Even if cancer represents a burden for human society, an exhaustive cure has not been discovered yet. Low therapeutic index and resistance to pharmacotherapy are two of the major limits of antitumour ...treatments. Natural products represent an excellent library of bioactive molecules. Thus, tapping into the natural world may prove useful in identifying new therapeutic options with favourable pharmaco-toxicological profiles.
, or common walnut, is a very resilient tree that has inhabited our planet for thousands of years. Many studies correlate walnut consumption to beneficial effects towards several chronic diseases, such as cancer, mainly due to the bioactive molecules stored in different parts of the plant. Among others, polyphenols, quinones, proteins, and essential fatty acids contribute to its pharmacologic activity. The present review aims to offer a comprehensive perspective about the antitumour potential of the most promising compounds stored in this plant, such as juglanin, juglone, and the ellagitannin-metabolites urolithins or deriving from walnut dietary intake. All molecules and a chronic intake of the fruit provide tangible anticancer effects. However, the scarcity of studies on humans does not allow results to be conclusive.
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•The ethanolic extract from Mela Rosa Marchigiana pulp callus contains triterpenes.•The biological effects of the ethanolic extract were investigated.•Cell-free and cell-based models ...were used.•Cell-free models showed antioxidant and genoprotective activities.•Cell models showed positive effect on inflammation, mitochondrial biogenesis and wound.
The biological effects of the ethanolic extract from Mela Rosa Marchigiana pulp callus were investigated. In terms of the antioxidant activity, the extract exhibited free radical scavenging activity of 67% and 39% using the DPPH assay and ABTS assay respectively. Furthermore, it reduced the ROS production in the keratinocyte cell model of H2O2 induced oxidative stress. The genoprotective effect was evaluated using the DNA nicking assay, which revealed significant protection up to 70%. The anti-inflammatory response was detected at 0.5 mg/ml through the release of nitric oxide using bacterial LPS and RAW 264.7 cells. Finally, preliminary studies on keratinocytes suggested a possible positive effect of the extract on mitochondrial biogenesis and wound healing. The obtained results encourage further studies to deep the biological effects of this callus with the future objective to propose a product for nutraceutical, cosmetic and food-tech industries, as well as an alternative to normal ways of chemical synthesis.
A small library of 6-
-sucrose monoester surfactants has been synthesized and tested against various microorganisms. The synthetic procedure involved a modified Mitsunobu reaction, which showed ...improved results compared to those present in the literature (higher yields and larger scope). The antifungal activities of most of these glycolipids were satisfactory. In particular, sucrose palmitoleate (URB1537) showed good activity against Candida albicans ATCC 10231,
spp., and
IDRAH01 (MIC value: 16, 32, 64 µg/mL, respectively), and was further characterized through radical scavenging, anti-inflammatory, and biocompatibility tests. URB1537 has been shown to control the inflammatory response and to have a safe profile.
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•Mela Rosa Marchigiana pulp callus extract (MRME) reduces inflammatory response.•MRME can contrast senescence or High Glucose-induced inflammation.•In High Glucose- and LPS-induced ...inflammation, MRME reduces U937 mitochondrial respiration.•MRME modulates digestive enzymes that can help decreasing the absorption of glucose and triglycerides.
The anti-inflammatory activity of the “Mela Rosa Marchigiana” (MRM) pulp callus ethanol Extract (MRME) was tested in different cellular models including (i) LPS-treated RAW 264.7; (ii) HUVEC exposed to short-term high Glucose (HG, 45 mM) or normal glucose (NG, 5 mM) concentrations; and (iii) HG (30 mN) and LPS-treated U937. To evaluate the anti-inflammatory effect of the extract, Nitric Oxide (NO) production was measured in RAW 264.6 cells, while IL-8, IL-1ß and MCP-1 expressions, along with modulation of some inflammation- or senescence-associated miRNAs (miR-21, miR-126, miR-17 and miR-217) were assessed in HUVECs and/or U937. MRME treatment reduced pro-inflammatory markers amount, suggesting a decreased generalised inflammatory response. Present findings indicate that MRME can contrast senescence- or HG-induced inflammation. Moreover, in HG- and LPS-induced inflammation, MRME reduced U937 monocyte activation by inhibiting mitochondrial respiration and inflammatory markers. Finally, the inhibitory potential of MRME on the digestive enzymes α-glucosidase, α-amylase and lipase activity was investigated. Our results support the idea that MRME has a positive effect on inhibition of endothelial/macrophage dysfunction under HG/senescence inflammatory conditions. Furthermore, the obtained results showed a modest inhibitory power of the extract (IC50 values: 2.98 ± 0.24, 1.77 ± 0.15, and 2.06 ± 0.31 mg/ml, respectively), which, however, could be of some help in decreasing the absorption of glucose and triglycerides.
