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Mountain caviar is a fruit of Kochia scoparia that contains momordin Ic as a major saponin constituent. Its extract (MCE) has been shown to suppress blood glucose elevations in the human oral glucose tolerance test (OGTT) as well as increases in blood glucose in OGTT, gastric emptying (GE), and glucose incorporation in the small intestine in rats. However, the effects of MCE and momordin Ic on glucose absorption in mice and these action mechanisms have not been examined for more than 2 decades. Therefore, we herein investigated the effects of MCE, its saponin fraction, and momordin Ic on blood glucose elevations in mice. Mouse blood glucose elevation tests were performed on carbohydrate-loaded mice. The mountain caviar saponin fraction significantly delayed blood glucose elevations in glucose-, sucrose-, and soluble starch-loaded mice. In glucose-loaded mice, the saponin fraction, MCE, and momordin Ic significantly suppressed rapid glucose elevations after glucose loading, but not sucrose loading. A mouse GE study was performed by loading with glucose and phenolphthalein solution. Momordin Ic and MCE strongly suppressed mouse GE. Intestinal glucose absorption was evaluated by the incorporation of 2-deoxyglucose (2-DG) into Caco-2 cell layers and mouse duodenum wall vesicles. The results obtained showed that momordin Ic inhibited the incorporation of 2-DG into Caco-2 cells and mouse duodenum vesicles. Collectively, these results suggest that MCE, particularly the principal saponin, momordin Ic, preferably suppressed glucose-induced blood glucose elevations and delayed carbohydrate-induced glucose elevations in mice. The underlying mechanism was found to involve the suppression of GE and intestinal glucose absorption.
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Glicemia , Glucose , Hipoglicemiantes , Extratos Vegetais , Saponinas , Animais , Camundongos , Saponinas/farmacologia , Saponinas/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Humanos , Células CACO-2 , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Masculino , Glicemia/efeitos dos fármacos , Glucose/metabolismo , Absorção Intestinal/efeitos dos fármacos , Teste de Tolerância a Glucose , Esvaziamento Gástrico/efeitos dos fármacos , Frutas/química , Camundongos Endogâmicos ICRRESUMO
Ion chromatography (IC) is a novel high performance liquid chromatographic technique that is suitable for the separation and analysis of ionic substances in different matrix samples. Since 1975, it has been widely used in many fields, such as the environment, energy, food, and medicine. IC compensates for the separation limitations of traditional gas chromatography and high performance liquid chromatography and can realize the qualitative analysis and quantitative detection of strongly polar components. This chromatographic technique features not only simple operations but also rapid analysis. The sensors used in IC are characterized by high sensitivity and selectivity, and the technique can simultaneously separate and determine multiple components. Several advances in IC instrumentation and chromatographic theories have been developed in recent years. IC can analyze various types of samples, including ions, sugars, amino acids, and organic acids (bases). Chinese herbal medicines are typically characterized by highly complex chemical compositions and may contain carbohydrates, proteins, alkaloids, and other active components. They also contain toxic residues such as sulfur dioxide, which may be produced during the processing of medicinal materials. Therefore, the analysis and elucidation of the precise chemical constituents of Chinese herbal medicines present key problems that must be resolved in modern Chinese herbal medicine research. In this context, IC has become an important method for analyzing and identifying the complex components of Chinese herbal medicines because this method is suitable for detecting a single active ingredients among complex components. This paper introduces the different types and principles of IC as well as research progress in this technique. As the applications of IC-based methods in pharmaceutical science, cell biology, and microbiology increase, further development is necessary to expand the applications of this technique. The development of innovative techniques has enabled IC technologies to achieve higher analytical sensitivity, better selectivity, and wider application. The components of Chinese herbal medicines can be divided into endogenous and exogenous components according to their source: endogenous components include glycosides, amino acids, and organic acids, while exogenous components include toxic residues such as sulfur dioxide. Next, the applications of IC to the complex components of Chinese herbal medicines in recent decades are summarized. The most commonly used IC technologies and methods include ion exchange chromatography and conductivity detection. The advantages of IC for the analysis of alkaloids have been demonstrated. This method exhibits better characteristics than traditional analytical methods. However, the applications of IC for the speciation analysis of inorganic anions are limited. Moreover, few reports on the direct application of the technique for the determination of the main active substances in Chinese herbal medicines, including flavonoids, phenylpropanoids, and steroids, have been reported. Finally, this paper reviews new IC technologies and their application progress in Chinese herbal medicine, focusing on their prospects for the effective separation and analysis of complex components. In particular, we discuss the available sample (on-line) pretreatment technologies and explore possible technologies for the selective and efficient enrichment and separation of different components. Next, we assess innovative research on solid-phase materials that can improve the separation effect and analytical sensitivity of IC. We also describe the features of multidimensional chromatography, which combines the advantages of various chromatographic techniques. This review provides a theoretical reference for the further development of IC technology for the analysis of the complex chemical components of Chinese herbal medicines.
