Review
manuscripts: Before writing their manuscripts, potential authors of
review articles
should forward the title and a short abstract to the Guest Editor. The
Guest Editor will then provide feedback on the suitability of the topic
upon
consultation with other editors and/or members of the Editorial Board.
Authors
are encouraged to write reviews that provide a critical appraisal of
areas of 5-fluorouracil research.
Ning Zhang 1,
Ying Yin 2, Sheng-Jie Xu 2 and Wei-Shan Chen 1,*
1
Department of Orthopaedics, 2nd Affiliated Hospital, School of
Medicine, Zhejiang University, #88 Jiefang Road, Hangzhou, 310009, P.R.
China; E-mail: zhangning98@gmail.com
2 Institute of Clinical
Research, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang
University, #3 East Qingchun Road, Hangzhou, 310016, P.R. China;
E-mails: dy1225@gmail.com, xusj@zju.edu.cn
* Author to whom correspondence should be addressed; E-mail:
zrspine@gmail.com
Received: 18 June 2008; in revised
form: 1 July 2008 / Accepted: 15 July 2008 / Published: 5 August 2008
Review: 5-Fluorouracil: Mechanisms of Resistance
and Reversal Strategies
Molecules
2008, 13, 1551-1569
(PDF
format 214 K); DOI:
10.3390/molecules13081551Georgios V. Koukourakis 1,*, Vassilios Kouloulias 1, Michael J. Koukourakis 2, Georgios A. Zacharias 3, Haralabos Zabatis 4, John Kouvaris 51
Attikon University Hospital of Athens, 2nd Radiology Department,
Radiation Therapy Unit, Medical School of Athens, Greece; Emails:
gkoyokoyrakis@yahoo.gr (Koukourakis); vkouloul@cc.ece.ntua.gr
(Kouloulias)
2 University Hospital of Thrace, Radiation Therapy Unit, Alexandroupolis, Greece; Email: targ@her.forthnet.gr
3 Policlinic of Athens, Section of Pathology, Athens Greece. Email: george_zaharias@yahoo.gr
4 Saint Savvas Anticancer Institute of Athens, 1st Radiation Therapy Unit Athens Greece; Email: bzabatis@hol.gr
5
Aretaieion University Hospital, 1st Radiology Department, Radiation
Therapy Unit, Medical School of Athens, Greece; Email:
johnkouv@aretaieio.uoa.gr
* Author to whom correspondence should be addressed. Email: gkoyokoyrakis@yahoo.gr.
Received: 30 May 2008; in revised form: 15 August 2008 / Accepted: 25 August 2008 / Published: 27 August 2008Review: Efficacy of the Oral Fluorouracil Pro-drug Capecitabine in Cancer Treatment: a ReviewMolecules
2008,
13, 1897-1922 (PDF format 289 K); DOI:
10.3390/molecules13081897Manuscript ID: fluorouracil-20080415-Nishimoto-jp
Title:
Radiation- and photo-induced
activation of 5-fluorouracil prodrugs as a strategy for selective
treatment of solid tumors
Authors: Sei-ichi Nishimoto, Kazuhito Tanabe, Takeo Ito, Hisatsugu
Yamada,and Hiroshi Hatta
Corresponding author: Sei-ichi Nishimoto, Ph.D. Professor of
Excited-State Hydrocarbon Chemistry, Graduate School of Engineering,
Kyoto University, Katsura Campus, Kyoto 615-8530, Japan
Tel: +81-75-383-2500/FAX: +81-75-383-2501
E-mail:
nishimot@scl.kyoto-u.ac.jp
URL:
http://www.ehcc.kyoto-u.ac.jp/eh32/home/web-content/index-e.htm
Abstract: Nowadays, 5-fluorouracil (5FU) is widely used as an
anticancer drug to treat solid cancers, such as colon, breast, rectal,
and pancreatic cancers, although its clinical application is limited
because 5FU shows gastrointestinal and hematological toxicities.
A great deal of efforts have been made in the search for prodrugs with
functions that are
tumor-selectively delivered and activated to improve the clinical
utility of 5FU as an important cancer chemotherapeutic agent.
Since UV-light and ionizing radiations can cause chemical reactions in
a localized area of the body,their applications into site-specific drug
activation and sensitization have been thus developed. In this
review, we describe recent progress in
The development of novel 5FU prodrugs that are site-specifically
activated by UV-light and ionizing radiations under tumor
microenvironments, and discuss chemical mechanisms of the activation.
Manuscript ID: fluorouracil-20080630-Breda-it
Title:
A Review of Analytical Methods for the Determination of 5-Flurouracil in Biological Matrices
Authors: Massimo Breda, Simona Barattè
Corresponding author: Massimo Breda, Accelera, Nerviano Medical Sciences, Viale Pasteur 14, 20014 Nerviano, Milan, Italy
E-mail:
Massimo.Breda@nervianoms.com
Abstract: 5-Fluorouracil (5-FU) is a cytostatic agent, which has been
widely used in the treatment of various solid tumours for more than 20
years, and is still considered amongst the most active antineoplastic
agent in the advanced colorectal cancer and malignancies of head and
neck. A large number of non-chromatographic and chromatographic methods
for the quantitation of 5-FU, related pro-drugs, and their metabolites
in biological matrices have been developed in the last 30 years to
support preclinical and clinical studies. In this review the advantages
and disadvantages of these analytical methods will be discussed.
