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1Colon-specific prodrugs of 4-aminosalicylic acid for inflammatory bowel disease显示文摘Despite the advent of biological products,such as antitumor necrosis factor-αmonoclonal antibodies(infliximab and adalimumab),for treatment of moderate to severe cases of inflammatory bowel disease(IBD),most patients depend upon aminosalicylates as the conventional treatment option.In recent years,the increased knowledge of complex pathophysiological processes underlying IBD has resulted in development of a number of newer pharmaceutical agents like low-molecular-weight heparin,omega-3 fatty acids,probiotics and innovative formulations such as high-dose,oncedaily multi-matrix mesalamine,which are designed to minimize the inflammatory process through inhibition of different targets.Optimization of delivery of existing drugs to the colon using the prodrug approach is another attractive alternative that has been utilized and commercialized for 5-aminosalicylic acid(ASA)in the form of sulfasalazine,balsalazide,olsalazine and ipsalazine,but rarely for its positional isomer 4-ASA-a wellestablished antitubercular drug that is twice as potent as 5-ASA against IBD,and more specifically,ulcerativecolitis.The present review focuses on the complete profile of 4-ASA and its advantages over 5-ASA and colon-targeting prodrugs reported so far for the management of IBD.The review also emphasizes the need for reappraisal of this promising but unexplored entity as a potential treatment option for IBD.Suneela S Dhaneshwar 2014World Journal of Gastroenterology2014,20,13:4
2Adherence to self-care practices, glycemic status and influencing factors in diabetes patients in a tertiary care hospital in Delhi显示文摘AIM To assess the adherence to self-care practices,glycemic status and influencing factors in diabetes patients.METHODS This was a cross-sectional observational analysis of baseline data from a quasi-experimental study conducted among 375 diabetic patients aged between 18 to 65years at a major public tertiary care centre in New Delhi,India during February-September’2016.The Summary of Diabetes Self-care activities measure was used to assess medical adherence in diabetic patients.Open ended questions were used to identify facilitators and inhibitors of medical adherence.RESULTS Mean age of the study subjects was 49.7±10.2 years.A total of 201 men and 174 women were enrolled in the study.Three hundred nine(82.4%)subjects were adherent to their intake of anti-diabetic medication.On binary logistic regression,education level below primary school completion and absence of hypertensioncomorbidity were found to be independent predictors of medication non-adherence.Sociocultural resistance was an important factor impeding outdoor exercise among younger women.Knowledge of diabetes in the study subjects was low with mean score of 3.1±2(maximum score=10).Suboptimal glycemic control was found in259(69%)subjects which was significantly more likely in patients on Insulin therapy compared to those on Oral Hypoglycemic agents alone(P<0.006).DISCUSSION Our study found a large gap existed between selfreported medication adherence and glycemic control.This suggests the need for enhanced physician focus for diabetic patient management.Saurav Basu Suneela Garg Nandini Sharma M Meghachandra Singh Sandeep Garg 2018World Journal of Diabetes2018,9,5:4
3Role of prebiotics, probiotics, and synbiotics in management of inflammatory bowel disease: Current perspectives显示文摘Experimental evidence supports the fact that changes in the bowel microflora due to environmental or dietary factors have been investigated as implicating factors in the etiopathogenesis of inflammatory bowel disease(IBD).The amassing knowledge that the inhabited microbiome regulates the gut physiology and immune functions in IBD,has led researchers to explore the effectiveness of prebiotics,probiotics,and synbiotics in treating IBD.This therapeutic approach focuses on restoring the dynamic balance between the microflora and host defense