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1.
Biomed Chromatogr ; 38(7): e5869, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38599336

RESUMO

The increasing demand for honey purification and authentication necessitates the global utilization of advanced processing tools. Common honey processing techniques, such as chromatography, are commonly used to assess the quality and quantity of valuable honey. In this study, 15 honey samples were authenticated using HPLC and GC-MS chromatographic methods to analyze their pollen spectrum. Various monofloral honey samples were collected, including Acacia, Hypoestes, Lavandula, Tamarix, Trifolium, and Ziziphus species, based on accurate identification by apiarists in 2023 from the Kingdom of Saudi Arabia. Honey analysis revealed the extraction of pollen from 20 different honeybee floral species. Pollen identified from honey samples using advanced chromatographic tools revealed dominant vegetation resources: Ziziphus species (23%), Acacia species (25%), Tamarix species (34%), Lavandula species (26%), Hypoestes species (34%), and Trifolium species (31%). This study uses HPLC to extract phenolic compounds, revealing dominant protocatechuic acid (4.71 mg g-1), and GC-MS to analyze organic compounds in honey pollen. Specifically, 2-dodecanone was detected with a retention time of 7.34 min. The utilization of chromatographic tools in assessing honey samples for pollen identification provides a reliable and efficient method for determining their botanical origins, thereby contributing to the quality control and authentication of honey products.


Assuntos
Cromatografia Gasosa-Espectrometria de Massas , Mel , Pólen , Pólen/química , Mel/análise , Cromatografia Líquida de Alta Pressão/métodos , Arábia Saudita , Cromatografia Gasosa-Espectrometria de Massas/métodos , Abelhas , Animais , Fenóis/análise
2.
Chem Biodivers ; : e202402136, 2024 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-39352081

RESUMO

Despite several studies on the Satureja L. genus, the chemical composition and biological activities of the traditional medicinal plant Satureja thymbrifolia (White Thyme), a Palestinian endemic species, are still unknown. It grows in arid regions and is used by Bedouins as a traditional medicinal herb. This study aimed to investigate S. thymbrifolia essential oils (EOs), mainly from its phytochemical pattern and biological properties. The GC-MS study identified p-cymene (48.53%) and thymol (23.27%) as the leading EOs components. Compared to Trolox, the EOs showed potential anti-DPPH free radical activity and had broad-spectrum antimicrobial potentials, with MIC values ranging from 0.13 ± 0.05 to 25 ± 0.00 µL/mL. They were most effective against Candida albicans species. The S. thymbrifolia EOs most effectively eliminated cancer cells when tested against CaCo-2 and HeLa cell lines (IC50 values of 192.15 ± 2.47 and 194.80 ± 1.87 µg/mL, respectively). The present investigation is the first documented study of S. thymbrifolia EOs' phytochemical composition and bioactivities. The results revealed that S. thymbrifolia EOs have potential antioxidant, antimicrobial, and cytotoxic effects. These outcomes emphasized S. thymbrifolia EO's potential dietary, pharmacological, and cosmetic applications.

3.
Molecules ; 28(19)2023 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-37836713

RESUMO

Cymbopogon flexuosus is a highly valued botanical species with significant applications in the food and food supplement industries, medicine, and cosmetics. The effects of four extraction techniques, supercritical CO2, microwave-ultrasonic, steam distillation, and hydrodistillation techniques, on the yield, phytochemical constituents, and antifungal activity against nine fungal species of Cymbopogon flexuosus aromatic oil (AO) were explored in this investigation. Gas chromatography connected with a mass spectrometry apparatus was employed for the qualitative and quantitative analyses of the investigated plant AOs. In addition, using the broth microdilution method, minimum inhibitory concentrations (MICs) were calculated for several fungi species. The supercritical CO2 method gave the highest yield of AO (11.62 ± 0.03 (w/w)) followed by the microwave-ultrasonic method (1.55 ± 0.05% (w/w)) and the steam distillation method (1.24 ± 0.04% (w/w)), while the hydrodistillation methods gave the lowest yield (1.17 ± 0.01 (w/w)). In addition, eighteen molecules were specified in the AOs obtained with the supercritical CO2, microwave-ultrasonic, steam distillation, and hydrodistillation techniques, which constituted 99.36, 98.6, 98.21, and 98.31% (v/v) of the total oils, respectively. Additionally, linalyl acetate was the trending molecule in the microwave-ultrasonic and steam distillation methods, representing 24.61 and 24.34% (v/v), respectively, while geranial was the dominant molecule in the AOs extracted with the hydrodistillation and supercritical CO2 extraction techniques (27.01 and 25.6% (v/v), respectively). The antifungal screening results revealed that the tested C. flexuosus AOs have potential antifungal effects against all the screened fungi species. The antifungal effect of the AOs extracted with the steam distillation and microwave-ultrasonic methods was remarkable compared with that of the commercial antifungal drug Fluconazole. However, the AOs extracted with these two methods have a more potent antifungal effect against Candida parapsilosis than that of Fluconazole with MICs of 3.13 ± 0.01, 3.13 ± 0.01, and 6.25 ± 0.91 µg/mL, respectively. The same effects were also observed against Trichophyton rubrum with MICs of 6.25 ± 0.91 µg/mL, respectively. The results of this investigation demonstrated that the steam distillation and microwave-ultrasonic methods are promising processes for the extraction of C. flexuosus AO with a potent antifungal effect. This may be an advantage for the utilization of C. flexuosus AO over some antifungal synthetic agents commonly utilized as medicines, preservatives, food additives, cosmetics, and nutrient supplements.


