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2022 ◽  
Vol 18 ◽  
pp. 102-109
Author(s):  
Jolita Bruzgulienė ◽  
Greta Račkauskienė ◽  
Aurimas Bieliauskas ◽  
Vaida Milišiūnaitė ◽  
Miglė Dagilienė ◽  
...  

A convenient and efficient synthesis of novel achiral and chiral heterocyclic amino acid-like building blocks was developed. Regioisomeric methyl 5-(N-Boc-cycloaminyl)-1,2-oxazole-4-carboxylates were prepared by the reaction of β-enamino ketoesters (including azetidine, pyrrolidine or piperidine enamines) with hydroxylamine hydrochloride. Unambiguous structural assignments were based on chiral HPLC analysis, 1H, 13C, and 15N NMR spectroscopy, HRMS, and single-crystal X-ray diffraction data.


2022 ◽  
Author(s):  
Yu Xu ◽  
Wujie Xu ◽  
Xiaojuan Hu ◽  
Haochang Su ◽  
Guoliang Wen ◽  
...  

Abstract Microcystis aeruginosa is a common kind of harmful bloom algae, which was also frequently found as a dominant microalgae specie in shrimp breeding ponds. And it was found that blooms always induced massive death of shrimp, but the toxic effects of M. aeruginosa on Litopenaeus vannamei are still not completely understood. In this paper, the toxicity of M. aeruginosa cells to L. vannamei was examined, and the toxic components in the cells were analyzed through high-pressure liquid chromatography (HLPC). In addition, the immune response of shrimp to the microalgal extract was assessed by measuring the activity of immune-related enzymes, as well as the transcription of the relevant genes. Overall, both M. aeruginosa cells and the algal extract resulted in a 100% mortality rate in shrimp, whereas the cell-free culture medium was ineffective. And HPLC analysis results revealed the presence of microcystin-LR (MC-LR) at a concentration of 190.40 mg/kg of cells. In addition, the activity and gene transcription of two immune related enzymes, SOD and LZM, were both significantly reduced in shrimp hepatopancreas (p<0.05) after injection with cell extract. However, reduced glutathione (GSH) content was slightly increased, but the ratio of GSH to GSSG was down, and the transcription of gst gene function as detoxification, was significantly downregulated (p<0.05). The results demonstrated that M. aeruginosa cell extract was highly toxic to L. vannamei, and exerted a negative effect on shrimp immunity including reduction of antioxidant capacity, antibacterial activity and detoxification activity, due to microcystin-LR.


Author(s):  
Fumiyuki Kiuchi

AbstractAchyranthes root is a crude drug used as diuretic, tonic and remedy for blood stasis. Characteristic oleanolic acid saponins with a dicarboxylic acid moiety have been isolated as one of the representative constituents of this crude drug. This review focuses on the triterpene saponin constituents, especially those with a characteristic dicarboxylic acid moiety, of A. bidentata and A. fauriei. Several groups isolated the saponins and different names were given to one compound in some cases. The names of the compounds are sorted out and the stereochemistry of the dicarboxylic acid moieties are summarized. HPLC analysis of the composition of the saponin constituents and the effect of processing and extraction conditions on the composition are reviewed. Biological activities of the saponin constituents are also summarized.


2022 ◽  
Vol 8 (1) ◽  
Author(s):  
R. N. Hota ◽  
B. K. Nanda ◽  
B. R. Behera ◽  
A. Bose

Abstract Background Limnophila rugosa (Scrophulariaceae) is a perennial aquatic plant used as a diuretic and digestive tonic as well as in the treatment of diarrhea, dysentery, dyspepsia and urinary ailments. Genus Limnophila has been reported as hepatoprotective. The present study was undertaken to evaluate the hepatoprotective activity of the ethanolic extract of L. rugosa aerial part in paracetamol- and carbon tetrachloride-induced (CCl4) hepatotoxicity in albino Wistar rats. Ethanolic extract was subjected to high-performance liquid chromatography (HPLC) analysis for the estimation of phenolic and flavonoid compounds and gas chromatography–mass spectrometry (GC–MS) analysis for phytochemical analysis. The in vitro antioxidant activity was carried out by 2,2-diphenyl-1-picrylhydrazyl, nitric oxide radical and hydrogen peroxide assay. Hepatoprotective potential of L. rugosa was studied in paracetamol (750 mg/mg)- and CCl4 (1.25 ml/kg)-induced liver damage in albino rats at dose 200 and 300 mg/kg using silymarin (100 mg/kg) as standard. Lipid peroxidation, superoxide dismutase (SOD), catalase (CAT) and glutathione (GSH) were determined in liver tissue homogenate. Serum biochemical and histopathological examination was performed. Molecular docking analysis was performed to understand the molecular mechanism of hepatoprotective activity. Results HPLC analysis revealed predominance of rutin. GC–MS analysis revealed camphor as principal component. Ethanolic extract exhibited significant concentration-dependent scavenging efficacy. The altered biochemical chemical parameters: aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, bilirubin, cholesterol, albumin, globulin and total protein, were significantly improved at 200 and 300 mg/kg in experimental rats. Extract signified hepatoprotective by decreasing lipid peroxidation and upregulating SOD, CAT and GSH. The findings were well supported by histological analysis. 2-Butyl-2, 7-octadien-1-ol (-5.8) and camphor (-4.8) gave the highest docking score on the transforming growth factor-β1. Conclusions The ameliorative effect of L. rugosa in the rat model of hepatotoxicity could be attributed to its antioxidant potential and bioactive principles such as betulin, 5-hydroxy-6,7,4′-trimethoxyflavone (salvigenin), betulinic acid, ursolic acid, 3-octanol, acetophenone, anisylacetone, caryophyllene, cis-anethole and the compounds camphor and 2-butyl-2,7-octadien-1-ol identified from GC–MS analysis.


