phenylthiourea and Neoplasms

Genetically mediated sensitivity to the bitter taste of phenylthiocarbamide (PTC) and 6-n-propylthiouracil (Prop) has long been associated with enhanced sensitivity to other sweet and bitter compounds. New studies suggest that tasters and supertasters of Prop may also differ from notasters in their taste preferences and in their patterns of food rejection and food acceptance. One question is whether the acceptability of bitter-tasting vegetables is influenced by Prop taster status. Cruciferous vegetables are among the major dietary sources of potentially chemoprotective agents in cancer control, and their consumption is reported to alter cancer risk. Strategies aimed at dietary change in individuals or groups should consider the role of genetic taste markers and their potential influences on food preferences and dietary habits.

Topics: Alcoholism; Food Preferences; Genetic Markers; Humans; Neoplasms; Nutritional Physiological Phenomena; Phenylthiourea; Propylthiouracil; Risk Factors; Taste; Vegetables

New halogenated thiourea derivatives were synthesized via the reaction of substituted phenylisothiocyanates with aromatic amines. Their cytotoxic activity was examined in in vitro studies against solid tumors (SW480, SW620, PC3), a hematological malignance (K-562), and normal keratinocytes (HaCaT). Most of the compounds were more effective against SW480 (1a, 3a, 3b, 5j), K-562 (2b, 3a, 4a), or PC3 (5d) cells than cisplatin, with favorable selectivity. Their anticancer mechanisms were studied by Annexin V-fluorescein-5-isothiocyanate apoptosis, caspase-3/caspase-7 assessment, cell cycle analysis, interleukin-6 (IL-6) release inhibition, and reactive oxygen species (ROS) generation assay. Thioureas 1a, 2b, 3a, and 4a were the most potent activators of early apoptosis in K-562 cells, and substances 1a, 3b, 5j triggered late-apoptosis or necrosis in SW480 cells. This proapoptotic effect was proved by the significant increase of caspase-3/caspase-7 activation. Cell cycle analysis revealed that derivatives 1a, 3a, 5j increased the number of SW480 and K-562 cells in the sub-G1 and/or G0/G1 phases, and one evoked cycle arrest at the G2 phase. The most potent thioureas inhibited IL-6 cytokine secretion from PC3 cells and both colon cancer cell lines. Apoptosis-inducing compounds also increased ROS production in all tumor cell cultures, which may enhance their anticancer properties.

Topics: Antineoplastic Agents; Apoptosis; Caspase 3; Caspase 7; Cell Line, Tumor; Cell Proliferation; Interleukin-6; Neoplasms; Phenylthiourea; Reactive Oxygen Species; Structure-Activity Relationship

Topics: Adenoma; Carcinoma; Female; Gastrointestinal Neoplasms; Humans; Lung Neoplasms; Male; Neoplasms; Ovarian Neoplasms; Phenylthiourea; Prostatic Neoplasms; Taste; Uterine Neoplasms

Topics: Adolescent; Child; Diabetes Mellitus; Geriatrics; Italy; Neoplasms; Phenylthiourea; Research; Taste; Thiourea; Tuberculosis