Mycophenolic acid derivatives Penicacids A, B, C and their application in preparing immunosuppression medicaments

A technology of immunosuppression, mycophenolic acid, applied in the field of medicine

Inactive Publication Date: 2012-03-28
SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the biggest problem when transplanting other people's organs is autologous immune rejection

Method used

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  • Mycophenolic acid derivatives Penicacids A, B, C and their application in preparing immunosuppression medicaments
  • Mycophenolic acid derivatives Penicacids A, B, C and their application in preparing immunosuppression medicaments
  • Mycophenolic acid derivatives Penicacids A, B, C and their application in preparing immunosuppression medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Preparation and Structure Identification of Penicacids A, B, C

[0020] One, the preparation of Penicacids A, B, C

[0021] 1. Seed culture:

[0022] (1) Preparation of seed medium: 200g of potatoes (peeled), 20g of glucose, 30g of sea salt, add water to make up to 1L, evenly distribute in ten 500mL Erlenmeyer flasks, and sterilize at 121°C for 25 minutes to obtain sterilized seed culture.

[0023] (2) Cultivation of seeds: Inoculate the strain of marine fungus (Penicillium sp.) SOF07 into the above-mentioned seed culture medium, place it on a shaker at a speed of 150 rpm at a temperature of 28° C., and cultivate for 48 hours to obtain a seed culture solution.

[0024] 2. Solid fermentation culture:

[0025] (1) Preparation of fermentation medium: 2000g of rice, 60g of sea salt, and 2000mL of water were evenly distributed in 20 500mL Erlenmeyer flasks, and sterilized at 121°C for 25 minutes to obtain sterilized fermentation medium.

[0026] (2) Fermentation culture:...

Embodiment 2

[0047] The compounds Penicacids A, B and C separated and purified in Example 1 were tested for IMPDH inhibitory activity and mouse splenocyte proliferation inhibitory activity.

[0048] The specific steps are: IMPDH (type II) enzyme inhibitory activity test, adopt the method reported by Magasanik etc. (Magasanik, B.; Moyed, H.; Gehring, L.J.Biol.Chem.1957,226,339-350.), adopt 96 Well plate, IMPDH (type II) enzyme activity was assessed by detecting NADH formation at 340 nm. Penicacids A, B, and C were dissolved in DMSO, then diluted three times, and then added to the mixture to be tested for pre-incubation, and the final concentration of the enzyme was not more than 2% (V / V). Mycophenolic acid was used as a control.

[0049] The mouse spleen cell proliferation inhibitory activity test, the specific operation is: take the spleen of C57BL / 6 mice, obtain a sterile single-cell suspension through nylon membrane filtration, then centrifuge the cells at 1000rpm for 5 minutes, and the...

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Abstract

The invention discloses mycophenolic acid derivatives Penicacids A, B, C and their application in preparing immunosuppression medicaments. Penicacids A and B have a specific structure shown in (I), wherein, Penicacids A: R1=CH3, R2=OH; Penicacids B: R1=H, R2=OGlu. And Penicacids C has a specific structure shown in formula (II). Immunosuppressive activity evaluations on Penicacids A, B, and C find that Penicacids A, B and C have an obvious inhibiting effect on inosine monophosphate dehydrogenase (IMPDH), especially the compound Penicacids B which has good inhibitory activity. Therefore, Penicacids A, B, C can be used for preparing immunosuppression medicaments applicable in kidney, liver and other organ transplantations.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and in particular relates to a class of mycophenolic acid derivatives Penicacids A, B, C and their application in the preparation of immunosuppressive drugs. Background technique: [0002] At present, in clinical practice, if the disease cannot be cured by chemotherapy, the method of transplanting other people's healthy organs to replace the organs of the sick body or part of the organs of the sick body is adopted. Research on transplantation of livers, kidneys, hearts, corneas, etc. is ongoing, and cases of organ transplantation are also increasing. However, the biggest problem when transplanting other people's organs is autologous immune rejection. Therefore, starting in the 1970s, scientists conducted research on immunosuppressants to prevent rejection in transplant recipients. [0003] Mycophenolic acid (MPA) is an active substance found in the fermentation broth of Penicillium brevicompa...

Claims

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Application Information

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IPC IPC(8): C07D307/88C07H15/26A61K31/365A61K31/7048A61P37/06C12P17/04C12P19/58C12R1/80
Inventor 鞠建华陈子明黄洪波宋永相张长生
Owner SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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