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Curcumin and Its Derivatives
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Curcumin and Its Derivatives

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: 31 May 2025 | Viewed by 29867

Special Issue Editor

Dr. Erika Ferrari

E-Mail Website
Guest Editor
Department of Chemical and Geological Sciences, University of Modena and Reggio Emilia, via Campi, 103-41125 Modena, Italy
Interests: curcumin; metal-based drugs; PET-radiotracers; gallium-68; curcuminoids; NMR spectroscopy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In the last decades, the naturally occurring polyphenol curcumin has earned increased attention in view of its in vitro beneficial effects comprising antioxidant, anti-inflammatory, and anti-cancer activities. Unfortunately, curcumin has poor water-solubility and bioavailability, drawbacks that hamper its great therapeutic properties and hold back its use in biomedical applications. This limit could be overcome by designing new methods of administration or by synthesizing novel daughter compounds with modified chemical structures. Curcumin and its derivatives also have applications in the development of new materials and chemical sensors.

In the last decade, there has been an increase in the number of published papers dealing with curcumin, indicating a bloom in research activity and attention from the scientific community to this topic.

In this landscape, this Special Issue of Molecules dedicated to “Curcumin and its derivatives” aims to collect the latest cutting-edge discoveries in the synthesis, characterization, theoretical calculations, delivery, and applications of curcumin-based compounds and materials.

Dr. Erika Ferrari
Guest Editor

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Keywords

  • curcumin
  • curcuminoids
  • synthesis
  • drug delivery systems
  • theoretical calculations
  • hybrid materials
  • sensors

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Published Papers (7 papers)

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Research

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12 pages, 3483 KiB  
Article
Changes in Lysine Methylation Contribute to the Cytotoxicity of Curcumin in Colon Cancer Cells
by Roberta Santarelli, Paola Currà, Michele Di Crosta, Roberta Gonnella, Maria Saveria Gilardini Montani and Mara Cirone
Molecules 2025, 30(2), 335; https://doi.org/10.3390/molecules30020335 - 16 Jan 2025
Cited by 1 | Viewed by 1048
Abstract
Epigenetic abnormalities play a critical role in colon carcinogenesis, making them a promising target for therapeutic interventions. In this study, we demonstrated that curcumin reduces colon cancer cell survival and that a decrease in lysine methylation was involved in such an effect. This [...] Read more.
Epigenetic abnormalities play a critical role in colon carcinogenesis, making them a promising target for therapeutic interventions. In this study, we demonstrated that curcumin reduces colon cancer cell survival and that a decrease in lysine methylation was involved in such an effect. This correlated with the downregulation of methyltransferases EZH2, MLL1, and G9a, in both wild-type p53 (wtp53) HCT116 cells and mutant p53 (mutp53) SW480 cells, as well as SET7/9 specifically in wtp53 HCT116 cells. The effects induced by curcumin were more pronounced in wtp53 cells, where it induced a stronger apoptosis and ferroptosis. Interestingly, curcumin also reduced mutp53 expression, suggesting that it could enhance the efficacy of other therapies, particularly in overcoming drug resistance mechanisms associated with mutp53. For instance, in this study, we show that curcumin sensitized SW480 cells to SET7/9 inhibition by sinefungin, further supporting its potential as a combinatorial therapeutic agent. However, although to a lesser extent, curcumin also impaired cell survival in HCT 116 p53 null cells, suggesting that other molecular pathways or factors, beyond p53, may be involved in curcumin-induced cytotoxicity. Full article
(This article belongs to the Special Issue Curcumin and Its Derivatives)
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15 pages, 5189 KiB  
Article
Discovery of Novel Mono-Carbonyl Curcumin Derivatives as Potential Anti-Hepatoma Agents
by Weiya Cao, Pan Yu, Shilong Yang, Zheyu Li, Qixuan Zhang, Zengge Liu and Hongzhuo Li
Molecules 2023, 28(19), 6796; https://doi.org/10.3390/molecules28196796 - 25 Sep 2023
Cited by 4 | Viewed by 1898
Abstract
Curcumin possesses a wide spectrum of liver cancer inhibition effects, yet it has chemical instability and poor metabolic properties as a drug candidate. To alleviate these problems, a series of new mono-carbonyl curcumin derivatives G1–G7 were designed, synthesized, and evaluated by in vitro [...] Read more.
Curcumin possesses a wide spectrum of liver cancer inhibition effects, yet it has chemical instability and poor metabolic properties as a drug candidate. To alleviate these problems, a series of new mono-carbonyl curcumin derivatives G1–G7 were designed, synthesized, and evaluated by in vitro and in vivo studies. Compound G2 was found to be the most potent derivative (IC50 = 15.39 μM) compared to curcumin (IC50 = 40.56 μM) by anti-proliferation assay. Subsequently, molecular docking, wound healing, transwell, JC-1 staining, and Western blotting experiments were performed, and it was found that compound G2 could suppress cell migration and induce cell apoptosis by inhibiting the phosphorylation of AKT and affecting the expression of apoptosis-related proteins. Moreover, the HepG2 cell xenograft model and H&E staining results confirmed that compound G2 was more effective than curcumin in inhibiting tumor growth. Hence, G2 is a promising leading compound with the potential to be developed as a chemotherapy agent for hepatocellular carcinoma. Full article
(This article belongs to the Special Issue Curcumin and Its Derivatives)
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15 pages, 2484 KiB  
Article
13C CPMAS NMR as an Alternative Method to Verify the Quality of Dietary Supplements Containing Curcumin
by Paweł Siudem, Łukasz Szeleszczuk, Agnieszka Zielińska and Katarzyna Paradowska
Molecules 2023, 28(8), 3442; https://doi.org/10.3390/molecules28083442 - 13 Apr 2023
Cited by 4 | Viewed by 2706
Abstract
Turmeric is a traditional Indian spice that has recently become very popular worldwide because it contains a powerful ingredient called curcumin, which has strong anti-inflammatory properties. Hence, dietary supplements containing extracts rich in curcumin have gained great popularity. The main problems related to [...] Read more.
Turmeric is a traditional Indian spice that has recently become very popular worldwide because it contains a powerful ingredient called curcumin, which has strong anti-inflammatory properties. Hence, dietary supplements containing extracts rich in curcumin have gained great popularity. The main problems related to curcumin-containing dietary supplements are poor water solubility and the fact that they are often faked by using synthetic curcumin instead of the plant extract. In this article, we propose the use of the 13C CPMAS NMR method to control the quality of dietary supplements. The analysis of 13C CPMAS NMR spectra supported by GIPAW computations allowed us to identify a polymorphic form present in dietary supplements (which affected the solubility of curcumin) and to point out a dietary supplement that could be faked by using synthetic curcumin. Further PXRD and HPLC investigations confirmed that the examined supplement contained synthetic curcumin instead of the genuine extract. Our method can be used for routine control, especially because the investigation is performed directly from the capsule/tablet content and does not require any special sample preparation. Full article
(This article belongs to the Special Issue Curcumin and Its Derivatives)
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Review

