CN112426446A - Sophora japonica extract, preparation method of pharmaceutical composition of extract and antimalarial application of extract - Google Patents

Sophora japonica extract, preparation method of pharmaceutical composition of extract and antimalarial application of extract Download PDF

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Publication number
CN112426446A
CN112426446A CN202011557132.6A CN202011557132A CN112426446A CN 112426446 A CN112426446 A CN 112426446A CN 202011557132 A CN202011557132 A CN 202011557132A CN 112426446 A CN112426446 A CN 112426446A
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extract
pagodatree
preparation
sophora japonica
whole plants
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姜北
肖朝江
张伟
郝艺
刘蓉
刁红梅
董相
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Dali University
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Dali University
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/48Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/489Sophora, e.g. necklacepod or mamani
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/33Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/333Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/35Extraction with lipophilic solvents, e.g. Hexane or petrol ether
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/39Complex extraction schemes, e.g. fractionation or repeated extraction steps
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biotechnology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Medical Informatics (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Epidemiology (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

The invention relates to a preparation method and application of a pagodatree extract and a pharmaceutical composition thereof, belonging to the field of pharmacy of traditional Chinese medicines and natural medicines. The preparation method of the anti-malarial medicine taking the extract of the invention as an active ingredient comprises the steps of taking dry overground parts or whole plants of the Sophora japonica plants, crushing the dry overground parts or the whole plants to 30 meshes, and extracting the crushed dry overground parts or the whole plants with organic solvent petroleum ether, chloroform, ethyl acetate, acetone, methanol, ethanol or water. The application of the pagodatree extract in preparing the antimalarial agent comprises the following steps: preferably, the antimalarial activity is obtained by applying the composition to a substrate or a population in an amount of 0.01-30 g, optionally in combination with a carrier and/or vehicle. The invention expands the indications of the medicinal material of the pagodatree, and improves the medicinal value of the traditional pagodatree medicinal material.

