Isothiocyanate Research Articles

AB0971 Chondroprotective effect of sulforaphane and PLGA-based delivery system

BackgroundSulforaphane [SFN; 1-isothiocyanato-4-(methylsulphinyl)-butane], a naturally occurring isothiocyanates (ITC) obtained through the consumption of broccoli, is one of the most potent inducers of the phase 2 enzymes implicated in carcinogen detoxification...

Expression of an apoptosis-regulating molecule BclGL and apoptosis in peripheral blood monoclear cells from patients with systemic lupus erythematosus

Objective To detect the expression of BclGL in peripheral blood mononuclear cells (PBMCs) from patients with systemic lupus erythematosus (SLE) and to investigate its significance.Methods Peripheral blood was obtained from 20 patients with active SLE (A-SLE),18 patients with inactive SLE (Ⅰ-SLE) and 30 healthy controls.Flow cytometry was performed to calculate the number of PBMCs,flow cytometry combined with annexin V-fluorescein isothiocyanate (FITC)/propidium iodide (PI) staining to determine the early apoptotic rates of PBMCs,fluorescence-based quantitative PCR and Western blot to measure the expression of BclGL mRNA and protein,respectively.The serum level of interferon (IFN)-α was determined by enzyme-linked immunosorbent assay (ELISA).Data were analyzed by using the software SPSS13.0.Mann-Whitney U-test or Kruskal-Wallis test was used for group comparisons.Pearson correlation coefficient test was applied to evaluate the relationship of BclGL expression with cell apoptotic rate and some clinical parameters.Results The number of PBMCs was significantly lower in patients with A-SLE than in those with Ⅰ-SLE and healthy controls ((0.16 ± 0.06) × 109/L vs.(0.27 ± 0.14) × 109/L and (0.34 ± 0.23) × 109/L,both P ＜ 0.01).Increased apoptotic rate of PBMCs was observed in patients with A-SLE compared with those with Ⅰ-SLE and healthy controls ((22.6 ± 1.1)％ vs.(16.4 ±0.9)％ and (10.1 ± 0.4)％,both P ＜ 0.01),and in patients with Ⅰ-SLE compared with the healthy controls (P ＜0.01).The mRNA and protein expressions of BclGL in PBMCs were both significantly higher in patients with ASLE than in those with Ⅰ-SLE and healthy controls (all P ＜ 0.01).A significant increase was observed in serum IFN-α level in the patients with SLE compared with the healthy controls ((32.5 ± 2.2) μg/L vs.(15.5 ± 1.3) μg/L,P ＜ 0.01).The mRNA expression of BclGL in PBMCs from patients with SLE was positively correlated with the apoptotic rate in PBMCs (r =0.486,P ＜ 0.01),SLE disease activity index score (r =0.496,P ＜ 0.01),titers of antinuclear antibodies (r =0.516,P ＜ 0.01) and serum IFN-o level (r =0.535,P ＜ 0.01),but was negatively correlated with complement C3 level (r =-0.515,P ＜ 0.01).Conclusions The increased expression of BclGL in PBMCs may contribute to the abnormal apoptosis in PBMCs,which in turn takes part in the pathogenesis of SLE. Key words: Lupus erythematosus,systemic; Peripheral blood mononuclear cells; BclGL; Apoptosis

Human metabolic fate of glucosinolates from kailan-hybrid broccoli. Differences between raw and microwaved consumption

