CN113057974A - Yunnan kaki extract, its pharmaceutical composition preparation method and antimalarial application - Google Patents
Yunnan kaki extract, its pharmaceutical composition preparation method and antimalarial application Download PDFInfo
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- CN113057974A CN113057974A CN202110373874.1A CN202110373874A CN113057974A CN 113057974 A CN113057974 A CN 113057974A CN 202110373874 A CN202110373874 A CN 202110373874A CN 113057974 A CN113057974 A CN 113057974A
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- 238000002360 preparation method Methods 0.000 title claims abstract description 12
- 239000003430 antimalarial agent Substances 0.000 title claims abstract description 11
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 11
- 230000000078 anti-malarial effect Effects 0.000 title abstract description 9
- 244000236655 Diospyros kaki Species 0.000 title abstract description 3
- 235000008597 Diospyros kaki Nutrition 0.000 title abstract description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims abstract description 21
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 20
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims abstract description 18
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims abstract description 18
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims abstract description 12
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims abstract description 12
- 239000003960 organic solvent Substances 0.000 claims abstract description 6
- 239000003208 petroleum Substances 0.000 claims abstract description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 5
- 238000010992 reflux Methods 0.000 claims description 6
- 238000000034 method Methods 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 4
- 239000002671 adjuvant Substances 0.000 claims description 2
- 238000000874 microwave-assisted extraction Methods 0.000 claims description 2
- 238000002791 soaking Methods 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 238000002137 ultrasound extraction Methods 0.000 claims description 2
- 238000007654 immersion Methods 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 abstract description 17
- 241000196324 Embryophyta Species 0.000 abstract description 12
- 239000004480 active ingredient Substances 0.000 abstract description 8
- 240000005546 Piper methysticum Species 0.000 abstract description 7
- 235000016787 Piper methysticum Nutrition 0.000 abstract description 7
- 239000003814 drug Substances 0.000 abstract description 3
- 239000000203 mixture Substances 0.000 abstract description 3
- 229940079593 drug Drugs 0.000 abstract description 2
- 239000000758 substrate Substances 0.000 abstract description 2
- 229940126680 traditional chinese medicines Drugs 0.000 abstract description 2
- 239000003981 vehicle Substances 0.000 abstract description 2
- 229930192500 bigelovii Natural products 0.000 description 8
- 241000224016 Plasmodium Species 0.000 description 6
- 239000000243 solution Substances 0.000 description 5
- 210000003743 erythrocyte Anatomy 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 4
- 235000004871 Osmanthus yunnanensis Nutrition 0.000 description 3
- 241001350159 Osmanthus yunnanensis Species 0.000 description 3
- 208000015181 infectious disease Diseases 0.000 description 3
- 201000004792 malaria Diseases 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 238000010298 pulverizing process Methods 0.000 description 3
- 244000025254 Cannabis sativa Species 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000007911 parenteral administration Methods 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 230000000007 visual effect Effects 0.000 description 2
- 241000207965 Acanthaceae Species 0.000 description 1
- 241000208327 Apocynaceae Species 0.000 description 1
- 208000006820 Arthralgia Diseases 0.000 description 1
- 241001071161 Asclepias Species 0.000 description 1
- 208000010392 Bone Fractures Diseases 0.000 description 1
- 206010017076 Fracture Diseases 0.000 description 1
- 208000032843 Hemorrhage Diseases 0.000 description 1
- 241001290728 Pseuderanthemum Species 0.000 description 1
- 241000730303 Pseuderanthemum graciliflorum Species 0.000 description 1
- 208000025747 Rheumatic disease Diseases 0.000 description 1
- 206010053476 Traumatic haemorrhage Diseases 0.000 description 1
- 210000000683 abdominal cavity Anatomy 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 208000036878 aneuploidy Diseases 0.000 description 1
- 231100001075 aneuploidy Toxicity 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 229960003677 chloroquine Drugs 0.000 description 1
- WHTVZRBIWZFKQO-UHFFFAOYSA-N chloroquine Chemical compound ClC1=CC=C2C(NC(C)CCCN(CC)CC)=CC=NC2=C1 WHTVZRBIWZFKQO-UHFFFAOYSA-N 0.000 description 1
- 239000012059 conventional drug carrier Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- -1 etc. Substances 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 238000011081 inoculation Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000002398 materia medica Substances 0.000 description 1
