Curcumin and Cinnamaldehyde as PTP1B Inhibitors With Antidiabetic and Anticancer Potential

Kostrzewa, Tomasz; Przychodzeń, Paulina; Górska‐Ponikowska, Magdalena; Kuban–Jankowska, Alicja

doi:10.21873/anticanres.13171

Cited by 40 publications

(22 citation statements)

References 25 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The results showed that natural compounds found to inhibit PTP1B were diverse including pterocarpan derivatives, 9,10 diterpenoids and triterpenoids, 11 flavonoids, 12 sesquiterpenoids, 12 coumarins, 12 alkaloids, 12 and phenolic compounds. 13,14 These results encourage us to continue our studies in the discovery of PTP1B inhibitors from natural sources.…”

mentioning

confidence: 81%

“…The 1 H-nuclear magnetic resonance (NMR) spectrum of 1, 2, 3, 5, and 6 displayed characteristic signals due to 5 aromatic protons of 2 benzene rings (rings A and B), together with those of hydroxyl (C-3) and methoxy groups (Figure 1), while their 13 C-NMR spectrum revealed the signals of a ketone (C-4), oxygen-substituted carbons, and 2 quaternary carbons (Figure 1). The 1 H-and 13 C-NMR spectra indicated that these compounds are derivatives of kaempferol (for 1 and 2) and quercetin (for 3, 5, and 6). 39 Detailed analysis of the 1 H-and 13 C-NMR spectra of compound 1 revealed that 1 possessed 1 ketone carbon, 6 oxygenated carbons, and 2 methoxy carbons at C-7 and C-4′.…”

mentioning

confidence: 99%

See 1 more Smart Citation

PTP1B Inhibitory Flavonoids FromOrthosiphon stamineusBenth. and Their Growth Inhibition on Human Breast Cancer Cells

Hoang

Tran

et al. 2020

Natural Product Communications

View full text Add to dashboard Cite

In our preliminary screening study on the protein tyrosine phosphatase 1B (PTP1B) inhibitory and cytotoxic activities, an ethyl acetate soluble fraction of the aerial part of Orthosiphon stamineus Benth. was found to inhibit PTP1B activity. Thus, based on assay-guided isolation of this active fraction, ten compounds (1-10) were purified and evaluated for their inhibitory effects on PTP1B and their growth inhibition on MCF7, tamoxifen-resistant MCF7 (MCF7/TAMR), and MDA-MB-231 human breast cancer cell lines. Among the isolates, compounds 5, 6, 9, and 10 showed potencies against PTP1B with IC50 values of 9.76, 10.12, 6.88, and 8.92 μM, respectively, followed by compounds 1 and 4 with IC50 values of 16.92 and 22.25 μM. Kinetic study showed that the active compounds (1, 5, 9, and 10) possessed mixed-competitive inhibition, which was similar to the positive control (ursolic acid, IC50 value of 3.42 μM, mixed-competitive). The others showed noncompetitive inhibition (4 and 6). In addition, all these active compounds (1, 4-6, and 9-10) displayed growth inhibition on three cancer cell lines, especially the most PTP1B inhibitory flavanones (9 and 10) exhibited comparable inhibitory effects on MCF7, MCF7/TAMR, and MDA-MB-231 cancer cells (IC50 values of 11.5 and 15.4, 8.9 and 10.5, and 17.6 and 21.3 μM, respectively) with tamoxifen, the positive control used in this assay (IC50 values of 11.9, 12.1, and 12.7 μM, respectively). The results suggest that these active constituents from O. stamineus might be considered as new natural compounds for the development of anticancer agents via PTP1B inhibition.

show abstract

mentioning

confidence: 81%

mentioning

confidence: 99%

PTP1B Inhibitory Flavonoids FromOrthosiphon stamineusBenth. and Their Growth Inhibition on Human Breast Cancer Cells

Hoang

Tran

et al. 2020

Natural Product Communications

View full text Add to dashboard Cite

show abstract

“…Curcumin and cinnamaldehyde decreased PTP1B enzymatic activity in breast cancer MCF-7 cell line (139), despite curcumin was more effective than cinnamaldehyde. Briefly, curcumin inhibited PTP1B at concentrations starting from 1 mM (IC 50 ≈ 100 mM) (139). In fructose-fed rats, curcumin ingestion inhibited PTP1B and improved insulin and leptin sensitivity in the liver of rats, also protecting hypertriglyceridemia and hepatic steatosis induced by fructose diet (140).…”