Glucosinolates are sulphur-containing compounds present in Brassica species that are hydrolyzed by the plant enzyme myrosinase to isothiocyanates (ITC), which have previously reported chemopreventive properties. In vivo, ITC are metabolized and excreted in urine as mercapturic acids. A cross-over-design study of 7 subjects after ingestion of 200-g raw or microwaved kailan-hybrid broccoli was conducted. Total ITC equivalents in the vegetable, urine and blood samples were determined by HPLC as the cyclocondensation product of 1,2-benzenedithiol. The highest ITC metabolization (53.6±15.7% over the total ITC ingested) was observed during the first 4h after ingestion of raw product. However, the highest ITC metabolization after consumption of microwaved samples was delayed to 4–10h, with 23.2±27.6%. The high ITC metabolization during the first 4h was most likely due to absorption in the small intestine, while the second peak (4–8h) could be presumably attributed to an ITC absorption in the colon. The total ITC metabolization after raw kalian-hybrid consumption (79.1±18.8%) was approximately 2-fold higher than that from microwaved broccoli (41.3±8.8%), which was statistically significant (P, t test=0.005). The ITC absorption of the kailan-hybrid was 2 times higher for raw and 3–9 times higher for cooked samples than the values previously reported in the bibliography with conventional broccoli varieties. Compared to other brassicas, kailan-hybrid can be presented as a vegetable with both, a high concentration and a great ITC metabolization.

Rapid detection of the avian influenza virus H5N1 subtype in Egypt

Influenza A virus continue to cause widespread morbidity and mortality. The unprecedented spread of highly pathogenic avian influenza virus subtype H5N1 in Egypt is threatening poultry and public health systems. Effective diagnosis and control management are needed to control the disease. To this end, polyclonal antibodies (PAbs) were developed against the H5N1 avian influenza virus (AIV) and implemented an enzyme-linked immunosorbent assay (ELISA) to detect the H5 viral antigen. A group of rabbits was immunized with viral vaccine (H5N1) therefore, purifiedantibodies from rabbit serum, which secrete immunoglobulin G (IgG) was served as the detector antibody after conjugation with horse radish peroxidase and fluorescent isothiocyanate (FITC). The reactivity of the obtained peroxidase and fluorescent conjugated PAb of influenza virus revealed that they are specifically recognized H5N1 virus antigen. Specimens containing AIV subtypes collected from different Governments in Egypt yielded specific and strong signals with hemagglutination test. The detection limit of ELISA using the prepared peroxidae conjugated PAbs was 1:100000, while using fluorescent conjugated PAb was 1:10000. Reconstituted clinicalsamples consisting of H5 AIVs mixed with pharyngeal-tracheal mucus from healthy chickens also yielded positive signals in ELISA, and the results were confirmed using reference virus antigens. This investigation enhanced the usage of these PAbs in the surveillance and diagnosis of H5N1 AIV in Egypt. Key words: Avian influenza virus, H5N1, fluorescent antibody enzyme-linked immunosorbent assay (ELISA) technique, polyclonal antibodies.

Protective Role of (RS)-glucoraphanin Bioactivated with Myrosinase in an Experimental Model of Multiple Sclerosis

The discovery of new natural compounds with pharmacological properties is a field of interest widely growing. Recent literature shows that Brassica vegetables (Cruciferae) possess therapeutic effects particularly ascribed due to their content in glucosinolates, which upon myrosinase hydrolysis release the corresponding isothiocyanates. This study examines the potential neuroprotective and immunomodulatory effects of (RS )-glucoraphanin from Tuscan black kale (Brassica oleracea L. var. acephala sabellica) bioactivated with myrosinase (bioactive RS -GRA) (10 mg/kg/day intraperitoneally), in an experimental autoimmune encephalomyelitis (EAE), a model of multiple sclerosis. EAE was induced by immunization with myelin oligodendroglial glycoprotein peptide (MOG35-55 ) in mice. After immunization, mice were observed daily for signs of EAE and weight loss. Clinical score was evaluated using a standardized scoring system. By Western blot analysis of spinal cord tissues, we have demonstrated that treatment with bioactive RS -GRA significantly decreased nuclear factor (NF)-kB translocation, pro-inflammatory cytokine production such as interleukin-1β (IL-1β), and apoptosis (Bax and caspase 3 expression). Our results clearly demonstrate that bioactive RS -GRA treatment may represent a useful therapeutic perspective in the treatment of this disease.

ChemInform Abstract: Homoallenyl Azines in Criss‐Cross Cycloaddition Reactions.

