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Tetrahedron
Abstract Volume 129, 17 December 2022, 133117 Bismuth(III) bromide catalyzed synthesis

Introduction of polyhydroquinoline derivatives via t…

Tetrahedron Letters, Volume 56, Issue 27, 2015, pp. …
Section snippets
Medicinal bismuth: Bismuth-organic Joshua S. Yoo, …, Ram S. Mohan

References (120)
frameworks as pharmaceutically Bismuth and metal-doped bismuth
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Abstract

Historically organometallic compounds have been used to cure certain diseases with
limited applications. Although bismuth belongs to the category of heavy metals,
many of its derivatives have found applications in modern drug discovery research,
mainly because of its low toxicity and higher bioavailability. Being an eco-friendly
mild Lewis acid, compounds having bismuth as a central atom are capable of
binding several proteins in humans and other species. Bismuth complexes
demonstrated antibacterial potential in syphilis, diarrhea, gastritis, and colitis. Apart
from antibacterial activities, bismuth compounds exhibited anticancer,
antileishmanial, and some extent of antifungal and other medicinal properties. This
article discusses major synthetic methods and pharmacological potentials of
bismuth complexes exhibiting in vitro activity to significant clinical performance in a
systematic and timely manner.

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Introduction

For hundreds of years, metal-containing substances have been employed in

medicine and health applications [1,2]. As early as 3500 years ago, gold-based
treatments were developed in India, China, and the Middle East [3], while
mercurous chloride (Hg2Cl2) was used as a diuretic during the Renaissance period
[4]. Metal-based medicines and diagnostics have a long history of success. Arsenic
trioxide was also used as a lead compound for treating acute promyelocytic
leukemia as a traditional medicine in ancient China [5,6]. The current applications
of metal compounds for therapy and diagnosis are primarily inspired by the success
of cisplatin (cis[Pt(NH3)2Cl2]) as an anticancer medication [7].

Bismuth is the 83rd element (Group 15, Period 6) in the modern periodic table, and
belongs to the same group as nitrogen, phosphorus, arsenic, and antimony in the
periodic table. Although bismuth belongs to the group of toxic metals, bismuth itself
and its compounds are considered significantly harmless because some of the
bismuth drugs are less toxic than table salt. This nontoxic property makes bismuth
unique among all the heavy metals, and it has earned the title of “green element”
because of its environmentally benign character although long-term use of bismuth
derivatives may cause toxicity to some extent [[8], [9], [10], [11], [12], [13], [14],
[15]].

Bismuth has long been used to cure some diseases for its medicinal property. The
major applications of bismuth in medicine and health care are related to a variety of
gastrointestinal disorders, antitumor, antimicrobial, and antibacterial activities [16].
The first bismuth-containing drug, for the treatment of dyspepsia, was published in
1786, indicating the use of bismuth complexes in medical aspects [17]. Following
that, many bismuth complexes were investigated for the treatment of
gastrointestinal diseases and microbiological infections, such as syphilis, diarrhea,
gastritis, and colitis and many of them showed therapeutic activity with fewer side
effects. Improving novel therapies and a greater understanding of bismuth's
mechanism of action will extend the usage of bismuth-based pharmaceuticals in
health care [18]. In this study, we have explored synthesis methods and medicinal
properties of bismuth complexes, bismuth nanoparticles, and some bismuth
heterocyclic compounds.

Section snippets

Bismuth in medicine: historical perspectives

The word bismuth means “White mass” in German (wismuth). Bismuth (Bi) is the
83rd element in the periodic table, has a mass of 208.98, a melting point of 271.3 °C,
a boiling point of 1837 K, and a density of 9.7 g/cm3. Bismuth possesses two major
oxidation states, bismuth (III) and bismuth (V), but oxidation states (II) and (IV) have
been reported. However, the bismuth (III) is the most stable form, so that is the most
common oxidation state [[19], [20], [21]]. Trivalent bismuth has a high …

Bismuth complexes: side effects and toxicity

Although bismuth is considered as green element and nontoxic, as previously

stated, long-term usage of bismuth in human subjects may result in some negative
effects. Patients can experience toxicity at various amounts of bismuth in their
blood, but the illness is uncommon when bismuth levels are less than 50 mg/L [111].
In the 1970s, reckless usage of bismuth (over 10 g per day) resulted in an outbreak of
bismuth-induced neurotoxicity in France and Australia [112,113]. Among the
bismuth-based …

Mechanism of low toxicity bismuth drugs

Although the molecular mechanism of bismuth drug is still unclear, Metallodrugs

sometimes show their actions through functional interference or binding with
metalloproteins/metalloenzymes by disrupting the multiple biological pathways.
For example, H. pylori has built complex system for survival, colonization, and
persistence in the host and regulate metal homeostasis. After in-depth investigation
on H. pylori it is identified that a total of 63 Bi-binding proteins and 119 Bi-regulated
…

Conclusion and future perspectives

Although bismuth compounds are extensively used in different gastrointestinal

diseases for many years, the applications of bismuth complexes in biomedical and
pharmaceutical fields are still growing. Using different synthetic procedures,
ligands, catalysts unique medicinally privileged bismuth compounds have been
synthesized with higher potency and low toxicity. The major biological target of
bismuth appears to various proteins and enzymes and in many cases the
mechanistic studies at the …

Funding

This research received no external funding. …

Declaration of competing interest

The authors declare that they have no known competing financial interests or
personal relationships that could have appeared to influence the work reported in
this paper. …

Acknowledgments
The authors are grateful to the Department of Chemistry and the School of Earth
Environment & Marine Sciences (SEEMS) of the University of Texas Rio Grande
Valley for start-up funding (to DB) and for extending facilities for this study. The
Department of Chemistry at the University of Texas Rio Grande Valley is grateful for
the generous support provided by a Departmental Grant from the Robert A. Welch
Foundation (Grant No. BX-0048). …

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