Bucillamine / iron chelator / diabetic retinopathy

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Bucillamine may have therapeutic efficacy in preventing the development
of diabetic retinopathy.
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Jpn J Ophthalmol. ;50:377-9 [Pubmed] [Scholar] [Select] [Drop] [Hide]
[Show]
Inhibitory effect of bucillamine on the increased leukocyte entrapment
in the retinal microcirculation of diabetic rats.
Fumihiko Mori, Junichi Takahashi, Taiji Nagaoka, Toru Abiko, Taiichi
Hikichi, Akitoshi Yoshida
PURPOSE: To evaluate quantitatively the effects of bucillamine on the
entrapment of leukocytes in the retinal microcirculation of diabetic
rats. METHODS: 13 male Brown Norway rats were injected with
streptozotocin (STZ). After the animals developed diabetes, they were
divided into two groups. Group 1 (n = 7) received fresh drinking water
without bucillamine, and group 2 (n = 6) received fresh drinking water
supplemented with bucillamine (200 mg/kg per day). Rats that were not
injected with STZ and received water without bucillamine served as
controls (n = 6). Four weeks after the injection of STZ, the leukocytes
in the retina were observed by acridine orange digital fluorography.
The number of leukocytes trapped in the retinal vessels was compared
among the three groups. RESULTS: In the untreated diabetic rats, the
number of trapped leukocytes was significantly higher than in control
rats or bucillamine-treated diabetic rats (P < 0.05). CONCLUSIONS: We
demonstrated an inhibitory effect of bucillamine on leukocyte
entrapment in the retinal vessels of diabetic rats. Bucillamine may
have therapeutic efficacy in preventing the development of diabetic
retinopathy. Jpn J Ophthalmol 2006;50:377-379 (c) Japanese
Ophthalmological Society 2006.

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Bucillamine is a strong iron chelator
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these metal ions are significantly higher in RA patients and may be
involved in oxidative stress-induced damage
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Antioxidant properties of bucillamine: possible mode of action.
Mazor D, Greenberg L, Shamir D, Meyerstein D, Meyerstein N
Biochem Biophys Res Commun. 2006 Oct 27; 349(3): 1171-5


The antioxidant properties of Bucillamine (BUC), a di-thiol compound
used for treatment of rheumatoid arthritis (RA) and its possible mode
of action, were investigated. BUC exhibits potent antioxidant activity
similar to those of trolox and ascorbic acid. It reduces the stable
free radical diphenyl-2-picrylhydrazyl (DPPH) with IC(50) of 18.5+/-0.1

micromol, its relative antioxidant activity by the ferric reducing
ability (FRAP) is 2.07+/-0.01 mM and by the trolox equivalent
antioxidant capacity (TEAC), 1.46+/-0.05 mM. However, its superoxide
and apparent hydroxyl radical scavenging activities are low (IC(50) at
millimolar concentrations). We found that BUC is a strong iron (II) and

copper (II) chelator. This finding is very important since these metal
ions are significantly higher in RA patients and may be involved in
oxidative stress-induced damage. Our study suggests that BUC is a
potent antioxidant which exerts its beneficial therapeutic activities
in RA patients by metal chelation rather than by scavenging free
radical species.


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