Manuscript ID: fluorouracil-20080706-Farquharson-us
Title:
Detection of 5-Fluorouricil in Saliva by Surface-Enhanced Raman
Spectroscopy
Authors: Stuart Farquharson, Alan Gift, Chetan Shende, Frank Inscore, Beth Ordway, Carl Farquharson and John Murran
Corresponding author: Stuart Farquharson, President & CEO,
Real-Time Analyzers, Inc. 362 Industrial Park Rd. (#8) Middletown, CT
06457 860-635-9800, x230
E-mail:
Stu@rta.biz
Abstract: The ability of surface-enhanced Raman spectroscopy (SERS) to
measure 5-fluorouracil (5-FU) in saliva is presented. The approach is
based on the ability of Raman spectroscopy to provide a unique spectral
signature for virtually every chemical, and the ability of SERS to
provide microgram/milliliter sensitivity. A simple sampling method,
that employed 1-mm glass capillaries filled with silver-doped sol-gels,
was developed to isolate 5-FU from potential interfering chemical
components of saliva and simultaneously provide SERS-activity. The
method involved treating a 1 milliliter saliva sample with 1 milliliter
of acetic acid, drawing 10 microliters of sample into a SERS-active
capillary by syringe, and then measuring the SER spectrum. Quality SER
spectra were obtained for samples containing as little as 2 micrograms
of 5-FU in 1 milliliter saliva. The entire process, the acid
pretreatment, extraction and spectral measurement, took less than 5
minutes. The surface-enhanced Raman spectra of 5-fluorouridine and
5-fluoro-2-deoxyuridine, two major metabolites of 5-FU, were also
measured and shown to have unique spectral peaks. These measurements
suggest that disposable SERS-active capillaries could be used to
measure 5-FU and metabolite concentrations in chemotherapy patient
saliva, thereby providing metabolic data that would allow regulating
dosage. Tentative vibrational mode assignments for 5-FU and its
metabolites are also given.
Received: 6 July 2008
Manuscript ID: fluorouracil-20080626-Arias-es
Title:
Novel Strategies to Improve the Anticancer Action of 5-Fluorouracil by Using Drug Delivery Systems
Author: Jose L. Arias
Corresponding author: Dr. Jose L. Arias, Grupo Investigación Farmacia
Práctica (CTS-205), Dept. Farmacia y Tecnología Farmacéutica Facultad
de Farmacia, Campus Universitario de Cartuja, s/n, Universidad de
Granada, 18071 Granada
Tel.: (+34) 958 24 39 02; Fax: (+34) 958 24 89 58
E-mail:
jlarias@ugr.es
Abstract: Because of the fundamental importance of new therapeutic routes
for cancer treatment, a number of systems based on colloidal particles as
vehicles for the delivery of the anticancer drug 5-fluorouracil have been
devised. The target is always to provide the proper dose of the antitumour
agent only at the desired locus of action, thus reducing the unwanted side
effects. In this review, the main strategies and the more significant
results in the development of 5-fluorouracil carriers for cancer treatment
are discussed.
Yasuhiro Tsume 1,
Balvinder S. Vig 2, Jing Sun 3, Christopher P.
Landowski 4, John M. Hilfinger 5,
Chandrasekharan Ramachandran 1 and Gordon L. Amidon 1,*
1 Department of Pharmaceutical Science, College of Pharmacy, University
of Michigan, 428 Church Street, Ann Arbor, MI 48109-1065, USA; E-mails:
ytsume@umich.edu; rcmad@umich.edu
2 Pharmaceutical Research Institute, Bristol-Myers Squibb Company, New
Brunswick, NJ 08502; E-mail: balvinder.vig@bms.com
3 Department of Medicinal Chemistry, University of Michigan, Ann Arbor,
Michigan 48109, USA; Email: sunjing@umich.edu
4 Institute of Biochemistry and Molecular Medicine, University of Bern,
CH-3012 Bern, Switzerland; E-mail: christopher.landowski@mci.unibe.ch
5 TSRL, Inc. Ann Arbor, Michigan 48108, USA; Email:
jhilfinger@tsrlinc.com
* Author to whom correspondence should be addressed; E-mail:
glamidon@umich.edu; Phone: +1-734-764-2440; Fax: +1-734-763-6423.
Received: 12 June 2008 / Accepted: 27
June 2008 / Published: 28 June 2008
Article: Enhanced Absorption and Growth
Inhibition
with Amino Acid
Monoester Prodrugs of Floxuridine by Targeting hPEPT1 Transporters
Molecules
2008, 13, 1441-1454
(PDF
format 132 K); DOI:
10.3390/molecules13071441
Francesco Puoci 1,*,
Francesca
Iemma
1, Giuseppe Cirillo 1, Nevio Picci 1, Pietro Matricardi 2
and
Franco Alhaique 2
1 Dipartimento di Scienze Farmaceutiche, Università della
Calabria, Edificio Polifunzionale, Arcavacata di Rende (CS) 87036, Italy
2 Dipartimento di Studi di Chimica e Tecnologia delle Sostanze
Biologicamente Attive, University “La Sapienza”, P.le A. Moro 5, 00185
Roma, Italy
* Author to whom correspondence should be addressed; email:
francesco.puoci@unical.it; Tel. (+39) 0984493151, fax (+39) 0984493151
Received: 21 March 2007;
in revised
form: 13 March 2007 / Accepted: 16 April 2007 / Published: 18 April 2007
Full Paper: Molecularly Imprinted Polymers
for
5-Fluorouracil Release in Biological Fluids
Molecules
2007,
12, 805-814 (PDF
format 69 K
)