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Ionic liquids (ILs) represent an exciting and promising solution for advancing drug delivery platforms. Their unique properties, including broad chemical diversity, adaptable structures, and exceptional thermal stability, make them ideal candidates for overcoming challenges in transdermal drug delivery. Despite encountering obstacles such as side reactions, impurity effects, biocompatibility concerns, and stability issues, ILs offer substantial potential in enhancing drug solubility, navigating physiological barriers, and improving particle stability. To propel the use of IL-based drug delivery in pharmaceutical innovation, it is imperative to devise new strategies and solvents that can amplify drug effectiveness, facilitate drug delivery to cells at the molecular level, and ensure compatibility with the human body. This review introduces innovative methods to effectively address the challenges associated with transdermal drug delivery, presenting progressive approaches to significantly improve the efficacy of this drug delivery system.
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In this investigation, the chemical composition of the hydro-distilled essential oil (HD-EO), obtained from the fresh aerial parts (inflorescence heads (Inf), leaves (L), and stems (St)) of Conyza canadensis growing wild in Jordan was determined by GC/MS. Additionally, the methanolic extract obtained from the whole aerial parts of C. canadensis (CCM) was examined for its total phenolic content (TPC), total flavonoids content (TFC), DPPH radical scavenging activity, iron chelating activity and was then analyzed with LC-MS/MS for the presence of certain selected phenolic compounds and flavonoids. The GC/MS analysis of CCHD-EOs obtained from the different aerial parts revealed the presence of (2E, 8Z)-matricaria ester as the main component, amounting to 15.4% (Inf), 60.7% (L), and 31.6% (St) of the total content. Oxygenated monoterpenes were the main class of volatile compounds detected in the Inf-CCHD-EO. However, oils obtained from the leaves and stems were rich in polyacetylene derivatives. The evaluation of the CCM extract showed a richness in phenolic content (95.59 ± 0.40 mg GAE/g extract), flavonoids contents (467.0 ± 10.5 mg QE/ g extract), moderate DPPH radical scavenging power (IC50 of 23.75 ± 0.86 µg/mL) and low iron chelating activity (IC50 = 5396.07 ± 15.05 µg/mL). The LC-MS/MS profiling of the CCM extract allowed for the detection of twenty-five phenolic compounds and flavonoids. Results revealed that the CCM extract contained high concentration levels of rosmarinic acid (1441.1 mg/kg plant), in addition to caffeic acid phenethyl ester (231.8 mg/kg plant). An antimicrobial activity assessment of the CCM extract against a set of Gram-positive and Gram-negative bacteria, in addition to two other fungal species including Candida and Cryptococcus, showed significant antibacterial activity of the extract against S. aureus with MIC value of 3.125 µg/mL. The current study is the first phytochemical screening for the essential oil and methanolic extract composition of C. canadensis growing in Jordan, its antioxidant and antimicrobial activity.
