Calixarenes (CAs) are promising in biomedicine, biosensing, bioimaging and gene delivery systems

2021 ◽  
Author(s):  
Moataz Dowaidar
Keyword(s):  
Gene Delivery ◽  
Supramolecular Chemistry ◽  
Biological Activities ◽  
Molecular Structures ◽  
Biological Applications ◽  
Ongoing Research ◽  
Biological Potential ◽  
Wide Range

Calixarenes (CAs) are widely employed in biomedicine, e.g. biosensing and bioimaging, and contributed to in vivo and in vitro diagnostics. CAs were also employed to construct medication and gene delivery devices that helped create targeted treatments. CAs' ability to inhibit antibacterial, antiviral, anticancer, detoxifying, and amyloid fibrillation also aids in the development of macrocyclic therapies.Because of their ease of modification, CAs' rich (supramolecular) chemistry and their extensive chemical design space benefit such a wide range of medicinal applications. CAs' supramolecular chemistry permits studying biological functions. CAs have unique recognition properties as its cavity can identify and quench many dyes' fluorescence and photoactivity, making them excellent for turn-on fluorescence sensing, imaging, and activatable PDT. CA skeleton may also be utilized as a podand-like ligand to develop novel recognition systems. CAs are also skilled at assembling things. While these early investigations highlighted the biological potential of CA homologues for biosensing, bioimaging, drug/gene delivery, and therapy, there are currently few examples of clinical CA application. CAs' bench-to-bedside translation in biological applications is highly demanded. One CA is undertaking a phase I clinical study, a good indicator. However, from both scientific research and clinical trials, CAs still confront significant practical hurdles in biological applications. To make biosensing applications practicable in clinical settings, sensing systems need to be further developed into sensors or even in-vitro diagnostic kits. In vivo diagnosis and therapy More CA safety investigations including long-term toxicity effects, metabolic pathways, and immune reactions are needed. Some advanced modalities can be employed and explored to improve diagnostic and therapeutic performance, such as multimodal imaging, multiple targeting, and combination therapy. Moreover, despite the huge number of CA derivatives described, their physicochemical features and biological roles remain unclear. Exploring the novel functionalities of existing CAs is crucial, taking the combined efforts of diverse specialists from the domains of supramolecular chemistry, chemical biology, life sciences, pharmacy, and medicine. We believe that ancient molecules can still be employed for various new tricks. This can summarize the underlying link between molecular structures and biological activities to assist drive the creation of novel CA derivatives. We anticipate that CA-based biomedicine will deliver considerable benefits in the near future with ongoing research and development.

Associated microflora of medicinal ferns: biotechnological potentials and possible applications

2016 ◽  
Vol 5 (03) ◽  
pp. 4927 ◽  
Author(s):  
Shubhi Srivastava ◽  
Paul A. K.
Keyword(s):  
Secondary Metabolites ◽  
Growth Promotion ◽  
Biological Activities ◽  
Hydrolytic Enzymes ◽  
In Vitro Production ◽  
Wide Range ◽  
Negative Effect ◽  
Bacteria And Fungi

Plant associated microorganisms that colonize the upper and internal tissues of roots, stems, leaves and flowers of healthy plants without causing any visible harmful or negative effect on their host. Diversity of microbes have been extensively studied in a wide variety of vascular plants and shown to promote plant establishment, growth and development and impart resistance against pathogenic infections. Ferns and their associated microbes have also attracted the attention of the scientific communities as sources of novel bioactive secondary metabolites. The ferns and fern alleles, which are well adapted to diverse environmental conditions, produce various secondary metabolites such as flavonoids, steroids, alkaloids, phenols, triterpenoid compounds, variety of amino acids and fatty acids along with some unique metabolites as adaptive features and are traditionally used for human health and medicine. In this review attention has been focused to prepare a comprehensive account of ethnomedicinal properties of some common ferns and fern alleles. Association of bacteria and fungi in the rhizosphere, phyllosphere and endosphere of these medicinally important ferns and their interaction with the host plant has been emphasized keeping in view their possible biotechnological potentials and applications. The processes of host-microbe interaction leading to establishment and colonization of endophytes are less-well characterized in comparison to rhizospheric and phyllospheric microflora. However, the endophytes are possessing same characteristics as rhizospheric and phyllospheric to stimulate the in vivo synthesis as well as in vitro production of secondary metabolites with a wide range of biological activities such as plant growth promotion by production of phytohormones, siderophores, fixation of nitrogen, and phosphate solubilization. Synthesis of pharmaceutically important products such as anticancer compounds, antioxidants, antimicrobials, antiviral substances and hydrolytic enzymes could be some of the promising areas of research and commercial exploitation.

