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1.
Chem Biodivers ; 21(4): e202301946, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38433095

RESUMEN

In Turkish folk medicine, the roots of Onosma armeniacum Klokov are used to heal wounds, burns, hemorrhoids, hoarseness, dyspnea, stomach ulcers, and abdominal aches. The objective was to evaluate the plant's ethnopharmacological applications using in vivo pharmacological experimental models. In vivo linear incision and circular excision the wound models were used to assess the wound healing activity along with histopathological investigation. The active component(s) were isolated and identified after being exposed to several chromatographic separation procedures on the primary extract. The n-hexane-dichloromethane mixture extract was subjected to chromatographic separation after the wound-healing activity was confirmed. Deoxyshikonin (1), ß,ß-dimethylacrylshikonin (2), α-methyl-n-butylshikonin (3), isovalerylshikonin (4), acetylshikonin (5), ß-hydroxyisovalerylshikonin (6), and 5,8-O-dimethylacetylshikonin (7) were identified as the structures of the isolated compounds. The efficacy of O. armeniacum to heal wounds was investigated in this study. Shikonin derivatives were identified as the primary active components of the roots by bioassay-guided fractionation and isolation procedures.


Asunto(s)
Boraginaceae , Naftoquinonas , Boraginaceae/química , Extractos Vegetales/química , Cicatrización de Heridas , Raíces de Plantas/química , Naftoquinonas/química
2.
Chem Biodivers ; 20(12): e202301529, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37955210

RESUMEN

The study's objective is to clarify the probable mechanisms underlying the wound-healing properties of Helianthemum canum L. (Cistaceae), a traditional anti-inflammatory and wound-healing medicine. LC/MS-MS was used to perform phytochemical analyses on a 70 % methanol extract of the plant's aerial parts. In vivo, linear incision and circular excision models were used to evaluate the wound healing activity. For anti-inflammatory effect, in vivo acetic acid capillary permeability assay and in vitro Interleukin 1, Interleukin 6, and Interferon É£ levels in LPS-induced FR skin fibroblast cell line were also evaluated. The extract significantly improved wound healing in experimental models, with tensile strength values of 27.8 % and a contraction value of 35.09 %. Histopathological examinations, hydroxyproline estimation, hyaluronidase, collagenase, and elastase enzyme inhibitory assays confirmed wound healing potential. Inflammatory cytokines were significantly inhibited in the LPS-induced FR cell line, with the highest effect seen on IL-6 (34.5±2.12 pg/mL). This study offered the first concrete proof that H. canum can be used to treat wounds by suggesting that the myricetin and quinic acid content identified by LCMS-MS analysis may be accountable for the effect of H. canum on wound contraction and hydroxyproline production.


Asunto(s)
Cistaceae , Extractos Vegetales , Ratas , Animales , Extractos Vegetales/química , Ratas Sprague-Dawley , Hidroxiprolina/metabolismo , Lipopolisacáridos/farmacología , Cicatrización de Heridas , Fitoquímicos/farmacología , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Cistaceae/metabolismo
3.
Front Biosci (Landmark Ed) ; 28(7): 142, 2023 Jul 21.
Artículo en Inglés | MEDLINE | ID: mdl-37525912

RESUMEN

BACKGROUND: Aerial parts of Malva nicaeensis All. are preferred in the prevention and treatment of intestinal infections and hemorrhoids in Turkish traditional medicine. This study is planned to evaluate the pharmacological activity of M. nicaeensis extracts on rats with acetic acid-induced colitis. METHODS: The plant material was subsequently extracted with n-hexane, ethanol, and water, respectively. All of these extracts were tested for efficacy in the acetic acid-induced rat colitis model. The aqueous and polysaccharide extracts regulated cytokine levels and antioxidant parameters. Furthermore, the aqueous extract in particular regulated myeloperoxidase and caspase-3 levels in this rat model. In addition, the polysaccharide-rich fraction was separated from the aqueous extract. RESULTS: The polysaccharide-rich fraction and aqueous extract regulated cytokine levels and antioxidant parameters. The aqueous extract also positively affected myeloperoxidase and caspase-3 levels. The phytochemical studies revealed that the aqueous extract had the highest phenolic content. In addition, the polysaccharide fraction was found to contain total sugars, sulfated groups, uronic acids, and total proteins in 78.4%, 0.9%, 1.5%, and 14.7%, respectively, and was rich in monosaccharide-type compounds, especially galactose (36.4%). CONCLUSIONS: M. nicaeensis was discovered to be a drug lead in the future treatment of irritable bowel diseases or as a complementary therapeutic agent that aided conventional treatments.

