scholarly journals Tumor-growth Inhibitory Activity of the Terpene Compound Isolated from Buna-shimeji Mushroom

2006 ◽  
Vol 53 (1) ◽  
pp. 55-61 ◽  
Author(s):  
Shigetoshi Mizutani ◽  
Takashi Kawai ◽  
Tatsuji Enoki ◽  
Hiroaki Sagawa ◽  
Kazuo Shimanaka ◽  
...  
Keyword(s):  
Tumor Growth ◽  
Inhibitory Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity

scholarly journals Synthesis of Novel Shikonin Derivatives and Pharmacological Effects of Cyclopropylacetylshikonin on Melanoma Cells

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2820 ◽  
Author(s):  
Christin Durchschein ◽  
Antje Hufner ◽  
Beate Rinner ◽  
Alexander Stallinger ◽  
Alexander Deutsch ◽  
...  
Keyword(s):  
Tumor Growth ◽  
Cell Lines ◽  
Melanoma Cell ◽  
Inhibitory Activity ◽  
Melanoma Cells ◽  
Dna Breaks ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Shikonin Derivatives ◽  
Melanoma Cell Lines

Despite much research in the last centuries, treatment of malignant melanoma is still challenging because of its mostly unnoticeable metastatic spreading and aggressive growth rate. Therefore, the discovery of novel drug leads is an important goal. In a previous study, we have isolated several shikonin derivatives from the roots of Onosma paniculata Bureau & Franchet (Boraginaceae) which evolved as promising anticancer candidates. β,β-Dimethylacrylshikonin (1) was the most cytotoxic derivative and exhibited strong tumor growth inhibitory activity, in particular, towards melanoma cells. In this study, we synthesized eighteen novel shikonin derivatives in order to obtain compounds which exhibit a higher cytotoxicity than 1. We investigated their cytotoxic potential against various melanoma cell lines and juvenile skin fibroblasts. The most active compound was (R)-1-(1,4-dihydro-5,8-dihydroxy-1,4-dioxonaphthalen-2-yl)-4-methylpent-3-enyl cyclopropylacetate (cyclopropylacetylshikonin) (6). It revealed significant stronger tumor growth inhibitory activity towards two melanoma cell lines derived from metastatic lesions (WM164 and MUG-Mel2). Further investigations have shown that 6 induced apoptosis caspase-dependently, increased the protein levels of cleaved PARP, and led to double-stranded DNA breaks as shown by phosphorylation of H2AX. Cell membrane damage and cell cycle arrest were not observed.

Total Synthesis of Murisolins and Evaluation of Tumor-Growth Inhibitory Activity

2005 ◽  
Vol 11 (21) ◽  
pp. 6237-6245 ◽  
Author(s):  
Naoyoshi Maezaki ◽  
Hiroaki Tominaga ◽  
Naoto Kojima ◽  
Minori Yanai ◽  
Daisuke Urabe ◽  
...  
Keyword(s):  
Tumor Growth ◽  
Total Synthesis ◽  
Inhibitory Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity

scholarly journals Enterohepatic recirculation of bioactive ginger phytochemicals is associated with enhanced tumor growth-inhibitory activity of ginger extract

2014 ◽  
Vol 35 (6) ◽  
pp. 1320-1329 ◽  
Author(s):  
Sushma R. Gundala ◽  
Rao Mukkavilli ◽  
Chunhua Yang ◽  
Pooja Yadav ◽  
Vibha Tandon ◽  
...  
Keyword(s):  
Tumor Growth ◽  
Inhibitory Activity ◽  
Enterohepatic Recirculation ◽  
Ginger Extract ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity

Total Synthesis of Murisolins and Evaluation of Tumor-Growth Inhibitory Activity.