scholarly journals IN VITRO CALLUS INDUCTION AND COMPARATIVE GC-MS ANALYSIS OF METHANOLIC EXTRACTS OF CALLUS AND LEAF SAMPLES OF AMPELOCISSUS LATIFOLIA (ROXB.) PLANCH

2018 ◽  
Vol 10 (9) ◽  
pp. 68
Author(s):  
Deep Chhavi Anand ◽  
Rishikesh Meena ◽  
Vidya Patni
Keyword(s):  
Callus Induction ◽  
Culture Media ◽  
Biological Activities ◽  
Gas Chromatography Mass Spectrometry ◽  
Dodecanoic Acid ◽  
Stem Explants ◽  
Ms Analysis ◽  
Wide Range

Objective: The aim of the present study was to develop a callus induction protocol and comparative study of therapeutic phytochemicals present in in vivo leaf and in vitro callus extracts through Gas Chromatography-Mass Spectrometry analysis.Methods: Murashige and Skoog media was used as culture media for callus induction. In vitro callus induction protocol was developed by studying the effects of various plant growth regulators like auxin, 2, 4-D (2,4-dichlorophenoxyacetic acid), NAA (naphthalic acetic acid), alone and in combination with cytokinin BAP (benzyl aminopurine), on leaf and stem explants. The GC-MS analysis of Ampelocissus latifolia was carried out on Shimadzu QP-2010 plus with thermal desorption system TD 20 to study the phytochemical profile.Results: In vitro callus induction protocol was developed for the plant and callusing was done from leaf and stem explants of Ampelocissus latifolia. The best result for callus induction was obtained using leaf explant, and callus production were maximum in Murashige and Skoog medium fortified with BAP (0.5 mg/l) and NAA (1.0 mg/l). Major compounds identified in the GC-MS analysis were Campesterol, Stigmasterol, Beta-Sitosterol, Docosanol, Dodecanoic acid, etc., in in vitro extract and Beta Sitosterol, Tocopherol, Squalene, Bergamot oil, Margarinic acid, Hexadecanoic acid, etc., in in vivo extract. The different active phytochemicals identified have been found to possess a wide range of biological activities, thus this analysis forms a basis for the biological characterization and importance of the compounds identified for human benefits.Conclusion: This is the first report on callus induction in Ampelocissus latifolia. From the results obtained through the in vitro callus induction and its comparative GCMS analysis with in vivo extract, it is revealed that Ampelocissus latifolia contains various bioactive compounds that are of importance for phytopharmaceutical uses. The GCMS analysis revealed that the amount of Beta-sitosterol and 5-Hydroxymethylfurfural (HMF) was very high in in vitro extract as compared to in vivo extract.

scholarly journals Anti-Inflammatory and Antinociceptive Activity of Pollen Extract Collected by Stingless Bee Melipona fasciculata