AbstractOnly one diastereomer and regioisomer of type (III) or (VI) is obtained by intra‐intermolecular cycloadditions when (I) or (IV) are reacted with isocyanates or isothiocyanates as dipolarophiles.

Nematicidal potential of Brassicaceae

Brassicaceae Burnett (syn. Cruciferae A. L. de Jussieu) include many important economic plants used as edibile or ornamental. They are commonly known as the “mustard” plant family due to the sharp, potent flavour of their main metabolites, the glucosinolates (GLSs) which contain sulfur. Glucosinolates coexist in vivo with glycosylated thioglucosidases, myrosinase(s), responsible of their hydrolysis with the production of bioactive cognate isothiocyanates (ITC). GLSs and ITCs function as defence bioactive metabolites against plant pathogens, insects and herbivores. The present review paper focus on GLSs role as bionematicides. The current knowledge on the efficacy of these phytochemicals against the most common phytoparasitic nematodes affecting crops of agriculture importance such as tomato, potato and grapevine is reported. Data from our ongoing research on the in vitro biocidal activity of glucosinolate extracts, and their main components, against the virus-vector nematode Xiphinema index Thorne & Allen and the carrot cyst nematode Heterodera carotae Jones are also described.

Response surface optimization and identification of isothiocyanates produced from broccoli sprouts

Isothiocyanates (ITCs) are proved as one of natural anticarcinogenic compounds, which are produced from the decomposition of glucosinolates by myrosinase. The present study optimized the enzymolysis conditions (pH, addition of EDTA and ascorbic acid) for ITCs production from glucosinolates in broccoli sprouts using response surface methodology. ITCs production was clearly enhanced by a suitable pH, addition content of EDTA and ascorbic acid. The optimal enzymolysis conditions were determined to be adding EDTA 0.02mmol and 0.16mg ascorbic acid to 4ml of the homogenized phosphate–citrate buffer solution (pH 4.00). ITCs profiles were identified and seven kinds of individual ITCs were detected, among which sulforaphane accounted the most. Four kinds of individual ITCs including isobutyl isothiocyanate, 4-isothiocyanato-1-butene, 1-isothiocyanato-3-methyl-butane and 1-isothiocyanato-butane are firstly reported in broccoli sprouts.

Differential Effects of Phenethyl Isothiocyanate and D,L-Sulforaphane on TLR3 Signaling

Naturally occurring isothiocyanates (ITCs) from cruciferous vegetables are widely studied for their cancer chemopreventive effects. In this study, we investigated the effects of ITCs on TLR signaling, and found that the two most promising ITCs, phenethyl ITCs (PEITC) and D,L-sulforaphane (SFN), have differential effects on dsRNA-mediated innate immune signaling through TLR3. PEITC preferentially inhibited TLR3-mediated IFN regulatory factor 3 (IRF3) signaling and downstream gene expression in vivo and in vitro, whereas SFN caused inhibition of TLR3-mediated NF-κB signaling and downstream gene expression. Mechanistically, PEITC inhibited ligand (dsRNA)-dependent dimerization of TLR3, resulting in inhibition of signaling through IFN regulatory factor 3. In contrast, SFN did not disrupt TLR3 dimerization, indicating that it affects further downstream pathway resulting in NF-κB inhibition. To examine the biological significance of these findings in the context of antitumor activities of these compounds, we used two approaches: first, we showed that dsRNA-mediated apoptosis of tumor cells via TLR3 was inhibited in the presence of PEITC, whereas this response was augmented by SFN treatment; second, in a separate assay measuring anchorage-independent growth and colony formation by immortalized fibroblasts, we made similar observations. Again in this study, PEITC antagonized dsRNA-mediated inhibition of colony formation, whereas SFN enhanced the inhibition. These results indicate biologically relevant functional differences between two structurally similar ITCs and may provide important insights in therapeutic development of these compounds targeted to specific cancer.