Assuntos
Cymbopogon , Óleos Voláteis , Óleos Voláteis/química , Destilação/métodos , Antifúngicos/farmacologia , Antifúngicos/análise , Vapor , Dióxido de Carbono , Micro-Ondas , Fluconazol , Ultrassom , Cromatografia Gasosa-Espectrometria de Massas
4.
Microb Pathog ; 172: 105805, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36179974

RESUMO

Phyto-natural products are deeply associated with ethno-medicinal practices with less or more scientific validation for curing many vital diseases. Thus, the present study was carried out to asses chemical constituents and bioactivities of Grantia aucheri Boiss at different growth stages (vegetative, flowering, and seeding). For this aim, the chemical composition of G. aucheri ethanolic extracts was analyzed by gas chromatography with mass spectrometry detection (GC-MS), their total phenolics, total flavonoids, total tannins, and total anthocyanins concentrations were also spectrophotometrically determined. Antifungal and antibacterial activities were determined against three pathogenic fungi and six human pathogenic bacteria. Furthermore, antioxidant activity (DPPH and ABTS scavenging) and anti-inflammatory activity (Human Red Blood Cell Stabilization Method) were evaluated. The highest content of total phenolics, total flavonoids, total tannins, and total anthocyanins were established in the extract of G. aucheri at its flowering stage. Such phyto-compounds as boranyl acetate, ß-himachalene and himachalol were major compounds found among 34 chemical constituents identified. The best antioxidant, anti-inflammatory, antifungal, and antibacterial activities were also found for this extract. Its phytochemicals presented bactericidal activities, mainly against Staphylococcus aureus, Bacillus subtilis, and Streptococcus pyogenes along with moderate fungicidal activity, however, it was less effective than the first one. Apart from antioxidant, antimicrobial, and anti-inflammatory activities, chemical constituents of G. aucheri may be potential alternative biomedical applications to reduce synthetic chemicals drugs.


Assuntos
Anti-Infecciosos , Antioxidantes , Humanos , Antioxidantes/farmacologia , Antioxidantes/química , Antifúngicos/farmacologia , Antocianinas , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Compostos Fitoquímicos/química , Antibacterianos/farmacologia , Antibacterianos/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Anti-Inflamatórios/farmacologia , Fenóis/farmacologia , Fenóis/análise , Taninos/farmacologia , Flavonoides/farmacologia , Flavonoides/análise
5.
Drug Chem Toxicol ; 45(5): 2292-2300, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34121557

RESUMO

Water pipe smoking is highly prevalent in developing countries, especially in Eastern Mediterranean regions. Research finds that more than 100 million people smoke a water pipe. Furthermore, tobacco smoking is one of the leading behavioral factors related to an increased risk of cancer, a leading cause of death globally. We aim to introduce a novel filtration system for water-pipe smoking and evaluate cytotoxic effects of common water pipe condensed smoke in comparison with our novel filtration system on normal (HEK293t) and cancer cell lines (Hep3B and MCF7) by MTS assay, alpha-fetoprotein (aFP), and apoptosis/necrosis effects. More so, the smoke substituents' neurotoxicity effect was evaluated by analyzing the depressive property on AMPA receptors (AMPARs). Our results showed that the silica filtration system was more effective than the water filtration system. The number of toxic compounds was reduced from 145 mg in distilled water extract (DWE) to 57.5 mg in silica solution extract (SSE). The SSE method also showed lower toxicity impacts on normal and cancerous cell lines (HEK293t, Hep3B, and MCF7) with CC50 values 149.9, 10.14, and 8.9 µg/ml, relative to the DWE method (CC50 values 77.1, 3.1, and 5.24 µg/ml, respectively). SSE extraction also reduced the α-FP (tumor marker test) to 2273.3 ng/ml which was closer in value to untreated cells (4066.7 ng/ml) in comparison with DWE which reduced it greatly to 1658.7 ng/ml, and the biophysical properties of AMPAR subunits demonstrate a reduced effect on desensitization rates of GluA2 homomer and GluA1/2 heteromer, using SSE relative to DWE. In conclusion, the condensed smoke of ordinary water pipe (DWE) has cytotoxic and neurotoxic impacts on various cell lines, while our newly developed system (SSE) was less toxic.


Assuntos
Neoplasias , Fumar Cachimbo de Água , Células HEK293 , Humanos , Receptores de AMPA , Dióxido de Silício/toxicidade
6.
Chem Biodivers ; 19(4): e202100872, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35167185

RESUMO

Essential oils (EOs) of Salvia fruticosa Mill. gathered from three Palestinian localities were studied to determine their constituents, antibacterial adhesion impact against Klebsiella pneumonia, cytotoxicity, and their function in cancer cell migration. Gas chromatography-mass spectrometry identified the chemical components, while the MTT technique was used to measure the EOs' cytotoxicity against HeLa (cervical) and Caco-2 (colorectal) cancer cells. Antibacterial adhesion was assessed by examining Klebsiella pneumoniae's ability to adhere to Caco-2 cells. Our study found that eucalyptol was present as the main constituent in all S. fruticosa EOs. In addition, K. pneumoniae adhesion and metastasis were reduced after 48 h of application. Salfit's and Hebron's EOs had the most potent cytotoxic effects on Caco-2 and HeLa, with IC50 values in the range of 0.7-1.3 µg/mL. Taking into account the obtained results, it may be concluded that S. fruticosa EOs can serve as potential disinfectant agents for the treatment and prevention of K. pneumoniae-associated illness and cancer.


