For centuries, macrofungi have been used as food and medicine in different parts of the world. This is mainly attributed to their nutritional value as a potential source of carbohydrates, proteins, ...amino acids, and minerals. In addition, they also include many bioactive metabolites which make mushrooms and truffles common components in folk medicine, especially in Africa, the Middle East, China, and Japan. The reported medicinal effects of mushrooms include anti-inflammatory effects, with anti-inflammatory compounds of mushrooms comprising a highly diversified group in terms of their chemical structure. They include polysaccharides, terpenoids, phenolic compounds, and many other low molecular weight molecules. The aims of this review are to report the different types of bioactive metabolites and their relevant producers, as well as the different mechanisms of action of mushroom compounds as potent anti-inflammatory agents.
In the process of profiling the secondary metabolites of actinobacteria isolated from the Saudi coastal habitats for production of antibiotics and anti-cancer drugs, the cultures of strain WH1 that ...was identified as
exhibited strong antibacterial activity against
. By means of MS and NMR techniques, the active compounds were characterized as actinomycins X
, X
, and D, respectively. The research on the productivity of this strain for actinomycins revealed that the highest production of actinomycins X
, X
, and D was reached in the medium MII within 5% salinity and pH 8.5. In this optimized condition, the fermentation titers of actinomycins X
, X
, and D were 107.6 ± 4.2, 283.4 ± 75.3, and 458.0 ± 76.3 mg/L, respectively. All the three actinomycins X
, X
, and D showed potent cytotoxicities against the MCF-7, K562, and A549 tumor cell lines, in which actinomycin X
was the most active against the three tumor cell lines with the IC
values of 0.8-1.8 nM. Both actinomycins X
and D showed potent antibacterial activities against
and the methicillin-resistant
, and
and the actinomycin X
was more potent.
(Syn.
) (
) is used in the rural Egypt to treat oral ulcers in newborn children. The current study aimed to discover new natural products suitable for treating candidiasis disease with minimal side ...effects. Characterization of bioactive compounds by LC-QTOF-HR-MS/MS from
fresh leaves' juice (CMJ) was carried out in order to elucidate their potential anti-fungal and immunomodulatory effects in oral candidiasis in immunosuppressed rats. An oral ulcer candidiasis model was created in three stages: (i) immunosuppression by drinking dexamethasone (0.5 mg/L) for two weeks; (ii)
infection (3.00 × 10
viable cell/mL) for one week; and (iii) treatment with CMJ (0.5 and 1.0 g/kg orally) or nystatin (1,000,000 U/L orally) for one week. Two doses of CMJ exhibited antifungal effects, for example, through a significant reduction in CFU/Petri (236.67 ± 37.86 and 4.33 ± 0.58 CFU/Petri), compared to the
control (5.86 × 10
± 1.21 CFU/Petri),
≤ 0.001. In addition, CMJ significantly induced neutrophil production (32.92% ± 1.29 and 35.68% ± 1.77) compared to the
control level of 26.50% ± 2.44. An immunomodulatory effect of CMJ at two doses appeared, with a considerable elevation in INF-γ (103.88 and 115.91%), IL-2 (143.50, 182.33%), and IL-17 (83.97 and 141.95% Pg/mL) compared with the
group. LC-MS/MS analysis operated in negative mode was used for tentative identification of secondary (SM) metabolites based on their retention times and fragment ions. A total of 42 phytoconstituents were tentatively identified. Finally, CMJ exhibited a potent antifungal effect. CMJ fought
through four strategies: (i) promotion of classical phagocytosis of neutrophils; (ii) activation of T cells that activate IFN-γ, IL-2, and IL-17; (iii) increasing the production of cytotoxic NO and H
O
that can kill
; and (iv) activation of SOD, which converts superoxide to antimicrobial materials. These activities could be due to its active constituents, which are documented as anti-fungal, or due to its richness in flavonoids, especially the active compounds of kaempferol glycosides and aglycone, which have been documented as antifungal. After repetition on another type of small experimental animal, their offspring, and an experimental large animal, this study may lead to clinical trials.