Urease from Helicobacter pylori is inactivated by sulforaphane and other isothiocyanates

Infections by Helicobacter pylori are very common, causing gastroduodenal inflammation including peptic ulcers, and increasing the risk of gastric neoplasia. The isothiocyanate (ITC) sulforaphane [SF; 1-isothiocyanato-4-(methylsulfinyl)butane] derived from edible crucifers such as broccoli is potently bactericidal against Helicobacter, including antibiotic-resistant strains, suggesting a possible dietary therapy. Gastric H. pylori infections express high urease activity which generates ammonia, neutralizes gastric acidity, and promotes inflammation. The finding that SF inhibits (inactivates) urease (jack bean and Helicobacter) raised the issue of whether these properties might be functionally related. The rates of inactivation of urease activity depend on enzyme and SF concentrations and show first order kinetics. Treatment with SF results in time-dependent increases in the ultraviolet absorption of partially purified Helicobacter urease in the 260–320 nm region. This provides direct spectroscopic evidence for the formation of dithiocarbamates between the ITC group of SF and cysteine thiols of urease. The potencies of inactivation of Helicobacter urease by isothiocyanates structurally related to SF were surprisingly variable. Natural isothiocyanates closely related to SF, previously shown to be bactericidal (berteroin, hirsutin, phenethyl isothiocyanate, alyssin, and erucin), did not inactivate urease activity. Furthermore, SF is bactericidal against both urease positive and negative H. pylori strains. In contrast, some isothiocyanates such as benzoyl-ITC, are very potent urease inactivators, but are not bactericidal. The bactericidal effects of SF and other ITC against Helicobacter are therefore not obligatorily linked to urease inactivation, but may reduce the inflammatory component of Helicobacter infections.

Mitochondrial apoptosis pathway contributes to polysaccharide of astragalus-induced apoptosis of EC9706 cells and enhances their sensitivty to cisplatin

Objective To investigate the antiproliferative,cytotoxic,apoptogenic activities of polysaccharide of astragalus (APS) and its synergistic effects with cisplatin in inducing apoptosis of esophageal carcinoma cells.Methods Methyl thiazol tetrazolium (MTT) assay was used to detect the antiproliferative effect of APS and cisplatin on EC9706 cells,Annexin V-lluoresceine isothiocyanate (FITC)/propidium iodide (PI) stained fluorescence-activated cell sorter (FACS) was used to detect the apoptosis rate,and immunocytochemistry was used to examine cdlular localisation and B lymphocytes/leukemia-2 (bcl-2),bcl-2 associated X protein (bax),nuclear factor-κB (NF-κB) protein levels.Results APS and cisplatin produced dose-dependent inhibition of EC9706 cell growth.The apoptosis rate in APS ± cisplatin group (41.3％) was higher than in APS group (18.7％) or cisplatin group (27.6％).APS could up-regulate the grey values of Bax protein (185.54 ± 11.27),and down-reguate those of bcl-2 (179.22 ± 12.47) and NF-κB (131.66 ± 18.83) proteins.The grey values bcl-2,NF-κB and Bax in control group were 142.11 ±13.35,140.21 ± 14.75 and 199.67 ± 15.43,respectiely.Conclusion Mitochondrial apoptosis pathway contributes to APS-induced apoptosis.APS enhanced the sensitivity of EC9706 cells to cisplatin by down-regulating the expression of NF-κB protein. Key words: Esophageal carcinoma; Polysaccharide of astragalus; Cisplatin; Apoptosis; Drug-resistance

Comparison of bioactive phytochemical content and release of isothiocyanates in selected brassica sprouts

The consumption of brassica sprouts as raw vegetables provides a fair amount of glucosinolates (GLs) and active plant myrosinase, which enables the breakdown of GLs into health-promoting isothiocyanates (ITCs). This study reports the determination of the main constituents related to human health found in edible sprouts of two Brassica oleracea varieties, broccoli and Tuscan black kale, and two Raphanus sativus varieties, Daikon and Sango. Radish sprouts exhibited the highest ability to produce ITCs, with Daikon showing the greatest level of conversion of GLs into bioactive ITCs (96.5%), followed by Sango (90.0%). Tuscan black kale gave a value of 68.5%, whereas broccoli displayed the lowest with 18.7%. ITCs were not the exclusive GL breakdown products in the two B. oleracea varieties, since nitriles were also produced, thus accounting for the lower conversion observed. Measuring the release of plant ITCs is a valuable tool in predicting the potential level of exposure to these bioactive compounds after the consumption of raw brassica sprouts.

