Nerium oleander, a member of family Apocynaceae, is commonly known as Kaner in various countries of Asia and Mediterranean region. This plant has been renowned to possess significant therapeutic potential due to its various bioactive compounds which have been isolated from this plant e.g., cardiac glycosides, oleandrin, α-tocopherol, digitoxingenin, urosolic acid, quercetin, odorosides, and adigoside. Oleandrin, a saponin glycoside is one of the most potent and pharmacologically active phytochemicals of N. oleander. Its remarkable pharmacotherapeutic potential have been interpreted as anticancer, anti-inflammatory, anti-HIV, neuroprotective, antimicrobial and antioxidant. This particular bioactive entity is known to target the multiple deregulated signaling cascades of cancer such as NF-κB, MAPK, and PI3K/Akt. The main focus of the current study is to comprehend the action mechanisms of oleandrin against various pathological conditions. The current review is a comprehensive summary to facilitate the researchers to understand the pharmacological position of the oleandrin in the arena of drug discovery, representing this compound as a new drug candidate for further researches. Moreover, in vivo and in silico based studies are required to explore the mechanistic approaches regarding the pharmacokinetics and biosafety profiling of this compound to completely track its candidature status in natural drug discovery.

夹竹桃，夹竹桃科的一员，在亚洲和地中海地区的许多国家通常被称为Kaner。由于从植物中分离出的各种生物活性化合物，例如强心苷，夹竹桃苷，α-生育酚，洋地黄毒苷，熊果酸，槲皮素，阿糖苷和阿迪果苷，该植物因具有多种生物活性化合物而广受赞誉。夹竹桃苷的夹竹桃苷是夹竹桃中最有力和药理活性的植物化学物质之一。其非凡的药物治疗潜力已被解释为抗癌，抗炎，抗HIV，神经保护，抗微生物和抗氧化剂。已知这种特定的生物活性实体靶向多种失控的癌症信号传导级联，例如NF-κB，MAPK和PI3K / Akt。当前研究的主要重点是理解夹竹桃苷对各种病理状况的作用机制。当前的综述是一个全面的摘要，以方便研究人员了解夹竹桃苷在药物发现领域的药理地位，并将其表示为进一步研究的新候选药物。此外，体内和计算机模拟 需要进行基础研究来探索有关此化合物的药代动力学和生物安全性分析的机制方法，以完全跟踪其在天然药物发现中的候选资格。