Apocynin And Analogues Affects Arthritis Aspects
Apocynin And Analogues Affects Arthritis Aspects
Summary of the invention
It was found that osteoarthritis can be effectively treated by
administration of a suitable amount of apocynin or its functional and
structural analogues, preferably in the form of an extract from a
Picrorhiza plant, and preferably together with further components
enhancing the beneficial effect of the apocynin.
Thus, the invention in a first aspect provides compositions for the
treatment of osteoarthritis, containing an effective amount of
apocynin or its analogues.
In a second aspect, the invention provides methods for treating
osteoarthritis comprising administering to a person in need of said
treatment an effective amount of apocynin or its analogues.
In a third aspect, the invention provides compositions comprising
apocynin or analogues and methods for the treatment of arthritis in
general as caused by wear-and-tear processes, due to labour, ageing or
obesity, for the treatment of developed arthritis and for the
treatment of the first symptoms of joint disorders in patients not
having a familial history of rheumatism.
In a fourth aspect the invention provides compositions that are
characterized by the simultaneous presence of apocynin or analogues
and other components, in particular an inhibitor of inducible nitric
oxide synthase and methods for treatment of arthritis in general
caused by wear-and-tear, autoimmune responses in the joints, goute, or
other causes of cartilage degradation.
Detailed description of the invention
According to the invention apocynin is a highly useful component for
treating osteoarthritis and related conditions.
In particular, apocynin was found to be effective in retarding
progression of osteoarthritis.
It was found furthermore, that the inflammatory processes in arthritis
can be controlled and the accompanying symptoms of stiffness and pain
can be alleviated by combined administration of an inhibitor of NADPH
oxidase, such as apocynin, and an inhibitor of inducible nitric oxide
synthase (iNOS), such as curcumin.
Consequently, the composition of the invention contains at least 50
pg, preferably at least 100 ug, up to 1000 mg of apocynin on the basis
of daily intake. The preferred daily intake is between 1 and 100 mg.
Apocynin (acetovanillone) is a known compound (4-hydroxy-3-methoxy-
acetophenone); most preferred is a dosage of at least 15 mg/day.
According to the invention, analogues of apocynin may be used instead
of or in addition to apocynin.
Such analogues are in particular those in which the 4-hydroxyl group
is etherified, especially with a hydroxylated alkyl group, such as 2-
hydroxyethyl, 2,3- dihydroxypropyl or a sugar moiety.
The latter analogue in which the sugar moiety is ß- D-glucose, is
commonly known as androsin.
This is the usual form in which apocynin is present in fresh plants.
Eur J Pharmacol (2006) 531: 264-9.
Oral administration of the NADPH-oxidase inhibitor apocynin partially
restores diminished cartilage proteoglycan synthesis and reduces
inflammation in mice.
S (S) Hougee, A Hartog, A Sanders, YM Graus, MA (M A) Hoijer, J
Garssen, WB Van Den Berg, HM van Beuningen, HF Smit
Apocynin, an inhibitor of NADPH-oxidase, is known to partially reverse
the inflammation-mediated cartilage proteoglycan synthesis in
More recently, it was reported that apocynin prevents cyclooxygenase
(COX)-2 expression in monocytes.
The present study aimed to investigate whether these in vitro features
of apocynin could be confirmed in vivo.
In a mouse model of zymosan-induced acute arthritis apocynin was
administered orally (0, 3.2, 16 and 80 mug/ml in the drinking water)
and the effects on cartilage proteoglycan synthesis were monitored.
In a mouse model of zymosan-induced inflammation of the ears apocynin
was administered orally (14 mg/kg/day by gavage) and the effects on
ear swelling and ex vivo produced prostaglandin E(2) (PGE(2)) by
lipopolysaccharide (LPS)-stimulated blood cells were measured. In this
study, ibuprofen was used as a positive control (50 mg/kg/day by
gavage) and animals received vehicle as a negative control.
Apocynin dose-dependently reversed the inhibition of proteoglycan
synthesis in articular cartilage of the arthritic joint.
A statistically significant increase in proteoglycan synthesis was
found at a dose of 80 mug/ml apocynin.
Apocynin did not affect the proteoglycan synthesis of the control knee
joints. Apocynin significantly decreased the zymosan-induced ear
swelling at 1, 2 and 4 h (hours) after zymosan injection versus the
vehicle treated group at 14 mg/kg/day. The ex vivo production of
PGE(2) by LPS-stimulated blood cells was significantly decreased after
in vivo apocynin treatment. Ibuprofen decreased ear swelling at the
same time-points as apocynin and inhibited the ex vivo produced
In conclusion, the present study confirmed two important features of
apocynin in vivo: (1) oral administration of apocynin can partially
reverse the inflammation-induced inhibition of cartilage proteoglycan
synthesis, and (2) oral administration of apocynin has COX inhibitory
effects similar to the non-steroidal anti-inflammatory drug (NSAID)
Therefore, apocynin might be of potential use during the treatment of
chronic inflammatory joint diseases like osteoarthritis or rheumatoid
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