Inter simple sequence repeat polymorphism in Alternaria genomic DNA exposed to lethal concentrations of isothiocyanates

Isothiocyanates (ITCs) is a group of defense related compounds synthesized byBrassicas that have positive effects on human health which suggest that they are environmentally friendly compounds to control fungi infections. However, the development of ITC-resistant strains of fungi is a matter of concern. The objective of the present work was to study the response of Alternaria alternata to allyl-isothiocyanate (AITC) and benzyl isothiocyanate (BITC) chronic exposure and the effect of the treatment on some of the inter simple sequence repeats (ISSR) regions. Five strains of A. alternata isolated from tomato and five isolated from cabbage were independently exposed in vitro to AITC and BITC. Concentrations were increased until it reached 0.08 and 0.6 mg/mL of AITC and BITC, respectively. Genomic DNA from both wild type and isogenic adapted strains to ITCs was isolated and five primers were used for ISSR amplification: (GACA)4: 5´-GACAGACAGACAGACA-3´; M13:5´-GAGGGTGGCGGCGGTTCT-3´;(AAG)8:5´-AAGAAGAAGAAGAAGAAGAAGAAG-3´; (ACA)5: 5´-ACAACAACAACAACA-3´ and T3B: 5´-AGGTCGCGGGTTCGAATCC-3´. A lower degree of polymorphism was found to be induced by the treatment in the wild-type strains isolated from cabbage as compared with the wild-type strains isolated from tomato. It can be concluded that ITCs exposure induced random mutations in different ISSR regions of the A. alternata genome which does not lead to the development of strains with a hereditable resistant phenotype. Key words: Alternaria alternata, fungicide, allyl-isothiocyanate, benzyl-isothiocyanate, inter-simple sequence repeat

Analyse comparative des indices de performance de la DMS des CHU de Strasbourg, Nancy et Dijon et du CHR de Metz-Thionville en 2011

Glucosinolates are sulphur-containing compounds present in Brassica species that are hydrolyzed by the plant enzyme myrosinase to isothiocyanates (ITC), which have previously reported chemopreventive properties. In vivo, ITC are metabolized and excreted in urine as mercapturic acids. A cross-over-design study of 7 subjects after ingestion of 200-g raw or microwaved kailan-hybrid broccoli was conducted. Total ITC equivalents in the vegetable, urine and blood samples were determined by HPLC as the cyclocondensation product of 1,2-benzenedithiol. The highest ITC metabolization (53.6 ± 15.7% over the total ITC ingested) was observed during the first 4 h after ingestion of raw product. However, the highest ITC metabolization after consumption of microwaved samples was delayed to 4–10 h, with 23.2 ± 27.6%. The high ITC metabolization during the first 4 h was most likely due to absorption in the small intestine, while the second peak (4–8 h) could be presumably attributed to an ITC absorption in the colon. The total ITC metabolization after raw kalian-hybrid consumption (79.1 ± 18.8%) was approximately 2-fold higher than that from microwaved broccoli (41.3 ± 8.8%), which was statistically significant (P, t test = 0.005). The ITC absorption of the kailan-hybrid was 2 times higher for raw and 3–9 times higher for cooked samples than the values previously reported in the bibliography with conventional broccoli varieties. Compared to other brassicas, kailan-hybrid can be presented as a vegetable with both, a high concentration and a great ITC metabolization.

