Plants and plant extracts have long been acknowledged as valuable resources for the development of therapeutic formulations for various diseases. Among them, numerous plants and plant-derived products have demonstrated cytotoxic and/or anti-tumor properties. Saffron, particularly due to its major compounds, namely crocin, crocetin, and safranal, stands out as a promising candidate in this regard. Our research undertakes a literature review, reaffirming the antioxidant, anti-inflammatory, and, notably, anti-tumor properties of saffron and its major constituents. Additionally, this study examines relevant patent documents, highlighting innovative applications for saffron and its major compounds in cancer therapy. The review discusses the progress in purifying the compounds extracted from saffron and assesses their impact on cytotoxic trial outcomes, the potential synergies between certain saffron compounds and established cytotoxic molecules, and the limitations of the patents examined, particularly concerning reported clinical evidence. Researchers who focus on advances in oncology will know from our findings the evolution of the patent landscape regarding cytotoxic and/or anti-tumor therapeutic applications using saffron or its main compounds. Moreover, investigators can draw inspiration from patents leveraging traditional knowledge, particularly from Chinese medicine, to clarify specific active molecules and their mechanisms of action and can expedite the translation of these findings into clinically relevant interventions, potentially enhancing cancer therapy outcomes.

Crocus sativus L. (saffron), a sterile geophyte of the Iridaceae family, has been traditionally used in culinary and medicinal practices and is currently gaining attention as a source of pharmacologically active metabolites. The main bioactive compounds (BACs) of saffron, crocin, crocetin, picrocrocin, and safranal, are associated with a wide range of biological activities, including anti-inflammatory, antioxidant, immunomodulatory, antimicrobial, antiproliferative, and antidiabetic properties, among others. This review aims to comprehensively and critically summarize the preclinical and clinical evidence for saffron-derived BACs in the context of the most prevalent non-communicable diseases. A literature search of the main scientific databases was conducted to identify peer-reviewed articles on neurodegenerative disorders, cancer, cardiovascular diseases, and diabetes mellitus, with additional topics on ethnopharmacology, phytochemistry, safety, and toxicity. The mechanistic findings include anti-inflammatory, immunomodulatory, antioxidant, antiproliferative, and neuroprotective effects, mediated by activation of the Nrf2 pathway and inhibition of NF-κB. Eligibility criteria were applied, excluding publications focused primarily on food, cosmetics, or technological applications, to prioritize mechanistic and therapeutic endpoints. The findings suggest that BACs from saffron extracts have promising disease-modifying properties and symptom-relieving actions, especially in the case of neurologic disorders, mild cognitive impairment, and some models of metabolic and oncological diseases. Nevertheless, the current variability in study design, dosage, standardization of plant extracts, and sample size limits a conclusive clinical application. More carefully designed studies with a representative number of cases and well-defined plant preparations are needed to validate efficacy, establish structure-activity relationships, and define the prevention and therapeutic potential of saffron in evidence-based pharmacotherapy.