Assuntos
Antineoplásicos , Óleos Voláteis , Salvia , Antibacterianos/química , Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Árabes , Células CACO-2 , Humanos , Klebsiella pneumoniae , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Salvia/química
7.
Molecules ; 27(14)2022 Jul 18.
Artigo em Inglês | MEDLINE | ID: mdl-35889448

RESUMO

Hypericum lanuginosum is one of the traditional medicinal plants that grows in the arid area of the Al-Naqab desert in Palestine and is used by Bedouins to heal various communicable and non-communicable illnesses. The purpose of this investigation was to estimate the total phenolic, flavonoid, and tannin contents of aqueous, methanol, acetone, and hexane H. lanuginosum extracts and evaluate their cytotoxic, anti-oxidative, and antimicrobial properties. Qualitative phytochemical tests were used to identify the major phytochemical classes in H. lanuginosum extracts, while total phenol, flavonoid, and tannin contents were determined using Folin-Ciocalteu, aluminum chloride, and vanillin assays, respectively. Moreover, a microdilution test was employed to estimate the antimicrobial activity of H. lanuginosum extracts against several microbial species. At the same time, the cytotoxic and free radical scavenging effects were evaluated using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) and 2, 2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) assays, respectively. Quantitative examinations showed that the highest amounts of phenols, flavonoids, and tannins were noticed in the H. lanuginosum aqueous extract. Moreover, H. lanuginosum aqueous extract showed potent activity against methicillin-resistant Staphylococcus aureus even more than Amoxicillin and Ofloxacin antibiotics, with Minimum Inhibitory Concentrations (MICs) of 0.78 ± 0.01, 0, and 1.56 ± 0.03 µg/mL, respectively. Additionally, the aqueous extract exhibited the highest activity against Candida albicans and Epidermatophyton floccosum pathogens, with MIC values of 0.78 ± 0.01 µg/mL. Actually, the aqueous extract showed more potent antimold activity than Ketoconazole against E. floccosum with MICs of 0.78 ± 0.01 and 1.56 ± 0.02 µg/mL, respectively. Furthermore, all H. lanuginosum extracts showed potential cytotoxic effects against breast cancer (MCF-7), hepatocellular carcinoma (Hep 3B and Hep G2), and cervical adenocarcinoma (HeLa) tumor cell lines. In addition, the highest free radical scavenging activity was demonstrated by H. lanuginosum aqueous extract compared with Trolox with IC50 doses of 6.16 ± 0.75 and 2.23 ± 0.57 µg/mL, respectively. Studying H. lanuginosum aqueous extract could lead to the development of new treatments for diseases such as antibiotic-resistant microbes and cancer, as well as for oxidative stress-related disorders such as oxidative stress. H. lanuginosum aqueous extract may help in the design of novel natural preservatives and therapeutic agents.


Assuntos
Anti-Infecciosos , Hypericum , Staphylococcus aureus Resistente à Meticilina , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Árabes , Flavonoides , Radicais Livres , Humanos , Fenóis/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Taninos
8.
Molecules ; 27(3)2022 Feb 03.
Artigo em Inglês | MEDLINE | ID: mdl-35164311

RESUMO

Since ancient times, Mandragora autumnalis has been used as a traditional medicinal plant for the treatment of numerous ailments. In light of this, the current study was designed to isolate and identify the chemical constituents of the flavonoids fraction from M. autumnalis ripe fruit (FFM), and evaluate its DPPH scavenging, anti-lipase, cytotoxicity, antimicrobial and antidiabetic effects. An ethyl acetate extract of M. autumnalis was subjected to a sequence of silica gel column chromatography using different eluents with various polarities. The chemical structures of the isolated compounds were identified using different spectral techniques, including 1H NMR and 13C NMR. FFM's anti-diabetic activity was assessed using a glucose transporter-4 (GLUT4) translocation assay, as well as an inhibition against α-amylase and α-glucosidase using standard biochemical assays. The FFM anti-lipase effect against porcine pancreatic lipase was also evaluated. Moreover, FFM free radical scavenging activity using the DPPH test and antimicrobial properties against eight microbial strains using the micro-dilution method were also assessed. Four flavonoid aglycones were separated from FFM and their chemical structures were identified. The structures of the isolated compounds were established as kaempferol 1, luteolin 2, myricetin 3 and (+)-taxifolin 4, based on NMR spectroscopic analyses. The cytotoxicity test results showed high cell viability (at least 90%) for up to 1 mg/mL concentration of FFM, which is considered to be safe. A dose-dependent increase in GLUT4 translocation was significantly shown (p < 0.05) when the muscle cells were treated with FFM up to 0.5 mg/mL. Moreover, FFM revealed potent α-amylase, α-glucosidase, DPPH scavenging and porcine pancreatic lipase inhibitory activities compared with the positive controls, with IC50 values of 72.44 ± 0.89, 39.81 ± 0.74, 5.37 ± 0.41 and 39.81 ± 1.23 µg/mL, respectively. In addition, FFM inhibited the growth of all of the tested bacterial and fungal strains and showed the greatest antibacterial activity against the K. pneumoniae strain with a MIC value of 0.135 µg/mL. The four flavonoid molecules that constitute the FFM have been shown to have medicinal promise. Further in vivo testing and formulation design are needed to corroborate these findings, which are integral to the pharmaceutical and food supplement industries.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Inibidores Enzimáticos/química , Flavonoides/química , Hipoglicemiantes/química , Mandragora/química , Animais , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Linhagem Celular , Inibidores Enzimáticos/farmacologia , Flavonoides/farmacologia , Frutas/química , Humanos , Hipoglicemiantes/farmacologia , Lipase/antagonistas & inibidores , Suínos
9.
Molecules ; 27(24)2022 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-36558005

