Preparation method and application range of 3-bromopyruvate lipid cubic liquid crystal

Abstract

The invention discloses a preparation method and application range of a 3-bromopyruvate lipid cubic liquid crystal, and belongs to the technical field of biology. The preparation method comprises thefollowing steps: weighing 0.889 g of GMO and 0.111 g of F127, putting the GMO and the F127 into a beaker, and carrying out constant-temperature water bath at 60 DEG C; performing magnetic stirring until the mixture is completely molten, adding 26.67 mg of 3-BP, and slowly adding 25 ml of pure water preheated in advance into the oil phase to serve as a precursor solution; and carrying out high-pressure homogenization on the precursor solution under the conditions of 14900 psi and 9 cycles to obtain milk white 3-BP-LCNP. According to the preparation method, the influence of the dosage of an auxiliary material, a stabilizer, a dispersion phase and a medicine on a crystal form of the lipid cubic liquid crystal is preliminarily screened, a preparation prescription process is optimized by adopting orthogonal design, a particle size and an encapsulation rate both meet requirements, the screened prescription and preparation process are simple and feasible, and prepared cubic liquid crystallinenanoparticles are good in stability.

Description

technical field [0001] The invention relates to prescription screening and application scope, in particular to a preparation method and application scope of a 3-bromopyruvate lipid cubic liquid crystal, belonging to the technical field of biology. Background technique [0002] 3-Bromopyruvate, 3-BP, molecular weight 166.96, acts on the key rate-limiting enzyme hexokinase Ⅱ HK Ⅱ in glycolysis, as a powerful glycolysis inhibitor, because it interacts with the cell metabolites lactic acid and acetone in the body The acid structure is similar, so that it can be transported into tumor cells by means of proteins that transport lactic acid and pyruvate, such as the monocarboxylic acid transporter MCT1, which can effectively reduce the generation of ATP in tumor cells, cut off the energy supply of tumor cells, and starve tumor cells to death. To achieve the purpose of killing tumor cells, but due to the simple structure and unclear side effects, the safety of long-term use of 3-BP s...

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Problems solved by technology

[0002] 3-Bromopyruvate, 3-BP, molecular weight 166.96, acts on the key rate-limiting enzyme hexokinase Ⅱ HK Ⅱ in glycolysis, as a powerful glycolysis inhibitor, because it interacts with the cell metabolites lactic acid and acetone in the body The acid structure is similar, so that it can be transported into tumor cells by means of proteins that transport lactic acid and pyruvate, such as the monocarboxylic acid transporter MCT1, which can effectively reduce the generation of ATP in tumor cells, cut off the energy supply of tumor cells, and starve tumor cells to death. To achieve the purpose of killing tumor cells, but due to the simple structure and unclear side effects, the safety of long-term use of 3-BP still needs to be investigated, and the clinical use is still limited. Therefore, the structural modification of 3-BP such as the formation of drug copolymers, Or use new drug delivery systems such as liposomes, gold nanoparticles, microencapsulation, micro-nano lipids, etc. for anti-tumor research, which is of great significance

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