Lycorine hydrochloride is a natural alkaloid extracted from the Amaryllidaceae plant family, it is also an HCV inhibitor with strong activity. Lycorine HCl inhibits cell proliferation and induces cell apoptosis in acute myeloid leukemia (AML) cell line HL-60, monocyte leukemia cell line U937, and T-cell leukemia cell line Jurkat. Lycorine also blocks multiple myeloma KM3 cell cycle, induces K562 cell-cycle arrest at the G0/G1 phase and suppresses tumorigenesis and the growth of various tumor cells, including melanoma C8161, ovarian cancer Hey1B, lung cancer A549, glioblatatoma U373, and esophageal cancer OE21.
In vivo, Lycorine exhibits its numerous pharmacological effects on various diseases with very low toxicity and mild side effects. Lycorine hydrochloride effectively inhibits tumor growth in several mouse xenograft models. It effectively inhibits tumor neovascularization. Lycorine has trivial toxicity to normal cells and normal bodies. The animal toxicological experiments show that the 50% lethal death rate (LD50) of lycorine in mice is 112.2±0.024 mg/kg via intraperitoneal injection. The LD50 of lycorine in mice is 344 mg/kg via gastric lavage injection, suggesting that lycorine is very low toxicity in gastrointestinal administration.
|Cell lines||K562 cells|
|Preparation method||Briefly, nuclear proteins were extracted from K562 cells treated with different concentrations of lycorine (2.5 or 5.0 μM) or without lycorine for 24 h. About 50 μg of nuclear protein from each group was added to a 96-well tissue culture plate and HDAC enzymatic activities in the cell nucleus was determined according to the HDAC colorimetric assay kit instructions.|
|Concentrations||2.5 or 5.0 μM|
|Incubation time||24 h|
|Animal models||SCID mice inoculated with HL-60 cells|
|Formulation||dissolved in DMSO as a stock solution and then diluted in normal saline just prior to usage|
|Dosages||5 or 10 mg/kg/day|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
Lycorine induces cell-cycle arrest in the G0/G1 phase in K562 cells via HDAC inhibition.
Li L, et al. Cancer Cell Int. 2012 Nov 23;12(1):49. PMID: 23176676.
Treatment of lycorine on SCID mice model with human APL cells.
Liu J, et al. Biomed Pharmacother. 2007 May;61(4):229-34. PMID: 17336028.
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