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Biological Chemistry of Arsenic, Antimony and Bismuth

Hongzhe Sun (Editor)
ISBN: 978-0-470-71390-7
400 pages
January 2011
Biological Chemistry of Arsenic, Antimony and Bismuth (0470713909) cover image


Arsenic, antimony and bismuth, three related elements of group 15, are all found in trace quantities in nature and have interesting biological properties and uses. While arsenic is most well known as a poison - and indeed the contamination of groundwater by arsenic is becoming a major health problem in Asia - it also has uses for the treatment of blood cancer and has long been used in traditional chinese medicine. Antimony and bismuth compounds are used in the clinic for the treatment of parasitic and bacterial infections.

Biological Chemistry of Arsenic, Antimony and Bismuth is an essential overview of the biological chemistry of these three elements, with contributions from an international panel of experts. Topics covered include:

  • chemistry of As, Sb and Bi
  • biological chemistry of arsenic
  • biological chemistry of Sb and Bi
  • arsenic and antimony speciation in environmental and biological samples
  • arsenic in traditional chinese medicine
  • arsenic in aquifers
  • biomethylation of As, Sb and Bi
  • uptake of metalloids by cells
  • bismuth complexes of porphyrins and their potential in medical applications
  • Helicobacter pylori and bismuth
  • metabolism of arsenic trioxide in blood of the acute promyelocytic leukemia patients
  • anticancer properties of As, Sb and Bi
  • radio-Bi in cancer therapy
  • genotoxicity of As, Sb and Bi
  • metallomics as a new technique for As, Sb and Bi
  • metalloproteomics for As, Sb and Bi

Biological Chemistry of Arsenic, Antimony and Bismuth conveys the essential aspects of the bioinorganic chemistry of these three elements, making this book a valuable complement to more general bioinorganic chemistry texts and more specialized topical reviews. It will find a place on the bookshelves of practitioners, researchers and students working in bioinorganic chemistry and medicinal chemistry.

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Table of Contents

List of Contributors.


1 The Chemistry of Arsenic, Antimony and Bismuth (Neil Burford, Yuen-ying Carpenter, Eamonn Conrad and Cheryl D.L. Saunders).

1.1 Properties of the Elements.

1.2 Allotropes.

1.3 Bond Energies.

1.4 Oxidation States.

1.5 Relativistic Effects and Orbital Contraction.

1.6 Structure and Bonding.

1.7 Clusters and Extended Structures.

1.8 Hybridization and Inversion.

1.9 Coordination Chemistry.

1.10 Geological Occurrence.

1.11 Aqueous Chemistry and Speciation.

1.12 Analytical Methods and Characterization.

1.13 Conclusions.

2 Arsenic's Interactions with Macromolecules and its Relationship to Carcinogenesis (Kirk T. Kitchin).

2.1 Introduction.

2.2 Arsenic's Interactions with DNA and Proteins.

2.3 Cancer – MOA.

2.4 Arsenic's Many Connections to Carcinogenesis.

2.5 Sources of Information on Arsenic's Mode of Action, Biochemical Effects, Carcinogenesis in Animals and Man, Metabolism and Analytical Chemistry.

