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WO1995031993A1 - Extrait de plantes du genre taxus et son utilisation - Google Patents

Extrait de plantes du genre taxus et son utilisation Download PDF

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Publication number
WO1995031993A1
WO1995031993A1 PCT/CN1995/000045 CN9500045W WO9531993A1 WO 1995031993 A1 WO1995031993 A1 WO 1995031993A1 CN 9500045 W CN9500045 W CN 9500045W WO 9531993 A1 WO9531993 A1 WO 9531993A1
Authority
WO
WIPO (PCT)
Prior art keywords
extract
yew
anticancer
taxus
solvent
Prior art date
Application number
PCT/CN1995/000045
Other languages
English (en)
Chinese (zh)
Inventor
Ming Guo
Original Assignee
Ming Guo
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ming Guo filed Critical Ming Guo
Priority to AU25210/95A priority Critical patent/AU2521095A/en
Publication of WO1995031993A1 publication Critical patent/WO1995031993A1/fr

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Classifications

    • 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
    • A61K36/13—Coniferophyta (gymnosperms)

Definitions

  • the present invention relates to a Taxus plant extract and a preparation method and application thereof. More specifically, the present invention relates to an extract obtained from the bark, root, and / or stem and leaf of a Taxus plant. Its preparation method and its application as an anticancer drug.
  • paclitaxel has excellent anti-cancer activity
  • the United States FDA has approved the treatment of ovarian cancer in December 1992, but due to limited resources of Taxus in the United States, and the total amount of paclitaxel in its skin is less than 0.02% Coupled with the difficulty of extraction and separation, the amount of pure paclitaxel obtained is very small, so its price is quite expensive and it has not been possible to expand its application. People have been pinning their hopes on chemical synthesis, but so far they have not advised. Disclosure of invention
  • One of the objects of the present invention is to provide an extract from a yew plant and a preparation method thereof.
  • Another object of the present invention is to provide an extract which combines the extract and can be widely used. Anticancer drug composition and preparation method thereof.
  • the present invention provides a yew plant extract, which is characterized by:
  • the extract has excellent anticancer activity.
  • the extract of the present invention is extracted from the bark, roots, stems and leaves of a yew plant, or a mixture thereof by a specific method.
  • the yew plants include plants of all species of the yew family, such as yew yunnan, yew tibet, yew southern, yew northeast, yew chinese, yew european, yew Pacific , Japanese yew and yew. Yunnan yew, yew tibet and yew pacific are preferred.
  • the anticancer active ingredient incorporated in the extract of the present invention includes two parts, known and unknown.
  • the known part includes all effective compounds that have been isolated so far. Examples of representative compounds are: Taxol, Paclitaxel B (cephalmanine), Yunnaxane, and Taxus yunanensi) and so on.
  • the unknown section includes all active compounds that have not yet been isolated and discovered.
  • the extract of the invention has excellent anti-cancer activity.
  • the hair was measured by a standard method
  • the extract of Ming Ming has a concentration of 0.01, 0.1, 1, 10 and 100 g / ml against nasopharyngeal squamous carcinoma cell line (KB), cervical squamous carcinoma cell line (Hela), and gastric adenocarcinoma cell line (MGC80- 3)
  • Surviving cancer cells were picked up 48 hours after drug action, and the percentage inhibition rate was calculated. The results are shown in Table 1 (the average of the three results).
  • the extract of the present invention has the following advantages over paclitaxel:
  • the extraction rate is 100 times higher than that of paclitaxel, which can not only save resources, but also provide a large number of drugs conveniently;
  • paclitaxel must be higher than 97%, and its total amount in yew plants is less than 0.02%. It is quite difficult to meet the requirements of clinical application; and the extract of the present invention only requires paclitaxel binding amount of not less than 2.25%, and anticancer activity of the present invention thus extracts a low binding amount of 97% paclitaxel equivalent paclitaxel (taxol
  • the solubility of the extract of the present invention is significantly better than that of paclitaxel.
  • the present invention also provides a method for preparing an extract of Taxus spp., Which comprises fully extracting the bark, roots, and / or stems and leaves of Taxus spp. With a solvent, then evaporating the solvent, and performing necessary treatment on the obtained residue, An extract of the present invention is prepared.