Section: Enhance Insulin Activity Via Protein Tyrosine Phosphatase 1b Inhibitionmentioning

confidence: 99%

Phytochemicals as Potential Epidrugs in Type 2 Diabetes Mellitus

et al. 2021

View full text Add to dashboard Cite

Type 2 diabetes Mellitus (T2DM) prevalence has significantly increased worldwide in recent years due to population age, obesity, and modern sedentary lifestyles. The projections estimate that 439 million people will be diabetic in 2030. T2DM is characterized by an impaired β-pancreatic cell function and insulin secretion, hyperglycemia and insulin resistance, and recently the epigenetic regulation of β-pancreatic cells differentiation has been underlined as being involved. It is currently known that several bioactive molecules, widely abundant in plants used as food or infusions, have a key role in histone modification and DNA methylation, and constituted potential epidrugs candidates against T2DM. In this sense, in this review the epigenetic mechanisms involved in T2DM and protein targets are reviewed, with special focus in studies addressing the potential use of phytochemicals as epidrugs that prevent and/or control T2DM in vivo and in vitro. As main findings, and although some controversial results have been found, bioactive molecules with epigenetic regulatory function, appear to be a potential replacement/complementary therapy of pharmacological hypoglycemic drugs, with minimal side effects. Indeed, natural epidrugs have shown to prevent or delay the T2DM development and the morbidity associated to dysfunction of blood vessels, eyes and kidneys due to sustained hyperglycemia in T2DM patients.

show abstract

“…Curcumin as a phytochemical, has been widely explored for its therapeutic potential through in vitro and in vivo investigations. It has been shown to possess biological activity against a large spectrum of physiological conditions, which include antioxidant [17][18][19][20] , chemo-protective [21][22][23] , antidiabetic [24][25][26] and anti-proliferative activity against cancer cells [27][28][29][30][31] .…”

Section: Introductionmentioning

confidence: 99%

Curcumin: reclaiming the lost ground against cancer resistance

Shaikh¹,

Shaikh²,

Naba³

et al. 2021

CDR

View full text Add to dashboard Cite

Curcumin, a polyphenol, has a wide range of biological properties such as anticancer, antibacterial, antitubercular, cardioprotective and neuroprotective. Moreover, the anti-proliferative activities of Curcumin have been widely studied against several types of cancers due to its ability to target multiple pathways in cancer. Although Curcumin exhibited potent anticancer activity, its clinical use is limited due to its poor water solubility and faster metabolism. Hence, there is an immense interest among researchers to develop potent, water-soluble, and metabolically stable Curcumin analogs for cancer treatment. While drug resistance remains a major problem in cancer therapy that renders current chemotherapy ineffective, curcumin has shown promise to overcome the resistance and resensitize cancer to chemotherapeutic drugs in many studies. In the present review, we are summarizing the role of curcumin in controlling the proliferation of drug-resistant cancers and development of curcumin-based therapeutic applications from cell culture studies up to clinical trials.

show abstract

Curcumin and Cinnamaldehyde as PTP1B Inhibitors With Antidiabetic and Anticancer Potential

Abstract: oxygen species (ROS) production that lead to cancer cell death (24).This study aimed to evaluate the inhibitory effect of curcumin and cinnamaldehyde on the activity of PTP1B phosphatase. The impact of these compounds on breast cancer cell viability was also analyzed.

Cited by 40 publications

References 25 publications

PTP1B Inhibitory Flavonoids FromOrthosiphon stamineusBenth. and Their Growth Inhibition on Human Breast Cancer Cells

PTP1B Inhibitory Flavonoids FromOrthosiphon stamineusBenth. and Their Growth Inhibition on Human Breast Cancer Cells

Phytochemicals as Potential Epidrugs in Type 2 Diabetes Mellitus

Curcumin: reclaiming the lost ground against cancer resistance

Contact Info

Product

Resources

About