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生物活性类黄酮:生物发生和化学合成方法的比较概述。

Bioactive Flavonoids: A Comparative Overview of the Biogenetic and Chemical Synthesis Approach.

机构信息

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144411, India.

Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER) Guwahati, Changsari, Kamrup, Assam, 781101, India.

出版信息

Mini Rev Med Chem. 2023;23(18):1818-1837. doi: 10.2174/1389557523666230214101821.

Abstract

Flavonoids are natural polyphenolic compounds and constitute a major class of plant secondary metabolites. To date, structures of more than 10,000 different flavonoids have been elucidated, and most of them are present in cells and tissues of plant parts. Flavonoids have been reported to exert multiple physiological activities and are also consumed as dietary supplements. Flavonoids have been extensively explored as anticancer, anti-inflammatory, antidiabetic, antirheumatic, antioxidant, antimalarial, neuroprotective, cardioprotective, anti-angiogenic, and antiproliferative agents. Most of the flavonoids are biosynthesized in plants via the phenylpropanoid pathway. However, they are associated with some limitations. Chemical synthesis is an alternative strategy to improve the yield and obtain purified products but is hampered by drawbacks, such as intolerance to stressful lab conditions. Pharmacokinetics is the rate-limiting step defining the bioavailability and metabolism of flavonoids, though greatly influenced by their chemical structure. However, nanoformulation is an emerging technique to improve biopharmaceutical fate and achieve target drug delivery. Thus, much attention should be given to identifying other possible chemical approaches for synthesizing flavonoids and improving their pharmacokinetic profiling, hence potentiating their efficacy in clinic.

摘要

类黄酮是天然多酚化合物,构成植物次生代谢物的主要类别。迄今为止,已经阐明了超过 10000 种不同类黄酮的结构,其中大多数存在于植物部分的细胞和组织中。类黄酮被报道具有多种生理活性,也被用作膳食补充剂。类黄酮已被广泛探索作为抗癌、抗炎、抗糖尿病、抗风湿、抗氧化、抗疟、神经保护、心脏保护、抗血管生成和抗增殖剂。大多数类黄酮通过苯丙烷途径在植物中生物合成。然而,它们与一些局限性有关。化学合成是一种提高产量和获得纯化产品的替代策略,但由于对恶劣实验室条件的不耐受等缺点而受到阻碍。药代动力学是定义类黄酮生物利用度和代谢的限速步骤,尽管其化学结构有很大影响。然而,纳米制剂是一种新兴技术,可以改善生物制药的命运并实现靶向药物输送。因此,应该关注确定其他可能的化学方法来合成类黄酮并改善其药代动力学特征,从而提高其在临床上的疗效。

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