Description

Sophora japonica extract, preparation method of pharmaceutical composition of extract and antimalarial application of extract
The technical field is as follows:
the invention belongs to the field of pharmacy of traditional Chinese medicines and natural medicines, and particularly relates to a preparation method of a pagodatree extract, a medicinal composition taking the extract as an active ingredient, and application of the pagodatree extract in an antimalarial agent.
Technical background:
pagoda tree (A)Sophora japonicaL.) is Sophora (Leguminosae)Sophora) Plants, deciduous trees, up to 25 meters; the native China is widely cultivated in the south and north provinces, and north China and loess plateau regions are particularly common. According to records of Chinese pharmacopoeia, Chinese materia medica and the like, the whole body of the pagoda tree is treasure, and branches, leaves, roots, flowers and fruits of the pagoda tree can be used as medicines; the branch has effects of removing blood stasis, stopping bleeding, clearing heat, eliminating dampness, dispelling pathogenic wind, and killing parasite, and can be used for treating metrorrhagia, leucorrhea with red and white discharge, hemorrhoid, pudendal sac pruritus, cardialgia, conjunctival congestion, and scabies; the leaf has effects of clearing liver-fire, cooling blood, removing toxic substance, eliminating dampness, and killing parasite, and can be used for treating infantile convulsion, fever, intestinal wind, hematuria, hemorrhoid, eczema, scabies, carbuncle, sore, and furuncle; the root has effects of removing blood stasis, relieving swelling, and killing parasite, and can be used for treating hemorrhoid, pharyngitis, ascariasis, etc.; the flower has effects of cooling blood, stopping bleeding, clearing liver-fire, and can be used for treating hematochezia, hemorrhoidal bleeding, bloody dysentery, metrorrhagia, hematemesis, blood circulation promoting, liver heat with conjunctival congestion, headache, giddiness, etc.; the fruit has effects of clearing heat-fire, cooling blood and stopping bleeding, and can be used for treating intestinal heat hematochezia, hemorrhoid hemorrhage, liver heat headache, giddiness conjunctival congestion, etc. In addition, the wood can be used for construction. Modern researches show that the pagoda tree is rich in flavonoid compounds, and nearly 200 chemical components have been reported from the pagoda tree by adding triterpenes, alkaloids and other types of compounds. Pharmacological research shows that the pagodatree has various biological activities including hemostasis, antioxidation, anti-inflammation, blood sugar reduction, anti-tumor, antibiosis, neuroprotection and the like (Information on traditional Chinese medicine, 2019, 36(4): 125-128; Tianjin Chinese medicine Learning newspaper, 2016, 35(3): 211-216; Chinese herbal medicine, 2018, 49(18): 4461-4467; Journal of Ethnopharmacology, 2016, 187: 160-182). At present, a preparation method of a pagodatree extract, a medicinal composition taking the extract as an active ingredient and a report of application of the extract in malaria resistance are not found at home and abroad.
The invention content is as follows:
the invention aims to provide a preparation method of a pagodatree extract, a pharmaceutical composition taking the pagodatree extract as an active ingredient, and application of the pagodatree extract and the pharmaceutical composition in preparation of an antimalarial agent.
The above object of the present invention is achieved by the following technical solutions:
a method for preparing Sophora japonica extract comprises pulverizing dried aerial parts or whole plant of Sophora japonica plantExtracting with organic solvent such as petroleum ether, chloroform, ethyl acetate, acetone, methanol, ethanol or water at room temperature for 12-48 hr for 2-5 times, mixing extractive solutions, and concentrating to obtain extract. Or drying aerial parts or whole plant of Sophora japonica, pulverizing to 30 mesh, and dissolving in organic solvent such as petroleum ether, chloroform, ethyl acetate, acetone, methanol, ethanol or water at 80-120 deg.CoExtracting under reflux for 2-5 times (each for 2-8 hr), mixing extractive solutions, and concentrating to obtain extract. During soaking or hot reflux, ultrasonic or microwave extraction may be adopted, and the solvent amount is 5-25 times of the weight of the soaked medicine residue.
An antimalarial agent comprises an extract of Sophora japonica and conventional adjuvants.
A pharmaceutical composition comprises a therapeutically effective amount of Sophora japonica extract and a pharmaceutically acceptable carrier.
Use of Sophora japonica extract in preparing antimalarial agent is provided.
The invention relates to a pharmaceutical composition for resisting malaria, which contains a pagodatree extract and a pharmaceutically acceptable carrier.
The pharmaceutically acceptable carrier in the pharmaceutical composition of the invention refers to a conventional pharmaceutical carrier in the pharmaceutical field. The extract of Sophora japonica according to the present invention may be administered in the form of a composition to a patient in need of such treatment by oral, nasal inhalation, rectal or parenteral administration. For oral administration, it can be made into conventional solid preparations such as tablet, powder, granule, capsule, etc., and liquid preparations such as oil suspension, syrup, elixir, etc.; for parenteral administration, it can be made into solution for injection, etc. Preferred forms are tablets, capsules and injections.
Various dosage forms of the pharmaceutical composition of the present invention can be prepared according to conventional production methods in the pharmaceutical field. For example, the active ingredient may be combined with one or more carriers and then formulated into the desired dosage form.
The pharmaceutical compositions of the present invention preferably contain 0.1% to 99.5% by weight of the active ingredient, most preferably 0.5% to 95% by weight of the active ingredient.
The administration amount of the Sophora japonica extract of the present invention may vary depending on the route of administration, age, weight of the patient, type and severity of the disease to be treated, etc., and the daily dose thereof may be 0.1 to 100 mg/kg of body weight, preferably 0.5 to 50 mg/kg of body weight. One or more administrations may be carried out.
The sophora japonica extract of the invention shows better antimalarial activity.
The invention screens the anti-malarial activity of the pagodatree extract, and the pagodatree extract shows better anti-malarial activity. In antimalarial applications, the Sophora japonica extract is applied to a substrate or a population in an amount ranging from 0.01 to 30 g, preferably from 0.03 to 10 g, optionally in association with a carrier and/or vehicle.
The specific implementation mode is as follows:
the following examples are provided to further illustrate the essence of the present invention, which will enable a person skilled in the art to more fully understand the invention, but are not intended to limit the invention in any way.
Example 1:
the preparation of the pagodatree extract of the invention comprises the following steps:
pulverizing dried aerial parts 118 g of Sophora japonica into 30 mesh powder, adding 75% ethanol at 95%oExtracting under reflux for 3 times (2 hr each time) under C condition, mixing extractive solutions, and concentrating under reduced pressure to obtain extract 28.1 g with extraction rate of 23.8%.
Example 2:
the antimalarial activity of the extract of the invention is detected:
adopting an international 4-day inhibition experiment method, 1 × 10 percent of the total amount of the active ingredients is inoculated into the abdominal cavity of each mouse7Inoculating plasmodium into erythrocyte, administering intragastrically after 3 hr, and administering once every 24 hr for 4 days (day of inoculation is D)0The next day is D1And so on) at day 5 (D)4) The tail vein was bled, filmed, fixed with methanol, stained by mixed staining with Wright-Giemsa (Wright-Giemsa), and observed under a 10 × 100 microscope under oil microscope. If no plasmodium aneuploid is found after randomly checking 50 visual fields, judging the result as negative, randomly counting 5 visual fields of positive blood film sheet, and calculating plasmodium inhibition according to the following formulaAnd (4) rate.
Plasmodium infection rate (%). The total number of erythrocytes/erythrocytes x 100% that infected plasmodium
Plasmodium inhibition (%) (mean control mean infection ‒ sample group mean infection)/control mean infection ] × 100%
The activity data are shown in Table 1.
TABLE 1 anti-malarial Activity data of Sophora japonica extract: (n = 4)
Figure DEST_PATH_IMAGE002

