Methods of Isolation of Active Substances from Garlic (Allium sativum L.) and Its Impact on the Composition and Biological Properties of Garlic Extracts.

Garlic (Allium sativum L.) is widely used in the human diet and in scientific research due to its biological properties. Various factors, e.g., temperature, pressure, extraction method, type of solvent, size, and territorial origin of garlic, affect the amount and type of bioactive compounds obtained from garlic extracts. In turn, the content of bioactive compounds correlates with the biological activity of the extracts. Therefore, the aim of this review was to summarize the current state of knowledge of the methods and effectiveness of isolation of active substances from garlic and their impact on the garlic extract composition and, consequently, biological properties. According to the literature, extracts obtained using water as a solvent are mainly responsible for antimicrobial properties, which is related to, inter alia, the high content of allicin. The use of alcohols, such as methanol or ethanol, is associated with the outstanding antioxidant power of extracts resulting from the presence of phenolic compounds. In turn, due to the presence of diallyl disulfide and disulfide trisulfide, garlic oil has anticancer potential. Acetone is the most effective organic solvent; however, it is not suitable for immediate consumption.

Characterisation of Biologically Active Hydrolysates and Peptide Fractions of Vacuum Packaging String Bean (Phaseolus vulgaris L.).

The aim of the study is to characterise biologically active hydolysates and peptide fractions obtained from vacuum-packed string beans (Phaseolus vulragis L.) (PB). Unpacked beans were a control sample. The influence on human squamous carcinoma cell line SCC-15 (ATCC CRL-1623) was determined. Packed bean (PB) and unpacked bean (UB) extracts were found to exert no effect on the tongue squamous carcinoma cells. The results of the study indicated that the packing process contributed to the retention of protein, soluble dietary fibre, and free sugar (2.36, 3.5, and 1.79 g/100 d.m., respectively). PB was characterised by higher antioxidant activity (expressed as neutralisation of 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS ABTS•+) and 2,2-diphenyl-1-picrylhydrazyl (DPPH·) free radicals) as well as Fe2+ chelation and reducing power (IC50 = 54.56, 0.46, 3.85 mg mL-1; 0.088 A700/peptide content, respectively) than the UB samples before hydrolysis. The hydrolysis process enhanced these properties. The IC50 value of lipase and α-amylase inhibitory activity of the hydrolysates obtained from UB was reduced. The PB and UB fractions exhibited a certain level of antimicrobial activity against S. aureus and E. coli. Candida albicans were not sensitive to these peptide fractions.

Cytotoxic effects of two extracts from garlic (Allium sativum L.) cultivars on the human squamous carcinoma cell line SCC-15.

Garlic (Allium sativum L., Alliaceae) has acquired a reputation as a therapeutic agent and herbal remedy to prevent and treat several pathologies. The aim of the present study was to determine the effect of two Allium sativum L. cultivars, Harnas and Morado, on reactive oxygen species (ROS) production, viability and apoptotic process in human squamous carcinoma cell line SCC-15. The experiments were conducted on SCC-15 cell line exposed to increasing concentrations of garlic extracts of 0.062, 0.125, 0.250, 0.500 and 1.000 mg/mL. After the experiments, ROS formation, caspase-3 activity and neutral red uptake were measured in the cells, and in a collected medium lactate dehydrogenase (LDH) release was measured. The Spanish cultivar Morado has demonstrated higher potential to stimulate ROS production in SCC-15 cells after a short time period (6 h) than the Polish cultivar Harnas. However, the Polish cultivar Harnas manifested more prolonged potential to stimulate ROS production in SCC-15 cells. Both studied garlic extracts induced cytotoxicity on SCC-15 cell line which was probably ROS-dependent. We also determined that in SCC-15 cells high concentrations of studied extracts did not cause activation of caspase-3 which suggested caspase-independent or necrotic cell death.

Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma (PPARγ).

Peroxisome proliferator-activated receptors (PPARs) play an important role in numerous chronic diseases such as diabetes, obesity, atherosclerosis and cancer, and PPAR modulators are among the approved drugs and drug-candidates for their treatment. The aim of this study was to elucidate the involvement of PPARs in the mechanism of cytotoxic and pro-apoptotic action of novel anticancer 4-thiazolidinone derivatives (Les-2194, Les-3377, Les-3640) and approved 4-thiazolidinones (Rosiglitazone, Pioglitazone) towards the human squamous carcinoma (SCC-15) cell line. Experiments with 4-thiazaolidinone derivatives and PPAR-specific siRNA were conducted and PPARα, PPARß and PPARγ mRNA expression was studied. Moreover, after PPARα, PPARß and PPARγ siRNA gene silencing, cell viability, cell metabolism and caspase-3 activity were measured. The results showed a decrease of mRNA expression of the studied PPARs in SCC-15 cells treated with 10 and 50 µM Les-2194, Les-3377 and Les-3640. PPARγ knockdown protected the cells from the cytotoxic effect of the tested compounds (50 µM). It was established that novel anticancer 4-thiazolidinone derivatives act mainly through the PPARγ pathway in SCC-15 cells. Our results suggest that all studied compounds act as PPARs agonists. Interestingly, silencing of PPARγ gene increases the expression of PPARα, PPARß mRNA in SCC-15 cells. The anticancer potential of new studied compounds was more expressed as compared to Rosiglitazone and Pioglitazone.

Study of novel anticancer 4-thiazolidinone derivatives.

4-Thiazolidinones are a known class of prospective drug-like molecules, especially in the design of new anticancer agents. Two of the most prominent subtypes of these compounds are 5-ene-2-amino(amino)-4-thiazolidinones and thiopyrano[2,3-d]thiazoles. The latter are considered to be cyclic mimetics of biologically active 5-ene-4-thiazolidinones with similar pharmacological profiles. Therefore, the aim of this study was to evaluate the impact of 4-thiazolidinone-based compounds on cytotoxicity, the apoptotic process, and metabolism in the human squamous carcinoma (SCC-15) cell line. The SCC-15 cells were cultured in phenol red-free DMEM/F12 medium supplemented with 10% FBS, hydrocortisone, and exposed to rising concentrations (1 nM-100 µM) of the studied compounds for 6, 24 and 48 h. Afterwards, reactive oxygen species (ROS) formation, cell viability, caspase-3 activity, and cell metabolism were measured. The obtained results showed that all of the studied compounds in a wide range of concentrations (1 nM-100 µM) increased DCF fluorescence which suggests a stimulation of ROS production. Nevertheless, these new compounds showed cytotoxic and proapoptotic properties only at high (10-100 µM) concentrations. Our studies are the first to be carried out on these compounds and require further investigation to clarify the mechanism of action of their anticancer potential.