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Alcaloides , Medicamentos de Ervas Chinesas , Medicamentos de Ervas Chinesas/análise , Dióxido de Enxofre/análise , Alcaloides/análise , Cromatografia Líquida de Alta Pressão , Íons , Medicina Tradicional ChinesaRESUMO
The study focused on the morphological and chemical characteristics of 200 Hymenocrater longiflorus Benth. genotypes found in natural habitats of eight regions in west of Iran. The primary objective of the study was to assess the morphological and phytochemical variability within populations grown in their natural habitats, with the aim of identifying their potential for domestication and utilization in pre-breeding programs. The plant height (PH) ranged from 50.32 to 69.65 cm, with the highest observed in population P8. The internode distances ranged from 4.7 to 6.47 cm, with the maximum distance found in P4. Flower lengths varied from 1.95 to 2.45 cm, with the minimum and maximum values observed in P4 and P3, respectively. The highest leaf length (5.20 cm) and width (3.87 cm) were recorded in P2. The aerial parts of the plant were utilized to extraction and determine the essential oil (EO) content and composition, which ranged from 0.40 to 0.78% (v/w). The analysis of EO by gas chromatography (GC) and gas chromatography mass spectrometry (GC/MS) identified 26 compounds, constituting 99-99.5% of the EOs. The main compounds in the EO and their percentage range (v/w DW) were tau-cadinol (0.62-55.56), mono (2-ethylhexyl) phthalate (8.10-94.70), elemol (0.21-19.11), ß-spathulenol (0.08-14.39), 4-terpineol (0.23-10.19), and ß-eudesmol (0.21-9.94). The main chemical groups found in EOs included oxygenated sesquiterpenes (1.12-68.43), and phthalates (9.73-94.72). Cluster analysis revealed three distinct chemotypes: chemotype I (populations 1 and 2) with major components of mono (2-ethylhexyl) phthalate, tau-cadinol, and α-elemol; chemotype II (population 5) rich in mono (2-ethylhexyl) phthalate; and chemotype III (populations 3, 4, 6-8) containing tau-cadinol, ß-eudesmol, and 4-terpineol. The study also evaluated total phenolic, total flavonoid, and DPPH free radical scavenging activity in the fifty percent inhibitory concentration (IC50) in leaf and flower samples of the genotypes, along with estimating total anthocyanin content in the flower samples. The total phenolic content (TPC) in leaf and flower samples ranged from 7.89 to 107.18 mg GAE/g DW and 39.98 to 86.62 mg gallic acid equivalent (GAE)/g DW, respectively. Total flavonoid content (TFC) ranged from 81.04 to 143.46 mg QUE/g DW in leaf samples and from 94.82 to 133.26 mg quercetin equivalent (QUE)/g DW in flower samples. DPPHsc IC50 (µg/mL) ranged from 0.65 to 78.74 in leaf samples and from 4.38 to 7.71 in flower samples. Anthocyanin content ranged from 1.89 to 3.75 mg cyanidin-3-glucoside equivalent (C3GE)/g DW among populations. Canonical correspondence analysis and simple correlation demonstrated a strong association and correlations among the studied attributes. The negative correlations between leaf DPPH (DPPH L) IC50 and TFC (- 0.73), TPC (- 0.63), Elemol (- 0.90), and EO (- 0.85) indicate that these compounds have a significant impact on the antioxidant activity of the leaves. Furthermore, Fruit DPPH (DPPH F) IC50 showed a negative correlation with TPC (- 0.79) and TFC (- 0.78), but a positive correlation with flower anthocyanins (0.51), (Z)-ß-Farnesene (0.66), and 4-Terpineol (0.57). Circular cluster analysis categorized the genotypes of all individuals in the eight studied populations into three main categories based on all the studied traits, indicating significant variation in phytochemical and morphological traits among populations, surpassing the within-populations variation.
