DE4117854A1 - Lipoxygenase inhibiting Celastroloid(s) - used for treating rheumatism, malaria, tumours or bacterial infection - Google Patents
Lipoxygenase inhibiting Celastroloid(s) - used for treating rheumatism, malaria, tumours or bacterial infectionInfo
- Publication number
- DE4117854A1 DE4117854A1 DE4117854A DE4117854A DE4117854A1 DE 4117854 A1 DE4117854 A1 DE 4117854A1 DE 4117854 A DE4117854 A DE 4117854A DE 4117854 A DE4117854 A DE 4117854A DE 4117854 A1 DE4117854 A1 DE 4117854A1
- Authority
- DE
- Germany
- Prior art keywords
- pristimer
- celastroloid
- use according
- malaria
- celastroloids
- 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- Withdrawn
Links
- 201000004792 malaria Diseases 0.000 title claims abstract description 6
- 208000035143 Bacterial infection Diseases 0.000 title claims description 4
- 102000003820 Lipoxygenases Human genes 0.000 title description 2
- 108090000128 Lipoxygenases Proteins 0.000 title description 2
- 206010028980 Neoplasm Diseases 0.000 title 1
- 208000022362 bacterial infectious disease Diseases 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- JFACETXYABVHFD-WXPPGMDDSA-N Pristimerin Chemical compound CC1=C(O)C(=O)C=C2[C@@](CC[C@]3(C)[C@]4(C)CC[C@@]5(C)CC[C@@](C[C@H]53)(C)C(=O)OC)(C)C4=CC=C21 JFACETXYABVHFD-WXPPGMDDSA-N 0.000 claims abstract description 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 11
- 239000003814 drug Substances 0.000 claims abstract description 11
- JFACETXYABVHFD-UHFFFAOYSA-N pristimerine Natural products CC1=C(O)C(=O)C=C2C(CCC3(C)C4(C)CCC5(C)CCC(CC53)(C)C(=O)OC)(C)C4=CC=C21 JFACETXYABVHFD-UHFFFAOYSA-N 0.000 claims abstract description 10
- 201000010099 disease Diseases 0.000 claims description 10
- FMPJNBPZCVETGY-UHFFFAOYSA-N Pristimerinen Natural products C12=CC=C3C(C)=C(O)C(=O)C=C3C2=C(C)CC2(C)C1(C)CCC1(C)CCC(C(=O)OC)(C)CC12 FMPJNBPZCVETGY-UHFFFAOYSA-N 0.000 claims description 7
- IXWGHMMOEFOOFA-UHFFFAOYSA-N pristimerin Natural products COC(=O)C1(C)CCC2(C)CCC3(C)C4CC=C5C(=C(O)C(=O)C=C5C4(C)CCC3(C)C2C1)C IXWGHMMOEFOOFA-UHFFFAOYSA-N 0.000 claims description 7
- 229940126601 medicinal product Drugs 0.000 claims description 5
- 150000003648 triterpenes Chemical class 0.000 claims description 4
- 230000005764 inhibitory process Effects 0.000 abstract description 6
- 210000004698 lymphocyte Anatomy 0.000 abstract description 5
- 230000009466 transformation Effects 0.000 abstract description 3
- 230000000118 anti-neoplastic effect Effects 0.000 abstract description 2
- 230000003115 biocidal effect Effects 0.000 abstract description 2
- 238000010790 dilution Methods 0.000 abstract description 2
- 239000012895 dilution Substances 0.000 abstract description 2
- 230000001629 suppression Effects 0.000 abstract description 2
- 239000003904 antiprotozoal agent Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 description 5
- AZQWKYJCGOJGHM-UHFFFAOYSA-N para-benzoquinone Natural products O=C1C=CC(=O)C=C1 AZQWKYJCGOJGHM-UHFFFAOYSA-N 0.000 description 3
- 239000002026 chloroform extract Substances 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 241000953815 Geositta maritima Species 0.000 description 1
- 201000005569 Gout Diseases 0.000 description 1
- 208000025747 Rheumatic disease Diseases 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000000842 anti-protozoal effect Effects 0.000 description 1
- 230000003356 anti-rheumatic effect Effects 0.000 description 1
- 229940034982 antineoplastic agent Drugs 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- LGRLWUINFJPLSH-UHFFFAOYSA-N methanide Chemical compound [CH3-] LGRLWUINFJPLSH-UHFFFAOYSA-N 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 239000000419 plant extract Substances 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 230000000552 rheumatic effect Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Emergency Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (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
Description
