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Synthesis of Ibuprofen Conjugated Molecular Transporter Capable of Enhanced Brain Penetration
Biswas, Goutam,Kim, Wanil,Kim, Kyong-Tai,Cho, Junhwi,Jeong, Dongjun,Song, Keon-Hyoung,Im, Jungkyun Hindawi Limited 2017 Journal of chemistry Vol.2017 No.-
<P>Based on the strong evidences between inflammation and neurodegeneration, nonsteroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen, are considered as effective agents to reduce the risk of Alzheimer’s and Parkinson’s disease. However, the clinical use of NSAIDs in these diseases is limited by low brain distribution. In this study, we had synthesized ibuprofen conjugate which has good brain penetration.<I> S</I>-(+)-Ibuprofen was covalently attached to a molecular transporter having FITC and eight terminal guanidine groups. This conjugate showed good cellular uptake property in live cells. It was also injected into a mouse and the distribution of the compound was examined in each organ. The conjugate was well delivered to mouse brain indicating the conjugate is able to cross the blood-brain barrier. Our novel synthetic ibuprofen conjugate will hopefully deliver other NSAIDs into brain and is therefore applicable to the neurodegenerative diseases treatment or prevention.</P>
임정균,Goutam Biswas,김완일,김경태,정성기 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.3
5-Fluorouracil (5-FU), an anticancer agent was covalently attached to the recently developed sorbitol-based G8transporter, and the conjugate (7) with FITC was found to have an affinity toward mitochondria and to readily cross BBB to gain an entry into mouse brain. Measured by IC_50, the conjugate (9) without the fluorophore showed enhanced cytotoxic activity toward two types of multidrug-resistant cell lines. These results strongly suggest that the sorbitol-based G8 transporter can be utilized as a good CNS delivery vector.
Unusual truncation of <i>N</i>-acylated peptoids under acidic conditions
Kim, Soomin,Biswas, Goutam,Park, Shinae,Kim, Arim,Park, Hyunjung,Park, Eunsook,Kim, Jeongmi,Kwon, Yong-Uk The Royal Society of Chemistry 2014 Organic & biomolecular chemistry Vol.12 No.28
<P>The terminal amino groups of peptoids have often been protected with acetyl groups to improve cell permeability and therapeutic potential, and to prevent the poisoning of the catalysts in organometallic reactions. Interestingly, the unusual truncation of the terminal peptoid unit has sometimes been encountered when the acetylated linear peptoids were treated with a TFA cleavage cocktail. In this study, we systematically investigated the electronic effects of acyl groups on the truncation of <I>N</I>-acylated peptoids to rationalize the formation of the deleted peptoids and to establish an appropriate strategy for preventing such undesired truncation.</P> <P>Graphic Abstract</P><P>Systematic studies on the unusual truncation of <I>N</I>-acylated peptoids were carried out to examine the electronic effects of acyl groups, and thus to control the formation of deletion sequences based on a plausible mechanism. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=c3ob42572j'> </P>
Surjyo Jyoti Biswas,Goutam Ghosh 셀메드 세포교정의약학회 2014 셀메드 (CellMed) Vol.4 No.3
Ethanolic leaf extract of Bauhinia variegata has been tested for its possible antioxidant potentials against sodium arsenite induced toxicity in mice. Mice were randomized into two groups of five and fifty mice. Group I consisting of 5 mice without any treatment with food and water ad libitum which served as normal control. Group II mice were fed with sodium arsenite in drinking water at 100 ppm concentration for two monthsthen they were segregated into five groups which were treated differently. Group II a mice received only arsenic as sodium arsenite with drinking water, Group II b were fed chronically 1 : 20 alcohol to distilled water (vehicle), Group II c, d, e mice were orally fed 50 mg/kg, 150 mg/kg and 250 mg/kg of B. variegata leaf extract of once daily for 15 and 30 days respectively along with arsenic. Several toxicity marker enzymes such as gamma glutamyl transferase, lactate dehydrogenase, aspartate and alanine aminotransferase, acid and alkaline phosphatase, catalase and superoxide dismutase along with haematological variables such as glucose 6-phosphate dehydrogenase, creatinine, bilirubin, haemoglobin and sugar in different groups of treated and control mice were studied. Results obtained from the in vivo experiment revealed that administration of sodium arsenite caused a significant increase in some enzymes while decrease in some. A similar trend was also observed with haematological variables. In contrast B. variegata treatment at 150 mg/kg favourably modulated these alterations and maintained the antioxidant status than other two doses i.e. 50 mg/kg and 250 mg/kg thereby making it a good candidate to be used as supportive palliating measures in arsenic induced toxicity.
