Reversal effect of 2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone on multi-drug resistance in resistant human hepatocellular carcinoma cell line BEL-7402/5-FU

Hai-ya, Huang; Niu, Jiang-long; Zhao, Liming; Lü, Yanhua

doi:10.1016/j.phymed.2011.04.001

Cited by 36 publications

(12 citation statements)

References 20 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…For the NO assay, cells were pretreated with DMC for 2 h and then stimulated with LPS (1 μg/mL) for 24 h. The supernatants were collected at the designed time points. NO production was examined via Griess reaction method ( Huang et al ., 2011 ). The amounts of the cytokines in the cell culture supernatants including TNF-α, IL-1β, IL-6, and HMGB1 were respectively measured via ELISA Kits following the manufacture’s specification.…”

Section: Methodsmentioning

confidence: 99%

“…1A ) ( Ye et al ., 2004 ). DMC has many health beneficial effects including hepatoprotective activities ( Yu et al ., 2011 ), anti-tumor ( Ye et al ., 2005a ; Ye et al ., 2005b ), anti-virus ( Dao et al ., 2010 ), anti-microbial ( Salem and Werbovetz, 2005 ), anti-oxidant ( Su et al ., 2011 ; Martinez et al ., 2012 ), anti-diarrheal ( Amor et al ., 2005 ; Ghayur et al ., 2006 ), anti-drug efflux ( Huang et al ., 2011 ; Huang et al ., 2012 ), and anti-diabetic ( Hu et al ., 2012 ; Hu et al ., 2014a ; Hu et al ., 2014b ). However, the anti-inflammatory effects of DMC along with the underlying mechanisms remain unclear.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Dimethyl Cardamonin Exhibits Anti-inflammatory Effects via Interfering with the PI3K-PDK1-PKCα Signaling Pathway

Wan

Yao

et al. 2015

Biomolecules & Therapeutics

Self Cite

View full text Add to dashboard Cite

Consumption of herbal tea [flower buds of Cleistocalyx operculatus (Roxb.) Merr. et Perry (Myrtaceae)] is associated with health beneficial effects against multiple diseases including diabetes, asthma, and inflammatory bowel disease. Emerging evidences have reported that High mobility group box 1 (HMGB1) is considered as a key “late” proinflammatory factor by its unique secretion pattern in aforementioned diseases. Dimethyl cardamonin (2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone, DMC) is a major ingredient of C. operculatus flower buds. In this study, the anti-inflammatory effects of DMC and its underlying molecular mechanisms were investigated on lipopolysaccharide (LPS)-induced macrophages. DMC notably suppressed the mRNA expressions of TNF-α, IL-1β, IL-6, and HMGB1, and also markedly decreased their productions in a time- and dose-dependent manner. Intriguingly, DMC could notably reduce LPS-stimulated HMGB1 secretion and its nucleo-cytoplasmic translocation. Furthermore, DMC dose-dependently inhibited the activation of phosphatidylinositol 3-kinase (PI3K), phosphoinositide-dependent kinase 1 (PDK1), and protein kinase C alpha (PKCα). All these data demonstrated that DMC had anti-inflammatory effects through reducing both early (TNF-α, IL-1β, and IL-6) and late (HMGB1) cytokines expressions via interfering with the PI3K-PDK1-PKCα signaling pathway.

show abstract

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Dimethyl Cardamonin Exhibits Anti-inflammatory Effects via Interfering with the PI3K-PDK1-PKCα Signaling Pathway

Wan

Yao

et al. 2015

Biomolecules & Therapeutics

Self Cite

View full text Add to dashboard Cite

show abstract

“…The compound DMC has been isolated from C. operculatus [7], M. serrata [8], and S. samarangense [9]. DMC possessed hepatoprotective [10], cytoprotective [11], anti-inflammatory [12], antifungal, antibacterial [8], anti-TB [13], antiviral [14], antispasmodic [15], antidiarrhoeal [16], antihyperglycaemic [17], anti-MDR [18, 19], and antiapoptotic effect [20]. DMC has been evaluated for its cytotoxic activity on various human cancer cells including liver cancer (SMMC-7721s), HeLa (SPC-A-1, 95-D, and GBC-SD) [7], colon (SW-480) [9], leukemia (K562) [21], colorectal carcinoma (HCT-116 and LOVO) [22], breast (MDA-MB-453), and ovarian [23] cell lines.…”

