An appraisal of cinnamyl sulfonamide hydroxamate derivatives (HDAC inhibitors) for anti-cancer, anti-angiogenic and anti-metastatic activities in human cancer cells

2016 ◽  
Vol 253 ◽  
pp. 112-124 ◽  
Author(s):  
Neetinkumar D. Reddy ◽  
M.H. Shoja ◽  
Subhankar Biswas ◽  
Pawan G. Nayak ◽  
Nitesh Kumar ◽  
...  
2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Chia-Jung Li ◽  
Shih-Fang Tsang ◽  
Chun-Hao Tsai ◽  
Hsin-Yi Tsai ◽  
Jong-Ho Chyuan ◽  
...  

Plants are an invaluable source of potential new anti-cancer drugs.Momordica charantiais one of these plants with both edible and medical value and reported to exhibit anticancer activity. To explore the potential effectiveness ofMomordica charantia, methanol extract ofMomordica charantia(MCME) was used to evaluate the cytotoxic activity on four human cancer cell lines, Hone-1 nasopharyngeal carcinoma cells, AGS gastric adenocarcinoma cells, HCT-116 colorectal carcinoma cells, and CL1-0 lung adenocarcinoma cells, in this study. MCME showed cytotoxic activity towards all cancer cells tested, with the approximate IC50ranging from 0.25 to 0.35 mg/mL at 24 h. MCME induced cell death was found to be time-dependent in these cells. Apoptosis was demonstrated by DAPI staining and DNA fragmentation analysis using agarose gel electrophoresis. MCME activated caspase-3 and enhanced the cleavage of downstream DFF45 and PARP, subsequently leading to DNA fragmentation and nuclear condensation. The apoptogenic protein, Bax, was increased, whereas Bcl-2 was decreased after treating for 24 h in all cancer cells, indicating the involvement of mitochondrial pathway in MCME-induced cell death. These findings indicate that MCME has cytotoxic effects on human cancer cells and exhibits promising anti-cancer activity by triggering apoptosis through the regulation of caspases and mitochondria.


2016 ◽  
Vol 26 (9) ◽  
pp. 2164-2169 ◽  
Author(s):  
Nikhil R. Madadi ◽  
Amit Ketkar ◽  
Narsimha R. Penthala ◽  
April C.L. Bostian ◽  
Robert L. Eoff ◽  
...  

2021 ◽  
Author(s):  
Jing Song ◽  
Arie Dagan

AbstractCeramide metabolism is a potential target for anti-cancer therapy. Studies show that chemotherapeutic agents can induce apoptosis and it is mediated by ceramide. Synthesized sphingolipid analogs can induce cell death in human lymphocytes and leukemia cells. By screening a group of synthetic sphingolipid analogs, we found that low concentrations of AD2750 and AD2646 induced cell death in human cancer cells by preventing ceramide from converting to sphingomyelin, individually or in combination with commercial cancer drugs. The combination of low concentrations of Taxol and AD2750 or AD2646 significantly increased cell death on human colon cancer cells (HT29). Co-administering low concentrations of Doxorubicin with AD2750 or AD2646 elevated cellular toxicity on human pancreatic cancer cells (CRL1687). This synergistic effect is related to the elevated cellular ceramide. Combining AD2750 or AD2646 with chemotherapy drugs can be used to manipulate ceramide and sphingomyelin metabolism, potentially to affect the growth of human cancer cells and increase the effectiveness of anti-cancer drugs on killing cancer cells.


2020 ◽  
Vol 32 (8) ◽  
pp. 085105
Author(s):  
Nazim Muhammad ◽  
He Zhao ◽  
Wenjing Song ◽  
Mingyang Gu ◽  
Qian Li ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 278 ◽  
Author(s):  
Bu Choi

Apple is a rich source of bioactive phytochemicals that help improve health by preventing and/or curing many disease processes, including cancer. One of the apple polyphenols is phloretin [2′,4′,6′-Trihydroxy-3-(4-hydroxyphenyl)-propiophenone], which has been widely investigated for its antioxidant, anti-inflammatory and anti-cancer activities in a wide array of preclinical studies. The efficacy of phloretin in suppressing xenograft tumor growth in athymic nude mice implanted with a variety of human cancer cells, and the ability of the compound to interfere with cancer cells signaling, have made it a promising candidate for anti-cancer drug development. Mechanistically, phloretin has been reported to arrest the growth of tumor cells by blocking cyclins and cyclin-dependent kinases and induce apoptosis by activating mitochondria-mediated cell death. The blockade of the glycolytic pathway via downregulation of GLUT2 mRNA and proteins, and the inhibition of tumor cells migration, also corroborates the anti-cancer effects of phloretin. This review sheds light on the molecular targets of phloretin as a potential anti-cancer and anti-inflammatory natural agent.


2015 ◽  
Vol 33 (15_suppl) ◽  
pp. e13042-e13042
Author(s):  
Pengfei Jiang ◽  
Rajesh Mukthavaram ◽  
Natsuko Nomura ◽  
Sandeep C. Pingle ◽  
Santosh Kesari

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