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Membrane-permeable short peptide/matrine as well as preparation method and application thereof

A membrane-permeable short peptide and matrine technology, which can be used in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problems of lack of effective drugs and poor prognosis of liver cancer patients.

Inactive Publication Date: 2016-06-15
INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The prognosis of patients with liver cancer is poor and there is a lack of effective drugs (Torre, Bray et al. 2015)

Method used

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  • Membrane-permeable short peptide/matrine as well as preparation method and application thereof
  • Membrane-permeable short peptide/matrine as well as preparation method and application thereof
  • Membrane-permeable short peptide/matrine as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1 Preparation of the membrane-penetrating short peptide-matrine

[0080] Proceed as follows:

[0081] (1)(41S,7aS,13bR)-10-Oxododecahydro-1H,5H,8H-dipyrido[2,1-f:3',2',1'-ij][1,6 Synthesis of ]naphthyridine-12-ol (TM1):

[0082] Add 30 milliliters of water and 3.36 grams of potassium hydroxide in 100 milliliters of round bottom flasks, solution is heated to 100 ℃, adds 1.2 grams of SM1, after reacting for 8 hours, system is down to room temperature, extracts four times with dichloromethane, 30 ml each time; the organic phases were combined, dried with anhydrous sodium sulfate, and the solvent was removed to obtain a crude oil, which was recrystallized with n-hexane to obtain 0.12 g of white solid TM1, with a yield of 9%.

[0083] (2) 5-oxo-5-(((41S,7aS,13bR)-10-oxodocahydro-1H,5H,8H-dipyrido[2,1-f:3',2', Preparation of 1'-ij][1,6]naphthyridin-12-yl)oxy)pentanoic acid (TM2):

[0084] Add 120 mg of TM1 and 1.2 ml of tetrahydrofuran into a 50 ml round bottom fl...

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Abstract

The invention discloses an antitumor drug, namely, a membrane-permeable short peptide / matrine antitumor drug, with a targeting effect on epithelial-sourced malignant tumors. The antitumor drug is prepared from matrine derivative active ester reacting with membrane-permeable short peptides containing seven amino acids under the basic condition. The membrane-permeable short peptide / matrine reserves the anti-cancer effect of matrine and membrane permeability and targeting ability of the short peptides, and can perform the targeting effect on the epithelial-sourced malignant tumors, especially liver cancer. Compared with clinically applied matrine, the membrane-permeable short peptide / matrine has obvious liver cancer cell targeting ability, and can rapidly penetrate through the liver cancer cell membrane, inhibit liver cancer cell proliferation and induce liver cancer cell apoptosis.

Description

technical field [0001] The invention relates to an antitumor drug with a targeting effect (targeting effect on epithelial-derived malignant tumors) - membrane-penetrating short peptide-matrine, a preparation method and application thereof, and belongs to the technical field of antitumor drugs. Background technique [0002] Matrine is an alkaloid extracted from the leguminous plant Sophora flavescens (Zhang, Cheng et al. 2014), molecular formula: C 15 h 24 N 2 O; molecular weight: 248.3674; CAS number: 519-02-8; its chemical name is (41S, 7aS, 13bR)-10-oxododecano-1H, 5H, 8H-dipyrido[2,1-f :3',2',1'-ij][1,6]naphthyridine; its structure is as follows: [0003] [0004] Matrine injection can inhibit the replication of hepatitis B virus, improve the symptoms and signs of pathological hepatitis, and has little toxic and side effects. It has been used in the clinical treatment of chronic hepatitis and liver cirrhosis (Zhang, Wang et al. 2011). In recent years, studies have ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/4375A61P35/00
CPCA61K31/4375
Inventor 姚庆强孙学英牟艳玲齐放路国梁
Owner INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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