Erkrankungen des rheumatoiden Formenkreises werden nach und nach zur Volkskrankheit Nr. 1. Hierunter zu sub sumieren sind Erkrankungen wie Rheuma, Athritis, ent zündliche Athrose, rheumatisch bedingte Bewegungsein schränkungen, Wirbelsäulenbeschwerden, Sinusithis sowie Gicht. Erkrankungen des rheumatoiden Formenkreises führen abhängig vom Intensitätsgrad der Erkrankung zu starken Schmerz- und Behinderungszuständen bis hin zur vollständigen Invalidität. Die soziale Bedeutung des Rheumatismus ist sehr groß. Die jährlich durch Rheumatismus ausfallenden Arbeitstage werden auf mindestens 1-2 je Beschäftigten geschätzt. Bestimmte Berufe (z. B. Bergleute, Preßluftarbeiter, Fischer) sind besonders bedroht. Die vorzeitigen Pensionierungen wegen Rheumatismus werden auf 19-25% der Frühpensionierungen geschätzt. In Anbetracht dessen ist man bestrebt, das Problem Rheumatismus durch Vorbeugungs-, Heil- und Kur maßnahmen so gut es geht zu beherrschen. Dennoch ist es unter Umständen nicht zu vermeiden, daß besonders akute Fälle medikamentös behandelt werden müssen. Man greift hier regelmäßig auf hochwirksame Drogen z. B. von Corticosteroiden zurück, welche jedoch bekanntermaßen beträchtliche Nebenwirkungen mit sich bringen.Diseases of the rheumatoid form are regressed and after to the widespread disease No. 1. Below to sub add up are diseases such as rheumatism, athritis, ent inflammatory osteoarthritis, rheumatic movement restrictions, spinal complaints, sinusithis as well Gout. Rheumatoid diseases lead depending on the degree of intensity of the disease severe pain and disability up to complete disability. The social importance of Rheumatism is very big. The annually by Working days that fail rheumatism are on estimated at least 1-2 per employee. Certain Professions (e.g. miners, compressed air workers, fishermen) particularly threatened. The early retirement because of Rheumatism is on 19-25% of early retirement estimated. In view of this, one strives to do that Problem of rheumatism through preventive, curative and cure mastering measures as best as possible. Still it is under certain circumstances not to be avoided that particularly acute Cases need to be treated with medication. You grab here regularly on highly effective drugs such. B. from Corticosteroids return, which however are known bring considerable side effects.
Aufgabe der vorliegenden Erfindung besteht darin, neue Möglichkeiten der medikamentösen Behandlung von Rheumatismus aufzuzeigen. The object of the present invention is to create new ones Possibilities of drug treatment of To show rheumatism.
Diese Aufgabe wird durch die Verwendung mindestens eines Celastroloids als Bestandteil d. h. als wirksamer Be standteil eines Arzneimittels zur Behandlung von Rheumatismus bzw. Erkrankungen des rheumatoiden Formen kreises gelöst. Eine sehr genaue Beschreibung der sog. Celastroloide ist in der Zeitschrift "Phytochemistry, 1978, Band 17, Seiten 1821-1858 zu finden. Es handelt sich hierbei um pentazyklische Triterpene mit Glutinan- Grundgerüst, die als strukturelle Gemeinsamkeit ein konjugiertes 10 π-System mit einem Chinonmethidteil in den Ringen A und B besitzen. Der Einfachheit halber wird auf die vorstehend bezeichnete Literaturstelle vollinhaltlich Bezug genommen.This task is accomplished by using at least one Celastroloids as part of d. H. as an effective Be component of a medicinal product for the treatment of Rheumatism or diseases of the rheumatoid forms circle solved. A very precise description of the so-called Celastroloide is in the journal "Phytochemistry, 1978, volume 17, pages 1821-1858. It deals pentacyclic triterpenes with glutinane Basic framework that as a structural commonality conjugated 10 π system with a quinone methide part in have rings A and B. For the sake of simplicity to the reference cited above fully referenced.
Die Durchführung von pharmakologischen Tests hat nun gezeigt, daß die Celastroloide bei unterschiedlichen pharmakologischen Tests positive Wirkungen aufweisen bzw. bei Pflanzenextrakten, die nachweislich Celastroloide enthalten, eine antirheumatische Wirkung festgestellt werden konnte.The implementation of pharmacological tests has now shown that the celastroloids at different pharmacological tests have positive effects or with plant extracts that are proven Celastroloids contain an anti-rheumatic effect could be determined.
Zweckmäßigerweise wird als Bestandteil des Arzneimittels das Pristimerin aus der Reihe der Celastroloide zur Behandlung von Erkrankungen des rheumatoiden Formen kreises, insbesondere Rheumatismus verwendet.It is expedient to use it as part of the drug the pristimer from the series of Celastroloids Treatment of diseases of the rheumatoid forms circle, especially rheumatism used.
Alternativ dazu ist auch ein Pristimerin-Analogon ins besondere ein um eine chromophore Gruppe erweitertes Pristimerin als Bestandteil für ein Arzneimittel zur Behandlung des oben genannten Art einzusetzen.Alternatively, a pristimerin analog is ins in particular a chromophore group Pristimerin as an ingredient in a medicinal product Treatment of the type mentioned above.
