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Kansuininol compounds as well as extraction method and application thereof

An ingenious diterpene and extraction method technology, which is applied in the application field of medicine, can solve the problems of low specific binding rate, strong toxic and side effects of human body, and limit clinical application, and achieve enhanced sensitivity, good safety, and good application foreground effect

Pending Publication Date: 2021-03-05
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tumor multidrug resistance reversal agents targeting P-gp are divided into the following categories in order of development: the first generation of P-gp inhibitors represented by verapamil, which are specific The sex binding rate is low, and it has strong toxic and side effects on the human body; the second-generation P-gp inhibitors, represented by VX-710, are modified on the basis of the first-generation inhibitor structure. These drugs interfere with the normal metabolism in the body and limit the clinical application
The representative drug of the third-generation P-gp inhibitor is tariguidar, which has a high affinity for P-gp protein, but this type of drug is poorly absorbed and the clinical effect is poor

Method used

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  • Kansuininol compounds as well as extraction method and application thereof
  • Kansuininol compounds as well as extraction method and application thereof
  • Kansuininol compounds as well as extraction method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] (1) Under the room temperature condition, soak and extract the pulverized Gansui lump root (5kg) powder in 10L of 95% ethanol for 3 times, each time for 7 days, combine the extracts, and concentrate to obtain 491g of the extract. The kansui mentioned above was purchased from Bozhou in April 2017, and its origin is Houma, Shanxi. It was identified as Euphorbia kansui. The sample specimen was preserved by the Institute of Natural Medicine, School of Pharmacy, Zhejiang University of Technology, No. 20170422.

[0026] (2) the root extract 491g of Radix Kansui obtained by step (1), add 1L water for dissolving, extract twice with sherwood oil, each use 1L sherwood oil, concentrate the organic phase under reduced pressure, obtain organic phase (108g).

[0027] (3) Take the organic phase in step (2), adopt silica gel of 100-200 mesh silica gel as column chromatography packing column chromatography, column volume is 500mL, carry out gradient elution with sherwood oil / ethyl acetat...

Embodiment 2

[0039] Embodiment 2: compound reverses the tumor cell multidrug resistance effect of P-gp mediation

[0040] Compounds 1 and 2 prepared in Example 1 were formulated into 20 μM high-concentration solutions using cell culture medium, and their inhibitory effect on MCF-7 / Adr cell lines resistant to doxorubicin was evaluated. The results showed that after adding the above two compounds, , the number of cells in the drug-dosed group (compound 1 and 2) was 141% and 153% of the blank control, respectively, confirming that the two compounds had no obvious toxic activity on MCF-7 / Adr cells, which was similar to that of the short-chain branched chain in the literature. This coincides with the pro-proliferative effect of diterpenoids on cells at high concentrations.

[0041] MCF-7 / Adr cells with logarithmic growth were selected and seeded in a 96-well plate at a cell density of approximately 7×10 3 / well, the experimental group was compound (1 or 5 μM) combined with doxorubicin (0.25, 0...

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Abstract

The invention provides kansuininol compounds as shown in a formula 1 or a formula 2 in the specification. The safety of the compound 1 and the compound 2 is good, the cytotoxicity of the compound 1 and the compound 2 to different cells is small (wherein the value of IC50 is smaller than 20 [mu]M), and the compound 1 and the compound 2 have good safety; and when the compounds 1 and 2 with differentdosages are given, the inhibition of adriamycin on MCF-7 / Adr can be effectively enhanced, and a reverse multiple can reach 6.5 to 21.5. The two novel kansuininol compounds can obviously reverse the drug resistance of drug-resistant tumor cells MCF-7 / Adr, enhance the sensitivity of the tumor cells to chemotherapeutic drugs, and have good application prospects in anti-tumor multidrug resistance.

Description

technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to two new ingenoid compounds and their extraction methods and their application as active ingredients in the preparation of drugs for reversing multidrug resistance of tumor cells. Background technique [0002] Cancer is one of the major diseases that affect human health. With the aging trend of the population and the rapid growth of the population, the number of cancer incidence and death worldwide is also increasing rapidly. Cancer is becoming an important cause of death and will be an important obstacle to the improvement of human life expectancy. Among the existing cancer treatment methods, chemotherapy is one of the important methods. However, once tumor cells acquire drug resistance during the use of chemotherapy drugs, the effect of tumor chemotherapy will be significantly reduced. According to statistics, in the process of cancer chemotherapy, about 90% of patients c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/33C07C67/56C07C67/52C07C67/58C07C67/48A61K31/22A61K31/704A61P35/00
CPCC07C69/33C07C67/56C07C67/52C07C67/58C07C67/48A61K31/22A61K31/704A61P35/00C07C2603/98A61K2300/00Y02A50/30
Inventor 占扎君章璇章乐马列峰单伟光
Owner ZHEJIANG UNIV OF TECH
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