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1.
Arch Pharm (Weinheim) ; : e2300726, 2024 Mar 28.
Artículo en Inglés | MEDLINE | ID: mdl-38548681

RESUMEN

Due to its characteristic aroma and diverse therapeutic properties, lemongrass essential oil (LEO) has garnered increased attention in the pharmaceutical, food, and cosmetic industries. However, LEO's volatile nature, low chemical stability, and limited solubility in water limits its applications in the industry. Micro- and nanoencapsulation technologies emerge as a promising solution to overcome these challenges. A systematic methodology involving keyword searches in databases was employed to gather relevant literature on LEO micro- and nanoencapsulation, providing an extensive overview of techniques, processes, encapsulating materials, and possible applications. Beyond established methods, emerging techniques were explored. This review highlights the critical role of encapsulation in enhancing the thermal and chemical stability, applicability, bioavailability, and controlled release of LEO.

2.
Chem Biodivers ; 20(12): e202301243, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37983672

RESUMEN

Leonurus japonicus Houtt. is a medicinal plant popular in Brazil as "rubim", used in local folk medicine for several applications as an anti-inflammatory, antioxidant, analgesic, and antimicrobial phytomedicine. The traditional use for wound healing is related; however, few studies have evaluated the wound healing activity. Thus, this study aimed to analyse the popular indication of the hydroalcoholic and aqueous extracts of L. japonicus aerial parts in a rat wound healing model. The initial chemical characterization was performed using flavonoid quantification and complemented with mass spectroscopy/chemometrics analysis. The wound's lesion contraction and tissue regeneration (histological study stained with hematoxylin-eosin and picrosirius) were determined. Hydroalcoholic and aqueous extracts presented high flavonoid content, and mass spectrometry analysis of the extracts demonstrated the presence of compounds with a mass between 100-650, reinforcing the presence of polyphenolic constituents. The extracts of L. japonicus improve various wound healing phases, like inflammatory modulation, wound contraction, and collagen synthesis, resulting in faster healing in rats. These effects could be related to the extracts' polyphenolic compounds.


Asunto(s)
Leonurus , Plantas Medicinales , Ratas , Animales , Leonurus/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Plantas Medicinales/química , Cicatrización de Heridas , Flavonoides/farmacología
3.
Chem Biodivers ; 20(11): e202300863, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37747297

RESUMEN

Oreochromis niloticus (Nile tilapia) skin is a by-product of Brazilian fish farming, rich in collagen. The present study aims to evaluate the wound healing, antioxidant, and antimicrobial potential of the raw hydrolyzed extract of Nile tilapia skin, as well as the identification of the main compounds. The in vitro activity was performed using antioxidant, antimicrobial and scratch wound healing assays. An in vivo experiment was performed to evaluate the wound healing potential. On days 1, 7, 14 and 21, the lesions were photographed to assess wound retraction and on the 7th , 14th and 21st  days the skins were removed for histological evaluation and the blood of the animals was collected for glutamic oxaloacetic transaminase and glutamic pyruvic transaminase determination. The chemical study was carried out through liquid chromatography-tandem mass spectrometry and de novo sequencing of peptides. The in vitro assays showed a reduction of the gap area in 24 h, dose-dependent antimicrobial activity for both bacteria, and antioxidant activity. The chemical analysis highlighted the presence of active biopeptides. The histological evaluation showed that the raw hydrolyzed extract of Nile tilapia skin has a healing potential, and does not present toxicological effects; therefore, is promising for the treatment of wounds.


Asunto(s)
Antiinfecciosos , Cíclidos , Animales , Cíclidos/microbiología , Antioxidantes/farmacología , Cromatografía de Gases y Espectrometría de Masas , Antiinfecciosos/farmacología , Cicatrización de Heridas
4.
Molecules ; 28(14)2023 Jul 21.
Artículo en Inglés | MEDLINE | ID: mdl-37513446

RESUMEN

Species of the genus Kalanchoe have a long history of therapeutic use in ethnomedicine linked to their remarkable healing properties. Several species have chemical and anatomical similarities, often leading to confusion when they are used in folk medicine. This review aims to provide an overview and discussion of the reported traditional uses, botanical aspects, chemical constituents, and pharmacological potential of the Kalanchoe species. Published scientific materials were collected from the PubMed and SciFinder databases without restriction regarding the year of publication through April 2023. Ethnopharmacological knowledge suggests that these species have been used to treat infections, inflammation, injuries, and other disorders. Typically, all parts of the plant are used for medicinal purposes either as crude extract or juice. Botanical evaluation can clarify species differentiation and can enable correct identification and validation of the scientific data. Flavonoids are the most common classes of secondary metabolites identified from Kalanchoe species and can be correlated with some biological studies (antioxidant, anti-inflammatory, and antimicrobial potential). This review summarizes several topics related to the Kalanchoe genus, supporting future studies regarding other unexplored research areas. The need to conduct further studies to confirm the popular uses and biological activities of bioactive compounds is also highlighted.


