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Dicranostigma leptopodum (maxim) fedde alkaloid effective part preparation method

A technology of effective parts and flower organisms, applied in the field of natural product chemistry, can solve the problems of high dosage of extracts, large daily dosage of patients, and insignificant biological activity, so as to reduce the toxicity in vivo, reduce the content and separate impurities. full effect

Active Publication Date: 2016-01-20
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 32.167mg / kg (Wang Bo, Preliminary Study on the Chemical Components of Yunnan Dirong and the Antiarrhythmic Structure-Activity Relationship of Aporphi-type Alkaloids, Master's Thesis), resulting in certain defects in the clinical application of its extracts

Method used

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  • Dicranostigma leptopodum (maxim) fedde alkaloid effective part preparation method
  • Dicranostigma leptopodum (maxim) fedde alkaloid effective part preparation method
  • Dicranostigma leptopodum (maxim) fedde alkaloid effective part preparation method

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: 4Kg of bald sore flower medical material is pulverized, add 60L concentration and be the sulfuric acid aqueous solution of 0.05%, place 4h, reflux extraction 1h, filter, add 40L concentration of medicine dregs and be the sulfuric acid aqueous solution of 0.05%, reflux extraction 2 times, Extract for 1 hour 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, and detect by HPLC-DAD.

[0039] 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 1h, leave it for 4h naturally, filter and remove impurities through Buchner funnel, and recover the solvent under reduced pressure ...

Embodiment 2

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

[0045] A, acid water extraction steps: 4Kg of the bald sore flower medicinal material is crushed, add 40L of 0.01% aqueous hydrochloric acid solution, stand for 24h, reflux for 1h, extract 3 times, filter, discard the medicinal residues, combine the filtrates, and neutralize with NaOH solution value to neutral, the solvent was recovered under reduced pressure, concentrated to 4L, and sampled for HPLC-DAD detection.

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

[0047] C. Extraction and separation step...

Embodiment 3

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

[0052] A, acid water extraction steps: 4Kg of bald sore flower medicinal material is crushed, add 40L concentration of 0.01% sulfuric acid aqueous solution, place to soak for 4h, reflux extraction for 1h, filter, and reflux extract 2 times with 40L concentration of 0.01% sulfuric acid aqueous solution for medicinal residues , 1 hour each time, combine three filtrates, use NaOH solution to neutralize the value to neutral, recover the solvent under reduced pressure, concentrate to 4L, 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 hour, let it stand naturally for 4 hours, centrifugally filter and remove impurities, and recover the solvent from the mother liquor under reduced pressure to no alcohol taste, to obtain 5L of p...

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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 Dicranostigmaleptopodum (Maxim) Fedde, also known as Hongmao grass, bald flower, Lemahui (Shaanxi), is a plant of the genus bald sore flower in the family 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...

Claims

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Application Information

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IPC IPC(8): A61K36/66A61P29/00
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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