Doxorubicin

Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC₅₀ of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy^[1][2]. Doxorubicin inhibits human DNA topoisomerase I with an IC₅₀ of 0.8 μM^[3]. IC50 & Target:Topoisomerase II^[1] In Vitro:Combination of Doxorubicin (Hydroxydaunorubicin) and Simvastatin (HY-17502) in the highest tested concentrations (2 μM and 10 μM, respec-tively) kills 97% of the Hela cells^[4].
Doxorubicin can label neuron cells, and it is bright red under Rhodamine filter bag, and light red-orange under catecholamine filter bag^[8].
Doxorubicin (5 μM; 10-30 min) can be accumulated in B16-F10 melanoma cell line CRL-6475 in a time-dependent manner, and can be detected by green or red fluorescence (green fluorescence has higher detection sensitivity) with a maximum excitation wavelength (λ_ex) and a maximum emission wavelength (λ_em) of 470 nm and 560 nm, respectively^[10].
In Vivo:Doxorubicin (4-8 mg/kg) can delay tumor growth and reduce the expression of c-FLIP in PC3 xenograft nude mice.
Doxorubicin (Intraperitoneal injection; single dose (10 mg/kg) / once daily for 10 days (1 mg/kg) / once per week for 5 weeks (2 mg/kg)) has cardiotoxicity in Sprague-Dawley rats, but compared with a single dose of 10 mg/kg, cumulative dosing of 10 mg/kg over several days or weeks can increase the survival rate of rats.^[6] Doxorubicin (4%-20%; Intrastriatal injection; Single dose) is neurotoxic in Sprague-Dawley rats^[8].
Doxorubicin can be coupled to gold nanoparticles (Au NPs) by PH-sensitive bonding under acidic conditions, allowing it to pass through the blood-brain barrier with a maximum absorption wavelength of 528 nm^[9].