关键词: Panax ginseng Anticancer Ginsenoside Rg5 Pharmacokinetics properties SAR

Mesh : Humans Ginsenosides / pharmacology therapeutic use Apoptosis Antineoplastic Agents / pharmacology therapeutic use Neoplasms / drug therapy Structure-Activity Relationship

来  源:   DOI:10.1007/s43440-024-00586-5

Abstract:
Cancer remains one of the leading causes of death in the world. Despite the considerable success of conventional treatment strategies, the incidence and mortality rates are still high, making developing new effective anticancer therapies an urgent priority. Ginsenoside Rg5 (Rg5) is a minor ginsenoside constituent obtained exclusively from ginseng species and is known for its broad spectrum of pharmacological activities. This article aimed to comprehensively review the anticancer properties of Rg5, focusing on action mechanisms, structure-activity relationship (SAR), and pharmacokinetics attributes. The in vitro and in vivo activities of Rg5 have been proven against several cancer types, such as breast, liver, lung, bone, and gastrointestinal (GI) cancers. The modulation of multiple signaling pathways critical for cancer growth and survival mediates these activities. Nevertheless, human clinical studies of Rg5 have not been addressed before, and there is still considerable ambiguity regarding its pharmacokinetics properties. In addition, a significant shortage in the structure-activity relationship (SAR) of Rg5 has been identified. Therefore, future efforts should focus on further optimization by performing extensive SAR studies to uncover the structural features essential for the potent anticancer activity of Rg5. Thus, this review highlights the value of Rg5 as a potential anticancer drug candidate and identifies the research areas requiring more investigation.
摘要:
癌症仍然是世界上主要的死亡原因之一。尽管常规治疗策略取得了相当大的成功,发病率和死亡率仍然很高,使开发新的有效抗癌疗法成为当务之急。人参皂苷Rg5(Rg5)是仅从人参物种获得的少量人参皂苷成分,并且以其广谱的药理活性而闻名。本文旨在全面综述Rg5的抗癌特性,重点介绍其作用机制,构效关系(SAR),和药代动力学属性。Rg5的体外和体内活性已被证明可以抵抗几种癌症类型,如乳房,肝脏,肺,骨头,和胃肠道(GI)癌症。对癌症生长和存活至关重要的多种信号传导途径的调节介导这些活性。然而,Rg5的人体临床研究以前没有得到解决,关于其药代动力学特性仍然存在相当大的歧义。此外,已发现Rg5的结构-活性关系(SAR)存在明显不足。因此,未来的努力应集中在通过进行广泛的SAR研究来揭示Rg5有效抗癌活性所必需的结构特征,从而进一步优化.因此,这篇综述强调了Rg5作为潜在抗癌药物候选药物的价值,并确定了需要更多研究的研究领域.
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