Green Chemistry Approaches to the Synthesis of Coumarin Derivatives

(E-pub Abstract Ahead of Print)

Author(s): Maja Molnar*, Melita Lončarić, Marija Kovač.

Journal Name: Current Organic Chemistry

Abstract:

This review is a compilation of the green synthetic methods used in the synthesis of coumarin derivatives. Coumarins are a class of compounds with a pronounced wide range of biological activities, which have found their application in medicine, pharmacology, cosmetics and food industry. Their biological activity and potential application is highly dependent on their structure. Therefore, many researchers have been performing the synthesis of coumarin derivatives on a daily basis. High demands for their synthesis often result in the increased generation of different waste chemicals. In order to minimize a utilization and generation of toxic organic substances, green synthetic methods are applied in this manner. These methods are getting more attention in the last few decades. Green chemistry methods cover a wide range of methods, including application of ultrasound and microwaves, ionic liquids and deep eutectic solvents, solvent-free synthesis, mechanosynthesis and multicomponent reactions. All typical condensation reactions for coumarin synthesis like Knoevenagel, Perkin, Kostanecki-Robinson, Pechmann, Reformansky reactions, have been successfully performed using these green synthetic methods. According to the authors mentioned in this review, not only these methods reduce the utilization and generation of toxic chemicals, they can also enhance the reaction performance in terms of product yields, purity, energy consumption and postsynthetic procedures when comapred to the conventional methods. Due to the significance of coumarins as biologically active systems and the recent demands of reducing toxic solvents, catalysts and energy consumption, this review provides a first full literature overview on the application of green synthetic methods in the coumarin synthesis. It covers a literature search over the period from 1995-2019. The importance of this work is its comprehensive literature survey on a specific class of heterocyclic compounds, and those researchers working on the coumarin synthesis can find very useful information on the green synthetic approaches to their synthesis. There are some reviews on the coumarin synthesis, but most of them cover only specific reactions on coumarin synthesis and none of them the whole range of green chemistry methods.

Keywords: Coumarin derivatives, Green methods, Deep eutectis solvents, Ionic liquids, Solvent-free, mechanosynthesis

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1385272824666200120144305
Price: $95

Special-new-year-discount


Terpenoids and Aromatic Compounds from Bryophytes and their Central Nervous System Activity

(E-pub Abstract Ahead of Print)

Author(s): Agnieszka Ludwiczuk*, Yoshinori Asakawa.

Journal Name: Current Organic Chemistry

Abstract:

Bryophytes, phylogenetically placed between algae and pteridophytes, are divided into three classes, mosses, liverworts, and hornworts. Traditional system of medicine throughout the world has been utilizing this group of plants to treat various ailments. One of the outstanding features of these spore forming plants is their chemistry, especially that of the liverworts. Liverworts, and other bryophytes have yielded of rich array of secondary metabolites. Many of these compounds are characterized by unprecedented structures, and some have not been found in any other plants, fungi or marine organisms. Among the bryophytes, the chemical constituents of liverworts and their biological activity have been studied in the most detail. In this review, we demonstrate the chemistry of the liverworts, mosses and hornworts, and also neuroptotective activity of dimeric herbertane-type sesquiterpenoids, mastigophorenes and secoaromadendrane-type sesquiterpenoids, marchantin-type cyclic bisbibenzyls with muscle-relaxant activity, or ent-longipinane-type sesqiterpenoids with acetylcholinesterase inhibitory activity, among others.

Keywords: Bryophytes, Liverworts, Sesquiterpenoids, Bisbibenzyls, Neuroprotective activity, Acetylcholinesterase inhibitors

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1385272824666200120143558
Price: $95

Special-new-year-discount


Neuronal Excitability in Epileptogenic Zones Regulated by the Wnt/Β-Catenin Pathway

(E-pub Abstract Ahead of Print)

Author(s): Carmen Rubio, Elisa Taddei, Jorge Acosta, Verónica Custodio, Carlos Paz*.

Journal Name: CNS & Neurological Disorders - Drug Targets
(Formerly Current Drug Targets - CNS & Neurological Disorders)

Abstract:

Epilepsy is a neurological disorder that involves abnormal and recurrent neuronal discharges, producing epileptic seizures. Recently, it has been proposed that the Wnt signaling pathway is essential for central nervous system development and function because it modulates important processes such as hippocampal neurogenesis, synaptic clefting, and mitochondrial regulation. Wnt/β-catenin signaling regulates changes induced by epileptic seizures, including neuronal death. Several genetic studies associate Wnt/β-catenin signaling with neuronal excitability and epileptic activity. Mutations and chromosomal defects underlying syndromic or inherited epileptic seizures have been identified. However, genetic factors underlying the susceptibility of an individual to develop epileptic seizures have not been fully studied yet. In this review, we describe the genes involved in neuronal excitability in epileptogenic zones dependent on the Wnt/β-catenin pathway.