RESUMO

Herbal treatment for diabetes mellitus is widely used. The pharmacological activity is thought to be due to the phenolic compounds found in the plant leaves. The present study aims to investigate the phytochemical composition of Urtica dioica (UD) hydroethanolic extract and to screen its antidiabetic activity by disaccharidase hindering and glucose transport in Caco-2 cells. The results have shown that a total of 13 phenolic compounds in this work, viz. caffeic and coumaric acid esters (1, 2, 4-7, 10), ferulic derivative (3), and flavonoid glycosides (8, 9, 11-13), were identified using HPLC-DAD-ESI/MS2. The most abundant phenolic compounds were 8 (rutin) followed by 6 (caffeoylquinic acid III). Less predominant compounds were 4 (caffeoylquinic acid II) and 11 (kaempferol-O-rutinoside). The UD hydroethanolic extract showed 56%, 45%, and 28% (1.0 mg/mL) inhibition level for maltase, sucrase, and lactase, respectively. On the other hand, glucose transport was 1.48 times less at 1.0 mg/mL UD extract compared with the control containing no UD extract. The results confirmed that U. dioica is a potential antidiabetic herb having both anti-disaccharidase and glucose transport inhibitory properties, which explained the use of UD in traditional medicine.


Assuntos
Urtica dioica , Urticaceae , Humanos , Urtica dioica/química , Extratos Vegetais/química , Células CACO-2 , Dissacaridases/análise , Folhas de Planta/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Fenóis/análise , Glucose/análise
10.
Molecules ; 27(5)2022 Feb 25.
Artigo em Inglês | MEDLINE | ID: mdl-35268662

RESUMO

The aim of the present study was to investigate the changes in the content of phytochemical compounds and in vitro antioxidant, antibacterial, and anti-inflammatory activities of Teucrium polium L. aerial parts and root methanolic extracts at different phenological stages (vegetative, flowering, and seeding). The T. polium extracts were analyzed using gas chromatography−mass spectrometry (GC-MS), and their antioxidant properties were tested with the 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), ferrous ions (Fe2+), and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) methods. Forty-nine compounds were identified with the majority of germacrene D, t-cadinol, ß-pinene, carvacrol, bicyclogermacrene, α-pinene, and limonene. The results show that the extracts significantly differ between different phenological stages of the plant material used in terms of the phytochemical composition (total phenolic compounds, total flavonoids, total alkaloids, and total saponin contents) and bioactivities (antioxidant, antibacterial, and anti-inflammatory) (p < 0.05). The highest total contents of phenolics (72.4 ± 2.5 mg gallic acid equivalent (GAE)/g dry weight), flavonoids (36.2 ± 3.1 mg quercetin equivalent (QE)/g dry weight), alkaloids (105.7 ± 2.8 mg atropine equivalent (AE)/g dry weight), and saponins (653 ± 6.2 mg escin equivalent (EE)/g dry weight), as well as antioxidant, antibacterial, and anti-inflammatory activities, were measured for the extract of the aerial parts obtained at the flowering stage. The minimum inhibitory concentration (MIC) values for the extracts were varied within 9.4−300 µg/mL, while the minimum bactericidal concentration (MBC) values were varied within 18.75−600 µg/mL. In addition, they were more active on Gram-positive bacteria than Gram-negative bacteria. The data of this work confirm that the T. polium extracts have significant biological activity and hence can be used in the pharmaceutical industry, clinical applications, and medical research, as well as cosmetic and food industries.


