Search

Several sesquiterpene lactones (STLs) have been tested as lead drugs in cancer clinical trials. Salograviolide-A (Sal-A) and salograviolide-B (Sal-B) are two STLs that have been isolated from Centaurea ainetensis, an indigenous medicinal plant of the Middle Eastern region. The parent compounds Sal-A and Sal-B were modified and successfully prepared into eight novel guaianolide-type STLs (compounds 1–8) bearing ester groups of different geometries. Sal-A, Sal-B, and compounds 1–8 were tested against a human colorectal cancer cell line model with differing p53 status; HCT116 with wild-type p53 and HCT116 p53−/− null for p53, and the normal-like human colon mucosa cells with wild-type p53, NCM460. IC50 values indicated that derivatization of Sal-A and Sal-B resulted in potentiation of HCT116 cell growth inhibition by 97% and 66%, respectively. The effects of the different molecules on cancer cell growth were independent of p53 status. Interestingly, the derivatization of Sal-A and Sal-B molecules enhanced their anti-growth properties versus 5-Fluorouracil (5-FU), which is the drug of choice in colorectal cancer. Structure-activity analysis revealed that the enhanced molecule potencies were mainly attributed to the position and number of the hydroxy groups, the lipophilicity, and the superiority of ester groups over hydroxy substituents in terms of their branching and chain lengths. The favorable cytotoxicity and selectivity of the potent molecules, to cancer cells versus their normal counterparts, pointed them out as promising leads for anti-cancer drug design.

Beetroot (Beta vulgaris) pomace, processing by-product from food industry, was investigated in this work as a starting raw material. The contents of phenolics (1.87–11.98 mg GAE/g of dry weight) and betalains (0.75–3.75 mg betalains/g of dry weight) in the extracts were determinated spectrophotometrically. Some individual phenolic compounds, including ferulic, vanillic, p-hydroxybenzoic, caffeic and protocatehuic acids, were identified and quantified by HPLC. The antioxidative activity of beetroot extracts was tested using DPPH, hydroxyl and superoxide anion radicals by ESR spectroscopy. IC50·OH (0.05–0.108 mg/ml), IC50DPPH· (0.183–0.333 mg/ml), and IC50O2·- (0.198–1.000 mg/ml) were calculated. The regression analysis produced moderate to high correlation coefficients between the scavenging activities and phenolics, and some individual phenolic compounds which indicated that beetroot pomace may be used as functional food ingredient. Cell growth effects were determined in MCF7 and MRC-5 cell lines, using SRB assay. IC50 values were in the range of 362.478–503.525 and 383–587.880 μg/ml in MRC-5 and MCF7, respectively.

The carotenoid content, antioxidant and cell growth activities of tomato waste extracts, obtained from five different tomato genotypes, was investigated. High performance liquid chromatography was used to identify and quantify the main carotenoids present in tomato waste extracts. The antioxidant activity of tomato waste extracts was tested using spectrophotometric methods, 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity and reducing power assay. The highest DPPH scavenging activity (IC 50 = 0.057 mg/ml) was obtained for Bačka extract. The Knjaz extract showed the best reducing power (IC 50 = 2.12 mg/ml). Cell growth effects were determined in HeLa, MCF7 and MRC-5 cell lines by sulforhodamine B test. Anti-proliferative effects were observed in all cell lines at higher concentrations (⩾0.125 mg/ml). The carotenoid contents exhibited a strong correlation with antioxidant and anti-proliferation activity. The results obtained indicated that tomato waste should be regarded as potential nutraceutic resource and may be used as a functional food ingredient. [ABSTRACT FROM AUTHOR]

Abstract: Tomato waste, a by-product in juice processing, obtained from different tomato genotypes, was subjected to evaluation as potential source of phenolic antioxidants and anticancer agents. Some individual phenolic compounds, including phenolic acids and flavonoids, were identified and quantified by HPLC. The antioxidant activity of tomato waste extracts was tested by measuring their ability to scavenge hydroxyl and superoxide anion radicals by ESR spectroscopy. The highest hydroxyl radical scavenging activity (IC50 =0.03mg/ml) was obtained in the case of Novosadski niski waste extract. The Rutgers waste extract showed the best performance in scavenging superoxide anion radicals (IC50 =0.45mg/ml). Cell growth effects were determined in HeLa, MCF7 and MRC-5 cell lines by SRB test. In all cell lines antiproliferative effects were observed at higher investigated concentrations (⩾6.3mg/ml). The strongest activity against cancer cells was observed by Saint Pierre extract in HeLa cell line (IC50 =13.7mg/ml). [Copyright &y& Elsevier]