4.
Front Biosci (Landmark Ed) ; 28(12): 353, 2023 12 27.
Artículo en Inglés | MEDLINE | ID: mdl-38179764

RESUMEN

BACKGROUND: The current research centers on exploring the antioxidant, antimicrobial, and antidiabetic features of Schinus molle L. grown in Turkey. METHODS: Quantitative analysis of chlorogenic acid, caffeic acid, and hyperoside levels in leaf, ripe fruit, and raw fruit extracts was conducted using High-Performance Liquid Chromatography (HPLC) in a 70% methanol-water mixture. Among the extracts, the methanol extract from ripe fruits displayed the highest chlorogenic acid concentration, measuring at 2.040% ± 0.172% standard deviation (SD). Moreover, analysis of their total phenolic and flavonoid contents was carried out. Antioxidant power was assessed through different chemical assays, together with their antimicrobial and anti-diabetic properties. RESULTS: The results of DPPH (2,2-Diphenyl-1-picrylhydrazyl), ABTS (2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), and reducing power assays showed that leaf and ripe fruit alcoholic extract exhibited peak performance. While the MIC ( minimum inhibitory concentration) values of the extracts were determined to have moderate bactericidal effects on Staphylococcus aureus, Escherichia coli, and Candida albicans it was observed that none of the extracts displayed biofilm inhibition. The inhibition percentage of α-glucosidase enzyme activity for the methanol extract of raw fruits was determined to be 99.11 ± 1.61. In diabetic ß-TC cells, glucose level was measured as 129 ± 2.03 mg/dL, and insulin amount was measured as 37.2 ± 0.02 mg/dL. CONCLUSIONS: The findings of our study seem to have important implications for future research, as Schinus molle L. may be a potential pharmaceutical candidate with important pharmacological activities.


Asunto(s)
Antiinfecciosos , Antioxidantes , Antioxidantes/farmacología , Antioxidantes/química , Frutas/química , Schinus , Ácido Clorogénico/análisis , Hipoglucemiantes/farmacología , Metanol , Extractos Vegetales/farmacología , Extractos Vegetales/química , Antiinfecciosos/farmacología , Fenoles/farmacología , Hojas de la Planta/química
5.
Antioxidants (Basel) ; 11(10)2022 Sep 20.
Artículo en Inglés | MEDLINE | ID: mdl-36290576