2019 ◽  
Vol 20 (18) ◽  
pp. 4512 ◽  
Author(s):  
Alberto Jorge Oliveira Lopes ◽  
Cleydlenne Costa Vasconcelos ◽  
Francisco Assis Nascimento Pereira ◽  
Rosa Helena Moraes Silva ◽  
Pedro Felipe dos Santos Queiroz ◽  
...  
Keyword(s):  
Native Species ◽  
Biological Activities ◽  
Stingless Bee ◽  
In Vitro Assays ◽  
Pollen Extract ◽  
Biological Potential ◽  
Anti Inflammatory ◽  
Analgesic Activities

The stingless bee, Melipona fasciculata Smith (Apidae, Meliponini), is a native species from Brazil. Their products have high biotechnological potential, however there are no studies about the biological activities of pollen collected by M. fasciculata. In this context, the present study investigated the chemical composition, anti-oxidant, anti-inflammatory, and analgesic activities of hydroethanolic pollen extracts collected by M. fasciculata in three cities in Maranhão State, Brazil. We verified the antioxidant activity of the extracts and inhibitory activity against the cyclooxygenase enzyme using in vitro assays and in allowed to select the extract with higher efficiency to be used on in vivo assays. In these trials, the selected extract showed high anti-inflammatory activity as well as nociceptive effects at central and peripheral level, suggesting that this extract acts on inhibition of histamine release and decreased synthesis of prostaglandins and the in-silico study suggested that polyphenols and acids fatty acids in the extract may be associated with these activities. The results of the present study report the high biological potential of pollen extract and we conclude that the pollen collected by M. fasciculata can be considered as the object of research for new pharmacological alternatives.

Preparation, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Bovine Serum Album Nanoparticles

2011 ◽  
Vol 345 ◽  
pp. 349-354 ◽  
Author(s):  
Jia Lei Li ◽  
Yuan Gang Zu ◽  
Xiu Hua Zhao ◽  
Dong Mei Zhao ◽  
Xiao Qiang Chen ◽  
...  
Keyword(s):  
Bovine Serum ◽  
Biological Activities ◽  
Cardiovascular Effects ◽  
Entrapment Efficiency ◽  
Cross Linking ◽  
Nano Technology ◽  
Beneficial Effects ◽  
Wide Range

Resveratrol (RES) is a naturally occurring triphenolic phytoalexin compound exerting numerous beneficial effects in the organism. It has a wide range of biological activities in vitro as well as in vivo, such as anti-cancer, antioxidant, anti-inflammatory and beneficial cardiovascular effects. But, its low solubility in water led to its poor absorption in vivo and low bioavailability. Bovine serum album (BSA) nanoparticles have emerged as versatile desired carrier systems due to its ready availability, biodegradability, lack of toxicity and immunogenicity with fast development of nano technology. In this study, RES-BSANPS were prepared by a desolvation method and chemical cross-linking with glutaraldehyde successfully. Results controlled conditions (concentration of BSA, 10 mg/ml; pH = 9.0; volume of ethanol, 6 ml; volume of 0.25 % glutaraldehyde, 100 µl; amount of RES, 6.7 mg; cross-linking time, 24 h at room temperature (1 ml/min)) for entrapment efficiency, loading efficiency, mean particle size and zeta potential, were found to be 88.7 %, 39.4 %, 175.4 ± 0.5 nm, -35.93 ± 0.79 mV, respectively.

scholarly journals Exploitation of Cytotoxicity of Some Essential Oils for Translation in Cancer Therapy

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Rossella Russo ◽  
Maria Tiziana Corasaniti ◽  
Giacinto Bagetta ◽  
Luigi Antonio Morrone
Keyword(s):  
Multidrug Resistance ◽  
Essential Oils ◽  
Biological Activities ◽  
Complex Mixtures ◽  
Antitumor Drugs ◽  
Wide Range ◽  
Growing Body ◽  
Anticancer Treatment

Essential oils are complex mixtures of several components endowed with a wide range of biological activities, including antiseptic, anti-inflammatory, spasmolytic, sedative, analgesic, and anesthetic properties. A growing body of scientific reports has recently focused on the potential of essential oils as anticancer treatment in the attempt to overcome the development of multidrug resistance and important side effects associated with the antitumor drugs currently used. In this review we discuss the literature on the effects of essential oils in  in vitroandin vivomodels of cancer, focusing on the studies performed with the whole phytocomplex rather than single constituents.