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27 pages, 3045 KiB  
Review
Curcumin in Ophthalmology: Mechanisms, Challenges, and Emerging Opportunities
by Adriana Ribeiro, Daniele Oliveira and Helena Cabral-Marques
Molecules 2025, 30(3), 457; https://doi.org/10.3390/molecules30030457 - 21 Jan 2025
Viewed by 1883
Abstract
Ocular diseases affecting the anterior and posterior segments of the eye are major causes of global vision impairment. Curcumin, a natural polyphenol, exhibits anti-inflammatory, antioxidant, antibacterial, and neuroprotective properties, making it a promising candidate for ocular therapy. However, its clinical use is hindered [...] Read more.
Ocular diseases affecting the anterior and posterior segments of the eye are major causes of global vision impairment. Curcumin, a natural polyphenol, exhibits anti-inflammatory, antioxidant, antibacterial, and neuroprotective properties, making it a promising candidate for ocular therapy. However, its clinical use is hindered by low aqueous solubility, poor bioavailability, and rapid systemic elimination. This review comprehensively highlights advances in curcumin delivery systems aimed at overcoming these challenges. Emerging platforms, including proniosomal gels, transferosomes, and cyclodextrin complexes, have improved solubility, permeability, and ocular retention. Nanoparticle-based carriers, such as hybrid hydrogels and biodegradable nanoparticles, enable sustained release and targeted delivery, supporting treatments for posterior segment diseases like diabetic retinopathy and age-related macular degeneration. For anterior segment conditions, including keratitis and dry eye syndrome, cyclodextrin-based complexes and mucoadhesive systems enhance corneal permeability and drug retention. Mechanistically, curcumin modulates key pathways, such as NF-κB and TLR4, reducing oxidative stress, angiogenesis, and apoptosis. Emerging strategies like photodynamic therapy and neuroprotective approaches broaden their application to eyelid conditions and neuroinflammatory ocular diseases. These advancements address curcumin’s pharmacokinetic limitations, supporting its clinical translation into ophthalmic therapies. This work underscores curcumin’s potential in ocular disease management and advocates clinical trials to validate its safety, efficacy, and therapeutic relevance. Full article
(This article belongs to the Special Issue Curcumin and Its Derivatives)
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35 pages, 4474 KiB  
Review
Curcumin Derivatives in Medicinal Chemistry: Potential Applications in Cancer Treatment
by Joanna Kuzminska, Piotr Szyk, Dariusz T. Mlynarczyk, Pawel Bakun, Izabela Muszalska-Kolos, Katarzyna Dettlaff, Agnieszka Sobczak, Tomasz Goslinski and Anna Jelinska
Molecules 2024, 29(22), 5321; https://doi.org/10.3390/molecules29225321 - 12 Nov 2024
Cited by 4 | Viewed by 3152
Abstract
Curcumin, a naturally occurring compound found in the rhizome of Curcuma plants, particularly in turmeric (Curcuma longa L.), exhibits a broad range of biological activities, including anti-inflammatory, antioxidant, and anticancer properties. Curcumin has demonstrated effectiveness in inhibiting tumor growth, arousing interest for [...] Read more.
Curcumin, a naturally occurring compound found in the rhizome of Curcuma plants, particularly in turmeric (Curcuma longa L.), exhibits a broad range of biological activities, including anti-inflammatory, antioxidant, and anticancer properties. Curcumin has demonstrated effectiveness in inhibiting tumor growth, arousing interest for its potential in treating various cancers, such as breast, lung, prostate, and brain cancers. However, the clinical application of curcumin is limited due to its low chemical stability, poor water solubility, and low bioavailability. In response to these challenges, structural modifications of curcumin have been explored to improve its pharmacological properties, including enhanced anticancer selectivity index and bioavailability. This review highlights promising chemical modifications of curcumin that could lead to the development of more effective anticancer therapies. By functionalizing the parent curcumin molecule, researchers aim to create more stable and bioavailable compounds with enhanced therapeutic potential, making curcumin derivatives promising candidates for medical applications. Full article