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Antioxidantes , Conyza , Flavonoides , Óleos Voláteis , Compostos Fitoquímicos , Extratos Vegetais , Antioxidantes/farmacologia , Antioxidantes/química , Jordânia , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Conyza/química , Flavonoides/análise , Flavonoides/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Cromatografia Gasosa-Espectrometria de Massas , Fenóis/química , Fenóis/análise , Testes de Sensibilidade Microbiana , Folhas de Planta/química , Espectrometria de Massas em TandemRESUMO
Colorectal cancer is one of the major causes of global cancer, with chemotherapy and radiation therapy being effective but limited due to low specificity. Regorafenib, a multikinase inhibitor, provides hope to patients with metastatic colorectal cancer and was approved by the FDA in 2012. However, due to resistance issues and adverse events, its efficacy is compromised, necessitating further refinement. Meanwhile, curcumin, a compound of turmeric, exhibits anticancer effects through antioxidant and anti-inflammatory actions, induction of the apoptosis, arrest of cell cycle, inhibition of angiogenesis, and modulation of signaling pathways. Unfortunately, its clinical utility is limited by its poor bioavailability, pointing towards innovative drug delivery strategies for enhanced efficacy in colorectal cancer treatment. Hyaluronic acid (HA)-decorated liposomes (LIPO) have been developed to target colorectal cells through an overexpressed CD44 receptor, increasing antitumor and antimetastasis efficacy. This study investigates the possibility of loading curcumin (CUR) or regorafenib (REGO) into a liposomal formulation for passive and HA-actively targeted treatment, evaluating its critical quality attributes (CQA) (size, zeta potential, polydispersity index) and cytotoxic activity in the HT29 colorectal cancer cell line. The average particle size of the plain liposomes and those decorated with HA was 144.00 ± 0.78 nm and 140.77 ± 1.64 nm, respectively. In contrast, curcumin-loaded plain liposomes and HA-decorated liposomes had 140 ± 2.46 nm and 164.53 ± 15.13 nm, respectively. The prepared liposomes had a spherical shape with a narrow size distribution and an acceptable zeta potential of less than -30 mV. The encapsulation efficiency was 99.2 % ± 0.3 and 99.9 ± 0.2 % for HA-decorated and bare regorafenib loaded. The % EE was 98.9 ± 0.2 % and 97.5 ± 0.2 % for bare liposomal nanoparticles loaded with curcumin and coated with curcumin. The IC50 of free REGO, CUR, REGO-LIPO, CUR-LIPO, REGO-LIPO-HA and CUR-LIPO-HA were 20.17 ± 0.78, 64.4 ± 0.33, 224.8 ± 0.06, 49.66 ± 0.22, 73.66 ± 0.6, and 27.86 ± 0.49 µM, respectively. The MTT assay in HT29 cells showed significant cytotoxic activity of the HA-decorated liposomal formulation compared to the base uncoated formulation, indicating that hyaluronic acid-targeted liposomes loaded with regorafenib or curcumin could be a promising targeted formulation against colorectal cancer cells.
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Sitophilus oryzae is a kind of stored grain pest. This is controlled by using natural pesticides, which are more reliable, cost-effective, biodegradable, and eco-friendly than synthetic pesticides. Several plants show different insecticidal activities against various pests on their different parts (leaves, seeds, etc.). In this study, methanolic extracts of Lantana camara (leaves), Carica papaya (seeds), Ricinus communis (leaves), Calotropis gigantea (flowers), and Gliciridia sepium (leaves) were used to identify the best insecticidal activity against the rice weevil by doing mortality tests for one week with four replications under laboratory conditions. Gliciridia sepium leaves showed the highest insecticidal activity (100 ± 0) after seven days, and its extract was fractionated by using column chromatography and yielded 12 fractions. A contact bioassay of each fraction was performed, and fraction-11 showed the highest insecticidal activity against Sitophilus oryzae with a 100 % mortality after four days. Fraction-11 was analyzed by using GC-MS and FT-IR. Results revealed that the major constituent identified in fraction-11 was 4-C-methyl-myo-inositol. Therefore, 4-C-methyl-myo-inositol acts as a natural insecticide against rice weevils.
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This study was conducted to compare dissolution profiles of four Jordanian registered sildenafil (SDF) products to the originator. Dissolution samples were analyzed utilizing a validated and stability-indicating HPLC method in human plasma. Validation was performed for specificity, linearity, limit of detection, lower limit of quantification, precision, trueness and stability. SDF was extracted from plasma samples using liquid-liquid extraction. The analysis was performed utilizing isocratic elution on C18 column with 1.0 ml/min flow rate. The regression value was â¼0.999 over 3 days with drug recovery between 86.6 to 89.8%with 10 ng/ml lower limit of quantitation. This method displayed a good selectivity of SDF with improved stability under various conditions. The method was used for SDF quantification in dissolution medium. Similarity factors for local products varied according to the used mediums, but all SDF local products passed the dissolution in vitro test since all of them showed a released of >85% after 60 min at the dissolution mediums.