Asunto(s)
Crassulaceae , Kalanchoe , Plantas Medicinales , Fitoterapia , Fitoquímicos/química , Etnofarmacología , Extractos Vegetales/química
7.
Chem Biodivers ; 19(12): e202200568, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36259393

RESUMEN

The species Euphorbia umbellata has been used to treat inflammatory diseases, cancer, and ulcers. Biological activities reported in the literature, including antiproliferative, cytotoxic and anti-inflammatory, are attributed to the chemical constituents present in its composition as terpenes and polyphenolic compounds. The most recurrently verified metabolites in the Euphorbiaceae family plant species are terpenes, of which euphol is a major constituent with broadly reported cytotoxic, antinociceptive and anti-inflammatory effects; it frequently appears in various extracts obtained from the plant. Euphol has a documented inhibitory effect on neutrophil chemotaxis and can modulate the complement system. Since complement system activation is intimately intertwined with autoimmune and inflammatory diseases, tumor growth promotion and metastasis, plant metabolites from Euphorbia umbellata might influence the outcomes of inflammatory processes. We believe that this is the first review presenting the current knowledge on Euphorbia umbellata secondary metabolites and their biological activities.


Asunto(s)
Antineoplásicos , Euphorbia , Euphorbiaceae , Neoplasias , Humanos , Euphorbia/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Lanosterol/farmacología , Antiinflamatorios
9.
Life Sci ; 280: 119700, 2021 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-34111465

RESUMEN

AIMS: This study evaluated the effect of euphol isolated from Euphorbia umbellata (Pax) Bruyns latex on the activation of complement pathways (classical (CP), alternative (AP) and lectin (LP)), neutrophil chemotaxis, cytotoxic activity, cell morphology and death in HRT-18 and 3T3 cells lines. MAIN METHODS: CP and AP were assessed using hemolytic assays and ELISA for LP; neutrophil chemotaxis was performed using Boyden's chamber; cytotoxicity was evaluated by neutral red methodology and characteristics of cell death were assessed by cell morphology with hematological staining. KEY FINDINGS: Although euphol increased CP activation (38% at a concentration of 976.1 µM), an inhibitory effect on AP, LP (31% and 32% reduction in the concentration of 976.1 µM) and neutrophil chemotaxis (inhibit 84% of neutrophil migration at a concentration 292.9 µM) was observed. In addiction euphol was able to induce significant cell death in a time-dependent manner, presenting an IC50 of 70.8 µM and 39.2 µM for HRT-18 and 3T3 cell lines respectively and it was also observed apoptotic characteristics as cellular rounding, chromatin condensation and blebs formation for both cell lines. SIGNIFICANCE: Euphol has a potential use for the treatment of complement-related inflammatory diseases due to its ability to downregulate inflammation. On the other hand, the controlled activation of CP can contribute to complement-dependent cytotoxicity in the context of monoclonal antibody-based cancer treatment.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Activación de Complemento/efectos de los fármacos , Factores Inmunológicos/farmacología , Lanosterol/análogos & derivados , Células 3T3 , Animales , Muerte Celular/efectos de los fármacos , Línea Celular Tumoral , Euphorbia/química , Humanos , Lanosterol/farmacología , Ratones , Neoplasias/tratamiento farmacológico
10.
J Ethnopharmacol ; 265: 113348, 2021 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-32896626

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: The species Euphorbia umbellata (leitosinha) has been traditionally used for the treatment of inflammatory diseases and cancer. AIM OF THE STUDY: Evaluation the effect of E. umbellata latex extracts obtained with hexane, chloroform, ethyl acetate and methanol on the activation of the complement pathways and neutrophil chemotaxis. MATERIALS AND METHODS: The latex was partitioned using Soxhlet apparatus and hexane, chloroform, ethyl acetate and methanol as solvents. The classical and alternative pathway activity were performed by hemolytic assays with sensitized sheep or rabbit erythrocytes, respectively; the lectin pathway activity was quantified by ELISA, through the measurement of C4 molecules and the chemotaxis of human neutrophils was performed using 1% casein as the chemotactic inducer and Boyden's chamber. GC-Q-ToF and NMR analyses were applied to evaluate the chemical composition of E. umbellata latex extracts. RESULTS: All E. umbellata latex extracts exhibited an inhibitory effect on the activation of the alternative pathway. Methanol and ethyl acetate extracts inhibited the classical pathway while chloroform extract activated this pathway. Ethyl acetate and hexane extracts inhibited lectin activation. All E. umbellata extracts inhibited casein-induced neutrophil chemotaxis. Terpenes and phenolic compounds have been suggested to be present in the E. umbellta latex extracts. CONCLUSION: The E. umbellata latex was able to modulate the functions of the immune system. Thus, it is possible to infer that the terpenes and phenolic compounds of the phytocomplex of E. umbellata latex can contribute for the activity on the complement pathways.


