scholarly journals Artemisia annua Growing Wild in Romania—A Metabolite Profile Approach to Target a Drug Delivery System Based on Magnetite Nanoparticles

Plants ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 2245
Author(s):  
Adina-Elena Segneanu ◽  
Catalin Nicolae Marin ◽  
Ioan Ovidiu-Florin Ghirlea ◽  
Catalin Vladut Ionut Feier ◽  
Cornelia Muntean ◽  
...  

The metabolites profile of a plant is greatly influenced by geographical factors and the ecological environment. Various studies focused on artemisinin and its derivates for their antiparasitic and antitumoral effects. However, after the isolation and purification stage, their pharmaceutical potential is limited due to their low bioavailability, permeability and lifetime. The antibacterial activity of essential oils has been another topic of interest for many studies on this plant. Nevertheless, only a few studies investigate other metabolites in Artemisia annua. Considering that secondary metabolites act synergistically in a plant, the existence of other metabolites with antitumor and high immunomodulating activity is even more important. Novel nano-carrier systems obtained by loading herbs into magnetic nanoparticles ensures the increase in the antitumor effect, but also, overcoming the barriers related to permeability, localization. This study reported the first complete metabolic profile from wild grown Romanian Artemisia annua. A total of 103 metabolites were identified under mass spectra (MS) positive mode from 13 secondary metabolite categories: amino acids, terpenoids, steroids, coumarins, flavonoids, organic acids, fatty acids, phenolic acids, carbohydrates, glycosides, aldehydes, hydrocarbons, etc. In addition, the biological activity of each class of metabolites was discussed. We further developed a simple and inexpensive nano-carrier system with the intention to capitalize on the beneficial properties of both components. Evaluation of the nano-carrier system’s morpho-structural and magnetic properties was performed.

1995 ◽  
Vol 305 (1) ◽  
pp. 321-328 ◽  
Author(s):  
X Bossuyt ◽  
N Blanckaert

We propose the existence in rat liver endoplasmic reticulum (ER) of two asymmetric carrier systems. One system couples UDP-N-acetylglucosamine (UDPGlcNAc) transport to UDP-glucuronic acid (UDPGlcA) transport. When UDPGlcNAc was presented at the cytosolic side of the ER, it then acted as a weak inhibitor of UDPGlcA uptake. By contrast, UDPGlcNAc produced a forceful trans-stimulation of microsomal UDPGlcA uptake when it was present within the lumen of the ER. Likewise, cytosolic UDPGlcA strongly trans-stimulated efflux of intravesicular UDPGlcNAc, whereas cytosolic UDPGlcNAc was ineffective in trans-stimulating efflux of UDPGlcA. A second asymmetric carrier system couples UDPGlcNAc transport to UMP transport. Microsomal UDPGlcNAc influx was markedly stimulated by UMP present inside the microsomes. Such stimulation was only apparent when microsomes had been preincubated and thereby preloaded with UMP, indicating that UMP exerted its effect on UDPGlcNAc uptake by trans-stimulation from the lumenal side of the ER membrane. Contrariwise, extravesicular UMP only minimally trans-stimulated efflux of intramicrosomal UDPGlcNAc. It is widely accepted that UDPGlcNAc acts as a physiological activator of hepatic glucuronidation, but the mechanism of this effect has remained elusive. Based on our findings, we propose a model in which the interaction of two asymmetric transport pathways, i.e. UDPGlcA influx coupled to UDPGlcNAc efflux and UDPGlcNAc influx coupled to UMP efflux, combined with intravesicular metabolism of UDPGlcA, forms a mechanism that leads to stimulation of glucuronidation by UDPGlcNAc.


2021 ◽  
Vol 89 (3) ◽  
pp. 35
Author(s):  
Ulrike Söpper ◽  
Anja Hoffmann ◽  
Rolf Daniels

Transmucosal drug delivery represents a promising noninvasive option when drugs are employed which have a low oral bioavailability like CBD. However, this concept can only be successful as long as the formulation provides sufficient buccal retention and mucosal penetration. In this study, mucoadhesive carrier systems were evaluated consisting of CBD-loaded silica (Aeroperl 300) carriers, mucoadhesive polymers (Hypromellose (HPMC), chitosan and carbomer) and propylene glycol as a penetration enhancer. Mucoadhesive effect, drug release and penetration ability were evaluated for each carrier system. The results show that the addition of HPMC and carbomer substantially improve mucoadhesion compared to pure CBD, with an increase of 16-fold and 20-fold, respectively. However, due to their strong swelling, HPMC and carbomer hinder the penetration of CBD and rely on co-administration of propylene glycol as an enhancer to achieve sufficient mucosal absorption. Chitosan, on the other hand, achieves an 8-fold increase in mucoadhesion and enhances the amount of CBD absorbed by three times compared to pure CBD. Thus, chitosan represents a promising polymer to combine both effects. Considering the results, the development of silica-based buccal drug delivery systems is a promising approach for the effective delivery of CBD.


