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Total alkaloid extract of seeds of harmel genus, and preparation thereof

A technology of total alkaloids and camelamine, applied in medical preparations containing active ingredients, drug combinations, plant raw materials, etc., can solve the problem of incomplete and difficult conversion of acetate and hydrochloride, resin regeneration and pre-treatment deal with complex issues

Active Publication Date: 2013-06-05
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 Camelina chinensis 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 it is difficult to filter the acid solution ; 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 preparation thereof
  • Total alkaloid extract of seeds of harmel genus, and preparation thereof
  • Total alkaloid extract of seeds of harmel genus, and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Embodiment 1, the total alkaloid extract prepared from camel's cape (P.harmala L) seeds

[0068] Get the camel shell seeds and grind them into coarse powder, take 50g and add 8 times the amount of medicinal material (W / W) 70-90% ethanol according to the conditions in Table 1, heat and reflux to extract 1-3 times, each time for 2 hours, filter, and combine Filtrate, recover ethanol to a thick paste, add 1, 2, 3 times the weight of medicinal materials with 2-10% hydrochloric acid acidification (pH 1.0-2.0) under reduced pressure (or stirring while hot or ultrasonic dissolution) while hot, knead to dissolve, cool Filter, the filtrate is added ammoniacal liquor to make the pH value 9.0-11.0, and the precipitate is filtered and then dried under reduced pressure (vacuum, spray) to obtain the total alkaloid extract mainly containing dehydrohaeline and harmine in different proportions (see Table 1 below). The optimal process is: take the camel cape seeds and pulverize them, ad...

Embodiment 2

[0072] Embodiment 2, the preparation of the total alkaloid extract of P.multisectum (Maxim.) Bobr and Artemisia camel (P.nigelastrum Beg.) seeds

[0073] According to the optimal process described in example 1, get 50g of camel scutellaria seeds and pulverize, add 8 times the amount of 85% ethanol to heat and reflux to extract 3 times, each 2 hours, filter, merge the filtrate, reclaim ethanol to thick paste, take advantage of Add 10% hydrochloric acid to acidify and knead to dissolve under heat and decompression (or stir while hot or ultrasonically dissolve), cool and filter, add ammonia water to the filtrate to make the pH value = 11.0, filter the precipitate and dry it 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 total alkaloid extracts from Camelina multidistaste

[0075]

[0076] According to the optimal process described in Ex...

Embodiment 3

[0079] Example 3, Separation and Preparation of Monomer Components in the Total Alkaloid Extract of Camelia chinensis

[0080] Take 14 g of total alkaloids, mix the sample with diatomaceous earth, put it on a silica gel column, and chloroform-methanol (20:1; 10:1; 5:1; 1:1; 0:1) gradient elution to obtain different fractions A, B, C, D, E. Fraction A was separated by gel column chromatography and thin layer preparation method and methanol recrystallization to obtain compound 1; fraction B was separated by gel column chromatography and thin layer preparation method and recrystallized by methanol to obtain compounds 2 and 3 , 4, 5, 6; fraction C was separated by gel column chromatography and thin layer preparation method and recrystallized from methanol to obtain compound 7; fraction D was separated by gel column chromatography and thin layer preparation method and obtained by Compound 8 was obtained by methanol recrystallization; Fraction E was separated by gel column chromato...

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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 medicines, in particular to total alkaloid extracts from seeds of plants of the genus Camelia and their effective monomer components, as well as their preparation and application. Background technique [0002] Peganum harmala L. is a perennial herb of the genus Peganum in the family Zygophyllaceae. It is widely distributed in the temperate regions of the Old World and has abundant medicinal resources in Northwest China. It is bitter in taste, cool in nature, and poisonous. It is a traditional medicinal material that has been used by Uygur and Mongolian people for a long time. It has been included in the drug standard of Uygur Medicine and Health Department (WS3-BW-0080-98). Both the seeds and the whole plant are used for medicinal purposes. , Indications cough asthma, nameless swelling and pain embolism. The chemical constituents in its seeds have been reported as far back as 1841, mainly Harmine (HAR), Har...

Claims

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Application Information

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Patent Type & Authority Patents(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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