Croton tiglium Linn., commonly known as Jamalgota or Purging Croton, is a well-recognized medicinal shrub belonging to the family Euphorbiaceae. Traditionally employed in Ayurveda, Traditional Chinese Medicine (TCM), and Southeast Asian ethnomedicine, the plant has been valued for its potent purgative, antimicrobial, and anti-inflammatory properties. Despite its known toxicity, particularly from phorbol ester-rich seeds, C. tiglium remains a subject of contemporary pharmacognostic interest due to its wide-ranging bioactive phytochemicals and potential therapeutic applications. The plant’s phytochemical profile includes tigliane diterpenoids, alkaloids, fatty acids, proteins, and phenolic compounds, many of which contribute to its biological versatility. Diterpenoids such as croton oil phorbol esters exhibit both therapeutic and toxic effects by modulating protein kinase C (PKC) pathways, influencing cell proliferation, inflammation, and differentiation. Recent studies highlight its promising pharmacological activities encompassing anticancer, antiviral, antibacterial, anti-inflammatory, and neuroprotective effects. Moreover, preliminary mechanistic insights suggest potential applications in promoting hair growth through PKC-mediated signaling, improved microcirculation, and antioxidative mechanisms that may stimulate hair follicle regeneration. However, the plant’s inherent toxicity poses significant challenges for safe clinical translation, necessitating rigorous detoxification procedures (Shodhana) and standardized formulation approaches. This review consolidates current phytochemical and pharmacological evidence, critically analyzing the dual therapeutic–toxic nature of C. tiglium and exploring its future prospects as a promising candidate for hair-growth formulations and beyond.