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Lamiaceae , Óleos Voláteis , Ácidos Ftálicos , Sesquiterpenos de Eudesmano , Sesquiterpenos , Humanos , Antioxidantes/farmacologia , Óleos Voláteis/farmacologia , Antocianinas , Irã (Geográfico) , Extratos Vegetais/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Melhoramento Vegetal , Fenóis/análise , Quercetina , Flavonoides/análise , Compostos FitoquímicosRESUMO
The current study aimed to find an effective, simple, ecological, and nontoxic method for bacterial green synthesis of zinc oxide nanoparticles (ZnONPs) using the bacterial strain Priestia megaterium BASMA 2022 (OP572246). The biosynthesis was confirmed by the change in color of the cell-free supernatant added to the zinc nitrate from yellow to pale brown. The Priestia megaterium zinc oxide nanoparticles (Pm/ZnONPs) were characterized using UV-Vis spectroscopy, high-resolution transmission electron microscopy (HR-TEM), energy-dispersive X-ray spectroscopy (EDX), Fourier transform infrared spectroscopy (FTIR), and zeta potential. The Pm/ZnONPs characterization showed that they have a size ranging between 5.77 and 13.9 nm with a semi-sphere shape that is coated with a protein-carbohydrate complex. An EDX analysis of the Pm/ZnONPs revealed the presence of the shield matrix, which was composed of carbon, nitrogen, oxygen, chlorine, potassium, sodium, aluminum, sulfur, and zinc. The results of the FTIR analysis showed that the reduction and stabilization of the zinc salt solution were caused by the presence of O-H alcohols and phenols, O=C=O stretching of carbon dioxide, N=C=S stretching of isothiocyanate, and N-H bending of amine functional groups. The produced ZnONPs had good stability with a charge of - 16.2 mV, as evidenced by zeta potential analysis. The MTT assay revealed IC50 values of 8.42% and 200%, respectively, for the human A375 skin melanoma and human bone marrow 2M-302 cell lines. These findings revealed that the obtained Pm/ZnONPs have the biocompatibility to be applied in the pharmaceutical and biomedical sectors.
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Nanopartículas Metálicas , Nanopartículas , Óxido de Zinco , Humanos , Óxido de Zinco/farmacologia , Óxido de Zinco/química , Nanopartículas Metálicas/química , Nanopartículas/química , Linhagem Celular , Extratos Vegetais/química , Bactérias , Zinco , Antibacterianos/químicaRESUMO
BACKGROUND: Nuciferine's extensive therapeutic potential, including its robust antioxidant properties, is explored in response to the growing consumer preference for value-added organic foods. OBJECTIVE: This study focuses on the formulation of gummy bear supplements fortified with nuciferine from Nelumbonucifera. The research highlights nuciferine's ability to combat oxidative stress induced by reactive oxygen species (ROS) and examines its application in maintaining basal ROS levels during oxidative stress conditions in skin melanoma cells. METHODS: Characterization of extracted nuciferine through FTIR and UV-vis spectroscopy ensures product quality, while sensory evaluation compares honey and sugar as natural sweeteners for optimal flavor and consumer preference. SK-Mel-28 cellular ROS levels were measured using 2',7' -dichlorofluorescin diacetate dye before and after nuciferine treatment. SK-Mel-28 cell viability and dose response of nuciferine treatment was assessed using MTT assay. RESULTS: Nuciferine shows potent inhibition of SK-Mel-28 cell proliferation with an IC50 of 39.31 ± 5.280 µg/ml and showed no cytotoxicity in normal L6 skeletal muscle cells. This study compares the sensory properties of honey and sugar based gummy bear formulations. CONCLUSION: This project aims to create a high-quality, health-promoting dietary supplement that aligns with the evolving trends in organic nutrition and antioxidant supplementation.
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BACKGROUND: The diverse specificity mode of cancer treatment targets and chemo resistance demands the necessity of drug entities which can address the devastating dynamicity of the disease. OBJECTIVES: To check the anti-tumour potential of traditional medicine rich in polyherbal components and metal nanoparticle namely Arkeshwara rasa (AR). MATERIAL METHODS: The AR was prepared in a modified version with reference from Rasaratna Samuchaya and characterized using sophisticated instrumental analysis including XRD, SEM-EDAX, TEM, TGA-DSC, and LC-MS and tested against the MDA-MB-231 cell line to screen cell viability and the cytotoxicity with MTT, SRB and the AO assay. RESULTS: XRD pattern shows cubic tetrahedrite structure with Sb, Cu, S peaks and trace elements like Fe, Mg, etc. The particle size of AR ranges between 20 and 30 nm. The TGA points thermal decomposition at 210 °C and the metal sulphide peaks in DSC. LC-MS analysis reveals the components of the formulation more on the flavonoid portion. The IC50 value of MTT and SRB are 25.28 µg/mL and 31.7 µg/mL respectively. The AO colorimeter substantiated the cell viability and the apoptosis figures of the same cell line. The AR exhibits cytotoxicity and reaffirms the apoptosis fraction with SRB assay. CONCLUSIONS: The Hesperidine, Neohesperidin, Rutin components in the phytochemical pool can synergize the anti-tumour potential with either influencing cellular pathways or decreasing chemo resistance to conventional treatment. AR need to be further experimented with reverse transcription, flow cytometry, western blotting, etc.
