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Triptolide acrylate, and preparation method and application thereof

A technology of laurine ester and acrylic acid, applied in the field of medicine, can solve problems such as toxic and side effects, and achieve the effects of weakening toxicity, inhibiting cancer cell metastasis, and promoting apoptosis

Inactive Publication Date: 2020-04-21
GUANGDONG HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0003] However, although triptolide has good activity, it also has strong toxicity. Clinical trials have shown that it is effective in the digestive system, urinary system, cardiovascular system, blood system, allergic reaction, nervous system, reproductive system, etc. Show strong toxic side effects

Method used

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  • Triptolide acrylate, and preparation method and application thereof
  • Triptolide acrylate, and preparation method and application thereof
  • Triptolide acrylate, and preparation method and application thereof

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Embodiment Construction

[0024] The present invention will be described in further detail below in conjunction with specific embodiments and accompanying drawings.

[0025]

[0026] Take 103.4mg (0.287mmol) of triptolide and 1.75mg (0.01435mmol) of 4-dimethylaminopyridine and dissolve in 5mL of anhydrous dichloromethane, add 319.5mg (3.157mmol) of triethylamine, ice-bath to about 0°C, add 259.7 mg (2.87 mmol) of acryloyl chloride dropwise, gradually return to room temperature after dropping, stir for 2 hours, TLC detects that the reaction is complete, stop stirring, quench the reaction with saturated aqueous sodium bicarbonate, extract with dichloromethane, water The layer was extracted twice with dichloromethane, the dichloromethane extracts were combined, and most of the water in the dichloromethane extracts was washed away with saturated aqueous sodium chloride solution, then dried over anhydrous sodium sulfate, evaporated to dryness under reduced pressure, and prepared Separation on a thin-laye...

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Abstract

The invention relates to triptolide acrylate, and a preparation method and an application thereof, and discloses a novel triptolide derivative. The novel triptolide derivative is shown in a formula Iwhich is described in the specification. The invention also discloses a preparation method for the compound and a medical application of the compound in preparation of anti-cancer drugs. The triptolide acrylate and pharmaceutically acceptable salts thereof have anti-cancer activity, and can effectively inhibit tumor growth of animals through animal in-vivo experiments. A plurality of in-vitro experiment results prove that the protein expression quantity of p53 can be obviously increased; the apoptosis of tumor cells is promoted; the growth of the tumor cells is effectively inhibited; and the effect of inhibiting cancer cell metastasis is achieved. More importantly, the toxicity of the compound to normal cells is less than the toxicity of triptolide.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a derivative of triptolide, its preparation method and its medical application. Background technique [0002] Triptolide, also known as triptolide and triptolide alcohol, is an epoxy diterpene lactone compound extracted from the root, leaf, flower and fruit of Euonymus plant Tripterygium wilfordii. Alkaloids such as tergenine, tripterine, tripterine, tripterine and tripterine constitute the main active ingredients of tripterygium extract, which are insoluble in water but easily soluble in methanol, dimethyl Sulfoxide, absolute ethanol, ethyl acetate, chloroform, etc. Current research shows that it has anti-oxidation, anti-rheumatoid, anti-senile dementia, anti-cancer and other effects. Modern research shows that triptolide not only has anti-rheumatoid effects, but also anti-senile dementia and anti-cancer effects. [0003] However, although triptolide has good act...

Claims

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Application Information

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IPC IPC(8): C07J73/00A61P35/00
CPCC07J73/003A61P35/00
Inventor 刘博黄宪章韩丽乔杨祎琦王凯吴云山王晓婉李恩念王意黄闰月韩晓东钟金浪陆金健张玉琴祝春香
Owner GUANGDONG HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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