eng Oriental Scientific Publishing Company Biosciences Biotechnology Research Asia 0973-1245 2026-09-01 23 3 59651 article Shaik Kamar Jaha 1 Kota Srivalli Maha Lakshmi 1 Salman Khan 1 Mabbu Viswanath Reddy 1 Department of Pharmacology, Jawaharlal Nehru Technological University Kakinada, Andhra Pradesh, India This review critically evaluates the phytochemistry, pharmacological activities, and toxicological profile of Tithonia diversifolia (Asteraceae). Evidence from preclinical studies indicates that the plant contains bioactive constituents, particularly sesquiterpene lactones and chlorogenic acids, which may contribute to anti-inflammatory, antimicrobial, antiparasitic, antioxidant, immunomodulatory, and metabolic effects. However, the reported therapeutic outcomes vary considerably according to extraction solvent, plant source, experimental model, and dose. Available toxicity studies also suggest a relatively narrow safety margin at higher exposure levels, with hepatotoxic, nephrotoxic, and gastrointestinal effects observed in animal models. Current literature is limited by heterogeneous methodologies, inconsistent phytochemical standardization, and the absence of human clinical studies. Future research should prioritize standardized extraction procedures, quantitative marker analysis, pharmacokinetic investigations, and well-designed clinical evaluations before therapeutic applications can be established. https://www.biotech-asia.org/vol23no3/phytochemical-profile-and-therapeutic-potential-of-tithonia-diversifolia-a-critical-review-of-pharmacological-activities-and-toxicological-considerations/ Anti-hyperglycaemic; Anti-inflammatory; Antimicrobial; Antioxidant activity; Antiparasitic; Immunomodulatory; Mexican Sunflower; Secondary metabolites; Tithonia diversifolia; Toxicity profile