Comparison of the Ames assay and the induction of sister chromatid exchanges: Results with ten pharmaceuticals and five selected agents

Shubber, E. K.; Jacobson‐Kram, David; Williams, Jerry R.

doi:10.1007/bf00121853

Cited by 17 publications

(6 citation statements)

References 37 publications

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“…In contrast, MQ was not mutagenic in the same study, but it could be tested only to 2.5 lg/ml owing to its great toxicity [Schüpbach, 1979]. Weak-to-moderate bacterial mutagenicity of CQ has been confirmed in other studies [Shubber et al, 1986;Thomas et al, 1987;Chatterjee et al, 1998;Riccio et al, 2001], and there is a mixture of modestly positive, equivocal, and negative results in eukaryotic systems, compatible with CQ being a weak mutagen and clastogen [O'Donovan, 1984;Xamena et al, 1985;Shubber et al, 1986;Chatterjee et al, 1998;Riccio et al, 2001;Roy et al, 2008]. Although there are few published genotoxicity studies of MQ, in vivo cytogenetic testing and carcinogenicity tests in mice and rats are reportedly negative [Grisolia and Takahashi, 1994;Snyder and Green, 2001].…”

Section: Discussionmentioning

confidence: 82%

Potentiation of the mutagenicity and recombinagenicity of bleomycin in yeast by unconventional intercalating agents

Hoffmann

Laterza

Sylvia

et al. 2011

Environ and Mol Mutagen

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Interactions between bleomycin (BLM) and conventional or unconventional intercalating agents were analyzed in an assay for mitotic gene conversion at the trp5 locus and reversion of the ilv1-92 allele in Saccharomyces cerevisiae strain D7. BLM is a potent recombinagen and mutagen in the assay. Various chemicals modulate the genetic activity of BLM, producing either antimutagenic effects or enhanced genotoxicity. Effects of cationic amino compounds include enhancement of BLM activity by aminoacridines and protection against BLM by aliphatic amines. The potentiation of BLM is similar to findings in a micronucleus-based BLM amplification assay in Chinese hamster V79 cells. In this study, the amplification of BLM activity was explored in yeast using known intercalators, compounds structurally related to known intercalators, and unconventional intercalators that were identified on the basis of computer modeling or results in the Chinese hamster BLM amplification assay. As shown in previous studies, the classical intercalator 9-aminoacridine (9AA) caused dose-dependent enhancement of BLM activity. Other compounds found to enhance the induction of mitotic recombination and point mutations in strain D7 were chlorpromazine, chloroquine, mefloquine, tamoxifen, diphenhydramine, benzophenone, and 3-hydroxybenzophenone. The increased activity was detectable by cotreatment of yeast with BLM and the modulator compound in growth medium or by separate interaction of the intercalator with DNA followed by BLM treatment of nongrowing cells in buffer. The data support the interpretation drawn from micronucleus assays in mammalian cells that BLM enhancement results from DNA intercalation and may be useful in detecting noncovalent interactions with DNA. Environ.

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Section: Discussionmentioning

confidence: 82%

Potentiation of the mutagenicity and recombinagenicity of bleomycin in yeast by unconventional intercalating agents

Hoffmann

Laterza

Sylvia

et al. 2011

Environ and Mol Mutagen

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“…For background to and the biological activity of acridine derivatives, see: Shubber et al (1986); Sondhi et al (2006); Salamanca & Khalil (2005). For related structures, see: Aghabozorg et al (2010); Mei & Wolf (2004).…”

Section: Related Literaturementioning

confidence: 99%

“…9-Aminoacridine (9-AA) and its derivatives present a very interesting object of research. This group of compounds exhibits a wide spectrum of biological activities: antibacterial, mutagenic, antitumor and antiinflammatory (Shubber et al, 1986;Sondhi et al, 2006;Salamanca & Khalil, 2005) In the viewpoint of crystal engineering, acridine and its 9amino derivative are very interesting because of their capability for hydrogen bonding via N atom of the ring and π-π stacking since they possess three rings (Aghabozorg et al, 2010;Mei & Wolf, 2004). In order to study potential hydrogen bonding interactions the crystal structure determination of the title compound (I) was carried out.…”

