Key considerations when using the sulforhodamine B assay for screening novel anticancer agents

Rhodanine and its derivatives are not only valued for their interesting chemical properties but also present a wide range of bioactivities and their chemical and pharmacological applications have been investigated. From 3-methyl-4-thiorhodanine we synthesized S-acylated and C-acylated products using (some) carboxylic acid chlorides and the obtained products were studied the anti-proliferative activity by a SRB (sulforhodamine B) assay against a human breast cancer cell line. The results showed that C-acylated products are better inhibitors than S-acylated products.

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In vitro Photoprotective Evaluation and Development of Novel Nanoemulsion with Chromone Derivative

Journal of the Brazilian Chemical Society ◽

10.21577/0103-5053.20210072 ◽

2021 ◽

Author(s):

Amanda Antunes ◽

Ana Paula Gouveia ◽

Gabriela Diogo ◽

Jason Taylor ◽

Lucas Sousa ◽

...

Keyword(s):

High Resolution Mass Spectrometry ◽

Human Fibroblasts ◽

Protection Factor ◽

Chromone Derivatives ◽

In Vivo Assays ◽

Sulforhodamine B ◽

Sulforhodamine B Assay ◽

Excellent Stability

Chromone derivatives exhibiting high absorbance values in the UVA/UVB region were synthesized, and their photoprotective properties were evaluated. Chromones were prepared according to known literature procedures and characterized by high resolution mass spectrometry, infrared (IR) and nuclear magnetic resonance (NMR) spectroscopy. The in vitro solar protection factor (SPF) was determined by the Mansur method and cytotoxicity was evaluated using the sulforhodamine B assay. Two of the chromones synthesized demonstrated suitable SPF values and displayed no cytotoxic effect towards MRC-5 human fibroblasts at the tested concentrations, indicating great potential for future in vivo assays and clinical trials. Finally, the lead compound was incorporated into a nanoemulsion. Nanoemulsions showed high droplet size homogeneity and excellent stability. Chromones bearing methoxy substituents were found to be the most promising compounds with ideal photoprotective properties desirable for utilization and incorporation in sunscreen formulations.

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Fluoroquinolones as a potentially novel class of antidiabesity and antiproliferative compounds: synthesis and docking studies

Canadian Journal of Chemistry ◽

10.1139/cjc-2020-0162 ◽

2020 ◽

Vol 98 (10) ◽

pp. 635-645

Author(s):

Violet Kasabri ◽

Shereen Arabiyat ◽

Yusuf Al-Hiari ◽

Hiba Zalloum ◽

Jehad Almaliti ◽

...

Keyword(s):

Docking Studies ◽

Obesity Management ◽

Periodontal Ligament Fibroblasts ◽

Triacylglycerol Lipase ◽

Sulforhodamine B ◽

Putative Target ◽

Sulforhodamine B Assay ◽

Colorectal Cancer Cell Lines

Intense efforts by the pharmaceutical industry have been made to identify new targets for obesity diabetes (diabesity). Pancreatic triacylglycerol lipase (PL) inhibition is an interesting putative target for obesity management. Fluoroquinolones (FQs) have been identified as potent inhibitors of PL. The aim of this research was to synthesize novel FQs and evaluate their in vitro antilipolytic and antiproliferative properties. Characterization of the synthesized FQs was carried out with NMR, MS, IR, and EA. Like orlistat, potential FQs’ modulation of PL was quantified colorimetrically (n = 3) and was further supported by docking studies. Compared with cisplatin, FQs’ antiproliferative propensities against a panel of obesity related colorectal cancer cell lines were investigated with Sulforhodamine B assay. Twelve novel FQs (2A–5A, 2B–5B, and 2C–5C) were synthesized and characterized. The PL-IC50 values of tested FQs were in the range of 6.8–165.7 μmol/L. FQ 4A was the most active antiproliferative compound against HCT116 with an IC50 value of 3.5 μmol/L. Their selectivity of growth inhibition for safety examination using normal periodontal ligament fibroblasts (PDL) in comparison with cisplatin’s lack of differential cytotoxicity was reported. Lipophilicity and hydrogen bonding were found essential for both activities. Conclusively, FQs are robustly proven for their emerging in vitro anti-obesity and antiproliferative activities.

