neuroinflammation. Moreover, whenever possible, to establish a relationship between the studied activities and the traditional usage of the species.

MATERIALS AND METHODS

The phenolic profiles of the aqueous extracts were validated by HPLC-DAD. The effect of the extracts over mushroom tyrosinase and 5-lipoxygenase activities, as well as their capacity to impair bovine serum albumin glycation, were assessed by in vitro assays. The anti-neuroinflammatory potential of the same extracts was evaluated by their capacity to mitigate the pro-inflammatory stimulus induced in BV-2 microglia cells by interferon-gamma.

RESULTS

T. catigua extract, a rich mixture of phenolic acids, catechins and flavonolignans, excels by its ability to decrease lipid peroxidation (EC = 227.18 ± 9.04 μg/mL), and to work as anti-glycation agent, and inhibitor of both tyrosinase and 5-lipoxigenase (IC = 358.84 ± 19.05 and 56.25 ± 14.53 μg/mL, respectively). However, only T. diffusa extract, mainly composed by luteolin derivatives, is able to lower NO production by BV-2 microglia cells stimulated with interferon-gamma, despite its lower activities in the other assays.

CONCLUSIONS

Overall, this work highlights the value of medicinal plant extracts as sources of bioactive flavonoid-rich extracts with neuroactive effects. Furthermore, these results support their application as alternative strategies to develop functional foods and therapeutics to fight chronic neurodegenerative disorders.

摘要

民族药理学相关性

类黄酮与中枢神经系统中的多个靶标相互作用,通过互补过程和协同作用介导广泛的神经保护。因此,基于类黄酮的治疗方法可能会在预防和早期治疗神经退行性疾病方面带来积极的结果。在巴西民间医学中,Trichilia catigua 因其具有神经活性特性而被使用,例如神经刺激剂、抗氧化剂和抗神经炎症,而 Turnera diffusa 传统上被用作神经疲劳的补品。这两个物种都富含类黄酮。

研究目的

研究 T. catigua 和 T. diffusa 的水提物在抗氧化和抗糖化作用、抑制酪氨酸酶活性以及与参与神经炎症的酶和途径相互作用方面的作用。此外,只要有可能,将研究活动与物种的传统用途建立联系。

材料和方法

通过 HPLC-DAD 验证水提物的酚类图谱。通过体外测定评估提取物对蘑菇酪氨酸酶和 5-脂氧合酶活性的影响,以及它们破坏牛血清白蛋白糖化的能力。通过评估相同提取物减轻干扰素-γ诱导的 BV-2 小胶质细胞中促炎刺激的能力来评估其抗神经炎症潜力。

结果

T. catigua 提取物是一种富含酚酸、儿茶素和黄酮木脂素的混合物,具有降低脂质过氧化(EC=227.18±9.04μg/mL)的能力,并且是一种抗糖化剂和酪氨酸酶和 5-脂氧合酶的抑制剂(IC=358.84±19.05 和 56.25±14.53μg/mL)。然而,只有 T. diffusa 提取物(主要由木犀草素衍生物组成)能够降低干扰素-γ刺激的 BV-2 小胶质细胞中 NO 的产生,尽管它在其他测定中的活性较低。

结论

总的来说,这项工作强调了药用植物提取物作为具有神经活性作用的富含类黄酮的生物活性提取物的来源的价值。此外,这些结果支持将它们作为开发功能性食品和治疗慢性神经退行性疾病的替代策略的应用。

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