mechanisms in the intestinal mucosa to prevent the onset and persistence of intestinal inflammation.Numerous microbial strains and carbohydrate blends,along with their combinations have been examined in experimental colitis models and clinical trials,and the results indicated that it can be an attractive therapeutic strategy for the suppression of inflammation,remission induction,and relapse prevention in IBD with minimal side effects.Several mechanisms of action of probiotics(for e.g.,Lactobacillus species,and Bifidobacterium species)have been reported such as suppression of pathogen growth by releasing certain antimicrobial mediators(lactic and hydrogen peroxide,acetic acid,and bacteriocins),immunomodulation and initiation of an immune response,enhancement of barrier activity,and suppression of human T-cell proliferation.Prebiotics such as lactulose,lactosucrose,oligofructose,and inulin have been found to induce the growth of certain types of host microflora,resulting in an enriched enteric function.These non-digestible food dietary components have been reported to exert anti-inflammatory effects by inhibiting the expression of tumor necrosis factor-α-related cytokines while augmenting interleukin-10 levels.Although proand prebiotics has established their efficacy in healthy subjects,a better understanding of the luminal ecosystem is required to determine which specific bacterial strain or combination of probiotics and prebiotics would prove to be the ideal treatment for IBD.Clinical trials,however,have given some conflicting results,requiring the necessity to cite the more profound clinical effect of these treatments on IBD remission and prevention.The purpose of this review article is to provide the most comprehensive and updated review on the utility of prebiotics,probiotics,and synbiotics in the management of active Crohn’s disease and ulcerative colitis/pouchitis.Supriya Roy Suneela Dhaneshwar 2023World Journal of Gastroenterology2023,29,14:4
4Determination of the mitigating effect of colon-specific bioreversible codrugs of mycophenolic acid and aminosugars in an experimental colitis model in Wistar rats显示文摘AIM To design colon-targeted codrugs of mycophenolic acid(MPA) and aminosugars as a safer option to mycophenolate mofetil(MMF) in the management of inflammatory bowel disease. METHODS Codrugs were synthesized by coupling MPA with aminosugars(D-glucosamine and D-galactosamine) using EDCI coupling. The structures were confirmed by infrared radiation, nuclear magnetic resonance, mass spectroscopy and elemental analysis. The release profile of codrugs was extensively studied in aqueous buffers, upper gastrointestinal homogenates, faecal matter and caecal homogenates(in vitro) and rat blood(in vitro). Anti-colitic activity was assessed in 2,4,6-trinitrobezenesulfonic acid-induced colitis in Wistar rats by the estimation of various demarcating parameters. Statistical evaluation was performed by applying one-way and two-way ANOVA when compared with the disease control.RESULTS The prodrugs resisted activation in HCl buffer(pH 1.2) and stomach homogenates of rats with negligible hydrolysis in phosphate buffer(p H 7.4) and intestinal homogenates. Incubation with colon homogenates(in vitro) produced 76% to 89% release of MPA emphasizing colon-specific activation of codrugs and the release of MPA and aminosugars at the site of action. In the in vitro studies, the prodrug of MPA with D-glucosamine(MGLS) was selected which resulted in 68% release of MPA in blood. in vitro studies on MGLS revealed its colon-specific activation after a lag time of 8 h which could be ascribed to the hydrolytic action of N-acyl amidases found in the colon. The synthesized codrugs markedly diminished disease activity score and revived the disrupted architecture of the colon that was comparable to MMF but superior to MPA. CONCLUSION The significant attenuating effect of prodrugs and individual aminosugars on colonic inflammation proved that the rationale of the codrug approach is valid.Shakuntala Santosh Chopade Suneela Sunil Dhaneshwar 2018World Journal of Gastroenterology2018,24,10:2