Zweckmäßigerweise ist als Pristimerin-Analogon eine Triterpen-Chinonmethid vorgesehen, welches gegenüber Pristimerin einen um eine Doppelbindung erweiterten Chromophor besitzt. Appropriately as a pristimer analogue Triterpene quinone methide is provided, which is opposite Pristimerin one extended by a double bond Chromophore owns.
Desweiteren wurde gefunden, daß die eingangs erwähnten Stoffe auch als Bestandteil für ein Arzneimittel zur Behandlung von Malaria Wirksamkeit besitzen sowie anti neoplastische, antibiotische und antiprotozoische Eigen schaften aufweisen. Sie besitzen dehalb als Bestandteil von Arzneimittel zur Behandlung von tumorösen und bakteriellen Erkrankungen ebenfalls Wirksamkeit.Furthermore, it was found that the aforementioned Substances also as an ingredient for a medicinal product Treat malaria efficacy as well as anti neoplastic, antibiotic and antiprotozoal properties have shafts. They therefore have a component of drugs for the treatment of tumorous and bacterial diseases also effectiveness.
Celastroloide und insbesondere Pristimerin sowie das eingangs beschriebene Pristimerin-Analogon lassen sich mit Hilfe des sog. Chloroform-Extrakts beispielsweise aus der Rinde von Pflanzen isolieren, welche Celastroloide enthalten. Solche Pflanzen sind ebenfalls in der eingangs erwähnten Veröffentlichung angegeben.Celastroloids and especially pristimerine as well as that Pristimerin analog described above can be with the help of the so-called chloroform extract, for example isolate from the bark of plants which Celastroloids included. Such plants are also stated in the publication mentioned at the beginning.
Die isolierten Celastroloide wurden einem Lipoxygenase- Test sowie einem Lymphozyten-Transformations-Test unter zogen. Folgende Ergebnisse wurden erzielt:The isolated celastroloids were subjected to a lipoxygenase Test as well as a lymphocyte transformation test pulled. The following results were achieved:
1. Lipoxigenase-Test
Wirksamkeit zeigten:
a. Chloroform-Extrakt mit Celastroloiden
(19,2 µg/ml: 56,3% Hemmung)
b. Celastroloid-Anreicherung (ca. 80%)
(9,6 µg/ml: 94,2% Hemmung)1. Lipoxigenase test
Efficacy showed:
a. Chloroform extract with celastroloids (19.2 µg / ml: 56.3% inhibition)
b. Celastroloid enrichment (approx. 80%) (9.6 µg / ml: 94.2% inhibition)
2. Lymphozyten-Transformations-Test
Supression der Lymphozyten bis zu einer Verdünnung
von 100 ng/ml:
a. Pristimerin 100 ng/ml: 84,8% Hemmung
b. Celastroloid II 100 ng/ml: 92,4 Hemmung.2. Lymphocyte transformation test
Lymphocyte suppression up to a dilution of 100 ng / ml:
a. Pristimerin 100ng / ml: 84.8% inhibition
b. Celastroloid II 100ng / ml: 92.4 inhibition.
Die Ergebnisse dieser Tests können zumindest als erstes Indiz für eine Wirksamkeit bei Rheumatismus angesehen werden.The results of these tests can at least be the first Indicated for efficacy in rheumatism will.
Claims (10)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4117854A DE4117854A1 (en) | 1991-05-31 | 1991-05-31 | Lipoxygenase inhibiting Celastroloid(s) - used for treating rheumatism, malaria, tumours or bacterial infection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4117854A DE4117854A1 (en) | 1991-05-31 | 1991-05-31 | Lipoxygenase inhibiting Celastroloid(s) - used for treating rheumatism, malaria, tumours or bacterial infection |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE4117854A1 true DE4117854A1 (en) | 1992-12-03 |
Family
ID=6432882
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE4117854A Withdrawn DE4117854A1 (en) | 1991-05-31 | 1991-05-31 | Lipoxygenase inhibiting Celastroloid(s) - used for treating rheumatism, malaria, tumours or bacterial infection |
Country Status (1)
| Country | Link |
|---|---|
| DE (1) | DE4117854A1 (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5650167A (en) * | 1995-11-16 | 1997-07-22 | Dawa Incorporated | Method and composition for treating hepatitis B |
| WO2007077203A3 (en) * | 2005-12-30 | 2007-08-30 | Consejo Superior Investigacion | Triterpenequinone and triterpenephenol derivatives and their application for the treatment of tumors and parasitic diseases |
-
1991
- 1991-05-31 DE DE4117854A patent/DE4117854A1/en not_active Withdrawn
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5650167A (en) * | 1995-11-16 | 1997-07-22 | Dawa Incorporated | Method and composition for treating hepatitis B |
| WO2007077203A3 (en) * | 2005-12-30 | 2007-08-30 | Consejo Superior Investigacion | Triterpenequinone and triterpenephenol derivatives and their application for the treatment of tumors and parasitic diseases |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8139 | Disposal/non-payment of the annual fee |