scholarly journals Constitutive and Regulated Shedding of Soluble FGF Receptors Releases Biologically Active Inhibitors of FGF-2

2021 ◽  
Vol 22 (5) ◽  
pp. 2712
Author(s):  
Anne Hanneken ◽  
Maluz Mercado ◽  
Pamela Maher
Keyword(s):  
Cell Surface ◽  
Ligand Binding ◽  
Cellular Proliferation ◽  
Biological Activities ◽  
Biological Properties ◽  
Matrix Metalloproteases ◽  
Biologically Active ◽  
Ectodomain Shedding ◽  
High Affinity

The identification of soluble fibroblast growth factor (FGF) receptors in blood and the extracellular matrix has led to the prediction that these proteins modulate the diverse biological activities of the FGF family of ligands in vivo. A recent structural characterization of the soluble FGF receptors revealed that they are primarily generated by proteolytic cleavage of the FGFR-1 ectodomain. Efforts to examine their biological properties are now focused on understanding the functional consequences of FGFR-1 ectodomain shedding and how the shedding event is regulated. We have purified an FGFR-1 ectodomain that is constitutively cleaved from the full-length FGFR-1(IIIc) receptor and released into conditioned media. This shed receptor binds FGF-2; inhibits FGF-2-induced cellular proliferation; and competes with high affinity, cell surface FGF receptors for ligand binding. FGFR-1 ectodomain shedding downregulates the number of high affinity receptors from the cell surface. The shedding mechanism is regulated by ligand binding and by activators of PKC, and the two signaling pathways appear to be independent of each other. Deletions and substitutions at the proposed cleavage site of FGFR-1 do not prevent ectodomain shedding. Broad spectrum inhibitors of matrix metalloproteases decrease FGFR-1 ectodomain shedding, suggesting that the enzyme responsible for constitutive, ligand-activated, and protein kinase C-activated shedding is a matrix metalloprotease. In summary, shedding of the FGFR-1 ectodomain is a highly regulated event, sharing many features with a common system that governs the release of diverse membrane proteins from the cell surface. Most importantly, the FGFR ectodomains are biologically active after shedding and are capable of functioning as inhibitors of FGF-2.

scholarly journals In vitro and in vivo biological activities of azulene derivatives with potential applications in medicine

2021 ◽  
Author(s):  
Paweł Bakun ◽  
Beata Czarczynska-Goslinska ◽  
Tomasz Goslinski ◽  
Sebastian Lijewski
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Peptic Ulcers ◽  
Artemisia Absinthium ◽  
Potential Applications ◽  
Anti Inflammatory ◽  
Unique Chemical

AbstractAzulene is an aromatic hydrocarbon that possesses a unique chemical structure and interesting biological properties. Azulene derivatives, including guaiazulene or chamazulene, occur in nature as components of many plants and mushrooms, such as Matricaria chamomilla, Artemisia absinthium, Achillea millefolium, and Lactarius indigo. Due to physicochemical properties, azulene and its derivatives have found many potential applications in technology, especially in optoelectronic devices. In medicine, the ingredients of these plants have been widely used for hundreds of years in antiallergic, antibacterial, and anti-inflammatory therapies. Herein, the applications of azulene, its derivatives and their conjugates with biologically active compounds are presented. The potential use of these compounds concerns various areas of medicine, including anti-inflammatory with peptic ulcers, antineoplastic with leukemia, antidiabetes, antiretroviral with HIV-1, antimicrobial, including antimicrobial photodynamic therapy, and antifungal.

