Posted by admin on Feb 29, 2020 in |
Radioisotopic imaging based on small molecules like carbohydrate has been regarded as a promising candidate for in-vivo imaging for cancer diagnosis in recent years. In this study, we report that N-acetyl neuraminic acid (Neu5Ac), a type of sialic acid with 9-carbon amino sugar and low pKa value coordinates with the transition radioactive metal 99mTc. The radiochemical yield of 99mTc labeled Neu5Ac was observed to be greater than 90% and was confirmed by Instant Thin Layer Chromatography. Molecular docking studies showed greater affinity of 99mTc labeled Neu5Ac towards the lectin receptor when compared to cold Neu5Ac. The radiolabeled complex (99mTc-Neu5Ac) binds specifically to the HT-29 cells and was mildly cytotoxic at a concentration of 402 µM. Cellular internalization of 99mTc-Neu5Ac was mainly in the cytosolic proteins and free membranes as compared to nuclear fraction and large organelles. In conclusion, Neu5Ac was successfully radiolabeled with 99mTc, and in-vitro binding studies confirmed that our developed radionuclide probe binds selectively to the cancer cells. Further, efficacy of our developed complex may be useful...
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Posted by admin on Feb 29, 2020 in |
To achieve initial conformation of the observed in-vivo antiepileptic activity by utilization of molecular target gamma-aminobutyric acid (GABA) with the help of software i.e., Molegro Virtual Docker ver. 6.0 molecular docking studies were performed. According to the docking studies it was found that the title compounds of series combine and bind precisely with 1OHY subunits of gamma-aminobutyric acid (GABA), which is accountable for antiepileptic activity. On the basis of the study, it was found that Compound C1, C3, C5, C11, C16, C17, C19, C23, and C24 showed good binding interaction. The results were produced on the basis of evaluation of three scoring functions i.e. mol dock score (-115.737, -102.781, -94.5148, -94.9588, -96.8756, -93.8359, -74.5031, -99.2451 and -89.0893), re-rank score (-72.9177, -81.2145, -59.4376, -81.2145, -59.1531, -80.1486, -63.2278, -61.2916 and -75.9803) and hydrogen bonding (-6.67928, -10.0939, -7.40405,-8.47986, -12.952, -8.39746, -5.77098, -13.9623 and -8.37248) which was very close to reference drug phenytoin which having Moldock score, re-rank score and hydrogen bonding score -76.1363, -60.0613 and -6.83431...
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Posted by admin on Feb 29, 2020 in |
A progression of fourteen narrative quinolonyl diketo acid analogs were planned, synthesized, identified by IR, NMR, CHN and MS supernatural analysis and evaluated as potential HIV-1 Integrase hinders. Compounds of Zinc database were surfed considering Elvitegravir as standard. Nearly 99 compounds were identified and docked in the active site of HIV-1 integrase. Molecular docking study of compounds 1, 4 and 7 showed docking score -10.38, -9.31 and -10.12 respectively as that of set drug Elvitegravir -4.93. The docking poses to open the interaction of the ligands with preferred amino acids. The standard drug Elvitegravir displayed connections with lys156, Asn155, Lys159 and Thr66. Raltegravir showed hydrogen bonding with Asp 116. A round fourteen target diketoquinolines were chosen for advance synthesis with the help of substituted oxoquinoline-3-carboxylate as starting material. In-vitro biological evaluation open that some of the upper-class compounds exhibited moderate to good inhibitory activity besides HIV1 Integrase compared to the reference drugs Raltegravir and Nevirapine. Compounds 1, 2, 3 and 4 weakly inhibited HIV-1 integrase at EC50 of 0.31,...
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Posted by admin on Feb 29, 2020 in |
Dairy and milk consumption are habitually included as important essentials in a healthy and balanced diet. It is the principal food for mammals and provides all the essential energy and nutrients to guarantee proper growth and development. Whey protein present in the milk is quickly digested and therefore amino acids are delivered quickly to muscles to help start the muscle-building process. The major components of milk whey of nutraceutical potential include beta-lactoglobulin, alpha-lactalbumin, bovine serum albumin (BSA), lactoferrin (Lf), immunoglobulin’s (Igs), lactoperoxidase (Lp) enzymes, glycomacropeptides (GMP), lactose and minerals. The main aim of this study is to determine the antimicrobial and antioxidant activity of whey protein concentration from cow’s milk. The result of the present study reveals the fact that the whey milk exhibited good antimicrobial activity. Whey protein α – lacto albumin and β – globulin were confirmed by two peaks with the retention time of 3.96 and 9.45. Thus, HPLC confirmed the presence of protein in the whey milk...
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Posted by admin on Feb 29, 2020 in |
In the present study novel matrix diffusion controlled transdermal patches of Hydralazine hydrochloride, a hypertensive drug to ensure satisfactory drug release were successfully prepared by solvent casting method with optimization of suitable polymeric blend of Eudragit L100 (EL-100), ethyl cellulose (EC), polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), carbopol, hydroxypropyl cellulose (HPC) to achieve sustained release pattern within the therapeutic range. N-dibutyl phthalate (n-DB) used as a plasticizer and oleic acid used as a permeation enhancer. Different batches of transdermal patches were prepared by varying different polymers with the difference in ratio. Prepared transdermal patches from each batch, gave release profile for over 12 h. Fourier Transform Infrared analysis shows no interaction between drugs and polymers. Cumulative amount of drug release in 12 h from all the prepared formulation were found to be in following order: F1> F2> F3> F4> F9> F8> F7> F10> F5.F6. Combination of Eudragit L100 and PVP (F1 and F2) and Ethylcellulose and PVP (F3 and F4) exhibited good characteristics for sustained release...
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