  • the solvents include: ice; aliphatic hydrocarbons, such as hexane, cyclohexane, petroleum ether, etc .; aromatic hydrocarbons, such as benzene, toluene, xylene, etc .; halogenated hydrocarbons, such as dichloromethane, chloroform, and tetrachloride.
  • the extraction solvent used in the method of the present invention can be arbitrarily selected as long as it can sufficiently extract the anti-cancer active ingredients. Taxus bark, roots and / or stems and leaves are preferably crushed into
  • the method of the invention comprises the following steps:
  • Another aspect of the present invention is to provide an anti-cancer pharmaceutical composition
  • an anti-cancer pharmaceutical composition comprising an anti-cancer effective amount of the Taxus plant extract of the present invention and a pharmaceutically acceptable carrier.
  • the invention also provides a method for preparing an anticancer pharmaceutical composition of the invention, which method comprises dispersing an effective amount of the extract of the invention in a pharmaceutically acceptable carrier.
  • Pharmaceutically acceptable carriers refer to all non-toxic solid, semi-solid and liquid diluents or excipients commonly used in pharmacy that do not adversely affect the extracts of the invention. Examples of them include-water, ethanol, ethylene glycol, propanol, glycerol, polyethylene glycol, peanut oil, castor oil, sorbitol, starch, retinoid cellulose, sodium carboxymethyl cellulose, talc, etc., or they mixture.
  • a lubricant In the pharmaceutical composition of the present invention, a lubricant, a disintegrant, a flavoring agent, a pigment, a solubilizer, a dispersant, an emulsifier, a surfactant, a pH adjuster, and the like may be added.
  • the pharmaceutical composition of the present invention can be formulated in the form of seed preparations commonly used in the pharmaceutical field, and examples thereof include tablets, powders, granules, soft or hard gelatin capsules, pills, lozenges, suppositories, emulsions, soluble waves or Among them, injections are preferred.
  • the pharmaceutical composition of the present invention can be used for preventing and treating various cancers, such as ovarian cancer, breast cancer, endometrial cancer, colon cancer and the like.
  • the pharmaceutical composition of the present invention can be administered orally or parenterally, preferably parenterally, such as intravenously.
  • the dosage used is based on the patient's age, gender, response to the drug, and severity of the condition.
  • the daily dose for adults is usually 10 mg ⁇ : LOOOmg, preferably 100mg ⁇ 500mg.
  • the paste was extracted with a mixture of 19 kg of water and 19 kg of dichloromethane.
  • the organic layer was separated and the dichloromethane was evaporated to give a residual solid.
  • the solid was washed with 1.2 kg of n-hexane and 1.2 kg of methanol, respectively.
  • the residue was dissolved in dichloromethane, filtered, and the filtrate was evaporated.
  • the remaining yellow-brown solid was extracted with ether and ethyl acetate. and acetic acid - ethyl extracts were evaporated to give 250g and 300g respectively yellow powdery solid, which is the combined extract of the present invention, a total of 5 5 0g, the extraction rate of 1.10% (by weight of crude drug).
  • the pharmaceutical composition tablet of the present invention is prepared with the following ingredients:
  • Talcum powder 1 lOOmg The extract, starch and retinoid cellulose were sieved through a 4 5 mesh sieve and thoroughly mixed. The water-soluble waves of polyvinyl alkane were mixed with it, and then passed through a 14 mesh sieve. The obtained granules were 50-6 (18 after TC drying). added to the granules after mesh screen. carboxymethyl starch, talc, magnesium stearate through a 60 mesh sieve and, after mixing, are compressed tablets, each weighing lOOmg, wherein the co-extract 20m g.

Landscapes

  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Medicinal Chemistry (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne un extrait d'écorces, de racines et de tiges et/ou de feuilles de plantes du genre Taxus ainsi qu'une composition pharmaceutique anticancéreuse contenant ledit extrait.
PCT/CN1995/000045 1994-05-24 1995-05-22 Extrait de plantes du genre taxus et son utilisation WO1995031993A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU25210/95A AU2521095A (en) 1994-05-24 1995-05-22 The extract from plants of the genus taxus and use thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN94106189.2 1994-05-24
CN 94106189 CN1112433A (zh) 1994-05-24 1994-05-24 红豆杉属植物提取物及其应用

Publications (1)

