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Radiopharmaceuticals for diagnosis of Primary Hyperparathyroidism

Hyperparathyroidism (HPTH) is a condition in which the level of parathyroid hormone in blood is raised. Gold standard for the diagnosis of HPTH is a measurement of serum parathyroid hormone levels, accompanied by testing serum calcium levels, to differentiate between primary and secondary HPTH. The first line of treatment with primary HPTH is surgery to remove the adenoma or the tumor, whenever possible. It is in these cases that the imaging plays an important role for localization of tumor before surgery.Imaging can be anatomical that is ultrasound, CT and MRI or functional that is using nuclear medicine modalities (SPECT, SPECT/CT, PET/CT). This article reviews the nuclear medicine modalities, various radiopharmaceuticals and imaging techniques for parathyroid imaging.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/726

      

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Radiolabelled nanoparticles in cancer treatment: current status and developments

The current concepts of cancer therapy are moving towards personalized treatment regimen aiming to reduce toxicity and improve efficacy of therapeutic agents. With the development of molecular imaging and targeted therapies personalized care has received a shot in the arm. However, these developments are not without challenges. Drug delivery, metabolism, toxicity etc. challenge the effective utilization of such agents. Nanoparticles offer to overcome these hurdles with their unique physico-chemical properties which can be labeled with radionuclides and conjugated with ligands to achieve high specific activity in the intended areas. In this article, we discuss the present status of radiolabeled nanoparticles, the areas where they are being used and challenges that lie ahead. We intend to provide a basic outlook on the utilization of radiolabeled nanoparticles in cancer diagnosis and therapy.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/728

      

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Synthesis and Evaluation of [DUPA-6-Ahx-Lys (DOTA)-6-Ahx-RM2], a Novel, Bivalent Targeting Ligand for GRPr/PSMA Biomarkers of Prostate Cancer

In this study, we have prepared a novel, dual-biomarker, targeting ligand having high affinity and specificity for PSMA/GRPr receptors that are expressed on most prostate cancers. [DUPA-6-Ahx-Lys(DOTA)-6-Ahx-RM2] was synthesized and the new conjugate was metallated macroscopically with GaCl3, InCl3, and LuCl3 to form [DUPA-6-Ahx-Lys(M-DOTA)-6-Ahx-RM2] (where M = Ga, In, or Lu). These new agents, when radiolabeled with Ga-68, In-111, or Lu-177 hold theranostic potential for patients presenting with prostate cancer disease.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/718

      

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Synthesis and evaluation of a novel 68Ga-NODAGA-Erlotinib analogue towards PET imaging of Epidermal Growth Factor Receptor over-expressing cancers

In this paper we report the synthesis of 68Ga labeled NODAGA-Erlotinib for imaging of EGFR over-expressing tumors. NODAGA-Erlotinib conjugate was synthesized by reaction of the terminal alkyne of Erlotinib using Cu catalyzed click reaction. The conjugate was then radiolabeled with 68Ga in high radiochemical yields. The 68Ga NODAGA-Erlotinib conjugate also exhibited high in vitro stability. The log P value of 68Ga-NODAGA-Erlotinib was lower than that of 68Ga-NOTA-Erlotinib, a 68Ga based Erlotinib conjugate previously reported by our group. In the in vitro cell binding studies carried out in EGFR-positive A431 cells, 68Ga-NODAGA-erlotinib exhibited an uptake (7.8±1.3 %) lower than that of 68Ga-NOTA-Erlotinib (9.8±0.4%) showing that an increase in hydrophilicity possibly effected a decrease in cell permeability. The higher hydrophilicity of 68Ga-NODAGA-Erlotinib also led to significantly lower accumulation of 68Ga-NODAGA-Erlotinib in non-target organs in the biodistribution studies in Swiss mice. The overall properties of the 68Ga-NODAGA-Erlotinib conjugate are promising and reflect the role of hydrophilicity in reducing the non-specific uptake of the final radiotracer towards improving signal/noise ratio for further imaging studies.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/727

      

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Optimization of recovery of antioxidants from the coconut shell using Response Surface Methodology

Coconut shell is an important byproduct of Cocos nucifera L. which is largely being wasted. The present study is focused on optimizing the extraction process of phenolic compounds and also to evaluate its physico-chemical and antioxidant properties. After studying the effect of different solvents and different extraction conditions, methanol was found to be the most effective solvent and extraction at 90oC was suitable to give high phenolic yield (4045 mg GAE/100 g). For further precision of the ideal conditions, response surface methodology was carried out to optimize the solvent concentration, temperature and extraction time. The results revealed that methanol at 72%, extraction time 167 min and temperature 68oC yielded maximal level of polyphenols from coconut shell. Both extraction temperature and solvent concentration were found to have significant effect on the phenolic yield. Suitable conditions could be applied to recover the antioxidant phenolic compounds from the coconut shell, an agricultural byproduct available at huge quantity in India. The physico-chemical and antioxidant properties of methanolic extract of coconut shell were noticed to be suitable for its application in food and pharmaceutical industries.