Dissipation of pure and broccoli-released glucosinolates in soil under high and low moisture content

Glucosinolates (GSLs) are secondary metabolites found in Brassica species. Upon tissue disruption GSLs are hydrolyzed by myrosinase enzymes to isothiocyanates (ITCs) which are highly toxic to microbes. Therefore the incorporation of fresh Brassicaceae tissues into soil for the control of soil-born plant pathogens is viewed as a biofumigation process. Its efficacy relies on the rate of GSL conversion to ITCs, but also on environmental factors controlling GSL availability in the soil matrix. We studied the dissipation of GSLs, applied either by broccoli leaves or as pure compounds, in a clay loam soil at two soil moisture content levels. Regardless of their mode of application, GSLs were rapidly dissipated in soil with half-life values ranging from 3.2 to 15.5 h. Increasing moisture from 20 to 90% of the soil water holding capacity significantly accelerated their dissipation. Indolyl broccoli-derived GSLs dissipated faster than aliphatic GSLs at high moisture levels, while at low moisture levels a three-fold reduction in their dissipation rates was observed. The dissipation of aliphatic GSLs was less affected by soil moisture levels. Application of pure GSLs resulted in increased soil metabolic quotients (qCO2), suggesting a decline is microbial metabolic efficiency. Their dissipation was related to myrosinase activity apparently derived from soil microbes.

The action of selected isothiocyanates on bacterial biofilm prevention and control

The activity of two selected isothiocyanates (ITCs), allylisothiocyanate (AITC) and 2-phenylethy-lisothiocyanate (PEITC) was evaluated on the prevention and control of biofilms formed by Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Listeria monocytogenes. In addition, the effect of ITCs was also tested on planktonic cell susceptibility, bacterial motility and adhesion. Biofilm prevention and control were tested using a microtiter plate assay and the effect of ITCs was assessed on biofilm mass and metabolic activity. The minimum bactericidal concentration for E. coli and P. aeruginosa was 1000 μg mL−1 (AITC) and >1000 μg mL−1 (PEITC), for S. aureus and L. monocytogenes was >1000 μg mL−1 (for both ITCs). AITC caused total inhibition of swimming (P. aeruginosa) and swarming (E. coli) motilities. PEITC caused total inhibition of swimming (E. coli, P. aeruginosa and L. monocytogenes) and swarming (E. coli and P. aeruginosa) motilities. Colony spreading of S. aureus was completely inhibited with PEITC. Adhesion assessed in terms of free energy was less favorable when bacteria were exposed to AITC for E. coli and P. aeruginosa and PEITC for P. aeruginosa. Both ITCs had preventive action on biofilm formation and showed a higher potential to reduce the mass of biofilms formed by the Gram-negative bacteria. AITC and PEITC promoted reductions in biofilm activity higher than 60% for all the biofilms tested. The overall study emphasizes the potential of ITCs as emergent products to inhibit bacterial motility and prevent/control biofilms of important human pathogenic bacteria.

Identification of MicroRNAs Regulated by Isothiocyanates and Association of Polymorphisms Inside Their Target Sites with Risk of Sporadic Colorectal Cancer

Sporadic colorectal cancer (CRC) is a typical multifactorial disease. Isothiocyanates (ITC) have been recently shown to inhibit development of CRC in many experimental models. MicroRNAs (miRNAs) are short noncoding RNAs that posttranscriptionally regulate gene expression through binding to 3′ untranslated regions (3′UTR) of target mRNAs. MiRNAs are regulated by natural agents, ITCs included. In our study, using global expression profiling based on TaqMan Low-Density Arrays, we identified 3 common miRNAs (miR-155, miR-23b, miR-27b) regulated by ITCs (sulforaphane, iberin) in colonic epithelial cell lines NCM460 and NCM356. In silico predictions allowed us to find 9 relevant single nucleotide polymorphisms (SNPs) localized within the 3′UTRs of genes (AGTR1, TNFAIP2, PRKCB, HSPA9, RABGAP1, DICER1, ADAM19, VWA5A, and SIRT5) targeted by these ITC-related miRNAs. Finally, we observed that homozygous CC genotype of DICER1, rs1057035, was significantly associated with decreased risk of CRC (odds ratio = 0.49; 95% confidence interval: 0.25–0.95, P = 0.036) when compared to TT homozygote genotype; also, the C allele tended to have a protective effect (P = 0.072). This study showed that miRNAs could be involved in chemoprotective effects of natural agents; their function alteration through SNPs in their binding sites and flanking regions presents a new class of CRC risk factors.