A comprehensive review on the ethnopharmacology, phytochemistry, ‎pharmacology, and toxicology of the Mandragora genus; from folk ‎medicine to the modern

2021 ◽  
Vol 27 ◽  
Author(s):  
Taha Monadi ◽  
Mohammad Azadbakht ◽  
Amirhossein Ahmadi ◽  
Aroona Chabra
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Extensive Literature ◽  
Traditional Use ◽  
Toxicological Studies ◽  
Persian Medicine

The Mandragora genus (Solanaceae) is well known for its association with myths and has been used in herbal medicine since ancient times. This extensive literature review synthesizes the information currently available on the ethnobotany, Persian medicine (PM), traditional use, phytochemistry, pharmacology, and toxicity profile of Mandragora spp. The electronic search engines Scopus, Web of Science, PubMed, Google Scholar, and ScienceDirect were searched using keywords such as Mandragora, mandrake, phytochemistry, ethnopharmacology, Persian medicine, ethnobotany, and toxicity. Pertinent information was also extracted from books on PM, ethnomedicine, and dissertations. Mandragora species are found throughout the Mediterranean basin, Europe, Northern Africa, and the Himalayan regions. Traditionally, the species have been used to treat insomnia, dysuria, hemorrhoids, rheumatic pain, toothache, melancholia, and depression, among many others. In vitro studies have confirmed the biological properties of Mandragora spp. crude extracts, such as antioxidant, immunomodulatory, and enzyme-inhibiting effects. Various phytochemicals, such as alkaloids (e.g., atropine and scopolamine), coumarins (e.g., umbelliferone and scopoletin), withanolides (e.g., salpichrolide C), and lipid-like compounds (e.g., beta-sitosterol), have been isolated from Mandragora spp. Some of the pure compounds composing this plant are highlighted for their biologically active effects, including anticholinergic, antidepressant, antioxidant, and anti-inflammatory effects. Modern identifications of biological activities of the compounds isolated from Mandragora, especially alkaloids, support its traditional uses (e.g., for their narcotic effects). More in vivo studies are required to further understanding and most effectively utilize this genus, and extensive toxicological studies are required to validate its safety in clinical use.

scholarly journals Linalool – a Review of a Biologically Active Compound of Commercial Importance

2008 ◽  
Vol 3 (7) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Guy P. P. Kamatou ◽  
Alvaro M. Viljoen
Keyword(s):  
Essential Oils ◽  
Biological Activities ◽  
Modern Society ◽  
Biological Properties ◽  
Biologically Active ◽  
In Vivo Studies ◽  
The Central Nervous System ◽  
Anti Oxidant ◽  
Domestic Products

Since the earliest times fragrant materials have been used in rituals. Today, a lucrative industry has developed to produce and deliver fragrances and aromatic chemicals with various applications in modern society. Linalool, a much sought after compound in the flavor and fragrance industry is a monoterpene alcohol which occurs naturally in many aromatic plants. Linalool and linalool-rich essential oils are known to exhibit various biological activities such as antimicrobial, anti-inflammatory, anticancer, anti-oxidant properties and several in vivo studies have confirmed various effects of linalool on the central nervous system. The applications of linalool are not confined to simply adding or enhancing a specific scent to domestic products such as soaps, detergents and shampoos. Linalool also plays an import role in nature as a key compound in the complex pollination biology of various plant species to ensure reproduction and survival. Linalool is also a key compound for the industrial production of a variety of fragrance chemicals such as geraniol, nerol, citral and its derivatives, as well as a lead compound in the synthesis of vitamins A and E. The repellent properties of linalool on various crop-destroying insects has been well documented accentuating the application of this molecule in eco-friendly pest management. This review aims to highlight the various biological properties of linalool and to emphasize the value of linalool and linalool-rich essential oils in phytotherapy.

Metabolomics of Healthy Berry Fruits

2019 ◽  
Vol 25 (37) ◽  
pp. 4888-4902 ◽  
Author(s):  
Gilda D'Urso ◽  
Sonia Piacente ◽  
Cosimo Pizza ◽  
Paola Montoro
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Bioactive Metabolites ◽  
Active Metabolites ◽  
Positive Effects ◽  
Cell Functions ◽  
Berry Fruits

The consumption of berry-type fruits has become very popular in recent years because of their positive effects on human health. Berries are in fact widely known for their health-promoting benefits, including prevention of chronic disease, cardiovascular disease and cancer. Berries are a rich source of bioactive metabolites, such as vitamins, minerals, and phenolic compounds, mainly anthocyanins. Numerous in vitro and in vivo studies recognized the health effects of berries and their function as bioactive modulators of various cell functions associated with oxidative stress. Plants have one of the largest metabolome databases, with over 1200 papers on plant metabolomics published only in the last decade. Mass spectrometry (MS) and NMR (Nuclear Magnetic Resonance) are the most important analytical technologies on which the emerging ''omics'' approaches are based. They may provide detection and quantization of thousands of biologically active metabolites from a tissue, working in a ''global'' or ''targeted'' manner, down to ultra-trace levels. In the present review, we highlighted the use of MS and NMR-based strategies and Multivariate Data Analysis for the valorization of berries known for their biological activities, important as food and often used in the preparation of nutraceutical formulations.