Keywords: Wnt/ β -catenin, Neuronal excitability, Epileptogenesis, Genetic signaling, Hippocampal formation

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1871527319666200120143133
Price: $95

Special-new-year-discount



An evaluation of the effects of pyridoxal phosphate in chlorpromazine-induced Parkinsonism using mice

(E-pub Abstract Ahead of Print)

Author(s): Olofinnade A.T., Onaolapo T.M., Oladimeji S., Fatoki A.M., Balogun C.I., Onaolapo A.Y.*, Onaolapo O.J..

Journal Name: Central Nervous System Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Central Nervous System Agents)

Abstract:

Background: Parkinsonism is a neurodegenerative disorder with a heavy disease burden, despite the discovery and application of drugs. Current research is beginning to suggest the possible crucial roles of micronutrients such as pyridoxal phosphate in the prevention or management of neurodegenerative disorders.

Objectives: We investigated the possible protective effects of supplemental pyridoxal phosphate in Chlorpromazine (CPZ)-induced Parkinsonism-like changes in mice.

Methods: Mice were assigned to eight groups of 30 mice each. Groups included Vehicle control (fed standard diet (SD), and administered intraperitoneal {ip} injection of saline and saline per oram), levodopa-carbidopa (LD) group (SD, saline ip and LD per oram), two groups fed pyridoxal phosphate-supplemented diet (at 100 and 200 mg/kg of feed), and administered saline both ip and orally, CPZ group (SD, CPZ ip and saline per oram), CPZ/LD group (SD, CPZ ip and LD per oram) and finally two groups fed pyridoxal phosphate -supplemented diet (at 100 and 200 mg/kg of feed) and administered CPZ ip plus saline per oram. Treatments were administered daily for a period of 21 days to allow for induction of Parkinsonism features. Body weight and food intake were measured weekly while, neurobehavioural and biochemical tests were assessed at the end of the experimental period.

Results: Pyridoxal phosphate supplementation was associated with a reduction in CPZ-induced suppression of open-field horizontal locomotion and rearing; and a significant increase in grooming activity. Administration of pyridoxal phosphate-supplemented diet was also associated with improvements in working-memory in CPZ-treated mice; and there were reduction in index of anxiety and catalepsy score.

Conclusion: Pyridoxal phosphate supplementation was associated with significant benefits in CPZ-induced Parkinsonism-like changes in mice.

Keywords: Dopamine, Micronutrients, Neurobehaviour, Neurodegenerative disease, Neurotransmitter, Vitamins

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1871524920666200120142508
Price: $95

Special-new-year-discount



Evaluation of Two Fast Virtual Stenting Algorithms for Intracranial Aneurysm Flow Diversion

(E-pub Abstract Ahead of Print)

Author(s): Saeb R. Lamooki, Vincent M. Tutino, Nikhil Paliwal, Robert J. Damiano, Mohammad Waqas, Setlur S.V. Nagesh, Hamidreza Rajabzadeh-Oghaz, Kunal Vakharia, Adnan H. Siddiqui*, Hui Meng.

Journal Name: Current Neurovascular Research

Abstract:

Endovascular treatment of intracranial aneurysms (IAs) by flow diverter (FD) stents depends on flow modification. Patient-specific modeling of FD deployment and computational fluid dynamics (CFD) could enable a priori endovascular strategy optimization. We developed a fast, simplistic, expansion-free balls-weeping algorithm to model FDs in patient-specific aneurysm geometry. However, since such strong simplification could result in less accurate simulations, we also developed a fast virtual stenting workflow (VSW) that explicitly models stent expansion using pseudo-physical forces. To test which of these two fast algorithms more accurately simulates real FDs, we applied them to virtually treat three representative patient-specific IAs. We deployed Pipeline Embolization Device into 3 patient-specific silicone aneurysm phantoms and simulated the treatments using both balls-weeping and VSW algorithms in computational aneurysm models. We then compared the virtually deployed FD stents against experimental results in terms of geometry and post-treatment flow fields. For stent geometry, we evaluated gross configurations and porosity. For post-treatment aneurysmal flow, we compared CFD results against experimental measurements by particle image velocimetry. We found that VSW created more realistic FD deployments than balls-weeping in terms of stent geometry, porosity and pore density. In particular, balls-weeping produced unrealistic FD bulging at the aneurysm neck, and this artifact drastically increased with neck size. Both FD deployment methods resulted in similar flow patterns, but the VSW had less error in flow velocity and inflow rate. In conclusion, modeling stent expansion is critical for preventing unrealistic bulging effects and thus should be considered in virtual FD deployment algorithms. Due to its high computational efficiency and superior accuracy, the VSW algorithm is a better candidate for implementation into a bedside clinical tool for FD deployment simulation.