RESUMEN

Arctium minus (Hill) Bernh. (Asteraceae), which has a wide distribution area in Turkey, is a medicinally important plant. Eighty percent methanol extracts of the leaf, flower head, and root parts of A. minus were prepared and their sub-fractions were obtained. Spectrophotometric and chromatographic (high-performance liquid chromatography) techniques were used to assess the phytochemical composition. The extracts were evaluated for antioxidant activity by diphenyl-2-picrylhydrazil radical (DPPH●), 2,2'-Azino-bis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS●+) radical scavenging, and ß-carotene linoleic acid bleaching assays. Furthermore, the extracts were subjected to α-amylase, α-glucosidase, lipoxygenase, and tyrosinase enzyme inhibition tests. The cytotoxic effects of extracts were investigated on MCF-7 and MDA-MB-231 breast cancer cell lines. The richest extract in terms of phenolic compounds was identified as the ethyl acetate sub-fraction of the root extract (364.37 ± 7.18 mgGAE/gextact). Furthermore, chlorogenic acid (8.855 ± 0.175%) and rutin (8.359 ± 0.125%) were identified as the primary components in the leaves' ethyl acetate sub-fraction. According to all methods, it was observed that the extracts with the highest antioxidant activity were the flower and leaf ethyl acetate fractions. Additionally, ABTS radical scavenging activity of roots' ethyl acetate sub-fraction (2.51 ± 0.09 mmol/L Trolox) was observed to be as effective as that of flower and leaf ethyl acetate fractions at 0.5 mg/mL. In the ß-carotene linoleic acid bleaching assay, leaves' methanol extract showed the highest antioxidant capacity (1422.47 ± 76.85) at 30 min. The enzyme activity data showed that α-glucosidase enzyme inhibition of leaf dichloromethane extract was moderately high, with an 87.12 ± 8.06% inhibition value. Lipoxygenase enzyme inhibition was weakly detected in all sub-fractions. Leaf methanol extract, leaf butanol, and root ethyl acetate sub-fractions showed 99% tyrosinase enzyme inhibition. Finally, it was discovered that dichloromethane extracts of leaves, roots, and flowers had high cytotoxic effects on the MDA-MB-231 cell line, with IC50 values of 21.39 ± 2.43, 13.41 ± 2.37, and 10.80 ± 1.26 µg/mL, respectively. The evaluation of the plant extracts in terms of several bioactivity tests revealed extremely positive outcomes. The data of this study, in which all parts of the plant were investigated in detail for the first time, offer promising results for future research.

6.
Chem Biodivers ; 19(12): e202200582, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36310134

RESUMEN

Primula vulgaris Huds. leaves and roots were used to treat skin damage and inflammation in Anatolian Folk Medicine. This study aimed to assess the ethnopharmacological use of the plant using in vivo, in vitro, and in silico test models. Linear incision and circular excision wound models were used to determine the in vivo wound-healing potential of the plant extracts and fractions. In vitro assays including hyaluronidase, collagenase, and elastase inhibitory activities were carried out for the active compounds to discover their activity pathways. Structure-based molecular modeling was performed to understand inhibitory mechanisms regarding collagenase and elastase at the molecular level. The butanol fraction of the roots of P. vulgaris showed the highest wound-healing activity. Through activity-guided fractionation and isolation techniques, primulasaponin I (1) and primulasaponin I methyl ester (2) were stated as the major active compounds. These compounds exerted their activities through the inhibition of collagenase and elastase enzymes. Primulasaponin I methyl ester isolated from butanol fraction was found to be the strongest agent, especially with the values of 29.65 % on collagenase and 38.92 % on elastase inhibitory activity assays, as well as molecular docking studies. The present study supports scientific data for the traditional use of P. vulgaris and the wound healing properties of the plant can be referred to secondary metabolites as especially saponins found in the roots.


Asunto(s)
Primula , Saponinas , Elastasa Pancreática , Saponinas/farmacología , Simulación del Acoplamiento Molecular , Extractos Vegetales , Cicatrización de Heridas , Colagenasas/metabolismo
7.
Artículo en Inglés | MEDLINE | ID: mdl-35911153

RESUMEN

Rumex dentatus L. (Polygonaceae), also known as toothed dock or Aegean dock, is a medicinal plant with a high culinary value in addition to being used as an ethnomedicinal plant. This review focuses on the botanical, nutritional, phytochemical, and pharmacological activities of R. dentatus, as well as the future prospects for systematic investigations into these areas. R. dentatus has been subjected to scientific evaluation, which has confirmed its traditional uses and demonstrated a wide range of biological and pharmacological potentials, including antioxidant, anticancer, antifungal, antibacterial, anti-inflammatory, and other biological properties. Phytochemical analyses showed the presence of anthraquinones, chromones, flavonoids, and essential oils. As a result of this current review, the medicinal significance of R. dentatus has been confirmed, and future research on its unexplored aspects, such as the identification of pharmacologically active chemical constituents and related mechanisms and safety, may be stimulated, with the goal of developing it into a drug.