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•An innovative method was developed to obtain Cydonia oblonga pulp callus culture.•Pulp callus extract provides a high quantity of secondary compared to fruit pulp.•Pulp callus ...extract has antioxidant and genoprotective effects.•Pulp callus extract inhibits α-glucosidase lipase and α-amylase.
This study has developed an innovative method for the production of secondary metabolites starting from Cydonia oblonga Mill (quince) pulp callus culture. The qualitative and quantitative content of phenolic and triterpenic acids of quince callus extract were elucidated by GC–MS, GC, and HPLC-DAD-ESI-MSn. The callus extract was rich of 5-O-caffeoylquinic acid (5-CQA), 5-p-coumaroylquinic acid (5-p-CoQA) and maslinic and corosolic acid. Quince callus extract's radical scavenging and antioxidant activity were evaluated by 2,2-diphenyl-1-picrylhydrazyl, 2,2,-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid), and Oxygen Radical Absorbance Capacity methods. The genoprotection was evaluated by gel electrophoresis analysis and quantitative Real-Time PCR. In addition to the good antioxidant activity the quince callus extract is a strong inhibitor of α-glucosidase (IC50 of 0.25 ± 0.02 mg dw/mL) and lipase (IC50 of 1.99 ± 0.005 mg dw/mL), but mild inhibitor of α-amylase. Therefore, this work would be significant for the future development of a nutraceutical approach to the management of hyperglycemia and dyslipidemia.
•Mela Rosa Marchigiana pulp callus cultures produce long-lasting bioactive compounds.•Mela Rosa Marchigiana pulp callus extract showed in vitro antioxidant activity.•Mela Rosa Marchigiana pulp callus ...extract showed ex vivo antioxidant activity.•Mela Rosa Marchigiana pulp callus extract showed in vivo antioxidant activity.
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The Mela Rosa Marchigiana (MRM) pulp callus, kept alive since 2017 by monthly sub-cultures, was investigated and morphologically described. In the present paper, the MRM callus ethanolic Extract (MRME) was prepared from one of the 2022 callus sub-cultures and analysed by GC-MS and GC-FID. The investigation was carried out to test whether a long-term culture could affect either the amount or the bioactivity (or both) of the triterpenes produced by the callus. To this aim, the 2022 extract (MRME 2022) was compared to the extract prepared a few years ago (i.e., MRME 2019). Obtained results showed that the composition of both extracts was almost the same, thus revealing that the callus culture efficiency of triterpenes production was nearly unchanged over time. When analysing the biological effect of the extract, all experimental tests, including cell-free, in vitro, ex vivo, and in vivo assays, confirmed that MRME 2022 significantly protected cells, tissues, or whole organisms from oxidative stress-induced damage. Present results could lead to future studies to test MRME as a possible ingredient of a nutraceutical formulation for healthy aging or for the prevention of oxidative stress-associated pathologies.
As a follow-up to our previous studies on glycolipid surfactants, a new molecule, that is lactose 6′-O-undecylenate (URB1418), was investigated. To this end, a practical synthesis and studies aimed ...at exploring its specific properties were carried out. URB1418 showed antifungal activities against Trichophyton rubrum F2 and Candida albicans ATCC 10231 (MIC 512 μg/mL) and no significant antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa. At the same time, it presented anti-inflammatory properties, as documented by the dose-dependent reduction in LPS-induced NO release in RAW 264.7 cells, while a low antioxidant capacity in the range of concentrations tested (EC50 > 200 µM) was also observed. Moreover, URB1418 offers the advantage of being more stable than the reference polyunsaturated lactose esters and of being synthesized using a “green” procedure, involving an enzymatic method, high yield and low manufacturing cost. For all these reasons and the absence of toxicity (HaCaT cells), the new glycolipid presented herein could be considered an interesting compound for applications in various fields.