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Synthesis, Characterization, Antimicrobial and Anticancer Studies of Metal Complexes of 2-methoxy-4-((3-methylpyridin-2-ylimino)methyl)phenol

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557520666200505124125 ◽

2020 ◽

Vol 20 (13) ◽

pp. 1311-1317

Author(s):

Akanksha Mishra ◽

Sumit Tahlan ◽

Kalavathy Ramasamy ◽

Siong Meng Lim ◽

Syed Adnan Ali Shah ◽

...

Keyword(s):

Schiff Base ◽

Metal Complexes ◽

Cell Line ◽

Copper Complex ◽

Hct116 Cell ◽

Analytical Data ◽

Cancer Cell Line ◽

Salmonella Typhi ◽

Sulforhodamine B ◽

Sulforhodamine B Assay

Background: Being derived from primary amine and aromatic aldehyde, Schiff base and their complexes have an imperative role in the improvement of inorganic chemistry, which are broadly studied as coordination compounds and are gradually becoming more important in biochemical and analytical applications. Methods: They have also been used for antibacterial, antifungal, anticancer, antitubercular activities. Novel synthesised Schiff’s base 2-methoxy-4-((3-methylpyridin-2-ylimino)methyl)phenol (SB) and its metal complexes (Zn[II], Cu[II], Co[II] and Ni[II]) were characterised by UV, IR and NMR spectroscopy. Formation of the Schiff base and the metal (Zn[II], Cu[II], Co[II] and Ni[II]) chelates was supported by spectral and analytical data. The ligand and metal complexes have been screened for their antibacterial activity against Staphylococcus aureus, Salmonella typhi, Escherichia coli, Klebsiella pneumoniae and antifungal activity against the fungi Candida albicans and Aspergillus niger. Further, the synthesised compounds were also screened for antiproliferative activity against the human colorectal carcinoma (HCT116) cell line using the Sulforhodamine B assay. Results: Metal complexes formed were found to enhance the potency of the Schiff base due to coordination with a copper complex, showing better activity than others. Conclusion: Copper complex was observed to be more potent than other complexes against all the pathogenic microbes and cancer cell line (HCT116).

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In vitro cytotoxicity studies on Carissa congesta, Polyalthia longifolia, and Benincasa hispida extracts by Sulforhodamine B assay method

International Journal of Green Pharmacy ◽

10.4103/0973-8258.161232 ◽

2015 ◽

Vol 9 (3) ◽

pp. 157 ◽

Cited By ~ 2

Author(s):

GauravMahesh Doshi ◽

HemantD Une

Keyword(s):

In Vitro Cytotoxicity ◽

Assay Method ◽

Sulforhodamine B ◽

Cytotoxicity Studies ◽

Sulforhodamine B Assay ◽

Benincasa Hispida ◽

Polyalthia Longifolia

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Design of Oleanolic Acid-Based Hybrid Compounds as Potential Pharmaceutical Scaffolds

Letters in Drug Design & Discovery ◽

10.2174/1570180818666210604112451 ◽

2021 ◽

Vol 18 ◽

Author(s):

Vuyolwethu Khwaza ◽

Opeoluwa Oyehan Oyedeji ◽

Blessing Atim Aderibigbe ◽

Eric Morifi ◽

Youmbi Thierry Fonkui ◽

...

Keyword(s):

Oleanolic Acid ◽

Klebsiella Oxytoca ◽

In Vitro Cytotoxicity ◽

Hybrid Compounds ◽

Sulforhodamine B ◽

Cytotoxicity Studies ◽

Sulforhodamine B Assay ◽

Ic50 Values ◽

Further Development

Background: Infectious diseases as well as cancer are the leading causes of death worldwide. Drug resistance usually results in their treatment requiring a combination of two or more drugs. Objective: Oleanolic-based hybrid compounds were prepared via esterification and characterized using FTIR, NMR, and LC-MS. In vitro antibacterial and in vitro cytotoxicity studies were performed. Method: Oleanolic acid was hybridized with selected known pharmaceutical scaffolds via the carboxylic acid functionality to develop therapeutics with increased biological activity. Antibacterial activity was determined using the micro-dilution assay against selected Gram-positive and Gram-negative bacteria and cytotoxicity using the sulforhodamine B assay. Results: Compound 8 displayed potent antibacterial effect against five strains of bacteria such as Bacillus subtilis, Staphylococcus aureus, Proteus vulgaris, Klebsiella oxytoca, and Escherichia coli with MIC values of 1.25, 0.078, 0.078, 1.25, 1.25 mg/mL when compared to the control, oleanolic acid (MIC = 2.5 mg/mL). Furthermore, in vitro cytotoxicity, as determined using the SRB assay, against selected cancer cells revealed that compound 7 was the most cytotoxic to MDA, DU145, and MCF-7 cell lines with IC50 values of 69.87±1.04, 73.2±1.08, and 85.27±1.02 µg/mL, respectively, than oleanolic acid with an IC50 ˃200 µg/mL. Conclusion: Hybridization of oleanolic acids was successful, and further development of these potential antibacterial compounds with reduced cytotoxicity is warranted.

