1-1-diphenyl-2-picrylhydrazyl and Cataract

Films have been prepared from the natural antioxidant gallic acid and a proteinaceous source, the discarded emulsion obtained after cataract surgery referred to as the cataractous eye protein isolate (CEPI). Fourier transform spectroscopy (FTIR) and SDS PAGE studies confirmed the crosslinking of gallic acid with CEPI. The cross-section and surface of films were further characterized by scanning electron microscopy (SEM). The decrease in crystallinity of the films was confirmed by X-ray diffraction studies. The thermal property of the films is enhanced by the addition of gallic acid as evidenced from the Thermogravimetric analysis (TGA) studies. Films having 2% (w/w) gallic acid exhibited the maximum tensile strength of 2.88 ± 0.32 MPa comparable to other cross-linked films such as soy, casein, canola based protein films. The light barrier property of the films improved with incorporation of gallic acid. The cross-linked films were degraded by the application of the enzyme trypsin. The films also showed good antioxidant properties as determined from the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The gallic acid incorporated nontoxic CEPI films are biodegradable and possess appreciable mechanical properties and could find use in diverse applications including pharmaceuticals.

Topics: Biphenyl Compounds; Cataract; Eye Proteins; Gallic Acid; Humans; Mechanical Phenomena; Picrates

Tephrosia purpurea (T. purpurea) has been reported to prevent cataract formation in senile cataract model as well as proven effective in STZ induced type 1 diabetes. Aldose reductase (AR) is a key enzyme in the intracellular polyol pathway responsible for the development of diabetic cataract.. To investigate the effects of T. purpurea in the light of inhibition of aldose reductase enzyme in polyol pathway.. We studied the effects of alcoholic extract and flavonoid fraction of T. purpurea in streptozotocin (STZ, 45mg/kg, i.v.)-induced type I diabetic cataract in rats. The animals were divided into five groups as control, control treated with alcoholic and flavonoid fraction, diabetic control and diabetic treated with alcoholic and flavonoid fraction. In-vitro aldose reductase inhibitory activity was also evaluated. Further, molecular docking study was performed with crystal structure of aldose reductase and its known chemical constituents of the plant.. Our data suggested that both the extracts might be helpful in delaying the development of diabetic cataract due to the presence of rutin and quercetin. This beneficial effect may be due to its significant inhibition of aldose reductase enzyme and anti-oxidant activity.

Topics: Aldehyde Reductase; Animals; Antioxidants; Binding Sites; Biphenyl Compounds; Blood Glucose; Cataract; Diabetes Complications; Enzyme Inhibitors; Female; Free Radical Scavengers; Insulin; Lens, Crystalline; Male; Molecular Docking Simulation; Phytochemicals; Picrates; Plant Extracts; Protective Agents; Rats, Sprague-Dawley; Solubility; Tephrosia

The polyherbal eye drop (Itone™) is a mixture of aqueous distillates of nineteen traditionally used ingredients that sum up to impart potency to the formulation and make it a useful adjunct in various ocular pathologies. However, as there have been no controlled experimental studies accounting to the above claim, therefore, the present study was designed to evaluate the polyherbal formulation (PHF) for antiangiogenic, anti-inflammatory, anticataract, antioxidant and cytotoxicity in addition to the evaluation of intraocular penetration of PHF in rabbit eyes using LC-MS/MS.. Antiangiogenic activity of the PHF was evaluated using in ovo chick chorio-allantoic membrane (CAM) assay and in vivo cautery induced corneal neovascularization assay in rats. Anticataract potential was evaluated using steroid induced cataract in developing chick embryos, sodium selenite induced cataract in rat pups and galactose induced cataract in rats. The antioxidant activity was evaluated using di-phenyl picryl hydrazyl (DPPH) radical scavenging assay. Anti-inflammatory activity was evaluated in vitro using inhibition of LTB4 formation in human WBCs and in vivo using carrageenan induced paw edema assay in rats. The cytotoxicity was evaluated against HeLa cancer cell lines using (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Furthermore evaluation of the intraocular penetration of the PHF was carried out in rabbit eyes via aqueous humor paracentesis and further analysis using LC-MS/MS.. PHF significantly inhibited VEGF induced proliferation of new blood vessels in CAM assay and inhibited the cautery induced corneal neovascularization in rats. Additionally, PHF showed noticeable delay in the progression of cataract in the selenite and galactose induced cataract models whereby the PHF treated lenses were graded for stages II and III respectively. However, the PHF did not show any anticataract activity in the hydrocortisone induced cataract model. Moreover, PHF exhibited anti-inflammatory activity whereby it showed 39.34% inhibition of LTB4 formation and significantly inhibited carrageenan induced paw edema in rats. Eight compounds of PHF viz. camphor, casticin, curcumin-II, quercetin, rosmarinic acid, γ-terpinene, β-pinene and dipentene exhibited transcorneal penetration in rabbit eyes.. The significant antiangiogenic and anti-inflammatory activities evinced by the PHF merits further investigation for ocular neovascular and inflammatory diseases in humans.