[Box: see text].
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Citrato de Sildenafila , Citrato de Sildenafila/sangue , Citrato de Sildenafila/química , Citrato de Sildenafila/análise , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Medicamentos Genéricos/química , Medicamentos Genéricos/análise , Solubilidade , Jordânia , Estabilidade de Medicamentos , Limite de DetecçãoRESUMO
The rise in the resistance to antibiotics is due to their inappropriate use and the use of a broad spectrum of antibiotics. This has also contributed to the development of multidrug-resistant microorganisms, and due to the unavailability of suitable new drugs for treatments, it is difficult to control. Hence, there is a need for the development of new novel, target-specific antimicrobials. Nanotechnology, involving the synthesis of nanoparticles, may be one of the best options, as it can be manipulated by using physicochemical properties to develop intelligent NPs with desired properties. NPs, because of their unique properties, can deliver drugs to specific targets and release them in a sustained fashion. The chance of developing resistance is very low. Polymeric nanoparticles are solid colloids synthesized using either natural or synthetic polymers. These polymers are used as carriers of drugs to deliver them to the targets. NPs, synthesized using poly-lactic acid (PLA) or the copolymer of lactic and glycolic acid (PLGA), are used in the delivery of controlled drug release, as they are biodegradable, biocompatible and have been approved by the USFDA. In this article, we will be reviewing the synthesis of PLGA-based nanoparticles encapsulated or loaded with antibiotics, natural products, or metal ions and their antibacterial potential in various medical applications.
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The outbreak of the COVID-19 pandemic has spread throughout the world, affecting almost all nations and territories. The current double-blind, randomized, placebo-controlled, phase II clinical trial sought to evaluate the clinical efficacy and safety of mebendazole as an adjuvant therapy for outpatients with COVID-19. The patients were recruited and divided into two groups: a Mebendazole-treated group and placebo group. The mebendazole and placebo groups were matched for age, sex, and complete blood count (CBC) with differential and liver and kidney function tests at baseline. On the third day, the C-reactive protein (CRP) levels were lower (2.03 ± 1.45 vs. 5.45 ± 3.95, p < 0.001) and the cycle threshold (CT) levels were higher (27.21 ± 3.81 vs. 24.40 ± 3.09, p = 0.046) significantly in the mebendazole group than in the placebo group on the third day. Furthermore, CRP decreased and CT dramatically increased on day three compared to the baseline day in the mebendazole group (p < 0.001 and p = 0.008, respectively). There was a significant inverse correlation between lymphocytes and CT levels in the mebendazole group (r = -0.491, p = 0.039) but not in the placebo group (r = 0.051, p = 0.888). Mebendazole therapy increased innate immunity and returned inflammation to normal levels in COVID-19 outpatients faster than it did in the placebo group in this clinical trial. Our findings add to the growing body of research on the clinical and microbiological benefits of repurposing antiparasitic therapy, specifically mebendazole, for SARS-CoV-2 infection and other viral infections.
