scholarly journals Synthesis and Anticancer Activity of Dimeric Polyether Ionophores

Biomolecules ◽  
2020 ◽  
Vol 10 (7) ◽  
pp. 1039
Author(s):  
Michał Sulik ◽  
Ewa Maj ◽  
Joanna Wietrzyk ◽  
Adam Huczyński ◽  
Michał Antoszczak
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Parent Compound ◽  
Colon Adenocarcinoma ◽  
Cancer Cell Line ◽  
Functional Evaluation ◽  
Selective Targeting ◽  
Synthetic Approaches

Polyether ionophores represent a group of natural lipid-soluble biomolecules with a broad spectrum of bioactivity, ranging from antibacterial to anticancer activity. Three seem to be particularly interesting in this context, namely lasalocid acid, monensin, and salinomycin, as they are able to selectively target cancer cells of various origin including cancer stem cells. Due to their potent biological activity and abundant availability, some research groups around the world have successfully followed semi-synthetic approaches to generate original derivatives of ionophores. However, a definitely less explored avenue is the synthesis and functional evaluation of their multivalent structures. Thus, in this paper, we describe the synthetic access to a series of original homo- and heterodimers of polyether ionophores, in which (i) two salinomycin molecules are joined through triazole linkers, or (ii) salinomycin is combined with lasalocid acid, monensin, or betulinic acid partners to form ‘mixed’ dimeric structures. Of note, all 11 products were tested in vitro for their antiproliferative activity against a panel of six cancer cell lines including the doxorubicin resistant colon adenocarcinoma LoVo/DX cell line; five dimers (14–15, 17–18 and 22) were identified to be more potent than the reference agents (i.e., both parent compound(s) and commonly used cytostatic drugs) in selective targeting of various types of cancer. Dimers 16 and 21 were also found to effectively overcome the resistance of the LoVo/DX cancer cell line.

Evaluation of in vitro Antioxidant and Anticancer Activity of Simarouba glauca Leaf Extracts on T-24 Bladder Cancer Cell Line

2017 ◽  
Vol 9 (6) ◽  
pp. 906-912 ◽  
Author(s):  
Sridevi I. Puranik ◽  
Shridhar C. Ghagane ◽  
Rajendra B. Nerli ◽  
Sunil S. Jalalpure ◽  
Murigendra B. Hiremath
Keyword(s):  
Bladder Cancer ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Bladder Cancer Cell ◽  
Bladder Cancer Cell Line ◽  
Leaf Extracts ◽  
Simarouba Glauca

scholarly journals PHYTOCHEMICAL ANALYSIS, LIQUID CHROMATOGRAPHY, AND MASS SPECTROSCOPY AND IN VITRO ANTICANCER ACTIVITY OF ANNONA SQUAMOSA SEEDS LINN.

2018 ◽  
Vol 11 (3) ◽  
pp. 101
Author(s):  
Shuchi Dave Mehta ◽  
Sarvesh Paliwal
Keyword(s):  
Liquid Chromatography ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Mass Spectroscopy ◽  
Cancer Cell Line ◽  
Phytochemical Analysis ◽  
Annona Squamosa

 Objective: The objective of the present study is to evaluate in vitro anticancer property and phytochemical analysis using liquid chromatography and mass spectroscopy (LCMS) method of hydroalcoholic extract of seeds of Annona squamosa (AS) Linn. Seeds of AS Linn. are traditional medicine treating various diseases and have shown anticancer activity. Due to lack of survival benefit, cancer is a deadly global disease.Method: The anticancer activity was evaluated using the sulforhodamine B assay method on five cancer cell lines: Breast cancer cell line, cervix cancer cell line (SiHa), colon cancer cell line (HT)-29, liver cancer cell line, and ovary cancer cell line (Ovcar). The phytochemical analysis was performed using LCMS method.Result: The phytochemical characterization was done using LCMS method which showed 15 different molecular weight compounds. The extract showed an average in vitro anticancer activity at a concentration of 100 μg/ml against all cancer cell lines. The best activity was observed against Ovcar-5 cell line (69.72) and was also significant against HT and SiHa cell lines.Conclusion: The phytochemical analysis showed the wide range of phenols and flavonoid which are showing potent anticancer activity of AS seeds.

scholarly journals Cytotoxicity and Antiproliferation of Phycocyanin from Spirulina platensis Extract on WiDr Colon Cancer Cell Line

2020 ◽  
Vol 12 (1) ◽  
pp. 42-49 ◽  
Author(s):  
Ajeng Kurniasari Putri ◽  
Safira Chairani Dimarti ◽  
Renni Yuniati ◽  
Neni Susilaningsih
Keyword(s):  
Colon Cancer ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Spirulina Platensis ◽  
Cancer Cell Line ◽  
Colon Cancer Cell Line ◽  
Colon Cancer Cell ◽  
Inhibition Of Proliferation

Phycocyanin from Spirulina platensis extract has anticancer activity against various types of cancer cell cultures. However study about its effect on colon cancer cell lines, especially the WiDr, has not been reported before. This study aimed to reveal the anticancer activity of phycocyanin from Spirulina platensis extract on WiDr cells. The research was an in vitro experimental study, with the investigation on cytotoxicity also antiproliferation as the anticancer parameters. Both cytotoxicity and antiproliferation test was conducted through MTT assay to observe the visualization and inhibition of proliferation of different concentrations of phycocyanin in several incubation times on the WiDr colon cancer cell line. The obtained data were then processed statistically with the Two Way ANOVA test at a significance value of p <0.05 and followed with the Post Hoc test since there were significant differences. Based on the results, it could be postulated that phycocyanin extracted from freshwater Spirulina platensis was classified as non-toxic (IC50 of 855 µg/ml). Consequently, it is less potential to be used as the treatment for colon cancer. However, phycocyanin could inhibit the proliferation of the WiDr cell for approximately 47.4%, specifically at the concentration of 1710 µg/ml for 72 hours. It could be concluded that freshwater phycocyanin is less effective as an anticancer substance. The benefit of this study is to provide the new scientific evidence of the contrary results of freshwater phycocyanin activity from Spirulina platensis as an anticancer agent of colon cancer.

