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A molecular imprinted polymer was fabricated for determination of aminoglycoside drug. It is based on creation of cavities suitable for Cu (II)-kanamycin where Cu(II) acts as signal tracer and amplifier.

The current study proposed the in vivo antidepressant and anxiolytic activities of the aqueous extract from Solanum melongena fruits (AESM) in mice. The mice were administered with AESM 100 and 200 mg/kg, p.o. for anxiolytic (elevated plus maze test (EPMT) and locomotor action), and antidepressant (forced swimming test (FST) and tail suspension test (TST) activities. The possible mechanism of action of Solanum melongena fruits was also analyzed by measuring the level of serotonin (5HT), monoamine oxidase enzyme (MAO-A) and GABA activity in the blood of experimental animals. When mice were treated for seven days with 100 (*** P < 0.01) and 200 mg / kg, AESM p.o. and 2 mg / kg, diazepam p.o. (*** P < 0.001) showed significant increases in the average time expended and the number of entries into the open arms of the EPMT, as compared to control group in dose dependent fashion. However, when mice were treated with standard Imipramine (10 mg/kg) (***P < 0.001), AESM 100 mg/kg (**P < 0.01) and 200 mg/kg (*P < 0.05) after day 7, there was significant reduction in locomotor activity in both TST and FST in dose dependent fashion. Monoamine oxidase - A level in the entire brain of mice were significantly reduced when pretreated with AESM 100 and 200 mg/kg, p.o. for 7 days as compared to control group in dose dependent fashion. The mechanisms of action of antidepressant effect of Solanum melongena fruits extract act by increasing serotonin and also GABA. Moreover, the extract also decreased the MAO-A enzyme in the experimental animals. These results demonstrated that both of these doses. Of aqueous extract from Solanum melongena fruits possess potential antidepressant activities in dose dependent fashion.

Herein, yellow emissive nitrogen doped graphene quantum dots (N@GQDs) were prepared by a novel advanced thermal driven oxidation. The N@GQDs was functionalized with β-cyclodextrin (β-CD) to improve its catalytic performance towards dopamine (DA) detection. The β-CD/N@GQDs exhibited strong fluorescence at λem. = 550 nm after excitation at 460 nm with a quantum yield of 38.6%. The β-CD/N@GQDs showed good peroxidase like activity via catalyzing the oxidation of tetramethylbenzidine (TMB) in presence of H2O2 to form blue colored product at λmax = 652 nm. In the colorimetric assay of DA, the detection based on the oxidation of TMB by H2O2 in presence of β-CD/N@GQDs as a catalyst. Then, the color of the blue oxidized TMB (oxTMB) product was reduced by addition of DA. While the fluorometric detection of DA based on the “inner filter effect” of the overlapped emission spectrum of β-CD/N@GQDs with the absorption spectrum of oxTMB, where, addition of DA reduces oxTMB to TMB and restores the fluorescence intensity of β-CD/N@GQDs. Under the optimized conditions, the colorimetric method achieved linearity range of 0.12–7.5 µM and LOD (S/N = 3) of 0.04 µM, while the fluorometric method achieved linearity range of 0.028–1.5 µM and LOD (S/N = 3) of 0.009 µM. The peroxidase like activity of β-CD/N@GQDs was used to detect DA in human plasma and serum samples with good % recoveries. The colorimetric and fluorometric methods exhibited good sensitivity and selectivity toward DA detection.

Ultrasound-assisted extraction (UAE) or ultrasonic extraction technology has been used for the isolation of bioactive compounds from Argyreia speciosa (Linn. f.) Sweet plant (family: Convolvulaceae). Argyreia speciosa is an Indian traditional medicinal plant having strong evidence of various properties widely used in Ayurveda. Dried flowers were used for extraction and the response surface methodology (RSM) was used to optimize the conditions of extraction for the yield of total phenolics and antioxidants from A. speciosa flowers (ASF) in respect of three variables: temperature, power, and time. Damage and structural changes of the bioactive compounds were studied by scanning electron microscopy (SEM) and Fourier-transform infrared (FTIR) spectroscopy techniques. The optimum UAE conditions obtained by RSM for the yield of total phenolic content from ASF were 42.41°C temperature, 43.62 % power, and 26.51 min process time and conditions for the maximum antioxidant activity by DPPH radical scavenging were 41.36°C temperature, 57.02 % power, and 26.63 min. These findings showed that the UAE under optimum conditions increased the percentage yield of bioactive compounds. SEM results showed that there was no relevant damage to the cells, and FTIR spectroscopy verified that there were no changes in chemical structure. It has been concluded that UAE method is an effective technique for enhancing the yields of major phenolic compounds from A. speciosa flowers.

