EP2035025A1 - Utilisation d'extraits ou de matières extractives des espèces de guaiacum, ces extraits ou matières extractives produisant une inhibition de la phosphodiestérase-4, et leur procédé de production - Google Patents

Utilisation d'extraits ou de matières extractives des espèces de guaiacum, ces extraits ou matières extractives produisant une inhibition de la phosphodiestérase-4, et leur procédé de production

Info

Publication number
EP2035025A1
EP2035025A1 EP07763932A EP07763932A EP2035025A1 EP 2035025 A1 EP2035025 A1 EP 2035025A1 EP 07763932 A EP07763932 A EP 07763932A EP 07763932 A EP07763932 A EP 07763932A EP 2035025 A1 EP2035025 A1 EP 2035025A1
Authority
EP
European Patent Office
Prior art keywords
guajacum
disease
extract
extracts
alcohol
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP07763932A
Other languages
German (de)
English (en)
Inventor
Matthias-Heinrich Kreuter
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Max Zeller Soehne AG
Original Assignee
Max Zeller Soehne AG
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 Max Zeller Soehne AG filed Critical Max Zeller Soehne AG
Publication of EP2035025A1 publication Critical patent/EP2035025A1/fr
Withdrawn legal-status Critical Current

Links

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
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • the present invention relates to the use of extracts or extractives from guaiacum species, which extracts or these extractives cause a phosphodiesterase-4 inhibition, and a process for their recovery.
  • the resin obtained by melting the heartwood from Guajacum officinale L. and Guajacum sanctum L. is used.
  • the resin is used to prepare preparations based on a mother tincture and liquid HAB 1 dilutions.
  • An allopathic reprocessing monograph of Commission E is based on guaiac wood; published in the Federal Gazette 76 of 23 April 1987.
  • the area of application is the supportive treatment of rheumatic complaints.
  • DE 101 31 036 A1 describes an elixir which contains per 100 grams 70 grams of an alcoholic macerate (15 vol.% Ethanol) of 50 grams of condoorango rind, 0.60 grams of guaiac wood, 0.40 grams of dandelion root with cabbage and 0 , Contains 40 grams of peppermint leaves.
  • US Pat. No. 4,774,229 claims a method for the treatment of tumors of the skin of mammals.
  • the tumors are treated topically with a novel mixture of a plant extract of the family Zygophyllaceae and a non-alkaline metal halide.
  • this invention is based on the idea that, depending on the particular concentration, highly cytotoxic salts of antimony, cadmium, copper and zinc can be converted into complexes with phenolic compounds and thus better applied for the desired applications.
  • a dry extract of plant parts of guaiac should be produced, which should be suitable for the supportive treatment of rheumatic complaints in accordance with Commission E's monograph.
  • the addition and concentration must be such that during this process, such an alcohol and water concentration is maintained that neither the gum arabic precipitates nor separate the plant extractives contained in the extract.
  • the dry extract can be obtained either by conventional spray drying, belt drying or paddle drying of the spissum extract, in particular the post-concentrated spissum extract.
  • a fluid extract which was prepared with 80 m / m% ethanol, as a moderate inhibitor of cyclooxygenase I.
  • the IC was 5 o value for COXl 30 ug / ml was found.
  • Human leukocyte elastase HLE was 50% inhibited at 60 ⁇ g / ml.
  • the release of interleukin-1 beta from human macrophages was 50% at 45 ug / ml to 'inhibited.
  • the release of interleukin-6 was 50% inhibited at 5 ⁇ g / ml.
  • the release of tumor necrosis factor- ⁇ was 50% inhibited at 7 ⁇ g / ml.
  • the dry extract prepared according to the method according to the invention was additionally tested in the pharmacological in vitro test system of human phosphodiesterase-5, abbreviated to PDE5, to find out whether the extract has a specificity for one of the phosphodiesterases.
  • dry extracts prepared according to the invention apparently inhibit phosphodiesterase-4, and apparently contain at least one extractive agent which inhibits phosphodiesterase-4.
  • Sapwood with a cut size of about 1 mm to about 2 mm of Guajacum sanctum L. were extracted at a temperature between 30 0 C and 45 ° C for 2 hours with a mixture of 80 parts by weight of ethanol and 20 parts by weight of water with stirring.
  • the weight ratio of drug to extractant mixture was 1: 7.
  • the drug thus extracted was separated by stratified filtration.
  • the remaining portion of the fluid extract was continuously added to the evaporator until the entire amount of the fluid extract was drawn in and concentrated.
  • the spissum extract thus obtained had a light brown color, was free-flowing and of homogeneous consistency.
  • This spissum extract was concentrated under vacuum (300 mbar to 20 mbar) and elevated temperature (40 0 C to 55 ° C) to a dry matter content of 45% to 55%.
  • the resulting concentrated spissum extract (2 kg with 50% dry matter content) had a light brown color, was thick-flowing and of homogeneous consistency.
  • This post-concentrated spissum extract was dried in a dryer under vacuum at a pressure of 150 mbar to 10 mbar and a temperature of 40 ° C to 55 ° C.
  • the dry extract prepared according to the invention was dissolved in 90 v / v% ethanol and diluted so that a maximum concentration of 1 v / v% ethanol in Test system resulted.
  • the extract thus dissolved was tested for its inhibitory effect in the following concentrations, calculated on the extract without adjuvant:
  • Rolipram a specific PDE4 inhibitor
  • the dry extract prepared according to the invention was dissolved in 90 v / v% ethanol and diluted so that a maximum concentration of 1 v / v% ethanol resulted in the test system.
  • the extract thus dissolved was tested for its inhibitory effect in the following concentrations, calculated on the extract without adjuvant:
  • sildenafil a specific PDE5 inhibitor, was comparatively tested for its inhibitory effect in the following concentrations:
  • the dry extract or at least one extractant contained therein is suitable for treating diseases in which phosphodiesterase 4 inhibition is therapeutically desirable and effective is to be employed.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Microbiology (AREA)
  • Epidemiology (AREA)
  • Mycology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Biotechnology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne l'utilisation d'extraits ou de matières extractibles d'espèces de guaiacum, ces extraits ou ces matières extractibles produisant une inhibition de la phosphodiestérase-4; l'invention concerne également un procédé pour obtenir ces extraits ou matières extractibles.
EP07763932A 2006-07-05 2007-07-04 Utilisation d'extraits ou de matières extractives des espèces de guaiacum, ces extraits ou matières extractives produisant une inhibition de la phosphodiestérase-4, et leur procédé de production Withdrawn EP2035025A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH10762006 2006-07-05
PCT/CH2007/000325 WO2008003185A1 (fr) 2006-07-05 2007-07-04 Utilisation d'extraits ou de matières extractives des espèces de guaiacum, ces extraits ou matières extractives produisant une inhibition de la phosphodiestérase-4, et leur procédé de production

