Development and characterization of electrospun curcumin-loaded antimicrobial nanofibrous membranes

2020 ◽  
pp. 004051752092551
Author(s):  
Javeed A Awan ◽  
Saif Ur Rehman ◽  
Muhammad Kashif Bangash ◽  
Fiaz Hussain ◽  
Jean-Noël Jaubert
Keyword(s):  
Biological Activities ◽  
Research Work ◽  
Medical Applications ◽  
Electrospinning Technique ◽  
Naturally Occurring ◽  
Wide Range ◽  
Nanofibrous Membranes ◽  
Antimicrobial Barrier ◽  
Anti Hiv

Curcumin is a naturally occurring hydrophobic polyphenol compound. It exhibits a wide range of biological activities such as antibacterial, anti-inflammatory, anti-carcinogenic, antifungal, anti-HIV, and antimicrobial activity. In this research work, antimicrobial curcumin nanofibrous membranes are produce by an electrospinning technique using the Eudragit RS 100 (C19H34ClNO6) polymer solution enriched with curcumin. The morphology and chemistry of the membrane are analyzed using scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) spectroscopy. Kirby Bauer disk diffusion tests are carried out to examine the antibacterial effectiveness of the membrane. Experimental results show that the nanofibers produced are of uniform thickness morphology and curcumin is successfully incorporated into the nanofibrous mat, while no chemical bonding was observed between curcumin and the polymer. The antimicrobial curcumin nanofibrous membranes can be effectively applied as antimicrobial barrier in a wide variety of medical applications such as wound healing, scaffolds, and tissue engineering.

Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Justyna Żwawiak ◽  
Anna Pawełczyk ◽  
Dorota Olender ◽  
Lucjusz Zaprutko
Keyword(s):  
Biological Activities ◽  
Anticancer Activities ◽  
Drug Molecule ◽  
Pentacyclic Triterpene ◽  
Formation Pathway ◽  
Chemical Systems ◽  
Drug Molecules ◽  
Wide Range ◽  
Anti Hiv ◽  
Structure And Activity

: Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

Development and Evaluation of Sustained Release Lipid Nanocarriers for Curcumin

2020 ◽  
Vol 5 (3) ◽  
pp. 224-235
Author(s):  
Harshal A. Pawar ◽  
Bhagyashree D. Bhangale
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Drug Delivery Systems ◽  
Biological Activities ◽  
Curcuma Longa ◽  
Research Work ◽  
Elimination Rate ◽  
Delivery Systems ◽  
Physicochemical Stability ◽  
Wide Range

Background: Lipid based excipients have increased acceptance nowadays in the development of novel drug delivery systems in order to improve their pharmacokinetic profiles. Drugs encapsulated in lipids have enhanced stability due to the protection they experience in the lipid core of these nano-formulations. Phytosomes are newly discovered drug delivery systems and novel botanical formulation to produce lipophilic molecular complex which imparts stability, increases absorption and bioavailability of phytoconstituent. Curcumin, obtained from turmeric (Curcuma longa), has a wide range of biological activities. The poor solubility and wettability of curcumin are responsible for poor dissolution and this, in turn, results in poor bioavailability. To overcome these limitations, the curcumin-loaded nano phytosomes were developed to improve its physicochemical stability and bioavailability. Objective: The objective of the present research work was to develop nano-phytosomes of curcumin to improve its physicochemical stability and bioavailability. Methods: Curcumin-loaded nano phytosomes were prepared by using phospholipid Phospholipon 90 H using a modified solvent evaporation method. The developed curcumin nano phytosomes were evaluated by particle size analyzer and differential scanning calorimetry (DSC). Results: Results indicated that phytosomes prepared using curcumin and lipid in the ratio of 1:2 show good entrapment efficiency. The obtained curcumin phytosomes were spherical in shape with a size less than 100 nm. The prepared nano phytosomal formulation of curcumin showed promising potential as an antioxidant. Conclusion: The phytosomal complex showed sustained release of curcumin from vesicles. The sustained release of curcumin from phytosome may improve its absorption and lowers the elimination rate with an increase in bioavailability.

