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Preparation method of total diterpenoids of stellera chamaejasme L. and application of total diterpenoids in medicine preparation

A technology of Ruixiang lupus venom and total diterpenes, applied in the directions of antiviral agents, organic chemistry, etc., can solve the problems of serious grassland damage and inability to realize polycyclic structures in chemical synthesis pathways, and achieves low toxicity, strong anti-HIV activity, The effect of simple enrichment methods

Active Publication Date: 2017-02-22
FUDAN UNIV
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AI Technical Summary

Problems solved by technology

It is reported that daphne-type diterpenoids in Daphne chamaejasme have extremely strong anti-HIV activity and have no obvious cytotoxicity, but the content of such constituents in Daphne chamaejasme is extremely low, usually no more than 0.05% , and the chemical synthesis pathway cannot be realized due to its complex polycyclic structure. At the same time, Daphne chamaejasma is one of the common poisonous weeds in grasslands. Due to its strong vitality and rich resources, it is also regarded as a "warning light" for grassland desertification. It is seriously harmful to grassland in my country, and Daphne chamaejasme contains some highly toxic chemical components. Therefore, if a method for quickly enriching daphne-type diterpenes from Daphne chamaejasme will be established, it will be beneficial to the development of highly effective and low-toxic anti-HIV New drugs and the "turning harm into treasure" of this grassland poisonous weed will have very important practical significance

Method used

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  • Preparation method of total diterpenoids of stellera chamaejasme L. and application of total diterpenoids in medicine preparation
  • Preparation method of total diterpenoids of stellera chamaejasme L. and application of total diterpenoids in medicine preparation
  • Preparation method of total diterpenoids of stellera chamaejasme L. and application of total diterpenoids in medicine preparation

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1: small test enrichment method of daphne-type diterpenes

[0018] Dry and pulverize the Rhizoma chamaejasma root to obtain the Rhizoma chamaejasma powder; Weigh the Rhizoma chamaejasma powder (5kg), add 10L of 95% ethanol to heat and extract 3 times, filter, combine the filtrates obtained three times, concentrate the filtrate, and evaporate to dryness to obtain Ethanol extract 500g (DFC-GYSL-T), the ethanol extract (490g) is dispersed in 2L of water, then extracted with 2L of cyclohexane, extracted 4 times, combined with the extracts of 4 times of gained cyclohexane, Concentrate and evaporate to dryness to obtain 40g of cyclohexane part (DFC-GYSL-H), subject the cyclohexane part (40g) to vacuum column chromatography, and use cyclohexane: acetone (10:1, 3:1, 1:1 ) was eluted to obtain three components, namely DFC-GYSL-H1 (24g), DFC-GYSL-H2 (2g), and DFC-GYSL-H3 (8g). DFC-GYSL-H2 (2g) was subjected to Sephadex LH-20 gel column chromatography, eluted with cycl...

Embodiment 2

[0019] Example 2: Pilot-scale enrichment method for daphne-type diterpenes

[0020] Dry and pulverize the root of Rhizoma chamaejasma, get Rhizoma chamaejasma powder; weigh the powder of Rhizoma chamaejasma (10kg), add 60L 95% ethanol, extract 6 times with flash extractor, each time for 1.5min, filter and combine 6 times The resulting filtrate was concentrated and evaporated to dryness to obtain 1466.8 g of ethanol extract (DFC-GYSL-E). Disperse the ethanol extract (1460g) in 4.5L of water, then extract with 4.5L of petroleum ether, extract 5 times, combine the extracts of petroleum ether parts obtained 5 times, concentrate and evaporate to dryness, and obtain 118.0g of petroleum ether parts (DFC- GYSL-P), the petroleum ether part was mixed with 118g of silica gel, subjected to decompression column chromatography, eluted with petroleum ether: acetone (10:1, 3:1, 1:1), collected once per 500mL, and combined 1-35, 36-48, 49-58 bottles, to obtain 3 components, namely DFC-GYSL-P1...

Embodiment 3

[0021] Example 3: Determination of the content of main active ingredients in each sample obtained by the enrichment method

[0022] Get the key active components DFC-GYSL-H, DFC-GYSL-H2, DFC-GYSL-H23, DFC-GYSL-H24, DFC-GYSL-P, DFC-GYSL-P2, DFC-GYSL-P23 and DFC-GYSL-P24 were made into samples of about 0.5 mg / mL respectively, and the main active ingredients in each sample were analyzed by UPLC-MS method, stelleralide C (C1), subtoxin A (C2), huratoxin (C3 ), wikstrolide B (C4) carry out content determination; The method for content determination adopts standard curve method, and liquid chromatography condition is: 0~2min, acetonitrile: water (53:47~56:44); 2~32min acetonitrile: water ( 56:44); 32~35min, acetonitrile:water (56:44~71:29); 35~50min, acetonitrile:water (71:29~100:0); flow rate 0.3mL / min; column temperature 25℃; The detection wavelength is 233nm; the content of each sample is shown in Table 1 below.

[0023] Table 1 The yield of each sample in the enrichment proces...

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Abstract

The invention belongs to the field of traditional Chinese medicine preparation, and relates to a method for enriching daphnane type total diterpenoid ingredients from a grassland poisonous weed-stellera chamaejasme L. and application of the daphnane type total diterpenoid ingredients in preparation of anti-HIV medicine. According to the method, the total diterpenoid ingredients are enriched from the thymelaeaceae plant-stellera chamaejasme L., anti-HIV activity testing and main active ingredient content determining are conducted on all components, and results show that the anti-HIV activity is in an obvious rising trend along with increasing of the content of the daphnane type total diterpenoid ingredients in the components; when the total diterpenoid content of the enriched components is higher than 27%, the extremely high anti-HIV activity is displayed, the EC50 value can reach 0.005 microgram or below, the selection index SI is larger than 2,000, and high efficiency and low toxicity are achieved. The method for quickly enriching the daphnane type total diterpenoids from the stellera chamaejasme L. is established, and the enriched total diterpenoids can be used for preparing the anti-HIV medicine.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a preparation method of total diterpenes of Daphne chamaejasme and its use in pharmacy, in particular to a preparation method for enriching daphne-type total diterpenes from Daphne chamaejasme and its application in Use in the preparation of anti-HIV drugs. Background technique [0002] Stellera chamaejasme (Stellera chamaejasme L.), commonly known as heartbroken grass, steamed bun flower, chervil, etc., is a perennial herb of the genus Stelleralinn in the family Thymelaeaceae. Its medicinal part is the root and is widely distributed in northeast and northwest my country. , southwest, and Nepal and other places, its nature is flat, bitter and pungent, poisonous, and has the effects of dispelling phlegm by dispelling water, destroying accumulation and killing insects. Folks have long been used to treat mustard moss, intractable skin diseases, chronic bronchitis a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/22A61P31/18
CPCC07D493/22
Inventor 陈道峰卢燕严敏黄雅思李国雄
Owner FUDAN UNIV
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