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To explore new compounds with antitumour activity, fifteen phenolic nor-tripterpenes isolated from Celastraceae species, Maytenus jelskii, Maytenus cuzcoina, and Celastrus vulcanicola, have been studied. Their chemical structures were elucidated through spectroscopic and spectrometric techniques, resulting in the identification of three novel chemical compounds. Evaluation on human tumour cell lines (A549 and SW1573, non-small cell lung; HBL-100 and T-47D, breast; HeLa, cervix, and WiDr, colon) revealed that three compounds, named 6-oxo-pristimerol, demethyl-zeylasteral, and zeylasteral, exhibited significant activity (GI50 ranging from 0.45 to 8.6 µM) on at least five of the cell lines tested. Continuous live cell imaging identified apoptosis as the mode of action of selective cell killing in HeLa cells. Furthermore, their effect on a drug-sensitive Saccharomyces cerevisiae strain has been investigated to deepen on their mechanism of action. In dose-response growth curves, zeylasteral and 7α-hydroxy-blepharodol were markedly active. Additionally, halo assays were conducted to assess the involvement of oxidative stress and/or mitochondrial function in the anticancer profile, ruling out these modes of action for the active compounds. Finally, we also delve into the structure-activity relationship, providing insights into how the molecular structure of these compounds influences their biological activity. This comprehensive analysis enhances our understanding of the therapeutic potential of this triterpene type and underscores its relevance for further research in this field. [ABSTRACT FROM AUTHOR]

To explore new compounds with antitumour activity, fifteen phenolic nor-tripterpenes isolated from Celastraceae species, Maytenus jelskii, Maytenus cuzcoina, and Celastrus vulcanicola, have been studied. Their chemical structures were elucidated through spectroscopic and spectrometric techniques, resulting in the identification of three novel chemical compounds. Evaluation on human tumour cell lines (A549 and SW1573, non-small cell lung; HBL-100 and T-47D, breast; HeLa, cervix, and WiDr, colon) revealed that three compounds, named 6-oxo-pristimerol, demethyl-zeylasteral, and zeylasteral, exhibited significant activity (GI50 ranging from 0.45 to 8.6 µM) on at least five of the cell lines tested. Continuous live cell imaging identified apoptosis as the mode of action of selective cell killing in HeLa cells. Furthermore, their effect on a drug-sensitive Saccharomyces cerevisiae strain has been investigated to deepen on their mechanism of action. In dose-response growth curves, zeylasteral and 7α-hydroxy-blepharodol were markedly active. Additionally, halo assays were conducted to assess the involvement of oxidative stress and/or mitochondrial function in the anticancer profile, ruling out these modes of action for the active compounds. Finally, we also delve into the structure-activity relationship, providing insights into how the molecular structure of these compounds influences their biological activity. This comprehensive analysis enhances our understanding of the therapeutic potential of this triterpene type and underscores its relevance for further research in this field.

Herein, the antiproliferative potential of the essential oil obtained from fresh leaves of Croton campestris against human tumour cell lines was investigated for the first time. Furthermore, the essential oil obtained by hydrodistillation had the composition determined by gas chromatography–mass spectrometry (GC/MS). Ten major components were identified that comprised 91.59% of the total content, with 23.8% consisting of (Z)-caryophyllene and 16.08% consisting of γ-elemene as main components. The cytotoxic activity was observed mainly for breast (MCF-7) and colon (HT-29) human tumour cell lines, with GI50 (50% growth inhibition) concentration of 8.61 and 9.94 μg/mL, respectively. The results of this study showed that the essential oil obtained from Croton campestris A.St.-Hil. represents a potential source for the search of new antitumour agents. [ABSTRACT FROM AUTHOR]

A new bioessential Knoevenagel condensate Schiff base ligand (L) was synthesized by the reaction of 3-(4-hydroxy-3-methoxybenzyl)pentane-2,4-dione and 4-aminoantipyrine. The ligand forms monomeric divalent transition metal complexes ( 1- 4) which were characterized using spectral and analytical data. All these complexes have the general formula [ML]Cl2, where M = Co(II), Ni(II), Cu(II) and Zn(II). They are electrolytic in nature and adopt square planar geometry. The binding propensity of these complexes with calf thymus DNA was investigated using absorption spectrophotometric titration, cyclic voltammetry and viscosity measurements. The binding constant values imply that the complexes bind with DNA via intercalation mode. The in vitro antibacterial and antifungal activities reveal that the complexes have good antimicrobial efficacy against a set of pathogens. The nucleolytic cleavage activity of these complexes on pUC18 DNA was investigated using agarose gel electrophoresis. Also, the in vitro cytotoxicity of the synthesized complexes against a panel of human tumour cell lines (MCF-7 and HeLa) and normal cell lines (NHDF and HEK) was assayed using the MTT method. Interestingly, complex 1 exhibits more potent anticancer activity than cisplatin and other complexes. [ABSTRACT FROM AUTHOR]

