Showing papers by "Yogesh A. Kulkarni published in 2021"
TL;DR: In this paper, the authors discuss the pharmacokinetics and mechanisms of the pharmacological actions of apocynin and highlight its off-target effects that it is able to function as a scavenger of non-radical oxidant species, which is relevant for its activity against NOX 4 mediated production of hydrogen peroxide.
Abstract: Apocynin is a naturally occurring acetophenone, found in the roots of Apocynum cannabinum and Picrorhiza kurroa. Various chemical and pharmaceutical modifications have been carried out to enhance the absorption and duration of action of apocynin, like, formulation of chitosan-based apocynin-loaded solid lipid nanoparticles, chitosan-oligosaccharide based nanoparticles, and biodegradable polyanhydride nanoparticles. Apocynin has been subjected to a wide range of experimental screening and has proved to be useful for amelioration of a variety of disorders, like diabetic complications, neurodegeneration, cardiovascular disorders, lung cancer, hepatocellular cancer, pancreatic cancer, and pheochromocytoma. Apocynin has been primarily reported as an NADPH oxidase (NOX) inhibitor and prevents translocation of its p47phox subunit to the plasma membrane, observed in neurodegeneration and hypertension. However, recent studies highlight its off-target effects that it is able to function as a scavenger of non-radical oxidant species, which is relevant for its activity against NOX 4 mediated production of hydrogen peroxide. Additionally, apocynin has shown inhibition of eNOS-dependent superoxide production in diabetic cardiomyopathy, reduction of NLRP3 activation and TGFβ/Smad signaling in diabetic nephropathy, diminished VEGF expression and decreased retinal NF-κB activation in diabetic retinopathy, inhibition of P38/MAPK/Caspase3 pathway in pheochromocytoma, inhibition of AKT-GSK3β and ERK1/2 pathways in pancreatic cancer, and decreased FAK/PI3K/Akt signaling in hepatocellular cancer. This review aims to discuss the pharmacokinetics and mechanisms of the pharmacological actions of apocynin.
22 citations
TL;DR: In this article, the interaction between SIRT1 and FOXO1 and FoxO3 has been explored for its beneficial effects in diabetic complications, including microvascular, retinopathy, and macrovascular (cardiomyopathy) complications.
19 citations
TL;DR: Daidzein treatment protected retina from damage in hyperglycaemic conditions and can be considered as an effective treatment option for diabetic retinopathy.
18 citations
TL;DR: In this paper, the role of dietary modifications in the development of type 2 diabetes and associated complications is discussed. Dietary modifications modulate various molecular key players linked with the functions of nutrient signalling, regulation of autophagy, and energy metabolism, and are associated with a reprogramming of nutrient intake, which are proven to be effective for the management of diabetes.
11 citations
TL;DR: In this article, the effect of paeonol in diabetic peripheral neuropathy in rats was studied and the results indicated that paeol may be considered as an effective option for management of diabetic neuropathy.
11 citations
TL;DR: In this paper, Berberine-loaded nanostructured lipid carriers (Berb-NLCs) were developed by melt-emulsification and ultrasonication using Geleol, Miglyol 812 N, Solutol HS 15 as a solid lipid, liquid lipid and surfactant, respectively.
10 citations
TL;DR: In this paper, the effect of Triphala churna on diabetic neuropathy was evaluated in rats, where animals were grouped and treated orally with tripla churna at a dose of 250, 500, and 1,000 mg/kg after 6 weeks of diabetes induction for the next 4 weeks.
