Do antidiabetic drugs prevent the transformation of Acanthamoeba trophozoite into cyst form?

This study examines the effects of three different drugs with metformin, acarbose and pioglitazone active ingredients used for antidiabetic purposes on Acanthamoeba cysts and trophozoites. Cultures of A. castellanii trophozoites and cysts were prepared to test the anti-amoebic activity of metformin, acarbose and pioglitazone. Cultures were then prepared for A. castellanii cyst and trophozoite forms and parasites were exposed to different concentrations (0.750 mg/mL, 0.375 mg/mL, 0.186 mg/mL and 0.093 mg/mL) of metformin, acarbose and pioglitazone. As a result of the study, the reproductive potential suppressive effects and conversion from trophozoite form to cyst form of all three substances on A. castellanii trophozoites and cysts were determined. Parasites were counted at 12, 24 and 48 hours in the cell counter after staining with trypan blue. In comparison of the effects of metformin, acarbose and pioglitazone used in the study on A. castellanii trophozoites and cysts, it was observed that all three substances were statistically effective against cysts and trophozoites at a concentration of 0.750 mg/mL. Furthermore, it was determined that all concentrations of the three active substances included in the study significantly decreased the rate of cyst formation even at the end of the 7th day. In this context, it was determined that all three substances have amebicidal effects, and they significantly inhibit the transformation of A. castellanii trophozoites to cyst form. It is thought that these active substances, which are currently used as anti-diabetic, can be used in combination with other drugs in A. castellanii infections based on our study findings.

Amoebicidal activity of benzothiazole on Acanthamoeba castellanii cysts and trophozoites and its cytotoxic potentials.

Acanthamoeba spp. are free-living amoebae isolated from many ecological areas such as swimming pools, dams and lakes, and soil. Granulomatous amebic encephalitis and amebic keratitis, caused by Acanthamoeba spp., usually occurs in chronically ill, debilitated individuals, in immunosuppressed patients and treatment is quite difficult. This study aimed to determine the effect of benzothiazole on trophozoite and cyst forms of Acanthamoeba castellanii (A.castellanii). Axenic cultures of A. castellanii trophozoites and cysts were prepared to test the amoebicidal activity of benzothiazole. The concentrations of benzothiazole in 24-well plates were prepared as 0.08%, 0.04%, 0.02%, 0.01%, 0.005%, and A. castellanii cysts and trophozoites were added to these cultures. Parasites were counted at 0, ½, 1, 3, 6, 12, 24 and 48 h in the cell counter after staining with trypan blue. Cytotoxicity of benzothiazole on the WI-38 human fibroblast cell line was also tested. Between 0.08% and 0.01% concentrations of benzothiazole showed a strong amoebicidal activity at 24 and 48 h. A significant decrease in 0.005% concentration in the number of live trophozoites and cysts was detected between 6 and 48 h. As a result of the cytotoxicity studies, benzothiazole did not show any cytotoxic effect on the WI-38 human fibroblast cell line even at 1% concentration. Benzothiazole could be concluded as a new therapeutic agent against Acanthamoeba. On the other hand, in vivo studies are needed to confirm the efficacy of the biological effect.

Comparison of the Effects of Contractubex Gel and Benzothiazole After Topical Application in an Experimental Model of Epidural Fibrosis in Rats.

BACKGROUND: Postoperative epidural adhesion is a frequent cause of failed back surgery syndrome, manifesting with back and leg pain or neurologic deficits. Development of preventive measures for epidural adhesion after laminectomy is critical to improve outcomes of lumbar surgery. We hypothesized that positive effects of topical application of Contractubex (CTX) gel and benzothiazole (BT) individually and in combination could aid in preventing epidural fibrosis in a rat laminectomy model. METHODS: Rats were randomly assigned to 2 control and 5 experimental groups (n = 8 for each group). The control(-) group received no surgery, whereas the control(+) group underwent laminectomy without any drug administration. In experimental groups, study agents applied to dura mater after laminectomy were 100mgCTX, 2.5%BT, 5%BT; 100mgCTXplus2.5%BT, and 100mgCTXplus5%BT. Laminectomy was performed at the L3 level for all rats. The extent of epidural fibrosis was assessed 4 weeks later macroscopically and histopathologically. Hepatic and renal toxicity of study drugs was assessed histopathologically. RESULTS: Topical CTX and BT individually and in combination reduced epidural fibrosis after laminectomy in rats. Although a meaningful decrease of epidural fibrosis with individual application of CTX and BT (2.5% or 5%) was obtained (P < 0.05), the effect of their combination was more pronounced without meaningful hepatic and renal toxicity (P < 0.05). CONCLUSIONS: Combined use of topical CTX and BT could be a potential therapy for epidural fibrosis. Further research with this agents for the prevention of epidural fibrosis is warranted.

The Effects of Erzincan Grape (Vitis vinifera spp., Cimin) and Benzothiazol on a Caenorhabditis elegans Organism Model.

BACKGROUND: Grapes and their products are known to have been used for the treatment of diseases throughout history. OBJECTIVE: It was aimed to investigate the effects of Erzincan Cimin grapes on an organism model of Caenorhabditis elegans N2 wild type and C. elegans BS913 strains with gonad cancer. MATERIALS AND METHODS: The effects of methanol extracts of the skin and seeds of Erzincan Cimin grapes were examined separately on C. elegans N2 wild type and an effect was determined on lifespan. By applying GS-MS analysis, a potential agent substance was determined in the skin and seed methanol extracts. This substance was purchased and the effects of this substance were investigated on lifespan and fertility in C. elegans BS913 strains with gonad cancer. In addition, the effects on young subjects exposed to this agent substance in L1 form were investigated. RESULTS: Grape seed and skin methanol extract was observed to prolong the lifespan most at a dose of 10 mg/100 mL. Lifespan was determined to be at a maximum in a gonad cancer organism model with benzothiazol at a dose of 50 ppm. At the same dose, positive effects were determined on the fertility of strains with cancer. When the effects of benzothiazol were examined on young L1 forms, an evident retardation of growth was determined at doses of 10, 50, and 100 ppm. CONCLUSION: Owing to anti-carcinogenic effects of benzothiazol and benzothiazol-derived substances, they can be considered as agent substances in academic studies related to cancer. SUMMARY: The effects of methanol extracts of the skin and seeds of Erzincan Cimin grapes were examined on C. elegans N2 wild type and an effect was determined on lifespanThrough GS-MS analysis, benzothiazol was determined in the skin methanol extractsBenzothiazol was purchased and the effects of this substance were investigated on lifespan and fertility in C. elegans BS913 strains with gonad cancerThe effects on young subjects exposed to benzothiazol in L1 formGrape seed, skin methanol extract, and benzothiazol was observed to prolong the lifespanPositive effects were determined on the fertility of gonad cancer strains. Abbreviations used: GC-MS: gas chromatography and mass spectrometry; C. elegans: Caenorhabditis elegans; NGM: Nematode growth medium; E. coli: Escherichia coli; FUDR: Fluorodeoxyuridine; LDL: Low-density lipoprotein.