<p><i>Curcuma longa</i> (turmeric) is a well-known medicinal plant that is rich in bioactive phytochemicals, among which curcuminoids (curcumin, demethoxycurcumin, and bisdemethoxycurcumin) are the principal constituents responsible for diverse pharmacological activities, ranging from antibacterial to anticancer. Despite its multifaceted therapeutic potential and clinical safety, the unfavorable pharmaceutical properties are limiting its clinical efficacy and hence are not able to attain the drug standard. Interestingly, this review provides a comprehensive overview of the complete phytochemical constituents of <i>C. longa</i>, and on the other hand, recent advancements (2020-2025) in the design and development of curcumin-based hybrid molecules aimed at overcoming the aforementioned limitations. Literature was systematically analyzed, focusing on structural modifications of curcuminoids, including functional group transformations, heterocycle incorporation, and monocarbonyl scaffold simplification to exploit these strategies’ significance on pharmacokinetic properties, metabolic stability, and anticancer activity. In particular, monocarbonyl curcumin-piperidone hybrids exhibit improved cytotoxicity, redox modulation, and multitarget mechanisms compared with curcumin and its other hybrids. Overall, curcumin hybridization represents a promising approach that bridges traditional herbal knowledge with modern drug discovery, offering valuable candidates for the development of effective anticancer therapeutics.</p><p></p>

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Chemical constituents in the rhizome of Curcuma longa and the pharmacological importance of curcumin hybrids

  • A. Jerin Rex,
  • P. Parthiban

摘要

Curcuma longa (turmeric) is a well-known medicinal plant that is rich in bioactive phytochemicals, among which curcuminoids (curcumin, demethoxycurcumin, and bisdemethoxycurcumin) are the principal constituents responsible for diverse pharmacological activities, ranging from antibacterial to anticancer. Despite its multifaceted therapeutic potential and clinical safety, the unfavorable pharmaceutical properties are limiting its clinical efficacy and hence are not able to attain the drug standard. Interestingly, this review provides a comprehensive overview of the complete phytochemical constituents of C. longa, and on the other hand, recent advancements (2020-2025) in the design and development of curcumin-based hybrid molecules aimed at overcoming the aforementioned limitations. Literature was systematically analyzed, focusing on structural modifications of curcuminoids, including functional group transformations, heterocycle incorporation, and monocarbonyl scaffold simplification to exploit these strategies’ significance on pharmacokinetic properties, metabolic stability, and anticancer activity. In particular, monocarbonyl curcumin-piperidone hybrids exhibit improved cytotoxicity, redox modulation, and multitarget mechanisms compared with curcumin and its other hybrids. Overall, curcumin hybridization represents a promising approach that bridges traditional herbal knowledge with modern drug discovery, offering valuable candidates for the development of effective anticancer therapeutics.