Combinatorial
Chemistry & High Throughput Screening
ISSN: 1386-2073
Combinatorial Chemistry
& High Throughput Screening
Volume 13, Number 10, December 2010
Contents
Traditional Chinese Medicine
Guest Editor: Ping Zhou
Editorial Pp. 836
High Throughput Screening for Bioactive Components
from Traditional Chinese Medicine Pp. 837-848
Yanhui Zhu, Zhiyun Zhang, Meng Zhang, Dale E. Mais and
Ming-Wei Wang
[Abstract] [Purchase
Article]
Natural Products Derived from Traditional Chinese Medicine
as Novel Inhibitors of the Epidermal Growth Factor Receptor
Pp. 849-854
Serkan Sertel, Peter K. Plinkert and Thomas Efferth
[Abstract] [Purchase
Article]
Progress on the Screening and Analysis of Bioactive Compounds
in Traditional Chinese Medicines by Biological Fingerprinting
Analysis Pp. 855-868
Fengjiao Yu, Liang Kong, Hanfa Zou and
Xiaoyuan Lei
[Abstract] [Purchase
Article]
Recent Advances in Quality Control of Traditional Chinese
Medicines Pp. 869-884
E-Hu Liu, Lian-Wen Qi, Kai Li, Chu Chu and Ping
Li
[Abstract] [Purchase
Article]
Screening of Enzyme Inhibitors from Traditional Chinese
Medicine Pp. 885-899
Yao Shen, Yuming Hu, Bo Chen and Shouzhuo Yao
[Abstract] [Purchase
Article]
Recent Developments in Chromatographic Fingerprints
from Herbal Products: Set-Up and Data Analysis Pp.
900-922
Goedele Alaerts, Bieke Dejaegher, Johanna Smeyers-Verbeke
and Yvan Vander Heyden
[Abstract] [Purchase
Article]
Chip-Based High Throughput Screening of Herbal Medicines
Pp. 923-931
Pravin K. Naoghare and Joon Myong Song
[Abstract] [Purchase
Article]
Counter-Current Chromatography for High Throughput
Analysis of Natural Products Pp. 932-942
Shihua Wu and Junling Liang
[Abstract] [Purchase
Article]
Chromatographic Fingerprinting and Metabolomics for
Quality Control of TCM Pp. 943-953
Yi-Zeng Liang, Pei-Shan Xie and Kelvin Chan
[Abstract] [Purchase
Article]
Recent Applications of Capillary Electrophoresis in
the Analysis of Traditional Chinese Medicines Pp.
954-965
Airong Feng, Bolin Tian, Jiming Hu and Ping
Zhou
[Abstract] [Purchase
Article]
MEET THE GUEST EDITOR Pp.
966
ERRATUM Pp. 967
Abstracts
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Editorial:
Medicinal herbs have been used to treat human diseases in
China for thousands of years. There has been great interest
in the research and development of bioactive components from
herbal medicines. Significant pharmacological properties have
been demonstrated for many herbs over recent decades. Not
only important in China, herbal preparations are becoming
increasingly popular in Europe and North America as complementary
therapeutics.
Traditional Chinese Medicine (TCM) is usually a mixture of
herbal plants or extracts which comprise hundreds of different
constituents with widely differing physiochemical properties.
The qualification and quantitative analysis of active constituents
from this mixture is often a challenging task especially when
the relevant compounds might be present in minute amounts
only. Additional challenge is batch-to-batch inconsistency
of constituents due to the natural variability of the herbal
plants. Thus, there is a substantial need to use modern bioassay
and analytical techniques, including developing high throughput
and sensitive technologies, to determine active constituents
and to monitor the quality control of herbal medicines. The
rapid growth in proteomics, genomics and metabonomics provides
a lot of new tools for the integration of traditional Chinese
medicine with modern technology and systems biology. This
special issue aims at providing the readers of CCHTS with
a perspective of the technology developments and their applications
in the rapid progress of up-to-date research in TCM.
I would like to express my thanks to all the contributors
for their valuable articles and to the referees for their
constructive comments as well as to Professor Rathnam Chaguturu,
the Editor-in-Chief, for his continuing support during the
preparation of this issue.
