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A solanesol derivative with tumor tissue reduction sensitivity, its preparation method and application

A tumor tissue and derivative technology, applied in the fields of pharmaceutical polymer materials and biomedicine, can solve problems such as drug resistance, toxic side effects, and heart damage, and achieve a good ability to load hydrophobic anticancer drugs, The effect of high drug dose and large drug load

Inactive Publication Date: 2018-11-20
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the low selectivity and high toxicity, it has obvious serious side effects, mainly including bone marrow suppression, heart damage and drug resistance.

Method used

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  • A solanesol derivative with tumor tissue reduction sensitivity, its preparation method and application
  • A solanesol derivative with tumor tissue reduction sensitivity, its preparation method and application
  • A solanesol derivative with tumor tissue reduction sensitivity, its preparation method and application

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Embodiment 1

[0028] A solanesol derivative with tumor tissue reduction sensitivity, the solanesol derivative is a compound of the following structure:

[0029]

[0030] The synthetic route of described solanesol derivative is as follows:

[0031]

[0032] (1) The specific synthesis steps are as follows:

[0033] Weigh 1.31g 3,3'-dithiodipropionic acid (6.4mmol), 1.32g DCC (6.4mmol) and 0.2g DMAP (1.6mmol) in a 100mL round bottom flask, add 15mL anhydrous DMF to dissolve a Liquid, weigh 2.00g solanesol (3.2mmol) and dissolve in 25mL anhydrous dichloromethane, N 2 Under protection, it was slowly dropped into liquid a through a constant pressure dropping funnel, and reacted at room temperature for 48 hours. After the reaction, 15 mL of distilled water was added and extracted through a constant pressure separatory funnel, and the dichloromethane layer was taken, and the operation was repeated twice, and the solvent was removed by rotary evaporation. Use the mobile phase system of petrol...

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PUM

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Abstract

The invention discloses a solanesol ramification of reductive sensibility of tumor tissue. The ramification structure is shown in the prediction. While serving as a micelle for carrying medicine, the solanesol ramification is characterized in that (1) the nano-scale grain size is smaller than 1000 nm, and the granulometric distribution is even and stable; (2) by means of the hydrophilic shell of polyethylene glycol and the nano-scale grain size, the long circulation of nano particles and passive targeting of EPR are achieved; (3) in the effect of the active targeting capable of reducing sensibility, the reductive material GSH which is richly contained in tumour cytoplasm can be utilized to achieve triggered-type drug release in tumor tissue portions; (4) the solanesol ramification has an excellent ability of loading hydrophobic anti-cancer drugs, a high drug loading capacity and great stability;(5) since the solanesol ramification has a great tumor targeting, medicine is more released in tumor tissue and less released in normal tissue, therefore the toxic and side effect performed on the normal tissue is decreased;(6) since the hydrophobic solanesol has an effect of inhibiting tumor cells and sensibilization of anti-cancer medicine, the inhibiting effect of tumor cells in anti-cancer medicine is enhanced.

Description

technical field [0001] The invention belongs to the fields of medicinal polymer materials and biomedicine, and specifically relates to a solanesol derivative with tumor tissue reduction sensitivity, its preparation method and application. Background technique [0002] Tumor is a lesion in which certain cells are altered at the gene level under the action of various carcinogenic factors, resulting in abnormal and infinite proliferation. It has become the main cause of threatening human life and health. At present, tumor treatment is still dominated by three traditional methods, namely radiation therapy, surgical resection and small molecule anticancer drug chemotherapy. The clinical application of radiotherapy and surgical treatment is limited due to the high toxicity and side effects and the tendency to relapse. Anticancer drug chemotherapy is the use of small molecule anticancer drugs to inhibit tumor cells, and is the most common primary and adjuvant treatment in clinica...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G65/334A61K47/54A61K9/107A61P35/00
CPCA61K9/1075C08G65/3344
Inventor 宋仕永秦本凯刘蕾潘洋洋吴晓贺朱迎春
Owner HENAN UNIVERSITY
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