Rashtrasant Tukadoji Maharaj Nagpur University
Recent publications
Background Cancer is a complex disease in which some of the cells grow uncontrollably and spread to other parts of the body. Objective: The present study focuses on molecular docking and synthesis of novel flavone derivatives substituted with heterocyclic rings. Objective The present study focuses on molecular docking and synthesis of novel flavone derivatives substituted with heterocyclic rings. Methods The anticancer activity of novel flavones against human aromatase enzyme using human breast cancer cell line MCF-7 through MTT assay was demonstrated. The synthesized compounds for the determination of single or double-strand DNA damage through the single-cell electrophoresis/comet assay were evaluated. Results In this study, we found that the derivative 3M with Morpholine ring showed the highest anticancer potency against the MCF-7 cell line compared to that of other flavone derivatives. Compound 3T showed less cytotoxicity against the MCF-7 cell line. Conclusion Based on the findings, flavone scaffolds can be selected as a skeleton for the development of heterocyclic amine-containing flavones with the potential to develop as anticancer drugs.
Neuroadaptations in neurocircuitry of reward memories govern the persistent and compulsive behaviors. The study of the role of hippocampus in processing of reward memory and its retrieval is critical to our understanding of addiction and relapse. The aim of this study is to probe the epigenetic mechanisms underlying reward memory in the frame of dentate gyrus (DG). To that end, the rats conditioned to the food baited arm of a Y-maze and subjected to memory probe trial. The hippocampus of conditioned rats displayed higher mRNA levels of Ten-eleven translocase 1 (Tet1) and brain-derived neurotrophic factor (Bdnf) after memory probe trial. The DNA hydroxymethylation and TET1 occupancy at the Bdnf promoters showed concomitant increase. Stereotactic administration of Tet1 siRNA in the DG before and after conditioning inhibited reward memory formation and recall, respectively. Administration of Tet1 siRNA impaired the reward memory recall that was reinstated following administration of exogenous BDNF peptide or after wash-off period of 8 days. Infusion of a MEK/ERK inhibitor, U0126 in the DG inhibited reward memory retrieval. The TET1-induced DNA demethylation at the Bdnf promoters raised BDNF levels in the hippocampus, thereby setting the stage for reward memory retrieval. The study underscores the causative role of TET1 in the DG for reward memory formation and recall.
Zebrafish is a useful model for understanding human genetics and diseases and has evolved into a prominent scientific research model. The genetic structure of zebrafish is 70% identical to that of humans. Its small size, low cost, and transparent embryo make it a valuable tool in experimentation. Zebrafish and mammals possess the same molecular mechanism of thyroid organogenesis and development. Thus, thyroid hormone signaling, embryonic development, thyroid-related disorders, and novel genes involved in early thyroid development can all be studied using zebrafish as a model. Here in this review, we emphasize the evolving role of zebrafish as a possible tool for studying the thyroid gland in the context of physiology and pathology. The transcription factors nkx2.1a, pax2a, and hhex which contribute a pivotal role in the differentiation of thyroid primordium are discussed. Further, we have described the role of zebrafish as a model for thyroid cancer, evaluation of defects in thyroid hormone transport, thyroid hormone (TH) metabolism, and as a screening tool to study thyrotoxins. Hence, the present review highlights the role of zebrafish as a novel approach to understand thyroid development and organogenesis.
The plant Begonia roxburghii (Miq.) A.DC (Begoniaceae) is a shrub widely distributed in the Himalayan regions of North East India. In Meghalaya and Assam states of India, the plant is regularly used as vegetables and the roots of the plant are traditionally used in the treatment of diarrhoea, bronchitis, dysentery, candidiasis, colds, in digestive disorders and liver problems. The present investigation was undertaken for the first time to report the complete cytomorphological and quality control profile of the roots from the plant. The study included morphological, microscopical, physicochemical and nutritional analysis. Further, the root extract was also subjected to phytochemical screening and quantitative estimation of various identified phytoconstituents and HPTLC standardization. Morphologically, the roots appeared brown, bulb shaped and tapering towards base, while microscopical examination of the root showed the presence of cortical cells with brown content, cork cambium, lignified xylem fibers, simple or compound starch grains and clustered oxalate crystals. All the physicochemical parameters, heavy metals, microbial counts were found to be within the limits of WHO guidelines, while aflatoxins were absent and nutritional analysis showed the presence of essential elements viz. Ca, Cu, Fe, K, Mg and Zn. The phytochemical standardization revealed the roots extract to be highly rich in flavonoids and tannins, while rutin quantified using HPTLC was found to be 6.83% w/w. Thus, the quality control profile developed through this study could be used as referential source for further research and also to minimize adulteration.
