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Triptolide derivatives and application thereof

A technology for triptolide and derivatives, which is applied to triptolide derivatives and their application fields, and can solve the problems of poor water solubility, high toxicity, and low target specificity.

Inactive Publication Date: 2015-02-04
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, triptolide has its shortcomings as an anticancer drug: its water solubility is poor, and its target specificity is not high, and its toxicity is relatively high.

Method used

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  • Triptolide derivatives and application thereof
  • Triptolide derivatives and application thereof
  • Triptolide derivatives and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Dose curve and IC of triptolide and its derivatives inhibiting cell viability 50 value determination

[0022] In this embodiment, the MTT method is used to measure the influence of triptolide derivatives on the proliferation of various cancer cells. The specific operations are as follows:

[0023] (1) Experimental materials

[0024] Cell lines: HepG2 (ATCC HB-8065), MCF-7 (ATCC HTB-22).

[0025] Cancer cell lines were cultured with DMEM (Gibco) + 10% fetal bovine serum (Hyclone). The experiment also needs triptolide and its derivatives (self-synthesized), 3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide (Sigma).

[0026] (2) Experimental method

[0027] The MTT method was used to detect that triptolide and its derivatives have an inhibitory effect on cell proliferation, and the specific determination method is as follows:

[0028] A. Digest the logarithmic phase cells with trypsin, collect by centrifugation after termination, make cell suspensi...

Embodiment 2

[0040] Example 2: Detection of PARP cleavage, RXRα and tRXRα degradation induced by triptolide and its derivatives by Western blot

[0041]Select liver cancer cells HepG2, and culture them in 6-well tissue culture plates at 37°C and 5% carbon dioxide incubator, with 50nM triptolide (TR01) and its derivatives (No. 1, No. 2, No. 3, No. 4, No. 5, No. 6 and No. 7), serum-free DMEM were treated for 24h. Then, it was lysed on ice for 30 min with improved RIPA lysis buffer (50 mM Tris-HCl, pH 7.4; 150 mM NaCl; 5 mM EDTA; 1% NP-40, 0.5% sodium deoxycholate, 0.1% SDS). With the same loading amount, 8% SDS-PAGE electrophoresis, transfer membrane, block with 5% skimmed milk powder TBST (50mM Tris-HCl (pH 7.4), 150mM NaCl and 0.1% Tween-20) at room temperature for 1h, at 4°C Incubate the primary antibody overnight, incubate the secondary antibody at room temperature for 1 h, develop color with ECL, and expose. Finally, PARP, RXRα, tRXRα and β-actin were detected.

[0042] Experimental ...

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Abstract

Triptolide derivatives and application thereof relate to triptolide. Triptolide and the derivatives thereof has different-degree anticancer activity on HepG2 cell and MCF-7 cell. A method for using tRXRalpha and RXRalpha to evaluate the anticancer activity and toxic and side effects of triptolide and the derivatives thereof is firstly provided. The triptolide and the derivatives thereof are confirmed to have the anticancer activity closely related to the tRXRalpha protein expression lowering capacity, and the stronger rRXRalpha lowering capacity, the higher anticancer acitivty. Also the technical scheme firstly confirms that reduction of the toxic and side effects of the triptolide derivatives is related to the stability of normal-cell full-length RXRalpha protein, and the stronger protection effect of the derivatives on full-length RXRalpha, the smaller toxic and side effects.

Description

technical field [0001] The present invention relates to triptolide, in particular to triptolide derivatives and applications thereof. Background technique [0002] Retinoid X receptor (RXR) belongs to the non-steroid hormone receptor superfamily and is a unique member of the nuclear receptor family. It can not only homodimerize, but also bind to other nuclear receptors (such as RAR, PPAR, VDR, TR and Nur77, etc.) form heterodimerization. Therefore, RXRα plays a very critical role in regulating the biological functions of cell growth, differentiation and apoptosis, and the expression and function changes of RXRα are involved in the occurrence of many diseases and cancers. Reduced expression of RXRα is associated with the formation of malignancies such as T-cell lymphoma, thyroid cancer, prostate cancer, and non-small cell lung cancer. RXRα ablation in adult tissue leads to precancerous lesions in the skin and prostate. Not only that, it is associated with liver and colon c...

Claims

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Application Information

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IPC IPC(8): C07J73/00A61K31/585A61P35/00
CPCC07J73/003
Inventor 曾锦章庞冀燕曾文军吴云龙
Owner XIAMEN UNIV
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