Publications (1)

Publication Number Publication Date
EP2035025A1 true EP2035025A1 (fr) 2009-03-18

Family

ID=37847140

Family Applications (1)

Application Number Title Priority Date Filing Date
EP07763932A Withdrawn EP2035025A1 (fr) 2006-07-05 2007-07-04 Utilisation d'extraits ou de matières extractives des espèces de guaiacum, ces extraits ou matières extractives produisant une inhibition de la phosphodiestérase-4, et leur procédé de production

Country Status (5)

Country Link
US (1) US7914827B2 (fr)
EP (1) EP2035025A1 (fr)
JP (1) JP2009541366A (fr)
KR (1) KR101170209B1 (fr)
WO (1) WO2008003185A1 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102625693B (zh) * 2009-08-26 2015-06-03 玫琳凯有限公司 包含植物提取物的局部皮肤护理配方
CN111321601B (zh) * 2020-03-16 2021-10-12 南通大学 一种防紫外竹纤维面料及其制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4774229A (en) 1982-04-05 1988-09-27 Chemex Pharmaceuticals, Inc. Modification of plant extracts from zygophyllaceae and pharmaceutical use therefor
JPS6393722A (ja) * 1986-09-22 1988-04-25 ブラディミール・バッドマージュ 医薬の処方
JPH07165597A (ja) * 1993-12-07 1995-06-27 Souyaku Gijutsu Kenkyusho:Kk ハマビシ科植物の有機抽出物を含有する抗ウイルス剤
JPH09255551A (ja) * 1996-03-28 1997-09-30 Shiseido Co Ltd 皮膚外用剤
DE10131036A1 (de) * 2001-06-29 2003-06-05 Johann Teubner Elexier gegen HIV
US20030055007A1 (en) * 2001-08-02 2003-03-20 Kazuo Sakuma Antimicrobial agents

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO2008003185A1 *

Also Published As

Publication number Publication date
KR20090026287A (ko) 2009-03-12
JP2009541366A (ja) 2009-11-26
KR101170209B1 (ko) 2012-07-31
WO2008003185A1 (fr) 2008-01-10
US7914827B2 (en) 2011-03-29
US20090142423A1 (en) 2009-06-04

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