Biological Activities of Bismuth Compounds: An Overview of the New Findings and the Old Challenges Not Yet Overcome

Abstract

Bismuth-based drugs have been used primarily to treat ulcers caused by Helicobacter pylori and other gastrointestinal ailments. Combined with antibiotics, these drugs also possess synergistic activity, making them ideal for multiple therapy regimens and overcoming bacterial resistance. Compounds based on bismuth have a low cost, are safe for human use, and some of them are also effective against tumoral cells, leishmaniasis, fungi, and viruses. However, these compounds have limited bioavailability in physiological environments. As a result, there is a growing interest in developing new bismuth compounds and approaches to overcome this challenge. Considering the beneficial properties of bismuth and the importance of discovering new drugs, this review focused on the last decade’s updates involving bismuth compounds, especially those with potent activity and low toxicity, desirable characteristics for developing new drugs. In addition, bismuth-based compounds with dual activity were also highlighted, as well as their modes of action and structure–activity relationship, among other relevant discoveries. In this way, we hope this review provides a fertile ground for rationalizing new bismuth-based drugs.

Bioactive Bismuth Compounds: Is Their Toxicity a Barrier to Therapeutic Use?

“…Presently, bismuth is being therapeutically explored in two main fields: antimicrobial and anticancer. In fact, bismuth can interact with nucleotides and amino acids in enzymes and other proteins, which is closely related to its uptake, accumulation, transport, and excretion in the human body, as well as to their antimicrobial and anticancer activities [31][32][33]. A summary of the biological properties of bismuth compounds as well as its main mechanisms of action are illustrated in Figure 1 and in Table S1 (Supplementary Materials).…”

Experimental and Theoretical Approaches to Monitor the Behavior of Bovine Liver Catalase in Interaction with a Binuclear Bismuth Complex

“…However, compounds containing bismuth have limited bioavailability in physiological environments. Therefore, there have been repeated attempts to synthesize bismuth compounds and explore new approaches to overcome this challenge . Bismuth commonly exhibits a +3 valence state and demonstrates significant chelation potential with multidentate ligands containing nitrogen and oxygen atoms during coordination.…”

Fusing Bismuth and Mercaptocarboranes: Design and Biological Evaluation of Low‐Toxicity Antimicrobial Thiolato Complexes

“…Complexes of bismuth(III) like bismuth subsalicylate (BSS, Pepto-Bismol®), colloidal bismuth subcitrate (CBS, De-Nol®) and bismuth citrate (RBC, Tritec® or Pylorid®) are wellestablished antimicrobial compounds for the treatment of various microbial infections, such as syphilis, colitis, wound infection, quartan malaria, dyspepsia, diarrhea, and peptic ulcers (Figure 1, top). [1,2] More recent drugs include bismuth tribromophenolate (Xeroform®) [6] and a complex of bismuth with d-polygalacturonic acid ("colloidal bismuth pectin") that was approved for clinical use in China. [1] Even though it is a rather rare heavy metal, bismuth has a low cost.…”