2.6 Conclusion.

3 Biological Chemistry of Antimony and Bismuth (Nan Yang and Hongzhe Sun).

3.1 Introduction.

3.2 Biorelevant Coordination Chemistry of Antimony and Bismuth.

3.3 Antimony and Bismuth Compounds in Medicine.

3.4 Interaction with Nucleic Acids.

3.5 Interaction with Amino Acids and Peptides.

3.6 Interaction with Proteins and Enzymes.

3.7 Conclusion and Perspectives.

4 Metallomics Research Related to Arsenic (Hiroki Haraguchi).

4.1 Metallomics – Integrated Biometal Science.

4.2 Analytical Feasibility of ICP-AES and ICP-MS.

4.3 Chemical Speciation of Trace Elements in Biological Samples.

4.4 Summary.

5 Arsenic in Traditional Chinese Medicine (Kui Wang, Siwang Yu and Tianlan Zhang).

5.1 Arsenic Bearing Minerals and their Clinical Applications.

5.2 Metabolism and Pharmacokinetics of Arsenic Bearing Minerals.

5.3 Pharmacological Activities and Mechanisms of Actions of ABMs.

5.4 Perspectives.

6 Microbial Transformations of Arsenic in Aquifers (Jonathan R. Lloyd).

6.1 An Introduction to the Microbial Cycling of Arsenic.

6.2 The Biochemistry of Microbial Arsenic Transformations.

6.3 Microbially Driven Mobilization of Arsenic in Aquifers: a Humanitarian Disaster.

6.4 Conclusions and Future Directions.

7 Biomethylation of Arsenic, Antimony and Bismuth (Richard O. Jenkins).

7.1 Introduction.

7.2 Biomethylation of Arsenic.

7.3 Biomethylation of Antimony.

7.4 Biomethylation of Bismuth.

8 Metalloid Transport Systems (Hsueh-Liang Fu, Xuan Jiang and Barry P. Rosen).

8.1 Introduction.

8.2 Metalloid Uptake Systems.

8.3 Metalloid Efflux Systems.

8.4 Summary and Conclusions.

9 Bismuth Complexes of Porphyrins and their Potential in Medical Applications (Bernard Boitrel).

9.1 Introduction.

9.2 Early Work (1969-1994).

9.3 Bismuth Complexes of Unfunctionalized Porphyrins.

9.4 Bismuth Complexes of Functionalized Porphyrins.

9.5 Future Strategies Towards Bifunctional Chelates (BFC) – Conclusions.

10 Helicobacter pylori and Bismuth (Aruni H.W. Mendis and Barry J. Marshall).

10.1 Introduction.

10.2 Helicobacter pylori.

10.3 Bismuth as an Antimicrobial Agent.

10.4 Mechanism of Action of Bismuth Citrate and CBS on H. pylori and Ulcer Healing.

10.5 In Vitro Susceptibility of H. pylori and other Bacteria to Bismuth Compounds and Antibiotics.

10.6 The Effect of pH on Bactericidal Activity of Bismuth Compounds.

10.7 Novel Preparations of Bismuth Compounds.

10.8 Novel Delivery Systems for Bismuth Compounds and Other Antibiotics.

10.9 The Biochemical Targets of Bismuth.

10.10 Binding of Bismuth Compounds to Plasma Proteins.

11 Application of Arsenic Trioxide Therapy for Patients with Leukaemia (Bo Yuan, Yuta Yoshino, Toshikazu Kaise and Hiroo Toyoda).

11.1 Introduction.

11.2 Cellular and Molecular Mechanisms of ATO Actions.

11.3 Pharmacokinetics of ATO in APL Patients.

11.4 Potential Combination Therapies with ATO.

11.5 Potential ATO Application to Other Leukaemias.

11.6 Conclusion.

12 Anticancer Activity of Molecular Compounds of Arsenic, Antimony and Bismuth (Edward R.T. Tiekink).

12.1 Introduction.

12.2 Arsenic Compounds.

12.3 Antimony Compounds.

12.4 Bismuth Compounds.

12.5 Conclusions.

13 Radiobismuth for Therapy (Martin W. Brechbiel and Ekaterina Dadachova).

13.1 Introduction.

13.2 Targeting Vectors.

13.3 α-Emitters versus β--Emitters.

13.4 Radionuclides.

13.5 Radiolabeling – Chemistry.

13.6 Preclinical Studies.

13.7 Targeted α-Therapy versus Targeted β-Therapy.

13.8 Clinical Studies.

13.9 Alternate Delivery Methods and Uses.

13.10 Prospects and Conclusions.

14 Genetic Toxicology of Arsenic and Antimony (Toby G. Rossman and Catherine B. Klein).

14.1 Introduction.

14.2 DNA Damage in Cells Treated with Arsenicals.

14.3 Mutagenesis in Cells Treated with Arsenicals.

14.4 Other Genotoxic Events in Cells Treated with Arsenicals.

14.5 Effects of Arsenicals on DNA Repair.

14.6 Indirect Mechanisms of Mutagenicity and Comutagenicity by Arsenicals.

14.7 Mutagenesis and Transformation as Secondary Effects of Genomic Instability.

14.8 Antimony.

15 Metalloproteomics of Arsenic, Antimony and Bismuth Based Drugs (Cheuk-Nam Tsang, Ruiguang Ge and Hongzhe Sun).

15.1 Introduction.

15.2 Chemical Speciation of Arsenic Based Drugs and their Metallometabolism.

15.3 Metalloproteomics and its Applications to As-, Sb- and Bi-Based Metallodrugs.

15.4 Biological Regulation of Arsenic and Antimony.

15.5 Conclusions.


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