Ping Zhou
(Guest Editor)
College of Chemistry and Molecular Sciences
Wuhan University
Wuhan 430072
P.R. China
E-mail: zbping@whu.edu.cn
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[Purchase Article]
High Throughput Screening for Bioactive Components from Traditional
Chinese Medicine
Yanhui Zhu, Zhiyun Zhang, Meng Zhang, Dale E. Mais and
Ming-Wei Wang
Throughout the centuries, traditional Chinese medicine has
been a rich resource in the development of new drugs. Modern
drug discovery, which relies increasingly on automated high
throughput screening and quick hit-to-lead development, however,
is confronted with the challenges of the chemical complexity
associated with natural products. New technologies for biological
screening as well as library building are in great demand
in order to meet the requirements. Here we review the developments
in these techniques under the perspective of their applicability
in natural product drug discovery. Methods in library construction,
component characterization, biological evaluation, and other
screening approaches including NMR and X-ray diffraction are
discussed.
[Back to top] [Purchase
Article]
Natural Products Derived from Traditional Chinese Medicine
as Novel Inhibitors of the Epidermal Growth Factor Receptor
Serkan Sertel, Peter K. Plinkert and Thomas Efferth
The epidermal growth factor receptor (EGFR) has become an
important molecular target in cancer therapy. Various small
molecules and therapeutic antibodies targeting EGFR family
members have been developed during recent years and are established
in clinical oncology. However, increasing clinical application
of EGFR tyrosine kinase inhibitors has resulted in the development
of resistance to EGFR-targeting drugs due to the selection
of EGFR-mutated variants. This phenomenon forced the search
for novel EGFR inhibitors with activity towards EGFR-mutant
tumors. This review describes recent achievements in natural
products derived from medicinal plants as novel EGFR inhibitors.
[Back to top] [Purchase
Article]
Progress on the Screening and Analysis of Bioactive Compounds
in Traditional Chinese Medicines by Biological Fingerprinting
Analysis
Fengjiao Yu, Liang Kong, Hanfa Zou and
Xiaoyuan Lei
Traditional Chinese medicines (TCMs), a key branch of natural
medicines, play an important role in the treatment of diseases
because of their reliable clinical performance. Identification
of their active compounds constitutes a bottleneck in the
development of TCMs. Screening and analysis of active compounds
is a challenge in TCM research. This review summarizes recent
progress in the development of biological fingerprinting strategies
for screening and analyzing bioactive compounds in TCMs using
molecular recognition, metabolism and omics tools. The evaluated
strategies include the following techniques: microdialysis/centrifugal
ultrafiltration-HPLC, biochromatography, metabolic fingerprinting
analysis, 2-dimensional biochromatography and omics fingerprinting
analysis.
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Article]
Recent Advances in Quality Control of Traditional Chinese
Medicines
E-Hu Liu, Lian-Wen Qi, Kai Li, Chu Chu and Ping
Li
Traditional Chinese medicines (TCMs) have been used for disease
prevention and therapy in China for a long history and are
becoming increasingly popular over the world. However, TCMs
are complex mixtures and contain usually hundreds of chemically
different constituents, which make the quality control of
crude drugs and their medical preparations extremely difficult.
Therefore, better analytical strategies to assure their efficacy,
safety and consistency are in great demand. The present work
provides an overview of the development of quality control
for TCMs based on microscopic and molecular identification,
quantitative and qualitative analysis, fingerprint, combination
of fingerprint and multi-component quantification, as well
as activity-integrated fingerprint over the last five years.
The biological fingerprinting analysis of TCMs with targeting
absorption, distribution, metabolism, excretion by chromatographic
and chemometric method are also highlighted due to its broad
application in the quality control of TCMs. The comprehensive
methods analyzed with modern hyphenated techniques are strongly
recommended to assess the authenticity, quality consistency
and stability of TCMs.
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Article]
Screening of Enzyme Inhibitors from Traditional Chinese
Medicine
Yao Shen, Yuming Hu, Bo Chen and Shouzhuo Yao
Traditional Chinese medicine (TCM) has been used for more
than 4000 years. By comparison with large combinatorial chemistry
libraries and natural products of the West for high-throughput
screening (HTS) of new drugs discovery, an advantage of TCM
is that the preparation has clear efficacies on the therapy
of some diseases. Although the effective components are not
clear, the clear efficacies of TCM have been identified for
long time practice, Therefore, TCMs should be valuable lead
compound libraries with a definite therapy efficacy from the
viewpoint of HTS. Nevertheless, current HTS technologies are
not easily adapted to investigate TCMs because they are designed
for screening a relatively pure known chemical at a known
concentration. In contrast, TCMs are mixtures of unknown compounds
in unknown concentrations that may differ markedly between
samples from different plants. This article reviews the current
and future researches on the enzyme inhibitors screening from
TCM.
