ANTICHOLINESTERASE ACTIVITY OF OCTA PEPTIDES RELATED TO HUMAN HISTATIN 8: IN-SILICO DRUG DESIGN AND IN-VITRO

Objective: To evaluate the octapeptides related to human histatin 8 by in-silico and in-vitro studies.Method: Schrodinger, LLC and Ellman's method.Results: The compound HH1 and HH2 was found to be potent docking score of −9.494 and −7.401 against acetylcholinesterase (AChE) enzyme. The IC50 value of HH1 and HH2 was found to be 0.39±0.28 and 0.78±0.15 μg/mL. However, these compounds are shown to be highly effective as compared with the control AChE inhibitor donepezil (0.065±0.0050 μg/mL).Conclusion: In-silico docking study was conducted for the designed octapeptides related to human histatin 8 against AChE enzyme shows significance binding affinity toward HH1 and HH2 peptides and the AChE inhibitory activity of octapeptides shown to be a highly potent inhibitor as compared with control donepezil

ANALYSIS OF COMPLEX CHROMOSOMAL ABNORMALITIES IN A CASE OF MULTIPLE MYELOMA USING SPECTRAL KARYOTYPING

Objective: It was proposed to determine the chromosomal abnormalities in a 49-year-old male patient with multiple myeloma (MM) employing both conventional and advanced molecular cytogenetic techniques.Methods: GTG-banding and spectral karyotyping (SKY) on fixed metaphases obtained from LPS-stimulated bone marrow cells and interphase fluorescence in situ hybridization (iFISH) on unsorted marrow cells were carried out to identify genetic markers of prognostic significance.Results: The abnormal chromosomes observed through conventional cytogenetics could be resolved with SKY technique. The translocation t(4;14) (p16;q32) indicating FGFR3/IGH fusion and deletion of 13q14.3 was noticed using iFISH. The genetic abnormalities confirmed a poor prognostic outcome in the patient who died within 6 months of diagnosis.Conclusion: This report emphasizes the need for multicolor FISH techniques besides iFISH to resolve complex abnormalities and to identify cryptic aberrations of importance in risk stratification of MM patients

Recent Progression and Opportunities of Polysaccharide Assisted Bio-Electrolyte Membranes for Rechargeable Charge Storage and Conversion Devices

Polysaccharide-based natural polymer electrolyte membranes have had tremendous consideration for the various energy storage operations including wearable electronic and hybrid vehicle industries, due to their unique and predominant qualities. Furthermore, they have fascinating oxygen functionality results of a higher flexible nature and help to form easier coordination of metal ions thus improving the conducting profiles of polymer electrolytes. Mixed operations of the various alkali and alkaline metal–salt-incorporated biopolymer electrolytes based on different polysaccharide materials and their charge transportation mechanisms are detailly explained in the review. Furthermore, recent developments in polysaccharide electrolyte separators and their important electrochemical findings are discussed and highlighted. Notably, the characteristics and ion-conducting mechanisms of different biopolymer electrolytes are reviewed in depth here. Finally, the overall conclusion and mandatory conditions that are required to implement biopolymer electrolytes as a potential candidate for the next generation of clean/green flexible bio-energy devices with enhanced safety; several future perspectives are also discussed and suggested

Hantzsch synthesis of polyhydroquinolines - A simple, efficient and neat protocol

1084-1090A variety of polyhydroquinolines have been synthesized under eco-benign conditions. The reaction proceeds smoothly without any catalyst at room temperature in short reaction time. The yields and purity are excellent

Antimicrobial peptides: the role of hydrophobicity in the alpha helical structure

The antimicrobial peptides (AMPs) are a class of molecule obtained from plants, insects, animals, and humans. These peptides have been classified into five categories: 1. Anionic peptide, 2. Linear alpha helical cationic peptide, 3. Cationic peptide, 4. Anionic and cationic peptides with disulphide bonds, and 5. Anionic and cationic peptide fragments of larger proteins. Factors affecting AMPs are sequence, size, charge, hydrophobicity, amphipathicity, structure and conformation. Synthesis of these peptides is convenient by using solid phase peptide synthesis by using FMOC chemistry protocol. The secondary structures of three synthetic peptides were determined by circular dichroism. Also, it was compared the stability of the α-helical structure and confirmed the percentage of helix of these peptides by using circular dichroism. Some of these AMPs show therapeutic properties like antimicrobial, antiviral, contraceptive, and anticancer. The formulations of some peptides have been entered into the phase I, II, or III of clinical trials. This article to review briefly the sources, classification, factors affecting AMPs activity, synthesis, characterization, mechanism of action and therapeutic concern of AMPs and mainly focussed on percentage of α-helical structure in various medium

DOCKING STUDIES ON ANTIMICROBIAL PEPTIDES RELATED TO APIDAECIN- IA AND HUMAN HISTATIN AGAINST GLUTAMINE SYNTHETASE AND RNA POLYMERASE IN MYCOBACTERIUM TUBERCULOSIS

Currently need of novel molecules can be used to treat the tuberculosis including resistance multiple drug regimen (MDR) tuberculosis. Glutamine synthetase is an essential enzyme that produced the condensation reaction along with glutamate. It catalyses the glutamate react with ammonia, leads to the formation of glutamine and hydrolysis of ATP. In the brain it interact with glutamate regulation leads to detoxification of  ammonia in the brain leads to termination of neurotransmitter signals. RNA polymerase catalyses the synthesis from a DNA template. It is a crucial enzyme for growth and survival of the mycobacteria. The compounds AIA-II, AIA-I were showed more potent against the Glutamine synthetase with glide score -8.79 and -7.97 as compared with standard Amikacin and Ciprofloxacin with glide score -7.71 and -3.45. The compounds AIA-I, AIA-II and HH-I were showed more potent against the RNA polymerase with glide score -10.12, -9.47 and -8.74 as compared with standard rifampicin and isoniazid with glide score -6.57 and -3.34.   Â

In-silico and in-vitro toxicological evaluation of Tiktakam kashayam

“TIKTAKAM KASHAYAM” is evaluated by in-silico study using PASS online software. Its having anti-inflammatory activity and also having anti-neoplastic activity especially colon cancer. In-vitro heavy metal analysis shows lead and mercury below the detection limit, cadmium not detected and arsenic is present below the approved range. Some important toxicities like hepatotoxicity shown by the compound azadirachtin present in Azadiracta indica, neurotoxic shown by the compound biflorne present Inoldenlandia corymbosa, Ototoxicity shown by the compound sweroside, reproductive dysfunction produced by the compound luteolin present in Gentiana kuro. Neurotoxic by kobusone, respiratory failure by swertiamarin, ototoxicity by sweroside present in the plant swertia chirayata. Parkinsonism like effect produced by the compound piperine and   pipperitin by Piper longum. The ayurvedic formulation “TIKTAKAM KASHAYAM” possess anti-inflammatory activity and will be beneficial for the treatment of inflammatory bowel disease