The molecular biology of mammalian arachidonic acid metabolism

1991 ◽  
Vol 260 (2) ◽  
pp. L13-L28 ◽  
Author(s):  
E. Sigal
Keyword(s):  
Arachidonic Acid ◽  
Acid Metabolism ◽  
Recombinant Dna ◽  
Biological Activities ◽  
Biological Effects ◽  
Arachidonic Acid Metabolism ◽  
Bioactive Metabolites ◽  
Wide Range

The metabolism of arachidonic acid by cyclooxygenase and lipoxygenase enzymes results in a wide range of oxidized products with potent biological activities. These metabolites, which include the prostaglandins and leukotrienes, have been implicated in the pathogenesis of a variety of inflammatory diseases. Research over the last decade has focused primarily on the elucidation of the chemical structure of the metabolites and their biological effects in vitro and in vivo. Recently, research on the enzymes that produce these bioactive metabolites through oxidization of arachidonic acid has intensified. Recombinant DNA techniques have enabled investigators to determine the nucleotide sequences for several of the enzymes in the arachidonic acid cascade. The resulting cDNAs are now being used to further investigate the biochemical and biological features of arachidonic acid metabolism. The purpose of this paper is to review how the cDNAs for these enzymes were obtained, what information they convey, and how they are being applied in current research.

scholarly journals Characterization of Andean Blueberry in Bioactive Compounds, Evaluation of Biological Properties and in vitro Bioaccessibility

2020 ◽  
Author(s):  
Nieves Baenas ◽  
Jenny Ruales ◽  
Diego A. Moreno ◽  
Daniel Alejandro Barrio ◽  
Carla M. Stinco ◽  
...  
Keyword(s):  
Antioxidant Capacity ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
In Vitro Digestion ◽  
Biological Properties ◽  
Wide Range ◽  
Zebrafish Embryogenesis

Andean blueberries are wild berries grown and consumed in Ecuador which contain high values of bioactive compounds, mainly anthocyanins, with powerful antioxidant activity. The aim of this study was to evaluate the profile and contents of (poly)phenols and carotenoids in Andean blueberry by HPLC-DAD-MSn and determine a wide range of its biological activities. The antioxidant capacity of this fruit was evaluated in vitro by three different methods and in vivo using the zebrafish animal model, also the toxicity effect was determined by the zebrafish embryogenesis test. Besides, the antimicrobial activity and the capacity of Andean blueberry to produce hemagglutination in blood cells were evaluated. Finally, the bioaccessibility of (poly)phenols and related antioxidant capacity were determined in the different phases of an in vitro digestion. The global results indicated no toxicity of Andean blueberry, weakly bacteriostatic activity, and high contents of anthocyanins and antioxidant capacity, which were partially bioaccesible in vitro (~ 50 % at the final intestinal step), contributing to the knowledge of its health benefits for consumers and its potential use in the food and pharmaceutical industry as functional ingredient.

scholarly journals Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 933
Author(s):  
Verônica da Silva Oliveira ◽  
Amanda Silva de Almeida ◽  
Ingrid da Silva Albuquerque ◽  
Fernanda Ílary Costa Duarte ◽  
Bárbara Cristina Silva Holanda Queiroz ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Solid Dispersions ◽  
Polymeric Matrices ◽  
Therapeutic Applications ◽  
Biological Potential ◽  
New Applications