Abstract: Neuropathy is a common complication of diabetes affecting a large number of people worldwide. Triphala churna is a formulation mentioned in Ayurveda-a traditional system of medicine. It is a simple powder formulation consisting of powders of three fruits, Emblica officinalis L., Terminalia bellirica (Gaertn.) Roxb. and Terminalia chebula Retz. Individual components of Triphala churna have anti-diabetic and antioxidant activities. Hence, this study was designed to evaluate the effect of Triphala churna on diabetic neuropathy. Diabetes was induced with streptozotocin (STZ, 55 mg/kg, i. p.) in rats. Animals were grouped and treated orally with Triphala churna at a dose of 250, 500, and 1,000 mg/kg after 6 weeks of diabetes induction for the next 4 weeks. At the end of study, parameters such as body weight, plasma glucose level, motor nerve conduction velocity were determined. The effect of Triphala churna on thermal hyperalgesia, mechanical hyperalgesia, and mechanical allodynia was also determined at the end of study. The plasma cytokine levels like TGF-β1, TNF-α, and IL-1β were determined by ELISA assay. Histopathology study of the sciatic nerve was studied. Western blotting was performed to study the expression of neuronal growth factor.Treatment with Triphala churna showed a significant reduction in plasma glucose and a significant rise in body weight. Triphala treatment significantly increased the motor nerve conduction velocity and decreased the thermal and mechanical hyperalgesia, as well as mechanical allodynia. The treatment significantly inhibited levels of circulatory cytokines like TGF-β1, TNF-α, and IL-1β. Histopathology study confirmed the neuroprotective effect of Triphala churna. The expression of NGF was significantly increased in sciatic nerves after treatment with Triphala churna. From the results, it can be concluded that Triphala churna delays the progression of neuropathy in diabetic rats.
8 citations
01 Jan 2021
TL;DR: In this paper, the effect of various plant derived glycosides and aglycones in diabetes is discussed and the mechanism of their antidiabetic activity involves stimulation of insulin secretion, inhibition of α-amylase, α-glucosidase, and tyrosine phosphatase 1B enzymes involved in glycemic control.
Abstract: Diabetes is one of the principal causes of death in developed and developing countries. Many synthetic drugs are being used for the treatment of diabetes. But these drugs have many adverse effects. Hence there is an immediate requirement of new therapies that can be useful for better management of diabetes. From ancient times, herbal drugs are well accepted for their therapeutic values in different disease conditions. Natural products obtained from medicinal plants can be one of the best options for the treatment of various diseases including diabetes. Plants synthesize various secondary metabolites like terpenoids, saponins, tannins, flavonoids, anthraquinones, alkaloids, and glycosides. Glycosides consist of sugar (glycone) moiety joined to a non-sugar moiety (aglycone) via a glycosidic bond. Many plants synthesize glycosides, which can be hydrolyzed to give glycone and aglycone part by enzyme hydrolysis. Various glycosides as well as aglycones are reported to have many biological activities. Glycosides like rutin, puerarin, gymnemic acid I, and stevioside have been reported for significant antidiabetic activity. Aglycones like securigenin, strictinin, and christinin-A have been reported for their antidiabetic activity. The mechanism of their antidiabetic activity involves stimulation of insulin secretion, inhibition of α-amylase, α-glucosidase, and tyrosine phosphatase 1B enzymes involved in glycemic control. The present book chapter focuses on the effect of various plant derived glycosides and aglycones in diabetes.
6 citations
TL;DR: Evaluated the effect of combination of lisinopril with naringenin in diabetic nephropathy in rats and showed promising effect, with significant improvement in the biochemical and urine parameters.
Abstract: Background Diabetes is a metabolic disorder affecting a large percentage of the population worldwide. The chronic hyperglycemic condition leads to the generation of advanced glycation end products, reactive oxygen species and inflammatory cytokines, which worsen the functioning of the kidney. Clinical management of diabetic nephropathy is difficult as it requires a multi-focused approach. Hence, a combination of lisinopril a drug used in clinical practice for nephropathy, and naringenin, a flavonoid reported to have a significant effect in nephropathy, may show additive or synergistic effect with less side effects. Objective The objective of the present study was to evaluate the effect of a combination of lisinopril with naringenin in diabetic nephropathy. Methods Diabetes was induced in male Sprague Dawley rats by streptozotocin (55 mg/kg, i.p.). After four weeks of diabetes induction animals were treated with naringenin alone and a combination of Lisinopril and naringenin for the next four weeks. At the end of the study, various urine and biochemical parameters were evaluated. Oxidative stress parameters like malondialdehyde, reduced glutathione; catalase and superoxide dismutase for kidney tissues were estimated and histopathology studies of kidneys were carried out. Results The combination of lisinopril (10 mg/kg) and naringenin (25 and 50 mg/kg) treatment showed significant improvement in the biochemical and urine parameters. Combination treatment also attenuated renal oxidative stress and renal damage as observed in histopathological studies. Conclusion Treatment with a combination of lisinopril and naringenin showed a promising effect on diabetic nephropathy in rats.