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In this article, we present the first detailed analysis of the hydro-distilled essential oil (HDEO) of the inflorescence heads of Echinops polyceras Boiss. (Asteraceae) from the flora of Jordan, offering observations at different growth (pre-flowering, full-flowering and post-flowering) stages. Additionally, we investigated the methanolic extract obtained from the aerial parts of the plant material at the full flowering stage in order to determine its inhibitory activity in terms of COX and protein denaturation and evaluate its antimicrobial effects against S. aureus (Gram-positive) and E. coli (Gram-negative) bacteria. Performing GC/MS analysis of HDEO, obtained from the fresh inflorescence heads at the different growth stages, resulted in the identification of 192 constituents. The main class of compounds detected in these three stages comprised aliphatic hydrocarbons and their derivatives, which amounted to 50.04% (pre-flower), 40.28% (full-flower) and 41.34% (post-flower) of the total composition. The oils also contained appreciable amounts of oxygenated terpenoids, primarily sesquiterpenoids and diterpenoids. The pre-flowering stage was dominated by (2E)-hexenal (8.03%) in addition to the oxygenated diterpene (6E,10E)-pseudo phytol (7.54%). The full-flowering stage primarily contained (6E,10E)-pseudo phytol (7.84%), ß-bisabolene (7.53%, SH) and the diterpene hydrocarbon dolabradiene (5.50%). The major constituents detected in the HDEO obtained at the post-flowering stage included the oxygenated sesquiterpenoid intermedeol (5.53%), the sesquiterpene hydrocarbon (E)-caryophyllene (5.01%) and (6E,10E)-pseudo phytol (4.47%). The methanolic extract obtained from air-dried aerial parts of E. polyceras displayed more COX-2 inhibition than COX-1 inhibition at a concentration level of 200 µg/mL. The extract exhibited a capacity to inhibit protein denaturation that was comparable with respect to the activity of diclofenac sodium and displayed moderate levels of antimicrobial activity against both bacterial species. The current results demonstrate the need to perform further detailed phytochemical investigations to isolate and characterize active constituents.
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Anti-Infecciosos , Diterpenos , Óleos Voláteis , Sesquiterpenos , Óleos Voláteis/química , Tenrecidae , Jordânia , Desnaturação Proteica , Escherichia coli , Staphylococcus aureus , Diterpenos/farmacologia , Sesquiterpenos/farmacologia , Bactérias Gram-Negativas , Fitol , Anti-Infecciosos/química , Extratos Vegetais/farmacologia , Testes de Sensibilidade MicrobianaRESUMO
There has been a new approach in the development of antibacterials in order to enhance the antibacterial potential. The nanoparticles are tagged on to the surface of other metals or metal oxides and polymers to achieve nanocomposites. These have shown significant antibacterial properties when compared to nanoparticles. In this article we explore the antibacterial potentials of metal-based and metal-polymer-based nanocomposites, various techniques which are involved in the synthesis of the metal-polymer, nanocomposites, mechanisms of action, and their advantages, disadvantages, and applications.
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The use of the synthetic drugs has increased in the last few decades; however, these drugs exhibit various side effects. Scientists are therefore seeking alternatives from natural sources. Commiphora gileadensis has long been used to treat various disorders. It is commonly known as bisham or balm of Makkah. This plant contains various phytochemicals, including polyphenols and flavonoids, with biological potential. We found that steam-distilled essential oil of C. gileadensis exhibited higher antioxidant activity (IC50, 22.2 µg/mL) than ascorbic acid (IC50, 1.25 µg/mL). The major constituents (>2%) in the essential oil were ß-myrcene, nonane, verticiol, ß-phellandrene, ß-cadinene, terpinen-4-ol, ß-eudesmol, α-pinene, cis-ß-copaene and verticillol, which might be responsible for the antioxidant and antimicrobial activity against Gram-positive bacteria. The extract of C. gileadensis exhibited inhibitory activity against cyclooxygenase (IC50, 450.1 µg/mL), xanthine oxidase (251.2 µg/mL) and protein denaturation (110.5 µg/mL) compared to standard treatments, making it a viable treatment from a natural plant source. LC-MS analysis revealed the presence of phenolic compounds such as caffeic acid phenyl ester, hesperetin, hesperidin, chrysin and transient amounts of catechin, gallic acid, rutin and caffeic acid. The chemical constituents of this plant can be explored further to investigate its wide variety of therapeutic potential.