This review aims to provide an overview of studies that address the use, in therapeutic applications, of solid dispersions (SDs) with biological activities in vitro and/or in vivo mainly made up of polymeric matrices, as well as to evaluate the bioactive activity of their constituents. This bibliographic survey shows that the development of solid dispersions provides benefits in the physicochemical properties of bioactive compounds, which lead to an increase in their biological potential. However, despite the reports found on solid dispersions, there is still a need for biological assay-based studies, mainly in vivo, to assist in the investigation and to devise new applications. Therefore, studies based on such an approach are of great importance to enhance and extend the use of solid dispersions in the most diverse therapeutic applications.

scholarly journals Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 3959
Author(s):  
Laísa Cordeiro ◽  
Hermes Diniz-Neto ◽  
Pedro Figueiredo ◽  
Helivaldo Souza ◽  
Aleson Sousa ◽  
...  
Keyword(s):  
Klebsiella Pneumoniae ◽  
Biological Activities ◽  
High Capacity ◽  
Pharmacokinetic Profile ◽  
In Vitro Toxicity ◽  
Antibacterial Drug ◽  
Wide Range ◽  
Good Potential

Klebsiella pneumoniae causes a wide range of community and nosocomial infections. The high capacity of this pathogen to acquire resistance drugs makes it necessary to develop therapeutic alternatives, discovering new antibacterial molecules. Acetamides are molecules that have several biological activities. However, there are no reports on the activity of 2-chloro-N-(4-fluoro-3-nitrophenyl)acetamide. Based on this, this study aimed to investigate the in vitro antibacterial activity of this molecule on K. pneumoniae, evaluating whether the presence of the chloro atom improves this effect. Then, analyzing its antibacterial action more thoroughly, as well as its cytotoxic and pharmacokinetic profile, in order to contribute to future studies for the viability of a new antibacterial drug. It was shown that the substance has good potential against K. pneumoniae and the chloro atom is responsible for improving this activity, stabilizing the molecule in the target enzyme at the site. The substance possibly acts on penicillin-binding protein, promoting cell lysis. The analysis of cytotoxicity and mutagenicity shows favorable results for future in vivo toxicological tests to be carried out, with the aim of investigating the potential of this molecule. In addition, the substance showed an excellent pharmacokinetic profile, indicating good parameters for oral use.

Polyoxometalates in Biomedicine: Update and Overview

2020 ◽  
Vol 27 (3) ◽  
pp. 362-379 ◽  
Author(s):  
Mirjana B. Čolović ◽  
Milan Lacković ◽  
Jovana Lalatović ◽  
Ali S. Mougharbel ◽  
Ulrich Kortz ◽  
...  
Keyword(s):  
Biological Activities ◽  
Transition Metal Ions ◽  
Fine Tuning ◽  
Comprehensive Overview ◽  
Early Transition Metal ◽  
Biological Targets ◽  
Wide Range ◽  
Treatment Of Diabetes

Background: Polyoxometalates (POMs) are negatively charged metal-oxo clusters of early transition metal ions in high oxidation states (e.g., WVI, MoVI, VV). POMs are of interest in the fields of catalysis, electronics, magnetic materials and nanotechnology. Moreover, POMs were shown to exhibit biological activities in vitro and in vivo, such as antitumor, antimicrobial, and antidiabetic. Methods: The literature search for this peer-reviewed article was performed using PubMed and Scopus databases with the help of appropriate keywords. Results: This review gives a comprehensive overview of recent studies regarding biological activities of polyoxometalates, and their biomedical applications as promising anti-viral, anti-bacterial, anti-tumor, and anti-diabetic agents. Additionally, their putative mechanisms of action and molecular targets are particularly considered. Conclusion: Although a wide range of biological activities of Polyoxometalates (POMs) has been reported, they are to the best of our knowledge not close to a clinical trial or a final application in the treatment of diabetes or infectious and malignant diseases. Accordingly, further studies should be directed towards determining the mechanism of POM biological actions, which would enable fine-tuning at the molecular level, and consequently efficient action towards biological targets and as low toxicity as possible. Furthermore, biomedical studies should be performed on solutionstable POMs employing physiological conditions and concentrations.

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