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Tripterine derivative and preparation method and application thereof

A technology of tripterine and its derivatives, applied in the field of medicine, to achieve the effects of increased selectivity, reduced toxicity, and good anti-tumor effects

Active Publication Date: 2020-10-30
MACAU UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the structural modification of the 2 and 3 positions of tripterine has been reported to have good cytotoxicity to many cancer cell lines, but further research is still needed to find a structural modification method with better performance

Method used

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  • Tripterine derivative and preparation method and application thereof
  • Tripterine derivative and preparation method and application thereof
  • Tripterine derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Tripterylide (compound 1) was coupled with the dipeptide through the 29-position carboxylic acid of tripteryne in the form of an amide bond to obtain the following series of tripteryne derivatives (compounds 2-7):

[0035]

Embodiment 2

[0037] Tripterylide (compound 1) and tripterylide derivatives (compound 2-7) of Example 1 were tested for cytotoxicity by the MTT method, and the cells used were normal human liver cells LO2 and lung epithelial cells BEAS-2B, The test results are shown in Table 1:

[0038] Table 1

[0039]

[0040] It can be seen from Table 1 that compared with compound 1, the toxicity of compounds 2-7 to normal cells is significantly reduced, which proves that the structural modification of tripterine in the present invention effectively improves its performance.

Embodiment 3

[0042] By testing the selectivity index of tripterine derivatives (IC of normal cells 50 / IC of cancer cells 50 ), the result obtained is: compared with natural tripterine (compound 1), the selectivity of a series of tripterine derivatives in Example 1 to tumor cells is improved. Among them, the selection specificity of compound 3 to the liver cancer cell line HepAD38 was more than 30 times and more than 10 times higher than that of the normal cell line LO2 and CCD19Lu, respectively; The selectivity of the cell line HepAD38 and the liver cancer cell line HepG2 was improved by more than 12 times; the specific test data are shown in Table 2:

[0043] Table 2

[0044]

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PUM

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Abstract

The invention belongs to the field of medicines, and discloses a tripterine derivative and a preparation method and application thereof. The tripterine derivative is coupled with dipeptide on 29-position carboxylic acid of tripterine through formation of amido bonds, and carboxyl of the dipeptide is connected with tert-butyl. According to the tripterine derivative, the cytotoxicity of tripterine can be reduced, the stability is improved, and the selectivity to tumor cells is enhanced, so that the practical application value of tripterine as an anti-cancer component is improved.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a tripterine derivative and its preparation method and application. Background technique [0002] Celastrol is mainly derived from the root of the traditional Chinese medicine Tripterygium wilfordii HookF, and its important drug component contains quinonemethyl triterpenoids. This natural compound has a variety of pharmacological activities, including anti-inflammatory, Anti-oxidation, cardioprotection, neuron degeneration, anti-obesity, inhibition of cancer cell growth, induction of apoptosis, inhibition of tumor cell invasion and metastasis, etc. Recent studies have shown that tripterine exhibits its pharmacological effects through a variety of molecular targets, such as SERCA, Hsp90-Cdc37, NF-κB / IKKβ, VEGFR1, VEGFR2, and PI3K / Akt signaling pathways. Recent studies have shown that tripterine induces substantial cytotoxicity and mobilizes cytosolic calcium in EGFR (epidermal growth fact...

Claims

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Application Information

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IPC IPC(8): C07K5/072C07K1/107C07K1/02A61K47/64A61K31/56A61P35/00
CPCA61K31/56A61K47/64A61P35/00C07K5/06104C07K5/06113
Inventor 黄锦伟刘良保罗高尔罗婉君吴柏霖
Owner MACAU UNIV OF SCI & TECH
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