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Antioxidantes , Óleos Voláteis , Antioxidantes/química , Commiphora/química , Xantina Oxidase , Extratos Vegetais/química , Arábia Saudita , Óleos Voláteis/químicaRESUMO
In recent decades, there has been a significant amount of research into breast cancer, with some important breakthroughs in the treatment of both primary and metastatic breast cancers. It's a well-known fact that treating breast cancer is still a challenging endeavour even though physicians have a fantastic toolset of the latest treatment options at their disposal. Due to limitations of current clinical treatment options, traditional chemotherapeutic drugs, and surgical options are still required to address this condition. In recent years, there have been several developments resulting in a wide range of treatment options. This review article discusses the cellular and molecular foundation of chemotherapeutic drugs, endocrine system-based treatments, biological therapies, gene therapy, and innovative techniques for treating breast cancer.
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Neoplasias da Mama , Humanos , Feminino , Neoplasias da Mama/terapia , Neoplasias da Mama/tratamento farmacológicoRESUMO
Research on natural products mainly focuses on developing a suitable drug to treat human disease. There has been a sharp increase in the development of drugs from natural products. Most of the drugs that are available are from the terrestrial origin. Marine natural products are less explored. Oceans are considered as a vast ecosystem with a wide variety of living organisms and natural products that are unexplored. Large numbers of antitumor drugs are from natural sources such as plants, marine, and microorganisms. 80% new chemical entities that were launched over the past 60 decades were from a natural source. In this article, the anticancer potential from the natural source such as plants, fungi, microorganisms, marine, and endophytes has been reviewed. Emphasis is given on the compound from the marine, plant, and of bacterial origin. Finally, we consider the future and how we might achieve better sustainability to alleviate human cancer suffering while having fewer side effects, more efficacies, and causing less harm than the present treatments.
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Sterculia diversifolia, widely distributed in Jordan as an ornamental plant, is a synonoum for Brachychiton populneus. Phytochemical studies examining the volatile chemicals in Sterculia diversifolia leaves are limited, despite the rising demand for their numerous applications. Furthermore, it was only recently that a report described the friendly synthesis of silver nanoparticles (AgNPs) using aqueous extract derived from Brachychiton populneus leaves. Therefore, AgNPs were produced using either aqueous plant extracts (AgWPE) or ethanolic plant extracts (AgEPE), and Shimadzu GC-MS equipment was used to detect volatile compounds in the ethanolic leaf extracts. GC-MS profile of leaf ethanolic extracts of the Jordanian chemotypes of S. diversifolia revealed the existence of major components: (3ß)-Lup-20(29)-en-3-ol acetate (30.97%) and 1-octadecyne (24.88). Other compounds are squalene (7.19%), germanicol (6.23), dl-α-tocopherol (5.24), heptacosane (4.41), phytol (3.54) and pentacosane (2.89). According to published studies, these reported chemicals have numerous uses, including as animal feed, vitamin precursors, possible eco-friendly herbicides, antioxidants, and anti-inflammatory agents. Aqueous extracts of S. diversifolia leaves had total phenolic of 5.33 mg GAE/g extract and flavonoid contents of 64.88 mg QE/g extract, respectively. The results indicated the contribution of phenolic and flavonoids to this plant's anti-inflammatory and antioxidant properties. The reduction in AgNO3 to AgNPs using S. diversifolia leaf extracts was confirmed by the change in solution color from colorless to dark black. Further characterization was attempted by X-ray diffraction, Malvern zeta-sizer and scanning electron microscope. The efficacy of synthesized Ag nanoparticles using aqueous or ethanolic plant extract of S. diversifolia against the Gram-negative bacteria Escherichia coli and Gram-positive bacteria Staphylococcus aureus showed appreciable activity at 25 µg/mL concentration compared to the source plant extracts.