Tamarix articulata (T. articulata) - An Important Halophytic Medicinal Plant with Potential Pharmacological Properties

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
In Vivo Model ◽  
Drug Candidate ◽  
Phytochemical Analysis ◽  
Pharmacological Properties

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.

The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

2019 ◽  
Vol 16 (7) ◽  
pp. 953-967 ◽  
Author(s):  
Ghodsi M. Ziarani ◽  
Fatemeh Mohajer ◽  
Razieh Moradi ◽  
Parisa Mofatehnia
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Microtubule Assembly ◽  
Heterocyclic Molecules ◽  
Biological Perspective ◽  
Highly Active ◽  
Anti Inflammatory ◽  
High Yields ◽  
Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

scholarly journals Buprenorphine Metabolites, Buprenorphine-3-glucuronide and Norbuprenorphine-3-glucuronide, Are Biologically Active

2011 ◽  
Vol 115 (6) ◽  
pp. 1251-1260 ◽  
Author(s):  
Sarah M. Brown ◽  
Michael Holtzman ◽  
Thomas Kim ◽  
Evan D. Kharasch
Keyword(s):  
Radioligand Binding ◽  
Competitive Inhibition ◽  
Antinociceptive Effect ◽  
Plasma Concentrations ◽  
Parent Drug ◽  
Biologically Active ◽  
Whole Body ◽  
Tail Flick ◽  
High Affinity

Background The long-lasting high-affinity opioid buprenorphine has complex pharmacology, including ceiling effects with respect to analgesia and respiratory depression. Plasma concentrations of the major buprenorphine metabolites norbuprenorphine, buprenorphine-3-glucuronide, and norbuprenorphine-3-glucuronide approximate or exceed those of the parent drug. Buprenorphine glucuronide metabolites pharmacology is undefined. This investigation determined binding and pharmacologic activity of the two glucuronide metabolites, and in comparison with buprenorphine and norbuprenorphine. Methods Competitive inhibition of radioligand binding to human μ, κ, and δ opioid and nociceptin receptors was used to determine glucuronide binding affinities for these receptors. Common opiate effects were assessed in vivo in SwissWebster mice. Antinociception was assessed using a tail-flick assay, respiratory effects were measured using unrestrained whole-body plethysmography, and sedation was assessed by inhibition of locomotion measured by open-field testing. Results Buprenorphine-3-glucuronide had high affinity for human μ (Ki [inhibition constant] = 4.9 ± 2.7 pM), δ (Ki = 270 ± 0.4 nM), and nociceptin (Ki = 36 ± 0.3 μM) but not κ receptors. Norbuprenorphine-3-glucuronide had affinity for human κ (Ki = 300 ± 0.5 nM) and nociceptin (Ki = 18 ± 0.2 μM) but not μ or δ receptors. At the dose tested, buprenorphine-3-glucuronide had a small antinociceptive effect. Neither glucuronide had significant effects on respiratory rate, but norbuprenorphine-3-glucuronide decreased tidal volume. Norbuprenorphine-3-glucuronide also caused sedation. Conclusions Both glucuronide metabolites of buprenorphine are biologically active at doses relevant to metabolite exposures, which occur after buprenorphine. Activity of the glucuronides may contribute to the overall pharmacology of buprenorphine.

