Curcumin and Its New Derivatives: Correlation between Cytotoxicity against Breast Cancer Cell Lines, Degradation of PTP1B Phosphatase and ROS Generation

Kostrzewa, Tomasz; Wołosewicz, Karol; Jamrozik, Marek; Drzeżdżon, Joanna; Siemińska, Julia; Jacewicz, Dagmara; Górska‐Ponikowska, Magdalena; Kołaczkowski, Marcin; Łaźny, Ryszard; Kuban–Jankowska, Alicja

doi:10.3390/ijms221910368

Cited by 15 publications

(8 citation statements)

References 58 publications

(86 reference statements)

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“…PTP1B was conventionally considered a routine treatment for diabetes [32] and obesity originally [33]. Recently, it has been considered as a therapeutic objective in other fields including tumors [34], neuroinflammation [10], vascular endothelium protection [35], and neuroprotection. Many researches have revealed that the PTP1B gene is exceedingly expressed in ovarian cancer, gastric cancer, prostate cancer, and breast cancer and is related to poor prognosis [36].…”

Section: Discussionmentioning

confidence: 99%

Role of Protein Tyrosine Phosphatase 1B Inhibitor in Early Brain Injury of Subarachnoid Hemorrhage in Mice

2023

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Clinically, early brain injury (EBI), which refers to the acute injuries to the whole brain in the phase of the first 72 h following subarachnoid hemorrhage (SAH), is intensely investigated to improve neurological and psychological function. Additionally, it will be meaningful to explore new therapeutic approaches for EBI treatment to improve the prognosis of patients with SAH. To investigate the underlying neuroprotection mechanism in vitro, the Protein tyrosine phosphatase 1B inhibitor (PTP1B-IN-1) was put in primary neurons induced by OxyHb to observe neuroapoptosis, neuroinflammation, and ER stress. Then, one hundred forty male mice were subjected to Experiment two and Experiment three. The mice in the SAH24h + PTP1B-IN-1 group were given an intraperitoneal injection of 5 mg/kg PTP1B-IN-1 30 min before anesthesia. SAH grade, neurological score, brain water content, Western blot, PCR, and Transmission Electron Microscopy (TEM) were performed to observe the underlying neuroprotection mechanism in vivo. Overall, this study suggests that PTP1B-IN-1 could ameliorate neuroapoptosis, neuroinflammation, and ER stress in vitro and in vivo by regulating the IRS-2/AKT signaling pathway, suggesting that PTP1B-IN-1 may be a candidate drug for the treatment of early brain injury after SAH.

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Section: Discussionmentioning

confidence: 99%

Role of Protein Tyrosine Phosphatase 1B Inhibitor in Early Brain Injury of Subarachnoid Hemorrhage in Mice

2023

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“…This is seemingly associated to differences in the structure of these compounds. CUR suppress p300-HAT activity and reportedly inhibits cardiomyocyte hypertrophy and the development of heart failure [23]. In addition, there have been extensive structure-activity studies on the natural product CUR, and studies targeting p300-HAT activity and cardiomyocyte hypertrophy have been carried out [9].…”

Section: Discussionmentioning

confidence: 99%

“…CUR, with many bioactivities, has attracted worldwide attention. In addition, many derivatives of CUR have been synthesized using CUR as a lead compound and are being actively investigated [22,23]. However, little research has been conducted on the structure-activity relationship of CUR using cardiomyocyte hypertrophy.…”

Section: Introductionmentioning

confidence: 99%

Pyrazole-Curcumin Suppresses Cardiomyocyte Hypertrophy by Disrupting the CDK9/CyclinT1 Complex