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Corona virus is quickly spreading around the world. The goal of viral management is to disrupt the virus's life cycle, minimize lung damage, and alleviate severe symptoms. Numerous strategies have been used, including repurposing existing antivirals or drugs used in previous viral outbreaks. One such strategy is to repurpose FDA-approved kinase inhibitors that are potential chemotherapeutic agents and have demonstrated antiviral activity against a variety of viruses, including MERS, SARS-CoV-1, and others, by inhibiting the viral life cycle and the inflammatory response associated with COVID-19. The purpose of this article is to identify licensed kinase inhibitors that have the ability to reduce the virus's life cycle, from entrance through viral propagation from cell to cell. Several of these inhibitors, including imatinib, ruxolitinib, silmitasertib, and tofacitinib (alone and in conjunction with hydroxychloroquine), are now undergoing clinical studies to determine their efficacy as a possible treatment drug. The FDA approved baricitinib (a Janus kinase inhibitor) in combination with remdesivir for the treatment of COVID-19 patients receiving hospital care in November 2020. While in vitro trials with gilteritinib, fedratinib, and osimertinib are encouraging, further research is necessary before these inhibitors may be used to treat COVID-19 patients.
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Quinolones are a type of bicyclic privileged building block with immense therapeutic potential. They are known for their crucial role in modulating numerous diseases conditions. In the present review, quinolone and its derivatives with different pharmacological properties like antibacterial, anticancer, anti-HIV, antitubercular and antimalarial activities are described on the basis of their structure activity relationship studies. Literature is mainly focused on the structural changes responsible for the significant increase in the therapeutic profile of the quinolone scaffold and its derivatives. The substitution pattern in the scaffold responsible for a substantial rise in the potency of specific activity has also been discussed, while emphasizing their potential as lead molecule for the drug discovery and development. Moreover, updates of recent research findings on this scaffold are also discussed.
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Antimaláricos , Quinolonas , Antibacterianos/farmacologia , Antimaláricos/farmacologia , Descoberta de Drogas , Estrutura Molecular , Quinolonas/química , Quinolonas/farmacologia , Relação Estrutura-AtividadeRESUMO
Protein kinases are enzymes that transfer phosphate to protein, resulting in the modification of the protein. The human genome encodes approximately 538 kinases. Kinases play a role in maintaining a number of cellular processes, including control of the cell cycle, metabolism, survival, and differentiation. Protein kinase dysregulation causes several diseases, and it has been shown that numerous kinases are deregulated in cancer. The oncogenic potential of these kinases is increased by a number of processes, including overexpression, relocation, fusion point mutations, and the disruption of upstream signaling. Understanding of the mechanism or role played by kinases has led to the development of a large number of kinase inhibitors with promising clinical benefits. In this review, we discuss FDA-approved kinase inhibitors and their mechanism, clinical benefits, and side effects, as well as the challenges of overcoming some of their side effects and future prospects for new kinase inhibitor discovery.
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The present paper reports the GC-HS-SPME analysis of volatile emission and GC-MS analysis of chemical composition of essential oil of R. coriaria fruits of eight different samples of R. coriaria L. fruits ("sumac" folk name), collected from Jordanian agricultural field and the local market. The analyses show an important variability among the Sumac samples probably due to the origin, cultivation, harvesting period, drying, and conservation of the plant material. The main class of component present in all samples was monoterpenes (43.1 to 72.9%), except for one sample which evidenced a high percentage of sesquiterpene hydrocarbons (38.5%). The oxygenated monoterpenes provided a contribution to total class of monoterpenes ranging from 10.1 to 24.3%. A few samples were rich in monoterpene hydrocarbons. Regarding the single components present in all the volatile emissions, ß-caryophyllene was the main compound in most of the analyzed samples, varying from 34.6% to 7.9%. Only two samples were characterized by α-pinene as the main constituent (42.2 and 40.8% respectively). Essential oils were collected using hydro-distillation method. Furfural was the main constituent in almost all the analyzed EOs (4.9 to 48.1%), except in one of them, where ß-caryophyllene was the most abundant one. ß-caryophyllene ranged from 1.2 to 10.6%. Oxygenated monoterpenes like carvone and carvacrol ranged from 3.2-9.1% and 1.0-7.7% respectively. Cembrene was present in good amount in EO samples EO-2 to EO-8. The antioxidant capacities of the fruit essential oils from R. coriaria were assessed using spectrophotometry to measure free radical scavenger 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and inhibition of ß-carotene bleaching (BCB). The essential oils from the fruits of the different samples of R. coriaria exhibited the MIC value ranging from 32.8 to 131.25 µg/mL against S. aureus ATCC 6538 and 131.25 to 262.5 µg/mL against E. coli ATCC 8739. The MIC values of ciprofloxacin were 0.59 and 2.34 µg/mL against S. aureus ATCC 6538 and E. coli ATCC 8739, respectively.