There is inadequate published data referring to bioactivity of lemon balm tea and its Kombucha. The aim of this study, therefore, was to investigate antimicrobial, antiproliferative, genotoxic, and antigenotoxic potential of lemon balm tea and its Kombucha with consuming acidity. Antimicrobial activity was determined by agar-well diffusion method. Cell growth effects were determined in HeLa, MCF7, and HT-29 human tumor cell lines. Genotoxic and antigenotoxic effects were determined using chromosome aberration assay in Chinese hamster cell line CHO-K1. Differences between control and treated groups were evaluated using analysis of variance, at significance level of p < 0.05. Kombucha from lemon balm tea ( Melissa officinalis L.) exibited antimicrobial activity against prokaryotic microorganisms independently of their cell wall structure (both Gram-positive and Gram-negative bacteria), while there was no observed activity against eukaryots (yeasts and moulds). There was absence of genotoxic effects while antigenotoxic effects of lemon balm Kombucha and tea were confirmed on MMC-damaged CHO-K1 cells. For the explanation of cell growth effects that were not concentration dependent, concept of hormesis was used. Antiproliferative activity was lower compared with traditional Kombucha and Satureja montana L. Kombucha, with lemon balm tea showing higher activity than its Kombucha. [ABSTRACT FROM AUTHOR]

Abstract: Beetroot (Beta vulgaris) pomace, processing by-product from food industry, was investigated in this work as a starting raw material. The contents of phenolics (1.87–11.98mg GAE/g of dry weight) and betalains (0.75–3.75mg betalains/g of dry weight) in the extracts were determinated spectrophotometrically. Some individual phenolic compounds, including ferulic, vanillic, p-hydroxybenzoic, caffeic and protocatehuic acids, were identified and quantified by HPLC. The antioxidative activity of beetroot extracts was tested using DPPH, hydroxyl and superoxide anion radicals by ESR spectroscopy. (0.05–0.108mg/ml), (0.183–0.333mg/ml), and (0.198–1.000mg/ml) were calculated. The regression analysis produced moderate to high correlation coefficients between the scavenging activities and phenolics, and some individual phenolic compounds which indicated that beetroot pomace may be used as functional food ingredient. Cell growth effects were determined in MCF7 and MRC-5 cell lines, using SRB assay. IC50 values were in the range of 362.478–503.525 and 383–587.880μg/ml in MRC-5 and MCF7, respectively. [Copyright &y& Elsevier]

Several sesquiterpene lactones (STLs) have been tested as lead drugs in cancer clinical trials. Salograviolide-A (Sal-A) and salograviolide-B (Sal-B) are two STLs that have been isolated from Centaurea ainetensis, an indigenous medicinal plant of the Middle Eastern region. The parent compounds Sal-A and Sal-B were modified and successfully prepared into eight novel guaianolide-type STLs (compounds 1–8) bearing ester groups of different geometries. Sal-A, Sal-B, and compounds 1–8 were tested against a human colorectal cancer cell line model with differing p53 status; HCT116 with wild-type p53 and HCT116 p53−/− null for p53, and the normal-like human colon mucosa cells with wild-type p53, NCM460. IC50 values indicated that derivatization of Sal-A and Sal-B resulted in potentiation of HCT116 cell growth inhibition by 97% and 66%, respectively. The effects of the different molecules on cancer cell growth were independent of p53 status. Interestingly, the derivatization of Sal-A and Sal-B molecules enhanced their anti-growth properties versus 5-Fluorouracil (5-FU), which is the drug of choice in colorectal cancer. Structure-activity analysis revealed that the enhanced molecule potencies were mainly attributed to the position and number of the hydroxy groups, the lipophilicity, and the superiority of ester groups over hydroxy substituents in terms of their branching and chain lengths. The favorable cytotoxicity and selectivity of the potent molecules, to cancer cells versus their normal counterparts, pointed them out as promising leads for anti-cancer drug design. [ABSTRACT FROM AUTHOR]