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Olive trees are one of the most widely cultivated fruit trees in the world. The chemical compositions and biological activities of olive tree fruit and leaves have been extensively researched for their nutritional and health-promoting properties. In contrast, limited data have been reported on olive flowers. The present study aimed to analyse bioactive compounds in olive flower extracts and the effect of fermentation-assisted extraction on phenolic content and antioxidant activity. High-performance thin-layer chromatography (HPTLC) hyphenated with the bioassay-guided detection and spectroscopic identification of bioactive compounds was used for the analysis. Enzymatic and bacterial in situ bioassays were used to detect COX-1 enzyme inhibition and antibacterial activity. Multiple zones of antibacterial activity and one zone of COX-1 inhibition were detected in both, non-fermented and fermented, extracts. A newly developed HPTLC-based experimental protocol was used to measure the high-maximal inhibitory concentrations (IC50) for the assessment of the relative potency of the extracts in inhibiting COX-1 enzyme and antibacterial activity. Strong antibacterial activities detected in zones 4 and 7 were significantly higher in comparison to ampicillin, as confirmed by low IC50 values (IC50 = 57-58 µg in zone 4 and IC50 = 157-167 µg in zone 7) compared to the ampicillin IC50 value (IC50 = 495 µg). The COX-1 inhibition by the extract (IC50 = 76-98 µg) was also strong compared to that of salicylic acid (IC50 = 557 µg). By comparing the locations of the bands to coeluted standards, compounds from detected bioactive bands were tentatively identified. The eluates from bioactive HPTLC zones were further analysed by FTIR NMR, and LC-MS spectroscopy. Multiple zones of antibacterial activity were associated with the presence of triterpenoid acids, while COX-1 inhibition was related to the presence of long-chain fatty acids.
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Olea , Olea/química , Cromatografia em Camada Fina/métodos , Árvores , Extratos Vegetais/química , Flores/química , Antibacterianos/farmacologia , Antibacterianos/análise , Antioxidantes/farmacologia , Espectroscopia de Ressonância Magnética , Ampicilina/análise , Bioensaio/métodosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The terrestrial stems of Ephedra (Ephedra spp.; including Ephedra sinica Stapf and Ephedra przewalskii Stapf) extracts are used in traditional medicines in East Asia. In Japan, the Kampo formula containing E. sinica extract is prescribed for the treatment of the common cold, influenza virus infections, and mild symptoms of coronavirus disease 2019 (COVID-19). Although ephedrine alkaloids in E. sinica exert antitussive effects, they may have side effects associated with the sympathetic nervous system. E. przewalskii extract, a drug used in traditional Uyghur and Mongolian medicine, is considered to be free of ephedrine alkaloids and is a promising candidate for the treatment of infectious diseases. However, its use is currently limited because evidence of its antiviral efficacy remains inconclusive. AIM OF THE STUDY: We compared the anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) effects of E. przewalskii and E. sinica extracts in vitro. Additionally, we examined the differences in their antiviral effects against different SARS-CoV-2 strains. MATERIALS AND METHODS: VeroE6/TMPRSS2 cells were infected with SARS-CoV-2 (Conventional, Delta, and Omicron strains-BA.1, BA.2, BA.4, and BA.5), and lysates prepared from each herbal extract were added. The infectious titer was determined using the 50% tissue culture infectious dose (TCID50) method; in turn, the half-maximal inhibitory concentration (IC50) was calculated for each extract to compare the antiviral efficacy of E. sinica and E. przewalskii extracts. Further, the extracts were compared with remdesivir for their antiviral efficacy against the conventional viral strain. To verify the effect of the inactivation of virus particles, these extracts were added to each SARS-CoV-2 strain, and the infectious titers were determined using the TCID50 method. RESULTS: The antiviral efficacy (i.e., IC50) of the E. przewalskii extract against each SARS-CoV-2 strain was 2.7-10.8-fold greater than that of the E. sinica extract. The antiviral efficacy of the E. przewalskii extract against conventional viral strains was compared with that of remdesivir, which was 1/27.6 of remdesivir's efficacy. The E. sinica extract showed minimal inactivation of virus particles of each strain, whereas the E. przewalskii extract resulted in substantial viral inactivation. CONCLUSIONS: The E. przewalskii extract showed higher antiviral activity against SARS-CoV-2 than the E. sinica extract. Overall, our study suggests that E. przewalskii extract can be used for the treatment of viral infections, including COVID-19.