Sixty Years Young: The Diverse Biological Activities of Metal Polypyridyl Complexes Pioneered by Francis P. Dwyer

2012 ◽  
Vol 65 (9) ◽  
pp. 1325 ◽  
Author(s):  
Nathan L. Kilah ◽  
Eric Meggers
Keyword(s):  
Inorganic Chemistry ◽  
Biological Activities ◽  
Biologically Active ◽  
Ruthenium Polypyridyl ◽  
Polypyridyl Complexes ◽  
Anti Cancer ◽  
Ruthenium Polypyridyl Complexes ◽  
Medicinal Inorganic Chemistry ◽  
Sixtieth Anniversary

Sixty years ago, the Australian chemist Francis P. Dwyer pioneered the use of ruthenium polypyridyl complexes as biologically active compounds. These chemically inert and configurationally stable complexes revealed an astonishing range of interesting biological activities, such as the inhibition of the enzyme acetylcholinesterase, anti-cancer activity in vivo, and bacteriostatic/bacteriocidal action. This review commemorates the sixtieth anniversary of Dwyer and co-workers’ landmark 1952 publication, summarises their broader achievements in biological inorganic chemistry, and discusses the contribution of this work to the development of modern biological and medicinal inorganic chemistry.

Przeciwnowotworowe działanie składników propolisu. Cz. 1. Ester fenyloetylowy kwasu kawowego (CAPE)

2020 ◽  
Vol 21 (3) ◽  
Author(s):  
Bogdan Kędzia ◽  
Elżbieta Hołderna-Kędzia
Keyword(s):  
Human Colon ◽  
Caffeic Acid Phenethyl Ester ◽  
Biological Properties ◽  
Biologically Active ◽  
Significant Activity ◽  
Colon Adenoma ◽  
Cancer Cell Survival ◽  
Ht 29

The paper presents a review of the publications on the anticancerogenic activity of the biologically active component of propolis – caffeic acid phenethyl ester (CAPE). Literature data indicate numerous biological properties of CAPE, namely: antioxidant, anti-inflammatory, antiviral, immunostimulatory, anti-angiogenic and others. In numerous tests, both in vitro and in vivo, the significant activity of CAPE has been confirmed, including an action against HT-29 human colon adenoma cells, and five: human, murine and other tumor cell cultures. The authors also emphasize that CAPE supports the anticancerogenic effect of drugs, including doxorubicin and cisplatin, due to the reduction of cancer cell survival by 45% and 34%, respectively, compared to the above-mentioned drugs used alone. The conducted research indicates that the induction of apoptosis in cells, i.e. programmed cell death, can be mentioned among the main mechanisms of the anticancerogenic activity of CAPE.

scholarly journals Chromatographic Analyses, In Vitro Biological Activities, and Cytotoxicity of Cannabis sativa L. Essential Oil: A Multidisciplinary Study

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3266 ◽  
Author(s):  
Gokhan Zengin ◽  
Luigi Menghini ◽  
Antonella Di Sotto ◽  
Romina Mancinelli ◽  
Francesca Sisto ◽  
...  
Keyword(s):  
Essential Oil ◽  
Galleria Mellonella ◽  
Cannabis Sativa ◽  
Biological Activities ◽  
Methodological Approach ◽  
Volatile Component ◽  
Biologically Active ◽  
Antioxidant Compounds

Due to renewed interest in the cultivation and production of Italian Cannabis sativa L., we proposed a multi-methodological approach to explore chemically and biologically both the essential oil and the aromatic water of this plant. We reported the chemical composition in terms of cannabinoid content, volatile component, phenolic and flavonoid pattern, and color characteristics. Then, we demonstrated the ethnopharmacological relevance of this plant cultivated in Italy as a source of antioxidant compounds toward a large panel of enzymes (pancreatic lipase, α-amylase, α-glucosidase, and cholinesterases) and selected clinically relevant, multidrug-sensible, and multidrug-resistant microbial strains (Staphylococcus aureus, Helicobacter pylori, Candida, and Malassezia spp.), evaluating the cytotoxic effects against normal and malignant cell lines. Preliminary in vivo cytotoxicity was also performed on Galleria mellonella larvae. The results corroborate the use of this natural product as a rich source of important biologically active molecules with particular emphasis on the role exerted by naringenin, one of the most important secondary metabolites.

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