Keywords: Particle image velocimetry, Computational fluid dynamics, Validation, Cerebral aneurysm, Eendovascular therapy, Flow diverting stent

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1567202617666200120141608
Price: $95

Special-new-year-discount



Elucidation of antibacterial compounds from inflorescences of banana (Musa balbisiana cv. Saba) using liquid chromatography-tandem mass spectrometry

(E-pub Abstract Ahead of Print)

Author(s): Hoe Seng Tin, Birdie Scott Padam, Fook Yee Chye*.

Journal Name: Current Nutrition & Food Science

Abstract:

Background: Banana by-products are under-valued and their potential remains untapped. They are often composted after the fruits are harvested reducing the cause of environmental pollutions due to open burning.

Objectives: The study aims to identify the bioactive compounds in banana [Musa acuminate x balbisiana Colla cv. Saba (Musaceae)] inflorescence buds that are responsible for the antibacterial activity on selected foodborne pathogens.

Method: Dried inflorescence buds were extracted using methanol and subsequently partitioned into chloroform, ethyl acetate, butanol and deionized water. Further isolation of bioactive components was based on a bioassay-guided fractionation and the inhibitory activity at various concentrations against selected foodborne pathogens was determined. The compounds were identified using high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry (LC-MS/MS).

Results: The SPE-fraction 3 (BWF-3) purified from the methanolic water partition of banana inflorescence showed the most prominent inhibition against Staphylococcus aureus with minimum inhibitory concentration at 12.0 µg/ml. The BWF-3 was later identified as proanthocyanidins with epigallocatechin as the main extension unit. Additionally, the survival of Listeria monocytogenes increased with the fortification of ferum (II) and (III) at concentration as low as 1 mM but not for the calcium, magnesium, manganese and glucose.

Conclusion: The methanolic partition of banana inflorescence buds could be a potential source of natural antibacterial for food and pharmaceutical applications.

Keywords: Banana by-product, Foodborne pathogens, Inflorescence buds, Proanthocyanidin, Epigallocatechin, Musa acuminate

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1573401316666200120125601
Price: $95

Special-new-year-discount



Characterization of Amorphophallus paeoniifolius (Dennst.) Nicolson Modified Fermented Flour by Three Different Starters

(E-pub Abstract Ahead of Print)

Author(s): Ikrar Taruna Syah*, Anto, Umar Hafidz Asy’ari Hasbullah.

Journal Name: Current Nutrition & Food Science

Abstract:

Background: Flour is generally evaluated by physicochemical analysis of its constituents to determine its functional properties. The modification of flour is reflected in many of physicochemical properties.

Objective: In the present study, samples of elephant foot yam (Amorphophallus paeoniifolius) modified fermented flour were characterized based on physicochemical properties, starch, amylose, and amylopectin content, and also flour morphology.

Method: Various starters were applied (mocaf, Bimo-cf, and tape yeast) for 12h fermentation before being processed to flour to modify its properties. The physicochemical parameters of flours consist of whiteness index, pasting properties, foaming capacity, flour morphology, and proximate compositions. All data were taken in triplicate using completely randomized design.

Result: All starters were able to improve whiteness index (WI) of flour. There was a correlation between fat and protein content with pasting properties of native flour and modified fermented elephant foot yam (MoEFY) flours. Fermentation processes caused slightly changes of flour pasting properties. The granule size of MoEFY flour became smaller than those in native elephant foot yam flour after fermentation, and granules were polyhedral with slightly pointed and protruding edges.

Conclusion: The results suggested that fermentation by Bimo-cf starter within 12h could provide a greater extent of flour modification.

Keywords: Amorphophallus paeoniifolius, Modified fermented flour, LAB, Yeast, Physicochemical

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1573401316666200120125006
Price: $95

Special-new-year-discount


Allopurinol loaded transferosomes for the alleviation of symptomatic after-effects of Gout: An Account of Pharmaceutical implications

(E-pub Abstract Ahead of Print)

Author(s): Ruchi Tiwari*, Gaurav Tiwari, Rachna Singh.

Journal Name: Current Drug Therapy

Abstract:

Background: The present study assessed the transdermal potential of transferosomes loaded with allopurinol for the treatment of gout.

Methods: Transferosomes of allopurinol were composed of different ratios of tween-80, soya lecithin and solvent using a thin-film hydration method. Transferosomes were characterized for scanning electron microscopy (SEM), zeta potential, % entrapment efficiency (%EE), Fourier transform infrared spectroscopy (FTIR), in-vitro drug release and kinetics as well as stability. Then optimized formulation was incorporated in gel and evaluated for viscosity, pH, extrudability, homogeneity, skin irritation study, spreadability, ex vivo skin permeation study, flux, and stability.