Section: S1 Commentmentioning

confidence: 99%

9-Aminoacridin-10-ium 4-aminobenzoate dihydrate

Dhanabalan¹,

Thanigaimani

Arshad

et al. 2014

Acta Cryst E

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The asymmetric unit of the title hydrated salt, C13H11N2 +·C7H6NO2 −·2H2O, consists of two independent 9-aminoacridinium cations, two 4-aminobenzoate anions and four water molecules. Both 9-aminoacridinium cations are essentially planar, with maximum deviations of 0.034 (1) and 0.025 (2) Å, and are protonated at the pyridine N atoms. The 4-aminobenzoate anions are approximately planar, with dihedral angles of 9.16 (19) and 5.4 (2)° between the benzene ring and the carboxylate group. In the crystal, the two independent anions are connected by N—H⋯O hydrogen bonds, forming a layer parallel to (100). The layers are connected through the cations by N—H⋯N and N—H⋯O hydrogen bonds. The water molecules, which form O—H⋯O hydrogen-bonded chains along the b-axis direction, connect the anions and the cations by O—H⋯O, N—H⋯O and C—H⋯O hydrogen bonds. The crystal structure also features π–π interactions [centroid–centroid distances = 3.6343 (9)–3.8366 (10) Å] and a C—H⋯π interaction.

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“…Nonetheless, the toxicological database on PQ is incomplete. PQ produced a weak to moderate positive response in genotoxicity assays including the Salmonella/microsome assay (Ames test) [20][21][22][23]. Notwithstanding the evidence of genotoxicity, no long-term carcinogenicity study was conducted nor were PQ effects on reproductive performance, fertility, and postnatal neurobehavioral development investigated.…”

Section: Discussionmentioning

confidence: 99%

Transplacental Transfer of Primaquine and Neurobehavioral Development of Prenatally Exposed Rats

Becker

Rosa

Fernandes

et al. 2021

Journal of Toxicology

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Primaquine (PQ) not only eliminates P. falciparum gametocytes but also kills liver dormant forms of P. vivax and P. ovale. Owing to these unique therapeutic properties, it is an essential drug. Although PQ has been used for over 70 years, its toxicological database has gaps such as the absence of studies on its reproductive and developmental toxicity and kinetics in pregnancy. This study investigated the transplacental transfer of PQ and the effects of intrauterine exposure on the postnatal growth, survival, and neurobehavioral development of the offspring. PQ kinetics and transplacental transfer were investigated in rats treated orally (40 mg.kg·bw−1) on gestation day (GD) 21. PQ was analyzed by high-performance liquid chromatography with diode array ultraviolet detection. To evaluate effects of intrauterine exposure on postnatal development, dams were treated orally with PQ (20 mg.kg·bw−1·d−1) or water (controls) on GD 0–21. Postnatal survival, body weight gain, somatic maturation, and reflex acquisition were evaluated. The open field test (OF) was conducted on PND 25. PQ concentration in the fetal plasma was nearly half that in maternal plasma. Except for increase in pregnancy loss, no effects of PQ were noted at term pregnancy and first days of life. Prenatal PQ did not affect postnatal weight gain nor did it impair somatic and neurologic development of the offspring. Pups born to PQ-treated dams showed reduced exploration and enhanced emotionality in the OF. PQ given in pregnancy, at doses greater than those recommended for malaria therapy, may affect pup postnatal survival and emotional behavior.

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Comparison of the Ames assay and the induction of sister chromatid exchanges: Results with ten pharmaceuticals and five selected agents

Cited by 17 publications

References 37 publications

Potentiation of the mutagenicity and recombinagenicity of bleomycin in yeast by unconventional intercalating agents

Potentiation of the mutagenicity and recombinagenicity of bleomycin in yeast by unconventional intercalating agents

9-Aminoacridin-10-ium 4-aminobenzoate dihydrate

Transplacental Transfer of Primaquine and Neurobehavioral Development of Prenatally Exposed Rats

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