ChemInform ◽  
2006 ◽  
Vol 37 (15) ◽  
Author(s):  
Naoyoshi Maezaki ◽  
Hiroaki Tominaga ◽  
Naoto Kojima ◽  
Minori Yanai ◽  
Daisuke Urabe ◽  
...  
Keyword(s):  
Tumor Growth ◽  
Total Synthesis ◽  
Inhibitory Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity

scholarly journals Modifications on the Tetrahydroquinoline Scaffold Targeting a Phenylalanine Cluster on GPER as Antiproliferative Compounds against Renal, Liver and Pancreatic Cancer Cells

2021 ◽  
Vol 14 (1) ◽  
pp. 49
Author(s):  
David Méndez-Luna ◽  
Loreley Araceli Morelos-Garnica ◽  
Juan Benjamín García-Vázquez ◽  
Martiniano Bello ◽  
Itzia Irene Padilla-Martínez ◽  
...  
Keyword(s):  
Binding Site ◽  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
In Silico ◽  
Cancer Cell Lines ◽  
Pancreatic Cancer Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
New Compounds

The implementation of chemo- and bioinformatics tools is a crucial step in the design of structure-based drugs, enabling the identification of more specific and effective molecules against cancer without side effects. In this study, three new compounds were designed and synthesized with suitable absorption, distribution, metabolism, excretion and toxicity (ADME-tox) properties and high affinity for the G protein-coupled estrogen receptor (GPER) binding site by in silico methods, which correlated with the growth inhibitory activity tested in a cluster of cancer cell lines. Docking and molecular dynamics (MD) simulations accompanied by a molecular mechanics/generalized Born surface area (MMGBSA) approach yielded the binding modes and energetic features of the proposed compounds on GPER. These in silico studies showed that the compounds reached the GPER binding site, establishing interactions with a phenylalanine cluster (F206, F208 and F278) required for GPER molecular recognition of its agonist and antagonist ligands. Finally, a 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyltetrazolium bromide (MTT) assay showed growth inhibitory activity of compounds 4, 5 and 7 in three different cancer cell lines—MIA Paca-2, RCC4-VA and Hep G2—at micromolar concentrations. These new molecules with specific chemical modifications of the GPER pharmacophore open up the possibility of generating new compounds capable of reaching the GPER binding site with potential growth inhibitory activities against nonconventional GPER cell models.

Indole-3-carbinol inhibits the proliferation of colorectal carcinoma LoVo cells through activation of the apoptotic signaling pathway

2021 ◽  
pp. 096032712110214
Author(s):  
JY Lee ◽  
HM Lim ◽  
CM Lee ◽  
S-H Park ◽  
MJ Nam
Keyword(s):  
Colorectal Carcinoma ◽  
Cancer Cells ◽  
Inhibitory Activity ◽  
Annexin V ◽  
Fluorescein Isothiocyanate ◽  
Cell Counting ◽  
Terminal Deoxynucleotidyl Transferase ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Lovo Cells

Indole-3-carbinol (I3C) is a phytochemical that exhibits growth-inhibitory activity against various cancer cells. However, there are limited studies on the effects of I3C on colon cancer cells. In this study, the growth-inhibitory activity of I3C against the human colorectal carcinoma cell line (LoVo) was examined. The results of the 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide, colony formation, and cell counting assays revealed that I3C suppressed the proliferation of LoVo cells. Microscopy and wound-healing analyses revealed that I3C affected the morphology and inhibited the migration of LoVo cells, respectively. I3C induced apoptosis and DNA fragmentation as evidenced by the results of fluorescein isothiocyanate-conjugated annexin V staining and terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick-end labeling assay, respectively. Additionally, I3C arrested the cell cycle at the G0/G1 phase and enhanced the reactive oxygen species levels. Western blotting analysis revealed that treatment with I3C resulted in the activation of apoptotic proteins, such as poly(ADP-ribose) polymerase, caspase-3, caspase-7, caspase-9, Bax, Bim, and p53 in LoVo cells. These results indicate that I3C induces apoptosis in LoVo cells by upregulating p53, leading to the activation of Bax and caspases. Taken together, I3C exerts cytotoxic effects on LoVo cells by activating apoptosis.

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