scholarly journals In vitro Anticancer Activity of Marine Sponges Against T47D and HeLa Cell Lines

2020 ◽  
Vol 19 (1) ◽  
pp. 25-28
Author(s):  
Suciati ◽  
Lusiana Arifianti
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Marine Sponges ◽  
Hela Cell Lines

Marine sponges have been known as the source of natural products. Various metabolites with potent bioactivities have been reported from this organism. The current study aims to investigate the anticancer potency of three marine sponges namely Diacarnus debeauforti, Haliclona amboinensis and Agelas cavernosa collected from Barrang Lompo Island, South Sulawesi, Indonesia. The ethyl acetate extracts of the sponges were screened against T47D breast cancer cells and HeLa cervical cancer cells by using the MTT method. The results showed that these sponges demonstrated anticancer activity against both cancer cell lines. The lowest IC50 of 18.2 μg/ml was given by the extract of A. cavernosa against T47D cell line, while in the screening against HeLa cancer cell line, the extract of D. debeauforti revealed the highest potency with IC50 of 15.7 μg/ml. Our results suggested that the marine sponges namely D. debeauforti, H. amboinensis and A. cavernosa can be good candidates for the development of anticancer agents. Dhaka Univ. J. Pharm. Sci. 19(1): 25-28, 2020 (June)

scholarly journals Evaluation of In-vitro Anticancer Activity and Quantitation of Active Ingredient of Adansonia digitata L. Fruit

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sandeep Dilip Kadam ◽  
M S Kondawar
Keyword(s):  
Liver Cancer ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Active Principle ◽  
Liver Cancer Cell ◽  
Hep G2 ◽  
Adansonia Digitata

In the world cancer is the major cause of death. Adansonia digitata L is commonly called as baobab belongs to Family Bombacaceae. Due to the high cost and toxic side effects like Bone marrow suppression, hepatotoxicity, nephrotoxicity, Immunosuppression, teratogenicity etc. of chemotherapeutic agents. So, for the proper controlling on cancer the trends of people are moving towards natural therapies. In light to above, in present research A. digitata L is selected for evaluation of in-vitro anticancer activity based on its reported phytoconstituents of fruit and quantitation of active principle of it. The extracts of fruit pulp, seed, and its combination were obtained using solvents like water, ethanol and n-hexane by maceration technique (Aqueous) and Soxhlet extraction method (organic). This extracts were used for further research possesses phytochemical constituents like Carbohydrates, tannins, Saponins, vitamins, alkaloids, terpenoids, phenol, glycoside flavonoids, steroids, etc. in-vitro antioxidant activity were evaluated via free scavenging assay by using DPPH assay method. Further in-vitro anticancer activity was evaluated against three human cancer cell lines MCF-7 (breast cancer cell line), Hep-G2 (liver cancer cell line) and COLO-205 (colon cancer cell line) using Brine Shrimp Lethality Assay (BSLA), Tryphan Blue Dye Cell Exclusion Assay (TBDCEA) and MTT assay. The quantitation of active ingredients Vit. C and Squalene from extracts was done by using titration method and HPLC method respectively. Formulation possesses highest percent antioxidant capacity (49.36). In BSLA formulation possesses highest rate of percent mortality than other extracts. In TBCE assay and in MTT assay formulation gives more significant effect in Hep-G2 liver cancer cell line than remaining cell lines. These findings introduce A. digitata L as potentially useful as anti-cancer agent. Further research is required to elucidate its specific mechanism of action and exact active principle responsible for action.

New Platinum (II) Ternary Complexes of Formamidine and Pyrophosphate: Synthesis, Characterization and DFT Calculations and In vitro Cytotoxicity

2020 ◽  
Vol 23 (7) ◽  
pp. 611-623
Author(s):  
Ahmed A. Soliman ◽  
Fawzy A. Attaby ◽  
Othman I. Alajrawy ◽  
Azza A.A. Abou-hussein ◽  
Wolfgang Linert
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Theoretical Calculations ◽  
Thermal Analyses ◽  
Cancer Cell Line ◽  
Cellular Growth ◽  
Planar Geometry ◽  
Square Planar ◽  
Vis Spectroscopy

Aim and Objective: Platinum (II) and platinum (IV) of pyrophosphate complexes have been prepared and characterized to discover their potential as antitumor drugs. This study was conducted to prepare and characterize new ternary platinum (II) complexes with formamidine and pyrophosphate as an antitumor candidate. Materials and Methods: The complexes have been characterized by mass, infrared, UV-Vis. spectroscopy, elemental analysis, magnetic susceptibility, thermal analyses, and theoretical calculations. They have been tested for their cytotoxicity, which was carried out using the fastcolorimetric assay for cellular growth and survival against MCF-7 (breast cancer cell line), HCT- 116 (colon carcinoma cell line), and HepG-2 (hepatocellular cancer cell line). Results: All complexes are diamagnetic, and the electronic spectral data displayed the bands due to square planar Pt(II) complexes. The optimized complexes structures (1-4) indicated a distorted square planar geometry where O-Pt-O and N-Pt-N bond angles were 82.04°-96.44°, respectively. Conclusion: The complexes showed noticeable cytotoxicity and are considered as promising antitumor candidates for further applications.

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