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关于阿朴色原酮的植物化学和医学进展的全面更新。

A comprehensive update on phytochemistry and medicinal developments of apocynin.

作者信息

Bhatia Anchal, Thakur Shimple, Kohal Rupali, Brar Seema, Gupta Ghanshyam Das, Verma Sant Kumar

机构信息

Department of Pharmacognosy, ISF College of Pharmacy, Moga 142 001, Punjab, India.

Department of Pharmaceutics, ISF College of Pharmacy, Moga 142 001, Punjab, India.

出版信息

Fitoterapia. 2025 Jun;183:106558. doi: 10.1016/j.fitote.2025.106558. Epub 2025 Apr 23.

Abstract

The natural phenolic compound apocynin, referred to as acetovanillone, generated significant attention due to its diverse pharmacological properties, especially as an NADPH oxidase inhibitor, and it was applicable orally and effectively even at small doses. During chronic inflammation, various pro-inflammatory-related factors such as nuclear factor kappa β (NF-kβ), nitrotyrosine, poly adenosine diphosphate ribose polymerase (PARP), inducible nitric oxide synthase (iNOS), cluster of differentiation 31 (CD), intercellular adhesion molecule-1 (ICAM-1), glycoproteins granule membrane protein 140 (GMP140), tumor necrosis factor-alpha (TNFα), p38 mitogen-activated protein kinases (p38 MAPK), membrane cofactor protein (MCP), interleukin-6 (IL-6), all of which could be targeted by apocynin. Research suggests that apocynin significantly benefits conditions like diabetes, cardiovascular diseases, and neurological disorders due to its ability to mitigate inflammation and enhance endothelial function. Further investigations are essential to examine apocynin and its derivatives, mainly its long-term potency. Future research must focus on clinical trials to evaluate its safety, effectiveness, and optimal dosing in various applications. This review provides a recent update on apocynin, covering aspects such as its extraction and isolation, chemical framework, biosynthesis, synthetic derivatives, pharmacological activities, patent landscape, stability and specifications.

摘要

天然酚类化合物夹竹桃麻素,又称乙酰香草酮,因其多样的药理特性,尤其是作为一种NADPH氧化酶抑制剂,而备受关注,并且它可以口服,即使小剂量也有效。在慢性炎症期间,各种促炎相关因子,如核因子κB(NF-kβ)、硝基酪氨酸、聚腺苷二磷酸核糖聚合酶(PARP)、诱导型一氧化氮合酶(iNOS)、分化簇31(CD)、细胞间黏附分子-1(ICAM-1)、糖蛋白颗粒膜蛋白140(GMP140)、肿瘤坏死因子-α(TNFα)、p38丝裂原活化蛋白激酶(p38 MAPK)、膜辅因子蛋白(MCP)、白细胞介素-6(IL-6),所有这些都可能是夹竹桃麻素的作用靶点。研究表明,夹竹桃麻素因其减轻炎症和增强内皮功能的能力,对糖尿病、心血管疾病和神经疾病等病症有显著益处。进一步的研究对于研究夹竹桃麻素及其衍生物至关重要,主要是其长期效力。未来的研究必须集中在临床试验上,以评估其在各种应用中的安全性、有效性和最佳剂量。这篇综述提供了夹竹桃麻素的最新进展,涵盖了其提取与分离、化学结构、生物合成、合成衍生物、药理活性、专利情况、稳定性和规格等方面。

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