The human nail plate is a formidable barrier to drug permeation. Development of therapeutics for management of nail diseases thus remains a challenge. This article reviews the current knowledge and ...recent advances in the field of transungual drug delivery and provides guidance on development of topical/ungual therapeutics for management of nail diseases, with special emphasis on management of onychomycosis, the most common nail disease. Selection of drug candidates, drug delivery approaches, and evaluation of formulations are among the topics discussed. A comprehensive mathematical description for transungual permeation is also introduced.
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Abstract
Gravitational energy storage systems are among the proper methods that can be used with renewable energy. However, these systems are highly affected by their design parameters. This paper ...presents a novel investigation of different design features of gravity energy storage systems. A theoretical model was developed using MATLAB SIMULINK to simulate the performance of the gravitational energy storage system while changing its design parameters. A parametric optimization study was also conducted using Taguchi and analysis of variance (ANOVA) techniques for optimizing the energy storage rate. Six parameters were studied; three are related to the piston design (diameter, height, and material density). The other parameters are the return pipe diameter, length, and charging/discharging time. Results revealed that the piston diameter and height are the two most significant parameters for the system performance compared to the other parameters, as they contributed by 35.11% and 30.28%, respectively. The optimization results indicated that the optimal piston diameter, height, and return pipe diameter were 0.25, 0.5, and 0.01 of the container height. The outcomes of this paper can significantly improve energy storage and power generation from renewable energy systems as it provides a reliable, economical, sustainable, and durable energy storage system.
Despite intensive research, the mechanisms by which vesicular systems deliver drugs into intact skin are not yet fully understood. In the current study, possible mechanisms by which deformable ...liposomes and ethosomes improve skin delivery of ketotifen under non-occlusive conditions were investigated. In vitro permeation and skin deposition behavior of deformable liposomes and ethosomes, having ketotifen both inside and outside the vesicles (no separation of free ketotifen), having ketotifen only inside the vesicles (free ketotifen separated) and having ketotifen only outside the vesicles (ketotifen solution added to empty vesicles), was studied using rabbit pinna skin. Results suggested that both the penetration enhancing effect and the intact vesicle permeation into the stratum corneum might play a role in improving skin delivery of drugs by deformable liposomes, under non-occlusive conditions, and that the penetration enhancing effect was of greater importance in case of ketotifen. Regarding ethosomes, results indicated that ketotifen should be incorporated in ethosomal vesicles for optimum skin delivery. Ethosomes were not able to improve skin delivery of non-entrapped ketotifen.
A novel series of pyrazole analogues including hydrazones, pyrazolo4,3-c-pyridazines, pyrazolo3,4-e1,2,4triazine and pyrazolo3,4-d1,2,3triazoles was designed, synthesised and screened for their ...in vitro antimicrobial and DHFR inhibition activity. Compounds bearing benzenesulphonamide moiety incorporated with 3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene) hydrazine 3a or 6-amino-7-cyano-3-methyl-5H-pyrazolo4,3-cpyridazine 6a revealed excellent and broad spectrum antimicrobial activity comparable to ciprofloxacin and amphotericin B as positive antibiotic and antifungal controls, respectively. Furthermore, these derivatives proved to be the most active DHFR inhibitors with IC
50
values 0.11 ± 1.05 and 0.09 ± 0.91 µM, in comparison with methotrexate (IC
50
= 0.14 ± 1.25 µM). The in silico studies were done to calculate the drug-likeness and toxicity risk parameters of the newly synthesised derivatives. Additionally, the high potency of the pyrazole derivatives bearing sulphonamide against DHFR was confirmed with molecular docking and might be used as an optimum lead for further modification.