Topics: Angiogenesis Inhibitors; Animals; Anti-Inflammatory Agents; Aqueous Humor; Biphenyl Compounds; Blood Vessels; Carrageenan; Cataract; Chick Embryo; Cornea; Edema; Eye; Female; Galactose; HeLa Cells; Humans; Hydrocortisone; Inflammation; Lens, Crystalline; Leukocytes; Leukotriene B4; Male; Medicine, Ayurvedic; Models, Animal; Ophthalmic Solutions; Phytotherapy; Picrates; Plant Extracts; Rabbits; Rats; Rats, Wistar; Sodium Selenite; Steroids; Vascular Endothelial Growth Factor A

Free radical mediated oxidative stress plays a crucial role in the pathogenesis of cataract and the present study was to determine the efficacy of luteolin in preventing selenite induced oxidative stress and cataractogenesis in vitro. Luteolin is a bioactive flavonoid, isolated and characterized from the leaves of Vitex negundo. Lenses were extracted from Sprague-Dawley strain rats and were organ cultured in DMEM medium. They were divided into three groups with eight lenses in each group as follows: lenses cultured in normal medium (G I), supplemented with 0.1mM sodium selenite (G II) and sodium selenite and 2 μg/ml luteolin (G III). Treatment was from the second to fifth day, while selenite administration was done on the third day. After the experimental period, lenses were taken out and various parameters were studied. The antioxidant potential of luteolin was assessed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity. In the selenite induced group, morphological examination of the lenses showed dense cortical opacification and vacuolization. Biochemical examinations revealed a significant decrease in activities of antioxidant enzymes and enzymes of the glutathione system. Additionally decreased glutathione level and increased reactive oxygen species (ROS) and thiobarbituric acid reactive substances (TBARS) were observed. Luteolin treatment abated selenite induced oxidative stress and cataractogenesis by maintaining antioxidant status, reducing ROS generation and lipid peroxidation in the lens. These finding demonstrated the anticataractogenic effect of luteolin by virtue of its antioxidant property, which has been reported in this paper for the first time.

Topics: Animals; Antioxidants; Biphenyl Compounds; Catalase; Cataract; Drug Interactions; Female; Glutathione; Glutathione Peroxidase; Glutathione Reductase; Luteolin; Organ Culture Techniques; Oxidative Stress; Picrates; Rats; Rats, Sprague-Dawley; Sodium Selenite; Superoxide Dismutase; Thiobarbituric Acid Reactive Substances; Vitex

The water, ethanol and chloroform extracts of selected plants such as Adhatoda vasica (L.) (Acanthaceae), Caesalpinia bonduc (L.), Cassia fistula (L.) (Caesalpiniaceae) and Biophytum sensitivum (L.) (Oxalidaceae) were evaluated for rat lens aldose reductase inhibitory (RLAR) potential, anti-cataract and antioxidant activities. All the samples inhibited the aldose reductase considerably and exhibited anti-cataract activity, while C. fistula (IC(50), 0.154 mg mL(-1)) showed significant RLAR inhibitory activity as compared to the other tested samples, and was further found to be more effective in maintaining sugar-induced lens opacity in the rat lens model. The antioxidant potential of plant extracts was determined using DPPH (2,2-diphenyl-1-picryl hydrazine), hydroxyl (OH), nitric oxide (NO) and hydrogen peroxide (H(2)O(2)) scavenging activities, along with determination of reducing power, ferrous ion chelating ability and inhibition of polyphenol oxidase (PPO). The extracts of the tested plant showed significant free radical scavenging activities and inhibited the activity of enzyme PPO, a model oxidising enzyme. The plant samples were found to possess considerable amounts of vitamin C, total polyphenols and flavonoids.

Topics: Aldehyde Reductase; Animals; Antioxidants; Biphenyl Compounds; Cataract; Catechol Oxidase; Hydrogen Peroxide; India; Inhibitory Concentration 50; Iron Chelating Agents; Picrates; Plant Extracts; Plants, Medicinal; Rats

The ability of N-beta-alanyl-5-S-glutathionyl-3,4-dihydroxyphenylalanine (5-S-GAD)-a novel catechol derivative isolated from an insect as an antibacterial substance-to scavenge free radicals and prevent cataract progression was examined. 5-S-GAD scavenged 1,1-diphenylpicrylhydrazyl (DPPH) and superoxide anions (O(2)(*)(-)), and inhibited lipid peroxidation. It also significantly inhibited the onset of glucocorticoid-induced lens opacification in chick embryos. These effects of 5-S-GAD were stronger than those of N-acetylcarnosine and TEMPOL, which are reported to be effective radical scavengers in the prevention of cataract progression. 5-S-GAD clearly delayed the maturation of cataracts induced by diamide in cultured lenses of rats. Daily instillation of 5-S-GAD retarded the development of lens opacity in galactose-fed rats. Biochemical analysis of the lenses revealed that 20-kDa proteins, presumably consisting of alpha-crystallin, were the most susceptible to oxidative stress, which leads to the carbonylation of the side chains of these proteins. alpha-Crystallin carbonylation induced by diamide or galactose was notably inhibited by 5-S-GAD in a dose-dependent manner. Our results show that 5-S-GAD prevents acute lens opacification in these short-term experimental models, possibly in part by virtue of its antioxidative property, and 5-S-GAD is expected to have long-term pharmaceutical effects.