- 239000012053 oil suspension Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000000552 rheumatic effect Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 230000008736 traumatic injury Effects 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/19—Acanthaceae (Acanthus family)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation 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
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation 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
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/331—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using water, e.g. cold water, infusion, tea, steam distillation or decoction
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation 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
- A61K2236/30—Extraction of the material
- A61K2236/35—Extraction with lipophilic solvents, e.g. Hexane or petrol ether
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation 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
- A61K2236/30—Extraction of the material
- A61K2236/39—Complex extraction schemes, e.g. fractionation or repeated extraction steps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation 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
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/51—Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying
-
- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against 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)
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- Tropical Medicine & Parasitology (AREA)
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- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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Abstract
The invention relates to a preparation method and application of a Yunnan kaki extract and a pharmaceutical composition thereof, belonging to the pharmaceutical field of traditional Chinese medicines and natural medicines. The preparation method of the antimalarial drug taking the extract of the invention as an active ingredient comprises the steps of taking dry aboveground parts or whole plants of the Yunnan kava, crushing the dried aboveground parts or whole plants into 30 meshes, and extracting the crushed parts or whole plants with organic solvent petroleum ether, chloroform, ethyl acetate, acetone, methanol, ethanol or water. The invention relates to an application of a Yunnan kava bone extract in preparing an antimalarial agent, which 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 develops the medicinal value of the Yunnan kam bone.
Description
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 Yunnan kava bone extract, a medicinal composition taking the extract as an active ingredient, and application of the extract in an antimalarial agent.
Technical background:
yunan mountain shell bone [ Yunan ]Pseuderanthemum graciliflorum (Nees) Ridl.]Is of the genus Asclepiadaceae (Acanthaceae) Asclepias: (Pseuderanthemum) Plants, half-shrubs or shrubs, up to 3 meters, under forest or in brush; southern Yunnan, Guangxi, Guizhou, and India (east Himalayan region), Central and south peninsula to Malaysia, and so on. According to records of Chinese materia medica, the root of the common plant of the Yunnan kava has the efficacies of removing blood stasis, reducing swelling and stopping bleeding, and is used for treating traumatic injury, fracture, traumatic bleeding and the like; haikang hooked meadow (Haikang grass of Henry weed) (Haikang grass of Henry weed)P. haikangenseC.Y. Wu et Lo) has the effects of clearing and activating the channels and collaterals, and is mainly used for treating rheumatic arthralgia and joint movement difficulty. At present, the preparation method of the extract of the pittosporum yunnanense, the pharmaceutical composition taking the extract as an active ingredient and the report of the application of the extract in resisting malaria are not seen at home and abroad.
The invention content is as follows:
the invention aims to provide a preparation method of a Yunnan mountain bigelovii bone extract, a pharmaceutical composition taking the Yunnan mountain bigelovii bone extract as an active ingredient, and application of the Yunnan mountain bigelovii bone extract in preparing an antimalarial agent.
The above object of the present invention is achieved by the following technical solutions:
a method for preparing Yunnan Shanhugu extract comprises pulverizing dried aerial parts or whole plant of Yunnan Shanhugu plant to 30 mesh, extracting with organic solvent petroleum ether, chloroform, ethyl acetate, acetone, methanol, ethanol or water at room temperature for 2-5 times (each for 12-48 hr), mixing extractive solutions, and concentrating to obtain extract. Or drying aerial parts or whole plant of Yunnan Shanhugu plant, pulverizing to 30 mesh, and extracting with organic solvent such as petroleum ether, chloroform, ethyl acetate, acetone, methanol, ethanol or water at 80-120%oExtracting 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 extract of the bones of the Yunnan mountain range and conventional adjuvants.
