scholarly journals Chemical Characterization and Cytotoxic Activity of Antarctic Macroalgae Extracts against Colorectal Cancer

2019 ◽  
Vol 09 (05) ◽  
pp. 167-177
Author(s):  
Rafaele Frassini ◽  
Yeslei Paulino da Silva ◽  
Sidnei Moura ◽  
Leonardo Zambotti Villela ◽  
Aline Paternostro Martins ◽  
...  

2017 ◽  
Vol 95 ◽  
pp. 298-307 ◽  
Author(s):  
Hiba Noureddine ◽  
Rouba Hage-Sleiman ◽  
Batoul Wehbi ◽  
Hussein Fayyad-Kazan ◽  
Salem Hayar ◽  
...  


2016 ◽  
Vol 36 (10) ◽  
pp. 1059-1070 ◽  
Author(s):  
MBO Chagas ◽  
NCC Cordeiro ◽  
KMR Marques ◽  
MG Rocha Pitta ◽  
MJBM Rêgo ◽  
...  

A series of new thiazacridine agents were synthesized and evaluated as antitumor agents, in terms of not only their cytotoxicity but also their selectivity. The cytotoxicity assay confirmed that all compounds showed cytotoxic activity and selectivity. The new compound, 3-acridin-9-ylmethyl-5-(5-bromo-1 H-indol-3-ylmethylene)-thiazolidine-2,4-dione (LPSF/AA29 – 7a), proved to be the most promising compound as it presents lower half-maximal inhibitory concentration (IC50) values (ranging from 0.25 to 68.03 µM) depending on cell lineage. In HepG2 cells, the lowest IC50 value was exhibited by 3-acridin-9-ylmethyl-5-(4-piperidin-1-yl-benzylidene)-thiazolidine-2,4-dione (LPSF/AA36 – 7b; 46.95 µM). None of the synthesized compounds showed cytotoxic activity against normal cells (IC50 > 100 µM). The mechanism of death induction and cell cycle effects was also evaluated. Flow cytometric analysis revealed that the compounds LPSF/AA29 – 7a and LPSF/AA36 – 7b significantly increased the percentage of apoptotic cells and induced G2/M arrest in the cell cycle progression. Therefore, these new thiazacridine derivatives constitute promising antitumor agents whose cytotoxicity and selectivity properties indicate they have potential to contribute to or serve as a basis for the development of new cancer drugs in the future.



Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4984
Author(s):  
Didi Nurhadi Illian ◽  
Ihsanul Hafiz ◽  
Okpri Meila ◽  
Ahmad Rusdan Handoyo Utomo ◽  
Arif Nuryawan ◽  
...  

In 2020, an estimated 19.3 million new cancer cases and nearly 10 million cancer deaths have occurred worldwide, with colorectal cancer ranking as the third most frequently diagnosed (10.0%). Several attempts have been conducted against cancer, including surgery, radiation, monoclonal antibodies, and chemotherapy. Many people choose natural products as alternatives against cancer. These products will not only help in human life preservation but also work as a source of up-to-date information, leading people away from incorrect information. We discuss the current status, distribution, and future implications of protecting populations with natural products as an alternative against colorectal cancer in Indonesia. Thirty-eight studies were included in this review for data extraction. The distribution of natural products in Indonesia that have potential activity against colorectal cancer cells was predominated by terpenoids, followed by phytosterols, phenolics, alkaloids, and polyisoprenoids. The type of cell line utilized in the cytotoxic activity analysis of natural products was the WiDr cell line, followed by HT-29 cells and HCT-116 cells. This review showed that MTT in vitro assay is a general method used to analyze the cytotoxic activity of a natural product against colorectal cancer cells, followed by other in vitro and in vivo methods. The systematic review provided predictions for several secondary metabolites to be utilized as an alternative treatment against colorectal cancer in Indonesia. It also might be a candidate for a future co-chemotherapy agent in safety, quality, and standardization. In addition, computational methods are being developed to predict the drug-likeness of compounds, thus, drug discovery is already on the road towards electronic research and development.



2019 ◽  
Vol 12 (1) ◽  
pp. 34 ◽  
Author(s):  
Ana Ferreira Farias ◽  
Alex Lobato Rodrigues ◽  
Rosany Lopes Martins ◽  
Érica de Menezes Rabelo ◽  
Carlos Ferreira Farias ◽  
...  

