In Vitro Anti-tumor Effects of Chemically Modified Polysaccharides from Cherokee Rose Fruit

2014 ◽  
Vol 10 (3) ◽  
pp. 473-479 ◽  
Author(s):  
Kai Jun Xiao ◽  
Ling Zhang ◽  
Xiao Hong Liu ◽  
Zhao Mei Wang ◽  
Shang Tian Yang

Abstract Cherokee rose fruit (CRF) is a Chinese traditional herb which has been used in medicine for hundreds of years. The anti-tumor activity of CRF polysaccharides (CRFPs) has not yet been evaluated. To study the in vitro anti-tumor effects of CRFP and its derivatives, native CRFP was isolated from CRF by hot water extraction, and its molecular weight analyzed with gel filtration chromatography was 227,000 Da. Native CRFP was sulfated with ClSO3H-DMF and carboxymethylated with monochloroacetic acid in alkaline aqueous medium. The resulting derivatives were isolated and labeled as SF-CRFP and CM-CRFP, respectively. The in vitro inhibition rates of CRFP and its derivatives for tumor cells SKVO (human ovarian cancer cell), HepG2 (human hepatoma cell), and LoVo (human colon cancer cell) were evaluated, the result showed that native CRFP exhibited no significant inhibition effect on the three tumor cells even at a concentration of 50 μg/ml, but sulfation and carboxymethylation substantially enhanced the anti-tumor activities of CRFP in a dose-dependent way. SF-CRFP at the dose of 50 μg/ml displayed a significant inhibitory effect on SKVO, HepG2, and LoVo, with the viability rates of 33.6%, 44.8%, and 43.2%, respectively. It has a dosage-dependence inhibition on tumor growth in this model, with IC50 for SKVO, HepG 2, and LoVo being 21 μg/ml, 36 μg/ml, and 49 μg/ml, respectively. CM-CRFP showed a specific inhibition on HepG2 with a viability rate of 12.2%, with an IC50 of 17 μg/ml, while it had hardly any anti-tumor effect on SKVO cells. Thus, chemical modifications of CRFPs by sulfation and carboxymethylation effectively improved their anti-tumor properties.

2005 ◽  
Vol 15 (17) ◽  
pp. 3930-3933 ◽  
Author(s):  
Rosaria Ottanà ◽  
Stefania Carotti ◽  
Rosanna Maccari ◽  
Ida Landini ◽  
Giuseppa Chiricosta ◽  
...  

2010 ◽  
Vol 62 (8) ◽  
pp. 1007-1016 ◽  
Author(s):  
Weimin Guo ◽  
Lin Nie ◽  
Dayong Wu ◽  
Mitchell L. Wise ◽  
F. William Collins ◽  
...  

Author(s):  
Longgang Wang ◽  
Jinxiang Guo ◽  
Jin Zhou ◽  
Dongyang Wang ◽  
Xiuwen Kang ◽  
...  

Abstract Background Colon cancer represents one of the leading causes of gastrointestinal tumors in industrialized countries, and its incidence appears to be increasing at an alarming rate. Accumulating evidence has unveiled the contributory roles of cancer stem cells (CSCs) in tumorigenicity, recurrence, and metastases. The functions of NF-kappa B (NF-κB) activation on cancer cell survival, including colon cancer cells have encouraged us to study the role of NF-κB in the maintenance of CSCs in colon cancer. Methods Tumor samples and matched normal samples were obtained from 35 colon cancer cases. CSCs were isolated from human colon cancer cell lines, where the stemness of the cells was evaluated by cell viability, colony-forming, spheroid-forming, invasion, migration, and apoptosis assays. NF-κB activation was then performed in subcutaneous tumor models of CSCs by injecting lipopolysaccharides (LPS) i.p. Results We found that NF-κB activation could reduce the expression of miR-195-5p and miR-497-5p, where these two miRNAs were determined to be downregulated in colon cancer tissues, cultured colon CSCs, and LPS-injected subcutaneous tumor models. Elevation of miR-195-5p and miR-497-5p levels by their specific mimic could ablate the effects of NF-κB on the stemness of colon cancer cells in vivo and in vitro, suggesting that NF-κB could maintain the stemness of colon cancer cells by downregulating miR-195-5p/497–5p. MCM2 was validated as the target gene of miR-195-5p and miR-497-5p in cultured colon CSCs. Overexpression of MCM2 was shown to restore the stemness of colon cancer cells in the presence of miR-195-5p and miR-497-5p, suggesting that miR-195-5p and miR-497-5p could impair the stemness of colon cancer cells by targeting MCM2 in vivo and in vitro. Conclusions Our work demonstrates that the restoration of miR-195-5p and miR-497-5p may be a therapeutic strategy for colon cancer treatment in relation to NF-κB activation.