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Article]
Recent Developments in Chromatographic Fingerprints from Herbal
Products: Set-Up and Data Analysis
Goedele Alaerts, Bieke Dejaegher, Johanna Smeyers-Verbeke
and Yvan Vander Heyden
The use of chromatographic fingerprints from herbal products
where the whole chromatographic profile is applied, is an
approach to evaluate the quality of the investigated product.
In this paper, recent developments in the set-up and data
analysis of chromatographic fingerprints for herbal products
are discussed. First, different set-ups for fingerprint development
are reviewed. Prior to the fingerprint development, a suitable
sample preparation, e.g. extraction, should be considered.
In a second instance, this review focuses on the data analysis
with regards to the different fingerprint applications. Usually,
chemometric data pretreatment is necessary. This is discussed
first, followed by a short overview of the data handling techniques
used in the two main application areas of herbal fingerprints,
i.e. quality assurance and classification or calibration.
The quality assurance, involving identification and quality
control of the herbal products, is reviewed, followed by the
use of fingerprints in classification or modelling. The different
application areas are illustrated and discussed with several
case studies.
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[Purchase
Article]
Chip-Based High Throughput Screening of Herbal
Medicines
Pravin K. Naoghare and Joon Myong Song
At present, high throughput screening (HTS) programs in drug
discovery rely mainly on compound libraries from combinational
chemistry. Similarly, natural flora has been used as a prominent
origin for new and potent herbal drugs. Herbal medicines have
been used worldwide for thousands of years to cure many diseases.
As such, herbal secondary metabolites show a remarkable structural
diversity that supplements chemically synthesized compound
analogs in drug discovery screening. Unfortunately, there
is often a considerable deterioration in the quality of herbal
drugs in such screening programs as there are time-consuming
manual processes involved in the isolation of active ingredients
from the highly complex mixtures of herbal plant products.
The quality and quantity of herbal samples are critical for
the success of HTS programs. In the recent past, there have
been substantial improvements in HTS due to the miniaturization
and integration of microchip (e.g., Herbochip®, DNA chip,
protein chip, cell chip, etc.)-based technologies so as to
design herbal drugs that compete with synthetic drug analogs.
Here we will review various technologies used for HTS of herbal
medicines. Finally, we will summarize our efforts to develop
a novel chip-based HTS assay to explore the antioxidant and
radioprotective properties of herbal plants.
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Article]
Counter-Current Chromatography for High Throughput
Analysis of Natural Products
Shihua Wu and Junling Liang
Counter-current chromatography (CCC) is a unique support-free
liquid-liquid partition chromatography winning wide applications
in the separation of various components from natural or synthetic
mixtures. It has been one of the prime methods for isolating
compounds from Traditional Chinese Medicines (TCM) and other
comprehensive natural products. Although early CCC models
produced a long-standing false image that CCC is a time-consuming
technique, rapid and high-performance CCC devices and methods
for high throughput analysis of natural mixtures have been
advanced. For instances, multi-channel CCC, dual CCC, elution-extrusion
CCC, and solvent simplification protocols can provide high
throughput CCC analysis and produce high purity of compounds
or large natural product libraries for drug discovery. This
review summarizes the recent advancements of CCC in the high
throughput analysis of natural product with an emphasis on
the developments of instruments and methods.
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Article]
Chromatographic Fingerprinting and Metabolomics for
Quality Control of TCM
Yi-Zeng Liang, Pei-Shan Xie and Kelvin Chan
Chromatographic fingerprinting technique of traditional Chinese
medicine (TCM) has proved to be a comprehensive strategy for
assessing the intact quality of herbal medicine. In general,
one could use the chromatographic techniques to obtain a relatively
complete picture of herbal medicines, which are in common
called chromatographic fingerprints of herbal medicines to
represent the so-called phytoequivalence. Based on this, the
features of chromatographic fingerprints of herbal medicines
have been discussed in some detail. The technique based on
chromatographic fingerprinting is essentially a kind of high-throughput
and integral tools to explore the complexity of herbal medicines.