Results: SEM studies suggested that vesicles were spherical and zeta potential were in the range of -11.4 mV to -29.6 mV and %EE was 52.4- 83.87%. FTIR study revealed that there was no interaction between allopurinol and excipients during the preparation of transferosomes. The cumulative percentage of drug release from various transferosomes was ranged from 51.87 to 81.87%. A transferosomal gel of F8 formulation was prepared using dispersion method showed pseudoplastic rheological behavior, optimum pH, spreadability and also showed maximum drug permeation i.e. 79.84% with flux 13.06 g/cm2/hr and followed zero-order release kinetics. Irritation and in-vivo studies of optimized transferosomal gel G8 on rabbits revealed better results than the standard allopurinol.

Conclusion: This research suggested that allopurinol loaded transferosomal gel can be potentially used as a transdermal drug delivery system for the treatment of gout.

Keywords: Allopurinol, Transferosomes, Transferosomal gel, Permeation studies, Irritation study and stability of gel

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1574885515666200120124214
Price: $95

Special-new-year-discount


Factors influencing adherence among youth with Type-1-Diabetes Mellitus - the Hungarian case

(E-pub Abstract Ahead of Print)

Author(s): Beáta Erika Nagy, Brigitta Munkácsi, Karolina Eszter Kovács*.

Journal Name: Current Diabetes Reviews

Abstract:

Background & Introduction: Due to the increasing prevalence of type-1-diabetes an increasing number of studies draws investigation draws attention to its psychological effects and long-term consequences. As Type 1 Diabetes Mellitus is a chronic, non-curable, yet maintanable condition, with the affected children and their families facing a lifelong challenge. Our research focuses on the factors influencing adherence.

Methods & Results: The adherence of youth was examined in a sample involving 114 patients treated in the Medical and Health Science Centre at the University of Debrecen by employing a new adherence questionnaire (DAQ abbreviated version, Munkácsi et al, 2019) (DAF 2017; N=114). The influence of socio-demographic variables and those related to the disease (age at the diagnosis, time elapsed since diagnosis, method of treatment, the time elapsed since the use of the pump) were measured by linear regression. Furthermore, the between-group comparisons were made by independent sample t-tests and variance analysis. The investigation was carried out between September 2017 and May 2018. The effect of using insulin pump as therapy is significant and positive (0.36. p=0.045). The adherence of the patients using insulin pump is higher while the effect of the age at the diagnosis has a significantly negative effect (-.247, p=0.035). Thus, earlier detection of the disease may lead to a higher level of adherence. The effects of the socio-demographic variables (gender, family structure, educational level, type of the settlement, owning sibling and birth order) were not significant (p>0.05). Regarding the between-group comparisons, a significant difference could be pointed out concerning the siblings and birth-order as the adherence of the those with siblings was higher (p=0.044). Moreover, concerning insulin pump therapy, the adherence of patients using pump was significantly better (p=0.048). Also, regarding the age of the diagnosis, the adherence of those diagnosed before 12 was seemingly higher (p=0.039). Concerning the other socio-demographical and disease-related variables, no significant differences could be detected.

Conclusions: The results suggest that the treatment has an outstanding role in the adherence of the disease. Moreover, the role of the appropriate treatment, living conditions as well as the early diagnosis is relevant.

Keywords: Type-1-diabetes, Adherence, Mental health, Insulin pump, Socio-economic background, Early diagnosis

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1573399816666200120123719
Price: $95

Special-new-year-discount



Diabetes without Manifest Cardiovascular Disease: A Novel Approach in Risk Stratification and Treatment Selection

(E-pub Abstract Ahead of Print)

Author(s): Emile Andari, Samir Arnaout, Sami T Azar*, Elie Chammas, Selim Jambart, Mounzer Saleh, Rita Nemr, Antoine Sarkis.

Journal Name: Current Diabetes Reviews

Abstract:

Background: Cardiovascular disease (CVD), the main macro vascular complication of type 2 diabetes (T2D), increases the risk of death significantly in patients with T2D.

Introduction: Most of patients with T2D do not have manifest CVD. Due to paucity of data, CVD screening in asymptomatic patients with T2D remains highly controversial.

Methods: This has driven a panel of experts to establish a novel consensus on how to approach patients with T2D at high CVD risk. The panel formulated a stepwise algorithm by which patients with T2D undergo initial risk stratification into low, intermediate and high risk using the ASCVD calculator. In patients with intermediate risk, coronary artery calcium measurement is used to further stratify those patients into new low and high-risk categories.

Results and Conclusion: The panel recommends using standard diabetes care in low risk patients and using SGLT2 inhibitors and GLP1 agonists with cardio protective effect, on top of standard care, in high risk individuals.

Keywords: Diabetes mellitus, Cardiovascular disease, Risk stratification, SGLT2 inhibitors, GLP1 agonists, Macrovascular complications

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1573399816666200120122929
Price: $95

Special-new-year-discount