5Characterization of cellulosic hot-melt extruded films containing lidocaine 显示文摘Michael A R Kavitha G Suneela P 2005Eur J Pharm Biopharm2005,59,1:1
6Macromolecular Prodrug of 4-Aminosalicylic Acid for Targeted Delivery to Inflamed Colon显示文摘Gaurav Vadnerkar Suneela Dhaneshwar 2013Current Drug Discovery Technologies2013,,1:1
7Design and Development of Novel Azo Prodrugs using Various Permutations and Combinations of 5- and 4-Aminosalicylic Acids for Inflammatory Bowel Disease: A Colon-Targeted Approach显示文摘Dhaneshwar Suneela Vadnerkar Gaurav Rai Himanshu 2013Inflammation & Allergy-Drug Targets2013,,5:1
8Colon-specific mutual amide prodrugs of 4-aminosalicylic acid for their mitigating effect on experimental colitis in rats显示文摘Suneela S. Dhaneshwar Mukta Chail Mahavir Patil Salma Naqvi Gaurav Vadnerkar 2008European Journal of Medicinal Chemistry2008,,1:1
9Investigation of mitigating effect of colon-specific prodrugs of boswellic acid on 2,4,6-trinitrobenzene sulfonic acidinduced colitis in Wistar rats: Design, kinetics and biological evaluation显示文摘AIM To develop a colon-targeting bioreversible delivery system for β-boswellic acid(BBA) and explore utility of its prodrugs in 2,4,6-trinitrobenzene sulfonic acid(TNBS)-induced colitis in rats.METHODS Synthesis of 4 co-drugs of BBA with essential amino acids was achieved by CDI coupling, followed by their spectral characterization. In vitro kinetics were studied by HPLC in aqueous buffers, homogenates of gastrointestinal tract and fecal matter. In vivo kinetic studies were performed in Wistar rat plasma, urine and feces. The prodrugs were screened in TNBS-induced colitis modeled Wistar rats. Statistical significance was assumed at P < 0.05, P < 0.01, P < 0.001 when compared with disease controls using one-way and two-way ANOVAs.RESULTS Prodrugs were stable in 0.05 mol/L HCl buffer(p H 1.2) and stomach homogenates. Negligible hydrolysis was observed in phosphate buffer and intestinal homogenates. Substantial release(55%-72% and 68%-86%) of BBA was achieved in rat fecal matter and homogenates of colon. In vivo studies of BBA with L-tryptophan(BT) authenticated colon-specific release of BBA. But, surprisingly substantial concentration of BBA was seen to reach the systemic circulation due to probable absorption through colonic mucosa. Sitespecifically enhanced bioavailability of BBA could be achieved in colon, which resulted in demonstration of significant mitigating effect on TNBS-induced colitis in rats without inducing any adverse effects on stomach, liver and pancreas. Prodrug of BT was found to be 1.7%(P < 0.001) superior than sulfasalazine in reducing the inflammation to colon among all prodrugs tested. CONCLUSION The outcome of this study strongly suggests that these prodrugs might have dual applicability to inflammatory bowel disease and chronotherapy of rheumatoid arthritis.Ajinkya Sarkate Suneela S Dhaneshwar 2017World Journal of Gastroenterology2017,23,7:1
10Dextran: a promising macromolecular drug carrier显示文摘Suneela S Dhaneshwar Mini Kandpal 2006Indian Journal of Pharmaceutical Sciences2006,1112,:1
11The Effects of Spherical Surface and Laser Polarization on the Photodetachment Cross Section of H^-显示文摘We report the combined effects of laser polarization and curvature of the spherical surface on the detached electron spectra from H-.The Theoretical imaging method is used as a tool of investigation.The photodetachment cross sections for various polarization angles,radii of curvatures and inter ion surface distances are displayed.The analysis of the spectra reveals that the laser polarization angle θL,curvature of the surface rc and inter ion surface distance d strongly affect oscillations in the spectra.Therefore,a fine control on the laser polarization and that of curvature in the surface can be used to control oscillations in the photodetachment of negative ions.Muhammad Haneef Suneela Arif Jehan Akbar Nasrullah Shah Muhammad Zahir Aneela Shamim Hameed Ullah 2013Communications in Theoretical Physics2013,59,3:0
