Organotin Implications in Anticarcinogenesis. Effects of Several Organotins on Tumour Growth Rate in Mice

Cardarelli, Nate F.; Cardarelli, B M; Libby, Eugene P; Dobbins, Emmy

doi:10.1038/icb.1984.21

Cited by 24 publications

(5 citation statements)

References 3 publications

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“…Melasoprol is the only drug that can cure Rhodesian and Gambian sleeping sicknesses both during early and late stages and low doses of arsenic trioxide and melasoprol are reported to reduce the viability and induce death in myeloma cell lines and in acute promyelocytic leukemia (Soignet et al 1998;Rousselot et al 1999). This dual therapeutic ability of organometallics is consistent with our present results and those of others (Cardarelli et al 1984;Crowe et al 1984;Nok et al 1992;Susperregui et al 1999;Shuaibu et al 2000;Bonire and Fricker. 2001;Ronconi et al 2002).…”

Section: Discussionsupporting

confidence: 95%

In vitro trypanocidal activity of dibutyltin dichloride and its fatty acid derivatives

Shuaibu

Kanbara

Yanagi

et al. 2003

Parasitology Research

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Searching for new compounds against pathogenic trypanosomes has been substantially accelerated by the development of in vitro screening assays. In an attempt to explore the chemotherapeutic potential of organotin compounds and to broaden the search for newer trypanocides, fatty acid derivatives of dibutyltin dichloride were synthesized and their in vitro trypanocidal profiles studied on Trypanosoma brucei brucei, Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense. A 24-h time course experiment was conducted with various concentrations of the compounds using a 24-well microtiter plate technique. The compounds tested were trypanocidal in a dose-dependent fashion: inhibiting survival and growth, resulting in irreversible morphological deformation and the eventual death of the parasites. The minimum inhibitory concentrations of the tested diorganotins are at low micromolar ranges: from 0.15-0.75 microM for T. b. brucei, T. b. gambiense and T. b. rhodesiense. These observations suggest that organotin has chemotherapeutic potential.

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Section: Discussionsupporting

confidence: 95%

In vitro trypanocidal activity of dibutyltin dichloride and its fatty acid derivatives

Shuaibu

Kanbara

Yanagi

et al. 2003

Parasitology Research

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“…14,15,19 Compounds with a Sn-O linkage have been shown to have better activity than compounds that have tin(IV) connected to sulfur. 20,21 For tri-n-alkyltin(IV) acetates, the methyl organotin(IV) compounds are the most active in insects and mammals while the propyl and butyl compounds are the most active in fungi and certain bacteria. Activity decreases as the number of alkyl groups decreases as follows R 4 Sn >R 3 Sn > R 2 Sn > RSn > Sn all for tin(IV) compounds with the anionic X group exerting little influence on activity.…”

Section: Biological Activitiesmentioning

confidence: 99%

Synthesis and Biological Activities of Organotin (IV) Carboxylates: A Review

Hadi¹,

Jawad²,

Ahmed³

et al. 2018

SRP

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Organotin(IV) compounds have gained significant interest in both the chemical and pharmaceutical industry. Tin (IV) form stable complexes with a unique structure and physicochemical properties that are used in organic synthesis as heat stabilizers and catalysts, in drug development as biologically active agents and in other areas. This review concentrates on recent progress in the classical and convenient synthesis procedure and biological activities as antitumoral and antimicrobial agents.

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“…Organotins (R y SnX 4-y ) are compounds that possess direct tin-carbon covalent bond(s) that are responsible for their various toxicological/biological properties. Of the four classes of these compounds, diorganotins (IV) [R 2 SnX 2 ] (R=hydrocarbon group; X=halogen or other anionic organic compounds) are the largest group of organotins studied for antitumor activity, and 50% of these compounds show reproducible activity against various kinds of tumor (Cardarelli et al 1984;Crowe et al 1984; Bara et al 1991;Ronconi et al 2002). They are also reported to have trypanocidal activity (Nok et al 1992;Susperregui et al 1999;Shuaibu et al 2000Shuaibu et al , 2003.…”

Section: Introductionmentioning

confidence: 96%

Effect of dibutyltin(IV) on the ultrastructure of African Trypanosoma spp.

Shuaibu

Kanbara

Yanagi

et al. 2004

Parasitology Research

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Diorganotins (R2SnX2) are compounds with a wide variety of biological properties. In an attempt to follow the morphological events and to characterize the toxic effects of diorganotins on in vitro cultured African Trypanosoma spp., the ultrastructural alterations induced on the parasites by dibutyltins (Bu2SnX2) were followed. The data obtained indicate that these compounds induced irreparable damage to the in vitro cultured bloodstream forms of the parasites. Transmission and scanning electron microscopy allowed observations on the perturbation of the kinetoplast, extensive cytoplasmic swellings, disconfiguration around the flagellar pocket and membrane disintegration. Fluorescence microscopy with 4,6-diamidine-2-phenylindole stain was also used to visualize the survival or degeneration of kDNA. Understanding the collateral cellular toxic effect of these compounds on the parasites may shed light on the possible mechanism by which they kill trypanosomes. Agarose gel electrophoresis resolution of isolated kDNAs revealed no fragmentation by these compounds following in vitro incubation at 37 degrees C. However, fragmentation was observed from the gel electrophoresis of kDNA isolated from in vitro cultured Bu2SnX2-exposed parasites. Transmission electron microscopy of the kDNAs revealed the same pattern as observed with gel electrophoresis. These results provide evidence for the possible involvement of the Bu2Sn moiety in the in vivo-induced fragmentation of trypanosomal kDNA and consequent trypanolysis. This observation also underlies the relevance of organometallics in the therapy of African trypanosomiasis.

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Organotin Implications in Anticarcinogenesis. Effects of Several Organotins on Tumour Growth Rate in Mice

Cited by 24 publications

References 3 publications

In vitro trypanocidal activity of dibutyltin dichloride and its fatty acid derivatives

In vitro trypanocidal activity of dibutyltin dichloride and its fatty acid derivatives

Synthesis and Biological Activities of Organotin (IV) Carboxylates: A Review

Effect of dibutyltin(IV) on the ultrastructure of African Trypanosoma spp.

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