Assuntos
Compostos Fitoquímicos
11.
Molecules ; 27(17)2022 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-36080486

RESUMO

Pelargonium graveolens leaves are widely used in traditional medicine for relieving some cardiovascular, dental, gastrointestinal, and respiratory disorders. They are also used as food and tea additives in Palestine and many other countries. Consequently, this investigation aimed to describe the chemical markers, cytotoxic, antioxidant, antimicrobial, metabolic, and cyclooxygenase (COX) enzymes inhibitory characteristics of P. graveolens essential oil (PGEO) from Palestine utilizing reference methods. There were 70 chemicals found in the GCMS analysis, and oxygenated terpenoids were the most abundant group of the total PGEO. Citronellol (24.44%), citronellyl formate (15.63%), γ-eudesmol (7.60%), and iso-menthone (7.66%) were the dominant chemical markers. The EO displayed strong antioxidant activity (IC50 = 3.88 ± 0.45 µg/mL) and weak lipase and α-amylase suppressant effects. Notably, the PGEO displayed high α-glucosidase inhibitory efficacy compared with Acarbose, with IC50 doses of 52.44 ± 0.29 and 37.15 ± 0.33 µg/mL, respectively. PGEO remarkably repressed the growth of methicillin-resistant Staphylococcus aureus (MRSA), even more than Ampicillin and Ciprofloxacin, and strongly inhibited Candida albicans compared with Fluconazole. The highest cytotoxic effect of the PGEO was noticed against MCF-7, followed by Hep3B and HeLa cancer cells, with IC50 doses of 32.71 ± 1.25, 40.71 ± 1.89, and 315.19 ± 20.5 µg/mL, respectively, compared with doxorubicin. Moreover, the screened EO demonstrated selective inhibitory activity against COX-1 (IC50 = 14.03 µg/mL). Additionally, PGEO showed a weak suppressant effect on COX-2 (IC50 = 275.97 µg/mL). The current research can be considered the most comprehensive investigation of the chemical and pharmacological characterization of the PGEO. The results obtained in this study demonstrate, without doubt, that this plant represents a rich source of bioactive substances that can be further investigated and authenticated for their medicinal potential.


Assuntos
Anti-Infecciosos , Staphylococcus aureus Resistente à Meticilina , Óleos Voláteis , Pelargonium , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Pelargonium/química
12.
Bioorg Chem ; 116: 105406, 2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34628227

RESUMO

INTRODUCTION: Investigating the binding site of six novel curcumin-based diazepine compounds as a non-competitive antagonist on ionotropic, AMPA-type glutamate receptors, including homomeric and heteromeric subunits. These receptors play a pivotal role in neurodegenerative diseases such as Alzheimer's and epilepsy due to excitotoxicity. Furthermore, it appears that AMPAR signaling plays a significant role in disease development outside the nervous system, as a potential relationship between AMPAR activation and cancer development may exist. OBJECTIVES: Study the biophysical gating effects of the curcumin-based diazepine on AMPAR variants and identify CBD binding sites on AMPARs with the hopes of discovering more potent drug candidates with less undesirable side effects. METHODS: Our current study uses patch-clamp electrophysiology technology to estimate whole-cell amplitudes changes when exposing HEK293T cells expressing AMPAR subunits to different curcumin-based diazepines. RESULTS: The non-competitive antagonist curcumin-based compounds successfully reduced AMPAR activation currents and increased the rate of desensitization and deactivation. CBD-4 and CBD-5 show the most significant impact on AMPARs, reducing the current by 7-fold. The results contrast with those obtained by the halogenated benzodiazepine-fused curcumins reported previously and lake pyrimidine and pyrazine moieties. This indicates that the N's presence in the effused rings plays a significant role in binding to receptors. CBD-4 showed the highest effect on GluA2 subunits in receptors, while CBD-5 most dramatically impacting GluA1 homomeric receptors, demonstrating that the compounds are more selective towards AMPA-type glutamate receptors. The compounds also showed significant cytotoxic activities against breast cancer cell line (MCF-7), with CBD-4 having the most significant impact. CONCLUSION: Curcumin-based compounds (i.e., CBD-4 and CBD-5) yield significant neurodegenerative drug potential, and it creates a novel structure with significant activities in reducing AMPAR excitation compared to traditional benzodiazepine analogs, yet their binding mechanisms are still not fully understood. Moreover, AMPARs appear to have a potential influence on cancer development, and the curcumin-based compounds might provide insight into the nature of this relationship.


Assuntos
Azepinas/farmacologia , Curcumina/farmacologia , Receptores de AMPA/antagonistas & inibidores , Azepinas/síntese química , Azepinas/química , Curcumina/síntese química , Curcumina/química , Relação Dose-Resposta a Droga , Células HEK293 , Humanos , Estrutura Molecular , Receptores de AMPA/metabolismo , Transdução de Sinais/efeitos dos fármacos , Relação Estrutura-Atividade
13.
Int J Mol Sci ; 22(15)2021 Jul 29.
Artigo em Inglês | MEDLINE | ID: mdl-34360915

RESUMO

Patients diagnosed with melanoma have a poor prognosis due to regional invasion and metastases. The receptor tyrosine kinase epidermal growth factor receptor (EGFR) is found in a subtype of melanoma with a poor prognosis and contributes to drug resistance. Aloysia citrodora essential oil (ALOC-EO) possesses an antitumor effect. Understanding signaling pathways that contribute to the antitumor of ALOC-EO is important to identify novel tumor types that can be targeted by ALOC-EO. Here, we investigated the effects of ALOC-EO on melanoma growth and tumor cell migration. ALOC-EO blocked melanoma growth in vitro and impaired primary tumor cell growth in vivo. Mechanistically, ALOC-EO blocked heparin-binding-epidermal growth factor (HB-EGF)-induced EGFR signaling and suppressed ERK1/2 phosphorylation. Myelosuppressive drugs upregulated HB-EGF and EGFR expression in melanoma cells. Cotreatment of myelosuppressive drugs with ALOC-EO improved the antitumor activity and inhibited the expression of matrix metalloproteinase-7 and -9 and a disintegrin and metalloproteinase domain-containing protein9. In summary, our study demonstrates that ALOC-EO blocks EGFR and ERK1/2 signaling, with preclinical efficacy as a monotherapy or in combination with myelosuppressive drugs in melanoma.