8.
Oxid Med Cell Longev ; 2022: 6044640, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36017236

RESUMEN

Among various cancers, breast cancer is the most prevalent type in women throughout the world. Breast cancer treatment is challenging due to complex nature of the etiology of disease. Cell division cycle alterations are often encountered in a variety of cancer types including breast cancer. Common treatments include chemotherapy, surgery, radiotherapy, and hormonal therapy; however, adverse effects and multidrug resistance lead to complications and noncompliance. Accordingly, there is an increasing demand for natural products from medicinal plants and foods. This review summarizes molecular mechanisms of signaling pathways in breast cancer and identifies mechanisms by which natural compounds may exert their efficacy in the treatment of breast cancer.


Asunto(s)
Productos Biológicos , Neoplasias de la Mama , Plantas Medicinales , Productos Biológicos/farmacología , Productos Biológicos/uso terapéutico , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/metabolismo , Neoplasias de la Mama/prevención & control , Femenino , Humanos , Transducción de Señal
9.
Artículo en Inglés | MEDLINE | ID: mdl-35656467

RESUMEN

Acute kidney injury (AKI) is a complex condition which has an intricate pathology mostly involving hemodynamic, inflammatory, and direct toxic effects at the cellular level with high morbidity and mortality ratios. Renal ischemic reperfusion injury (RIRI) is the main factor responsible for AKI, most often observed in different types of shock, kidney transplantation, sepsis, and postoperative procedures. The RIRI-induced AKI is accompanied by increased reactive oxygen species generation together with the activation of various inflammatory pathways. In this context, plant-derived medicines have shown encouraging nephroprotective properties. Evidence provided in this systemic review leads to the conclusion that plant-derived extracts and compounds exhibit nephroprotective action against renal ischemic reperfusion induced-AKI by increasing endogenous antioxidants and decreasing anti-inflammatory cytokines. However, there is no defined biomarker or target which can be used for treating AKI completely. These plant-derived extracts and compounds are only tested in selected transgenic animal models. To develop the results obtained into a therapeutic entity, one should apply them in proper vertebrate multitransgenic animal models prior to further validation in humans.

10.
J Ethnopharmacol ; 295: 115411, 2022 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-35636653

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: The genus Prunella L. (Lamiaceae) is represented by nine species in the world and four species in Turkey. The infusion prepared from the aerial parts of Prunella vulgaris L. is used internally for abdominal pain and as an expectorant, the decoction prepared from all parts is used internally or externally as a wound healing. AIM OF THE STUDY: This study aims to investigate the wound healing potential of Prunella vulgaris L. on the scientific platform. MATERIAL AND METHODS: The aerial parts of the plant were extracted with 80% methanol. The resulting aqueous methanol extract was partitioned with n-hexane and ethyl acetate, and sub-extracts were obtained. The wound healing effects of the methanol extract and sub-extracts were studied in mice and rats using linear incision and circular excision wound models, and the anti-inflammatory effect was investigated using acetic acid-induced capillary permeability test. Isolation studies were performed using the ethyl acetate sub-extract, which exhibited the highest activity. RESULTS: Using various chromatographic methods, 6 compounds were isolated from the ethyl acetate sub-extract. The structures of the compounds were identified as methyl arginolate, ursolic acid, chlorogenic acid, rosmarinic acid, methyl 3-epimaclinate, and ethyl rosmarinate by spectroscopic techniques (UV, IR, 13C-NMR, 1H-NMR, 2D-NMR, MS). The wound healing mechanisms of the pure compounds were investigated by performing assays to inhibit the enzymes hyaluronidase, collagenase, and elastase. Ursolic acid, chlorogenic acid, and rosmarinic acid were found to be responsible for the anti-inflammatory and wound healing effects. CONCLUSION: The experimental study revealed that Prunella vulgaris showed significant wound healing and anti-inflammatory activities.