et al. 2022

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The intrinsic histone acetyltransferase (HAT), p300, has an important role in the development and progression of heart failure. Curcumin (CUR), a natural p300-specific HAT inhibitor, suppresses hypertrophic responses and prevents deterioration of left-ventricular systolic function in heart-failure models. However, few structure–activity relationship studies on cardiomyocyte hypertrophy using CUR have been conducted. To evaluate if prenylated pyrazolo curcumin (PPC) and curcumin pyrazole (PyrC) can suppress cardiomyocyte hypertrophy, cultured cardiomyocytes were treated with CUR, PPC, or PyrC and then stimulated with phenylephrine (PE). PE-induced cardiomyocyte hypertrophy was inhibited by PyrC but not PPC at a lower concentration than CUR. Western blotting showed that PyrC suppressed PE-induced histone acetylation. However, an in vitro HAT assay showed that PyrC did not directly inhibit p300-HAT activity. As Cdk9 phosphorylates both RNA polymerase II and p300 and increases p300-HAT activity, the effects of CUR and PyrC on the kinase activity of Cdk9 were examined. Phosphorylation of p300 by Cdk9 was suppressed by PyrC. Immunoprecipitation-WB showed that PyrC inhibits Cdk9 binding to CyclinT1 in cultured cardiomyocytes. PyrC may prevent cardiomyocyte hypertrophic responses by indirectly suppressing both p300-HAT activity and RNA polymerase II transcription elongation activity via inhibition of Cdk9 kinase activity.

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“…Previous research study reported that curcumin had affected the enzyme PTP1B by increasing the sensitivity of hepatic leptin and insulin of rat liver [14,15]. Curcumin also inhibited PTP1B enzyme action that leads to improve hepatic leptin and insulin signaling in rats fed with fructose [16][17][18][19][20]. In addition, curcumin remarkably reduced the podocyte injury and proteinuria induced by fructose, the expression of PTP1B, and cut down the activity of insulin receptor and insulin receptor substrate 1 of fructose-fed rats [21].…”

Section: Introductionmentioning

confidence: 98%

Curcumins from <em>Curcuma longa </em>Potential Inhibit PTP1B and α-Glucosidase: Experimental and Computational Study

Dinh¹,

Nguyen²,

Quan³

et al. 2023

Preprint

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Curcuma longa is only a rich source of curcumin (1) and its major analogues demethoxycurcumin (2) and bisdemethoxycurcumin (3) among the Curcuma species. The content ratio of these three curcumins in turmeric is depended on the varieties and growing environment. Recently, curcumin (1) has been reported as potential inhibitor of hepatic and enzymatic protein tyrosine phosphatase 1B (PTP1B) and its related disorders such as hypertriglyceridemia, hyperlipidemia and liver steatosis. Thus, we further purified curcumins (1–3) from C. longa and investigated their inhibitory effects against PTP1B and α-glucosidase enzymes. As the result, curcumins (1–3) exhibited potential PTP1B inhibition with IC50 values of 37.8 ± 1.4, 45.3 ± 0.7, and 72.6 ± 1.1 μM, respectively, and α-glucosidase inhibition with similar manner (IC50 values of 78.2 ± 0.2, 82.4 ± 0.6, and 90.6 ± 1.0 μM, respectively). These results reveal a key role of methoxylation in the variation of PTP1B and α-glucosidase inhibitory activity for these curcumins. In addition, density functional theory (DFT) was used accompanying with molecular docking (MD) to analyze the ligand stability and the interaction of curcumins (1–3) with PTP1B and glucoside hydrolase proteins. Assay-based results and the MD data obtained are highly correlation suggesting that the deterioration of the enzyme activity caused by the distortion of structural conformation of PTP1B and glucoside hydrolase may be related to the arrangement of amino acids in protein structure. This reported for the first time that inhibitory effects of curcumins (1–3) against PTP1B and glucoside hydrolase have been examined in vitro and in silico as well.

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Curcumin and Its New Derivatives: Correlation between Cytotoxicity against Breast Cancer Cell Lines, Degradation of PTP1B Phosphatase and ROS Generation

Cited by 15 publications

References 58 publications

Role of Protein Tyrosine Phosphatase 1B Inhibitor in Early Brain Injury of Subarachnoid Hemorrhage in Mice

Role of Protein Tyrosine Phosphatase 1B Inhibitor in Early Brain Injury of Subarachnoid Hemorrhage in Mice

Pyrazole-Curcumin Suppresses Cardiomyocyte Hypertrophy by Disrupting the CDK9/CyclinT1 Complex

Curcumins from <em>Curcuma longa </em>Potential Inhibit PTP1B and α-Glucosidase: Experimental and Computational Study

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