A kind of preparation method of effective part of bald acne flower alkaloid

An effective part and flower biological technology is applied in the field of preparation of natural product extracts, extracting and purifying effective parts of alkaloids, and can solve the problems of high dosage of extracts, large daily dosage of patients, and insignificant biological activity. The effect of reducing in vivo toxicity, reducing content, and sufficient separation of impurities

Active Publication Date: 2019-06-21
LANZHOU INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The defect of the above patents is that the traditional natural product extraction method is used for water extraction or alcohol extraction to obtain the total extract of all chemical components contained in the plant, and the total extract is not effectively separated and purified, resulting in the given extract. The high dose and biological activity are not obvious at the same dose, and the daily dose of the patient is too large, and the toxicity of its main component and high content component isocridine is relatively obvious, and its LD 50 It is 32.167 mg / kg (Wang Bo, Preliminary Study on the Chemical Components of Yunnan Dirong and the Antiarrhythmic Structure-Activity Relationship of Aporphi-type Alkaloids, Master Thesis), which leads to certain defects in the clinical application of its extracts

Method used

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  • A kind of preparation method of effective part of bald acne flower alkaloid
  • A kind of preparation method of effective part of bald acne flower alkaloid
  • A kind of preparation method of effective part of bald acne flower alkaloid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: Extraction and separation of effective parts of alkaloids in Tuchuang flower

[0038] A, acid water extraction step: 4 Kg of bald sore flower medical material is pulverized, add 60 L concentration and be the sulfuric acid aqueous solution of 0.05%, place 4 h, reflux extraction 1 hour, filter, add 40 L concentration of medicinal dregs and be the sulfuric acid aqueous solution of 0.05%, Reflux extraction twice, 1 h each time, filter, combine the three filtrates, use 10% NaOH solution to neutralize the value to neutral, recover the solvent under reduced pressure, concentrate to obtain 6.5 L of alkaloid extract of bald acne flower, HPLC-DAD detection.

[0039] B. Alcohol precipitation and impurity removal step: in step A, add 20L of 95% ethanol to the alkaloid extract of bald acne flower under mechanical stirring, stir for 1 hour, let it stand naturally for 4 hours, filter the impurity removal through Buchner funnel, and recover the mother liquor under reduced pr...

Embodiment 2

[0044] Embodiment 2: Extraction and separation of effective parts of alkaloids in Tuchuang flower

[0045] A, acid water extraction step: 4 Kg of bald sore flower medicinal materials are pulverized, add 40 L concentration of 0.01% hydrochloric acid aqueous solution, place for 24 h, reflux extraction for 1 h, extract 3 times, filter, discard the medicinal residues, combine the filtrate, and use The neutralization value of the NaOH solution was neutralized, the solvent was recovered under reduced pressure, concentrated to 4 L, and samples were taken for HPLC-DAD detection.

[0046] B. Alcohol precipitation and impurity removal step: In step A, add 20 L of methanol to the alkaloid extract of bald acne flower under mechanical stirring, stir for 1 hour, let it stand naturally for 4 hours, centrifuge and filter to remove impurities, and recover the solvent from the mother liquor under reduced pressure until it becomes viscous shape, dissolved in water to obtain 5L of purified alkalo...

Embodiment 3

[0051] Example 3: Extraction and separation of effective parts of alkaloids in Tuchuang flower

[0052] A, acid water extraction step: 4 Kg of the bald sore flower medicinal material is crushed, add 40 L concentration of 0.01% sulfuric acid aqueous solution, place to soak for 4 hours, reflux extraction for 1 hour, filter, and use 40 L concentration of 0.01% sulfuric acid aqueous solution for the medicinal residues Reflux and extract twice, each time for 1 h, combine the filtrates three times, neutralize the value to neutral with NaOH solution, recover the solvent under reduced pressure, concentrate to 4 L, and sample for HPLC-DAD detection.

[0053] B. Alcohol precipitation and impurity removal step: in step A, add 20L of 95% ethanol to the alkaloid extract of bald sore flower under mechanical stirring, stir for 1 h, let it stand naturally for 4 h, centrifugal filter for impurity removal, and recover the solvent from the mother liquor under reduced pressure. Without alcoholic ...

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Abstract

The present invention discloses a dicranostigma leptopodum (maxim) fedde alkaloid effective part preparation method, wherein the dicranostigma leptopodum (maxim) fedde alkaloid effective part obtained through chemical steps is a brownish-black powdery solid, and comprises aporphine alkaloid, morphinane alkaloid, protopine alkaloid, protoberberine alkaloid and isoquinoline alkaloid. According to the present invention, with the method, the concentration of the active compound can be effectively improved, the drug taking dose can be lowered, and the pharmacological activity of the dicranostigma leptopodum (maxim) fedde alkaloid can be significantly improved.

Description

technical field [0001] The invention relates to a natural product extract, which belongs to the field of natural product chemistry. Specifically, the present invention relates to a preparation method for extracting and purifying effective fractions of alkaloids from Papaveraceae plant bald sore flower. Background technique [0002] Bald sore flower, the Latin name of the plant Dicranostigma leptopodum (Maxim) Fedde, also known as Hongmaocao, bald flower, Lemahui (Shaanxi), is a plant of the genus Papaveraceae. Tudouhua is a biennial or perennial herb, 25-80 cm high; Tudouhua is distributed in temperate Asia, hills, hillsides, roadsides, farmland, grasslands, walls, etc. at an altitude of 400-1300 meters, and is drought-resistant and barren-resistant It is produced in my country, mainly distributed in Gansu, Shaanxi, north and south of the Qinling Mountains, and the Weihe River Basin; the plant can be excavated in spring and summer as a whole herb with roots, dried in the s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/485A61K31/4375A61K31/4353A61K31/395A61K36/66A61P29/00
Inventor 柳军玺邸多隆钟梅陈亚丽
Owner LANZHOU INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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