2005 ◽  
Vol 11 (2) ◽  
pp. 243-256 ◽  
Author(s):  
Mark A. Arnould ◽  
Rafael Vargas ◽  
Rita W. Buehner ◽  
Chrys Wesdemiotis

Electrospray ionization of polyesters composed of isophthalic acid and neopentyl glycol produces carboxylate anions in negative mode and mainly sodium ion adducts in positive mode. A tandem mass spectrometry (MS/MS) study of these ions in a quadrupole ion trap shows that the collisionally-activated dissociation pathways of the anions are simpler than those of the corresponding cations. Charge-remote fragmentations predominate in both cases, but the spectra obtained in negative mode are devoid of the complicating cation exchange observed in positive mode. MS/MS of the Na+ adducts gives rise to a greater number of fragments but not necessarily more structural information. In either positive or negative mode, polyester oligomers with different end groups fragment by similar mechanisms. The observed fragments are consistent with rearrangements initiated by the end groups. Single-stage ESI mass spectra are also more complex in positive mode because of extensive H/Na substitutions; this is also true for matrix-assisted laser desorption ionization mass spectra. Hence, formation and analysis of anions might be the method of choice for determining block length, end group structure and copolymer sequence, provided the polyester contains at least one carboxylic acid end group that is ionizable to anions.


2015 ◽  
Vol 1085 ◽  
pp. 107-112 ◽  
Author(s):  
Ilya A. Lysak ◽  
Tatyana D. Malinovskaya ◽  
Olga N. Tchaikovskaya ◽  
Galina V. Lysak ◽  
Vyacheslav R. Artyushin

Using electronic spectroscopy and fluorescence techniques, the degradation of 2-methyl-4-chlorophenoxyacetic acid has been researched in water under the excitation with UV radiation produced by a KrCl excimer lamp in the presence of “TiO2, SnO2, SnO2/TiO2Nanoparticles – Polypropylene Fibrous Carrier” Systems. It has been determined that MCPA phototransformation is most efficient when using the “TiO2/SnO2heteronanoparticles – carrier” system with the concentration of 25/6 mg/g. The results indicate that systems with applied semiconductor particles do not exhibit sorption properties towards МСРА molecules. Therefore, the change in the spectral characteristics of a МСРА water solution after time-exposure and exposure to radiation is only associated with the phototransformations of non-adsorbed МСРА molecules and with the emergence of their photodegradation products.


1995 ◽  
Vol 198 (11) ◽  
pp. 2271-2278 ◽  
Author(s):  
G Mackie ◽  
R Meech

1. The ring giant axon in the outer nerve ring of the jellyfish Aglantha digitale is a multinucleate syncytium 85 % of which is occupied by an electron-dense fluid-filled vacuole apparently in a Gibbs­Donnan equilibrium with the surrounding band of cytoplasmic cortex. Micropipette recordings show small (-15 to -25 mV) and large (-62 to -66 mV) resting potentials. Low values, obtained with a high proportion of the micropipette penetrations, are assumed to be from the central vacuole; high values from the cytoplasmic cortex. Background electrical activity includes rhythmic oscillations and synaptic potentials representing hair cell input caused by vibration. 2. After the ring giant axon has been cut, propagating action potentials evoked by stimulation are conducted past the cut and re-enter the axon on the far side. The system responsible (the carrier system) through-conducts at a velocity approximately 25 % of that of the ring giant axon and is probably composed of small neurones running in parallel with it. Numerous small neurones are seen by electron microscopy, some making one-way and some two-way synapses with the ring giant. 3. Despite their different conduction velocities, the two systems normally appear to fire in synchrony and at the velocity of the ring giant axon. We suggest that, once initiated, ring giant spikes propagate rapidly around the margin, firing the carrier neurones through serial synapses and giving them, in effect, the same high conduction velocity. Initiation of ring giant spikes can, however, require input from the carrier system. The spikes are frequently seen to be mounted on slow positive potentials representing summed carrier postsynaptic potentials. 4. The carrier system fires one-for-one with the giant axons of the tentacles and may mediate impulse traffic between the latter and the ring giant axon. We suggest that the carrier system may also provide the pathways from the ring giant to the motor giant axons used in escape swimming. 5. The findings show that the ring giant axon functions in close collaboration with the carrier system, increasing the latter's effective conduction velocity, and that interactions with other neuronal sub-systems are probably mediated exclusively by the carrier system.


