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Preparation method of active total diterpenoids in Thymelaeaceae plants and application of active total diterpenoids in pharmacy

A technology of Daphneaceae and total diterpenes, which is applied in the field of preparation of anti-HIV drugs, can solve the problems of low content of daphne-type diterpenes, large consumption of organic solvents, and large sample loss, etc., to achieve strong anti-HIV activity and combination The effect of clear components and high recovery rate

Pending Publication Date: 2019-12-06
FUDAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The prior art discloses about 48 genera of Daphneaceae, which are widely distributed in tropical and temperate regions of the northern and southern hemispheres, but the content of daphne-type diterpenes is relatively low. Traditional enrichment methods such as column chromatography require repeated separation and enrichment. The operation is complicated, time-consuming, consumes a large amount of organic solvent, and the sample loss is large, while high-speed countercurrent chromatography is a fast enrichment chromatography technology that does not require a stationary phase as a carrier, with high recovery and high efficiency, especially suitable for low-content Components, which have been widely used in the enrichment and separation of natural products

Method used

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  • Preparation method of active total diterpenoids in Thymelaeaceae plants and application of active total diterpenoids in pharmacy
  • Preparation method of active total diterpenoids in Thymelaeaceae plants and application of active total diterpenoids in pharmacy
  • Preparation method of active total diterpenoids in Thymelaeaceae plants and application of active total diterpenoids in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: Enrichment method of total diterpenes in Daphne genkwa

[0023] Take 1000g of daphne genkwa medicinal material, pulverize it with a pulverizer, add 7L of methanol, heat and reflux for extraction three times, each time for 1 hour, combine the extracts, concentrate and evaporate to dryness, and obtain 202g of extract. The extract was dispersed in 3L of warm water, extracted 4 times with petroleum ether, 3L each time, to obtain 23.2g of petroleum ether extraction fraction (DFC-DG-P). The obtained extract was enriched by high-speed countercurrent chromatography several times, and a mixture of petroleum ether: ethyl acetate: methanol: water (2:1:1.5:1.5; v / v) was used as the solvent system. layer, the upper phase is the stationary phase, and the lower phase is the mobile phase. Fill the stationary phase with the chromatographic column of high-speed countercurrent chromatography, set the rotation speed at 600-1000r / min and the temperature of the water bath at 15...

Embodiment 2

[0024] Embodiment 2: the enrichment method of total diterpenoids in Pleurotus chinensis

[0025] Take 1000g of the medicinal material of Papilia chinensis, pulverize it with a small pulverizer, add methanol and ultrasonically extract 3 times for 30 minutes each time, filter, concentrate and evaporate to dryness to obtain 248g of extract (DFC-WC). Disperse the extract in 3L of warm water, and extract 4 times with n-hexane, 3L each time, to obtain 17.5g of n-hexane extraction parts (DFC-WC-P). The obtained extract was enriched by high-speed countercurrent chromatography, using a mixture of n-hexane:ethyl acetate:methanol:water (2:1:1:2; v / v) as the solvent system, fully mixed and then allowed to stand for stratification. The upper phase is the stationary phase, and the lower phase is the mobile phase. Fill the stationary phase with the chromatographic column of high-speed countercurrent chromatography, set the rotation speed at 600-1000r / min and the temperature of the water bath...

Embodiment 3

[0026] Embodiment 3: Enrichment method of total diterpenes in Tianshan pseudomayerus chamaejasme

[0027]Take 1000g of Tianshan chamaejasma medicinal material, pulverize it with a pulverizer, add 7L of 95% ethanol and heat it under reflux to extract 3 times, each time for 1 hour, combine the extracts, concentrate and evaporate to dryness to obtain 192g of extract (DFC-ST). The extract was dispersed in 3L of warm water, and extracted 4 times with cyclohexane, 3L each time, to obtain 18.2g of cyclohexane extraction fraction (DFC-ST-P). The obtained extract was enriched by high-speed countercurrent chromatography several times, and a mixture of petroleum ether: ethyl acetate: methanol: water (2:1:1.5:1.5; v / v) was used as the solvent system. layer, the upper phase is the stationary phase, and the lower phase is the mobile phase. Fill the stationary phase with the chromatographic column of high-speed countercurrent chromatography, set the rotation speed at 600-1000r / min and the te...

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Abstract

The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a preparation method of active total diterpenoids in Thymelaeaceae plants and application of the active total diterpenoids in pharmacy. According to the invention, the total diterpenoid components are enriched from Thymelaeaceae plants including Daphne genkwa Sieb.et Zucc, Wikstroemia canescens (Wall.) Meisn and Stelleropsis tianschanica Pobed, the obtained main components are subjected to content determination and anti-HIV activity test, and the result shows that the anti-HIV activity has an obvious rising trend along with the increase of the contents of the total diterpenoid components. When the content of the total diterpenoids in the enriched components is larger than 64%, extremely high anti-HIV activity is shown, the EC<50> value can reach 0.0047 microgram / mL, the selection index (SI) is larger than 2000, and the total diterpenoids are efficient and low in toxicity and have obvious advantages compared with a positive control medicine zidovudine. The invention establishes the method for rapidly enriching the total diterpenoids from the Thymelaeaceae plants, the method is simple, the process is reasonable, the recovery rate is high, and the enriched total 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 preparation method of active total diterpenes in Daphneaceae plants and its application in pharmacy, in particular to a method for preparing active total diterpenes from Daphneaceae plants Daphne genus Daphne genus Daphne genus Daphne genus Daphne genus Daphne genus Daphne genus Daphne spp. A method for enriching total diterpene components in Pseudomonas chinensis and its use in the preparation of anti-HIV drugs. Background technique [0002] Daphne-type diterpenes, also known as Daphne toxins, mainly exist in Daphneaceae plants. Modern pharmacological studies have found that they have various biological activities such as anti-HIV and anti-tumor. In particular, a series of daphne-type diterpenes have been found in recent years Terpene compounds have strong anti-HIV activity, low cytotoxicity, and high therapeutic index. The prior art discloses about 48 gener...

Claims

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Application Information

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IPC IPC(8): A61K36/83A61P31/18
CPCA61K36/83A61K2236/333A61K2236/35A61K2236/55A61P31/18
Inventor 陈道峰赵化顶卢燕李国雄
Owner FUDAN UNIV
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