02086nas a2200157 4500008004100000245014300041210006900184260000800253520141500261100002401676700002101700700002501721700002801746700002201774856013201796 2018 eng d00aChemo-biological evaluation of antidiabetic activity of M entha arvensis L. and it's role in inhibition of advanced glycation end products0 aChemobiological evaluation of antidiabetic activity of M entha a cFEB3 a

Background: There has been enormous curiosity in the development of alternative plant based medicines to control diabetes, oxidative stress and related disorders. One of the therapeutic approaches is to reduce postprandial release of glucose in the blood. Two key enzymes that are involved in reducing postprandial glucose are α-amylase and α-glucosidase. Mentha arvensis L. has been traditionally used by several tribes as a medicinal plant to treat various disorders. Objective: The present study was undertaken to test M. arvenisis L. for inhibition of postprandial hyperglycemia. Material and method: We performed various in vitro and in vivo tests to evaluate efficacy of M. arvenisis L. for antidiabetic activity (postprandial hyperglycemia). Results: Methanolic extract of M. arvensis L. leaves showed DPPH free radical scavenging activity (more than 78% μg/μl) and high antiglycation potential (more than 90% inhibition of AGE formation). Methanolic extract also showed remarkable inhibitory effects on α-amylase (more than 50% μg/μl) and α-glucosidase (68% μg/μl) and significant inhibition of postprandial hyperglycemia in starch induced diabetic Wistar rats. Conclusion: The non-insulin dependent antidiabetic or inhibition of postprandial hyperglycemic activity of methanolic extract of M. arvensis L. leaves was shown by using in vitro and in vivo approaches in the present study.

1 aAgawane, Sachin, B.1 aGupta, Vidya, S.1 aKulkarni, Mahesh, J.1 aBhattacharya, Asish, K.1 aKoratkar, Santosh uhttps://library.ncl.res.in/content/chemo-biological-evaluation-antidiabetic-activity-m-entha-arvensis-l-and-its-role-inhibition02887nas a2200169 4500008004100000245008700041210006900128260000800197520226400205100002002469700001802489700002502507700002502532700002202557700003002579856010802609 2018 eng d00aPatho-physiological evaluation of Duranta erecta for the treatment of urolithiasis0 aPathophysiological evaluation of Duranta erecta for the treatmen cMAY3 a

Background: Urolithiasis is the third common disorder of the urinary system affecting 10-15% of the general population. In recent years, search for new antilithiatic drugs from natural sources has assumed greater importance. Objectives: This study was performed to investigate the anti-urolithiatic activity of methanolic extract of Duranta erecta leaves by in vitro and in vivo analysis. Materials and methods: The study was designed to determine presence of phytochemicals in D. erecta, its yield in percentage, antioxidant activity against 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and anti-microbial property against few bacteria. In vitro analysis was carried out study anti-urolithiatic property of D. erecta by nucleation assay and synthetic urine assay for inhibition of calcium oxalate and calcium oxalate monohydrate crystals formation. An in vivo experiment was performed on Wistar rats for confirmation of anti-urolithiatic property of D. erecta in animal model. Results: D. erecta has the presence of primary and secondary metabolites like glycoside, saponins, sterols, flavonoids, phenols, tannins, alkaloids, carbohydrates and proteins. Methanolic extract of D. erecta gave a very good yield (60%). D. erecta proved its antioxidant potential by 93.51% inhibition of DPPH radical at a concentration of 1000 μg/mL where ascorbic showed 94.71% of DPPH radical at the same concentration. In vitro tests like nucleation assay and synthetic urine assay showed that D. erecta inhibits formation of calcium oxalate and calcium oxalate monohydrate crystals. It also showed the anti-microbial property by formation of zone of inhibition against few bacteria. An in vivo experiment on Wistar rat animal model confirmed the anti-urolithiatic property of D. erecta L. leaves extract. Conclusions: Based on the results, we reported that D. erecta may treat calcium oxalate crystal deposition in the kidney by preventing hyperoxaluria-induced peroxidative damage to the renal tubular membrane surface (lipid peroxidation). It has anti-microbial potential so it may also inhibit the secondary bacterial infection in kidney. Based on the data, it can be concluded that this herb can be used as a potential anti-urolithiasis agent for kidney stone removal.

