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Juvekar, Vinayak,Gong, Young Dae American Chemical Society 2016 ORGANIC LETTERS Vol.18 No.4
<P>The design, synthesis and utilization of an efficient acetamidomethyl derived resin for the peptide synthesis is presented using established Fmoc and Boc protocols via side chain anchoring. Cleavage of the target peptide from the resin is performed using carboxymethylsulfenyl chloride under mild conditions which gave in situ thiol-sulfenyl protection of the cysteine residues. The utility of the resin is successfully demonstrated through applications to the syntheses of model peptides and natural products Riparin 1.1 and Riparin 1.2.</P>
Vinayak Juvekar,김강태,공영대 대한화학회 2017 Bulletin of the Korean Chemical Society Vol.38 No.1
A very effective process on Pyroacm resin was developed for solid-phase peptide synthesis (SPPS) of C-terminal cysteine and cysteine ester peptides. The process uses cysteine side chain anchoring to the Pyroacm resin and the Boc protocol for SPPS. The Pyroacm resin showed remarkable stability under standard trifluoromethanesulfonic acid (TFMSA) cleavage condition. TFMSA cleavage of protecting groups generates a peptide-linked resin, which can be subjected to peptide modification reactions. Finally, the peptide can be cleaved from the resin using methoxycarbonylsulfenyl chloride. The utility of this protocol was demonstrated by its applications to the synthesis of model peptides, key intermediates in the preparation of natural products riparin 1.2 and a-factor.
Abhishek Mahajan,Amar Udare,Tanuja Shet,Shashikant Juvekar,Meenakshi Thakur 대한영상의학회 2013 Korean Journal of Radiology Vol.14 No.4
Metastases to intramammary nodes have been shown to be an independent predictor of poor outcome in patients with breast cancer, such as axillary lymph node metastases. The detection and accurate characterization of these nodes preoperatively is thus crucial for the staging and planning of treatment for breast carcinoma, particularly in cases with axillary lymph node negative disease as it upgrades the disease staging. We herein report the first case where we detected an intra-mammary node on specimen MRI after the primary pathological gross specimen evaluation failed to detect the node.
Snehal Nitin Mestry,Archana Ramesh Juvekar 경희대학교 융합한의과학연구소 2017 Oriental Pharmacy and Experimental Medicine Vol.17 No.3
Cataract is one of the primitive secondary complications of diabetes mellitus and contributes to 50% blindness worldwide. Aldose reductase (AR) is the first and rate limiting enzyme in the intracellular polyol pathway responsible for the development of cataract. Thus, there is an imperative need for modest, non-surgical way in order to treat cataract. In Ayurveda, Punica granatum (Pomegranate) is considered as “a pharmacy unto itself”. Pomegranate leaves are traditionally used for their anti-diabetic activity. In this study, we investigated AR inhibitory activity and anti-cataract potential of Pomegranate leaves in glucose - induced cataract in goat lens. AR inhibitory activity was evaluated in vitro in goat lenses. In glucose induced cataract model, goat lenses were incubated in artificial aqueous humor containing 55 mM glucose along with methanolic extract of Punica granatum leaves (MPGL) or quercetin for 72 h. After 72 h, photographic evaluation of the lens was carried out and the lens antioxidant parameters were determined. Different concentrations of MPGL were found to inhibit lens AR activity with an IC50 value of 83.55 ± 3.92 μg/ml. Quercetin was taken as positive control which exhibited 56.461% AR inhibition at a concentration of 500 μg/ml. Cataractous lenses exhibited marked opacity and decrease in the levels of reduced glutathione and superoxide dismutase. Treatment with MPGL and quercetin prevented the opacity and restored back the antioxidant activity. Together, Punica granatum leaves ameliorated glucose-induced cataractogenesis via AR inhibition, reduction in oxidative stress and improvement in antioxidant defense system.
Amar Udare,Nilesh Sable,Rajiv Kumar,Meenakshi Thakur,Shashikant Juvekar 대한영상의학회 2015 Korean Journal of Radiology Vol.16 No.1
Solitary metastases from colorectal carcinoma in the absence of hepatic or pulmonary metastases are rare. These can have a diverse imaging appearance, particularly after chemotherapy. It is important identify patients with solitary skeletal metastases, as they have a better prognosis than those with multiple skeletal or visceral metastases. We describe an unusual case of a solitary metastasis to the femur in a case of colon carcinoma that went undiagnosed and later presented with imaging features of osteogenic sarcoma.
Kim, Nayeon,Kwak, Se Hun,Lee, Seon-Hyeong,Juvekar, Vinayak,Lee, Byung-Il,Ahn, Hee-Chul,Kim, Soo-Youl,Gong, Young-Dae The Royal Society of Chemistry 2014 Organic & Biomolecular Chemistry Vol.12 No.27
<P>In the process of optimization, we developed a novel core skeleton of thieno[3,4-<I>b</I>]pyrazine <I>via</I><B>GK-13</B>. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-<I>b</I>]pyrazine derivatives were shown to exhibit promising activity for use as potential therapeutic small-molecules in renal cancer by inhibiting TGase 2 activity.</P> <P>Graphic Abstract</P><P>In the process of optimization, we developed a novel core skeleton of thieno[3,4-<I>b</I>]pyrazine <I>via</I><B>GK-13</B>. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=c4ob00179f'> </P>
Snehal Nitin Mestry,Nitin Bhanudas Gawali,Malvika Sunil Gursahani,Sarayu Arvind Pai,Jayesh Bachu Dhodi,Archana Ramesh Juvekar 경희대학교 융합한의과학연구소 2018 Oriental Pharmacy and Experimental Medicine Vol.18 No.2
Advanced glycation end products (AGEs) are the consequent products by virtue of non-enzymatic reaction of reducing sugars with amino groups present either in lipids, nucleic acids or proteins. Lately AGEs have been embroiled in the inception of diabetes induced complications. In Ayurveda, Punica granatum is contemplated as “a pharmacy unto itself”. Punica granatum leaves have been stated to have anti-diabetic activity. The purpose of the existing study was to determine the anti-glycation potential of methanolic extract of Punica granatum leaves (MPGL) and investigate the fundamental mechanisms in discouraging the glycation process. Antioxidant activity of MPGL was estimated by DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (3-ethyl-benzothiazoline-6-sulfonic acid) radical scavenging assays. Both MPGL and aminoguanidine were evaluated against the formation of AGEs. Antiglycation activity was evaluated by determining the fluorescence intensity of AGEs and formation of fructosamine. Protein oxidation in the glycation process was determined by evaluating the protein carbonyl content and thiol group. MPGL demonstrated IC50 value of 15.602 ± 0.296 and 724.323 ± 16.451 µg/ml for the DPPH and ABTS radical scavenging assays respectively. Current study revealed that MPGL had cogent effects on the in vitro formation of AGEs. MPGL decreased fructosamine level and significantly counteracted the oxidative damage of protein by curbing protein carbonyl content and impeding the loss of thiol group. The anti-glycation activity was farther cogent than the glycation inhibitory activity attained using the standard drug, aminoguanidine. Thereupon, MPGL presents to be more encouraging to be emerged as an competent AGE inhibitor.