Announcement from Editorial office:
We are currently accepting Commentaries, Letters, Regular Research and Review manuscripts submission for volume 4,
scheduled to be published in Fall, 2018. Please
email us your cover letter and manuscript to firstname.lastname@example.org (prepared following guidelines).
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Drug discovery and Clinical Treatments
In molecular perspective, diseases are considered to be associated with functions of specific target proteins in the body being
altered to abnormal states through various mechanisms including either genetic mutations or pathogens influences. Following this concept,
the goal of drug discovery is to either design or “discover” drugs that could be either small molecules, antibodies, peptides or short
nucleotides to interact with target proteins to modulate their abnormal functions to treat diseases. Unfortunately, effects and efficacy
of drugs can’t still be entirely predicted when patients are treated with them because complexity in proteins regulations in molecular
level, pharmacokinetics and pharmacodynamics in systems level has hampered the development of optimal treatments. To accomplish the
goal, one has to take all of these information into account to design appropriate drugs that can specifically interact with targets and
have desire pharmacokinetic and pharmacodynamic properties, develop optimal formulations and best treatment plans. ...
Oral Anti-Platelet Therapy for Acute Coronary Syndrome
Subhi J. Al’Aref, Robert M. Minutello
In recent days, medical treatment of coronary artery disease, and more specifically acute coronary syndrome with and without
revascularization, has seen significant improvement in outcomes driven by the discovery of newer P2Y12 receptor antagnosists
leading to more consistent inhibition of platelet function and fewer ischemic and/or thrombotic events. This review will
address a thorough analysis of this medical breakthrough.
Molecular dynamics and related computational methods with applications to drug discovery
Jack A. Tuszynski, T. Luchko, Philip Winter, Cassandra Churchill, Kamlesh Sahu, Francesco Gentile, Sara Ibrahim Omar, N. Nayebi, G. Hu, K. Wang and J. Ruan
The computational technique of molecular dynamics is discussed, with special attention to force fields for protein
simulations and to methods for the calculation of solvation free energies. Additionally, computational methods aimed
at characterizing and identifying ligand binding pockets on protein surfaces are discussed. Practical information about
databases and publicly-available software of use in drug design and discovery is provided. The main objective of this
paper is to give the reader a practical toolbox for applications in quantitative biology and computational drug discovery.
Sensitivity testing, yield and stability of antimicrobial metabolites obtained from soils of Menengai crater in Kenya
Waithaka N. Paul, Mwaura B. Francis, Wagacha M. John, Gathuru M. Eliud and Githaiga M. Benson
This study sought to determine the effectiveness of antimicrobial metabolites extracted using ethyl acetate.
The antimicrobial metabolites were obtained from previously isolated actinomycetes coded as PAN 30, PAN 37,
PAN 41 and PAN 154. The study also determined the yield of the extracts from the actinomycetes in addition to
testing the stability of the antimicrobial metabolites to degradation by enzymes, temperature and pH. To obtain
the antimicrobial metabolites from the actinomycetes, fermentation was carried out for a month using an orbital
shaker. Extraction of the metabolites was carried out using ethyl acetate. The metabolites were concentrated using
a vacuum evaporator. The metabolites were separately dried in pre-weighed containers using a hot air oven. To determine
the weight of the antimicrobial metabolites, the concentrated antimicrobials were placed in pre-weighed containers
followed by evaporation of the solvent to dryness in a hot air oven. The containers having the antimicrobial
metabolites were reweighed and the weight of the antimicrobials determined by subtracting the weight of the empty
container from that of the container plus the metabolites. The stability of the antimicrobial metabolites was determined
by exposing the metabolites to enzymes, varying levels of temperatures and pH. The antimicrobial metabolites yield of
PAN 30 was 253.6mg, PAN 37 (231.4mg), PAN 41 (258.0mg) and PAN 154 (259.0mg). There was no significant difference in the
weights of the antimicrobial metabolites among the four actinomycetes. The zones of inhibition presented by Staphylococcus
aureus, Bacillus subtilis, Escherichia faecalis, Escherichia coli, Klebsiella pneumoniae, Salmonella typhi, Xanthomonas
campestris, Erwinia carotovora, Candida albicans, Aspergillus niger, Fusarium oxysporum and Ustilago maydis were significantly
different (F=6.6046 P=0.001338). The zones of inhibition produced by the pathogens after incubating the antimicrobial
metabolites to enzymes trypsin, lysozyme, pepsin and lipase in addition to temperatures of 60oC, 70oC and 80oC were
not statistically different. However, there were significant differences when the antimicrobial metabolites were tested
for stability against pH in bacterial (F = 319.0101 P=<0.05) and fungal (F=55.58353, P<0.05) pathogens. The antimicrobial
metabolites obtained from PAN 41 and PAN 154 were not stable in trypsin, lysozyme, pepsin and lipase. All the antimicrobial
metabolites remained stable at 60oC, 70oC and 80oC. In addition, the antimicrobial metabolites remained effective in
pH 2, 4, 5 and 7 but were not effective in pH of 9 and 11. There is need to further purify the metabolites and determine their structure.
Cyclobenzaprine drug assay and Cyclobenzaprine-excipient interaction study by chromatography, thermal and spectral analysis
Rajasekhar Tulasi Baru, Prasanth Bitla
The present study was carried out to investigate the compatibility of Cyclobenzaprine hydrochloride, a muscle relaxant and
antidepressant with different pharmaceutical excipients. The study involved storing drug-excipient blends (200 mg) with 20%
added moisture in closed glass vials at 100°c for 24 hours. A LC method was developed and validated for determination of
cyclobenzaprine. The mobile phase consists of potassium dihydrogen phosphate buffer (20 mM, pH 3.0): methanol with flow rate 1.2 mL/min
and UV detection at 280 nm. A good linearity was obtained with concentration ranging from 5-50 µg/mL. The HPLC study showed, drug interacts
with some commonly used pharmaceutical excipients. The results were fairly good in agreement with the cyclobenzaprine hydrochloride-excipient
interaction analysis, obtained from DSC, FT-IR, UV-DRS. The HPLC method was validated as per ICH guidelines and applied for quality control
of bulk and formulation of cyclobenzaprine hydrochloride.