Annamycin

Annamycin is an anthracycline antibiotic with antitumor activity. Annamycin interacts with topoisomerase II, induces double-strand DNA breaks, triggers cell death, and exerts cytotoxic effects. In mice, Annamycin inhibits the growth of advanced subcutaneous melanoma and subcutaneous squamous cell carcinoma, and prolongs the survival of mice with subcutaneous reticulosarcoma and in lung cancer lung metastasis models. Annamycin can be used in research related to melanoma, reticulum cell sarcoma, lung cancer, non-small cell lung cancer, small cell lung cancer^[1][2][3]. In Vitro:Multidrug-resistant KB-V1, P388/Dox, CEM/Vbl and 8226/R cells exhibit partial loss of cross-resistance to free and multilamellar liposome-encapsulated Annamycin (4 h-72 h)^[1].
Annamycin (4.3 min) completely inhibits topoisomerase IIα-mediated DNA cleavage of linearized pBR322 plasmid at an incubation time of 4.3 min^[2].
Annamycin (0.1-10 μM; 1 h) potently inhibits P-glycoprotein-mediated efflux in P-gp-expressing cells, with an IC₅₀ of 0.7 μM^[2].
Annamycin (4-72 hr) circumvents MRP-mediated multidrug resistance in MCF-7, MCF-7/VP, UMCC-1 and UMCC-1/VP cells; it exhibits low resistance indices (1.1, 1.4, 1.3) at 4 and 72 hr exposure durations, with ID₅₀ values ranging from 2.10 to 8.30 μg/mL depending on the cell line and exposure time^[3].
Annamycin (5 μg/mL; 1 hr) induces DNA double-strand breaks in MCF-7 cells^[3]. In Vivo:Free Annamycin (5 mg/kg; i.v.; single dose), Multilamellar liposomal Annamycin (5 mg/kg; i.v.; single dose), and Small unilamellar liposomal Annamycin (5 mg/kg; i.v.; single dose) all inhibit the growth of advanced subcutaneous B16 melanoma, among which the small unilamellar liposome-encapsulated annamycin (S-Ann) exhibits the best efficacy, with a tumor growth inhibition rate (TGI) of 74.4%^[1].
Free Annamycin (4 mg/kg; i.v.; single dose), multilamellar liposomal Annamycin (4 mg/kg; i.v.; single dose), and small unilamellar liposomal Annamycin (4 mg/kg; i.v.; single dose) significantly prolong the survival time of mice subcutaneously inoculated with M5076 reticulosarcoma. Among them, small unilamellar liposome-encapsulated Annamycin (S-Ann) shows the highest efficacy, reaching an ILS of 74.4%^[1].
Free Annamycin (4 mg/kg; i.v.; single), multilamellar liposomal Annamycin (4 mg/kg; i.v.; single), and small unilamellar liposomal Annamycin (4 mg/kg; i.v.; single) significantly prolong the survival of mice bearing a Lewis lung carcinoma lung metastasis model. Among them, small unilamellar liposome-encapsulated Annamycin (S-Ann) exerts the optimal efficacy, achieving an 85.3 % ILS at low inoculum dose and a 57.6 % ILS at high inoculum dose, along with the highest long-term tumor-free survival rate^[1].
Free Annamycin (4 mg/kg; i.v.; weekly; 3 injections), multilamellar liposomal Annamycin (4 mg/kg; i.v.; weekly; 3 injections), and small unilamellar liposomal Annamycin (4 mg/kg; i.v.; weekly; 3 injections) all inhibit the growth of subcutaneous KB squamous cell carcinoma xenografts, among which small unilamellar liposome-encapsulated Annamycin (S-Ann) shows the highest efficacy, reaching a TGI of 87.8%^[1].
Free Annamycin (4 mg/kg; i.v.; weekly; 3 injections), multilamellar liposomal Annamycin (4 mg/kg; i.v.; weekly; 3 injections), and small unilamellar liposomal Annamycin (4 mg/kg; i.v.; weekly; 3 injections) potently inhibit the growth of subcutaneous multidrug-resistant KB-V1 squamous cell carcinoma xenografts. Among them, small unilamellar liposome-encapsulated Annamycin (S-Ann) shows the best efficacy, with a TGI of 92.6% and a 19-fold reduction in tumor growth rate^[1].