Asunto(s)
Antiinflamatorios , Extractos Vegetales , Prunella , Cicatrización de Heridas , Animales , Antiinflamatorios/farmacología , Ácido Clorogénico/farmacología , Cinamatos/farmacología , Depsidos/farmacología , Metanol , Ratones , Extractos Vegetales/farmacología , Prunella/química , Ratas , Triterpenos/farmacología , Cicatrización de Heridas/efectos de los fármacos , Ácido Rosmarínico , Ácido Ursólico
11.
Oxid Med Cell Longev ; 2022: 6168199, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35069976

RESUMEN

Sleep disturbances, as well as sleep-wake rhythm disorders, are characteristic symptoms of Alzheimer's disease (AD) that may head the other clinical signs of this neurodegenerative disease. Age-related structural and physiological changes in the brain lead to changes in sleep patterns. Conditions such as AD affect the cerebral cortex, basal forebrain, locus coeruleus, and the hypothalamus, thus changing the sleep-wake cycle. Sleep disorders likewise adversely affect the course of the disease. Since the sleep quality is important for the proper functioning of the memory, impaired sleep is associated with problems in the related areas of the brain that play a key role in learning and memory functions. In addition to synthetic drugs, utilization of medicinal plants has become popular in the treatment of neurological diseases. Curcuminoids, which are in a diarylheptanoid structure, are the main components of turmeric. Amongst them, curcumin has multiple applications in treatment regimens of various diseases such as cardiovascular diseases, obesity, cancer, inflammatory diseases, and aging. Besides, curcumin has been reported to be effective in different types of neurodegenerative diseases. Scientific studies exclusively showed that curcumin leads significant improvements in the pathological process of AD. Yet, its low solubility hence low bioavailability is the main therapeutic limitation of curcumin. Although previous studies have focused different types of advanced nanoformulations of curcumin, new approaches are needed to solve the solubility problem. This review summarizes the available scientific data, as reported by the most recent studies describing the utilization of curcumin in the treatment of AD and sleep deprivation-related consequences.


Asunto(s)
Enfermedad de Alzheimer/tratamiento farmacológico , Curcumina/uso terapéutico , Anciano , Anciano de 80 o más Años , Enfermedad de Alzheimer/patología , Curcumina/farmacología , Femenino , Humanos , Masculino , Persona de Mediana Edad , Estudios Prospectivos , Privación de Sueño/tratamiento farmacológico
12.
Oxid Med Cell Longev ; 2022: 7928200, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35087619

RESUMEN

Cancer is one of the important causes of death worldwide. Despite remarkable improvements in cancer research in the past few decades, several cancer patients still cannot be cured owing to the development of drug resistance. Natural sources might have prominence as potential drug candidates. Among the several chemical classes of natural products, anthraquinones are characterized by their large structural variety, noticeable biological activity, and low toxicity. Aloe emodin, an anthraquinone derivative, is a natural compound found in the roots and rhizomes of many plants. This compound has proven its antineoplastic, anti-inflammatory, antiangiogenic, and antiproliferative potential as well as ability to prevent cancer metastasis and potential in reversing multidrug resistance of cancer cells. The anticancer property of aloe emodin, a broad-spectrum inhibitory agent of cancer cells, has been detailed in many biological pathways. In cancer cells, these molecular mechanisms consist of inhibition of cell growth and proliferation, cell cycle arrest deterioration, initiation of apoptosis, antimetastasis, and antiangiogenic effect. In accordance with the strategy of developing potential drug candidates from natural products, aloe emodin's low bioavailability has been tried to be overcome by structural modifications and nanocarrier systems. Consequently, this review summarizes the antiproliferative and anticarcinogenic properties of aloe emodin, as well as the enhanced activity of its derivatives and the advantages of drug delivery systems on bioavailability.