Poulami Sarangi,Himani Biswas,Salil K. Gupta,Goutam K. Saha 한국응용곤충학회 2012 Journal of Asia-Pacific Entomology Vol.15 No.1
Two new species, Podapolipus husbandi and Podapolipoides channabasavannai, collected on Oxya sp. from West Bengal, India are described and illustrated.
Im, Jung-Kyun,Biswas, Goutam,Kim, Wan-Il,Kim, Kyong-Tai,Chung, Sung-Kee Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.3
5-Fluorouracil (5-FU), an anticancer agent was covalently attached to the recently developed sorbitol-based G8 transporter, and the conjugate (7) with FITC was found to have an affinity toward mitochondria and to readily cross BBB to gain an entry into mouse brain. Measured by $IC_{50}$, the conjugate (9) without the fluorophore showed enhanced cytotoxic activity toward two types of multidrug-resistant cell lines. These results strongly suggest that the sorbitol-based G8 transporter can be utilized as a good CNS delivery vector.
정동준,Tarun Pal,김형주,김태완,Goutam Biswas,이다은,Tejinder Singh,Akula S. N. Murthy,김완일,김경태,임정균 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.12
Camptothecin (CPT) and its derivatives are the only chemical class that targets the enzymatic activity of DNA topoisomerase I, which is involved in DNA damage and subsequent cell apoptosis. Despite CPT's advantages, its use has been restricted due to extremely poor solubility, drug resistance by several efflux pumps, short half-life, and poor bioavailability. To overcome these limitations, we designed and synthesized a water-soluble CPT-conjugated molecular transporter that successfully and rapidly delivered CPT into cells. The conjugate had affinity toward mitochondria inside cells and it was distributed mainly to kidney, lung, and spleen. MTT assay confirmed that the CPP-conjugate decreased cell viability of colon cancer cell lines to a much greater extent than the parent drug. This novel approach has the potential of improving CPT efficacy for future in vivo applications, especially for colon cancer therapy.
Jin, Juyoun,Lee, Woo Sirl,Joo, Kyeung Min,Maiti, Kaustabh K.,Biswas, Goutam,Kim, Wanil,Kim, Kyong-Tai,Lee, Se Jeong,Kim, Kang-Ho,Nam, Do-Hyun,Chung, Sung-Kee Royal Society of Chemistry 2011 MedChemComm Vol.2 No.4
<P>The per oral administration of compound 1, prepared by covalently attaching paclitaxel to a molecular carrier, shows good anti-tumor activity in the orthotopic mouse model of glioblastoma. The anti-tumor effects may be attributable to the cytotoxicity as well as the anti-angiogenic activity of the paclitaxel conjugate or paclitaxel itself in the brain parenchyma.</P> <P>Graphic Abstract</P><P>The per oral administration of 1, prepared by covalently attaching paclitaxel to a molecular carrier, shows good anti-tumor activity in the orthotopic mouse model of glioblastoma. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=c0md00235f'> </P>
Chanchal Das,Narendra Nath Ghosh,Ritu Bhardwaj,Kritika Narula,Prashant Mishra,Goutam Biswas 한국공업화학회 2023 Journal of Industrial and Engineering Chemistry Vol.128 No.-
Every year, due to usage, overproduction, and overprescribing, a huge amount of pharmaceutical wasteaccumulates. Among these, hydrocortisone (a corticosteroid) has lately been popular for COVID-19 therapy. Hence, removal of these pollutants by efficient, cheaper and greener way is needed. The photocatalyticdegradation of hydrocortisone by nanoparticles has yet to be investigated. In this study, thehydro-alcoholic extract of Nigella sativa seeds coated magnetite nanoparticles (NS@MNPs) was synthesizedas a low-cost, sustainable photocatalyst to degrade hydrocortisone from simulated wastewater. At neutral pH, the highest degradation percentage 97.1% was achieved with 15 mg of NS@MNPs within540 min for a 10 mL 60 mg/L of hydrocortisone solution. Experimentally, it was observed that the degradationwas more specific at 254 nm irradiation. The mechanism of degradation was established by scavengingexperiments, density functional theory (DFT) calculations, and liquid chromatography-massspectroscopy analysis of the treated simulated wastewater. Due to the presence of naturally occurringions, the degradation of hydrocortisone by NS@MNPs in the surface water was reduced. FTIR spectra after12th cycle revealed that the coating of NS@MNPs remains unchanged, thus increasing recyclability. NS@MNPs were also proved to be nontoxic towards NIH/3T3 normal cells at micromolar concentrations,demonstrating its vast applicability.