(This article belongs to the Special Issue Curcumin and Its Derivatives)
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16 pages, 814 KiB  
Review
Advancing Gastrointestinal Health: Curcumin’s Efficacy and Nanopreparations
by Jialin Ji, Zhaojie Ma and Yingshuai Wang
Molecules 2024, 29(7), 1659; https://doi.org/10.3390/molecules29071659 - 7 Apr 2024
Cited by 7 | Viewed by 4154
Abstract
Curcumin (CCM) is a polyphenol compound extracted from the turmeric rhizome. It has various biological activities, including antibacterial, anti-inflammatory, anti-cancer, and antioxidant. Due to its diverse activities, it is often used by researchers to study the therapeutic effects on various diseases. However, its [...] Read more.
Curcumin (CCM) is a polyphenol compound extracted from the turmeric rhizome. It has various biological activities, including antibacterial, anti-inflammatory, anti-cancer, and antioxidant. Due to its diverse activities, it is often used by researchers to study the therapeutic effects on various diseases. However, its poor solubility leads to poor bioavailability, and it is necessary to increase the water solubility with the help of carriers to improve the therapeutic effect. Gastrointestinal disease is a major global health problem that continues to affect human health. In this review, we have summarized the possible mechanism and therapeutic effect of CCM in various gastrointestinal diseases, and the improvement in the curative effect of CCM with nanopreparation. Finally, we concluded that there have been many clinical trials of CCM in combination with other drugs for the treatment of gastrointestinal disease, but so far, few have used CCM nanomaterials for treatment. Although in vitro and preclinical experiments have shown that nanopreparations can improve the efficacy of CCM, there are still insufficient studies on the safety of carriers. Full article
(This article belongs to the Special Issue Curcumin and Its Derivatives)
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27 pages, 1068 KiB  
Review
A Comprehensive Review on the Benefits and Problems of Curcumin with Respect to Human Health
by Siyu Liu, Jie Liu, Lan He, Liu Liu, Bo Cheng, Fangliang Zhou, Deliang Cao and Yingchun He
Molecules 2022, 27(14), 4400; https://doi.org/10.3390/molecules27144400 - 8 Jul 2022
Cited by 63 | Viewed by 14221
Abstract
Curcumin is the most important active component in turmeric extracts. Curcumin, a natural monomer from plants has received a considerable attention as a dietary supplement, exhibiting evident activity in a wide range of human pathological conditions. In general, curcumin is beneficial to human [...] Read more.
Curcumin is the most important active component in turmeric extracts. Curcumin, a natural monomer from plants has received a considerable attention as a dietary supplement, exhibiting evident activity in a wide range of human pathological conditions. In general, curcumin is beneficial to human health, demonstrating pharmacological activities of anti-inflammation and antioxidation, as well as antitumor and immune regulation activities. Curcumin also presents therapeutic potential in neurodegenerative, cardiovascular and cerebrovascular diseases. In this review article, we summarize the advancements made in recent years with respect to curcumin as a biologically active agent in malignant tumors, Alzheimer’s disease (AD), hematological diseases and viral infectious diseases. We also focus on problems associated with curcumin from basic research to clinical translation, such as its low solubility, leading to poor bioavailability, as well as the controversy surrounding the association between curcumin purity and effect. Through a review and summary of the clinical research on curcumin and case reports of adverse effects, we found that the clinical transformation of curcumin is not successful, and excessive intake of curcumin may have adverse effects on the kidneys, heart, liver, blood and immune system, which leads us to warn that curcumin has a long way to go from basic research to application transformation. Full article
(This article belongs to the Special Issue Curcumin and Its Derivatives)
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