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Toxins 2018, 10(8), 323;

Bouganin, an Attractive Weapon for Immunotoxins

Department of Experimental, Diagnostic and Specialty Medicine-DIMES, General Pathology Section, Alma Mater Studiorum—University of Bologna, Via S. Giacomo 14, 40126 Bologna, Italy
Author to whom correspondence should be addressed.
Received: 18 July 2018 / Revised: 27 July 2018 / Accepted: 2 August 2018 / Published: 8 August 2018
(This article belongs to the Special Issue Venom and Toxin as Targeted Therapy)
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Bougainvillea (Bougainvillea spectabilis Willd.) is a plant widely used in folk medicine and many extracts from different tissues of this plant have been employed against several pathologies. The observation that leaf extracts of Bougainvillea possess antiviral properties led to the purification and characterization of a protein, named bouganin, which exhibits typical characteristics of type 1 ribosome-inactivating proteins (RIPs). Beyond that, bouganin has some peculiarities, such as a higher activity on DNA with respect to ribosomal RNA, low systemic toxicity, and immunological properties quite different than other RIPs. The sequencing of bouganin and the knowledge of its three-dimensional structure allowed to obtain a not immunogenic mutant of bouganin. These features make bouganin a very attractive tool as a component of immunotoxins (ITs), chimeric proteins obtained by linking a toxin to a carrier molecule. Bouganin-containing ITs showed very promising results in the experimental treatment of both hematological and solid tumors, and one bouganin-containing IT has entered Phase I clinical trial. In this review, we summarize the milestones of the research on bouganin such as bouganin chemico-physical characteristics, the structural properties and de-immunization studies. In addition, the in vitro and in vivo results obtained with bouganin-containing ITs are summarized. View Full-Text
Keywords: antiviral activity; Bougainvillea; bouganin; cancer therapy; immunotherapy; immunotoxins; ribosome-inactivating proteins; rRNA N-glycosylase activity; VB6-845 antiviral activity; Bougainvillea; bouganin; cancer therapy; immunotherapy; immunotoxins; ribosome-inactivating proteins; rRNA N-glycosylase activity; VB6-845

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Bortolotti, M.; Bolognesi, A.; Polito, L. Bouganin, an Attractive Weapon for Immunotoxins. Toxins 2018, 10, 323.

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