2019 ◽  
Vol 20 (5) ◽  
pp. 1199 ◽  
Author(s):  
Liviuta Budisan ◽  
Diana Gulei ◽  
Ancuta Jurj ◽  
Cornelia Braicu ◽  
Oana Zanoaga ◽  
...  

Background: Phytochemicals are natural compounds synthesized as secondary metabolites in plants and represent an important source of molecules with therapeutic applications. Attention is accorded to their potential in anti-cancer therapies as single agents or adjuvant treatment. Herby, we evaluated the in vitro effects of a panel of natural compounds with focus on caffeic acid phenethyl ester (CAPE) and Kaempferol for the treatment of human colon cancer. Methods: We exposed two human colon cancer cell lines, RKO and HCT-116, followed by functional examination of cell viability, cell proliferation and invasion, cell cycle, apoptosis, and autophagy. Modifications in gene expression were investigated through microarray and detection of existing mutations and finding of new ones was done with the help of Next Generation Sequencing (NGS). Results: Both CAPE and Kaempferol inhibit cell proliferation, motility and invasion, and stimulate apoptosis and autophagy, concomitant with modifications in coding and noncoding genes’ expression. Moreover, there are pathogenic mutations that are no longer found upon treatment with CAPE and Kaempferol. Conclusions: Our findings indicate that CAPE and Kaempferol have the ability to negatively influence the development and advancement of colon cancer in vitro by specifically altering the cells at the molecular level; this activity can be exploited in possible adjuvant therapies once the optimal dose concentration with minimal side effects but with cancer inhibitory activity is set in vivo.


2001 ◽  
Vol 12 (9) ◽  
pp. 741-751 ◽  
Author(s):  
Sylvie Guichard ◽  
Stéphanie Arnould ◽  
Isabelle Hennebelle ◽  
Roland Bugat ◽  
Pierre Canal

2021 ◽  
Vol 2021 ◽  
pp. 1-5
Author(s):  
Abdulrhman Alsayari ◽  
Yahya I. Asiri ◽  
Abdullatif Bin Muhsinah ◽  
Mohd. Zaheen Hassan

Background. Pyrazoles are an interesting class of compounds showing potent anticancer activities. Our previous studies have demonstrated the potent anticancer activity of pyrazole analogues. Therefore, we focused on developing anticancer agents through structure optimization of the pyrazolyl lead molecule. Methods. The pyrazole derivatives were prepared by the appropriate synthetic protocols. The antiproliferative activities were evaluated using a sulforhodamine B assay against three cancer cell lines. In vitro and in silico molecular docking studies employing xanthine oxidase were used to explore the mechanism by which pyrazole derivatives exert anticancer effects. Results. One of the pyrazole derivatives demonstrated the greatest promise as an anticancer agent against the human colon cancer cell line (IC50 4.2 μM), with a potent xanthine oxidase inhibitory activity (IC50 0.83 μM). Conclusion. In summary, our findings suggest that these pyrazolyl analogues containing a pyridine nucleus could serve as a promising lead molecule in the development of novel anticancer agents.


Sci ◽  
2021 ◽  
Vol 3 (3) ◽  
pp. 31
Author(s):  
Milena Kfoury ◽  
Charbel Mouawad ◽  
Mariam Rifi ◽  
Riyad Sadek ◽  
Jean-Marc Sabatier ◽  
...  

In this work, we pursued the biological characterization of the venom of Montivipera bornmuelleri, a viper from the Lebanese mountains. In relation to its antibacterial potential, the inhibitory effect of this venom on the F1F0-ATPase enzymes of Gram-positive Staphylocoocus epidermidis and Gram-negative Escherichia coli bacteria was examined. In order to determine the degree of cytotoxicity of the venom on the HCT116 human colon cancer cell lines, the biological MTT proliferation and cell viability test were implemented. After validation of the enzymatic F1F0-ATPase model by the spectrophotometric method, using quercetin as the reference ligand, results revealed that M. bornmuelleri venom is able to inhibit the activity of the enzyme of these two bacteria with a concentration of the order of 100–150 µg/mL. In addition, a venom concentration of 10 µg/mL was sufficient to kill the totality of HCT116 cell lines cultivated in vitro. These data show that M. bornmuelleri venom is a mixture of diverse molecules presenting activities of interest, and is a potential source to explore in order to discover new drug candidates.


Sign in / Sign up

Export Citation Format

Share Document