Doxorubicin hydrochloride, a potent chemotherapeutic agent and cytotoxic anthracycline antibiotic, inhibits human DNA topoisomerase I and II with IC50 values of 0.8 µM and 2.67 µM, respectively. It diminishes the basal phosphorylation of AMPK and acetyl-CoA carboxylase, leading to the induction of apoptosis and autophagy[1][2][3].
体内研究
Doxorubicin hydrochloride, in animal studies, is utilized to develop models of heart failure. When administered alone, neither Doxorubicin at a dosage of 2 mg/kg nor Zoledronic acid at 100 μg/kg significantly reduces the final tumor volume compared to saline treatment. However, mice receiving a combined treatment of Doxorubicin and Zoledronic acid show significantly smaller final tumor volumes than those treated with Doxorubicin alone[6].
Administering Doxorubicin (ranging from 4% to 20% concentration; via a single intrastriatal injection) demonstrates neurotoxic effects in Sprague-Dawley mice[7].
Doxorubicin can be attached to gold nanoparticles (Au NPs) through pH-sensitive bonds in acidic environments, enhancing its ability to cross the blood-brain barrier. The maximum absorption wavelength for this conjugation is 528 nm[9].
体外研究
Doxorubicin hydrochloride, at concentrations ranging from 1 to 8 µM for durations of 24 and 48 hours, reduces cell viability in MCF-10F, MCF-7, and MDA-MB-231 cells in both time- and dose-dependent manners[4].
Doxorubicin hydrochloride, at a concentration of 1 µM over 3 and 24 hours, causes a decrease in the G0/G1 phase and an increase in the G2 phase of Hct-116 human colon carcinoma cells[5].
Doxorubicin hydrochloride, at specific dosages for different cell types over 48 hours (1 μM for MCF-10F and MDA-MB-231 cells, 4 μM for MCF-7 cells), triggers apoptosis through the upregulation of Bax, caspase-8, and caspase-3 and the downregulation of Bcl-2 protein[4].
Doxorubicin also serves as a marker for neuron cells, appearing bright red under a Rhodamine filter and light red-orange under a catecholamine filter[7].
Doxorubicin accumulates in the B16-F10 melanoma cell line CRL-6475 in a time-dependent manner, observable between 10 to 30 minutes at concentrations of 5 μM. It can be detected using either green or red fluorescence, with green fluorescence offering superior sensitivity. The optimal wavelengths for excitation and emission are 470 nm and 560 nm, respectively[8].
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