Pculin02H, a curcumin derivative, inhibits proliferation and clinical drug resistance of HER2-overexpressing cancer cells

Lien, Jin‐Cherng; Hung, Chao‐Ming; Lin, Yijing; Lin, Hong‐Cheu; Ko, Ting-Chia; Tseng, Li-Chung; Kuo, Sheng‐Chu; Ho, Chi‐Tang; Lee, Jang-Chang; Way, Tzong‐Der

doi:10.1016/j.cbi.2015.04.005

Cited by 15 publications

(7 citation statements)

References 29 publications

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“…These derivatives were much less prone to nucleophilic addition than CUR and benzyl mercaptan addition analyses showed that indeed they do not form isolable conjugated products, which might delay the degradation and enhance the reversal effect of MDR (Labbozzetta et al, 2009). For example, among CUR derivatives synthesized by Lien et al (2015), pculin 02h (Figure 3, Scheme 3) showed to be more effective in reversal MDR. Concretely, after treating with 2.5 μM pculin 02h for 24 hr in breast cancer, the inhibition rate of MCF‐7/HER18 cells and MDA‐MB 435/HER2 cells was over 40% higher than that of CUR.…”

Section: Application Of Cur Derivative In Tumor Mdrmentioning

confidence: 99%

Section: Modification Of the β-Diketonementioning

confidence: 99%

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Application of curcumin and its derivatives in tumor multidrug resistance

Guo

et al. 2020

Phytotherapy Research

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Malignant tumor endangers seriously the health of all mankind. Multidrug resistance (MDR) is one of the main causes of clinical tumor chemotherapy failure. Curcumin (CUR) has not only antitumor activity but also reversing tumor MDR effect. CUR reverses tumor MDR via regulating related signal pathways or corresponding expressed proteins or gene. When combined with chemotherapeutic agents, CUR can be a chemotherapeutic sensitive agent to enhance chemotherapy efficacy and weaken tumor MDR. On the other hand, to improve the MDR reversal effect of CUR, its derivatives have been extensively studied. Therefore, this article mainly focuses on reviewing the application of CUR and its derivatives in MDR and its mechanism of reversing MDR.

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Section: Application Of Cur Derivative In Tumor Mdrmentioning

confidence: 99%

Section: Modification Of the β-Diketonementioning

confidence: 99%

Application of curcumin and its derivatives in tumor multidrug resistance

Guo

et al. 2020

Phytotherapy Research

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“…In addition, several efforts are ongoing to improve the efficacy of curcumin by developing derivatives of curcumin, eg, Pculin02H. 20…”

Section: Anticancer Effects Of Curcuminmentioning

confidence: 99%

“…Pculin02H, a curcumin derivative, has been effective in inhibiting proliferation than that of curcumin and thus highlights the development of curcumin derivatives, which can potentially target the growth of cancer cells. 20…”

Section: Annotation Of Multiple Molecular Targets Of Curcuminmentioning

confidence: 99%

“…In addition, several efforts are ongoing to improve the efficacy of curcumin by developing derivatives of curcumin, eg, Pculin02H. 20 However, much recently, attention has been shifted in understanding the molecular regulation of this process. Curcumin negatively regulates MDM2 protein resulting in destabilization of the interaction of Mdm2 with p53 (Fig.…”

Section: Mdm2 Regulation Of P53mentioning

confidence: 99%

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The Complex Triad of Combinatorial Anticancer Therapy: Curcumin, p53, and Reactive Oxygen Species

Singh

Satapathy

Kumar

et al. 2015

Clinical Medicine Insights: Therapeutics

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Cancer therapies based on single target molecules have proved to be ineffective both in terms of their desired action and associated undesired side effects. Combinatorial cancer therapies involve selection of different components with targeted effects, which can lead to a synergistic effect for anticancer therapy. Curcumin induces the expression of p53 and downregulates that of Mdm2, ultimately resulting in induction of apoptosis. Subsequently, there is an elevated expression of p53-induced genes, which activate reactive oxygen species (ROS) thereby establishing cellular communication and disposition of any aberrant cell by growth arrest or apoptotic cell death. As a whole, the triad of curcumin, p53, and ROS presents a unique and promising solution to the designing of modern and patient-specific cancer therapeutics.

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