Cytotoxicity of Sanguinarine Chloride to Cultured Human Cells from Oral Tissue

Abstract

The in vitro cytotoxicity of sanguinarine chloride, a dental product used in the treatment of gingivitis and plaque, was compared using cell lines and primary cells from oral human tissues. For the established cell lines, sanguinarine chloride exhibited similar potencies to S-G gingival epithelial cells and to KB carcinoma cells, whereas HGF-1 gingival fibroblasts were more tolerant. However, a gingival primary cell culture was more sensitive to sanguinarine chloride than were the established cell lines. Detailed studies were performed with the S-G cells. The 24-hr midpoint (NR50) cytotoxicity value towards the S-G cells was 7.6 microM, based on the neutral red cytotoxicity assay; vacuolization and multinucleation were noted. When exposed to sanguinarine chloride for 3 days, a lag in growth kinetics was first observed at 1.7 microM. Damage to the integrity of the plasma membrane was evident, as leakage of lactic acid dehydrogenase occurred during a 3 hr exposure to sanguinarine chloride at 0.1275 mM and greater. The cytotoxicity of sanguinarine chloride to the S-G cells was lessened in the presence of an S9 hepatic microsomal fraction from Aroclor-induced rats or by including fetal bovine serum (15%) in the exposure medium. Progressively increasing the pH from 6.0 to 7.8 enhanced the potency of sanguinarine chloride, presumably due to the enhanced uptake of the lipophilic alkanolamine form, as compared to that of the cationic iminium form.

Molecular aspects on the interaction of protoberberine, benzophenanthridine, and aristolochia group of alkaloids with nucleic acid structures and biological perspectives

“…245 The in vitro study of cytotoxicity of sanguinarine using cell lines and primary cells from oral human tissues established the potential use of sanguinarine for the inhibition of growth of S-G gingival epithelial cells and KB carcinoma cells, and correlated with its complex formation with DNA. 247 The iminium ion of sanguinarine has been shown to be responsible for the antimicrotubule property through the formation of a pseudobase with sulfhydroxyl groups in tublin. 250 Sanguinarine, on the otherhand, has been identified as the principle constituent responsible for argemone oil toxicity causing epidemic dropsy syndrome.…”

Thermodynamic profiles of the DNA binding of benzophenanthridines sanguinarine and ethidium: A comparative study with sequence specific polynucleotides

“…Sanguinarine has potential anti-tumoral and antiinflammatory properties [21][22][23]. Dental products containing sanguinarine is in use for the treatment of gingivitis and periodontitis [24][25][26][27][28]. Ethidium (figure 1b), on the other hand, has been a universal fluorescent probe and DNA staining agent developed as an anti-trypanosmal agent [29][30][31].…”

Biophysical aspects and biological implications of the interaction of benzophenanthridine alkaloids with DNA

“…The in vitro cytotoxicity of sanguinarine was studied using cell lines and primary cells from oral human tissues (Babich et al 1996). The results established the potential use of sanguinarine for the inhibition of growth of SG gingival epithelial cells and KB carcinoma cells due to its complex formation with DNA.…”