Assuntos
Antineoplásicos/farmacologia , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Receptores ErbB/metabolismo , Fator de Crescimento Semelhante a EGF de Ligação à Heparina/metabolismo , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Melanoma/metabolismo , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Neoplasias Cutâneas/metabolismo , Verbenaceae/química , Animais , Apoptose/efeitos dos fármacos , Bortezomib/farmacologia , Doxorrubicina/farmacologia , Sinergismo Farmacológico , Humanos , Melanoma/patologia , Camundongos , Fosforilação/efeitos dos fármacos , Neoplasias Cutâneas/patologia
14.
Molecules ; 26(9)2021 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-34068826

RESUMO

Artemisia jordanica (AJ) is one of the folkloric medicinal plants and grows in the arid condition used by Palestinian Bedouins in the Al-Naqab desert for the treatment of diabetes and gastrointestinal infections. The current investigation aimed, for the first time, to characterize the (AJ) essential oil (EO) components and evaluate EO's antioxidant, anti-obesity, antidiabetic, antimicrobial, anti-inflammatory, and cytotoxic activities. The gas chromatography-mass spectrometer (GC-MS) technique was utilized to characterize the chemical ingredients of (AJ) EO, while validated biochemical approaches were utilized to evaluate the antioxidant, anti-obesity and antidiabetic. The microbicidal efficacy of (AJ) EO was measured utilizing the broth microdilution assay. Besides, the cytotoxic activity was estimated utilizing the (MTS) procedure. Finally, the anti-inflammatory activity was measured utilizing a COX inhibitory screening test kit. The analytical investigation revealed the presence of 19 molecules in the (AJ) EO. Oxygenated terpenoids, including bornyl acetate (63.40%) and endo-borneol (17.75%) presented as major components of the (AJ) EO. The EO exhibited potent antioxidant activity compared with Trolox, while it showed a weak anti-lipase effect compared with orlistat. In addition, the tested EO displayed a potent α-amylase suppressing effect compared with the positive control acarbose. Notably, the (AJ) EO exhibited strong α-glucosidase inhibitory potential compared with the positive control acarbose. The EO had has a cytotoxic effect against all the screened tumor cells. In fact, (AJ) EO showed potent antimicrobial properties. Besides, the EO inhibited the enzymes COX-1 and COX-2, compared with the anti-inflammatory drug ketoprofen. The (AJ) EO has strong antioxidant, antibacterial, antifungal, anti-α-amylase, anti-α-glucosidase, and COX inhibitory effects which could be a favorite candidate for the treatment of various neurodegenerative diseases caused by harmful free radicals, microbial resistance, diabetes, and inflammations. Further in-depth investigations are urgently crucial to explore the importance of such medicinal plants in pharmaceutical production.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Artemisia/química , Inibidores Enzimáticos/farmacologia , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/análise , Folhas de Planta/química , Animais , Compostos de Bifenilo/química , Morte Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Concentração Inibidora 50 , Oriente Médio , Orlistate/farmacologia , Picratos/química , Suínos
15.
Molecules ; 27(1)2021 Dec 26.
Artigo em Inglês | MEDLINE | ID: mdl-35011355

RESUMO

Satureja nabateorum (Danin and Hedge) Bräuchler is a perennial herb in the Lamiaceae family that was discovered and classified in 1998. This green herb is restricted to the mountains overlooking the Dead Sea, specifically in Jordan's southwest, the Edom mountains, and the Tubas mountains in Palestine. Gas chromatography-mass spectrometry (GC-MS) analysis of essential oil (EO) of air-dried and fresh S. nabateorum resulted in the identification of 30 and 42 phytochemicals accounting for 99.56 and 98.64% of the EO, respectively. Thymol (46.07 ± 1.1 and 40.64 ± 1.21%) was the major compound, followed by its biosynthetic precursors γ-terpinene (21.15 ± 1.05% and 20.65 ± 1.12%), and p-cymene (15.02 ± 1.02% and 11.51 ± 0.97%), respectively. Microdilution assay was used to evaluate the antimicrobial property of EOs against Staphylococcus aureus (ATCC 25923), clinical isolate Methicillin-Resistant Staphylococcus aureus (MRSA), Enterococcus faecium (ATCC 700221) Klebsiella pneumoniae (ATCC 13883), Proteus vulgaris (ATCC 700221), Escherichia coli (ATCC 25922) and Pseudomonas aeruginosa (ATCC 27853) and Candida albicans (ATCC-90028). With a MIC of 0.135 µg/mL, the EOs has the most potent antibacterial action against K. pneumonia. Both EOs display good antifungal efficacy against C. albicans, with a MIC value of 0.75 µg/mL, which was better than that of Fluconazole's (positive control, MIC = 1.56 µg/mL). The antioxidant capacity of EOs extracted from air-dried and fresh S. nabateorum was determined using the DPPH assay, with IC50 values of 4.78 ± 0.41 and 5.37 ± 0.40 µg/mL, respectively. The tested EOs showed significant cytotoxicity against Hela, HepG2, and COLO-205 cells, with IC50 values ranging from 82 ± 0.98 to 256 ± 1.95 µg/mL. The current work shows there is a possibility to use the S. nabateorum EOs for various applications.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Óleos Voláteis/química , Compostos Fitoquímicos/química , Extratos Vegetais/química , Satureja/química , Infecções Estafilocócicas/tratamento farmacológico , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Candida albicans/efeitos dos fármacos , Monoterpenos Cicloexânicos/química , Cimenos/química , Enterococcus faecium/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Sequestradores de Radicais Livres/metabolismo , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Proteus vulgaris/efeitos dos fármacos , Timol/química
16.
J Cosmet Sci ; 72(1): 1-16, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-35349422

