scholarly journals Ursolic and Oleanolic Acids: Plant Metabolites with Neuromodulatory Potential

Author(s):  
Evelina Gudoityte ◽  
Odeta Arandarcikaite ◽  
Ingrida Mazeikiene ◽  
Vidmantas Bendokas ◽  
Julius Liobikas

Ursolic and oleanolic acids are secondary plant metabolites that are known to be involved in the plant defence system against water loss and pathogens. Nowadays these triterpenoids are also regarded as potential pharmaceutical compounds and there is mounting experimental data that either purified compounds or triterpenoid-enriched plant extracts exert various beneficial effects, including anti-oxidative, anti-inflammatory and anticancer, on model systems of both human or animal origin. Some of those effects have been linked to the ability of ursolic and oleanolic acids to modulate intracellular antioxidant systems and also inflammation- and cell death-related pathways. Therefore, our aim was to review the current knowledge about the distribution of ursolic and oleanolic acids in plants, bioavailability and pharmacokinetic properties of these triterpenoids and their derivatives, and to discuss their neuromodulatory effects in vitro and in vivo.

2021 ◽  
Vol 22 (9) ◽  
pp. 4599
Author(s):  
Evelina Gudoityte ◽  
Odeta Arandarcikaite ◽  
Ingrida Mazeikiene ◽  
Vidmantas Bendokas ◽  
Julius Liobikas

Ursolic and oleanolic acids are secondary plant metabolites that are known to be involved in the plant defence system against water loss and pathogens. Nowadays these triterpenoids are also regarded as potential pharmaceutical compounds and there is mounting experimental data that either purified compounds or triterpenoid-enriched plant extracts exert various beneficial effects, including anti-oxidative, anti-inflammatory and anticancer, on model systems of both human or animal origin. Some of those effects have been linked to the ability of ursolic and oleanolic acids to modulate intracellular antioxidant systems and also inflammation and cell death-related pathways. Therefore, our aim was to review current studies on the distribution of ursolic and oleanolic acids in plants, bioavailability and pharmacokinetic properties of these triterpenoids and their derivatives, and to discuss their neuroprotective effects in vitro and in vivo.


2016 ◽  
Vol 4 (6) ◽  
pp. 307-310
Author(s):  
Dhwani T. Dave ◽  
◽  
Gaurang B. Shah ◽  

Since ancient times, plants have been serving as a promising source of medicines and in recent times, extensive research has been made to isolate, characterize and screen a number of phytoconstituents/secondary plant metabolites for their pharmacological activities and safety in various disease models – both in vitro and in vivo. One such category of phytoconstituents is “polysaccharides”. These are found in different parts of the plant such as roots, leaves, stem and leaves and are extracted maximally in polar solvent – for eg. water extract of the afore mentioned plant parts contain the crude polysaccharide fraction. These are non-starch type in nature and can be a mixture of more than one type of polysaccharide too. In this review, an attempt has been made to discuss such therapeutically active plant polysaccharides in terms of their wide pharmacologically active profile along with methods to isolate and characterize them in brief.


2018 ◽  
Vol 25 (10) ◽  
pp. 1094-1159 ◽  
Author(s):  
Viliam Brezani ◽  
Karel Smejkal ◽  
Jan Hosek ◽  
Veronika Tomasova

Background: Natural phenolics are secondary plant metabolites, which can be divided into several categories with the common structural feature of phenolic hydroxyl. The biological activity of phenolics is often modified and enhanced by prenylation by prenyl and geranyl; higher terpenoid chains are rare. The type of prenyl connection and modification affects their biological activity. Objective: This review summarizes information about prenylated phenols and some of their potential sources, and provides an overview of their anti-inflammatory potential in vitro and in vivo. Method: The literature search was performed using SciFinder and keywords prenyl, phenol, and inflammation. For individual compounds, an additional search was performed to find information about further activities and mechanisms of effects. Result: We summarized the effects of prenylated phenolics in vitro in cellular or biochemical systems on the production and release of inflammation-related cytokines; their effects on inhibition of cyclooxygenases and lipoxygenases; the effects on production of nitric oxide, antiradical and antioxidant activity; and the effect on the inhibition of the release of enzymes and mediators from neutrophils, mast cells and macrophages. The information about the antiphlogistic potential of prenylated phenolics is further supported by a review of their action in animal models. Conclusion: Almost 400 prenylated phenols were reviewed to overview their antiinflammatory effect. The bioactivity of several prenylated phenols was confirmed also using in vivo assays. A pool of natural prenylated phenols represents a source of inspiration for synthesis, and prenylated phenols as components of various medicinal plants used to combat inflammation could be their active principles.