Claims (7)

1. A preparation method of a pagodatree extract is characterized in that overground parts or whole plants of pagodatree plants are directly extracted by using organic solvents of petroleum ether, chloroform, ethyl acetate, acetone, methanol, ethanol or water through cold immersion or hot reflux to obtain an extracting solution, and the extracting solution is concentrated and dried to obtain the pagodatree extract.
2. The method for preparing the extract as claimed in claim 1, wherein the aerial parts or whole plants of the Sophora japonica plant are dried, pulverized to 30 mesh, extracted with organic solvent petroleum ether or chloroform or ethyl acetate or acetone or methanol or ethanol or water at room temperature, and the extract is concentrated to obtain extract.
3. The method for preparing the extract as claimed in claim 1, wherein the aerial parts or whole plants of the Sophora japonica plant are dried, pulverized to 30 mesh, extracted by organic solvent petroleum ether or chloroform or ethyl acetate or acetone or methanol or ethanol under hydrothermal reflux, and the extract is concentrated to obtain extract.
4. The method according to claims 2 and 3, wherein the soaking or thermal refluxing is assisted by ultrasonic or microwave extraction, and the amount of solvent used each time is 5-25 times the weight of the soaked herb residue.
5. A pharmaceutical composition comprising a therapeutically effective amount of the extract of claim 1 and a pharmaceutically acceptable carrier.
6. An antimalarial agent comprising the extract of claim 1 and conventional adjuvants.
7. Use of the extract of claim 1 for the preparation of an antimalarial agent.
CN202011557132.6A 2020-12-25 2020-12-25 Sophora japonica extract, preparation method of pharmaceutical composition of extract and antimalarial application of extract Pending CN112426446A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113115798A (en) * 2021-04-23 2021-07-16 北京农学院 Application of Chinese scholartree in biological control, biological control medicament and preparation method thereof

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
张兰军等: "槐属植物的化学成分及药理活性研究进展", 《云南民族大学学报(自然科学版)》 *
张奇文主编: "《中国膏敷疗法》", 31 January 2018, 中国医药科技出版社 *
方立生主编: "《<本草纲目>秘方全书:典藏精品版》", 31 August 2012, 黑龙江科学技术出版社 *
董小青等: "3种乔木树皮及枝叶提取物体外抑菌活性分析", 《武警后勤学院学报(医学版)》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113115798A (en) * 2021-04-23 2021-07-16 北京农学院 Application of Chinese scholartree in biological control, biological control medicament and preparation method thereof
CN113115798B (en) * 2021-04-23 2022-03-29 北京农学院 Application of Chinese scholartree in biological control, biological control medicament and preparation method thereof

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