Asunto(s)
Antraquinonas/uso terapéutico , Sistemas de Liberación de Medicamentos/métodos , Neoplasias/tratamiento farmacológico , Antraquinonas/farmacología , Humanos
14.
Front Pharmacol ; 12: 669638, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34054540

RESUMEN

Psychiatric disorders are frequently encountered in many neurological disorders, such as Alzheimer's and Parkinson diseases along with epilepsy, migraine, essential tremors, and stroke. The most common comorbid diagnoses in neurological diseases are depression and anxiety disorders along with cognitive impairment. Whether the underlying reason is due to common neurochemical mechanisms or loss of previous functioning level, comorbidities are often overlooked. Various treatment options are available, such as pharmacological treatments, cognitive-behavioral therapy, somatic interventions, or electroconvulsive therapy. However oral antidepressant therapy may have some disadvantages, such as interaction with other medications, low tolerability due to side effects, and low efficiency. Natural compounds of plant origin are extensively researched to find a better and safer alternative treatment. Experimental studies have shown that phytochemicals such as alkaloids, terpenes, flavonoids, phenolic acids as well as lipids have significant potential in in vitro and in vivo models of psychiatric disorders. In this review, various efficacy of natural products in in vitro and in vivo studies on neuroprotective and their roles in psychiatric disorders are examined and their neuro-therapeutic potentials are shed light.

15.
Nutrients ; 13(2)2021 Jan 27.
Artículo en Inglés | MEDLINE | ID: mdl-33513791

RESUMEN

Gut microbiota composition and function are major areas of research for functional gastrointestinal disorders. There is a connection between gastrointestinal tract and central nervous system and this is mediated by neurotransmitters, inflammatory cytokines, the vagus nerve and the hypothalamic-pituitary-adrenal axis. Functional gastrointestinal disorders are prevalent diseases affecting more than one third of the population. The etiology of these disorders is not clarified. Visceral hyperalgesia is the main hypothesis for explaining clinical symptoms, however gut-brain axis disorder is a new terminology for functional disorders. In this review, microbiota-gut-brain axis connection pathways and related disorders are discussed. Antibiotics are widely used in developed countries and recent evidence indicates antibiotic-induced dysbiosis as an important factor for functional disorders. Antibiotics exert negative effects on gut microbiota composition and functions. Antibiotic-induced dysbiosis is a major factor for occurrence of post-infectious irritable bowel syndrome. Cognitive and mood disorders are also frequent in functional gastrointestinal disorders. Animal and human trials show strong evidence for the causal relationship between gut microbiota and brain functions. Therapeutic implications of these newly defined pathogenic pathways are also discussed.


Asunto(s)
Antibacterianos/efectos adversos , Enfermedades Gastrointestinales/microbiología , Microbioma Gastrointestinal/efectos de los fármacos , Animales , Sistema Nervioso Autónomo/metabolismo , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Disbiosis/etiología , Disbiosis/metabolismo , Sistema Nervioso Entérico/metabolismo , Enfermedades Gastrointestinales/etiología , Tracto Gastrointestinal/microbiología , Humanos , Sistema Hipotálamo-Hipofisario/metabolismo , Sistema Inmunológico/metabolismo , Síndrome del Colon Irritable/etiología , Síndrome del Colon Irritable/metabolismo , Neurotransmisores/metabolismo , Nervio Vago/metabolismo
16.
Semin Cancer Biol ; 69: 24-42, 2021 02.
Artículo en Inglés | MEDLINE | ID: mdl-31870939

RESUMEN

Cancer is known as one of the most common diseases that are associated with high mobility and mortality in the world. Despite several efforts, current cancer treatment modalities often are highly toxic and lack efficacy and specificity. However, the application of nanotechnology has led to the development of effective nanosized drug delivery systems which are highly selective for tumors and allow a slow release of active anticancer agents. Different Nanoparticles (NPs) such as the silicon-based nano-materials, polymers, liposomes and metal NPs have been designed to deliver anti-cancer drugs to tumor sites. Among different drug delivery systems, carbohydrate-functionalized nanomaterials, specially based on their multi-valent binding capacities and desirable bio-compatibility, have attracted considerable attention as an excellent candidate for controlled release of therapeutic agents. In addition, these carbohydrate functionalized nano-carriers are more compatible with construction of the intracellular delivery platforms like the carbohydrate-modified metal NPs, quantum dots, and magnetic nano-materials. In this review, we discuss recent research in the field of multifunctional glycol-nanoparticles (GNPs) intended for cancer drug delivery applications.


