Characteristics of Molecularly Engineered Anticancer Drug Conjugated Organic Nanomicelles for Site-Selective Cancer Cell Rupture and Growth Inhibition of Tumor Spheroids

2020 ◽  
Vol 3 (10) ◽  
pp. 7067-7079
Author(s):  
Nishant Kumar Jain ◽  
Shalini Dimri ◽  
Rajendra Prasad ◽  
Gayathri Ravichandran ◽  
Vegi Naidu ◽  
...  
Author(s):  
Heidelinde Fiegl ◽  
Judith Hagenbuchner ◽  
Christiana Kyvelidou ◽  
Beata Seeber ◽  
Sieghart Sopper ◽  
...  

2021 ◽  
Vol 50 (15) ◽  
pp. 5197-5207
Author(s):  
Mohini Gupta ◽  
Rajamani Nagarajan ◽  
Chitteti Ramamurthy ◽  
Perumal Vivekanandan ◽  
G. Vijaya Prakash

Strong and site selective red-emitting photoluminescent/MRI multi-functional KLa(0.95−x)GdxF4:Eu3+ (x = 0–0.4) bio-compatible nanomaterials for targeted in-vitro liver cancer cell imaging.


Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2924
Author(s):  
Cláudia Camacho ◽  
Helena Tomás ◽  
João Rodrigues

The DACHPtCl2 compound (trans-(R,R)-1,2-diaminocyclohexanedichloroplatinum(II)) is a potent anticancer drug with a broad spectrum of activity and is less toxic than oxaliplatin (trans-l-diaminocyclohexane oxalate platinum II), with which it shares the active metal fragment DACHPt. Nevertheless, due to poor water solubility, its use as a chemotherapeutic drug is limited. Here, DACHPtCl2 was conjugated, in a bidentate form, with half-generation PAMAM dendrimers (G0.5–G3.5) with carboxylate end-groups, and the resulting conjugates were evaluated against various types of cancer cell lines. In this way, we aimed at increasing the solubility and availability at the target site of DACHPt while potentially reducing the adverse side effects. DNA binding assays showed a hyperchromic effect compatible with DNA helix’s disruption upon the interaction of the metallodendrimers and/or the released active metallic fragments with DNA. Furthermore, the prepared DACHPt metallodendrimers presented cytotoxicity in a wide set of cancer cell lines used (the relative potency regarding oxaliplatin was in general high) and were not hemotoxic. Importantly, their selectivity for A2780 and CACO-2 cancer cells with respect to non-cancer cells was particularly high. Subsequently, the anticancer drug 5-FU was loaded in a selected metallodendrimer (the G2.5COO(DACHPt)16) to investigate a possible synergistic effect between the two drugs carried by the same dendrimer scaffold and tested for cytotoxicity in A2780cisR and CACO-2 cancer cell lines. This combination resulted in IC50 values much lower than the IC50 for 5-FU but higher than those found for the metallodendrimers without 5-FU. It seems, thus, that the metallic fragment-induced cytotoxicity dominates over the cytotoxicity of 5-FU in the set of considered cell lines.


Author(s):  
Anirudh Menon ◽  
Vishnu Priya V ◽  
Gayathri R

<p>ABSTRACT<br />Objective: This study aims at performing a preliminary phytochemical analysis to evaluate the phytochemical composition of pineapple extract and<br />its cytotoxicity potential on oral cancer cell lines.<br />Methods: Preliminary phytochemical analysis of pineapple extract was done, 3-(4, 5-Dimethyl-2-thiazolyl)-2, 5-diphenyl-2H-tetrazolium bromide<br />assay for evaluating the cytotoxicity potential of the extract on oral cancer cell lines was performed.<br />Results: Phytoconstituents such as flavonoids, coumarins, and phenols were present in the pineapple extract. The extract also exhibited increased<br />cytotoxicity with increased concentration.<br />Conclusion: This study is conducted to see if pineapple extract is effective in treating oral cancer in a natural way instead of harmful treatments.<br />Keywords: Cytotoxicity, Pineapple extract, Anticancer drug.</p><p> </p>


2018 ◽  
Vol 24 (3) ◽  
pp. 242-263 ◽  
Author(s):  
David A. Close ◽  
Allen Xinwei Wang ◽  
Stanton J. Kochanek ◽  
Tongying Shun ◽  
Julie L. Eiseman ◽  
...  

Animal and clinical studies demonstrate that cancer drug combinations (DCs) are more effective than single agents. However, it is difficult to predict which DCs will be more efficacious than individual drugs. Systematic DC high-throughput screening (HTS) of 100 approved drugs in the National Cancer Institute’s panel of 60 cancer cell lines (NCI-60) produced data to help select DCs for further consideration. We miniaturized growth inhibition assays into 384-well format, increased the fetal bovine serum amount to 10%, lengthened compound exposure to 72 h, and used a homogeneous detection reagent. We determined the growth inhibition 50% values of individual drugs across 60 cell lines, selected drug concentrations for 4 × 4 DC matrices (DCMs), created DCM master and replica daughter plate sets, implemented the HTS, quality control reviewed the data, and analyzed the results. A total of 2620 DCMs were screened in 60 cancer cell lines to generate 3.04 million data points for the NCI ALMANAC (A Large Matrix of Anti-Neoplastic Agent Combinations) database. We confirmed in vitro a synergistic drug interaction flagged in the DC HTS between the vinca-alkaloid microtubule assembly inhibitor vinorelbine (Navelbine) tartrate and the epidermal growth factor-receptor tyrosine kinase inhibitor gefitinib (Iressa) in the SK-MEL-5 melanoma cell line. Seventy-five percent of the DCs examined in the screen are not currently in the clinical trials database. Selected synergistic drug interactions flagged in the DC HTS described herein were subsequently confirmed by the NCI in vitro, evaluated mechanistically, and were shown to have greater than single-agent efficacy in mouse xenograft human cancer models. Enrollment is open for two clinical trials for DCs that were identified in the DC HTS. The NCI ALMANAC database therefore constitutes a valuable resource for selecting promising DCs for confirmation, mechanistic studies, and clinical translation.


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