The present study aimed to evaluate the chemical composition, antioxidant potential, and the cytotoxic and antimicrobial activity of the essential oil of the plant species Tithonia diversifolia (Hemsl) A. Gray. The essential oil obtained was used to identify the chemical compounds present through the techniques of GC-MS and NMR. The antioxidant potential was calculated by the sequestration method of 2,2-diphenyl-1-picrylhydrazyl. For cytotoxic activity, the larval mortality of Artemia salina was evaluated. The main chemical constituents identified are αpinene (9.9%), Limonene (5.40%), (Z)-β-ocimene (4.02%), p-cymen-8-ol (3.0%), Piperitone (11.72%), (E)-nerolidol (3.78%) and Spathulenol (10.8%). In the evaluation of the antimicrobial activity, bacterial strains of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa were used. The results showed that the bacterium E. coli were more susceptible to the presence of the essential oil, presenting minimal inhibitory concentration at the concentrations that were exposed. The essential oil presented antioxidant activity of 54.6% at the concentration of 5 mg·mL−1 and provided a CI50 of 4.30. It was observed that the essential oil of this species was highly toxic against A. salina lavas, as its cytotoxic activity showed an LC50 of 3.11. Thus, it is concluded that T. diversifolia oils are effective in inhibiting bacterial growth and reducing oxidative stress.



2020 ◽  
Vol 13 (6) ◽  
pp. 125
Author(s):  
Joana Coelho ◽  
Lillian Barros ◽  
Maria Inês Dias ◽  
Tiane C. Finimundy ◽  
Joana S. Amaral ◽  
...  

Echinacea purpurea (L.) Moench is widely known for its medicinal properties, being one of the most used medicinal plants for its immunostimulant properties. Nevertheless, there is still scarce information on its cytotoxic activity. Thus, this study aims at evaluating the cytotoxicity and antimicrobial activity of several aqueous and organic extracts of the aerial parts of this plant and chemically characterizing the obtained extracts. The analysis was performed by HPLC–DAD–ESI/MS. Fifteen compounds were identified; of these, seven were phenolic acids and eight were flavonoids. Non-polar compounds were evaluated by GC/MS, with a total of sixty-four compounds identified, and the most abundant groups were the sterols, fatty acids and long-chain hydrocarbons. The highest antimicrobial activity was exhibited by the dichloromethane, ethyl acetate, and acetone extracts. Dichloromethane and n-hexane extracts showed the highest cytotoxic activity. Therefore, they were fractionated, and the obtained fractions were also assessed for their cytotoxicity. Notwithstanding, the cytotoxicity of the extracts was superior to that of the obtained fractions, evidencing a possible synergistic effect of different compounds in the whole extracts.



2016 ◽  
Vol 81 (8) ◽  
pp. H2076-H2084 ◽  
Author(s):  
Giovana Massarotto ◽  
Thiago Barcellos ◽  
Charlene Silvestrin Celi Garcia ◽  
Ana Paula Carneiro Brandalize ◽  
Sidnei Moura ◽  
...  


2017 ◽  
Vol 44 (3) ◽  
pp. 1038-1050 ◽  
Author(s):  
Lin Wang ◽  
Yingfeng Wei ◽  
Weijia Fang ◽  
Chong Lu ◽  
Jianing Chen ◽  
...  

Background/Aims: Cetuximab is a chimeric IgG1 monoclonal antibody which targets the extracellular domain of epidermal growth factor receptor. This antibody is widely used for colorectal cancer (CRC) treatment but its influence on the immune system is incompletely understood. Methods: The immune influence of cetuximab therapy in CRC patients was investigated by analyzing peripheral blood mononuclear cells using flow cytometry. We undertook in vitro cytotoxicity and cytokine-profile assays to ascertain the immunomodulatory effect of cetuximab treatment. Results: The number of CD3+ T, CD8+ T, and natural killer (NK) cells was increased significantly and T-regulatory cells reduced gradually after cetuximab treatment. Percentage of CD4+ T, natural killer T (NKT)-like, invariant NKT, and dendritic cells was similar between baseline patients and cetuximab patients. Expression of CD137 on NK and CD8+ T cells was increased significantly after 4 weeks of cetuximab therapy. In vitro cetuximab treatment markedly increased expression of CD137 and CD107a on NK and CD8+ T cells. Cetuximab treatment promoted the cytotoxic activity of NK and CD8+ T cells against tumor cells. Conclusion: Cetuximab treatment promotes activation of the immune response but alleviates immunosuppression: this might be the underlying anti-CRC effect of cetuximab.



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