Asunto(s)
Antineoplásicos/uso terapéutico , Carbohidratos/química , Sistemas de Liberación de Medicamentos , Nanopartículas/administración & dosificación , Nanotecnología/métodos , Neoplasias/tratamiento farmacológico , Polímeros/química , Animales , Humanos , Nanopartículas/química , Puntos Cuánticos
17.
Nat Prod Res ; 35(24): 6147-6152, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33025828

RESUMEN

Roemerine is a naturally occurring aporphine alkaloid. In this study, we screened a conformer library of Food and Drug Administration (FDA)-approved drugs to identify similar drugs that can assist in identifying the biological targets of roemerine. To assess the neuroactivity in vitro, we measured the levels of cell metabolites, Brain-Derived Neurotrophic Factor (BDNF) and serotonin (5-HT) in SH-SY5Y cell line. By means of structure-based virtual screening, we identified five drugs that are similar to roemerine; mirtazapine, atomoxetine, epinastine, diphenhydramine and orphenadrine. GC-MS metabolomics study revealed that roemerine has a high impact on alanine-aspartate-glutamate pathway in cell lysate and cultured medium. Additionally, roemerine increased intercellular 5-HT level and intracellular BDNF protein expression at 10 µM. In conclusion, roemerine - a major alkaloid in antidepressant-like effect possessing plants (P. lacerum and P. syriacum) - has a neuronal activity through increasing BDNF protein expression and affecting serotonergic and glutamatergic systems in SH-SY5Y cell line.


Asunto(s)
Alcaloides , Aporfinas , Alcaloides/farmacología , Aporfinas/farmacología , Factor Neurotrófico Derivado del Encéfalo , Línea Celular Tumoral , Humanos , Extractos Vegetales , Serotonina
18.
Biomed Pharmacother ; 132: 110874, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33080467

RESUMEN

Multiple sclerosis (MS) is an autoimmune disease of the central nervous system (CNS) that leads to progressive neurological disability due to axonal deterioration. Although MS presents profound heterogeneity in the clinical course, its underlying central mechanism is active demyelination and neurodegeneration associated with inflammation. Multiple autoimmune and neuroinflammatory pathways are involved in the demyelination process of MS. Analysis of MS lesions has shown that inflammatory genes are upregulated. Glycogen synthase kinase-3 (GSK-3) is part of the mitogen-activated protein kinase (MAPK) family and has important roles in many signaling cascades. GSK-3 is a highly conserved serine/threonine protein kinase expressed in both the central and the peripheral nervous systems. GSK-3 modulates several biological processes through phosphorylation of protein kinases, including cell signaling, neuronal growth, apoptosis and production of pro-inflammatory cytokines and interleukins, allowing adaptive changes in events such as cellular proliferation, migration, inflammation, and immunity. GSK-3 occurs in mammals in two isoforms GSK-3α and GSK-3ß, both of which are common in the brain, although GSK-3α is found particularly in the cerebral cortex, cerebellum, striated hippocampus and Purkinje cells, while GSK-3ß is found in all brain regions. In patients with chronic progressive MS, expression of GSK-3ß is elevated in several brain regions such as the corpus callosum and cerebral cortex. GSK-3ß inhibition may play a role in glial cell activation, reducing pathological pain induced by nerve injury by formalin injection. According to the role of GSK-3ß in pathological conditions, the aim of this article is review of the role of GSK-3ß in multiple sclerosis and inflammation of neurons.


Asunto(s)
Encéfalo/enzimología , Glucógeno Sintasa Quinasa 3 beta/metabolismo , Esclerosis Múltiple/enzimología , Vía de Señalización Wnt , Animales , Antiinflamatorios/uso terapéutico , Encéfalo/efectos de los fármacos , Encéfalo/inmunología , Encéfalo/fisiopatología , Glucógeno Sintasa Quinasa 3 beta/antagonistas & inhibidores , Humanos , Mediadores de Inflamación/metabolismo , Terapia Molecular Dirigida , Esclerosis Múltiple/tratamiento farmacológico , Esclerosis Múltiple/inmunología , Esclerosis Múltiple/fisiopatología , Inhibidores de Proteínas Quinasas/uso terapéutico , Regulación hacia Arriba , Vía de Señalización Wnt/efectos de los fármacos
19.
Int J Mol Sci ; 21(16)2020 Aug 06.
Artículo en Inglés | MEDLINE | ID: mdl-32781533