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Frutas/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Rhus/química , Antibacterianos/química , Antibacterianos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Monoterpenos Bicíclicos/análise , Destilação , Escherichia coli/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Jordânia , Monoterpenos/análise , Óleos Voláteis/análise , Óleos de Plantas/análise , Sesquiterpenos Policíclicos/análise , Análise de Componente Principal , Staphylococcus aureus/efeitos dos fármacosRESUMO
Propolis is a resinous natural product collected by honeybees (Apis mellifera and others) from tree exudates that has been widely used in folk medicine. The present study was carried out to investigate the fatty acid composition, chemical constituents, antioxidant, and xanthine oxidase (XO) inhibitory activity of Jordanian propolis, collected from Al-Ghour, Jordan. The hexane extract of Jordanian propolis contained different fatty acids, which are reported for the first time by using GC-FID. The HPLC was carried out to identify important chemical constituents such as fatty acids, polyphenols and α-tocopherol. The antioxidant and xanthine oxidase inhibitory activities were also monitored. The major fatty acid identified were palmitic acid (44.6%), oleic acid (18:1∆9cis, 24.6%), arachidic acid (7.4%), stearic acid (5.4%), linoleic acid (18:2∆9-12cis, 3.1%), caprylic acid (2.9%), lignoceric acid (2.6%), cis-11,14-eicosaldienoic acid (20:2∆11-14cis, 2.4%), palmitoleic acid (1.5%), cis-11-eicosenoic acid (1.2%), α-linolenic acid (18:3∆9-12-15cis, 1.1%), cis-13,16-docosadienoic acid (22:2∆13-16cis, 1.0%), along with other fatty acids. The major chemical constituents identified using gradient HPLC-PDA analysis were pinocembrin (2.82%), chrysin (1.83%), luteolin-7-O-glucoside (1.23%), caffeic acid (1.12%), caffeic acid phenethyl ester (CAPE, 0.79%), apigenin (0.54%), galangin (0.46%), and luteolin (0.30%); while the minor constituents were hesperidin, quercetin, rutin, and vanillic acid. The percentage of α-tocopherol was 2.01 µg/g of the lipid fraction of propolis. Antioxidant properties of the extracts were determined via DPPH radical scavenging. The DPPH radical scavenging activities (IC50) of different extracts ranged from 6.13 to 60.5 µg/mL compared to ascorbic acid (1.21 µg/mL). The xanthine oxidase inhibition (IC50) ranged from 75.11 to 250.74 µg/mL compared to allopurinol (0.38 µg/mL). The results indicate that the various flavonoids, phenolic compounds, α-tocopherol, and other constituents which are present in propolis are responsible for the antioxidant and xanthine oxidation inhibition activity. To evaluate the safety studies of propolis, the pesticide residues were also monitored by LC-MS-MS 4500 Q-Trap. Trace amounts of pesticide residue (ng/mL) were detected in the samples, which are far below the permissible limit as per international guidelines.