1 aAgawane, S., B.1 aGupta, V., S.1 aKulkarni, Mahesh, J.1 aBhattacharya, A., K.1 aKoratkar, Santosh1 aRao, Vankudoth, Koteswara uhttps://library.ncl.res.in/content/patho-physiological-evaluation-duranta-erecta-treatment-urolithiasis02817nas a2200289 4500008004100000022001400041245017700055210006900232260000800301300001100309490000800320520181800328653002102146653001502167653002302182653001502205653001602220653001302236100002502249700001802274700002202292700002202314700001902336700002802355700002202383856012202405 2020 eng d a0928-493100aLHRH-conjugated, PEGylated, poly-lactide-co-glycolide nanocapsules for targeted delivery of combinational chemotherapeutic drugs Docetaxel and Quercetin for prostate cancer0 aLHRHconjugated PEGylated polylactidecoglycolide nanocapsules for cSEP a1110350 v1143 a

One of the major challenges in effective cancer chemotherapy is the severe systemic cytotoxicities of anticancer drugs on healthy tissues. The present study reports chemically modified polymeric nanocapsules (NCs) encapsulating combination of chemotherapeutic drugs Docetaxel (DTX) and Quercetin (QU) for its active targeting to prostate cancer (PCa). The active targeting was achieved by conjugating Luteinizing-hormone-releasing hormone (LHRH) ligand to poly-lactide-co-glycolide (PLGA) using polyethylene glycol (PEG) as a spacer. The structure of the conjugates was characterized and confirmed using H-1 NMR and ATR-FTIR. The drug encapsulated NCs showed a homogenous size distribution with their size ranging between 120 and 150 nm, and exhibited a negative zeta potential in the range of - 20 to - 40 mV. The in vitro release studies highlighted the sustained drug release pattern from the respective NCs; while the PEG coating to polymeric NCs provided serum stability to the NCs. The in vitro biological evaluation of the NCs was conducted using PC-3 and LNCaP cell lines. The results of the cellular uptake studies showed a significantly higher untake of the LHRH targeted NCs, while the LHRH-targeted-PEGylated DTX: QU NCs exhibited higher caspase-3 activity. The cell viability assay results showed the enhanced cell inhibition activity of the combinatorial DTX: QU when compared to individual DTX. Further, higher cell cytotoxicity was achieved by LHRH-targeted DTX: QU NCs as compared to their free-form or non-targeted NCs. Finally, the results of in vivo tumor localization and in vivo antitumor activity studies complimented and upheld the in vitro results, demonstrating the beneficial role of PLGA-PEG-LHRH NCs encapsulating combination of DTX and QU in combating prostate cancer (PCa).

10aActive targeting10aAnticancer10aControlled release10aEPR effect10aHydrophobic10aProstate1 aShitole, Ajinkya, A.1 aSharma, Neeti1 aGiram, Prabhanjan1 aKhandwekar, Anand1 aBaruah, Meghna1 aGarnaik, Baijayantimala1 aKoratkar, Santosh uhttps://library.ncl.res.in/content/lhrh-conjugated-pegylated-poly-lactide-co-glycolide-nanocapsules-targeted-delivery02151nas a2200241 4500008004100000245011400041210006900155260000800224300001200232490000600244520132800250100001701578700002101595700001701616700002001633700001901653700002501672700001701697700002201714700002001736700002101756856013201777 2022 eng d00aBehavioral and proteomic studies reveal methylglyoxal activate pathways associated with alzheimer’s disease0 aBehavioral and proteomic studies reveal methylglyoxal activate p cDEC a65–750 v63 a

