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Total alkaloid extract of seeds of harmel genus and effective monomer component thereof, and preparation and use thereof

A technology of total alkaloids and camelamine, which is applied in the direction of medical preparations containing active ingredients, organic active ingredients, plant/algae/fungus/moss ingredients, etc. It can solve the problems of difficult filtration, difficult process, and increased cost.

Active Publication Date: 2009-05-20
SHANGHAI UNIV OF T C M +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] But above-mentioned method has some weak points: 1) although method technology is simple, extraction rate is not high, only separates dehydrohaemaline and lost other alkaloids, and acetate and hydrochloride conversion are not thorough; 2) Extraction and degreasing with ether, and use KI and HI for treatment, which increases the cost and is not suitable for industrial production
3) The method uses cation exchange resin to process alkaloids, resin regeneration and pretreatment are complex (easy to poison and difficult to regenerate), and ether and chloroform are used in subsequent treatment, which is not good for environmental protection
4) The method is not easy to carry out when dilute hydrochloric acid is used for transsolubility, because the seeds of camel cape contain a large amount of mucus, resin, gum, fatty oil, etc., cannot fully contact alkaloids with dilute hydrochloric acid, even if it is stirred, it is also difficult, and the acid solution is difficult to filter ; 5) method extracts with chloroform ammonia water soluble solvent, unfavorable to environmental protection
6) The method uses heavy metals (HgS) and H 2 S treatment, easy to cause environmental pollution and heavy metal residues damage human health
7) The method uses lye to infiltrate and extract, it is not easy to filter, and the process uses organic solvents, and the extraction and separation process is too complicated
However, most of the researches and applications on anti-tumor are focused on now, and the effects on other aspects are not deepened.

Method used

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  • Total alkaloid extract of seeds of harmel genus and effective monomer component thereof, and preparation and use thereof
  • Total alkaloid extract of seeds of harmel genus and effective monomer component thereof, and preparation and use thereof
  • Total alkaloid extract of seeds of harmel genus and effective monomer component thereof, and preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1. Preparation of total alkaloid extract from seeds of Peganum harmala (P.harmala L.)

[0068] Take the Peganum harmala seeds and crush them into coarse powder, take 50g and add 8 times the amount of medicinal materials (W / W) 70-90% ethanol to extract 1-3 times according to the conditions in Table 1, heating and refluxing for 2 hours each time, filter and combine The filtrate, recover the ethanol to a thick paste, add 1, 2, 3 times the weight of the medicinal material under 2-10% hydrochloric acid acidification (pH value 1.0-2.0) under reduced pressure while it is hot (or stir or dissolve by ultrasound), knead and dissolve, and cool The filtrate is alkalized by adding ammonia water to make the pH value 9.0-11.0. The precipitate is filtered and then dried under reduced pressure (vacuum, spray) to obtain the total alkaloid extract mainly containing different proportions of harmine and harmine (see Table 1) below. The optimal process is: take the Peganum harmala seeds ...

Embodiment 2

[0072] Example 2. Preparation of total alkaloid extracts from the seeds of P. multisectum (Maxim.) Bobr and P. nigelastrum Beg.

[0073] According to the best process described in Example 1, 50g of Peganum multisectum seeds were crushed, and 8 times of 85% ethanol was added to heat and reflux for extraction 3 times for 2 hours each time, filtered, combined the filtrate, and recovered the ethanol to a thick paste. Add 10% hydrochloric acid to acidify and knead under heat and decompression (or stir while hot or dissolve in ultrasound), cool and filter, add ammonia water to alkalize the filtrate to make pH = 11.0, the precipitate is filtered and dried under reduced pressure (vacuum, spray). The total alkaloid extract of P. multisectum (Maxim.) Bobr seeds was prepared, and the results are shown in Table 2.

[0074] Table 2 Preparation of the total alkaloid extract of Peganum multisectum

[0075]

[0076] According to the best process described in Example 1, pulverize the seeds of Ar...

Embodiment 3

[0079] Example 3 Separation and preparation of monomer components in Peganum harmala total alkaloid extract

[0080] Take 14 g of total alkaloids, mix the sample with diatomaceous earth, and apply it to a silica gel column. The gradient elution of chloroform-methanol (20:1; 10:1; 5:1; 1:1; 0:1) to obtain different fractions A, B, C, D, E. Fraction A was separated by gel column chromatography, thin-layer preparation and methanol recrystallization to obtain compound 1; Fraction B was separated by gel column chromatography and thin-layer preparation and recrystallized from methanol to obtain compound 2 , 4, 5, 6; fraction C was separated by gel column chromatography and thin-layer preparation and recrystallized with methanol to obtain compound 7; fraction D was separated by gel column chromatography and thin-layer preparation and passed Recrystallized from methanol to obtain compound 8; fraction E was separated by gel column chromatography and thin-layer preparation and recrystallize...

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Abstract

The invention discloses preparation and application of total alkaloids extract and effective components in peganum plant seeds. The peganum plant (comprising harmel, multisectum peganum and peganum nigellastrum) seeds are heated, refluxed and extracted by ethanol, dissolved along with heat, acidulated by added 2 to 10 percent hydrochloric acid, and basified by ammonia water to separate out sediment; and the sediment is dried to obtain the total alkaloids extract mainly containing dehydrogenized peganine and peganine according to a proportion of between 0.18 to 1 and 4.30 to 1, wherein the content of the total alkaloids is more than 50 percent. The total alkaloids extract is separated by chromatography to obtain ten effective monomer components such as the dehydrogenized peganine, the peganine, and the like. Through thin layer chromatography and biological self-developing analysis, the total alkaloids extract and the effective monomer components thereof have the effect of resisting activity of acetylcholine esterase, and can be used for preparing medicament for resisting the activity of the acetylcholine esterase and medicament for treating neurodegenerative diseases.

Description

Technical field [0001] The invention relates to traditional Chinese medicine, in particular to total alkaloid extracts from seeds of Peganum harmala and effective monomer components and their preparation and application. Background technique [0002] Peganum harmala L. is a perennial herb of the genus Peganum in the Zygophyllaceae family. It is widely distributed in the temperate regions of the Old World and has abundant medicinal resources in northwestern China. It has a bitter taste, cool in nature, and poisonous. It is a traditional medicinal material used by the Uyghur and Mongolian people for a long time. It has been listed in the Uyghur Medicine and Health Ministry Drug Standard (WS3-BW-0080-98). The seeds and whole plant are used for medicinal purposes. , Indications of cough, asthma, unnamed swelling and pain. The chemical constituents in its seeds have been reported as early as 1841, and the main ones are Harmine (HAR), Harmaline (HAL), Harmalol (Harmalol) and Harman (Ha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/185A61K31/519A61K31/437A61P25/16A61P25/24A61P25/28C07D487/04C07D471/04C07D519/00A61K131/00
Inventor 王长虹程雪梅王峥涛郑希元赵婷刘力周吉燕
Owner SHANGHAI UNIV OF T C M
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