The pharmaceutical composition comprises a therapeutically effective amount of the extract of the pittosporum yunnanense and a pharmaceutically acceptable carrier.
Application of Yunnan mountain shell bone extract in preparing antimalarial agent is provided.
The invention relates to a pharmaceutical composition for resisting malaria, which contains Yunnan kava bone 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 the Yunnan mountain bigelovii bone of the invention can be administered in the form of a composition by oral, nasal inhalation, rectal or parenteral administration to a patient in need of such treatment. 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 amount of the extract of the Yunnan mountain bigelovii bone of the present invention to be administered may vary depending on the route of administration, the age, weight, type and severity of the disease to be treated, etc., and the daily dose thereof may be 0.1 to 100 mg/kg body weight, preferably 0.5 to 50 mg/kg body weight. One or more administrations may be carried out.
The Yunnan kava bone extract shows better antimalarial activity.
The invention screens antimalarial activity of the Yunnan mountain bigelovii extract, and the Yunnan mountain bigelovii extract shows better antimalarial activity. In antimalarial applications, the extract of the bones of the Yunnan mountain bigelovii 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 a 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 method of the Yunnan kava bone extract comprises the following steps:
pulverizing dried aerial part 117 g of Yunnan Shankhstan bone plant to 30 mesh, 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 21.3 g extract with extraction rate of 18.2%.
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 aneuploidy is found after randomly checking 50 visual fields, the judgment is negative, 5 visual fields are randomly counted on a positive blood film sheet, the total number of red blood cells is not less than 1000, and then the plasmodium inhibition rate is calculated according to the following formula.
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 antimalarial Activity of extract of pittosporum yunnanense: (n = 4）
| Sample | Dosage (mg/kg/d) | Plasmodium inhibition (%) |
| Chloroquine diphosphate | 10 | 99.5±0.3 |
| Extract of Yunnan mountain shell bone | 1000 | 25.8±17.8 |
Claims (7)
1. The preparation method of the Yunnan Shanhugu extract is characterized in that the aboveground part or the whole plant of the Yunnan Shanhugu plant is directly extracted by using an organic solvent petroleum ether or chloroform or ethyl acetate or acetone or methanol or 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 Yunnan Shanhugu extract.
2. The method for preparing the extract as claimed in claim 1, wherein the aerial parts or whole plant of the Yunnan mountain bigelow is dried, crushed 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 the extract.
3. The method for preparing the extract as claimed in claim 1, wherein the aerial parts or whole plant of the Yunnan mountain bigelow plant are dried, crushed 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.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110373874.1A CN113057974A (en) | 2021-04-09 | 2021-04-09 | Yunnan kaki extract, its pharmaceutical composition preparation method and antimalarial application |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110373874.1A CN113057974A (en) | 2021-04-09 | 2021-04-09 | Yunnan kaki extract, its pharmaceutical composition preparation method and antimalarial application |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN113057974A true CN113057974A (en) | 2021-07-02 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202110373874.1A Pending CN113057974A (en) | 2021-04-09 | 2021-04-09 | Yunnan kaki extract, its pharmaceutical composition preparation method and antimalarial application |
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| Country | Link |
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| CN (1) | CN113057974A (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112402479A (en) * | 2020-12-25 | 2021-02-26 | 大理大学 | Rhododendron rubrum extract, preparation method of pharmaceutical composition of rhododendron rubrum extract and antimalarial application of rhododendron rubrum extract |
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2021
- 2021-04-09 CN CN202110373874.1A patent/CN113057974A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112402479A (en) * | 2020-12-25 | 2021-02-26 | 大理大学 | Rhododendron rubrum extract, preparation method of pharmaceutical composition of rhododendron rubrum extract and antimalarial application of rhododendron rubrum extract |
Non-Patent Citations (1)
| Title |
|---|
| ARPRON LEESOMBUN等: "Ethanol Extracts from Thai Plants have Anti-Plasmodium and Anti-Toxoplasma Activities In Vitro", 《ACTA PARASITOLOGICA》 * |
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Application publication date: 20210702 |