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Alcaloides , COVID-19 , Ephedra sinica , Ephedra , SARS-CoV-2 , Efedrina , Antivirais/farmacologia , Antivirais/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêuticoRESUMO
Cancer has become the second leading cause of death in the world. Integrative cancer therapy management is continuously evolving to enhance treatment outcomes. Chaga mushroom (Inonotus obliquus) is a parasitic fungus acclaimed to contain pharmaceutical and nutraceutical value in the fight against cancer. In particular, triterpenoid constituents derived from Chaga mushrooms have been recognized for their anti-cancer activity after distinguished cytotoxicity was repeatedly observed in cancer cells treated in vitro with lipophilic fractions of extract compared to aqueous ones. Studies that investigate the anti-cancer activity of Chaga mushroom triterpenoids are reviewed in this article to determine which cancer cell lines demonstrate the greatest susceptibility to them while highlighting the structure-activity relationships that are involved. Triterpenoid supplementation as an adjunct to cancer treatment may be a viable option as inotodiol and 3-ß-22 α-dihydroxylanosta-8, 25-diene-24-one have been shown to exhibit anti-cancer activity similar to that of conventional drugs. Advances in addressing bioavailability challenges are also included in this review as studies include in vivo components.
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<b>Background and Objective:</b> Safflower (<i>Carthamus tinctorius</i> Linn.) is one of the medicinal plants that contain secondary metabolites that have the potential to as anti-cancer by inducing apoptosis. This study aims to determine the content of secondary metabolite compounds and the induction activity of apoptosis from ethanol extract of safflower in the T47D breast cancer cell line. <b>Materials and Methods:</b> Safflower was extracted using 96% ethanol and assayed for phytochemical screening, cytotoxic tests by cell counting kit-8 to determine inhibitory concentration and apoptosis induction activity by flow cytometry to determine the ability of samples induce the programmed cell cancer in death. The data collected was analyzed with the PRISM GraphPad version. <b>Results:</b> The ethanol extract of safflower contains flavonoid compounds, alkaloids, saponins, tannins and terpenoids. The results of the anticancer activity test showed an IC<sub>50</sub> value of 479 µg mL<sup>1</sup> and the best percentage of apoptosis at a concentration of 200 µg mL<sup>1</sup> was 16.61% at the beginning of apoptosis and 10.52% at the end of apoptosis. <b>Conclusion:</b> The safflower can be developed as a breast anticancer agent that works through the induction of apoptosis to improve the effectiveness of breast cancer treatment.
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Carthamus tinctorius , Neoplasias , Humanos , Proliferação de Células , Etanol , Células MCF-7 , Extratos Vegetais/farmacologiaRESUMO
Background: Malaria is still one of the most severe public health problems worldwide. The development of treatment, prevention, and control of malaria is one of the substantial problems in the world. Aims: To investigate the in vitro antimalarial activity of Syzygium cumini methanol fruit fraction. Methods: Syzygium cumini L fruit powder was macerated with methanol (PA) and the extract obtained was fractionated using the liquid-liquid partition method with n-hexane, ethyl acetate, butanol, chloroform, methanol, and water solvents. In vitro antimalarial assay was conducted using the culture of Plasmodium falciparum 3D7 strain culture that had reached >5% growth and was examined for IC50 values using a 24-well microplate in duplicate. Each treatment and control well contained 1,080 µl of complete media. Well, number 1 was added with 120 µl fraction, and then the solution was diluted until it reached 0.01, 0.1, 1, 10, and 100 µg/ml the final concentration in the microtiter well. The control only contained complete media and infected erythrocytes without the addition of anti-malarial drugs. The microplate was incubated for 48 hours. After 48 hours, a thin blood smear was made fixed with methanol and stained with 20% Giemsa for 20 minutes to determine the IC50 value by plotting sample concentrations and percentage of parasitemia in Excel. Results: The IC50 values of ethyl acetate fraction, n.hexane fraction, butanol fraction, and water fraction were 1.189, 76.996, 1,769, and 15.058 µg/ml, respectively. Whereases the IC50 values of C1 fraction (mix fraction from chloroform: methanol 100:0 and 90:10) and C4 fraction (mix fraction from chloroform: methanol 20:80, 10:90, and 0:100) were 100.126 and 1.015 µg/ml, respectively. The results showed that the IC50 value of ethyl acetate, butanol, and C4 fraction were lower than 10µg/ml and were considered as good activity (strong antimalarial activity). Conclusion: The ethyl acetate, butanol and C4 subfraction from S. cumini fruit have the potential to be developed as an antimalarial agent.
