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| 1 | Colon-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 | 2014 | World Journal of Gastroenterology2014，20，13： | 4 |
| 2 | Role 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 | 2023 | World Journal of Gastroenterology2023，29，14： | 4 |
| 3 | Determination 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 | 2018 | World Journal of Gastroenterology2018，24，10： | 2 |
| 4 | Application of stability-indicating HPTLC method for quantitative determination of metadoxine in pharmaceutical dosage form显示文摘 | Neeraj Kaul Himani Agrawal Bharat Patil Abhijit Kakad S.R. Dhaneshwar | 2005 | Il Farmaco2005，，4： | 2 |
| 5 | Studies on Synthesis, Stability, Release and Pharma- codynamic Profile of a Novel Diacerein-thymol Pro- drug显示文摘 | DHANESHWAR S PATEL V PATIL D | 2013 | Bioorg Med Chem Lett2013，28，： | 1 |
| 6 | The Real Exchange Rate and Macroeconomic Performance in Sub - Saharan Africa显示文摘 | Ghura Dhaneshwar Grennes Thomas J | 1993 | Journal of Development Economics1993，42，1： | 1 |
| 7 | Stability indicating HPTLC and LC determination of dasatinib in pharmaceutical dosage form 显示文摘 | Mhaske DV Dhaneshwar SR | 2007 | Chromatographia2007，66，12： | 1 |
| 8 | Validated RP-HPLC method for simultaneous quantitation of losartan potassium and metolazone in bulk drug and formulation显示文摘 | Dubey R Bhusari VK Dhaneshwar SR | 2011 | Sci Pharm2011，79，3： | 1 |
| 9 | Exploring novel colon-targeting antitistaminic prodrug for colitis 显示文摘 | DHANESHWAR S GAUTAM H | 2012 | J Physiol Pharm2012，63，4： | 1 |
| 10 | Macromolecular Prodrug of 4-Aminosalicylic Acid for Targeted Delivery to Inflamed Colon显示文摘 | Gaurav Vadnerkar Suneela Dhaneshwar | 2013 | Current Drug Discovery Technologies2013，，1： | 1 |
| 11 | Diglyceride prodrug strategy for enhancing the bioavailability of norfloxacin 显示文摘 | Dhaneshwar S Tewari K Joshi S | 2011 | Chemistry and Physics of Lipids2011，164，： | 1 |
| 12 | Design 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 | 2013 | Inflammation & Allergy-Drug Targets2013，，5： | 1 |
| 13 | Colon-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 | 2008 | European Journal of Medicinal Chemistry2008，，1： | 1 |
| 14 | 'The real exchange rate and macroeconomic performance in Sub-Saharan Africa,'显示文摘 | Ghura Dhaneshwar Thomas J.Grennes | | 0，，01： | 1 |
| 15 | Dextran: a promising macromolecular drug cartier 显示文摘 | DHANESHWAR S S KANDPAL M GAIROLA N | 2006 | Indian J Pharm Sci2006，68，6： | 1 |
| 16 | Application of a stability-indicating HPTLC method for quantitative analysis of amtolmetin guacil in a pharmaceutical dosage form 显示文摘 | VK Bhusari MVM SR Dhaneshwar | 2009 | Acta Chromatographica2009，21，2： | 1 |
| 17 | Investigation 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 | 2017 | World Journal of Gastroenterology2017，23，7： | 1 |
| 18 | The real exchange rate and macroeconomic performance in Sub-Saharan Africa显示文摘 | Ghura Dhaneshwar Grennes Thomas J | 1993 | Journal of Development Economics1993，42，1： | 1 |
| 19 | The real exchange rate and macroeconomic performance in Suh-Saharan Africa显示文摘 | Ghura Dhaneshwar Grennes Thomas J | 1993 | Journal of Development Economics1993，42，1： | 1 |
| 20 | The structure of 24-methylene-9, 19-cyclolanostan-313-yl acetate 显示文摘 | Dhaneshwar N N Puranik V G Tavale S S | 1986 | Acta Cryst1986，42，5： | 1 |
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