Metal and metal oxide nanoparticles (NPs) have piqued the interest of material scientists in recent years due to their unique physicochemical properties which are dependent on their size, shape, and chemical surroundings. The sol gel combustion is one of the most straightforward and practical technique for getting tiny and similar size and shape of the powder out of all the current lead oxide nanoparticle synthesis techniques. In this study, PbO nanoparticles are prepared using the sol-gel method followed by an auto combustion process. This research is aimed at the particle size, shape, thermal analysis, and optical properties of nanostructured PbO. Several microscopic, spectroscopic, and thermogravimetric analysis are employed for the structural characterization of lead oxide nanoparticles. Tiny lead oxide particles with a diameter of 60 nanometres have been prepared. The prepares sample's optical band gap was discovered to be 2.44 electronvolt. Thermal investigations indicate the thermal behaviour and stability of synthesized lead oxide powder and are described in details.
Lentinan (LNT) a polysaccharide obtained from mushroom Lentinus edodes, possesses potent anticancer and antitumor activity. To improve the bioavailability, encapsulation of LNT in polymer -lipid hybrid nanostructures (PLHNs) is done and administration via nasal pathway will bypass hepatic first-pass metabolism, which possibly will give high prospect for treatment of brain tumors. The estimation of entrapped LNT within Hybrid Nanostructures is one of the important parameters for the characterization of nanoparticles. Therefore, an analytical method was developed and validated for estimating plain LNT and LNT-PLHNs in Nasal Simulated Fluid (NSF) by conjugating with Congo Red (CR) in dilute alkaline solutions by employing high-performance liquid chromatography (HPLC). The developed method was validated for selectivity, linearity, precision, accuracy, robustness. The linearity was checked over the concertation range of 2–10 μg/mL the and limit of detection (LOD) and limit of quantification (LOQ) were 38.02 ± 0.21 ng/mL and 86.71 ± 0.82 ng/mL respectively. The mean percent recovery of LNT was 99.18 %; relative standard deviation (RSD) of 0.386 % and intra- and interday coefficient of variation was <2 %. The developed HPLC method was found suitable for assessing percent entrapment efficiency (%EE), in-vitro drug release, intracellular uptake study and stability profile of LNT-PLHNs obtained by solvent injection technique.
In this study, an ultrasound-assisted spiral minireactor was used to synthesize Ag-doped Fe3O4 nanoparticles. When compared to the traditional (without ultrasonic) method of producing nanoparticles, the use of a minireactor with ultrasonication provides a more effective method of producing nanoparticles. Effect of various molar ratios of AgNO3:NaBH4 on the structure of synthesized Ag-doped Fe3O4 nanoparticles was investigated. Formation of the nanocomposite was examined by UV, FTIR, TEM, and XRD. For comparison purpose, Ag-doped Fe3O4 nanoparticles were also prepared using the same procedure and reaction conditions without the use of ultrasound. There is no study that provides the protocol to synthesize nanocomposite material continuously. Moreover, a fast synthesis method for production of Ag-doped Fe3O4 nanoparticles is not yet disclosed. It focuses on the optimization of AgNO3:NaBH4 ratio for achieving desired nanocomposite material. Assistance of ultrasound to the minireactor is an efficient method for nanoparticles production. This is due to the effective contact of reactants, exposure of Fe3O4 surface area, distribution of Ag nanoparticles over Fe3O4 surface, and particle size reduction. Thus, this method is proved to be eligible for scaling up for large-scale production of different types of nanoparticles.
