Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Reexamination Certificate
1999-04-21
2001-04-17
Prats, Francisco (Department: 1651)
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
Reexamination Certificate
active
06217877
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to the plant
Parthenium integrifolium
and more specifically to pharmaceutical compositions derived from it as well as the use of
Parthenium integrifolium
or parts thereof or an extract or component thereof for the preparation of medicines for the alleviation of pain or for the treatment or prevention of inflammatory or autoimmune disorders. The invention also relates to a method of preparing an extract of
Parthenium integrifolium
and to the extracts prepared by the method.
BACKGROUND OF THE INVENTION
Parthenium integrifolium
(L.) (family Asteraceae), also commonly known as Missouri snake root, grows wild in woodland and prairies of North America. The herb is 30-130 cm high with numerous white flowerheads forming a flat inflorescence up to 25 cm wide. The root is comprised of a short, conical or bulbshaped headstem that has a diameter of up to 4 cm and elongated secondary, twisted branches leading from the headstem.
A number of chemicals have been identified as major components of
Parthenium integrifolium
extracts. One group are the sesquiterpene lactones represented by tetraneurin E and tetraneurin C. Another group are the sesquiterpene esters represented by echinadiol cinnamate, epoxy echinadiol cinnamate, echinaxanthol cinnamate and dihydroxynardol cinnamate. Yet another group are the flavonoids represented by quercetagetin methyl ethers and their O-glycosides. Another characteristic component of
Parthenium integrifolium
is pyromeconic acid. Other chemicals present in the plant are coumarins and diverse phenolic glycosides.
The German patent application, publication no. 36 38 715 A1 describes the above mentioned sesquiterpene esters derived from
Parthenium integrifolium
. According to the experimental section of that application, immunological activity tests of the sesquiterpene esters showed that they enhanced granulocyte phagocytosis in vitro up to 30%. This effect is to be considered a pro-inflammatory action related to the non-specific part of the immune system (the reticuloendothelial phagocytic system).
At present the nonsteroidal antiinflammatory drugs (NSAIDS) are the most commonly applied therapeutic agents for the treatment of conditions associated with inflammation and pain. The NSAIDs exert their action by inhibiting the prostaglandin-generating enzyme cyclooxygenase (COX). There are two biochemical subtypes of cyclooxygenase denominated COX-1 and COX-2. COX-1 is constitutively expressed in most cells and is responsible for the formation of prostaglandins which mediate important basic physiological functions, e.g. providing an intact mucosa in the ventricle. COX-2 is not normally present, but may be induced by certain serum factors, cytokines and growth factors and responsible for the formation of inflammatory prostaglandins which mediate many symptoms of inflammation. The NSAIDs are generally non-selective, meaning that they inhibit both COX-2 and COX-1 resulting in an antiinflammatory and pain relieving effect due to the inhibition of COX-2 and a number of side effects due to the inhibition of COX-l, of which gastric ulceration is one of the most important.
Autoimmune disorders like multiple sclerosis, morbus Crohn, rheumatoid arthritis, diabetes mellitus, etc. are associated with an overactivation of the inflammatory arm of the immune system (T
H
1 pathway) leading to well known symptoms and serious tissue destruction. The most well established treatment for these disorders is the management of corticosteroids which exert their action by non-selectively inhibiting the function and proliferation of different types of immune cells. Unfortunately the corticosteroids are associated with a number of serious side effects e.g. immuno-suppression and osteoporosis.
SUMMARY OF THE INVENTION
I have found that
Parthenium integrifolium
or parts thereof or an extract or component thereof exert the following pharmacological actions: Enhancement of the T
H
2 pathway of the immune system, enhancement of the levels of interleukin-4 and interleukin-10, suppression of cyclooxygenase-2 (COX-2), reduction of chronic and acute pain, and reduction of inflammation. Compared to the NSAIDs
Parthenium integrifolium
or parts thereof or an extract or component thereof have the advantage that they are not associated with gastrointestinal and renal side effects. Further, by enhancing the formation of interleukin-4 and interleukin-10 they have a down regulating effect on the T
H
1 pathway of the immune system without exerting the serious side effects characteristic of the corticosteroids. Due to these effects
Parthenium integrifolium
or parts thereof or an extract or component thereof can be employed for the following therapeutic applications:
Alleviation of pain.
Treatment or prevention of inflammatory or autoimmune disorders.
Accordingly the present invention provides a pharmaceutical composition containing
Parthenium integrifolium
or parts thereof or an extract or component thereof and a pharmaceutically acceptable carrier.
More specifically the present invention provides the use of
Parthenium integrifolium
or parts thereof or an extract or component thereof for preparing a medicine for the enhancement of the T
H
2 pathway of the immune system, for the enhancement of the levels of interleukin-4 and interleukin-10, and for the selective suppression of COX-2.
Thus, according to the invention
Parthenium integrifolium
or parts thereof or an extract or component thereof can be used in a method for the alleviation of pain in an individual, which comprises administering such plant material or a pharmaceutical composition containing it to said individual; and the invention comprises the use of
Parthenium integrifolium
or parts thereof or an extract or component thereof for preparing a medicine for the alleviation of pain.
Also, according to the invention
Parthenium integrifolium
or parts thereof or an extract or component thereof can be used in a method for the treatment or prevention of an inflammatory or autoimmune disorder in an individual, which comprises administering such plant material or a pharmaceutical composition containing it to said individual; and the invention comprises the use of
Parthenium integrifolium
or parts thereof or an extract or component thereof for preparing a medicine for the treatment or prevention of inflammatory or autoimmune disorders.
Further, the invention provides a method of preparing an extract of
Parthenium integrifolium
, which comprises extracting said plant or parts thereof, preferably the root, with an extraction agent comprising an organic solvent or a mixture thereof with water and subsequently, if necessary, removing the extraction agent to obtain an extract suitable for utilisation.
DETAILED DESCRIPTION OF THE INVENTION
Surprisingly it has been found that
Parthenium integrifolium
or parts thereof or an extract or component thereof exert pharmacological actions relevant to the therapeutic treatment of conditions associated with pain, inflammation and autoimmunity.
More specifically
Parthenium integrifolium
or parts thereof or an extract or component thereof provide the following pharmacological effects upon administration to the living organism:
Enhancement of the T
H
2 pathway of the immune system.
Enhancement of the levels of interleukin-4 and interleukin-10.
Suppression of COX-2 without affecting COX-1.
Reduction of pain.
Reduction of inflammation.
These actions provide part of the rationale for the following therapeutic applications of
Parthenium integrifolium
or parts thereof or extracts or components thereof:
A method for the treatment of any condition associated with pain or inflammation characterised by the administration of
Parthenium integrifolium
or parts thereof or an extract or component thereof. The applicant puts forward the hypothesis that the antiinflammatory and pain relieving action is due to enhanced levels of interleukin-4 and -10 which on one hand down regulate the inflammatory part of the immune system (T
H
1 pathway) and on the other hand
Coe Susan D.
Darby & Darby
Prats Francisco
LandOfFree
Pharmaceutical compositions containing parthenium... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pharmaceutical compositions containing parthenium..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pharmaceutical compositions containing parthenium... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2546098