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Antimaláricos , Malária , Syzygium , Animais , Antimaláricos/farmacologia , Antimaláricos/uso terapêutico , Frutas , Metanol/uso terapêutico , Clorofórmio/uso terapêutico , Extratos Vegetais/farmacologia , Malária/tratamento farmacológico , Malária/veterinária , Água , Butanóis/uso terapêuticoRESUMO
BACKGROUND: Δ9-Tetrahydrocannabinol (Δ9-THC) is a principal psychoactive extract of Cannabis sativa and has been traditionally used as palliative medicine for neuropathic pain. Cannabidiol (CBD), an extract of hemp species, has recently attracted increased attention as a cancer treatment, but Δ9-THC is also requiring explored pharmacological application. OBJECTIVE: This study evaluated the pharmacological effects of Δ9-THC in two human colorectal cancer cell lines. We investigated whether Δ9-THC treatment induces cell death in human colorectal cancer cells. METHODS: We performed an MTT assay to determine the pharmacological concentration of Δ9-THC. Annxein V and Western blot analysis confirmed that Δ9-THC induced apoptosis in colorectal cancer cells. Metabolic activity was evaluated using MitoTracker staining and ATP determination. We investigated vesicle formation by Δ9-THC treatment using GW9662, known as a PPARγ inhibitor. RESULTS: The MTT assay showed that treatment with 40 µM Δ9-THC and above inhibited the proliferation of colorectal cancer cells. Multiple intracytoplasmic vesicles were detected upon microscopic observation, and fluorescence-activated cell sorting analysis showed cell death via G1 arrest. Δ9-THC treatment increased the expression of cell death marker proteins, including p53, cleaved PARP-1, RIP1, and RIP3, suggesting that Δ9-THC induced the death of colorectal cancer cells. Δ9-THC treatment also reduced ATP production via changes in Bax and Bcl-2. Δ9-THC regulated intracytoplasmic vesicle formation by modulating the expression of PPARγ and clathrin, adding that antiproliferative activity of Δ9-THC was also affected. CONCLUSION: In conclusion, Δ9-THC regulated two functional mechanisms, intracellular vesicle formation and cell death. These findings can help to determine how cannabinoids can be used most effectively to improve the efficacy of cancer treatment.
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Cannabis , Neoplasias Colorretais , Humanos , Dronabinol/farmacologia , PPAR gama , Apoptose , Neoplasias Colorretais/tratamento farmacológico , Extratos Vegetais , Trifosfato de AdenosinaRESUMO
Breast cancer is the most prevalent form of cancer in women globally, and TNBC (triple-negative breast cancer) is its aggressive type since it lacks the usual targets. JAK2/STAT3 pathway can be an important lead in anticancer drug discovery, as restraining the downstream signalling of this pathway results in the induction of cell apoptosis. Moreover, various limitations associated with chemotherapy are the reason to find an alternative herbal-based therapy. For this study, we collected Urtica dioica and U. parviflora from different regions of Uttarakhand, followed by preparation of their leaf and stem extracts in different solvents. The GC-MS analysis of these extracts revealed a total of 175 compounds to be present in them. Further, by molecular docking approach, we studied the interaction between these compounds and JAK2, and 12 major compounds with better binding energy than the control Paclitaxel were identified. In addition, the selected hits were also reported to display better pharmacokinetic properties. Moreover, extracts from both the Urtica spp. displayed significant anticancer activity against MDA-MB-231(TNBC cell line) and exhibited lower cytotoxicity in healthy cell lines, i.e. HEK293T, indicating that these extracts were safer to use. Hence, the findings in our study can be crucial in the area of herbal-based target-specific drug development against breast cancer.