Present work includes isolation of actinomycetes from marine, mangrove, and terrestrial environments followed by their screening for bioactivity. Study led to the isolation of 109 actinomycete isolates. Broth supernatants and ethyl acetate crude extracts were analyzed for bioactivity of which, 19 isolates showed a potent inhibition against E. coli , 17 isolates showed activity against S. aureus , 10 isolates exhibited activity against K. pneumoniae and B. subtilis each, and 9 isolates showed zone of inhibition against C . albicans . Potential actinomycetes were and identified by 16S rRNA gene analysis and their sequences were deposited in GenBank. Two isolates belonging to non- Streptomyces genera viz., Micromonospora and Nocardiopsis were obtained . The broad-spectrum antimicrobial activity against all the test organisms at very low concentration was shown by soil isolates D, D2, F30 (brown pigment), TS13 (Orange red), TS14 (green), TS4 (cherry red), and marine isolate M11 (yellow).
Efavirenz (EFV) with a booster dose of ritonavir (RTV) (EFV-RTV) inhibits the metabolism of EFV and improves its bioavailability. However, inadequate organ perfusion with surface permeability glycoprotein (P-gp) efflux sustains the viable HIV. Hence, the present investigations were aimed to evaluate the pharmacokinetics and tissue distribution efficiency of EFV by encapsulating it into PEGyalated PAMAM (polyamidoamine) G4 dendrimers with a booster dose of RTV (PPG4ER). The entrapment efficiency of PEGylated PAMAM G4 dendrimers was found to be 94% and 92.12% for EFV and RTV respectively with a zeta potential of 0.277 mV. The pharmacokinetics and tissue distribution behavior of EFV within PPG4ER was determined by developing and validating a simple, sensitive, and reliable bioanalytical method of RP-HPLC. The developed bioanalytical method was very sensitive with a quantification limit of 18.5 ng/ml and 139.2 ng/ml for EFV and RTV, respectively. The comparative noncompartmental pharmacokinetic parameters of EFV were determined by administrating a single intraperitoneal dose of EFV, EFV-RTV, and PPG4ER to Wistar rats. The PPG4ER produced prolonged release of EFV with a mean residential time (MRT) of 24 h with Cmax 7.68 µg/ml in plasma against EFV-RTV with MRT 11 h and Cmax 3.633 µg/ml. The PPG4ER was also detected in viral reservoir tissues (lymph node and spleen) for 3-4 days, whereas free EFV and EFV-RTV were cleared within 72 h. The pharmacokinetic data including Cmax, t1/2, AUCtot, and MRT were significantly improved in PPG4ER as compared with single EFV and EFV-RTV. This reveals that the PPG4ER has great potential to target the virus harbors tissues and improve bioavailability.
This study aimed to evaluate the 6D inter-fraction tumour localisation errors in 20 tongue and 20 prostate cancer patients treated with intensity-modulated radiation therapy and volumetric-modulated arc therapy. The patient tumour localisation errors in lateral, longitudinal and vertical translation axes and pitch, roll and yaw rotational axes were analysed by automatic image registration of daily pretreatment kilovoltage cone-beam computed tomography (kV-CBCT) with planning CT in 1000 fractions. The overall mean error (M), systematic error (Σ), random error (σ) and planning target volume (PTV) margins were evaluated. The frequency distributions of setup errors were normally distributed about the mean except for pitch in the tongue and prostate. The overall 3D vector length ≥ 5 mm was 14.2 and 49.8% in the ca-tongue and ca-prostate, respectively. The frequency of rotational errors ≥1 degree was a maximum of 37 and 59.5%, respectively, in ca-tongue and ca-prostate. The M, Σ and σ for all translational and rotational axes decreased with increasing frequency of verification correction in ca-tongue and ca-prostate patients. Similarly, the PTV margin was reduced with no correction to alternate day correction from a maximum of 4.7 to 2.5 mm in ca-tongue and from a maximum of 8.6 to 4.7 mm in ca-prostate. The results emphasised the vital role of the higher frequency of kV-CBCT based setup correction in reducing M, Σ, σ and PTV margins in ca-tongue and ca-prostate patients.
We study the contact process on layered networks in which each layer is unidirectionally coupled to the next layer. Each layer has elements sitting on (i) an Erdös-Réyni network, and (ii) a d-dimensional lattice. The top layer is not connected to any layer and undergoes an absorbing transition in the directed percolation class for the corresponding topology. The critical infection probability p_c for the transition is the same for all layers. For an Erdös-Réyni network the order parameter decays as t^{−δ_l} at p_c for the l'th layer with δ_l~ 2^{1−l}. This can be explained with a hierarchy of differential equations in the mean-field approximation. The dynamic exponent z=0.5 for all layers and ν_∥→2 for larger l. For a -dimensional lattice, we observe a stretched exponential decay of the order parameter for all but the top layer at p_c.