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Molybdenum oxide nanocolloids prepared by an external field-assisted laser ablation in water

EPJ Web of Conferences ◽

10.1051/epjconf/201816704009 ◽

2018 ◽

Vol 167 ◽

pp. 04009 ◽

Cited By ~ 3

Author(s):

Salvatore Spadaro ◽

Martina Bonsignore ◽

Enza Fazio ◽

Francesco Cimino ◽

Antonio Speciale ◽

...

Keyword(s):

Laser Ablation ◽

Molybdenum Oxide ◽

Pulsed Laser ◽

Spectroscopic Techniques ◽

Sulforhodamine B ◽

Transmission Electron ◽

Sulforhodamine B Assay ◽

Scanning Transmission ◽

Green Technique ◽

Nih 3T3

he synthesis of extremely stable molybdenum oxide nanocolloids by pulsed laser ablation was studied. This green technique ensures the formation of contaminant-free nanostructures and the absence of by-products. A focused picosecond pulsed laser beam was used to ablate a solid molybdenum target immersed in deionized water. Molybdenum oxide nearly spherical nanoparticles with dimensions within few nanometers (20-100 nm) are synthesized when the ablation processes were carried out, in water, at room temperature and 80°C. The application of an external electric field during the ablation process induces a nanostructures reorganization, as indicated by Scanning-Transmission Electron Microscopy images analysis. The ablation products were also characterized by some spectroscopic techniques: conventional UV-vis optical absorption, atomic absorption, dynamic light scattering, micro-Raman and X-ray photoelectron spectroscopies. Finally, NIH/3T3 mouse fibroblasts were used to evaluate cell viability by the sulforhodamine B assay

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Prucalopride exerts neuroprotection in human enteric neurons

AJP Gastrointestinal and Liver Physiology ◽

10.1152/ajpgi.00036.2016 ◽

2016 ◽

Vol 310 (10) ◽

pp. G768-G775 ◽

Cited By ~ 22

Author(s):

Francesca Bianco ◽

Elena Bonora ◽

Dipa Natarajan ◽

Manuela Vargiolu ◽

Nikhil Thapar ◽

...

Keyword(s):

Neuronal Degeneration ◽

Ex Vivo ◽

Neuroprotective Effect ◽

Enteric Neurons ◽

Protective Effects ◽

Therapeutic Implications ◽

Sulforhodamine B ◽

Sulforhodamine B Assay ◽

Intestinal Peristalsis ◽

Neuronal Maintenance

Serotonin (5-hydroxytryptamine, 5-HT) and its transporters and receptors are involved in a wide array of digestive functions. In particular, 5-HT4 receptors are known to mediate intestinal peristalsis and recent data in experimental animals have shown their role in neuronal maintenance and neurogenesis. This study has been designed to test whether prucalopride, a well-known full 5-HT4 agonist, exerts protective effects on neurons, including enteric neurons, exposed to oxidative stress challenge. Sulforhodamine B assay was used to determine the survival of SH-SY5Y cells, human enteric neurospheres, and ex vivo submucosal neurons following H2O2 exposure in the presence or absence of prucalopride (1 nM). Specificity of 5-HT4-mediated neuroprotection was established by experiments performed in the presence of GR113808, a 5-HT4 antagonist. Prucalopride exhibited a significant neuroprotective effect. SH-SY5Y cells pretreated with prucalopride were protected from the injury elicited by H2O2 as shown by increased survival (73.5 ± 0.1% of neuronal survival vs. 33.3 ± 0.1%, respectively; P < 0.0001) and a significant reduction of proapoptotic caspase-3 and caspase-9 activation in all neurons tested. The protective effect of prucalopride was reversed by the specific 5-HT4 antagonist GR113808. Prucalopride promotes a significant neuroprotection against oxidative-mediated proapoptotic mechanisms. Our data pave the way for novel therapeutic implications of full 5-HT4 agonists in gut dysmotility characterized by neuronal degeneration, which go beyond the well-known enterokinetic effect.

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