RESUMO

This study aimed to develop a topical emulgel formulation from olive oil and lemongrass (LG) extracts and to evaluate its in vitro and in vivo (sensorial) properties in addition to its sun protection factor (SPF) value. The primary emulsion and the gel were prepared separately, and then they were levigated together to formulate the emulgel. The produced emulgel was evaluated for its physical appearance, pH, spreadability, and stability. The SPF value of emulgel was evaluated by applying the Mansur equation. Moreover, an in vivo sensorial assessment was conducted on the emulgel through a crossover study by including 20 volunteers. The results confirm good stability for emulgel formulations because there was no significant change in the pH value, no micelle inversion, or phase separation detected. The emulgel recorded a moderate SPF value (5.5) which can be useful for daily use, especially in tanned skin subjects. Moreover, the sensorial assessment of LG and blank emulgels showed a significant change in the cooling effect, odor, and smoothness and add some kind of moisture. In fact, there was a significant difference in overall properties between the two formulations where the p-value was less than 0.05. It is concluded the emulgel formulation containing LG and olive oil could be beneficial in terms of applicability and stability and can be easily formulated in pharmaceutical facilities. Besides, it would be useful for daily use because of the overall suitable properties, especially odor, feel, and SPF value.


Assuntos
Cymbopogon , Óleos Voláteis , Química Farmacêutica/métodos , Estudos Cross-Over , Géis , Humanos
17.
Pak J Pharm Sci ; 34(4): 1421-1428, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34799317

RESUMO

Plumbago europaea L. is a plant utilized in Palestinian ethnomedicine for the treatment of various dermatological diseases. The current investigation was designed to isolate plumbagin from P. europaea leaves, roots and for the first time from the stems. Moreover, it aimed to evaluate the antimycotic activity against three human fungal pathogens causing dermatophytosis, also against an animal fungal pathogen. The qualitative analysis of plumbagin from the leaves, stems, and roots was conducted using HPLC and spectrophotometer techniques, while the structure of plumbagin was established utilizing Proton and Carbon-13 Nuclear Magnetic Resonance (NMR) and Infrared (IR) techniques. The entire plant constituents were determined by GC-MS. Moreover, the antimycotic activity against Ascosphaera apis, Microsporum canis, Trichophyton rubrum, and Trichophyton mentagrophytes was assessed utilizing the poison food technique method. The percentage of plumbagin recorded in the leaves, stems, and roots was found to be 0.51±0.001%, 0.16±0.001%, and 1.65±0.015%, respectively. The GC-MS examination declared the presence of 59 molecules in the plant extract. The plant extract and pure plumbagin exhibited complete inhibition against all tested dermatophytes at 6.0mg/mL for the extracts and 0.2mg/mL for plumbagin. P. europaea root is the best source of plumbagin and the plant extract could represent a potential drug candidate for the treatment of dermatophytosis infections. Further studies required to design suitable dosage forms from the natural P. europaea root extracts or plumbagin alone, to be utilized for the treatment of dermatological and veterinary ailments.


Assuntos
Antifúngicos/isolamento & purificação , Naftoquinonas/isolamento & purificação , Folhas de Planta/química , Raízes de Plantas/química , Caules de Planta/química , Plumbaginaceae/química , Antifúngicos/farmacologia , Arthrodermataceae/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Microsporum/efeitos dos fármacos , Estrutura Molecular , Naftoquinonas/farmacologia , Onygenales/efeitos dos fármacos , Espectrofotometria Infravermelho
18.
Molecules ; 25(9)2020 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-32403218