Nutritional habits can have a significant impact on cardiovascular health and disease. This may also apply to cardiotoxicity caused as a frequent side effect of chemotherapeutic drugs, such as ...doxorubicin (DXR). The aim of this work was to analyze if diet, in particular creatine (Cr) supplementation, can modulate cardiac biochemical (energy status, oxidative damage and antioxidant capacity, DNA integrity, cell signaling) and functional parameters at baseline and upon DXR treatment. Here, male Wistar rats were fed for 4 weeks with either standard rodent diet (NORMAL), soy-based diet (SOY), or Cr-supplemented soy-based diet (SOY + Cr). Hearts were either freeze-clamped in situ or following ex vivo Langendorff perfusion without or with 25 μM DXR and after recording cardiac function. The diets had distinct cardiac effects. Soy-based diet (SOY vs. NORMAL) did not alter cardiac performance but increased phosphorylation of acetyl-CoA carboxylase (ACC), indicating activation of rather pro-catabolic AMP-activated protein kinase (AMPK) signaling, consistent with increased ADP/ATP ratios and lower lipid peroxidation. Creatine addition to the soy-based diet (SOY + Cr vs. SOY) slightly increased left ventricular developed pressure (LVDP) and contractility dp/dt, as measured at baseline in perfused heart, and resulted in activation of the rather pro-anabolic protein kinases Akt and ERK. Challenging perfused heart with DXR, as analyzed across all nutritional regimens, deteriorated most cardiac functional parameters and also altered activation of the AMPK, ERK, and Akt signaling pathways. Despite partial reprogramming of cell signaling and metabolism in the rat heart, diet did not modify the functional response to supraclinical DXR concentrations in the used acute cardiotoxicity model. However, the long-term effect of these diets on cardiac sensitivity to chronic and clinically relevant DXR doses remains to be established.
Apples are rich in phytochemicals useful for human health. However, environmental factors can greatly affect the accumulation of these compounds. To face this problem, the callus culture technique ...was used to obtain large quantities of phytochemicals. Specifically, two callus cultures were obtained from ripe Annurca apple pulp (Malus pumila cv Miller) and cultivated under different light conditions: darkness and an 18-h photoperiod. The hydro-alcoholic extracts from the calli underwent analysis using GC-MS, GC-FID, and HPLC-DAD-ESI-MSn to determine the qualitative and quantitative content of phenolic and triterpenic acids. The study revealed the predominant presence of triterpenic compounds in both calli. Furthermore, we investigated their radical scavenging and antioxidant activities through DPPH, ABTS, ORAC assays, and lipoxygenase inhibition activity. Genoprotection was evaluated via nicking assay, and the anti-inflammatory effect was investigated via Griess assay on LPS-injured murine macrophages. All the analyses performed were compared with peel and pulp hydroalcoholic extracts. The results showed that both calli primarily show anti-inflammatory activity and moderate antioxidant effect and can protect DNA against oxidative stimuli. This data encouraged further research aimed at utilizing callus as a bioreactor to produce secondary metabolites for use in preventive and therapeutic applications to combat acute or chronic age-associated diseases.
The pharmacological activity of a callus extract from the pulp of
Mill., also known as quince, was investigated in murine macrophage (RAW 264.7) and human keratinocyte (HaCaT) cell lines. In ...particular, the anti-inflammatory activity of
Mill. pulp callus extract was assessed in lipopolysaccharides (LPS)-treated RAW 264.7 by the Griess test and in LPS-treated HaCaT human keratinocytes by examining the expression of genes involved in the inflammatory process, including nitric oxide synthase (iNOS), interleukin-6 (IL-6), interleukin-1β (IL-1β), nuclear factor-kappa-B inhibitor alfa (ikBα), and intercellular adhesion molecule (ICAM). The antioxidant activity was evaluated by quantizing the reactive oxygen species (ROS) production in the hydrogen peroxide and tert-butyl hydroperoxide-injured HaCaT cell line. The obtained results indicate that
callus from fruit pulp extract has anti-inflammatory and antioxidant activities, suggesting its possible application in delaying and preventing acute or chronic diseases associated with aging or in the treatment of wound dressing.
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