Combinatorial Synthesis of Novel 3/5(3,5)-(Di)nitro/chloropaeonol Carbonyl Hydrazone Derivatives as Nematicidal Agents

2021 ◽  
Vol 24 ◽  
Author(s):  
Genqiang Chen ◽  
Lina Zhu ◽  
Yanfei Xia ◽  
Jinming Yang ◽  
Song Zhang ◽  
...  
Keyword(s):  
High Efficiency ◽  
Biological Activities ◽  
Science Research ◽  
Nematicidal Activity ◽  
Effective Control ◽  
Root Bark ◽  
Naturally Occurring ◽  
Whole Plant ◽  
Wide Range

Background: Developing the high-efficiency and low-risk small-molecule green-nematocide is the key of effective control of the nematodes. Paeonol, is a naturally occurring phenolic compound, isolated from the root bark of Paeonia suffruticosa and the whole plant of Cynanchum paniculatum. Due to its crucial phenolic ketone skeleton, modern biological science research has indicated that paeonol has a wide range of biological activities. The structural modification of paeonol into paeonol carbonyl hydrazone derivatives is a potential approach for the development of novel nematodes, which showed more toxicity than paeonol. However, there are no reports on the nematicidal activity of paeonol carbonyl hydrazone derivatives to control Heterodera glycines. Results: We always endeavor to discover and develop biorational natural products-based pesticidal agents, 4 significant intermediates and 21 novel 3/5(3,5)-(di)nitro/chloropaeonol carbonyl hydrazone derivatives were prepared, and their structures well characterized by 1H NMR, HRMS, MS, and mp. Due to the steric hindrance, the substituents on the C=N double bond of all hydrazine compounds adopted E configuration. Results of nematicidal activity revealed that, among all compounds, especially 5-nitropaeonol (5) and 3,5-dinitropaeonol (7) displayed the most potent nematicidal activity H. glycines in vivo with LC50 values of 0.0323 and 0.0367 mg/mL, respectively. Conclusion: It suggested that for the 3/5(3,5)-(di)nitro/chloropaeonol carbonyl hydrazone derivatives, a nitro group introduced at C5 position of 1 was necessary for obtaining the potent compound as nematicidal agents. These preliminary results will pave the way for further modification of paeonol in the development of potential new nematicides.

scholarly journals Oxazolidinones as Chiral Auxiliaries in the Asymmetric 1,4-Conjugate Addition Reaction Applied to the Total Synthesis of Natural Products: A Supplemental Mini-Review

2018 ◽  
Vol 15 (1) ◽  
pp. 3-20 ◽  
Author(s):  
Vahideh Zadsirjan ◽  
Majid M. Heravi
Keyword(s):  
Total Synthesis ◽  
Biological Activities ◽  
Conjugate Addition ◽  
Chiral Auxiliary ◽  
Addition Reactions ◽  
Chiral Auxiliaries ◽  
Complex Molecules ◽  
Total Syntheses ◽  
Naturally Occurring ◽  
Wide Range