RESUMO

Three new tetradentate NNNS Schiff bases (L1-L3) derived from 2-(piperidin-4-yl)ethanamine were prepared in high yields. UV-Visible and FTIR spectroscopy were used to monitor the dehydration reaction between 2-(piperidin-4-yl)ethanamine and the corresponding aldehydes. Structures of the derived Schiff bases were deduced by 1H and 13C NMR, FTIR, UV-Vis, MS, EA, EDS, and TG-derived physical measurements. DFT/B3LYP theoretical calculations for optimization, TD-DFT, frequency, Molecular Electrostatic Potential (MEP), and highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) / were performed for L2. The in vitro antimicrobial activities of the three Schiff bases were evaluated against several types of bacteria by disk diffusion test using Gentamicin as the standard antibiotic. Schiff bases revealed good antioxidant activity by the DPPH method, and the IC50 values were compared to the Trolox standard. Pancreatic porcine lipase inhibition assay of the synthesized compounds revealed promising activity as compared to the Orlistat reference.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Lipase/antagonistas & inibidores , Bases de Schiff/química , Bases de Schiff/síntese química , Concentração Inibidora 50 , Klebsiella pneumoniae/efeitos dos fármacos , Ligantes , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Simulação de Acoplamento Molecular , Pâncreas/enzimologia , Piperazina/química , Pseudomonas aeruginosa/efeitos dos fármacos , Bases de Schiff/farmacologia , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Staphylococcus aureus/efeitos dos fármacos , Eletricidade Estática , Temperatura , Tiofenos/química , Difração de Raios X
19.
BMC Pediatr ; 19(1): 483, 2019 12 09.
Artigo em Inglês | MEDLINE | ID: mdl-31818270

RESUMO

BACKGROUND: Childhood obesity is rising in developed and developing countries, while childhood underweight is rising mainly in developing countries. Childhood underweight has been shown to increase a child's risk of rapid weight gain. Overweight and obese children are more likely to become obese adults, which increases the risk of type-II diabetes and cardiovascular diseases. Studies concerning obesity among Palestinian children are scarce. The prevalence of obesity among Palestinian children has increased from 3 to 6% within 5 years in comparison to the worldwide rise from 1 to 7%, within 41 years. We aim to determine the current prevalence of underweight, overweight and obesity among Palestinian school-age children and to assess the role of dietary and sociodemographic factors. METHODOLOGY: A cross sectional study was conducted in Palestine in 2017. A total of 1320 school-age children and their 2640 corresponding parents were recruited. A written questionnaire was filled out by the parents. Anthropometric indices were measured and categorized according to the Center for Disease Control and prevention (CDC). RESULTS: The mean ± SD age of the children was 9.5 ± 1.5 years and 48.8% were females. The prevalence of underweight, overweight and obesity among the children was approximately 7.3% (95% CI = 5.9-8.8%), 14.5% (95% CI = 12.7-16.6%) and 15.7% (95% CI = 13.8-17.8%) respectively. Multinomial logistic regression analysis demonstrated a significant correlation of waist circumference, age, gender and living place with the body mass indexes of the students. CONCLUSION: Our findings highlighted the accelerated increase in the prevalence of underweight, overweight and obesity (37.5%) among Palestinian children within a very short time in comparison to the globe. Therefore, Interventions aiming to prevent obesity and underweight at an early stage might be vital to avoid obesity later in life and its health-related co-morbidities, e.g. type-II diabetes and cardiovascular diseases.


Assuntos
Obesidade Infantil/epidemiologia , Magreza/epidemiologia , Criança , Estudos Transversais , Feminino , Humanos , Masculino , Oriente Médio/epidemiologia , Prevalência , Fatores de Risco
20.
BMC Complement Altern Med ; 19(1): 194, 2019 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-31366346

RESUMO

BACKGROUND: Infertility is considered one of the global public health problems and during human history, it is also considered one of the unsolved problems of the continuous human race. This study aimed to collect and document the ethnopharmacological data on herbal remedies, which traditionally used by Palestinian healers in the rural areas of the West Bank area for the treatment of infertility in males and females. METHODS: Using a semi-structured questionnaire, an ethnopharmacological survey of medicinal plants used for the treatment of infertility in the West Bank area of Palestine was investigated. This survey involved 51 traditional healers which were interviewed in rural areas from 9 Palestinian regions. RESULTS: Information about 31 plants used in the treatment of infertility in females and 24 plants used in the treatment of infertility in males were collected. This information including names of plants, parts used, mode and methods of preparation which were obtained from 51 traditional healers interviewed in rural areas of 9 regions of the West Bank/Palestine. This investigation is the first scientific work in the Middle East area which collected information about herbal remedies used by local Palestinian traditional healers for the treatments of infertility in males and females. The highest Frequency of Citation (FC) of herbal remedies used in case of infertility in females, were 98.04% for pollen grains from Ceratonia siliqua, 88.24% for Anastatica hierochuntica fruits and 84.31% for Parietaria judaica leaves, while the highest Frequency of Citation (FC) of herbal remedies used in case of infertility in males were 96.08% for Ferula hermonis roots, 88.24% for Phlomis brachyodon leaves and 86.27% for Phoenix dactylifera pollen grains. CONCLUSION: Herbal healers in the West Bank area of Palestine have a wide range of herbal remedies used in case of infertility in males and in females. Unfortunately, most of them lack scientific evidence of pharmacological or toxicological nature. Therefore, the information obtained in this study can serve as a scientific base for further investigations to determine their efficacy and safety which might contribute to better integration of Palestinian traditional medicine into the global health system in the future.


Assuntos
Infertilidade Feminina/tratamento farmacológico , Infertilidade Masculina/tratamento farmacológico , Preparações de Plantas/uso terapêutico , Adulto , Idoso , Feminino , Humanos , Masculino , Medicina Tradicional , Pessoa de Meia-Idade , Oriente Médio , Fitoterapia , Plantas Medicinais/química , População Rural/estatística & dados numéricos , Terapias Espirituais , Adulto Jovem
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