Multi-Targeting Andrographolide, a Novel NF-κB Inhibitor, as a Potential Therapeutic Agent for Stroke.
Multi-Targeting Andrographolide, a Novel NF-κB Inhibitor, as a Potential Therapeutic Agent for Stroke.
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新型NF-κB抑制剂穿心莲内酯的多靶向治疗作用
DOI：
10.3390/ijms18081638
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发表时间：
2017-07-27
影响因子：
5.6
通讯作者：
Jayakumar T
中科院分区：
文献类型：
--
作者：
Yang CH;Yen TL;Hsu CY;Thomas PA;Sheu JR;Jayakumar T
药物发现领域的一个关键焦点是天然化合物的神经保护作用。脑缺血是一个具有一系列机制的多方面病理过程，从传统草药或天然产物中开发神经保护剂是治疗该疾病的一种有前景的方法。具有抗氧化、抗炎、抗凋亡、神经功能调节作用的天然化合物对实验性缺血性脑损伤具有治疗作用。考虑到神经保护的药理学机制，一项研究发现，穿心莲内酯（一种二萜内酯化合物）在体外和体内中风实验模型中表现出不同程度的神经保护活性。穿心莲内酯的神经保护机制为：(I) 通过 p38-丝裂原激活蛋白激酶 (MAPK) 调节增加核因子 E2 相关因子 2-血红素加氧酶 (Nrf2-HO-1) 表达，(II) 诱导脑内皮细胞 (CEC) 凋亡和 caspase-3 激活，(III) 下调 Bax，诱导 一氧化氮合酶 (iNOS) 和 (IV) 抑制羟自由基 (OH−) 形成，并激活转录因子 NF-κB 信号通路。最近，一些研究人员也一直试图揭示穿心莲内酯神经保护作用的主要机制。因此，本综述旨在总结穿心莲内酯的神经保护作用的概述，并举例说明所涉及的基本机制。本文可以提供这样的信息：穿心莲内酯药物的发现可能是开发一类新型神经保护药物的有前途的策略。
A key focus in the field of drug discovery has been motivated by the neuroprotection of natural compounds. Cerebral ischemia is a multifaceted pathological process with a series of mechanisms, and a perspective for the development of neuroprotectants from traditional herbal medicine or natural products is a promising treatment for this disease. Natural compounds with the effects of anti-oxidation, anti-inflammation, anti-apoptosis, and neurofunctional regulation exhibit therapeutic effects on experimental ischemic brain injury. Conferring to the pharmacological mechanisms underlying neuroprotection, a study found that androgapholide, a diterpene lactone compound, exhibits varying degrees of neuroprotective activities in both in vitro and in vivo experimental models of stroke. The neuroprotective mechanisms of andrographolide are suggested as: (I) increasing nuclear factor E2-related factor 2-heme oxygenase (Nrf2-HO-1) expression through p38-mitogen activated protein kinase (MAPK) regulation, (II) inducing cerebral endothelial cells (CEC) apoptosis and caspase-3 activation, (III) down regulating Bax, inducible nitric oxide synthase (iNOS), and (IV) inhibiting hydroxyl radical (OH−) formation, and activating transcription factor NF-κB signaling pathways. Recently, several researchers have also been trying to unveil the principal mechanisms involved in the neuroprotective effects of andrographolide. Therefore, this review aims to summarize an overview on the neuroprotective effects of andrographolide and exemplifies the essential mechanisms involved. This paper can provide information that andrographolide drug discovery may be a promising strategy for the development of a novel class of neuroprotective drug.
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影响因子：
2.7
作者：
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通讯作者：
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影响因子：
5.3
作者：
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影响因子：
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作者：
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通讯作者：
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影响因子：
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作者：
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