Background: The most frequently used chiral auxiliaries, oxazolidinones (Evans' oxazolidinones) have been employed in 1,4-congugate addition reactions to α,β-unsaturated carbonyl compounds. Supplementary to our previous reports in this mini-review, we attempted to underscore the applications of this strategy in a step (steps) in the total synthesis of some naturally occurring compounds exhibiting diverse biological activities. Objective: In this mini-review, we try to underscore the applications of oxazolidinones (Evans’ oxazolidinones) in 1,4-congugate addition reactions to α,β-unsaturated carbonyl in the total synthesis of some naturally occurring compounds exhibiting diverse biological activities. Conclusion: In spite of well-known superiority of asymmetric catalyzed reactions, the use of auxiliarycontrolled reactions are still considered as commanding, vital and sometimes as only tools in the generation of stereogenic centers during the construction of complex molecules and total synthesis of naturally occurring compounds. The commercial availability, or readily accessibility of a wide variety of chiral amino alcohols as starting materials to synthesize a wide range of oxazolidinones is the merits of them. In addition, the ease of removal and subjection to various and diverse stereoselective reactions make oxazolidinones as the ideal and superior chiral auxiliaries. In this regard, they were successfully used in asymmetric 1,4-conjugate addition reactions with high stereoselectivities. The high degree of asymmetric induction can be attributed to the rigid chelation of N-acyloxazolidinones with metal ions, as well as the covering of one face of the system by the bulkiness of 4-substituent. In summary, in this report, the importance of the applications of chiral oxazolidinones as suitable chiral auxiliaries in the stereoselective, 1,4-conjugate addition reactions in asymmetric synthesis and in particular, the total synthesis of naturally occurring compounds and some complex molecules were underscored. Noticeably, in these total syntheses, this chiral auxiliary is controlling the stereochemistry of a newly created stereogenic center as well as preserving the configuration of other chiral centers, which already have been presented in the precursor. General methods have been established for the attachment of the chiral auxiliary as a moiety to the substrate molecule in high to excellent yields. At the end of these reactions, this auxiliary can be easily removed leaving various desired reactive motifs for the next step in multi-step synthesis.

scholarly journals Wearable Potentiometric Sensors for Medical Applications

Sensors ◽  
2019 ◽  
Vol 19 (2) ◽  
pp. 363 ◽  
Author(s):  
María Cuartero ◽  
Marc Parrilla ◽  
Gaston Crespo
Keyword(s):  
Sport Performance ◽  
Medical Utilization ◽  
Potentiometric Sensors ◽  
Sensor Calibration ◽  
Medical Applications ◽  
Sample Collection ◽  
Medical Settings ◽  
Wide Range ◽  
The Individual

Wearable potentiometric sensors have received considerable attention owing to their great potential in a wide range of physiological and clinical applications, particularly involving ion detection in sweat. Despite the significant progress in the manner that potentiometric sensors are integrated in wearable devices, in terms of materials and fabrication approaches, there is yet plenty of room for improvement in the strategy adopted for the sample collection. Essentially, this involves a fluidic sampling cell for continuous sweat analysis during sport performance or sweat accumulation via iontophoresis induction for one-spot measurements in medical settings. Even though the majority of the reported papers from the last five years describe on-body tests of wearable potentiometric sensors while the individual is practicing a physical activity, the medical utilization of these devices has been demonstrated on very few occasions and only in the context of cystic fibrosis diagnosis. In this sense, it may be important to explore the implementation of wearable potentiometric sensors into the analysis of other biofluids, such as saliva, tears and urine, as herein discussed. While the fabrication and uses of wearable potentiometric sensors vary widely, there are many common issues related to the analytical characterization of such devices that must be consciously addressed, especially in terms of sensor calibration and the validation of on-body measurements. After the assessment of key wearable potentiometric sensors reported over the last five years, with particular attention paid to those for medical applications, the present review offers tentative guidance regarding the characterization of analytical performance as well as analytical and clinical validations, thereby aiming at generating debate in the scientific community to allow for the establishment of well-conceived protocols.

scholarly journals ANTIOXIDANT POTENTIAL OF PIPERIDINE CONTAINING COMPOUNDS-A SHORT REVIEW

2018 ◽  
Vol 11 (8) ◽  
pp. 66
Author(s):  
Manjusha R K ◽  
Shaheen Begum ◽  
Arifa Begum ◽  
Bharathi K
Keyword(s):  
Biological Activities ◽  
Short Review ◽  
Heterocyclic Ring ◽  
Antioxidant Potential ◽  
Naturally Occurring ◽  
Antioxidant Profile ◽  
Antioxidant Agents ◽  
Wide Range ◽  
Privileged Scaffold ◽  
Candidate Molecule

Piperidine is a saturated heterocyclic ring, considered as a privileged scaffold in view of its role in wide range of biological activities. Piperidine is good candidate molecule for obtaining potent antioxidant agents. The planar nature of this heterocyclic nucleus allows the introduction of substituent groups at different positions on the ring. In the present review, the antioxidant profile of piperidine containing compounds has been focused. The compounds were classified into naturally occurring piperidines, unsaturated piperidines, N-substituted piperidines, piperamides, piperanols, piperidine oximes, and hydrazides.