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Neoplasias de Mama Triplo Negativas , Feminino , Humanos , Neoplasias de Mama Triplo Negativas/metabolismo , Simulação de Acoplamento Molecular , Células HEK293 , Linhagem Celular Tumoral , Paclitaxel/uso terapêutico , Apoptose , Proliferação de Células , Janus Quinase 2RESUMO
Botanicals are various plant-based products like plant extracts or essential oils. Anti-fungal activities of selected essential oils were tested on the pathogen causing potato and tomato late blight (Phytophthora infestans). Tests to evaluate anti-oomycete activities of commercial essential oils and their major compounds were carried out in vitro in microplate in liquid media. Anti-oomycete activities on Phytophthora infestans strain were obtained from essential oils/major compounds: Eucalyptus citriodora/citronellal; Syzygium aromaticum (clove)/eugenol; Mentha spicata/D-Carvone, L-Carvone; Origanum compactum/carvacrol; Satureja montana (savory)/carvacrol; Melaleuca alternifolia (tea tree)/terpinen-4-ol, and Thymus vulgaris/thymol. As an active substance of mineral origin, copper sulfate was chosen as a control. All selected essential oils showed an anti-oomycete activity calculated with IC50 indicator. The essential oils of clove, savory, and thyme showed the best anti-oomycete activities similar to copper sulfate, while oregano, eucalyptus, mint, and tea tree essential oils exhibited significantly weaker activities than copper sulfate. Clove essential oil showed the best activity (IC50 = 28 mg/L), while tea tree essential oil showed the worst activity (IC50 = 476 mg/L). For major compounds, three results were obtained: they were statistically more active than their essential oils (carvacrol for oregano, D- and L-Carvone for mint) or as active as their essential oils sources (thymol for thyme, carvacrol for savory, terpinen-4-ol for tea tree) or less active than their original essential oils (eugenol for clove, citronellal for eucalyptus). Microscopical observations carried out with the seven essential oils showed that they were all responsible for a modification of the morphology of the mycelium. The results demonstrated that various essential oils show different anti-oomycete activities, sometimes related to a major compound and sometimes unrelated, indicating that other compounds must play a role in total anti-oomycete activity.
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Mentha , Óleos Voláteis , Origanum , Phytophthora infestans , Thymus (Planta) , Timol/análise , Eugenol , Sulfato de Cobre , Chá , Óleos de PlantasRESUMO
Multiple sclerosis (MS) is an autoimmune disease of the central nervous system (CNS) with no curative treatment, and the available therapies aim to modify the course of the disease. It has been demonstrated that extracts of Tagetes lucida have immunomodulatory and neuroprotective effects. This work induced motor damage and neuroinflammation in male BALB/c mice by oral administration of cuprizone (CPZ) (40 mg/kg) for five weeks. In addition, the extracts and coumarins of Tagetes lucida (25 mg/kg) were used to control these damage variables; during the experiment, animals were subject to behavioral tests, and at the end of 5 weeks, mice from each group were used to measure the integrity of biological barriers (brain, kidneys, and spleen) through the extravasation test with blue Evans dye. In another group of animals, the ELISA method measured the brain concentrations of IL-1ß, IL-4, IL-10, and TNF-α. The results presented here allow us to conclude that the extracts and coumarins IC, HN, PE, DF, and SC of Tagetes lucida exert a neuroprotective effect by controlling the motor damage and neuroinflammation by increasing the expression of IL-4 and IL-10 and decreasing IL-1ß and TNF-α; notably, these treatments also protect organs from vascular permeability increase, mainly the BBB, in mice with CPZ-induced experimental encephalomyelitis (VEH * p < 0.05). However, more studies must be carried out to elucidate the molecular mechanisms of the pharmacological effects of this Mexican medicinal plant.
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Non-targeted and suspect screening analysis is gaining approval across the scientific and regulatory community to monitor the chemical status in the environment and thus environmental quality. These holistic screening analyses provides the means to perform suspect screening and go beyond to discover previously undescribed chemical pollutants in environmental samples. In a case study, we developed and optimized a high-resolution tandem mass spectrometry platform hyphenated with anion exchange chromatography to screen drinking water samples in Denmark. The optimized non-targeted screening method was able to detect anionic and polar compounds and was successfully applied to drinking water from two drinking water facilities. Following a data analysis pipeline optimization, anionic pesticide residues and other environmental contaminants were detected at confidence identification level 1 such as dimethachlor ESA, mecoprop, and dichlorprop in drinking water. In addition to these three substances, it was possible to detect another 1662 compounds, of which 97 were annotated at confidence identification level 2. More research is urgently needed to health risk prioritize the detected substances and to determine their concentrations.
