Piperazine derivatives of butyric acid as differentiating agents in human leukemic cells

doi:10.1007/s002800050737

Paper

Piperazine derivatives of butyric acid as differentiating agents in human leukemic cells

Published Dec 9, 1997 · R. Gillet, P. Jeannesson, H. Sefraoui

Cancer Chemotherapy and Pharmacology

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34

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Abstract

Butyric acid is a potent antineoplastic agent with a well-documented differentiation activity on a wide variety of tumor cells. However, its clinical development is strongly limited by its very short metabolic half-life. In this study we report on the in vitro effects of new original piperazine derivatives of butyric acid on the induction of differentiation and the growth inhibition of human erythroleukemia K562 cells and myeloid leukemia HL60 cells. 1-(2-hydroxyethyl) 4-(1-oxobutyl)-piperazine (HEPB) and [1-(2-hydroxyethyl) 4-(1-oxobutyl)-piperazine] butyrate (HEPDB) were efficient in acting on the differentiation and proliferation of both cell lines, whereas 1-phenyl 4-(1-oxobutyl)-piperazine (PPB) and 1-(3,4-methylene dioxybenzyl) 4-(1-oxobutyl)-piperazine (POB) acted only on proliferation rates. Such derivatives did not induce significant toxicity in mice. These preliminary results should enable, by the development of new series of piperazine derivatives, a better understanding of the mechanisms of action of butyric acid and its analogues on the coupling of growth and differentiation of neoplastic cells.

In Vitro Study

Study Snapshot

New piperazine derivatives of butyric acid effectively induce differentiation and growth inhibition in human leukemic cells, without significant toxicity in mice.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Paper

Piperazine derivatives of butyric acid as differentiating agents in human leukemic cells

References

Time-course of butyric acid-induced differentiation in human K562 leukemic cell line: rapid increase in γ-globin, porphobilinogen deaminase and NF-E2 mRNA levels

Butyric acid rapidly differentiates human K562 leukemic cells, with a notable increase in -globin and NF-E2 mRNA levels, suggesting involvement of the NF-E2 transcription factor.

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Anthracyclines stimulate tumor cell differentiation through distinct pathways, with ACLA mainly acting at the transcriptional level and DOX mainly acting at the posttranscriptional level.

Transcriptional upregulation of γ-globin by phenylbutyrate and analogous aromatic fatty acids

Phenylbutyrate and its analogues effectively stimulate fetal hemoglobin production in erythroid precursors, potentially due to stimulation of a butyrate responsive promoter.

Structure‐activity relationship of 17 structural analogues of N‐butyric acid upon c‐myc expression

N-butyric acid and its analogues can effectively down-regulate c-myc expression in Burkitt's lymphoma cells, potentially offering potential therapeutic treatments for this cancer.

Transcriptional and posttranscriptional regulation of erythroid gene expression in anthracycline-induced differentiation of human erythroleukemic cells.

Anthracyclines ACLA and DOX induce erythroid differentiation through distinct mechanisms, with ACLA enhancing gene transcription and DOX mainly regulating gene expression posttranscriptionally.

Citations

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4APMPP, an antipsychotic drug, shows potential for pharmaceutical use due to its chemical hardness, stability, and reduced sensitivity to negative effects caused by elevated activity in various solvents.

Synthesis and antimicrobial activity of new 2‐piperazin‐1‐yl‐N‐1,3‐thiazol‐2‐ylacetamides of cyclopenta[c]pyridines and pyrano[3,4‐c]pyridines

New disubstituted piperazines show promising antibacterial and antifungal activity, with compound 3k showing the most potent activity against Listeria monocytogenes and Staphylococcus aureus, and 3d, 3g, and 3k showing better activity against MRSA, P. a

Synthesis and Neurotropic Activity of Piperazino-Derivatives of Pyrano[3,4-c]Pyridines

New piperazino-derivatives from chloropyrano- [3,4-c]pyridines show neurotropic activity and pronounced anticonvulsant and anxiolytic properties.

Chitosan-coated liposomes loaded with butyric acid demonstrate anticancer and anti-inflammatory activity in human hepatoma HepG2 cells

Chitosan-coated liposomes loaded with butyric acid show increased cytotoxic activity and anti-inflammatory effects in human hepatoma HepG2 cells, offering potential for targeted therapy.

Piperazine clubbed with 2-azetidinone derivatives suppresses proliferation, migration and induces apoptosis in human cervical cancer HeLa cells through oxidative stress mediated intrinsic mitochondrial pathway

Compound 5e, a piperazine and 2-azetidinone derivative, effectively suppresses human cervical cancer cell growth and induces apoptosis through oxidative stress-mediated intrinsic mitochondrial pathway.