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Antioxidantes/química , Ácidos Graxos/química , Resíduos de Praguicidas/química , Própole/química , Antioxidantes/farmacologia , Ácidos Cafeicos/química , Ácidos Cafeicos/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Ácidos Graxos/isolamento & purificação , Flavonoides/química , Flavonoides/isolamento & purificação , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/isolamento & purificação , Resíduos de Praguicidas/isolamento & purificação , Fenóis/química , Fenóis/isolamento & purificação , Álcool Feniletílico/análogos & derivados , Álcool Feniletílico/química , Álcool Feniletílico/isolamento & purificação , Rutina/químicaRESUMO
BACKGROUND: Salvia eigii., Salvia hierosolymitana and Salvia viridis are native to the Mediterranean region, and are used in traditional medicine for the treatment of many ailments. In the current investigation, the methanolic extracts obtained from the air dried aerial parts of S. eigii, S. hierosolymitana and S. viridis from Jordan were screened for their total phenolics content (TPC), total flavonoids content (TFC) and their in vitro antioxidant activity. Additionally, the presence of four bioactive phenolic acids including gallic acid, caffeic acid, rosmarinic acid and salvianolic acid B and other seven flavonoids including luteolin-7-O-glucoside, apigenin, apigenin-7-O-glucoside, rutin, nariginin, hesperidin and quercetin was determined using Liquid chromatography-Electron Spray Ionization-Tandom Mass Spectrometry (LC-ESI-MS/MS). METHODS: Antioxidant activity of the obtained three extracts were examined via the DPPHâ¢, ABTS⢠+ radical scavenging methods in addition to Ferrous Ion Chelating (FIC) effect. TFC and TPC of the extracts were measured using the aluminum chloride colorimetric method and the Folin-Ciocalteau method, respectively. The presence and concentration of the selected 11 compounds was further determined through LC-ESI-MS/MS. RESULTS: The results indicated that three Salvia species had high total flavonoids content expressed in mg quercetin/g dry extract (S. heirosolymitana: 770.85 ± 5.26; S. eigii: 520.60 ± 6.24, S. viridis: 311.36 ± 4.41). S. heirosolymitana had the highest DPPH⢠activity (0.184 ± 1.22 × 10-2 mg/ml) and FIC effect (0.354 ± 0.018 mg/ml). S. heirosolymitana had slightly higher ABTS⢠+ scavenging activity than S. eigii (0.176 ± 1.16 × 10-2 mg/ml; 0.183 ± 0.031 mg/ml, respectively). All 11 compounds were detected in the extracts of the three Salvia species. Luteolin-7-O-glucoside was detected in high concentration levels in the three species (1756.73, 21651.36, and 26125.14 mg/kg dry plant; S. eigii, S. hierosolyimitana and S. viridis, respectively), yet rosmarinic acid had the highest contribution to both S. hierosolymitana (27124.93 mg/kg) and S. eigii (15783.33 mg/kg). Notably, S. hierosolymitana and S. viridis contained salvianolic acid B (896.11; 890.9 mg/kg). CONCLUSIONS: The three Salvia species exhibited good antioxidant activity, especially S. heirosolymitana due to its high TPC, TFC, and the presence of high concentration levels of romarinic acid and other phenolic acids and flavonoids. This is the first phytochemical and antioxidant evaluation of S. eigii, S. hierosolymitana and S. viridis from Jordan. Prior to this investigation, no phytochemical investigation on S. eigii was reported.
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Rhus coriaria L. (Anacardiaceae), sumac, is a common condiment, appetizer and souring agent in the Mediterranean region that has a long history in traditional medicine. R. coriaria has been prescribed for the treatment of many ailments including diarrhea, ulcer, hemorrhoids, hemorrhage, wound healing, hematemesis, and eye ailments like ophthalmia and conjunctivitis. The plant is also used as diuresis, antimicrobial, abortifacient and as a stomach tonic. Sumac is known to be rich in different classes of phytochemicals including tannins, polyphenols, flavonoids, organic acids and essential oils and continues to be a hot topic for extensive research work designed for revealing its phytochemical constituents and evaluating its bioactive properties. This review summarizes the recent phytochemical and diverse bioactivity studies on R. coriaria, especially those concerned with antitumor, antioxidant, hypoglycemic, antimicrobial, and anti-inflammatory studies.