Sumbul Rehman

Potent acetylcholinesterase inhibitors: Synthesis, biological assay and docking study of nitro acridone derivatives.

The reaction of o-halobenzoic acid with aniline derivatives and their subsequent cyclization reaction yielded the acridone derivatives. The series of nitro acridone derivatives were prepared by Ullmann condensation in presence of copper as catalyst and were characterized by FTIR, (1)H, (13)C NMR and mass spectra. The structure of 5-nitro-(2-phenyl amino) benzoic acid (4) was confirmed by X-ray crystallography and was found to crystallize in P21/c space group. The in vitro efficacy of the compounds for their acetylcholinesterase (AChE) and antimicrobial inhibitory activities have been evaluated against the standard drugs Ampicillin and Gentamicin against Gram positive and Gram negative bacteria. 1,7-Dinitroacridone was found to be the most potent AChE inhibitor (IC50=0.22μM). Moreover, the compounds have been screened for their antioxidant activity using the DPPH assay. Also, docking study results were found to be in good agreement with the results obtained through in vitro experiments. The docking study further predicted possible binding conformation.

Synthesis, characterization, and cytotoxicity of N-2′-hydroxyethyl-substituted azastigmastanes

Abstract The in vitro cytotoxicity of N-2′-hydroxyethyl-substituted azastigmastanes and its precursor steroidal ketones against cancer cell lines: MCF-7, HepG2, and HCT 116; has been carried out using MTT assay. The N-2′-hydroxyethyl-substituted azastigmastanes were synthesized by bespoke version of Schmidt reaction using common Lewis acids like BF3–OEt2, SnCl4 and H2SO4 as catalysts in substantial yields. Sulphuric acid was found to be the most suitable catalyst in terms of reaction yield and time, while SnCl4 was found to be the weakest in case of 3β-acetoxy-N-2′-hydroxyethyl-6-aza-B-homo-5α-stigmastan-7-one and 3β-chloro-N-2′-hydroxyethyl-6-aza-B-homo-5α-stigmastan-7-one and almost inactive in case of N-2′-hydroxyethyl-6-aza-B-homo-5α-stigmastan-7-one. The products were obtained in semi-solid state and characterized by spectroscopic techniques and microanalytical data. Moreover, on the basis of IC50, compound 5 was found to inhibit the cancer cells most effectively in conformity with our previous findings.

Biogenic synthesis of iron oxide nanoparticles using Agrewia optiva and Prunus persica phyto species: Characterization, antibacterial and antioxidant activity

A phytoextract mediated synthesis of iron oxide nanoparticles using Agrewia optiva (Dhaman or Biul) and Prunus persica (Peach) leaf extract as capping and stabilizing agent without using hazardous toxic chemicals via biogenic route has been studied. The biogenic method of synthesis is convenient, rapid, cost effective and ecofriendly. The green synthesized nanoparticles were characterized by Ultraviolet-visible spectroscopy, Fourier transform infrared spectroscopy, Attenuated total reflectance spectroscopy, X-ray diffraction analysis, scanning electron microscopy, energy dispersive X-ray spectroscopy, transmission electron microscopy and dynamic light scattering measurements. The antibacterial study was determined by agar well diffusion method to measure the efficiency of both phyto species extract and its mediated iron oxide nanoparticles against five gram positive bacterial stains such as Staphylococcus aureus (S. aureus), Streptococcus mutans (S. mutans), Streptococcus pyrogenes (S. pyrogenes), Corynebacterium diphtheriae (C. diphtheriae) and Corynebacterium xerosis (C. xerosis) and three gram negative bacterial stains such as Escherichia coli (E. coli), Klebsiella pneuomoniae (K. pneuomoniae) and Pseudomonas aeruginosa (P. aeruginosa). The antibiotic Ciprofloxacin and Gentamicin have been used as reference standard drugs for gram positive and gram negative bacterial stains, respectively. The antioxidant activity of the phyto extracts and prepared nanoparticles have been performed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical assay employing l-ascorbic acid as a standard.

Nanotization, Characterization and In-Vitro Activity of Kushta-E-Qalai (Tin Calx): A Traditional Unani Medicine of India

The present study reports a novel method of preparation of kushta-e-qalai, a well-known Indian traditional drug of Unani system of medicine prepared from stannum. In this work the Tin calx (kushta-e-qalai) was prepared by laboratory method in order to develop a standard protocol both in terms of synthesis and its subsequent conversion to nanoscale termed as nanotization. The finished kushta-e-qalai was characterized using standard analytical techniques like Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM) and X-Ray Diffraction (XRD). It was inferred that the kushta-e-qalai contains nano-particles of tin-oxide in the range of 20 to 40 nm. During the TLC examination of kushta-e-qalai a single spot was observed in a variety of solvents implying the complete conversion of stannum into its calx. The kushta-e-qalai was screened for its possible biological activity. The results obtained are indicative that the kushta-e-qalai possesses significant anti-bacterial activity against Streptococcus mutans and Corynebacterium xerosis. The LD50 of kushta-e-qalai was also analyzed by the graphical method of Miller and Tainter and was found to be 1250 mg/kg b.w.