ArticleScientific reports2019
Curcumin diethyl disuccinate, a prodrug of curcumin, enhances anti-proliferative effect of curcumin against HepG2 cells via apoptosis induction.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 37 citations in OpenAlex.
- Curcumin and Its Derivatives in Hepatology: Therapeutic Potential and Advances in Nanoparticle Formulations.Cancers · 2025Review
- Synthesis, Cytotoxicity, and Mechanistic Evaluation of Tetrahydrocurcumin-Amino Acid Conjugates as LAT1-Targeting Anticancer Agents in C6 Glioma Cells.International journal of molecular sciences · 2024Article
- Enhancing the Bioavailability and Bioactivity of Curcumin for Disease Prevention and Treatment.Antioxidants (Basel, Switzerland) · 2024Review
- Curcumin as a novel therapeutic candidate for cancer: can this natural compound revolutionize cancer treatment?Frontiers in oncology · 2024Review
- Potential Oral Anticancer Therapeutic Agents of Hexahydrocurcumin-Encapsulated Chitosan Nanoparticles against MDA-MB-231 Breast Cancer Cells.Pharmaceutics · 2023Article
- Using Computational Drug-Gene Analysis to Identify Novel Therapeutic Candidates for Retinal Neuroprotection.International journal of molecular sciences · 2022Article
- Curcumin Diethyl γ-Aminobutyrate, a Prodrug of Curcumin, for Enhanced Treatment of Inflammatory Pain.ACS pharmacology & translational science · 2022Article
- Enhancement of curcumin level and hepatoprotective effect in rats through antioxidant activity following modification into nanosized particles.Veterinary world · 2022Article
- Curcumin and Wnt/β‑catenin signaling in exudative age‑related macular degeneration (Review).International journal of molecular medicine · 2022Review
- Validation of a Quantification Method for Curcumin Derivatives and Their Hepatoprotective Effects on Nonalcoholic Fatty Liver Disease.Current issues in molecular biology · 2022Article
- Chinese medicinal herbs as potential prodrugs for obesity.Frontiers in pharmacology · 2022Review
- A Stability-Indicating Ultra Performance Liquid Chromato-Graphic (UPLC) Method for the Determination of a Mycophenolic Acid-Curcumin Conjugate and Its Applications to Chemical Kinetic Studies.Molecules (Basel, Switzerland) · 2021Article
- Mechanistic Insight into the Effects of Curcumin on Neuroinflammation-Driven Chronic Pain.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Anti-inflammatory role of curcumin in retinal disorders (Review).Experimental and therapeutic medicine · 2021Review
- A Novel Curcumin-Mycophenolic Acid Conjugate Inhibited Hyperproliferation of Tumor Necrosis Factor-Alpha-Induced Human Keratinocyte Cells.Pharmaceutics · 2021Article
- Protective Effects of a Lutein Ester Prodrug, Lutein Diglutaric Acid, against HInternational journal of molecular sciences · 2021Article
- Antioxidant Activities and Protective Effects of Dendropachol, a New Bisbibenzyl Compound fromAntioxidants (Basel, Switzerland) · 2021Article
- Hydroxyethyl Starch Curcumin Enhances Antiproliferative Effect of Curcumin Against HepG2 CellsFrontiers in pharmacology · 2021Article
- Curcumin and Photobiomodulation in Chronic Viral Hepatitis and Hepatocellular Carcinoma.International journal of molecular sciences · 2020Review
- Co-administration of Pregabalin and Curcumin Synergistically Decreases Pain-Like Behaviors in Acute Nociceptive Pain Murine Models.Molecules (Basel, Switzerland) · 2020Article
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Curcumin (Cur) has been reported to have anti-hepatocellular carcinoma activity but its poor oral bioavailability limits its further development as a chemotherapeutic agent. We synthesized previously a succinate ester prodrug of Cur, curcumin diethyl disuccinate (CurDD) with better chemical stability in a buffer solution pH 7.4. Here, we further investigated and compared the cellular transport and anti-proliferative activity against HepG2 cells of CurDD and Cur. Transport of CurDD across the Caco-2 monolayers provided a significantly higher amount of the bioavailable fraction (BF) of Cur with better cytotoxicity against HepG2 cells compared to that of Cur (p < 0.05). Flow cytometric analysis showed that the BF of CurDD shifted the cell fate to early and late apoptosis to a higher extent than that of Cur. The Western blot analysis revealed that CurDD increased Bax protein expression, downregulated Bcl-2 protein, activated caspase-3 and -9 and increased LC3-II protein level in HepG2 cells. Flow cytometric and immunoblotting results suggest that CurDD can induce HepG2 cell death via an apoptotic pathway. We suggest that CurDD can overcome the limitations of Cur in terms of cellular transport with a potential for further extensive in vitro and in vivo studies of anti-hepatocellular carcinoma effects.
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