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Design and In-Silico Molecular Docking Analysis of
Some Novel Benzimidazoles
Chhajed SANTOSH S., Upasani CHANDRASHEKAR D.
[Abstract] [FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00013]
Inflammation and Pancreatic Cancer: Recent Development
with Focusing on Potential New Drug Targets
Generoso UOMO
[Abstract] [FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00014]
TAKAYASU´S ARTERITIS AND PARAOXONASE IN A MEXICAN
POPULATION
Ma. Elena Soto Claudia Huesca-Gomez Vicente Castrejon-Tellez
[Abstract] [FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00015]
Naproxen: An Update On Physicochemical, Analytical
And Pharmacological
Prabodh Chander Sharma
[Abstract] [FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00016]
An overview of the actions of capsaicin and its receptor,
TRPV1, and small primary sensory neurons
Akio Hiura Hiroshi Nakagawa
[Abstract] [FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00018]
Sensory Nerves and Mast cells
Fatma Tore Nese Tuncel
[Abstract] [FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00019]
Abstracts

Design and In-Silico Molecular Docking Analysis of
Some Novel Benzimidazoles
Chhajed SANTOSH S., Upasani CHANDRASHEKAR D.
[FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00013]
Present investigation describes structure based design of
some novel selective COX-II inhibitors. Designed benzimidazoles
are docked in to active site of Cyclooxygenase II. Ligands
are designed based on the structure of receptor, COX-II and
known NSAID Celecoxib. In- Silico docking analysis of designed
ligands are performed to predict binding modes, orientations
and affinity of ligands for enzyme COX-II. Ligands number
38, 39, 40, 41, 42, 43 and 44 are having less binding energy
in kj/mole and said to possess more affinity for receptor
than other molecules and celecoxib.
[Back to top]
Inflammation and Pancreatic Cancer: Recent Development
with Focusing on Potential New Drug Targets
Generoso UOMO
[FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00014]
Chronic inflammation has been identified as a significant
factor in the carcinogenesis of various tumors, including
pancreatic cancer. Both hereditary and classical forms of
chronic pancreatitis are associated with an increased risk
of developing pancreatic cancer. Cytokines and other mediators
of the inflammatory process together with an up-regulation
of pro-inflammatory pathways play a pivotal role into the
stimulation of oncogenesis, tumor growth and metastasis. The
presence of a strong desmoplastic reaction within and around
pancreatic cancer cells renders the proteolytic degradation
of extracellular matrix components an essential process for
tumor invasion and metastasis. Various classes of proteases
produced by the pancreatic acinar cells are involved in these
proteolytic events. The multiple link between inflammation
and pancreatic cancer may represent the basis for a novel
antineoplastic strategy. Cytokines, proteases, reactive-oxygen-species,
cyclo-oxygenase-2, nuclear-factor-kB and perixosome proliferator-activated
receptor-γ may be a new molecular targets useful
for therapeutic purpose.
[Back to top]
TAKAYASU´S ARTERITIS AND PARAOXONASE IN A MEXICAN
POPULATION
Ma. Elena Soto Claudia Huesca-Gomez Vicente Castrejon-Tellez
[FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00015]
Background. Takayasu’s arteritis (TA), also known as
pulseless disease, is a chronic inflammation that affects
the large vessels, many factors have been associated to it;
however, its etiology is still unknown. Human serum paraoxonase
hydrolyzes oxidized lipids into low density lipoproteins and
could therefore be associated with the prevalence of inflammation
processes.
Methods. In the present study, 58 patients with TA and 173
clinically healthy unrelated Mexican individuals were studied.
No differences existed in the clinical parameters between
both groups. The PON1 polymorphism was determined by the TaqMan
real time polymerase chain reaction method. PON1 activity
was assessed spectrophotometrically by paraoxon (p-nitrophenylphosphate)
hydrolysis.
