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4BrABT (2-(4-Bromophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole) is a compound known for its interesting in vitro anticancer profile. 4BrABT inhibited proliferation and motility of several cancer cell lines in concentrations which were not toxic to normal cells. A major problem associated with cancer chemotherapy, but also caused by environmental factors such as pesticides, is neurotoxicity. Therefore, the aim of the presented study was an in vitro evaluation of the neuroprotective activity of this compound. 4BrABT activity (1-100 μM) was tested in cultures of mouse neurons, rat astrocytes and rat oligodendrocytes. A possible protective action of the compound in different neurodegenerative models, as serum deprivation (SD), excitotoxicity (presence of 500 μM glutamate in culture medium), as well as cisplatin toxicity (astroglia--50 μM and oligodendroglia--100 μM) was investigated. Cell viability in the tested cultures was assessed with the use of LDH and MTT methods. Moreover, 4BrABT ability to prevent the cisplatin-induced apoptosis in astrocyte and oligodendrocyte cultures was analysed after Hoechst 33342 fluorostaining. The obtained results indicate that 4BrABT was not toxic to neurons, astrocytes and oligodendrocytes. Moreover, a decrease in the neuronal LDH level was observed, which may suggest the ability of 4BrABT to act as a trophic agent. Furthermore, the protective action of the studied compound was shown in neuronal cultures exposed to neurotoxic conditions (presence of glutamate and trophic stress) and in cisplatin-treated astrocytes and oligodendrocytes. The expression of anticancer and neuroprotective activity raises hopes for the potential use of 4BrABT as a safe anticancer drug, or neuroprotective agent in chemotherapy-associated neurotoxicity.

Aim: Surgical procedures using synthetic implants are currently considered as the most efficient therapy for stress urinary incontinence (SUI) and pelvic organ prolapse (POP). Insertion of the tape or mesh causes enhanced collagen synthesis that largely affects the biomechanical property of the implant. This process is significantly modulated by estrogens and improper wound healing and treatment failure may result in hypoestrogenism. The aim of the study was to assess the rate of collagen type II synthesis by pubocervical fascia fibroblasts cultured with polypropylene meshes in the presence of estrogens and tamoxifen., Material and Methods: Fibroblasts were obtained from pubo-cervical fascia sampled from a 52-year-old premenopausal woman who underwent surgical treatment for SUI and cultured with monofilament or multifilament polypropylene meshes in the presence of 17B-estradiol, estriol, daidzein or tamoxifen. The cultures were run for 216 hr and the media were replaced every 72hr N-terminal propeptide of type III procollagen (PIIINP) was used as a marker of collagen type III synthesis. Its concentration in the media was measured by radioimmunoassay Pubocervical fascia fibroblast cultured with monofilament or multifilament meshes are capable of collagen type III synthesis. Following treatment with estradiol or tamoxifen, the highest PIIINP concentrations were observed after 72 hr whereas in case of estriol, daidzein or no treatment after 144hr of culture, regardless of the type of mesh used., Results: Only in cultures containing monofilament mesh and stimulated with estriol the high rate of collagen type III synthesis persisted until the end of the experiment. Paradoxically the highest total production of PIIINP was observed in culture treated with tamoxifen, both for multifilament and monofilament meshes., Conclusion: The rate of collagen type III synthesis by pubocervical fascia fibroblast cultured with polypropylene meshes is subjected to modulation by estrogens and antiestrogens.

Two 2-(monohalogenophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles were synthesized by reaction of sulfinyl bis(2,4-dihydroxythiobenzoyl) with 4-substituted 3-thiosemicarbazides and evaluated for their antiproliferative activity in tumor cells and for cytotoxicity in normal cells. Both derivatives in micromolar concentrations elicited a prominent antiproliferative effect in tumor cells derived from cancers of the nervous system (rhabdomyosarcoma/medulloblastoma, glioma) and peripheral cancers, including breast adenocarcinoma and lung carcinoma. The anticancer effect was attributed to decreased DNA synthesis and was not connected with apoptosis induction. Both compounds were not toxic to normal human skin fibroblasts.