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A sterol lactam compound piprolactam and its use in the preparation of anti-complement drugs

A technology of sterolactam and puffolactam, which is applied in the field of preparation of anti-complement drugs, which is a new compound of sterolactam, piprolactam, and can solve problems such as structure and biological activity that have not been reported.

Active Publication Date: 2017-12-01
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The invention of the present application intends to provide a new compound of sterol lactam isolated from puffball, named as puffball lactam. see the report

Method used

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  • A sterol lactam compound piprolactam and its use in the preparation of anti-complement drugs
  • A sterol lactam compound piprolactam and its use in the preparation of anti-complement drugs
  • A sterol lactam compound piprolactam and its use in the preparation of anti-complement drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1 prepares puff lactam

[0015] Take 25kg of the fruiting body of the medicinal material puffball, pulverize it, and reflux extract it with 95% ethanol for 3 times (50L×3), each time for 2h, combine the extracts and concentrate to obtain 0.85kg of extract, add water (4L) to suspend, respectively The volume of petroleum ether, ethyl acetate and n-butanol was extracted 5 times, and the extracts were combined and concentrated to dryness to obtain 160 g of ethyl acetate extract; the ethyl acetate extraction part was separated by silica gel (200-300 mesh) column chromatography, followed by Gradient elution with dichloromethane-methanol (50:1-0:1) gave 10 fractions (Fr.1-10), of which fraction Fr.6 (14g) was subjected to silica gel column chromatography (dichloromethane- methanol, 30:1,20:1,10:1,5:1,3:1), Sephadex LH-20 column chromatography (chloroform-methanol, 1:1) and HPLC (methanol-water, 20:80-80 :20, gradient elution) and other means to purify, separate and...

Embodiment 2

[0017] Example 2 Anti-complement classical pathway test in vitro

[0018] Take 0.04ml of complement (guinea pig serum), add barbiturate buffer solution (BBS) to prepare a 1:10 solution, and double-dilute with BBS to 1:20, 1:40, 1:80, 1:160, 1:10 320, 1:640 and 1:1280 solutions; take 0.1ml of 1:1000 hemolysin, 2% sheep red blood cell (SRBC) and 0.2ml of complement of each concentration, dissolve in 0.2ml BBS, mix well, and bathe in 37℃ water for 30min Put it into a low-temperature high-speed centrifuge, and centrifuge at 4000rpm and 4°C for 5min. Take 0.2ml of the supernatant from each tube in a 96-well plate, and measure its absorbance at 405nm; at the same time, a complete hemolysis group (0.1ml 2% SRBC, 0.1ml hemolysin dissolved in 0.4ml triple-distilled water) was set up to lyse the blood vessels with triple-distilled water. The absorbance was used as the whole hemolysis standard to calculate the hemolysis rate. Take the complement dilution as the X-axis and the hemolysis...

Embodiment 3

[0019] Example 3 Anti-complement alternative pathway test in vitro

[0020] Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH=7.4, containing 5mM Mg 2+,8mMEGTA) was prepared as a 1:5 solution, and double-diluted into 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solutions; take the complement of each concentration 0.15ml, 0.15ml of AP diluent and 0.20ml of 0.5% rabbit red blood cells (RE), mix well, put in a low-temperature high-speed centrifuge after 37°C water bath for 30min, and centrifuge at 4000rpm and 4°C for 5min. Take 0.2ml of the supernatant from each tube in a 96-well plate, and measure the absorbance at 405nm; at the same time, a complete hemolysis group (0.20ml 0.5% RE dissolved in 0.3ml triple-distilled water) was set up in the experiment, and the absorbance of triple-distilled water-lyzed blood vessel was used as the standard of total hemolysis , calculate the hemolysis rate, draw the graph with the complement dilution as the X-axis an...

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PUM

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Abstract

The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a sterol lactam compound and its application in preparing anti-complement drugs. The present invention separates and obtains the sterol lactam compound piprolactam from the fruiting body of puffball, and the compound is ergosterol of the B-ring lactam. After the anti-complement activity evaluation test, the results confirm that the sterol lactam compound piprolactam Amide has a strong inhibitory effect on the activation of the classical pathway and the alternative pathway of the complement system, with a CH50 value of 0.032±0.007mg / ml and an AP50 value of 0.067±0.009mg / ml. The compounds are useful in the preparation of complement inhibitors.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a new sterol lactam compound piprolactam and its application in preparing anti-complement drugs. Background technique [0002] It is disclosed in the prior art that excessive activation of the complement system can cause many major diseases such as systemic lupus erythematosus (SLE), rheumatoid arthritis (RA), and acute respiratory distress syndrome (ARDS). The study of anti-complement drugs has been the focus and focus of the world's pharmaceutical research for many years. However, there is still a lack of ideal therapeutic drugs for such diseases at present, so there is an urgent need for high-efficiency, low-toxicity, and specific new complement inhibitors in clinical practice. The research and development of complement inhibitors from natural products is an important research field that has received more and more attention in recent years, and it has the ch...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J73/00A61P37/02A61P19/02A61P29/00A61P11/00
Inventor 陈道峰范明松黄成钢
Owner FUDAN UNIV
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