Results. In TA patients, the frequency of PON1192R allele
(51% vs. 39%, pC = 0.043, OR = 1.60, 95%CI = 1.03-2.47), PON155M
allele (21% vs. 7%, pC = 0.0001, OR = 3.80, 95% CI = 2.03-7.10),
and PON1-108C (60.1% vs. 46% pC = 0.011, OR 1.79 (95%CI =
1.15-2.79) increased significantly with respect to healthy
controls. PON1 activity was significantly lower for PON1192
in TA vs. controls (147.4 ± 58.4 vs. 294.8 ±
146.4 µmol.min-1.ml-1, p < 0.05), showing a decreasing
activity accord to genotypes, QQ>QR>RR, in TA patients
and an increasing activity in control subjects.
Conclusions. These results show a higher frequency of PON1192R,
PON155M, and PON1-108C alleles and reduced PON1 activities
in TA patients; these could be factors contributing to the
development of Takayasu´s arteritis
[Back to top]
Naproxen: An Update On Physicochemical, Analytical
And Pharmacological
Prabodh Chander Sharma
[FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00016]
Naproxen is a propionic acid derivative related to the arylacetic
acid group. This drug is one of the most popular non-steroidal
anti-inflammatory agents. It is a non-selective cyclooxygenase
inhibitor and is advocated for use in painful and inflammatory
rheumatic and non-rheumatic conditions. In low risk patients,
naproxen and ibuprofen may be the first choice agents because
they are effective, well tolerated and inexpensive. Naproxen
is rapidly and completely absorbed from the gastrointestinal
tract with an in vivo bioavailability of 95% and elimination
half-life is 12 to 17 h. It has a volume of distribution of
0.16 L/Kg and at therapeutic levels, it is more than 99% albumin-bound.
Although introduced long back, several efforts have been done
to develop its prodrugs and analytical procedures. The current
article describes chemistry, pharmacology, pharmacokinetics,
adverse effects, interactions and contraindications of naproxen.
A special emphasis is laid on the review of recent literature
of various prodrugs synthesized and analytical methods developed
for determination of naproxen in pharmaceutical preparations
[Back to top]
An overview of the actions of capsaicin and its receptor,
TRPV1, and small primary sensory neurons
Akio Hiura Hiroshi Nakagawa
[FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00018]
The specific actions of capsaicin on the small primary afferent
neurons with regard to neurogenic inflammation and plasma
extravasation are examined in this review. First, a short
history of the study of capsaicin is introduced from the viewpoint
of the efferent function of capsaicin-sensitive nerve fibers.
Agonist (resiniferatoxin) and antagonists (capsazepine and
ruthenium red) of capsaicin are referred, to better understand
the action of the drug. The significance of the discovery
of capsaicin receptor, TRPV1, and its characteristic features
(plymodal receptor)are discussed based on recent reports,
although the sensitization or desensitization mechanisms are
not yet resolved. This review also briefly deals with the
therapeutic use of capsaicin and its agonist and antagonist
for relief pain. Whether or not capsaicin-sensitive nerve
fibers are involved in itching is examined by a recent literature
survey. TRPV1-expressing nerve fibers were recently reported
to be responsible for the itching sensation. Three possble
itching pathways were raised. The participation of pure sensory
nerve fibers which exclusively transmit itchiness has not
been found, as yet.
[Back to top]
Sensory Nerves and Mast cells
Fatma Tore Nese Tuncel
[FULL-TEXT
INQUIRY] [BSP/CMCAIAA/E-Pub/00019]
Mast cell and sensory nerve relation consists three indispensable
conditions: proximity, communication and a shared view of
life. Mast cells are found in all tissues of the human body,
especially located closely to nerves. Proven not to be a random
configuration, mast-nerve membrane to membrane contact is
highly common. This, should be by fate rather than an accident
since such spatial distributions mostly indicate a functional
relationship. Mast cells associated to sensory nerves contain
ammunitions of neuropeptides and also a range of neuropeptide
receptors enabling nerve to mast cell, mast cell to nerve
and reciprocal communications which form the basis of neuroimmune
interfacing. Wondering about the possible effects of this
intimacy and communication potential on several physiological
and pathophysiological events, specifically on diseases with
low success rate of therapy and mysterious mechanisms, sciencetists
have discovered many aspects of mast-nerve interactions. In
the light of these studies, from a focal point between nervous
and immune systems mast cells almost cover all the perspective
of collaboration as an indispensable building block of neuroimmune
system.
[Back to top]
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