Source:: http://www.pubs.iscience.in/journal/index.php/jbts/article/view/681

      

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Current trends in nanomedicine and nanobiotechnology research

Applications of Nanoparticles and nanopharmulations in drug development and drug delivery have been an extensive field of research to find out the alternative better therapeutics. The past research in nanomedicine and nanobiotechnology mostly emphasized on improving the profile of existing drugs, however, a recent pattern has seen in variation of field and aspects studied using nanomedicine. The current nanomedicine research has oriented in developing new drugs based on the interaction of nanoparticles on targets like cancer therapeutics, development of new biosensors, bioimaging (cellular and in vivo), new vistas of anti-viral drugs, besides the most researched field of nano delivery of drugs for cancer, diabetes, anti-bacterial, and other ailments. An overview of current research trends is presented based on the literature published at different platforms in recent time.

Source:: http://www.pubs.iscience.in/journal/index.php/appnanomed/article/view/747

      

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Synthesis of novel 2-(3-aryl/alkylamino propoxy)-12-aryl xanthene derivatives as antifungal and antibacterial agents

By Bhaskara Nand, Kalawati Meena, Shruti Gupta, J.M. Khurana, Amita Malik, Chetan Sharma, Harsh Panwar A series of novel 2-(3-aryl/alkylaminopropoxy)-12-aryl-9,10-dihydro-8H– benzo[a]xanthen-11-one derivatives were synthesized from 2-hydroxy-12-aryl 9,10-dihydro-8H-benzo[a]xanthen-11-ones by reaction with 1-bromo-3-chloropropane in presence of K2CO3 in dry acetone under reflux followed by reaction with aryl/alkyl amines in presence of KI in dry DMF at 100oC. Structures have been confirmed by spectroscopic analysis. All the newly synthesized 2-(3- aryl/alkylaminopropoxy)-12-aryl xanthene derivatives were screened for their antimicrobial activity against four microbial strains Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa. The selected synthesized compounds showed moderate antimicrobial activity.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/695

      

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Antiquorum sensing activity of selected Eritrean traditional medicinal plants against Pseudomonas aeruginosa

By Jeevan Jyoti Kaushik, Yacob Tesfamichael Keleta, Danait Kebede Emha, Estifanos Okbay Ghebrehans, Henok Tekie Araya, Kisanet Habtemichael Gebregziabher, Kisanet Teklemariam Kifle, Nabait G. Weldetnsaie, Atul Kaushik

The discovery of bacterial-communication systems (quorum-sensing systems), which orchestrate important temporal events during the infection process, has afforded a novel opportunity to ameliorate bacterial infection by means other than growth inhibition. In this study three different assays were performed; Las-A staphylolytic assay, anti-swarming assay, pyocyanin assay. In the anti-swarming activity, the highest anti-swarming activity were seen in the chloroform and petroleum extract of O.fruticosa. In the Las-A activity, the highest reduction in Las-A activity was seen in the chloroform extract of V.sinaiticum (70.5%) and also petroleum extract of V.sinaticum and chloroform extract O.fructicosa (70.3%).In the Pyocyanin assay, the chloroform extract of O.fructicosa and V.sinaiticum showed more significant effect in decreasing the Pyocyanin production by 81.8% and 79.5% respectively.

Source:: http://www.pubs.iscience.in/journal/index.php/jbts/article/view/685

      

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Narrative treatment of GERD: focus on the lower esophageal sphincter (LES) using raft forming in-situ gelling system

By Shalinee Jain, Dharmendra Jain Gastroesophagus reflux disease, acidity and hearts burning are the most common problems, which can be overcome by the raft forming in-situ gel system containing combination of H2 antagonist and GABAB antagonist as well as raft forming agents (alginate, pectin etc.). GERD develops when the reflux of the gastric contents occur into the esophagus which cause various complication into GIT. The main cause of GERD is an abnormal lower esophageal sphincter (LES) pressure and increased reflux during transient LES relaxation. This review mainly focus on the formulation development for reducing the transient lower esophageal sphincter relaxation (TLESR) rate, attenuating esophageal sensitivity and developing esophageal mucosal protectants. For this purpose GABAB is used which reduces TLESR rate by 40-50% and reflux episodes by 70%, also increase LES pressure and H2 antagonist is used as antisecretory agent in terms of symptomatic relief and mucosal healing. The combined effect of raft forming gelling system is more effective. The review also focuses on the physiological factors, physicochemical factors and formulation factors to be considered in the development of the raft forming system.

Source:: http://www.pubs.iscience.in/journal/index.php/jbts/article/view/688

      

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Synthesis, antimicrobial and antimalarial study of novel 1,3,4-thiadiazole derivatives incorporating imidazo [1,2-b] pyridazine and thiazolidinone moieties

By Ashish Bhatt, Rajesh Kumar Singh, Ravi Kant A new class of 1,3,4-thiadiazole derivatives 8a-i incorporating imidazo [1,2-b] pyridazine and thiazolidinone moieties were synthesized by the reaction of arylidene derivatives of 1,3,4-thiadiazoles 2-amine having imidazo [1,2-b] pyridazine moiety (Schiff base) 7a-i with thioglycolic acid. Schiff base 7a-i were synthesized by the reaction of 1,3,4-thiadiazoles 2-amine having imidazo [1,2-b] pyridazine moiety 6 with substituted benzaldehyde. These were screened for in-vitro antimicrobial activity against two gram positive (Streptococcus Pyogenes and Staphylococcus aureus) and two gram negative bacteria (Pseudomonas aeruginosa and Escherichia coli) as well as for antifungal and antimalarial activity against plasmodium falciparum strain. Compound 8a and 8b exhibited good antimicrobial and antimalarial activity.

Source:: http://www.pubs.iscience.in/journal/index.php/cbl/article/view/677

      

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