Marine Drugs ◽  
2018 ◽  
Vol 16 (8) ◽  
pp. 270
Author(s):  
Johannes Imhoff ◽  
Mingshuang Sun ◽  
Jutta Wiese ◽  
Marcus Tank ◽  
Axel Zeeck

The production of secondary metabolites by a new isolate of the purple sulfur bacterium Allochromatium vinosum, which had shown antibiotic activities during a preliminary study, revealed the production of several metabolites. Growth conditions suitable for the production of one of the compounds shown in the metabolite profile were established and compound 1 was purified. The molecular formula of compound 1 (C20H28O2) was determined by high resolution mass spectra, and its chemical structure by means of spectroscopic methods. The evaluation of these data revealed that the structure of the compound was identical to dehydroabietic acid, a compound known to be characteristically produced by conifer trees, but so far not known from bacteria, except cyanobacteria. The purified substance showed weak antibiotic activities against Bacillus subtilis and Staphylococcus lentus with IC50 values of 70.5 µM (±2.9) and 57.0 µM (±3.3), respectively.


2020 ◽  
Vol 17 ◽  
Author(s):  
Ritika Gupta ◽  
Amrish Kumar

: Vesicular systems have many advantages like prolong the existence of the drug in the systemic circulation, minimizes the undesirable side-effects, reaches the active moieties to its target sites using the carriers. But the main drawback related to transdermal delivery is to cross stratum corneum which can be overcome by the utilization of novel carrier systems e.g. transfersomes which are ultra-deformable carrier system composed of phospholipid (phosphatidylcholine) and edge activators (surfactants). Edge activators are responsible for the flexibility of the bilayer membranes of transfersomes. Different edge activators utilized for transfersomes include tween, span, bile salts (sodium cholate and sodium deoxycholate) and dipotassium glycyrrhizinate. These activators decrease the interfacial tension therefore increases the deformability of carrier system. Transfersomes can encapsulate both hydrophilic and hydrophobic drugs into a vesicular structure which consists of one or more concentric bilayers. Due to the elastic nature of transfersomes, they can easily cross the natural physiological barriers i.e., skin and deliver the drug to its active site. The main benefit of using transfersomes as a carrier is the delivery of macromolecules through the skin by non-invasive route therefore increasing the patient’s compliance. The transfersomal formulations can be used in the treatment of ocular diseases, alopecia, vulvovaginal candidiasis, osteoporosis, apotic dermatitis, tumor, leishmaniasis. It is also used in the delivery of growth hormones, anaesthesia, insulin, proteins, and herbal drugs. This review also focuses on the patents and clinical studies for various transfersomal products.


2020 ◽  
Vol 10 (5) ◽  
pp. 1677
Author(s):  
Min Wei ◽  
Xuyan Song ◽  
Xi Pan ◽  
Ran Li ◽  
Chan Chen ◽  
...  

The design of appropriate thermally responsive fragrance carrier systems is of significant importance for the application of fragrance in the food and tobacco industries. In this study, we investigate the potential of sorbitan monostearate and guar gum for the stabilization of menthol under ambient conditions and the thermally-induced release of menthol. Our results show that the sorbitan monostearate carrier could well stabilize the menthol for at least up to 15 days with neglectable menthol loss due to the favorable binding of menthol on the sorbitan monostearate carrier. In addition, rapid and controlled release of menthol could take place at a temperature of 80 °C in the sorbitan monostearate carrier system. As a comparison, guar gum could not stabilize menthol as a result of its poor compatibility. Our results suggest that sorbitan monostearate can be an ideal carrier material for the support of fragrance. In addition, our results also provide a useful guide for the tailored design of thermally responsive fragrance carriers.


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