RESUMEN

Cancer is one of the most extreme medical conditions in both developing and developed countries around the world, causing millions of deaths each year. Chemotherapy and/or radiotherapy are key for treatment approaches, but both have numerous adverse health effects. Furthermore, the resistance of cancerous cells to anticancer medication leads to treatment failure. The rising burden of cancer overall requires novel efficacious treatment modalities. Natural medications offer feasible alternative options against malignancy in contrast to western medication. Furanocoumarins' defensive and restorative impacts have been observed in leukemia, glioma, breast, lung, renal, liver, colon, cervical, ovarian, and prostate malignancies. Experimental findings have shown that furanocoumarins activate multiple signaling pathways, leading to apoptosis, autophagy, antioxidant, antimetastatic, and cell cycle arrest in malignant cells. Additionally, furanocoumarins have been shown to have chemo preventive and chemotherapeutic synergistic potential when used in combination with other anticancer drugs. Here, we address different pathways which are activated by furanocoumarins and their therapeutic efficacy in various tumors. Ideally, this review will trigger interest in furanocoumarins and their potential efficacy and safety as a cancer lessening agents.


Asunto(s)
Antineoplásicos/uso terapéutico , Furocumarinas/uso terapéutico , Animales , Antineoplásicos/química , Antineoplásicos/farmacología , Autofagia/efectos de los fármacos , Disponibilidad Biológica , Puntos de Control del Ciclo Celular/efectos de los fármacos , Furocumarinas/química , Furocumarinas/farmacología , Humanos , Neoplasias/tratamiento farmacológico , Neoplasias/patología
20.
Mar Drugs ; 18(8)2020 Aug 13.
Artículo en Inglés | MEDLINE | ID: mdl-32823595

RESUMEN

Carotenoids are natural fat-soluble pigments synthesized by plants, algae, fungi and microorganisms. They are responsible for the coloration of different photosynthetic organisms. Although they play a role in photosynthesis, they are also present in non-photosynthetic plant tissues, fungi, and bacteria. These metabolites have mainly been used in food, cosmetics, and the pharmaceutical industry. In addition to their utilization as pigmentation, they have significant therapeutically applications, such as improving immune system and preventing neurodegenerative diseases. Primarily, they have attracted attention due to their antioxidant activity. Several statistical investigations indicated an association between the use of carotenoids in diets and a decreased incidence of cancer types, suggesting the antioxidant properties of these compounds as an important factor in the scope of the studies against oxidative stress. Unusual marine environments are associated with a great chemical diversity, resulting in novel bioactive molecules. Thus, marine organisms may represent an important source of novel biologically active substances for the development of therapeutics. Marine carotenoids (astaxanthin, fucoxanthin, ß-carotene, lutein but also the rare siphonaxanthin, sioxanthin, and myxol) have recently shown antioxidant properties in reducing oxidative stress markers. Numerous of bioactive compounds such as marine carotenoids have low stability, are poorly absorbed, and own very limited bioavailability. The new technique is nanoencapsulation, which can be used to preserve marine carotenoids and their original properties during processing, storage, improve their physiochemical properties and increase their health-promoting effects. This review aims to describe the role of marine carotenoids, their potential applications and different types of advanced nanoformulations preventing and treating oxidative stress related disorders.


Asunto(s)
Antioxidantes/farmacología , Organismos Acuáticos/química , Carotenoides/farmacología , Nanopartículas , Estrés Oxidativo/efectos de los fármacos , Animales , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacocinética , Disponibilidad Biológica , Carotenoides/química , Carotenoides/aislamiento & purificación , Carotenoides/farmacocinética , Composición de Medicamentos , Agua Dulce , Humanos , Estructura Molecular , Nanotecnología , Agua de Mar , Relación Estructura-Actividad
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