Andrographis paniculata (Burm.f.) Nees (Acanthaceae) is a herbaceous plant and is commonly called 'King of Bitters'. It has gained attraction as a potential hepatoprotective agent and a natural molecule with various biological activities viz. anticancer, immunomodulatory, anti-inflammatory, antibacterial, neuroprotective, and so on. The andrographolide is one of the main diterpenoids responsible for the drug's bitter taste and various therapeutic activities. The poor cellular permeability, solubility and short biological half-life of its pure components limit its distribution to the target tissue. To conquer this obstacle, various researchers worldwide have been working on designing the synthetic derivatives of its active components and nanoformulations to improve the drug's efficiency and selectivity to develop more active leads for biomedical applications. This article discussed the recent research on synthetic derivatives, including their possible therapeutic applications and structure-activity relationship (SAR). Additionally, this article also presents essential information concerning the various nanoformulations developed to increase the delivery of pure compound/plant extract to the target site, thereby improving the drug's efficacy for multiple ailments.

穿心莲 (Burm.f.) Nees (Acanthaceae) 是一种草本植物，通常被称为“苦中之王”。它作为一种潜在的保肝剂和具有各种生物活性的天然分子而备受关注。抗癌、免疫调节、抗炎、抗菌、神经保护等。穿心莲内酯是导致药物苦味和各种治疗活性的主要二萜类化合物之一。其纯组分较差的细胞渗透性、溶解性和较短的生物半衰期限制了其在靶组织中的分布。为了克服这一障碍，世界各地的研究人员一直致力于设计其活性成分的合成衍生物和纳米制剂，以改善药物的性能。s 的效率和选择性，为生物医学应用开发更活跃的先导物。本文讨论了合成衍生物的最新研究，包括其可能的治疗应用和构效关系（SAR）。此外，本文还介绍了有关开发的各种纳米制剂的基本信息，这些纳米制剂旨在增加纯化合物/植物提取物向目标部位的输送，从而提高药物对多种疾病的疗效。