2 citations
TL;DR: In this paper, the effect of Daidzein in an experimental model of diabetic cardiomyopathy in rats was studied and a significant reduction in QT interval was observed in diabetic animals.
2 citations
TL;DR: In this article, the effects of aqueous and alcoholic extract (AE and AlcE) of Bauhinia variegata Linn. leaves in diabetic neuropathy were studied.
Abstract: Bauhinia variegata, a ayurvedic medicinal plant reported for its valuable effects in various diseases. It has shown significant effects in type 1 and type 2 diabetes. The present work was designed to study effects of aqueous and alcoholic extract (AE and AlcE) of Bauhinia variegata Linn. leaves in diabetic neuropathy. Male Sprague Dawley rats become diabetic using intraperitoneal injection of streptozotocin (STZ) at 55 mg/kg dose. After 6 weeks, animals were divided and were treated with AE and AlcE at a dose of 250, 500, and 1000 mg/kg (p. o.) for the next four weeks. Various parameters such as glucose, thermal hyperagesia, mechanical allodynia, MNCV and oxidative stess were assessed at the end of the study. Diabetic animals showed a significant reduction in response time in tail immersion and hot plate test as compared to animals in normal control group. AE and AlcE at 250, 500, and 1000 mg/kg dose significantly increased response time in the tail immersion test. Whereas, AE and AlcE at doses 500 and 1000 mg/kg showed significant improvement and in response time in the hot plate test. AlcE at 250, 500 and 1000 mg/kg dose increased the nociceptive threshold significantly. AE at doses 500 and 1000 mg/kg showed significant improvement in the nociceptive threshold. The decrease in motor nerve conduction velocity was observed in diabetic control animals, which was significantly improved after AlcE treatment as compared to AE treatment. Treatment with AE and AlcE decreased the lipid peroxidation and increased the antioxidant enzyme activity significantly in the sciatic nerve. The results showed that Bauhinia variegata extracts may be considered as a effective option for management of diabetic neuropathy.
TL;DR: In this article, the authors evaluated the effect of escin in diabetic cardiomyopathy and found that escin may significantly inhibit myocardial damage through its NF-κβ inhibitory, antidiabetic, neuroprotective, and potent anti-inflammatory activity.
Abstract: Objective Diabetic cardiomyopathy is one of the most common complications of diabetes. Escin may significantly inhibit myocardial damage through its NF-κβ inhibitory, antidiabetic, neuroprotective, and potent anti-inflammatory activity. Hence, the study was carried out to evaluate the effect of escin in diabetic cardiomyopathy. Methods Diabetes induction was done in rats with streptozotocin. After six weeks of induction, diabetic animals were administered with escin (5, 10, and 20 mg/kg) for the next four weeks. Results Escin prevented the progression of abnormalities in the biochemical, hemodynamic parameters and electrocardiogram. Escin also prevented the progression of abnormality in the oxidative stress parameters. The expression of NF-κβ and MCP-1 was significantly reduced with escin treatment. Furthermore, escin also prevented damage to myocardial cells and reduced collagen deposition in the cardiomyocytes. Conclusion Escin prevented the progression of cardiomyopathy in diabetic rats. Hence escin can be an alternative option for the management of diabetic cardiomyopathy.
TL;DR: Escin has effects on inflammation and is useful for the treatment of varicose veins and cancer as mentioned in this paper, however, the toxicity profile of escin is not available, and oral acute toxicity in rats is unknown.
Abstract: Escin has effects on inflammation and is useful for the treatment of varicose veins and cancer. Scientific reports on the toxicity profile of escin are not available. Oral acute toxicity in rats wa...
01 Jan 2021
TL;DR: According to the International Diabetic Federation 2017 report, there is tremendous increase in number of diabetic people throughout the world from last few decades as discussed by the authors, the total number had reached 327 million in the year 2017.
Abstract: Diabetes mellitus is a chronic metabolic disorder that occurs when the pancreas is no longer able to make insulin or the body is not able to make use of the insulin. Diabetes mellitus affects people from developed as well as developing countries. According to the International Diabetic Federation 2017 report, there is tremendous increase in number of diabetic people throughout the world from last few decades. The total number had reached 327 million in the year 2017. High prevalence, complex pathogenesis and rapidly developing complications result in an urge in the need of an effective treatment against diabetic progression.