Nutrients ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 4025
Author(s):  
Linda Nezbedova ◽  
Tony McGhie ◽  
Mark Christensen ◽  
Julian Heyes ◽  
Noha Ahmed Nasef ◽  
...  

Cancer is one of the leading causes of death globally. Epidemiological studies have strongly linked a diet high in fruits to a lower incidence of cancer. Furthermore, extensive research shows that secondary plant metabolites known as phytochemicals, which are commonly found in fruits, have onco-preventive and chemo-protective effects. Apple is a commonly consumed fruit worldwide that is available all year round and is a rich source of phytochemicals. In this review, we summarize the association of apple consumption with cancer incidence based on findings from epidemiological and cohort studies. We further provide a comprehensive review of the main phytochemical patterns observed in apples and their bioavailability after consumption. Finally, we report on the latest findings from in vitro and in vivo studies highlighting some of the key molecular mechanisms targeted by apple phytochemicals in relation to inhibiting multiple ‘hallmarks of cancer’ that are important in the progression of cancer.


Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6559
Author(s):  
Ahmed A. Al-Karmalawy ◽  
Mai M. Farid ◽  
Ahmed Mostafa ◽  
Alia Y. Ragheb ◽  
Sara H. Mahmoud ◽  
...  

Flavonoids are important secondary plant metabolites that have been studied for a long time for their therapeutic potential in inflammatory diseases because of their cytokine-modulatory effects. Five flavonoid aglycones were isolated and identified from the hydrolyzed aqueous methanol extracts of Anastatica hierochuntica L., Citrus reticulata Blanco, and Kickxia aegyptiaca (L.) Nabelek. They were identified as taxifolin (1), pectolinarigenin (2), tangeretin (3), gardenin B (4), and hispidulin (5). These structures were elucidated based on chromatographic and spectral analysis. In this study, molecular docking studies were carried out for the isolated and identified compounds against SARS-CoV-2 main protease (Mpro) compared to the co-crystallized inhibitor of SARS-CoV-2 Mpro (α-ketoamide inhibitor (KI), IC50 = 66.72 µg/mL) as a reference standard. Moreover, in vitro screening against SARS-CoV-2 was evaluated. Compounds 2 and 3 showed the highest virus inhibition with IC50 12.4 and 2.5 µg/mL, respectively. Our findings recommend further advanced in vitro and in vivo studies of the examined isolated flavonoids, especially pectolinarigenin (2), tangeretin (3), and gardenin B (4), either alone or in combination with each other to identify a promising lead to target SARS-CoV-2 effectively. This is the first report of the activity of these compounds against SARS-CoV-2.


Blood ◽  
2004 ◽  
Vol 104 (11) ◽  
pp. 2101-2101
Author(s):  
Michael D. Milsom ◽  
Laura Hollins ◽  
Dorothy Gagen ◽  
Lorna B. Woolford ◽  
Leslie J. Fairbairn

Abstract We have recently demonstrated that co-expression of HOXB4 enables the enhanced delivery of HSC harbouring a second therapeutic trans-gene. Nonetheless, it is of great importance to elaborate the current knowledge about the mechanism of HOXB4 action in order to both evaluate the safety implications of its use in a clinical strategy, and to gain greater insight into the regulation of HSC self-renewal/expansion. To these ends we have performed an extensive in vitro analysis of the consequences of HOXB4 overexpression in primary murine BMC and in a murine multipotent myeloid progenitor cell line (FDCP-mix). We demonstrate for the first time in murine cells, that ectopic HOXB4 reduces the responsiveness of murine hematopoietic cells to differentiation stimuli. Furthermore, by performing a detailed investigation into the kinetics of FDCP-mix differentiation, we reveal that HOXB4 overexpression results in a specific differentiation delay as opposed to an outright block. We propose that an analogous delay is in operation in repopulating cells in order that the shift to increased assymetrical self-renewal, a requirement for stem cell expansion, is achieved. Notwithstanding this, it is clear that any perturbation in differentiation constitutes an increased risk of cellular transformation if this technology were transferred to a clinical setting. In order to further define the repercussions of ectopic HOXB4 delivery, we have developed a retroviral vector which encodes an activatable version of HOXB4. We have shown that this vector is able to mediate an in vitro differentiation delay in primary murine BMC and FDCP-mix as well as enable enhanced engraftment of BMC in vivo, both dependent upon the addition of the estrogen analogue; tamoxifen. Using this system, we are currently examining the effect of ectopic HOXB4 on the transcriptome of FDCP-mix cells, in addition to performing an in depth study into the biological mechanisms affected by HOXB4 overexpression in BMC in vivo. We envisage that these model systems will be particularly amenable to the manipulation required for target gene identification/validation.