Assuntos
Água Potável , Poluentes Químicos da Água , Espectrometria de Massas em Tandem , Água Potável/análise , Xenobióticos , Poluentes Químicos da Água/análise , Cromatografia por Troca Iônica , DinamarcaRESUMO
Delayed release of vaccine coupled with a soluble vaccine acts as a primer and a booster with only a single administration, which would be very beneficial to livestock producers. We developed a subdermal pellet consisting of solid-phase pure stearic acid (SA) or palmitic acid (PA) that was used to encapsulate a small volume liquid vaccine consisting of fluorescently labeled *Ovalbumin (Cy5-*OVA) formulated with Emulsigen-D +/- Poly I:C (EMP) adjuvants. Mice were also immunized via the subcutaneous route with Cy5-*OVA-EMP (soluble liquid). The vaccine leached out of the pellet with very little dissolution of the fat itself resulting in the sustained subdermal delivery of antigens and adjuvants. Cy5-*OVA was still visible 60 days post administration in mice immunized with stearic acid-coated or palmitic acid-coated pellets. In these mice, persistently high IgG1 and IgG2a antibody titres were detected as well as significant IFNγ production at least 60 days post-injection. These responses were significantly higher than those observed after a single subcutaneous injection of the vaccine. A repeat trial with the pellets alone +/- the soluble vaccine showed comparable immune responses after surgical implantation of the pellet, suggesting that pellet alone may be sufficient. The PA-coated vaccines led to dermal inflammation in the mice that would limit usefulness of this vehicle, but this was largely absent when SA was used to coat the pellets. These data suggest that the SA-coated adjuvanted vaccine prolonged the release of the vaccine and triggered a comparable immune response to the mice that received the two liquid injections, and a single pellet vaccine should be tested as a novel immunization method for livestock.
Assuntos
Vacina Antivariólica , Animais , Camundongos , Ácido Palmítico , Adjuvantes Imunológicos , Imunoglobulina G , Imunidade Celular , Vacinas de Subunidades Antigênicas , Ovalbumina , Camundongos Endogâmicos BALB CRESUMO
In this work, the authors demonstrate a novel vertically-stacked thin film transistor (TFT) architecture for heterogeneously complementary inverter applications, composed of p-channel polycrystalline silicon (poly-Si) and n-channel amorphous indium tungsten oxide (a-IWO), with a low footprint than planar structure. The a-IWO TFT with channel thickness of approximately 3-4 atomic layers exhibits high mobility of 24 cm2 V-1 s-1 , near ideally subthreshold swing of 63 mV dec-1 , low leakage current below 10-13 A, high on/off current ratio of larger than 109 , extremely small hysteresis of 0 mV, low contact resistance of 0.44 kΩ-µm, and high stability after encapsulating a passivation layer. The electrical characteristics of n-channel a-IWO TFT are well-matched with p-channel poly-Si TFT for superior complementary metal-oxide-semiconductor technology applications. The inverter can exhibit a high voltage gain of 152 V V-1 at low supply voltage of 1.5 V. The noise margin can be up to 80% of supply voltage and perform the symmetrical window. The pico-watt static power consumption inverter is achieved by the wide energy bandgap of a-IWO channel and atomically-thin channel. The vertically-stacked complementary field-effect transistors (CFET) with high energy-efficiency can increase the circuit density in a chip to conform the development of next-generation semiconductor technology.
RESUMO
Lophatherum gracile (L. gracile) has long been used as a functional food and herbal medicine. Previous studies have demonstrated that extracts of L. gracile attenuate inflammatory response and inhibit SARS-CoV-2 replication; however, the underlying active constituents have yet to be identified. This study investigated the bioactive components of L. gracile. Flavone C-glycosides of L. gracile were found to dominate both anti-inflammatory and antiviral effects. A simple chromatography-based method was developed to obtain flavone C-glycoside-enriched extract (FlavoLG) from L. gracile. FlavoLG and its major flavone C-glycoside isoorientin were shown to restrict respiratory bursts and the formation of neutrophil extracellular traps in activated human neutrophils. FlavoLG and isoorientin were also shown to inhibit SARS-CoV-2 pseudovirus infection by interfering with the binding of the SARS-CoV-2 spike on ACE2. These results provide scientific evidence indicating the efficacy of L. gracile as a potential supplement for treating neutrophil-associated COVID-19.
RESUMO
A pilot-scale anaerobic-anoxic/nitrifying/induced crystallization (A2N-IC) process was established for phosphorus (P) recovery and nutrient removal from municipal wastewater with a treatment capacity of 80 m3d-1. Results show that the A2N-IC process can operate stably on a pilot scale; the recovery efficiency of influent P reached 62.2%, and the total P removal efficiency of the IC section was 65.4%. The IC section had little effect on the removal of chemical oxygen demand (COD) and nitrogen (N), and the P removal efficiency was improved. Soluble non-reactive P (sNRP) was the key factor affecting P recovery efficiency. Although P recovery increases the construction and maintenance costs, the process can be profitable if a market for P recovery products is established. To improve the P recovery efficiency, attention should be paid to the effects of sNRP and dissolved organic matter (DOM) on P recovery, and P-rich sludge should be considered.