In order to further control the comprehensive quality of TCMs,
some new strategies are proposed to trace the chemical changes
of chromatographic fingerprints both in product processing
and/or after their administration by modern chromatographic
techniques and chemometrics. Combined with metabolomics, it
seems possible for one to reveal the working mechanism of
TCMs and to further control their intrinsic quality. Finally,
the intensive study of chromatographic fingerprinting coupled
with multivariate analysis tools developed in bioinformatics
and chemometrics are emphasized in order to achieve the aim
to reveal the working mechanisms of TCMs and to further control
and strengthen TCMs’ intrinsic quality in a comprehensive
manner.
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[Purchase
Article]
Recent Applications of Capillary Electrophoresis in
the Analysis of Traditional Chinese Medicines
Airong Feng, Bolin Tian, Jiming Hu and Ping
Zhou
Traditional Chinese medicines (TCMs) are generally mixtures
of herbal plants or extracts which comprise hundreds of different
constituents with widely difference in the content and physiochemical
properties. In order to analyze bioactive compounds in TCMs
and control the quality, a large number of analytical tools
have been developed, among which capillary electrophoresis
(CE) has become a powerful technique with increasing importance.
Some formats of CE, including capillary zone electrophoresis,
micellar electrokinetic chromatography, non-aqueous CE and
capillary electrochromatography have been widely employed
for the analysis of TCMs. The general characteristics of these
formats are briefly described, and their applications to the
analysis of TCMs during the past five years are summarized.
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MEET THE GUEST EDITOR
Ping Zhou
College of Chemistry and Molecular Sciences
Wuhan University
Wuhan 430072
P.R. China
E-mail: zbping@whu.edu.cn
Ping Zhou holds an Honors MS in Botany from
the Wuhan University, China (1994) and a Ph.D. in Analytical
Chemistry (1997) from the same university. From 1997 to 1998,
he worked at the Faculty of Pharmaceutical Sciences, University
of Tokushima, Japan, as a foreign researcher in Pharmacognosy.
He joined the Wuhan University as an associate professor in
1999. From 2008-2009, he worked at the Institute for Biological
Sciences, National Research Council Canada, as a visiting
scholar in biological mass spectrometry. He is the Vice Director
of Centre for Analysis & Measurement of Wuhan University
and the Vice Chairman of Young Academic Committee of Chinese
Association for Instrumental Analysis. His scientific interests
include separation and analysis of active biomolecules, capillary
electrophoresis and biological mass spectrometry. Some selected
publications are cited below.
REFERENCES
[1] Zhou, P.; Takaishi, Y.; Duan H.; Chen,
B.; Honda, G.; Itoh, M.; Takeda, Y.; Kodzhimatov, O.K.; Lee,
K.H. Coumarins and bicoumarin from Ferula sumbul:
anti-HIV activity and inhibition of cytokine release, Phytochemistry,
2000, 53, 689-697.
[2] Zhou, P.; Yan, J.; Deng, Y. Rejection
of capillary wall background in an on-column confocal fluorescence
detector. Analyst, 2000, 125,
2241-2243.
[3] Zhou, P.; Yu, S.; Liu, Z.; Hu, J.M.;
Deng, Y.Z. Electrophoretic separation of DNA using a new matrix
in uncoated capillaries. J. Chromatogr. A, 2005,
1083, 173-178.
[4] Zhou, P.; Chandan, V.; Liu, X.; Chan,
K.; Altman E.; Li, J. Micro-wave-assisted sample preparation
for rapid and sensitive analysis of Helicobacter pylori
lipid A applicable to a single colony. J. Lipid Res.,
2009, 50, 1936-1944.
[5] Zhou, P.; Altman, E.; Perry, M.B.; Li,
J. Study of matrix additives for sensitive analysis of lipid
A by matrix-assisted laser desorption ionization mass spectrometry.
Appl. Environ. Microbiol., 2010,
76(11), 3437-3443.
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ERRATUM
Due to an oversight on the part of the authors, Emirhan Nemutlu,
Sedef Kir, Hakan Eroglu, Doruk Katlan, Aykut Özek, Özgür
Özyüncü and M. Sinan Beksaç, incorrect
name of one of the co-author was published in the article
entitled "Comparison of Pharmacokinetic Profiles
of Moxifloxacin in Caesarean versus Non-Pregnant Sectioned
Women by Fully Validated HPLC with Fluorescence Detection",
Combinatorial Chemistry & High throughput Screening,
2010, Vol. 13, Issue no. 6, pp. 502-509.
The correct name of the author is Özgür Özyüncü
instead of Özgür Öyüncü.
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