Diabetes is one of the major risk factors for Alzheimer’s disease (AD) development. The role of elevated levels of glucose, methylglyoxal (MGO), and advanced glycation end products (AGEs) in the pathogenesis of AD is not well understood. In this pursuit, we studied the role of methylglyoxal in the pathogenesis of AD in rat models. The elevated plus-maze (EPM) behavioral study indicated that MGO induces anxiety. Treatment of telmisartan (RAGE expression inhibitor) and aminoguanidine (MGO quencher) attenuated MGO induced anxiety. Further, hippocampal proteomics demonstrated that MGO treated rats differentially regulate proteins involved in calcium homeostasis, mitochondrial functioning, and apoptosis, which may affect neurotransmission and neuronal plasticity. The hippocampal tau phosphorylation level was increased in MGO treated rats, which was reduced in the presence of aminoguanidine and telmisartan. The plasma fructosamine level was increased upon MGO treatment. Hippocampal histochemistry showed vascular degeneration and neuronal loss upon MGO treatment. This study provides mechanistic insight into the role of MGO in the diabetes-associated development of AD.

1 aPatil, Gouri1 aKulsange, Shabda1 aKazi, Rubina1 aChirmade, Tejas1 aKale, Vaikhari1 aMote, Chandrashekhar1 aAswar, Manoj1 aKoratkar, Santosh1 aAgawane, Sachin1 aKulkarni, Mahesh uhttps://library.ncl.res.in/content/behavioral-and-proteomic-studies-reveal-methylglyoxal-activate-pathways-associated-alzheimer02494nas a2200313 4500008004100000022001400041245014300055210007200198260000800270300001100278490000800289520141700297653002901714653001801743653003001761653001901791653001801810100002701828700002101855700001701876700002201893700001801915700002201933700001901955700001901974700002101993700002202014856014402036 2025 eng d a0882-401000aCharacterization of novel phages KPAФ1, KP149Ф1, and KP149Ф2 for lytic efficiency against clinical MDR Klebsiella pneumoniae infections0 aCharacterization of novel phages KPAФ1 KP149Ф1 and KP149Ф2 for l cMAY a1074400 v2023 a

Phage therapy offers a promising approach to the increasing antimicrobial resistance of Klebsiella pneumoniae. This study highlights three novel lytic bacteriophages-KPAc1, KP149c1, and KP149c2-targeting multidrugresistant (MDR) K. pneumoniae. These phages belong to the Myoviridae and Podoviridae family and demonstrate their efficacy and stability across a wide range of temperatures (up to 60 degrees C) and pH levels (pH 4 to 11). Genomic analysis reveals that they are free from virulence, toxicity, and antimicrobial resistance genes, making them promising candidates for therapeutic use. Among these phages, KPAc1 showed the highest lytic activity with a 26.15% lysis against MDR K. pneumoniae isolates. Additionally, a phage cocktail comprising all three phages improved lytic efficacy to 32.30%. This study also examined the antimicrobial resistance profiles of K. pneumoniae isolates, emphasizing the critical need for alternative treatments. By effectively targeting resistant strains, these phages offer a potential candidacy to be used as a viable alternative or a complementary antimicrobial agent to traditional antibiotics, opening up the possibility for advanced phage-based therapies. The promising results from this study pave the way for developing new treatments that could significantly improve patient care and outcomes from the growing issue of resistant bacterial infections.

10aAntimicrobial resistance10aBacteriophage10aMDR-Klebsiella pneumoniae10aPhage cocktail10aPhage therapy1 aDandekar, Shraddha, S.1 aThanikkal, Sinta1 aLondhe, Arti1 aBhutada, Pankhudi1 aSaha, Ujjayni1 aPawar, Shubhankar1 aSamson, Rachel1 aDharne, Mahesh1 aSaroj, Sunil, D.1 aKoratkar, Santosh uhttps://library.ncl.res.in/content/characterization-novel-phages-kpa%D1%841-kp149%D1%841-and-kp149%D1%842-lytic-efficiency-against-clinical