In this research paper, a highly sensitive and selective molecular imprinted polymeric network (MIP) based electrochemical sensor was developed for the determination of histamine (HIS). The functional monomer (pyrrole) was electro-polymerized over the surface of AuNPs functionalized Fe-metal organic framework (Fe-BDC) and nitrogen-sulfur co-doped graphene quantum dots (N, S-GQDs). The MIP-Au@Fe-BDC/ N, S-GQDs /GCE exhibited an observable peak at −0.12 V, which corresponds to the anodic peak of Fe-BDC. This peak was increased and decreased by eluting and rebinding of HIS, respectively. This might be due to the binding constant between Fe-BDC and HIS is 3.5 × 106 mol−1 L. The electrochemical signal (Δi) was increased with the increase of HIS concentration in the range of 0.078–250 nM with a limit of detection (LOD, S/N = 3) of 0.026 nM. The combination of N, S-GQDs and Au@Fe-BDC improves the conductivity and the anchoring sites for binding the polymer film on the surface of the modified electrode. Factors affecting fabrication of MIP and HIS determination were optimized using standard orthogonal design using L25 (56) matrix. The MIP-based electrochemical sensor offered outstanding sensitivity, selectivity, reproducibility, and stability. The proposed electrode was used to quantify HIS in human serum and canned tuna fish samples with recoveries % and relative standard of deviations % (RSDs %) in the range of 97.2–103 % and 1.8–3.8%, respectively. The as-synthesized MIP-based electrochemical sensor opens a new venue for the fabrication of MIP-based sensors and biosensors.

Glioblastoma multiforme (GBM) is one of the most aggressive and lethal types of brain cancers with low 5-year survival rate. Therefore, search for better drugs and effective treatment strategies for GBM to improve patient outcomes is continuing. Since GBM is one of the most highly vascularized solid tumors and its growth is angiogenesis-dependent, antagonizing tumor angiogenesis by using angiogenesis inhibitors seems to be one of the promising approaches. In this context, intensive pre-clinical evaluation of our patented anti-angiogenic compound, code-named F16, has exhibited potent anti-angiogenic and anti-tumor activities via selectively antagonizing VEGFR-2 in both in vitro and in vivo models. More importantly, assessment of biochemical parameters that are reflecting the safety of F16 in the in vivo system showed no alterations in the toxicological parameters of heart, liver, kidney, and pancreas, after 30 days of treatment, at the dose of 100 mg/kg body weight. Hence, we tested the direct effects of F16 for inhibiting the growth, angiogenesis and the migratory abilities of the U87MG glioblastoma cells, which are known to express high levels of VEGFR. Our in vitro studies have confirmed potent inhibitory effects of F16 towards the migration and invasion of U87MG cells, and also revealed potent cytotoxic effects (IC50 26 µM) against U87MG cells in comparison to Temozolomide (IC50 430 µM) treatment. In addition, F16 inhibited the phosphorylation of VEGFR-2 through competitive binding and also induced cell cycle arrest and apoptosis by activating p53 pathway in U87MG cells. Furthermore, our in vivo results with ectopically implanted xenograft model confirm the fact that F16 can significantly inhibit tumor growth in the mice implanted with U87MG glioblastoma cell line. Based on our preliminary results, we are proposing that F16 could be a potential candidate for treating GBM, either in monotherapy or in combination with a cytoreductive drug. (This research was supported by the generous funds provided by the Community Foundation of Broward, Florida and also by the Royal Dames of Cancer Research Inc., Ft. Lauderdale, Florida) Citation Format: Mohammad Algahtani, Khalid Alhazzani, Thiagarajan Venkatesan, Ali Alaseem, Sivanesan Dhandayuthapani, Appu Rathinavelu. Direct cytotoxic effect of a novel anti-angiogenic drug F16 towards U87MG glioblastoma cell line [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2019; 2019 Mar 29-Apr 3; Atlanta, GA. Philadelphia (PA): AACR; Cancer Res 2019;79(13 Suppl):Abstract nr 185.