2022 ◽  
Vol 34 (2) ◽  
pp. 284-288
Author(s):  
K. Kerdchan ◽  
P. Srihanam

Crude ethanolic extracts of four cultivars of sugarcane (Saccharum officinarum L.) were firstly prepared and then fractionated using silica gel column chromatography before the determination of their oxidative substances. The fractionated extracts were then tested for antioxidant activity by various assays. Finally, high-performance liquid chromatography (HPLC) was applied for the quantitative determination of the individual phenolic compounds. Sub-fraction 2 has the highest phytochemical contents as well as antioxidant activity. All tested phytochemicals had positively correlated to antioxidant activity. HPLC analysis showed that the phytochemicals in the fractionated extracts varied by the sugarcane cultivars. The main flavonoid substances found in the fractionated extracts were epicatechin, catechin, quercetin, resveratrol, myricetin and rutin while gallic acid was the main phenolic substance. The obtained information is useful for further studies and applications.


2021 ◽  
Vol 19 (4) ◽  
pp. 619-626
Author(s):  
Sol-Hui Song ◽  
Hoon Kim

Purpose: In this study, we study to more effectively use anesthesia products used in beauty procedures following the popularization of anti-aging. Hydrogel, which contains lidocaine, is believed to be more effective in relieving pain if used in cosmetic procedures with ultrasonic waves.Methods: The availability of manufactured hydrogels and commercial gels for ultrasonic treatment was compared, and the effect on skin penetration and skin penetration due to ultrasonic limitations was evaluated based on their applicability. Usability and optimal ultrasound parameters were identified during ultrasound treatment.Results: Viscosity measurement, gelation rate, swelling, skin permeability experiment, and HPLC analysis of manufactured hydrogels all revealed properties, with skin permeability being highest at frequency 1 MHz, cycle low 200, and high 50.Conclusions: Finally, hydrogels containing lidocaine increased skin permeability during ultrasound treatment, allowing for faster targeted transdermal transmission that was more effective depending on the ultrasound parameters. As a result, it is determined that it can be used in cosmetic procedures.


Author(s):  
Julia Hesse ◽  
Mona K. Rosse ◽  
Bodo Steckel ◽  
Bernhard Blank-Landeshammer ◽  
Svenja Idel ◽  
...  

AbstractCD73-derived adenosine plays a major role in damage-induced tissue responses by inhibiting inflammation. Damage-associated stimuli, such as hypoxia and mechanical stress, induce the cellular release of ATP and NAD+ and upregulate the expression of the nucleotide-degrading purinergic ectoenzyme cascade, including adenosine-generating CD73. Extracellular NAD+ also serves as substrate for mono-ADP-ribosylation of cell surface proteins, which in human cells is mediated by ecto-ADP-ribosyltransferase 1 (ARTC1). Here we explored, whether human CD73 enzymatic activity is regulated by mono-ADP-ribosylation, using recombinant human CD73 in the presence of ARTC1 with etheno-labelled NAD+ as substrate. Multi-colour immunoblotting with an anti-etheno-adenosine antibody showed ARTC1-mediated transfer of ADP-ribose together with the etheno label to CD73. HPLC analysis of the enzymatic activity of in vitro-ribosylated CD73 revealed strong inhibition of adenosine generation in comparison to non-ribosylated CD73. Mass spectrometry of in vitro-ribosylated CD73 identified six ribosylation sites. 3D model analysis indicated that three of them (R328, R354, R545) can interfere with CD73 enzymatic activity. Our study identifies human CD73 as target for ARTC1-mediated mono-ADP-ribosylation, which can profoundly modulate its adenosine-generating activity. Thus, in settings with enhanced release of NAD+ as substrate for ARTC1, assessment of CD73 protein expression in human tissues may not be predictive of adenosine formation resulting in anti-inflammatory activity.