Antifungal activity of gaseous allyl, benzyl and phenyl isothiocyanate in vitro and their use for fumonisins reduction in bread

Fumonisins (FBs) are toxins produced mainly by the molds Fusarium verticillioides (synonym Fusarium moniliforme) and Fusarium proliferatum. These mycotoxins are contaminants of wheat, maize, maize-based foods and other grains worldwide. FB1, the most abundant and toxic metabolite, is known to cause a range of species-specific toxic responses. It has been associated with a high incidence of esophageal cancer in the Transkei region of South Africa and some provinces of China. In addition, FB1 has been declared a class 2B carcinogen or “possibly carcinogenic to humans”. Isothiocyanates (ITCs) are natural compounds produced by enzymatic conversion of metabolites called glucosinolates. They are potentially useful antimicrobial compounds for food applications. In this study, the reduction of the FBs present in loaf bread contaminated with Gibberella moniliformis CECT 2987, a fumonisin producer by allyl (AITC), phenyl (PITC) and benzyl isothiocyanates (BITC) was investigated. In addition, the antifungal activity of these ITCs toward Fusarium mycotoxigenic strains was also evaluated. The ITCs employed in this study inhibited the growth of three mycotoxigenic Fusarium, reducing 2.1–89.7% of the mycelium size. The ITCs used also reacted with the FB2 produced by G. moniliformis in the bread, reducing its levels by 73–100% depending on the dose and time of exposure.

Isothiocyanates: naturally occurring HEPG2 human liver carcinoma inhibitor

In vitro anticancer screening of different isothiocyanates (ITCs) [Allyl isothiocyanate (AITC), Phenylethyl isothiocyanate (PEITC) and Sulphoraphane (SUL)], derived from naturally occurring Eruca sativa seed oil (SO) against HepG2 human liver carcinoma cell line has been carried out using MTT, TBE and SRB bioassays. Combination of ITCs, in ratio (1:1:1) exhibited maximum percentage inhibition of 97.12%, 96.34% and 96.56% by MTT, TBE and SRB respectively against reference drug doxorubicin at concentration 50 µM. Percent inhibition has been found to be more pronounced in isothiocyanates combination compared to its natural source E. sativa seed oil.

Antiproliferative Activity of the Dietary Isothiocyanate Erucin, a Bioactive Compound from Cruciferous Vegetables, on Human Prostate Cancer Cells

It is becoming increasingly clear that many dietary agents, such as isothiocyanates (ITCs) from cruciferous vegetables, can retard or prevent the process of prostate carcinogenesis. Erucin (ER) is a dietary ITC, which has been recently considered a promising cancer chemopreventive phytochemical. The potential protective activity of ER against prostate cancer was investigated using prostate adenocarcinoma cells (PC3), to analyze its effects on pathways involved in cell growth regulation, such as the cyclin-dependent kinase (CDKs) inhibitor p21WAF1/CIP1 (p21), phosphatidylinositol-3 kinase/AKT, and extracellular signal-regulated kinases (ERK)1/2 signaling pathways. We have shown for the first time that ER increases significantly p21 protein expression and ERK1/2 phosphorylation in a dose-dependent manner to inhibit PC3 cell proliferation (P ≤ 0.01). Compared to the structurally related sulforaphane, a well-studied broccoli-derived ITC, ER showed lower potency in inhibiting proliferation of PC3 cells, as well as in modulating p21 and pERK1/2 protein levels. Neither of the naturally occurring ITCs was able to affect significantly pAKT protein levels in prostate cells at all concentrations tested (0–25 μM). It is clearly important for the translation of laboratory findings to clinical approaches to investigate in animal and cell studies the molecular mechanisms by which ITCs may exert health promoting effects.