Ravi Saklani

Bio: Ravi Saklani is an academic researcher from Delhi Institute of Pharmaceutical Sciences and Research. The author has contributed to research in topics: Rutin & Diabetic retinopathy. The author has an hindex of 3, co-authored 4 publications receiving 57 citations.

Cardioprotective effects of rutin via alteration in TNF-α, CRP, and BNP levels coupled with antioxidant effect in STZ-induced diabetic rats

Abstract: Diabetic cardiomyopathy (DCM) is a dreadful complication of diabetes responsible for 80 % mortality in diabetic patients, but unfortunately its pharmacotherapy is still incomplete. Rutin is a naturally occurring flavonoid having a long history of use in nutritional supplements for its action against oxidative stress, inflammation, and hyperglycemia, the key players involved in the progression of DCM, but remains unexplored for its role in DCM. This study was conducted to address this lacuna. It was performed in 4-week-old Streptozotocin-induced (45 mg/kg) diabetic rats for a period of 24 weeks to mimic the cardiotoxic effect of chronic hyperglycemia in diabetic patient's heart and to investigate the effect of rutin (50 mg/kg/day) in ameliorating these effects. Heart of the diabetic rats showed altered ECG parameters, reduced total antioxidant capacity, increased inflammatory assault, and degenerative changes. Interestingly, rutin treatment significantly ameliorated these changes with decrease in blood glucose level (p > 0.001), % HbA1c (p > 0.001) and reduced expression of TNF-α (p < 0.001), CRP (p < 0.001), and BNP (p < 0.01) compared to diabetic control rats. In addition, rutin provided significant protection against diabetes associated oxidative stress (p < 0.05), prevented degenerative changes in heart, and improved ECG parameters compared to diabetic control rats. The heart-to-body weight ratio was significantly reduced in rutin treatment group compared to diabetic control rats (p < 0.001). In conclusion, this study implicates that oxidative stress and inflammation are the central players involved in the progression of DCM and rutin ameliorates DCM through its antioxidant and anti-inflammatory actions on heart.

Clinical biomarkers and molecular basis for optimized treatment of diabetic retinopathy: current status and future prospects.

Abstract: Diabetic retinopathy is a highly specific microvascular complication of diabetes and a leading cause of blindness worldwide. It is triggered by hyperglycemia which causes increased oxidative stress leading to an adaptive inflammatory assault to the neuroretinal tissue and microvasculature. Prolonged hyperglycemia causes increased polyol pathway flux, increased formation of advanced glycation end-products, abnormal activation of signaling cascades such as activation of protein kinase C (PKC) pathway, increased hexosamine pathway flux, and peripheral nerve damage. All these changes lead to increased oxidative stress and inflammatory assault to the retina resulting in structural and functional changes. In addition, neuroretinal alterations affect diabetes progression. The most effective way to manage diabetic retinopathy is by primary prevention such as hyperglycemia control. While the current mainstay for the management of severe and proliferative diabetic retinopathy is laser photocoagulation, its role is diminishing with the development of newer drugs including corticosteroids, antioxidants, and antiangiogenic and anti-VEGF agents which work as an adjunct to laser therapy or independently. The current pharmacotherapy of diabetic retinopathy is incomplete as a sole treatment option in view of limited efficacy and short-term effect. There is a definite clinical need to develop new pharmacological therapies for diabetic retinopathy, particularly ones which would be effective through the oral route and help recover lost vision. The increasing understanding of the mechanisms of diabetic retinopathy and its biomarkers is likely to help generate better and more effective medications.

Effect of rutin on retinal VEGF, TNF-α, aldose reductase, and total antioxidant capacity in diabetic rats: molecular mechanism and ocular pharmacokinetics.

Abstract: The current study was conducted to explore the potential of rutin in preventing sight-threatening diabetic retinopathy. Wistar albino rats (either sex) weighing 200–225 g were intraperitoneally injected with 45 mg/kg streptozotocin (pH 4.5). Rats having blood glucose ≥ 300 mg/dL were divided into two groups (n = 8; each group). Group I served as diabetic control and received normal saline p.o. Group II received rutin 50 mg/kg p.o. for 24 weeks. At the end of 24 weeks, retinal fundus and fluorescein imaging were done, rats were killed, and retinal biochemical assessments were conducted. Moreover, ocular pharmacokinetics of rutin was assessed in the normal rats after a single oral dose of 50 mg/kg. Rutin treatment significantly (p < 0.001) lowered retinal vascular endothelial growth factor, tumor necrosis factor-α, and aldose reductase. Rutin treatment significantly (p < 0.001) elevated the levels of total antioxidant capacity of the retinas. Fundus examination of rutin-treated group showed significantly lower tortuosity index and normal fluorescein angiography. Rutin was detected in the retina as well as in aqueous humor of normal rats. Rutin treatment significantly arrested the biochemical disturbances of diabetic retinopathy. The distribution of orally ingested rutin in ocular tissues further substantiate its site-specific action.

In vitro antioxidant properties of rutin

Abstract: Much work has been carried out in recent years on the beneficial effect of phenolic compounds which act as natural antioxidants and help to neutralize free radicals. We analysed the antioxidant activity of the rutin (quercetin-3-rhamnosyl glucoside) using different assays including: total antioxidant activity and reducing power, hydroxyl radical scavenging assay, superoxide radical scavenging assay, 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging assay and lipid peroxidation assay which uses egg yolk as the lipid-rich source. Total antioxidant capacity was determined by the assay based on the decrease in absorbance of β-carotene by the sample. Rutin exhibited strong DPPH radical scavenging activity. At the concentration of 0.05 mg/ml, ascorbic acid (Vc), butylated hydroxytoluene (BHT) and rutin showed 92.8%, 58.8%, and 90.4% inhibition, respectively. In addition, rutin had effective inhibition of lipid peroxidation. Those various antioxidant activities were compared to standard antioxidants such as BHT and Vc.

Rutin: A review on extraction, identification and purification methods, biological activities and approaches to enhance its bioavailability

Abstract: Background Rutin is a common dietary flavonoid which has received great attention in literature, due to their pharmacological properties, including antimicrobial, anti-inflammatory, anticancer, antidiabetic, inter alia . Over 860 products containing rutin are currently marketed in the US. The major disadvantage associated with rutin is its constrained bioavailability, mainly caused by its low aqueous solubility, poor stability and limited membrane permeability. Scope and approach The aim of this contribution is to give an overview of the current methods (conventional and innovative) for the extraction, identification and purification of rutin. Furthermore, recent findings regarding its pharmacological activities and the different approaches to increase rutin solubility in both aqueous and lipid phases will be discussed. Key findings and conclusions Current trends on extraction process have been focused on the discovery and design of green and sustainable extraction techniques to optimize the recovery of rutin. Despite the bioactivity expressed in different in vitro systems, its biological effects in vivo are limited by the poor bioavailability of the flavonoid. The utilization of delivery systems for rutin or its enzymatic or chemical transformation towards highly soluble derivatives have the potential to improve rutin bioavailability, as well as its stability and/or specific biological properties. These novel rutin formulations may bring this promising flavonoid to the forefront of nutraceuticals for the prevention and/or treatment of various chronic human diseases.