2021 ◽  
Vol 10 (4) ◽  
pp. 122-128
Author(s):  
A. V. Lezina ◽  
I. I. Terninko ◽  
M. V. Krysko

Introduction. Orthilia secunda (L.) House is a perennial herb that grows in Europe, Siberia, Asia Minor and Central Asia. The herb of Orthilia secunda is actively used in folk medicine as a diuretic, wound-healing and anti-inflammatory agent. From literary sources it is known that this medicinal plant raw material (PRM) contains flavonoids, tannins, organic acids, vitamins, as well as simple phenols and their derivatives (arbutin and hydroquinone). The presence of arbutin is responsible for the plant's high antioxidant and anti-inflammatory properties. But the use of Orthilia secunda in official medicine is limited due to the lack of complete information on the chemical composition and criteria for standardization of this type of medicinal product.Aim. Identification and quantification of arbutin by chromatographic methods in Orthilia secunda (L.) House, harvested in various phytocenotic zones.Materials and methods. The investigated medicinal plant material – the herb of Orthilia secunda – was harvested in various phytocenotic zones: in July 2018, harvesting was carried out in the northern part of Kazakhstan (Kokshetau district), in July-August 2019 in the Perm Territory and in the Tyumen Region. Preliminary identification of arbutin and related phenols – gallic acid and hydroquinone – was carried out by high performance thin layer chromatography (HPTLC) on a CAMAG instrument with a UV cabinet (Merck HPTLC silica gel 60 F154 plates, 20 × 10), semi-automatic Linomat 5 applicator (sample application). Elution of the plates was performed in a CAMAG Automatic Developing Chamber (ADC2). Image fixation was performed on a CAMAG Scanner 3 spectrodensitometer. The quantitative determination of arbutin was carried out by the method of highperformance liquid chromatography, which was carried out on a Prominence LC-20 device (Shimadzu, Japan) according to the validated method described in the European Pharmacopoeia 10.0. Diode array detector SPD-M20A, column Intersil C18 column (250–4.6 mm, 5 μm) (Phenomenex, USA). The results were processed using the LabSolution software. The identification and quantification of arbutin was carried out in comparison with a standard solution containing a reference sample (RS) of arbutin (C = 0,025 mg/ml) and RS of hydroquinone (C = 0,0125 mg/ml).Results and discussion. HPTLC analysis made it possible to detect arbutin and gallic acid – the main product of hydrolytic degradation/ precursor of the biosynthesis of tannins of the hydrolysable group – in the herb of Orthilia secunda from different places of growth. HPLC analysis demonstrates a different chromatographic profile of Orthilia herb harvested in different phytocenotic zones. However, in all studied objects, the absence of hydroquinone and the presence of substances that can presumably be attributed to its derivatives were confirmed, which is confirmed by the visual similarity of the spectra of these compounds and the proximity of the extrema. It was found that arbutin does not belong to the marker (majority) compounds of Orthilia. Its content is low and reaches a maximum (about 0,021 %) in the herb of Orthilia secunda growing on the territory of Kazakhstan, while in the herb of Orthilia harvested in the Perm Territory arbutin was not identified. From the data obtained, it follows that the greatest accumulation of arbutin occurs in areas with a warmer and drier climate (northern part of Kazakhstan).Conclusion. HPTLC analysis of the herb Orthilia secunda allowed the identification of arbutin and gallic acid (the main precursor of tannins of the hydrolysable group). The results of HPLC analysis of Orthilia herb harvested in various phytocenotic zones suggest quantitative differences in the content of arbutin depending on the region of growth. From the experimental data, it follows that Orthilia growing in the northern part of Kazakhstan accumulates the maximum (0,021%) amount of arbutin, in comparison with the samples harvested in the Tyumen region and the Perm region. At the same time, Orthilia harvested in the Perm Territory does not accumulate arbutin. The presence of hydroquinone has not been confirmed (by HPTLC and HPLC methods); therefore, it is not justified to talk about the hydrolytic cleavage of arbutin in the process of biosynthesis or drying. However, in all studied objects there are peaks of substances with spectral characteristics like hydroquinone, which makes it possible to assume the presence of its derivatives. Therefore, it is not advisable to position arbutin as a marker compound of Orthilia secunda harvested on the territory of the Russian Federation, and to standardize raw materials for this compound.


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