2020 ◽  
Vol 21 (24) ◽  
pp. 9373
Author(s):  
Binod Prasad ◽  
Daniela Grimm ◽  
Sebastian M. Strauch ◽  
Gilmar Sidnei Erzinger ◽  
Thomas J. Corydon ◽  
...  

All life forms have evolved under the constant force of gravity on Earth and developed ways to counterbalance acceleration load. In space, shear forces, buoyance-driven convection, and hydrostatic pressure are nullified or strongly reduced. When subjected to microgravity in space, the equilibrium between cell architecture and the external force is disturbed, resulting in changes at the cellular and sub-cellular levels (e.g., cytoskeleton, signal transduction, membrane permeability, etc.). Cosmic radiation also poses great health risks to astronauts because it has high linear energy transfer values that evoke complex DNA and other cellular damage. Space environmental conditions have been shown to influence apoptosis in various cell types. Apoptosis has important functions in morphogenesis, organ development, and wound healing. This review provides an overview of microgravity research platforms and apoptosis. The sections summarize the current knowledge of the impact of microgravity and cosmic radiation on cells with respect to apoptosis. Apoptosis-related microgravity experiments conducted with different mammalian model systems are presented. Recent findings in cells of the immune system, cardiovascular system, brain, eyes, cartilage, bone, gastrointestinal tract, liver, and pancreas, as well as cancer cells investigated under real and simulated microgravity conditions, are discussed. This comprehensive review indicates the potential of the space environment in biomedical research.


2016 ◽  
Vol 17 (2) ◽  
pp. 85-91 ◽  
Author(s):  
Isaiah Oluwafemi Ademola

AbstractBioactive compounds from marine and terrestrial organisms have been used extensively in the treatment of many diseases in both their natural form and as templates for synthetic modifications. This review summarizes present knowledge about anthelmintic effects of the extracts of bioactive plants in Nigeria against helminth parasites of ruminants. Plants traditionally used in livestock production are discussed. The main focus is hinged on in vitro and in vivo activities of secondary plant metabolites against nematodes of livestock. This review provides insight into preliminary studies of medicinal plants, which can be investigated further to discover promising molecules in the search for novel anthelmintic drugs and nutraceuticals.


Plants ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 1252
Author(s):  
Mariangela Marrelli ◽  
Valentina Amodeo ◽  
Maria Rosaria Perri ◽  
Filomena Conforti ◽  
Giancarlo Statti

Essential oils (EOs) are known to possess a number of beneficial properties. Their antimicrobial, anti-inflammatory, antioxidant, antidiabetic, and cancer-preventing activities have been extensively reported. Due to their wide use as food preservers and additives, as well as their use in agriculture, perfumes, and make-up products, these complex mixtures of volatile compounds have gained importance from a commercial point of view, not only in the pharmaceutical industry, but also in agronomic, food, cosmetic, and perfume industries. An analysis of the recent scientific literature allowed us to highlight the presence of an increasing number of studies on the potential antiarthritic properties of EOs and their main constituents, which seems to suggest a new interesting potential therapeutic application. The aim of this review is to examine the current knowledge on the beneficial effects of essential oils in the treatment of arthritic diseases, providing an overview of the reports on the in vivo and in vitro effects of EOs. Furthermore, this review critically examines the recent findings on the potential roles of the main components of EOs in the exerted beneficial effects. Obtained negative results are also reported.


2021 ◽  
Vol 9 (8) ◽  
pp. 1599
Author(s):  
Nanci Santos-Ferreira ◽  
Jana Van Dycke ◽  
Johan Neyts ◽  
Joana Rocha-Pereira

Acute gastroenteritis caused by virus has a major impact on public health worldwide in terms of morbidity, mortality, and economic burden. The main culprits are rotaviruses, noroviruses, sapoviruses, astroviruses, and enteric adenoviruses. Currently, there are no antiviral drugs available for the prevention or treatment of viral gastroenteritis. Here, we describe the antivirals that were identified as having in vitro and/or in vivo activity against these viruses, originating from in silico design or library screening, natural sources or being repurposed drugs. We also highlight recent advances in model systems available for this (hard to cultivate) group of viruses, such as organoid technologies, and that will facilitate antiviral studies as well as fill some of current knowledge gaps that hamper the development of highly efficient therapies against gastroenteric viruses.


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