Sustained release of PI3K inhibitor from PHA nanoparticles and in vitro growth inhibition of cancer cell lines

2011 ◽  
Vol 89 (5) ◽  
pp. 1423-1433 ◽  
Author(s):  
Xiao-Yun Lu ◽  
Elisa Ciraolo ◽  
Rachele Stefenia ◽  
Guo-Qiang Chen ◽  
Yali Zhang ◽  
...  
2017 ◽  
Vol 31 (24) ◽  
pp. 2936-2940 ◽  
Author(s):  
Shaista Bano ◽  
Bina Shaheen Siddiqui ◽  
Ahsana Dar Farooq ◽  
Sabira Begum ◽  
Faheema Siddiqui ◽  
...  

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.


2007 ◽  
Vol 62 (3) ◽  
pp. 483-489 ◽  
Author(s):  
Marisa A. Navo ◽  
Judith A. Smith ◽  
Anjali Gaikwad ◽  
Thomas Burke ◽  
Jubilee Brown ◽  
...  

2021 ◽  
Vol 51 (1) ◽  
Author(s):  
Luis Bustos González ◽  
Mario Juan Simirgiotis ◽  
Claudio Parra ◽  
Susana Alfaro-Lira ◽  
Emilio Soto ◽  
...  

ABSTRACT: Cancer is still one of the leading causes of death worldwide. Many chemotherapeutics from plants have been tested in cancer, such as vinblastine and paclitaxel. The north of Chile, Arica & Parinacota region, is characterized by its vegetal biodiversity due to its unique geographical and climatological conditions, offering an unexplored and unique source of naturally-derived compounds. The present research has considered a screening of 26 highland herbs using an in vitro growth inhibition model in a panel of six cancer cell lines from different tissues. 5 of the 26 studied ethanolic extracts shows strong activity at least in one cell line when tested at 10 µg mL-1. We present a group of plants worthy to be evaluated as promissory extracts. This work is part of the systematic attempt to find new candidates to be used in cancer therapies.


2016 ◽  
Vol 11 (10) ◽  
pp. 1934578X1601101
Author(s):  
Alessio Cimmino ◽  
Patrizia Scafato ◽  
Veronique Mathieu ◽  
Aude Ingels ◽  
Wanda D'Amico ◽  
...  

This paper describes the enantioselective synthesis of analogues of sapinofuranones A and B, namely 5-substitutes dihydro- and 5 H-furan-ones, and their in vitro growth inhibitory activity against six cancer cell lines in comparison with fungal furanones such as diplofuranone A, diplobifuranylones A and B, as well as ( S,S)-enantiomer of sapinofuranone B. The compounds under study displayed weak if any in vitro growth inhibitory activity against the analysed cancer cell lines. However, it seems that among dihydro- and 5 H-furan-ones bearing a 1-hydroxypentyl side chain, the stereochemistry of the furanone ring and that of hydroxylated methine could modify the in vitro growth activity of these compounds. The natural furanones that showed a different unsaturated chain at C-4 or rearranged into a dihydrofuran ring appeared to be inactive in terms of growth inhibitory activity, e.g. displaying growth inhibitory concentration at 50% (GI50) > 100 μM in all six cancer cell lines analysed.


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