Section: Introductionmentioning

confidence: 99%

Isolation, Characterization, Crystal Structure Elucidation, and Anticancer Study of Dimethyl Cardamonin, Isolated from Syzygium campanulatum Korth

Memon

Ismail

Aisha

et al. 2014

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

Syzygium campanulatum Korth is an equatorial, evergreen, aboriginal shrub of Malaysia. Conventionally it has been used as a stomachic. However, in the currently conducted study dimethyl cardamonin or 2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (DMC) was isolated from S. campanulatum Korth, leaf extract. The structural characterization of DMC was carried out by making use of various techniques including UV, IR, NMR spectral followed by LC-MS, and X-ray crystallographic techniques. For determining the purity of compound, highly effective techniques including TLC, HPLC, and melting point were used. The cytotoxicity of DMC and three different extracts of S. campanulatum was evaluated against human colon cancer cell line (HT-29) by three different assays. DMC and ethanolic extract revealed potent and dose-dependent cytotoxic activity on the cancer cell line with IC50 12.6 and 90.1 µg/mL, respectively. Quite astonishingly to our knowledge, this is the very first report on S. campanulatum as being a rich source (3.5%) of DMC, X-ray crystallography, and anticancer activity on human colon cancer cells.

show abstract

“…DMC dose-dependently facilitated the penetration and accumulation of doxorubicin in the tumor and decreased the gene expression of MDR - 1 which encodes for the classical efflux pump P-glycoprotein [ 25 ]. A DMC-induced reversal of the multidrug resistance phenotype has been observed also using multidrug-resistant human hepatocellular carcinoma cells (BEL-7402/5-FU) in vitro and in vivo [ 26 , 27 ]. In this case DMC was found to decrease both the mRNA and protein expressions of MRP1.…”

Section: Anticancer Activitiesmentioning

confidence: 99%

Mechanistic insights into dimethyl cardamonin-mediated pharmacological effects: A double control of the AMPK-HMGB1 signaling axis

Bailly

Vergoten

2020

Life Sciences

View full text Add to dashboard Cite

Dimethyl cardamonin (DMC) has been isolated from diverse plants, notably from Cleistocalyx operculatus . We have reviewed the pharmacological properties of this natural product which displays anti-inflammatory, anti-hyperglycemic and anti-cancer properties. The pharmacological activities essentially derive from the capacity of DMC to interact with the protein targets HMGB1 and AMPK. Upon binding to HMGB1, DMC inhibits the nucleocytoplasmic transfer of the protein and its extracellular secretion, thereby blocking its alarmin function. DMC also binds to the AMP site of AMPK to activate phospho-AMPK and then to trigger downstream signals leading to the anti-inflammatory and anti-hyperglycemic effects. AMPK activation by DMC reinforces inhibition of HMGB1, to further reduce the release of the alarmin protein, likely contributing to the anticancer effects. The characterization of a tight control of DMC over the AMPK-HMGB1 axis not only helps to explain the known activities of DMC but also suggests opportunities to use this chalcone to treat other pathological conditions such as the acute respiratory distress syndrome (which affects patients with COVID-19). DMC structural analogues are also evoked.

show abstract

Reversal effect of 2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone on multi-drug resistance in resistant human hepatocellular carcinoma cell line BEL-7402/5-FU

Cited by 36 publications

References 20 publications

Dimethyl Cardamonin Exhibits Anti-inflammatory Effects via Interfering with the PI3K-PDK1-PKCα Signaling Pathway

Dimethyl Cardamonin Exhibits Anti-inflammatory Effects via Interfering with the PI3K-PDK1-PKCα Signaling Pathway

Isolation, Characterization, Crystal Structure Elucidation, and Anticancer Study of Dimethyl Cardamonin, Isolated from Syzygium campanulatum Korth

Mechanistic insights into dimethyl cardamonin-mediated pharmacological effects: A double control of the AMPK-HMGB1 signaling axis

Contact Info

Product

Resources

About