Disease relevance of 2,5-dihydroxybenzenesulfonic acid

• The value of calcium dobesilate in the treatment of diabetic retinopathy. A controlled clinical trial [1].
• In conclusion, oral treatment with calcium dobesilate significantly protected diabetic rat retina against oxidative stress induced by ischemia/reperfusion [2].
• METHODS: Twenty-nine well-documented adult patients with first- or second-degree internal hemorrhoids were treated with calcium dobesilate for two weeks, while16 patients received only a high-fiber diet to serve as control [3].
• Finally, 100 mg/kg calcium dobesilate significantly reduced retinal edema (measured by the thickness of the inner plexiform layer) in diabetic rats [2].
• BACKGROUND: In the last 20 years, some cases of agranulocytosis associated with calcium dobesilate consumption in Spain have been reported [4].

High impact information on 2,5-dihydroxybenzenesulfonic acid

• The effect of calcium dobesilate on capillary resistance and background retinopathy was compared with placebo in a double-blind cross-over trial on 18 diabetics [1].
• No effect of calcium dobesilate on endothelial function, blood pressure or markers of oxidation was observed compared with placebo [5].
• This randomised double-blind, placebo-controlled, clinical trial investigated the effect of 3 months of treatment with calcium dobesilate on endothelium-dependent vasodilation, markers of endothelial function, blood pressure, and markers of oxidation in obese, male smokers [5].
• Calcium dobesilate possesses antioxidant properties and protects against capillary permeability by reactive oxygen species in the rat peritoneal cavity, but whether a similar action can take place in the diabetic rat retina is unknown [2].
• After single oral administration, calcium dobesilate (5-500 mg/kg) dose dependently inhibited phenazine methosulfate-dependent Evans blue extravasation with an ID50 of 50-100 mg/kg (81% inhibition at 500 mg/kg, P < 0.003) [6].

Chemical compound and disease context of 2,5-dihydroxybenzenesulfonic acid

• In the third series of experiments, rats treated with 100 mg/kg of calcium dobesilate reduced the hydroxyl radical signal intensity to 41% (measured by electron paramagnetic resonance), induced by ischemia/reperfusion in diabetic rat retina [2].
• The effects of clopidogrel and calcium dobesilate on intimal hyperplasia following vascular injury [7].
• The effects of calcium dobesilate (Doxium, a drug already known to prevent or reverse the retinal microvascular lesions of diabetes mellitus) on sorbitol formation in human erythrocytes was studied, and compared with the effects of tetramethylene glutaric acid (TMGA), a specific aldose reductase inhibitor [8].
• In contrast, calcium dobesilate (2,5-dihydroxybenzenesulfonate), which was discovered more than 40 years ago and is registered for the treatment of diabetic retinopathy in more than 20 countries remains, to our knowledge, the only angioprotective agent that reduces the progression of this disease [9].
• AIM: The purpose of this study was to examine the effects of N-acetylcysteine (NAC), calcium dobesilate (DOBE) and aprotinin on the amelioration of lung damage following ischemia/reperfusion injury in a rat hind limb model [10].

Biological context of 2,5-dihydroxybenzenesulfonic acid

• Angioprotective action of calcium dobesilate against reactive oxygen species-induced capillary permeability in the rat [6].
• Calcium dobesilate significantly reduced platelet activating factor (PAF)-induced chemiluminescence in human PMN cells and lipid peroxidation by oxygen free radicals in human erythrocyte membranes, although these actions required calcium dobesilate concentrations > or = 50 microM [11].
• Effect of calcium dobesilate on blood viscosity in diabetic microangiopathy. A review [12].
• They further suggest that Doxium reduces blood hyperviscosity and lowers intraocular pressure, with a beneficial effect on retinal state and visual fields [13].
• Pharmacokinetics of calcium dobesilate in beagle dogs after repeated administration [14].

Anatomical context of 2,5-dihydroxybenzenesulfonic acid

• These results strongly suggest that calcium dobesilate stabilizes blood-retinal barrier in diabetic retinopathy via an in situ antioxidant action [15].
• Here, calcium dobesilate was tested in a newly developed in vivo model of microvascular permeabilization induced by reactive oxygen species in the rat peritoneal cavity [6].
• Calcium dobesilate ameliorates lung injury following lower limb ischemia/reperfusion [16].
• Calcium dobesilate (CLS 2210) protects the myocardium in early acute myocardial infarction: a preliminary randomized, double-blind, placebo-controlled study of its effects on biochemical markers [17].
• We examined the effects of calcium dobesilate on ameliorating the lung damage following ischemia-reperfusion injury in skeletal muscle of rats [16].

Associations of 2,5-dihydroxybenzenesulfonic acid with other chemical compounds

• The results have indicated that preoperative administration of ibuprofen and calcium dobesilate in this animal model significantly diminishes early platelet deposition [18].
• In conclusion, calcium dobesilate was effective in scavenging hydroxyl radicals in vitro, at therapeutically relevant concentrations [11].
• In the clopidogrel and calcium dobesilate groups, this ratio had significantly decreased when compared with the control group (p < 0.05) [7].
• Inhibition of sorbitol formation in human erythrocytes by calcium dobesilate [8].
• The following compounds are discussed: horse chestnut seed extracts, flavonoids, red vine leaves extracts, total triterpenic fraction of Centella asiatica (L), prociadins, calcium dobesilate, and pentoxifylline [19].

Gene context of 2,5-dihydroxybenzenesulfonic acid

• Effects of calcium dobesilate on glomerulus TIMP1 and collagen IV of diabetic rats [20].
• Further studies in vivo are required to determine if these antioxidant properties of calcium dobesilate can play a role in its vascular protective mechanisms [11].
• Plethysmographic confirmation of the beneficial effect of calcium dobesilate in primary varicose veins [21].
• Effect of CLS 2210 (calcium dobesilate) on survival and myocardial infarction size in the rat: influence of dose and duration of treatment [22].
• Ccr had no difference between group C and group D. It was concluded that calcium dobesilate could ameliorate renal lesions in diabetic rats through inhibiting PKC and TGF-beta1 [23].

Analytical, diagnostic and therapeutic context of 2,5-dihydroxybenzenesulfonic acid

• Calcium dobesilate-treated rats showed significantly low level muscle (p = 0.025) and lung TBARS (p = 0.004), compared with the control group [16].
• A pharmacokinetic study was carried out in beagle dogs after a single intravenous infusion of 100 mg/kg of calcium dobesilate, a dose claimed to produce a cardiac lymphagogue effect [24].
• The authors report a meta-analysis of the effectiveness and safety of calcium dobesilate in CVI [25].
• Many randomized clinical trials (RCTs) have shown a beneficial effect of calcium dobesilate, but consensus is lacking about efficacy and safety [25].
• Determination of calcium dobesilate in human plasma using ion-pairing extraction and high-performance liquid chromatography [26].

References