Publication Number Publication Date
WO1995031993A1 true WO1995031993A1 (fr) 1995-11-30

Family

ID=5032425

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN1995/000045 WO1995031993A1 (fr) 1994-05-24 1995-05-22 Extrait de plantes du genre taxus et son utilisation

Country Status (3)

Country Link
CN (1) CN1112433A (fr)
AU (1) AU2521095A (fr)
WO (1) WO1995031993A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6136989A (en) * 1998-12-30 2000-10-24 Phytogen Life Sciences, Incorporated Method for high yield and large scale extraction of paclitaxel from paclitaxel-containing material

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101716197B (zh) * 2009-12-30 2012-02-01 宁波泰康红豆杉生物工程有限公司 一种南方红豆杉叶片的提取物及制备方法
CN109662916B (zh) * 2019-02-26 2022-01-04 浙江中医药大学 一种具有抗菌消炎作用的纳米级身体乳及其生产方法

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS596880A (ja) * 1982-07-06 1984-01-13 Hiroshi Isono イチイの果実に含まれている諸成分の抽出法及びその利用方法
WO1992007842A1 (fr) * 1990-11-02 1992-05-14 University Of Florida Procede d'isolement et de purification de derives de taxane
WO1992018492A1 (fr) * 1991-04-19 1992-10-29 The University Of Mississippi Procede et compositions servant a l'isolation de taxanes
EP0553780A1 (fr) * 1992-01-31 1993-08-04 INDENA S.p.A. Procédé pour l'extraction du taxol et de ses dérivés des plantes du genre Taxus
CN1076695A (zh) * 1992-03-06 1993-09-29 因迪纳有限公司 浆果赤霉素iii的衍生物
US5279949A (en) * 1992-12-07 1994-01-18 Board Of Trustees Operating Michigan State University Process for the isolation and purification of taxol and taxanes from Taxus spp
CN1085551A (zh) * 1992-10-05 1994-04-20 罗纳-布朗克罗莱尔股份有限公司 10-脱乙酰基浆果赤霉素iii制造方法
CN1085552A (zh) * 1992-10-05 1994-04-20 罗纳-布朗克罗莱尔股份有限公司 10-脱乙酰基浆果赤霉素iii制造方法
JPH06157329A (ja) * 1992-11-19 1994-06-03 Mitsui Toatsu Chem Inc タキソール類含有レジンの効率的な抽出方法

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS596880A (ja) * 1982-07-06 1984-01-13 Hiroshi Isono イチイの果実に含まれている諸成分の抽出法及びその利用方法
WO1992007842A1 (fr) * 1990-11-02 1992-05-14 University Of Florida Procede d'isolement et de purification de derives de taxane
WO1992018492A1 (fr) * 1991-04-19 1992-10-29 The University Of Mississippi Procede et compositions servant a l'isolation de taxanes
EP0553780A1 (fr) * 1992-01-31 1993-08-04 INDENA S.p.A. Procédé pour l'extraction du taxol et de ses dérivés des plantes du genre Taxus
CN1076695A (zh) * 1992-03-06 1993-09-29 因迪纳有限公司 浆果赤霉素iii的衍生物
CN1085551A (zh) * 1992-10-05 1994-04-20 罗纳-布朗克罗莱尔股份有限公司 10-脱乙酰基浆果赤霉素iii制造方法
CN1085552A (zh) * 1992-10-05 1994-04-20 罗纳-布朗克罗莱尔股份有限公司 10-脱乙酰基浆果赤霉素iii制造方法
JPH06157329A (ja) * 1992-11-19 1994-06-03 Mitsui Toatsu Chem Inc タキソール類含有レジンの効率的な抽出方法
US5279949A (en) * 1992-12-07 1994-01-18 Board Of Trustees Operating Michigan State University Process for the isolation and purification of taxol and taxanes from Taxus spp

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ACTA PHARMACEUTICA SINICA, (1990), 25(3), CHENG et al., pages 227-240. *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6136989A (en) * 1998-12-30 2000-10-24 Phytogen Life Sciences, Incorporated Method for high yield and large scale extraction of paclitaxel from paclitaxel-containing material

Also Published As

Publication number Publication date
CN1112433A (zh) 1995-11-29
AU2521095A (en) 1995-12-18

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