Dehydrozingerone ameliorates thioacetamide-induced liver fibrosis via inhibition of hepatic stellate cells activation through modulation of the MAPK pathway

Sharma, Nidhi; Shaikh, Taslim B.; Eedara, Abhisheik; Kuncha, Madhusudhana; Sistla, Ramakrishna; Andugulapati, Sai Balaji

doi:10.1016/j.ejphar.2022.175366

Cited by 15 publications

(3 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…4T1 cells were cultured and treated with standard (cisplatin) and compound 9h (5 and 10 µM) after 48 h cells were subjected to Western‐blot analysis as described earlier (Sharma et al, 2022). Briefly, cells were harvested using RIPA lysis buffer and a specified amount of (30 µg) of protein was loaded into SDS‐PAGE Bis‐Tris gradient protein gel for electrophoresis and then transferred onto PVDF membrane and blocked with 5% bovine serum albumin followed by incubation with selected primary antibodies (BAX, pACC, AMPKα, and pAMPKα) overnight at 4°C.…”

Section: Experimental Methodsmentioning

confidence: 99%

Glucosyltriazole amphiphile treatment attenuates breast cancer by modulating the AMPK signaling

Chouhan,

Eedara,

Talati

et al. 2024

Drug Development Research

Self Cite

View full text Add to dashboard Cite

Breast cancer is the second most frequent cancer among women. Out of various subtypes, triple‐negative breast cancers (TNBCs) account for 15% of breast cancers and exhibit more aggressive characteristics as well as a worse prognosis due to their proclivity for metastatic progression and limited therapeutic strategies. It has been demonstrated that AMP‐activated protein kinase (AMPK) has context‐specific protumorigenic implications in breast cancer cells. A set of glucosyltriazole amphiphiles, consisting of acetylated (9a‐h) and unmodified sugar hydroxyl groups (10a‐h), were synthesized and subjected to in vitro biological evaluation. Among them, 9h exhibited significant anticancer activity against MDA‐MB‐231, MCF‐7, and 4T1 cell lines with IC50 values of 12.5, 15, and 12.55 μM, respectively. Further, compound 9h was evaluated for apoptosis and cell cycle analysis in in vitro models (using breast cancer cells) and antitumour activity in an in vivo model (orthotopic mouse model using 4T1 cells). Annexin‐V assay results revealed that treatment with 9h caused 34% and 28% cell death at a concentration of 15 or 7.5 μM, respectively, while cell cycle analysis demonstrated that 9h arrested the cells at the G2/M or G1 phase in MCF‐7, MDA‐MB‐231 and 4T1 cells, respectively. Further, in vivo, investigation showed that compound 9h exhibited equipotent as doxorubicin at 7.5 mg/kg, and superior efficacy than doxorubicin at 15 mg/kg. The mechanistic approach revealed that 9h showed potent anticancer activity in an in vivo orthotopic model (4T1 cells) partly by suppressing the AMPK activation. Therefore, modulating the AMPK activation could be a probable approach for targeting breast cancer and mitigating cancer progression.

show abstract

Section: Experimental Methodsmentioning

confidence: 99%

Glucosyltriazole amphiphile treatment attenuates breast cancer by modulating the AMPK signaling

Chouhan,

Eedara,

Talati

et al. 2024

Drug Development Research

Self Cite

View full text Add to dashboard Cite

show abstract

“…The author has cited the additional references within the supporting information. [30][31][32][33][34][35][36][37] After the incubation period, cells were harvested using RIPA lysis buffer and subjected to western blot analysis for specified antibodies (3A). Blots were quantified using ImageJ software and graphs were plotted (3B-3D).…”

Section: Supporting Informationmentioning

confidence: 99%

“…Synthesis protocols, compound characterization, NMR spectra, and Western blot (original blots) are provided in supporting information. The author has cited the additional references within the supporting information [30–37] …”

Section: Supporting Informationmentioning

confidence: 99%

N,N‐Diarylsulfonamide Reduces Proinflammatory Cytokine Interleukin‐6 Levels in Cells through Nuclear Factor‐κB Regulation

Babar,

Khansole,

Kumar Singh

et al. 2024

ChemMedChem

View full text Add to dashboard Cite

The synthesized sulfonamides were evaluated for cytotoxicity followed by the cytokine/inflammatory marker’s inhibition capability and its mechanism of action in RAW‐264.7 cells. Elevated interleukin‐6 (IL‐6) levels have been reported in inflammatory conditions and inflammation‐associated disorders. Hence, reducing the IL‐6 levels in inflammatory conditions can serve as an attractive therapeutic target in dealing the inflammation. Among 42 compounds, seven compounds showed significant inhibition of IL‐6 levels in lipopolysaccharide (LPS) challenged RAW‐264.7 cells at 12.5 µM concentration. Further, investigation revealed that the IC50 value of these compounds for reducing IL‐6 levels was found to be in the range of 9.7 to 2.6 µM. The promising compounds 5y (IC50 of 2.6 µM) and 5n (IC50 of 4.1 µM) along with other derivatives fulfil drug‐likeness parameters laid down by Lipinski’s rule of five. Further, analysis using RTqPCR and Western‐blot analysis revealed that treatment with 5n significantly reduced the expression of pro‐inflammatory, inflammatory and macrophage marker’s expression (IL‐1β, CCL2, COX2 and CD68) compared to LPS control. The mechanistic evaluation showed that RL‐442 exhibited anti‐inflammatory properties by modulating the nuclear factor‐κB (NF‐κB) activation. The identified compound can be a promising candidate for further discovery efforts to generate a preclinical candidate effective in inflammation.

show abstract

Sinigrin Attenuates the Dextran Sulfate Sodium-induced Colitis in Mice by Modulating the MAPK Pathway

et al. 2023

View full text Add to dashboard Cite

Dehydrozingerone ameliorates thioacetamide-induced liver fibrosis via inhibition of hepatic stellate cells activation through modulation of the MAPK pathway

Cited by 15 publications

References 33 publications

Glucosyltriazole amphiphile treatment attenuates breast cancer by modulating the AMPK signaling

Glucosyltriazole amphiphile treatment attenuates breast cancer by modulating the AMPK signaling

N,N‐Diarylsulfonamide Reduces Proinflammatory Cytokine Interleukin‐6 Levels in Cells through Nuclear Factor‐κB Regulation

Sinigrin Attenuates the Dextran Sulfate Sodium-induced Colitis in Mice by Modulating the MAPK Pathway

Contact Info

Product

Resources

About