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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

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World Journal of Gastroenterology 2017年第7期23卷 1147-1162页

作者： Ajinkya sarkate suneela s dhaneshwar Department of Pharmaceutical Chemistry Poona College of PharmacyBharati Vidyapeeth UniversityMaharashtra 411038India

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 *** 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 sease controls using one-way and two-way *** 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 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.

关键词：煽动性的肠疾病 Boswellic 酸互补、其他的药指向冒号相互的 prodrugs 氨基酸导致 TNBs 的大肠炎

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Colon-specific prodrugs of 4-aminosalicylic acid for inflammatory bowel disease

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World Journal of Gastroenterology 2014年第13期20卷 3564-3571页

作者： suneela s dhaneshwar Department of Pharmaceutical Chemistry Poona College of PharmacyBharati Vidyapeeth Deemed UniversityPune-411 038MaharashtraIndia

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 *** 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 *** 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,*** 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 *** review also emphasizes the need for reappraisal of this promising but unexplored entity as a potential treatment option for IBD.

关键词： 4-Aminosalicylic acid 5-Aminosalicylic acid sulfas

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Role of prebiotics, probiotics, and synbiotics in management of inflammatory bowel disease: Current perspectives

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World Journal of Gastroenterology 2023年第14期29卷 2078-2100页

作者： supriya Roy suneela dhaneshwar Amity Institute of Pharmacy LucknowAmity University Uttar PradeshSector 125Noida 201313Uttar PradeshIndia Amity Institute of Pharmacy Amity University MaharashtraMumbai 410206MaharashtraIndia

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 *** 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 *** 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 *** 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 *** 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 *** 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 *** 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

关键词： Ulcerative colitis Crohn’s disease Pouchitis Dysbiosis Microbiota Inflammation

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Correction to“Role of prebiotics,probiotics,and synbiotics in management of inflammatory bowel disease:Current perspectives”

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世界胃肠病学杂志:英文版 2023年第35期29卷 5178-5179页

作者： supriya Roy suneela dhaneshwar Department of Pharmacology Amity Institute of PharmacyLucknowAmity University Uttar PradeshNoida 201303Uttar PradeshIndia Department of Pharmaceutical Chemistry Amity Institute of PharmacyAmity University MaharashtraMumbai 410206MaharashtraIndia

Correction to“Roy s,dhaneshwar *** of prebiotics,probiotics,and synbiotics in management of inflammatory bowel disease:Current *** J Gastroenterol 2023;29:2078-2100[PMID:37122604 DOI:10.3748/wjg.v29.i14.20-78]”.In t... 详细信息

关键词： Ulcerative colitis Crohn’s disease Pouchitis Dysbiosis Microbiota Inflammation

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Determination of the mitigating effect of colon-specific bioreversible codrugs of mycophenolic acid and aminosugars in an experimental colitis model in Wistar rats

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World Journal of Gastroenterology 2018年第10期24卷 1093-1106页

作者： shakuntala santosh Chopade suneela sunil dhaneshwar Department of Pharmaceutical Chemistry Poona College of Pharmacy Bharati Vidyapeeth University

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 *** 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.

关键词： Mycophenolic acid Mutual prodrug Inflammatory bowel disease Mycophenolate mofetil

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Amelioration of hepatotoxicity by biocleavable aminothiol chimeras of isoniazid: Design, synthesis, kinetics and pharmacological evaluation

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World Journal of Hepatology 2018年第7期10卷 496-508页

作者： Neha Vithal Bhilare suneela sunil dhaneshwar Kakasaheb Ramoo Mahadik Department of Pharmaceutical Chemistry Poona College of Pharmacy Bharati Vidyapeeth University

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 *** 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 *** 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.

关键词： Aminothiols antioxidants N-acetyl cysteine N-(2-mercaptopropionyl)glycine isoniazid L-methionine liver injury tuberculosis

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