Celotno besedilo
Dostopno za:
DOBA, IZUM, KILJ, NUK, PILJ, PNG, SAZU, UILJ, UKNU, UL, UM, UPUK
High concentrations of graphene oxide (GO), a nanoparticle substance with rapid manufacturing development, have the ability to penetrate the soil surface down to the mineral-rich subsurface layers. ...The destiny and distribution of such an unusual sort of nanomaterial in the environment must therefore be fully understood. However, the way the chemistry of solutions impacts GO nanoparticle adsorption on clay minerals is still unclear. Here, the adsorption of GO on clay minerals (e.g., bentonite and kaolinite) was tested under various chemical conditions (e.g., GO concentration, soil pH, and cation valence). Non-linear Langmuir and Freundlich models have been applied to describe the adsorption isotherm by comparing the amount of adsorbed GO nanoparticle to the concentration at the equilibrium of the solution. Our results showed fondness for GO in bentonite and kaolinite under similar conditions, but the GO nanoparticle adsorption with bentonite was superior to kaolinite, mainly due to its higher surface area and surface charge. We also found that increasing the ionic strength and decreasing the pH increased the adsorption of GO nanoparticles to bentonite and kaolinite, mainly due to the interaction between these clay minerals and GO nanoparticles’ surface oxygen functional groups. Experimental data fit well to the non-linear pseudo-second-order kinetic model of Freundlich. The model of the Freundlich isotherm was more fitting at a lower pH and higher ionic strength in the bentonite soil while the lowest R2 value of the Freundlich model was recorded at a higher pH and lower ionic strength in the kaolinite soil. These results improve our understanding of GO behavior in soils by revealing environmental factors influencing GO nanoparticle movement and transmission towards groundwater.
It is imperative to distribution system operators to provide quantitative as well as qualitative power demand and satisfy consumers’ satisfaction. So, it is important to address one of the most ...promising combinatorial optimization problems for the optimal integration of power distribution network reconfiguration (PDNR) with distributed generations (DGs). In this regard, this paper proposes an improved equilibrium optimization algorithm (IEOA) combined with a proposed recycling strategy for configuring the power distribution networks with optimal allocation of multiple distributed generators. The recycling strategy is augmented to explore the solution space more effectively during iterations. The effectiveness of the proposed algorithm is checked on 23 standard benchmark functions. Simultaneous integration of PDNR and DG are carried out considering the 33 and 69-bus distribution test systems at three different load levels and its superiority is established. Verification of the proposed technique on large scale distribution system with a variety of control variables is introduced on a 137-bus large scale distribution system. These simulations lead to enhanced distribution system performance, quality and reliability. While, the integration represents a challenge for complexity and disability to achieve optimal solutions of the considered problem especially for multi-objective framework. To solve this challenge, a multi-objective function is developed considering total active power loss and overall voltage enhancement with respecting the system limitations. The proposed algorithm is contrasted with harmony search, genetic, refined genetic, fireworks, and firefly optimization algorithms. The obtained results confirm the effectiveness and robustness of the proposed technique compared with the competitive algorithms.
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•A newly proposed meta-heuristic IEOA is introduced in this work.•The proposed IEOA is applied on 23 standard benchmark functions.•The proposed technique verification is compared with other previous techniques.•The suggested IEOA is validated on three distribution systems.•The findings of simultaneous PDNR/DG allocation show the IFOA effectiveness.
The current study proposes a new strategy for using small hydroelectric turbines in downstream river branches with the least amount of construction and the lowest cost by comparing two different ...methods of installing the turbines, the first by installing the turbines at the river's bottom and the second by installing the turbines on floating boats. The methodology of this article is based on predicting the distribution of velocities through the watercourse using experimental data collected at various points in the river's depth, and then predicting the resulting electrical power for different sizes of turbines, as well as estimating the number of turbines for each row and the number of rows along the river. Therefore, Investigate the proposed systems. The proposed small hydropower system's economic viability and environmental impact are investigated in this article. According to the nature of the waterway, the best diameter of a turbine that can be used is 1.5 m based on water velocities and river depths. The proposed power plant generated 25.8 kW per single turbine row, with an estimated cost of produced power (0.035 USD/kWh) of approximately 20 turbines installed per row. Compared to other renewable energy sources, the proposed hydropower system is cost-effective and environmentally friendly, as generating electricity with the proposed small hydropower plant could reduce annual carbon dioxide emissions by 368 tones of CO2 per single turbine row.