Decrease in life span of electronic devices and consumer’s urge to use advanced technology leads to obsolescence of such devices, resulting in electronic waste generation. The technology for e-waste components recycling has made great progress. However, due to growing environmental concern, there is a need to find alternatives for conventional e-waste recycling methods to achieve a safer environment. Rapid surge in e-waste generation is a matter of concern due to elevated levels of heavy metals and persistent organic pollutants (POPs) in air, soil and water caused by informal recycling practices. Moreover, recycling of printed circuit board (PCB), a major part of electronic waste, in order to recover metals, results in release of waste acid leach water, if untreated, which contain heavy metals like Pb, Cr, Ni, etc. This has given rise to the development of several remediation techniques for soil- and water-like phytoremediation, soil washing, bioremediation, and application of nanoparticles, which have been compared and reviewed in this paper along with their limitations for application at larger scale for real-contaminated soil. This review focuses on the existing remediation techniques and their limitations to decrease environmental hazards caused by the release of various pollutants through e-waste recycling. Graphic abstract
In this paper, two newly developed garnet phosphors, BaY2Al4GeO12:Ce³⁺ and SrY2Al4GeO12:Ce³⁺ are reported. The materials were prepared by simple, facile combustion synthesis. The emission for these phosphors is in yellow region when excited by blue light. Decay for BaY2Al4GeO12:Ce³⁺ is nearly exponential with average lifetime of 70 ns. In case of SrY2Al4GeO12:Ce³⁺, decay curve could be fitted to second order exponential with fast component τ1 = 24.5 ns and slow component τ2 = 57 ns. Capability of excitation by blue LED, yellow emission, simple preparation make these phosphors suitable for white LED lamp fabrication. These could be suitable replacements for YAG:Ce.
In recent times there is continuous increasing demand for highly sensitive sensorsSensor in various fields such as food quality inspection, medical treatment, environmental cleanliness, domestic purposes, etc. Overall to make our life safer and more effortless highly efficient sensorsSensor in terms of cost and time are needed. Therefore, it is necessary to develop a gas sensorSensor that can detect gas quickly in real-time. Electrospun nanofibersElectrospun Nanofibers are found to be potential candidates for nanosensors to improve the sensing phenomenon. The high surface area to volume ratio of electrospun nanofibersElectrospun Nanofibers leads to an increase in chances of interaction between analyte and sensorSensor. In this chapter, the application of electrospun nanofibersElectrospun Nanofibers comprising semiconductor metal oxides, conducting polymer (polyanilinePolyaniline, PANI), and their compositesComposites for the detection of various toxic and harmful gases will be described. Reliability of compositesComposites towards chemiresistive gas sensorsSensor using sensing parameters and their mechanism of sensing are also discussed.
The present research was aimed to develop a terbinafin hydrochloride (TH)-encapsulated solid lipid nanoparticles (SLNs) hydrogel for improved antifungal efficacy. TH-loaded SLNs were obtained from glyceryl monostearate (lipid) and Pluronic® F68 (surfactant) employing high-pressure homogenization. The ratio of drug with respect to lipid was optimized, considering factors such as desired particle size and highest percent encapsulation efficiency. Lyophilized SLNs were then incorporated in the hydrogel prepared from 0.2–1.0% w/v carbopol 934P and further evaluated for rheological parameters. The z-average, zeta potential and polydispersity index were found to be 241.3 nm, −15.2 mV and 0.415, respectively. The SLNs show a higher entrapment efficiency of about 98.36%, with 2.12 to 6.3602% drug loading. SEM images, XRD and the results of the DSC, FTIR show successful preparation of SLNs after freeze drying. The TH-loaded SLNs hydrogel showed sustained drug release (95.47 ± 1.45%) over a period of 24 h. The results reported in this study show a significant effect on the zone of inhibition than the marketed formulation and pure drug in Candida albicans cultures, with better physical stability at cooler temperatures. It helped to enhance skin deposition inthe ex vivostudy and improved, in vitro and in vivo, the antifungal activity.
