Pharmacokinetic, synthesis and biological properties of rottlerin: Anticancer mechanism insights.

Rottlerin is a natural plant polyphenol derived from the fruit of Mallotus philippensis and is widely recognized as a selective inhibitor of PKCδ. It has attracted significant attention due to its broad spectrum of pharmacological properties, particularly its antitumor potential across various human cancers. This review aims to provide a comprehensive overview of rottlerin, including its natural source, synthesis, pharmacological activities, mechanisms of action, and pharmacokinetic characteristics, to assess its therapeutic potential and future applications. A comprehensive review of the literature was carried out using pertinent keywords from a number of scientific sources, including Web of Science, PubMed, and Scopus. Studies on the pharmacological and pharmacokinetic properties of rottlerin were collected, analyzed, and synthesized. Rottlerin demonstrates a wide range of pharmacological activities, such as antioxidant, antimicrobial, antiviral, antiallergic, and antidiabetic effects. It also shows protective effects in hepatic, neural, dermatological, cardiovascular, and vascular systems. Mechanistically, it acts through PKCδ inhibition, apoptosis induction, oxidative stress regulation, and suppression of inflammatory pathways. Pharmacokinetic data indicate strong plasma protein binding (>99 %) and high stability in mouse plasma. Rottlerin holds significant promise as a therapeutic agent due to its multifaceted biological activities. However, further research is necessary to clarify its precise molecular mechanisms, improve its pharmacokinetic profile, and enhance its synthetic yield, purity, and scalability for potential clinical applications.