Sahadevan Revathy, Singh Satyam, Binoy Anupama, Sadhukhan Sushabhan
Department of Chemistry, Indian Institute of Technology Palakkad, Kerala, India.
Department of Biosciences and Biomedical Engineering, Indian Institute of Technology Indore, Madhya Pradesh, India.
Crit Rev Food Sci Nutr. 2023;63(30):10382-10411. doi: 10.1080/10408398.2022.2068500. Epub 2022 May 2.
Natural products have been a bedrock for drug discovery for decades. -Epigallocatechin--gallate (EGCG) is one of the widely studied natural polyphenolic compounds derived from green tea. It is the key component believed to be responsible for the medicinal value of green tea. Significant studies implemented in , , and models have suggested its anti-oxidant, anti-cancer, anti-diabetic, anti-inflammatory, anti-microbial, neuroprotective activities etc. Despite having such a wide array of therapeutic potential and promising results in preclinical studies, its applicability to humans has encountered with rather limited success largely due to the poor bioavailability, poor membrane permeability, rapid metabolic clearance and lack of stability of EGCG. Therefore, novel techniques are warranted to address those limitations so that EGCG or its modified analogs can be used in the clinical setup. This review comprehensively covers different strategies such as structural modifications, nano-carriers as efficient drug delivery systems, synergistic studies with other bioactivities to improve the chemico-biological aspects (e.g., stability, bioavailability, permeability, etc.) of EGCG for its enhanced pharmacokinetics and pharmacological properties, eventually enhancing its therapeutic potentials. We think this review article will serve as a strong platform with comprehensive literature on the development of novel techniques to improve the bioavailability of EGCG so that it can be translated to the clinical applications.
几十年来，天然产物一直是药物发现的基石。表没食子儿茶素没食子酸酯（EGCG）是一种经过广泛研究的源自绿茶的天然多酚化合物。它被认为是绿茶具有药用价值的关键成分。在[具体模型1]、[具体模型2]和[具体模型3]模型中进行的大量研究表明了其抗氧化、抗癌、抗糖尿病、抗炎、抗微生物、神经保护等活性。尽管EGCG在临床前研究中具有如此广泛的治疗潜力和令人鼓舞的结果，但其在人体中的应用却取得了相当有限的成功，这主要是由于EGCG的生物利用度差、膜通透性差、代谢清除快以及缺乏稳定性。因此，需要新技术来解决这些局限性，以便EGCG或其修饰类似物能够用于临床。本综述全面涵盖了不同的策略，如结构修饰、作为高效药物递送系统的纳米载体、与其他生物活性的协同研究，以改善EGCG的化学-生物学特性（如稳定性、生物利用度、通透性等），从而增强其药代动力学和药理学性质，最终提高其治疗潜力。我们认为这篇综述文章将成为一个强大的平台，提供关于提高EGCG生物利用度的新技术开发的全面文献，以便将其转化为临床应用。
