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Pharmaceutical application of 3-trametenolic acid B methyl cyanide

A technology of hydrogenated pinic acid and cyanomethyl ester, which is applied in the direction of medical preparations containing active ingredients, digestive system, drug combination, etc., can solve the problem that hepatitis B virus cannot solve the adverse drug reaction and curative effect well, and cannot solve the problem of virus infection blocking problems and other problems, to achieve the effect of anti-viral recurrence, prevention of drug resistance, and enhancement of drug effects

Active Publication Date: 2019-07-30
CHINA THREE GORGES UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, even if the treatment of hepatitis B virus is carried out at the same time as anti-tumor treatment, it cannot solve the problems of adverse drug reactions and curative effects, let alone solve the problem of blocking the whole process from virus infection to liver cancer.

Method used

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  • Pharmaceutical application of 3-trametenolic acid B methyl cyanide
  • Pharmaceutical application of 3-trametenolic acid B methyl cyanide
  • Pharmaceutical application of 3-trametenolic acid B methyl cyanide

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The synthesis technique of 3-hydropine-pine acid B cyanomethyl ester is as follows:

[0027] Trametes lactinea (Berk.) Pat is a fungus of Polyporaceae, which contains steroids, triterpenoids, sugars, tannins and other compounds, and can be used as a germination fungus of Gastrodia elata. 3-Hydropinemic acid B is a kind of triterpenoid active substance isolated from Dabai suppository. It can enhance immunity, anti-inflammation, and anti-tumor effects, such as gastric cancer, liver cancer, breast cancer, etc., and can also reverse drug resistance to paclitaxel. It has synergistic effect with the chemotherapy drug paclitaxel. However, its solubility is poor and its bioavailability is low. The cyanated derivative 3-hydrogenated pinesic acid B cyanomethyl ester was synthesized from 3-hydrogenated pinesic acid B. 3-Hydropine acid B-cyanomethyl ester has improved solubility and low bioavailability.

[0028] 3-Hydropine acid B cyanomethyl ester is synthesized with 3-hydropin...

Embodiment 2

[0055] ELISA kit for detection of HBsAg secretion

[0056] HepG2 / 2.2.15 cells in the logarithmic growth phase were selected, digested with trypsin into a single cell suspension, 2×10 4 mL- 1 Cells were inoculated at a concentration of 100 μL / well in a 96-well plate, placed at 37°C, 5% CO 2 Cultivate in the incubator for 12h, and then add the MEM medium containing 0.0 (control), 2.5, 5, 10.0, 15.0 and 20.0 μg / mL 3-hydropinebic acid B cyanomethyl ester respectively, and set 3 duplicate holes for each concentration . After culturing for 24 and 48 hours, the supernatants of cells cultured for 24 and 48 hours were collected, respectively, and stored at -20°C. According to the instructions of the ELISA kit, the content of HBsAg in the supernatant was determined. Select a wavelength of 450nm, read the OD value of each well with a microplate reader, take the average value, and calculate the inhibition percentage.

[0057] After collecting part of the supernatant, add 20 μL of MTT...

Embodiment 3

[0085] ELISA Kit to Detect the Effect of 3-Hydropinate B-cyanomethyl Ester on the Secretion of Hepatitis B Surface Antigen

[0086] ELISA kit test analysis shows that 3-hydropinemic acid B cyanomethyl ester has a certain degree of inhibitory effect on the secretion of HBsAg in HepG2 / 2.2.15 cells. , 10, 5, 2.5 μg / mL. Such as figure 2 , 3 , it can be found that with the increase of drug action time, the inhibitory effect of various drugs on HBsAg secretion is also enhanced, but the concentration difference is not obvious.

[0087] qRT-PCR method to detect the expression level of HBx in liver cancer cells under the action of 3-hydropinebic acid B cyanomethyl ester

[0088] qRT-PCR method was used to detect the expression level of hepatitis B virus x protein (HBx) in liver cancer cell HepG2 / 2.2.15 under the action of three drugs, and the concentrations of 3-hydropinebic acid B cyanomethyl ester were 20 μg / mL and 15 μg / mL respectively , 10 μg / mL, 5 μg / mL, 2.5 μg / mL. After 24 ...

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Abstract

The invention provides application of 3-trametenolic acid B methyl cyanide in preparing anti-hepatitis B virus drugs, and further relates to application of the 3-trametenolic acid B methyl cyanide inpreparing drugs inhibiting HBsAg secretion of a human hepatocellular carcinoma HepG2 / 2.2.15 cell strain, or application of 3-trametenolic acid B methyl cyanide in preparing drugs expressing hepatoma carcinoma cell HBx expression. The 3-trametenolic acid B methyl cyanide has positive effects on preventing hepatitis b virus infection, treating hepatitis B infection, preventing hepatocellular carcinoma, treating hepatitis B related hepatocellular carcinoma and preventing relapse in the whole process of lesions. The great significance on solving the technical problem of clinically treating hepatitis B infection, and especially the hepatitis B related hepatocellular carcinoma is achieved.

Description

technical field [0001] The invention relates to a new pharmaceutical use of 3-hydropine-pine-acid B-cyanomethyl ester, in particular to the pharmaceutical use of 3-hydro-pine-pine-acid B-cyanomethyl ester in the preparation of anti-hepatitis B virus drugs. Background technique [0002] The human liver cancer HepG2 / 2.2.15 cell line is derived from the liver cancer cell line HepG2, which integrates two head-to-tail HBV complete genes in the HepG2 genome, and the cell line can stably and continuously express infectious HBV particles , and express HBV-related proteins HBsAg, HBeAg and HBcAg, etc., and produce a large number of viral replication intermediates. The mRNAs of HBV encode core antigen (HBcAg), envelope protein antigen (HBsAgs), polymerase (pol) and X protein (HBx), respectively. HBV has a double coat, and hepatitis B surface antigen (HBsAg) is the membrane protein of the HBV coat. The HBsAg envelope enters the endoplasmic reticulum after the hepatitis B virus replic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P31/20A61P1/16
CPCA61K31/575A61P1/16A61P31/20
Inventor 汪鋆植史非凡万雨莲黄年玉李莉娥贺海波罗发军邓改改
Owner CHINA THREE GORGES UNIV
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