Topics: alpha-Crystallins; Animals; Biphenyl Compounds; Carnosine; Cataract; Cells, Cultured; Chick Embryo; Cyclic N-Oxides; Diamide; Dihydroxyphenylalanine; Disease Progression; Dose-Response Relationship, Drug; Free Radical Scavengers; Galactose; Glucocorticoids; Glutathione; Insecta; Lens, Crystalline; Lipid Peroxidation; Male; Oxidative Stress; Picrates; Protein Carbonylation; Rats; Rats, Sprague-Dawley; Spin Labels; Superoxides

Retinopathy is a major cause of blindness in the Western world, while cataract is one of the three major causes of blindness worldwide. Diabetes is one of the major risk factor in retinopathy and cataract. The prevalence of blindness in India is 15 per 1000 while cataract alone accounts for 80% of this blindness. Diabetes induced cataract is characterized by an accumulation of sorbitol which is mediated by the action of a key enzyme aldose reductase (AR). Non-enzymatic glycation (binding of glucose to protein molecule) induced during diabetes appear to be the key factor for AR mediated sugar-induced cataract. Finger millet polyphenols (FMP) being a major anti-diabetic and antioxidant component, we have evaluated them for AR inhibiting activity. Phenolic constituents in FMP such as gallic, protocatechuic, p-hydroxy benzoic, p-coumaric, vanillic, syringic, ferulic, trans-cinnamic acids and the quercetin inhibited cataract eye lens effectively, the latter was more potent with an IC(50) of 14.8nM. Structure function analysis revealed that phenolics with OH group at 4th position was important for aldose reductase inhibitory property. Also the presence of neighboring O-methyl group in phenolics denatured the AR activity. Finger millet seed coat polyphenols (SCP) has been found to inhibit AR reversibly by non-competitive inhibition. Results thus, provide a stronger evidence for the potentials of FMP in inhibiting cataractogenesis in humans.

Topics: Aldehyde Reductase; Biphenyl Compounds; Cataract; Diabetes Complications; Eleusine; Flavonoids; Free Radical Scavengers; Humans; Indicators and Reagents; Inhibitory Concentration 50; Kinetics; Lens, Crystalline; Phenols; Picrates; Polyphenols; Sorbitol

The antioxidant activities of Chlorella in vitro and in vivo were investigated. Chlorella showed a strong antioxidant effect compared to various vegetables in a 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay. To evaluate the antioxidant and anti-cataract effects in vivo, a 7.3% Chlorella powder was fed to rats with streptozotocin-induced diabetes for 11 wk. At the end of the experiment, Chlorella had decreased the blood glycated hemoglobin (hemoglobin A1c) and serum cholesterol levels significantly, however, it had not affected the serum glucose concentration. The serum lipid peroxide value (TBARS value) in the rats fed Chlorella was lower than that of the control rats. In the liver and kidney, Chlorella also reduced chemiluminescent intensities. In addition, it delayed the development of lens opacities. The lens lipid peroxide content of the rats fed Chlorella was lower than that of the control rats, however the differences were not significant. These results indicate that Chlorella has antioxidant activity and may be beneficial for the prevention of diabetic complications such as cataracts.

Topics: Animals; Antioxidants; Biphenyl Compounds; Blood Glucose; Cataract; Chlorella; Cholesterol; Diabetes Mellitus, Experimental; Free Radical Scavengers; Glycated Hemoglobin; Lens, Crystalline; Lipid Peroxides; Male; Peroxides; Picrates; Powders; Probiotics; Rats; Rats, Wistar; Thiobarbituric Acid Reactive Substances

It is conceivable that drugs with anticataract potential possess antioxidant activity. Using defined chelating agents and reducing agents in a number of assays for antioxidant activity, we have demonstrated that paracetamol, aspirin, bendazac, and its metabolite 5-hydroxybendazac possess substantial reducing and/or metal-chelating activity. We found that paracetamol and 5-hydroxybendazac reduced the diphenylpicrylhydrazyl free radical; inhibited butyl peroxide-induced erythrocyte lysis as well as the haematin-catalyzed oxidative coupling of 4-aminoantipyrine and phenol by butyl peroxide. Furthermore, paracetamol, bendazac, and aspirin competed with 3-(2-pyridyl)-5,6-Diphenyl-1,2,4-triazine-4', 4"-disulphonic acid (ferrozine) for ferrous ion.

Topics: Acetaminophen; Ampyrone; Antioxidants; Aspirin; Biphenyl Compounds; Cataract; Chelating Agents; Erythrocytes; Free Radicals; Hemin; Humans; Hydrazines; Indazoles; Phenol; Phenols; Picrates