To determine the half-life for gemcitabine hydrochloride using microcalorimetry

Liu, Dai‐Huo; Zhao, Weiwei; Li, Zongxiao

doi:10.1007/s10973-013-3375-x

Cited by 4 publications

(3 citation statements)

References 12 publications

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“…Human liver microsomes were used to determine the systemic stability of MFU. We found that MFU was very stable both in vitro and in human liver microsomal studies with more than 80% remaining intact after 2h, suggestive that it is more stable compared to GemHCl as reported in literature 8, [19][20][21]23,24 .…”

Section: Discussionsupporting

confidence: 78%

“…There was no statistically signi cant difference in the initial concentration of MFU after 24 h in both cell lines. This could mean that MFU is quite stable in vitro, and its activities seems to be longer than that GemHCl whose concentration falls to less than half initial concentration between 32 to 94 minutes as documented in literature [19][20][21] .…”

Section: Mfu Stabilitymentioning

confidence: 91%

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Synthesis, characterization, and in vitro anticancer evaluation of 1,3-bistetrahydrofuran- 2yl-5-FU as a potential agent for pancreatic cancer

Ndemazie

Inkoom

Ebesoh

et al. 2022

Preprint

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The failure of current chemotherapeutic agents for pancreatic cancer (PCa) makes it the most aggressive soft tissue tumor with a 5-year survival of slightly above 10% and is estimated to be the second leading cause of cancer death by 2030. Objective: The main aim was to synthesize, characterize and evaluate the in-vitro anticancer activity of 1,3-bistetrahydrofuran-2yl-5FU (MFU). Methods: MFU was synthesized by using 5-fluorouracil (5-FU) and tetrahydrofuran acetate, and characterized by nuclear magnetic resonance (NMR), micro-elemental analysis, high-performance liquid chromatography (HPLC), and liquid chromatography with mass spectrophotometry (LC-MS). MFU and Gemcitabine hydrochloride (GemHCl) were tested for antiproliferative activity against MiaPaca-2 and Panc-1 cell lines. Results: The half-minimum inhibitory concentration (IC50) of MFU was twice lower than that of GemHCl when used in both cell lines. MiaPaca-2 cells (MFU-IC50 =4.5±1.2μM vs. GemHCl-IC50=10.3±1.1μM); meanwhile similar trend was observed in Panc-1 cells (MFU-IC50=3.0 ±1μM vs. GemHCl-IC50=6.1±1.03μM). The MFU and GemHCl effects on 3D spheroids showed a similar trend (IC50-GemHCl=14.3±1.1μM vs. IC50-MFU =7.2±1.1μM) for MiaPaca-2 cells, and (IC50-GemHCl=16.3±1.1μM vs. IC50-MFU=9.2±1.1μM) for Panc-1 cells. MFU significantly inhibited clonogenic cell growth, and induced cell death via apoptosis. Cell cycle data showed mean PI for GemHCl (48.5 - 55.7) twice higher than MFU (24.7 to 27.9) for MiaPaca-2 cells, and similarly to Panc-1 cells. The in-vivo model showed intensely stained EGFR (stained brown) in all mice tumors, however, HER2 expression was less stained in MFU-treated tumors compared to GemHCl-treated tumors and controls. Conclusion: MFU was synthesized with high purity and may have potential anticancer activity against Pca.

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Section: Discussionsupporting

confidence: 78%

Section: Mfu Stabilitymentioning

confidence: 91%

Synthesis, characterization, and in vitro anticancer evaluation of 1,3-bistetrahydrofuran- 2yl-5-FU as a potential agent for pancreatic cancer

Ndemazie

Inkoom

Ebesoh

et al. 2022

Preprint

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show abstract

“…Gemcitabine hydrochloride dissolved in aqueous solutions shows acidic character (pK a ¼ 3:95) due to protonating the nitrogen atom of the pyridimine part in the drug molecule [32]. Once the titration procedure is completed, the mixture tested shows acidity, pH 3.8, caused by the presence of trace quantities of acidic impurities in the cucurbituril tested (the macrocycles are synthesized in a medium of strong mineral acid) and the acidic hydrolysis of gemcitabine hydrochloride (cationic Brønsted acid).…”

Section: Discussionmentioning

confidence: 99%

Calorimetric and spectroscopic investigations of interactions between cucurbituril Q7 and gemcitabine in aqueous solutions

Buczkowski

Stępniak

Urbaniak

et al. 2018

J Therm Anal Calorim

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Studies on the interactions between cucurbituril Q7 and gemcitabine (Gem) hydrochloride in water were carried out using isothermal titration calorimetry (ITC) and electrospray ionization-mass spectrometry (ESI-MS). According to ITC and ESI-MS, the formation of this complex occurs in both the solution containing excess gemcitabine and the solution containing excess cucurbituril Q7. ITC results confirm the formation of a thermodynamically stable supramolecular complex with stoichiometry 1:1. The inclusion mechanism of Gem inside the cucurbituril macromolecule is spontaneous (DG\0). This process is exothermic (DH\0) and is characterized by the loss of entropy (DS\0).

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Physicochemical and in vitro cytotoxicity studies of inclusion complex between gemcitabine and cucurbit[7]uril host

Buczkowski

Gorzkiewicz

Stępniak

et al. 2020

Bioorganic Chemistry

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To determine the half-life for gemcitabine hydrochloride using microcalorimetry

Cited by 4 publications

References 12 publications

Synthesis, characterization, and in vitro anticancer evaluation of 1,3-bistetrahydrofuran- 2yl-5-FU as a potential agent for pancreatic cancer

Synthesis, characterization, and in vitro anticancer evaluation of 1,3-bistetrahydrofuran- 2yl-5-FU as a potential agent for pancreatic cancer

Calorimetric and spectroscopic investigations of interactions between cucurbituril Q7 and gemcitabine in aqueous solutions

Physicochemical and in vitro cytotoxicity studies of inclusion complex between gemcitabine and cucurbit[7]uril host

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