scholarly journals Structural characterization of four different naturally occurring porcine collagen membranes suitable for medical applications

PLoS ONE ◽  
2018 ◽  
Vol 13 (10) ◽  
pp. e0205027 ◽  
Author(s):  
Thimo Maurer ◽  
Michael H. Stoffel ◽  
Yury Belyaev ◽  
Niklaus G. Stiefel ◽  
Beatriz Vidondo ◽  
...  
Keyword(s):  
Structural Characterization ◽  
Medical Applications ◽  
Naturally Occurring ◽  
Collagen Membranes ◽  
Porcine Collagen

scholarly journals Therapeutic Potential of Cucumis Melo (L). Fruit Extract and Its Silver Nanopartciles Against Den Induced Hepatocellular Cancer in Rats

2021 ◽  
Author(s):  
R Vidya ◽  
K Kalaivani ◽  
P Amudha
Keyword(s):  
Silver Nanoparticles ◽  
Protective Effect ◽  
Cucumis Melo ◽  
Biological Activities ◽  
Hematological Parameters ◽  
Research Work ◽  
Histological Evaluation ◽  
Fruit Extract ◽  
Standard Drug ◽  
Wide Range

Abstract Biosynthesized silver nanoparticles have a wide range of biological activities and using nanoparticles as one of the novel approaches in cancer therapy. In this present research work, the anticancer efficacy of Cucumis melo fruit extract and its silver nanoparticles was explored. Wistar rats were divided into six groups and hepatic cancer was induced with 0.01 % DEN (diethylnitrosamine) through drinking water for 16 weeks. Cyclophosphamide was given as the standard drug at the dose of 50 mg / kg body weight. Hematological Parameters showed a decrease in the levels of hemoglobin (Hb), packed cell volume (PCV), red blood cells (RBC), mean corpuscular volume (MCV), mean corpuscular Hb (MCH), mean corpuscular Hb concentration (MCHC), and platelets (PLTS) levels except white blood cell (WBC) in DEN induced cancer animals. Significant alterations in the hematological parameters were observed after treatment which indicate the protective effect of Cucumis melo fruit on the hemopoietic system. The levels of liver function markers such as transaminases (AST ALT, ALP, LDH, GGT and 5’NT were significantly elevated in serum and liver of cancer bearing rats. Treatment with crude extract and silver nanoparticles of Cucumis melo fruit, indicating that Cucumis melo fruit could have exerted its protective effect. The levels of serum tumor markers viz., Alpha feto protein (AFP) and Carcinoembryonic antigen (CEA) elevated in rats induced with DEN, which then were reduced following Cucumis melo fruit treatment, indicating the anticancer activity of the drug. Histological evaluation of liver and kidney were also performed to authenticate the present work.

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.

An Overview on Pyranocoumarins: Synthesis and Biological Activities

2020 ◽  
Vol 23 (24) ◽  
pp. 2679-2721 ◽  
Author(s):  
Evangelia-Eirini N. Vlachou ◽  
Konstantinos E. Litinas
Keyword(s):  
Organic Compounds ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Biological Properties ◽  
Pyran Ring ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Anti Inflammatory ◽  
Antibacterial And Antifungal ◽  
Anti Hiv

Pyrano- and dipyranocoumarins are classes of naturally occurring organic compounds with very interesting biological activities. This review focuses on the synthetic strategies for the synthesis of pyranocoumarins and dipyranocoumarins and the biological properties of those compounds. The synthesis involves the formation of the pyran ring, at first, from a coumarin or the formation of pyranone moiety from an existing pyran. Pyranocoumarins and dipyranocoumarins present anti-HIV, anti-cancer, neuroprotective, antidiabetic, antibacterial, antifungal, anti-inflammatory activities. Especially khellactones and calanolides are usually potent and selective in anti-HIV activity. Decursin and decursinol derivatives are effective as anticancer, neuroprotective, antidiabetic, antibacterial, and antifungal agents.

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