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Diepoxy diterpene compound with anti-tumor effect as well as preparation method and application

An anti-tumor effect, diepoxy technology, applied in anti-tumor drugs, organic chemistry, drug combination and other directions, can solve problems such as less jasmine, and achieve the effect of improving medical and economic value and obvious inhibitory effect.

Active Publication Date: 2020-07-10
HANGHZOU HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still relatively few studies on Jasmine jasmine at present, and there are no systematic studies and reports on the nutritional value, potential toxicity, pharmacognosy characteristics, and chemical components of Jasmine jasmine. Guo Xiangqun et al. have carried out preliminary biological research on jasmine (Studies on pharmacognosy of jasmine jasmine [J]. Chinese folk medicine, 2014,23(22):19-20)

Method used

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  • Diepoxy diterpene compound with anti-tumor effect as well as preparation method and application
  • Diepoxy diterpene compound with anti-tumor effect as well as preparation method and application
  • Diepoxy diterpene compound with anti-tumor effect as well as preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A kind of preparation method of the diepoxy type diterpene compound with antitumor effect as shown in formula I, comprises following process:

[0039] (1) Get the branch fragments of dried Jasmine jasmine 5kg after crushing, leaching 2 times in methanol at normal temperature, leaching 10 days each time, the amount of methanol added is 10mL / g based on the jasmine jasmine branch mass, filter The insoluble matter was combined with the filtrate, and then evaporated to dryness at low temperature and reduced pressure at a vacuum of 0.08MPa and a temperature of 40°C to obtain 242g of methanol extract;

[0040] (2) The resulting methanol extract and water were mixed uniformly at a mass ratio of 1:5 to make a suspension, extracted three times with equal volumes of ethyl acetate, and the extracts were combined at a vacuum of 0.08MPa and a temperature of 45°C. Evaporate to dryness under reduced pressure at low temperature to obtain 61.71 g of ethyl acetate extract phase;

[0041]...

Embodiment 2

[0045] A kind of preparation method of the epoxy type diterpene compound that has antitumor effect as shown in formula I, comprises following process:

[0046] (1) get the branch fragments of the dry jasmine jasmine after 1kg pulverization, leaching 2 times in methanol at normal temperature, each leaching 10 days, methanol addition is 10mL / g with the twig fragment quality of jasmine jasmine, Filter the insoluble matter and combine the filtrates, then evaporate to dryness at low temperature and reduced pressure at a vacuum of 0.08MPa and a temperature of 40°C to obtain 48g of methanol extract;

[0047] (2) Mix the obtained methanol extract and water according to the mass ratio of 1:5 to make a suspension, extract with equal volume of ethyl acetate for 3 times, combine the extracts, and put the extract under a vacuum of 0.08MPa and a temperature of 45°C Evaporate to dryness under reduced pressure at low temperature to obtain 12 g of ethyl acetate extract phase;

[0048] (3) Mix...

Embodiment 3

[0052] A method for preparing a diepoxy diterpene compound having an antitumor effect as shown in formula I, comprising the following processes:

[0053] (1) get the branch fragments of the dried Jasmine jasmine 500g pulverized, leaching 2 times in methanol at normal temperature, each leaching for 10 days, the amount of methanol added is 10mL / g with the jasmine jasmine branch quality, Filter the insoluble matter and combine the filtrates, then evaporate to dryness at low temperature and reduced pressure at a vacuum of 0.08MPa and a temperature of 40°C to obtain 25g of methanol extract;

[0054] (2) The resulting methanol extract and water were mixed uniformly at a mass ratio of 1:5 to make a suspension, extracted three times with equal volumes of ethyl acetate, and the extracts were combined at a vacuum of 0.08MPa and a temperature of 45°C. Evaporate to dryness under reduced pressure at low temperature to obtain 6.25 g of ethyl acetate extract phase;

[0055] (3) Mix the obta...

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Abstract

The invention relates to the field of plant secondary metabolites. In order to develop a new natural anti-tumor medicine, the invention provides a diepoxy diterpene compound with an anti-tumor effectas well as a preparation method and application thereof. The chemical name of the diepoxy diterpene compound is 8(9), 12(16)-diepoxy-3, 7, 17-trihydroxy-17(15->16)-trans-5, 12-abietane diene-7, 11, 14-triketone. The compound is extracted and prepared from clerodendrum griffithianum, has an anti-tumor effect, has an inhibiting effect on various tumor cells such as human lung cancer cells A549, human cervical cancer HeLa cells, human breast cancer Bcap37 cells and human liver cancer SMMC7721 cells, especially has an obvious inhibitory effect on human breast cancer Bcap37 cells, has a very largeapplication prospect in preparation of anti-tumor drugs, and plays an important role in improving the medical and economic values of clerodendrum griffithianum and promoting development and research on the nutritional value, potential toxicity, pharmacological characteristics, chemical components and the like of clerodendrum griffithianum.

Description

technical field [0001] The invention relates to the technical field of plant secondary metabolites, in particular to a diepoxy diterpene compound with antitumor effect, a preparation method and an application. Background technique [0002] Tumors are characterized by abnormal hyperplasia of visceral tissues. The clinical manifestations are local masses, uneven surfaces, hard texture, pain, fever, and body weight loss. The treatment is difficult, the prognosis is poor, and the mortality rate is high, which seriously affects the lives of patients. Safety is a difficult problem in today's medical field. At present, tumor treatment methods mainly include surgery, chemotherapy, radiotherapy, interventional therapy, etc. Chemotherapy mainly uses anti-tumor drugs to treat tumors. The mainstream anti-tumor drugs on the market, such as gefitinib and sunitinib, have developed rapidly due to their effectiveness and specificity, and have occupied a large market share. In recent years,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/08A61P35/00
CPCA61P35/00C07D493/08
Inventor 林胜友王文龙
Owner HANGHZOU HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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