Natural compounds isolated from vegetables have protective and disease-preventing potential for the development of functional food. This study investigates the in vitro antioxidant capacity, total polyphenol and total flavonoid content, glucosinolate and glucosinolate degradation products of broccoli and collard extracts. In vitro antitumor activities on two human tumour cell lines (MCF-7 and HeLa) were studied. Broccoli and collard extracts were extracted from fresh, blanched and boiled broccoli florets and collard leaves. The Oxygen Radical Absorbance Capacity (ORAC) assay revealed that collard extracts exhibited higher antioxidant capacity than broccoli extracts. Total polyphenol and total flavonoid contents were also higher in collard extracts. The extracts were compared for the contents of total glucosinolates, indol glucosinolates and aliphatic glucosinolates. Glucoraphanin was the predominant compound in total glucosinolate content, followed by glucobrassicin and neoglucobrassicin (95.97 μmol 100 g −1 fresh weight (fw), 85.42 μmol 100 g −1 fw and 82.12 μmol 100 g −1 fw, respectively) in broccoli extracts; while in collard extracts, the major glucosinolate was glucobrassicin (80.33 μmol 100 g −1 fw), followed by glucoiberin (67.50) μmol 100 g −1 fw and sinigrin (21.91 μmol 100 g −1 fw). The strongest antiproliferative effect was observed in extracts obtained by blanching. The present study established that the extracts that were examined possess antioxidant and promising antitumour activities. [ABSTRACT FROM AUTHOR]

A flavanone has been isolated first time from the stem of Bauhinia variegata, and its structure was identified by colour reactions and spectral analysis. In a search for novel anticancer compounds from medicinal plants, the isolated flavanone was tested for cytotoxic activity against 57 human tumour lines, representing leukaemia, non-small cell lung, colon, central nervous system, melanoma, ovarian, renal, prostate and breast cancers. The results showed that the flavanone has cytotoxic activity against human tumour cell lines. [ABSTRACT FROM AUTHOR]

The family of NADPH oxidase (NOX) genes produces reactive oxygen species (ROS) pivotal for both cell signalling and host defense. To investigate whether NOX and NOX accessory gene expression might be a factor common to specific human tumour types, this study measured the expression levels of NOX genes 1-5, dual oxidase 1 and 2, as well as those of NOX accessory genes NoxO1, NoxA1, p47phox, p67phox and p22phox in human cancer cell lines and in tumour and adjacent normal tissue pairs by quantitative, real-time RT-PCR. The results demonstrate tumour-specific patterns of NOX gene expression that will inform further studies of the role of NOX activity in tumour cell invasion, growth factor response and proliferative potential. [ABSTRACT FROM AUTHOR]

A novel flavone glycoside has been isolated from the stem of Indigofera aspalathoides, and its structure was identified by colour reactions and spectral analysis. The isolated compound was tested for cytotoxic activity against 57 human tumour lines representing leukemia, non-small cell lung, colon, central nervous system, melanoma, ovarian, renal, prostate and breast cancers. The results showed that the flavone glycoside has cytotoxic activity against human tumour cell lines. [ABSTRACT FROM AUTHOR]

The anti-arthritic drug auranofin exerts also potent antitumour activity in in vitro and in vivo models, whose mechanisms are not yet well defined. From an auranofin-sensitive human ovarian cancer cell line A2780, a highly resistant (>20-fold) subline (A2780/AF-R) was developed and characterized. Marked reduction of gold accumulation occurred in auranofin-resistant A2780 cells. Also, moderately higher thioredoxin reductase activity in A2780/AF-R cells was observed while no changes in intracellular glutathione content occurred. Resistance to auranofin was associated with a low level of cross-resistance to some investigational gold compounds as well as to oxaliplatin and other anticancer drugs with different mode of action (i.e. melphalan, vinblastine, doxorubicin, etoposide, and paclitaxel). Reduced gold accumulation was associated to substantial gene expression changes in various influx (e.g. SLC22A1, SLC47A1, SLCO1B1 ) and efflux (e.g. ABCB1, ABCC2, ABCC3 ) transporters. The expression levels of selected proteins (i.e. SLC22A1, SLC47A1, P-gp) were also changed accordingly. These data provide evidence that multiple drug transporters may act as mediators of transport of auranofin and other gold compounds in cancer cells. Further investigation into the molecular mechanisms mediating transport of auranofin and new gold complexes in view of their potential clinical application in the treatment of cancer is warranted., Competing Interests: CONFLICTS OF INTEREST The authors declare no competing financial interests