Complex diseases such as neurodegenerative disorders and cancer constitute a growing public health problem due to the rising incidence and lack in effective therapies. Since pharmacotherapy based on a single target has been insufficient for drug development in complex diseases, the emerging multi-target approach is a promising strategy for the search of new drug candidates. Plant-derived isoquinoline alkaloids comprise a vast source of multimodal agents with unique structural diversity, and variated range of pharmacological activities. This review offers an exhaustive compilation of the pharmacological relevance and multi-target potential of natural isoquinolines, emphasizing their features and promising activity in complex diseases such as Alzheimer, Parkinson, and Cancer. Selected examples were discussed in depth to illustrate the most relevant structural motifs and their possible relationship with the multimodal activity offering a comprehensive baseline in the search and optimization of isoquinoline scaffolds with polypharmacological potential for complex diseases.

由于发病率上升和缺乏有效疗法，神经退行性疾病和癌症等复杂疾病构成了一个日益严重的公共卫生问题。由于基于单一靶点的药物治疗不足以用于复杂疾病的药物开发，因此新兴的多靶点方法是寻找新候选药物的有希望的策略。植物衍生的异喹啉生物碱包含大量具有独特结构多样性和不同药理活性的多模式药物来源。这篇综述对天然异喹啉的药理学相关性和多靶点潜力进行了详尽的汇编，强调了它们在阿尔茨海默病、帕金森和癌症等复杂疾病中的特征和有希望的活性。