12Amelioration of hepatotoxicity by biocleavable aminothiol chimeras of isoniazid: Design, synthesis, kinetics and pharmacological evaluation显示文摘AIM To overcome the hazardous effects on liver caused by long-term use of antitubercular agent isoniazid(INH) by developing a novel hepatoprotective prodrug strategy by conjugating INH with aminothiols as antioxidant promoities for probable synergistic effect.METHODS INH was conjugated with N-acetyl cysteine(NAC) and N-(2)-mercaptopropionyl glycine using the SchottenBaumann reaction and with L-methionine using Boc-anhydride through a biocleavable amide linkage. Synthesized prodrugs were characterized by spectral analysis, and in vitro and in vivo release studies were carried out using HPLC. Their hepatoprotective potential was evaluated in male Wistar rats by performing liver function tests, measuring markers of oxidative stress and carrying out histopathology studies.RESULTS Prodrugs were found to be stable in acidic(pH 1.2) and basic(pH 7.4) buffers and in rat stomach homogenates, whereas they were hydrolysed significantly(59.43%-94.93%) in intestinal homogenates over a period of 6 h. Upon oral administration of prodrug NI to rats, 52.4%-61.3% INH and 47.4%-56.8% of NAC were recovered in blood in 8-10 h. Urine and faeces samples pooled over a period of 24 h exhibited 1.3%-2.5% and 0.94%-0.9% of NAC, respectively, without any presence of intact NI or INH. Prodrugs were biologically evaluated for hepatoprotective activity. All the prodrugs were effective in abating oxidative stress and re-establishing the normal hepatic physiology. The effect of prodrug of INH with NAC in restoring the levels of the enzymes superoxide dismutase and glutathione peroxidase and abrogating liver damage was noteworthy especially. CONCLUSION The findings of this investigation demonstrated that the reported prodrugs can add safety and efficacy to future clinical protocols of tuberculosis treatment.Neha Vithal Bhilare Suneela Sunil Dhaneshwar Kakasaheb Ramoo Mahadik 2018World Journal of Hepatology2018,10,7:0
13Photodetachment of Di-atomic Negative Ion H^(-)_(2) near a Surface显示文摘We describe the effects of plane surface on the photo-detached electron spectra from H^(-)_(2).A z-polarized laser is used for the detachment of electrons.The detached electron flux and photodetachment cross section are derived.There exists strong dependence on the distance of the H^(-)_(2) from the surface and also on the separation of atomic centers of H^(-)_(2).The results show strong oscillations for smaller values of distances,whereas for larger values the oscillating structure disappears.Muhammad Haneef Saleh Mohammad Suneela Arif Jehan Akbar Nasrullah Shah Imran Ullah 2012Chinese Physics Letters2012,29,5:0
14Correction to“Role of prebiotics,probiotics,and synbiotics in management of inflammatory bowel disease:Current perspectives”显示文摘Correction to“Roy S,Dhaneshwar S.Role of prebiotics,probiotics,and synbiotics in management of inflammatory bowel disease:Current perspectives.World J Gastroenterol 2023;29:2078-2100[PMID:37122604 DOI:10.3748/wjg.v29.i14.20-78]”.In this article,a correction note is to be added.Supriya Roy Suneela Dhaneshwar 2023World Journal of Gastroenterology2023,29,35:0
15Detached Electron Spectra from H- near a Partially Reflecting Spherical Surface显示文摘The photodetachnent of a hydrogen negative ion (H-) near a partially reflecting surface with a spherical shape is investigated by a theoretical imaging method.Analytical expressions for the detached electron flux and total photodetachment cross section are derived.It is found that two parameters,i.e.curvature radius Tc and reflection parameter K,control the photodetachment spectra.Furthermore,these parameters can be used for the classification,identification and revelation of minor details like curvature of different types of surfaces.Muhammad Haneef Saleh Mohammad Jehan Akbar Suneela Arif Muhammad Zahir Humayun Khan 2012Chinese Physics Letters2012,29,7:0
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