Preparation method of ingenane-type diterpenoid and application of same in pharmacy

An ingena type and diterpene technology is applied in the field of preparing anti-HIV drugs, can solve the problems of difficult separation and high therapeutic index, and achieves the effects of simple enrichment method, clear components and high content

Active Publication Date: 2019-12-06
FUDAN UNIV
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

Especially in recent years, studies have found ingenoid diterpenoids with anti-HIV activity in Euphorbia lunata. This diterpenoid has strong anti-HIV activity, low cytotoxicity, and high therapeutic index. It was shown that the polarity of this diterpenoid is particularly small, and the polarity of the lipid compounds in Euphorbia is very similar, so it is difficult to separate them. The method of diterpenoids attracts the attention of those skilled in the art

Method used

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  • Preparation method of ingenane-type diterpenoid and application of same in pharmacy
  • Preparation method of ingenane-type diterpenoid and application of same in pharmacy
  • Preparation method of ingenane-type diterpenoid and application of same in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Enrichment method of ingenane type total diterpenes in Euphorbia lunata

[0023] Take 100g of the root of Euphorbia lunata, pulverize it with a small pulverizer, add 500mL of 95% ethanol to heat and reflux for extraction 3 times, each time for 1 hour, combine the extracts, concentrate and evaporate to dryness to obtain 15.4g of extract; disperse the extract in 250mL In warm water, extract 4 times with cyclohexane, 250 mL each time, to obtain 2.9 g of cyclohexane extraction parts; mix the above sample with 3.0 g of silica gel (200-300 mesh), and use petroleum ether: acetone (10:1; 5:1; 3:1) as the elution system, use a normal-phase silica gel column for gradient elution under reduced pressure, and collect 1400 mg of components of petroleum ether: acetone = 5:1; recover the solvent under reduced pressure and use Sephadex LH-20 gel column chromatography, eluted isocratically with methanol: dichloromethane = 1:1 system, combined the 13th to 18th column volumes, c...

Embodiment 2

[0024] Example 2: Enrichment method of ingenane type total diterpenes in Euphorbia lunata

[0025] Take 100 g of the root of Euphorbia lunata, pulverize it with a small pulverizer, add 500 mL of acetonitrile, perform flash extraction 6 times, each time for 1 minute, and filter the filtrate with suction, then concentrate and evaporate to dryness to obtain 13.9 g of extract; disperse the extract In 250mL of warm water, extract 4 times with petroleum ether, 250mL each time, to obtain 2.6g of petroleum ether extraction fraction; suspend the above sample with a small amount of methanol, and elute with high-speed countercurrent chromatography three times; use petroleum ether: ethyl acetate Esters: Methanol: Water (4:1:4:1) as the elution system, the upper phase as the stationary phase, and the lower phase solvent as the mobile phase, the flow rate is 2.0mL / min, the rotation speed is 900r / min, the detection wavelength is 210nm, each time The loading amount is about 860 mg. According ...

Embodiment 3

[0026] Example 3: Enrichment method of ingenane type total diterpenes in Euphorbia lunata

[0027] Take 100 g of the root of Euphorbia lunata, pulverize it with a small pulverizer, add 500 mL of methanol, ultrasonically extract 3 times for 30 minutes each time, filter, concentrate and evaporate to dryness to obtain 13.1 g of extract. Disperse the extract in 250mL warm water, extract 4 times with ethyl acetate, 250mL each time, to obtain 3.0g of ethyl acetate extraction part; mix the above sample with 3.0g of silica gel (200-300 mesh), and use petroleum ether: Ethyl acetate (5:1; 2:1; 1:1) was used as the elution system, and a normal phase silica gel column was used for pressure gradient elution to collect 1670 mg of petroleum ether: ethyl acetate = 2:1 components. After recovering the solvent under reduced pressure, the component was separated by Sephadex LH-20 gel column chromatography, eluted isocratically with methanol:dichloromethane=1:1 system, and the 13th to 18th column...

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Abstract

The invention relates to a preparation method of ingenane-type diterpenoid and application of the same in preparation of anti-HIV drugs, belonging to the field of Chinese pharmaceutical manufacturing.According to the method disclosed by the invention, ingenane-type diterpenoid components are enriched in the Euphorbia plant--Euphoria ebracteolata, the contents of main active ingredients are determined and anti-HIV activity tests are carried out. Results show that anti-HIV activity obviously increases with the increase of the content of the ingenane-type diterpenoid components; when the contentof the total ingenane-type diterpenoids in the enriched components is greater than 47%, extremely strong anti-HIV activity is obtained, the value of EC50 reaches 0.0063 [mu]g/mL, cytotoxicity is relatively small (CC50=14), and a selection index (SI) is greater than 2000; and the ingenane-type diterpenoid has obvious advantages compared with the positive control drug zidovudine. The invention establishes the method for rapidly enriching the total ingenane-type diterpenoids in Euphoria ebracteolata, and the enriched total ingenane-type diterpenoids can be used for preparing anti-HIV drugs.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a method for preparing ingenane-type total diterpenes in Euphorbia lunata and its application in pharmacy, in particular to a method for enriching ingenane-type total diterpenes from Euphorbia lunata Method for similar components and their use in the preparation of anti-HIV medicaments. Background technique [0002] Euphorbia ebracteolata Hayata is a perennial herbaceous plant of Euphorbiaceae (Euphorbiaceae), mainly produced in Henan, Shandong, Jiangsu, Anhui, Zhejiang, Fujian and other provinces. As one of the original plants of the traditional Chinese medicine chamaejasma, Its root is used as medicine. Wolf's poison was first recorded in "Shen Nong's Materia Medica", and it mainly treats edema, abdominal distension, phlegm, food, insect accumulation, subordinate pain, cough, asthma, scrofula, sputum nucleus, scabies, and killing fly maggots. In recent years,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C67/48C07C69/33A61K31/23A61K36/47A61P31/18
CPCC07C67/48A61K31/23A61K36/47A61P31/18C07C2603/86C07C69/33
Inventor 陈道峰黄雅思卢燕李国雄
Owner FUDAN UNIV
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