Strategies drawn at understanding the functional attributes of specific neural circuits often necessitate electrical stimulation and pharmacological manipulation at the same anatomical site. We describe a simple, inexpensive and reliable method to fabricate a bipolar electrode-cannula assembly for delivery of electric pulses and administration of neuroactive agents at the same site in the rat brain. The assembly consisting of a guide cannula, dummy cannula, internal cannula and bipolar electrode was fabricated using syringe needles, wires and simple electronic components. To test the usefulness of the device, it was implanted on the skull of a rat specifically targeting the posterior ventral tegmental area (pVTA). The rat was conditioned to press the lever in intracranial self-stimulation (ICSS) protocol in an operant chamber. The number of lever presses in a 30 min task was monitored. Intra-pVTA administration with bicuculline (GABAA receptor antagonist) increased the lever press activity, while muscimol (GABAA receptor agonist) had opposite effect. The results confirm that the group of neurons responding to the electrical stimulation probably receive GABAergic inputs. The device is light in weight, costs less than a dollar and can be fabricated from readily available components. It can serve a useful purpose in electrically stimulating any given target in the brain - before, during or after pharmacological manipulation at the same locus and may find application in neuropharmacological and neurobehavioral studies.
A series of 24 condensed pyrimidine derivatives was synthesized via multistep reactions using microwave radiation and have opted to explore the possible inhibition mechanism via virtual analysis by using V life MDS. The synthesized compounds were characterized by spectroscopic analysis. All the synthesized compounds were found to show good in-silico binding analysis which indicated their potential to explore as good antimicrobial agents. All the synthesized derivatives were screened in-vitro for their antibacterial activity against two gram positive and gram negative bacteria. Among the compounds tested, SAKB2, SAKB7, SAKB8, SAKB9 SAKB10, SAKB11, SAKB12 and SAKB13derivatives exhibited potent antimicrobial activity.
Nanofluid preparation is a crucial step in view of their thermophysical properties as well as the intended application. This work investigates the influence of ultrasonication duration on the thermal conductivity of Fe3O4 nanofluid. In this work, water-based Fe3O4 nanofluids of various volume concentrations (0.01 and 0.025 vol.%) were prepared and the effect of ultrasonication time (10 to 55 min) on their thermal conductivity was investigated. Ultrasonication, up to a time duration of 40 min, was found to raise the thermal conductivity of Fe3O4 nanofluids, after which it starts to deteriorate. For a nanofluid with a concentration of 0.025 vol.%, the thermal conductivity increased to 0.782 W m−1K−1 from 0.717 W m−1K−1 as the ultrasonication time increased from 10 min to 40 min; however, it further deteriorated to 0.745 W m−1K−1 after a further 15 min increase (up to a total of 55 min) in ultrasonication duration. Thermal conductivity is a strong function of concentration of the nanofluid; however, the optimum ultrasonication time is the same for different nanofluid concentrations.
Lentinan, a therapeutic bioactive molecule obtained from Lentinus edodes (Shitake mushrooms), possesses various pharmacological activities. A literature survey reveals that no simple UV-visible technique for the estimation of lentinan has yet been established; hence, there is a pressing need for a simple, yet precise and robust analytical method. We have developed a UV-visible spectrophotometric method for the estimation of lentinan in complex with Congo red azo dye in different concentrations of alkaline solutions. Lentinan was found to be freely soluble in deionized water, and the absorption maximum (λmax) was found to be 486 nm. The validation of the developed method gave satisfactory results, the lentinan–Congo red solution complex gave acceptable linearity within the concentration range 2–10 μg/mL and the correlation coefficient (r2) was found to be >0.99. The developed method was found to be accurate because the mean recovery value at various concentrations gave higher results than 90%. LOD and LOQ for lentinan were reported and found to be 0.014 and 0.0431 μg/mL, respectively. The developed method was found to be simple, specific, economic, reliable, accurate, precise, reproducible, and it could be used as a quality control tool for the analysis of pure lentinan and lentinan in formulations.
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667 members
Prafulla Sabale
  • Department of Pharmaceutical Science
Rupesh S. Badere
  • Department of Botany
Prashant Puranik
  • Department of Pharmaceutical Science
Sumedh K. Humane
  • Department of Geology
Nagpur, India