Asunto(s)
Activación de Complemento/efectos de los fármacos , Euphorbia/química , Neutrófilos/efectos de los fármacos , Extractos Vegetales/farmacología , Animales , Quimiotaxis/efectos de los fármacos , Eritrocitos/efectos de los fármacos , Hemólisis/efectos de los fármacos , Humanos , Fenoles/aislamiento & purificación , Fenoles/farmacología , Extractos Vegetales/química , Conejos , Ovinos , Solventes/química , Terpenos/aislamiento & purificación , Terpenos/farmacología
12.
Phytother Res ; 35(5): 2557-2567, 2021 May.
Artículo en Inglés | MEDLINE | ID: mdl-33350522

RESUMEN

Euphorbia umbellata is used for its anti-inflammatory properties; however, there are limited data available regarding its effects on vascular function. Its bark is rich in polyphenolic compounds, which potentially improve endothelial dysfunction (ED). This study proposes to investigate the effects of E. umbellata bark extracts and its polyphenolic compounds on arginase (ARG) activity and nitric oxide (NO)-related targets. Chromatographic procedures were used for the chemical characterisation of the extracts. Furthermore, in silico (molecular docking), in vitro (ARG inhibition), in vivo (streptozotocin-induced hyperglycemia model), and ex vivo (l-arginine metabolism, vascular reactivity, western blot, and biochemical) techniques were carried out. Quercetin, gallic acid, and ellagic acid were identified in the extracts. In silico screening predicted that gallic acid and quercetin would have the most promising interactions with ARG -identified cavities. This was confirmed in vitro as both compounds had a direct inhibitory effect on ARG, as was the case regarding the extracts. Oral treatment preserved endothelium-dependent vasodilation through ARG inhibition together with an increase in l-arginine bioavailability and endothelial NO synthase expression. Biochemical parameters determined the lack of toxicity for sub-chronic treatment. E. umbellata bark extracts and its compounds can contribute to ED treatment, at least partly, through the inhibition of vascular ARG.

13.
Chem Biodivers ; 17(9): e2000369, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32644295

RESUMEN

The current study was carried out by a bioguided fractionation of a hexane extract of the latex of Euphorbia umbellata against leukemic cells. Samples were analyzed by NMR, GC/MS, triterpenes quantification, and MTT reduction assay. Morphological, cell cycle, mitochondrial membrane potential and caspases 3/7 analyses were performed for the dichloromethane and ethanol fractions, and selectivity index for the dichloromethane fraction. NMR analysis presented characteristic signals of terpenes and steroids, data were confirmed by the quantification of triterpenes and GC/MS analysis. MTT reduction assay demonstrated that HL-60 was the most sensitive cell lineage against dichloromethane and ethanol fractions. Compounds of these matrices caused morphological changes compatible with apoptosis induction, altered cell cycle, increment of depolarized population cells and activation of caspases 3/7. Selectivity indices were higher than 22.44. Bioguided-fractionation study showed that samples of the latex of E. umbellata raised the activity of the phytocomplex against leukemic cells, and the cytotoxicity can be associated with an apoptosis pathway.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Apoptosis/efectos de los fármacos , Euphorbia/química , Látex/química , Terpenos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Ciclo Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Terpenos/química , Terpenos/aislamiento & purificación , Células Tumorales Cultivadas
19.
Planta Med ; 84(5): 277-295, 2018 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-29342480

RESUMEN

Endothelial dysfunction is characterised by the low bioavailability of nitric oxide with a relevant negative impact on the nitric oxide/cGMP pathway. The loss of nitric oxide/cGMP signaling may be caused by an increased arginase activity. Plant-derived substances, especially polyphenols, are compounds that have the potential to inhibit arginase activity and they may represent an attractive therapeutic option to combat clinical outcomes related to endothelial dysfunction. An extensive review was carried out using all available data published in English in the Pubmed database, and without restriction regarding the year of publication. Despite the increased number of new substances that have been tested as arginase inhibitors, it is rare to find a compound that satisfies all the toxicological criteria to be used in the development of a new drug. On the other hand, recent data have shown that substances from plants have great potential to be applied as arginase inhibitors, most of which are polyphenols. Of the relevant mechanisms in this process, the inhibition of arginase by natural products seems to act against endothelial dysfunction by reestablishing the vascular function and elevating nitric oxide levels (by increasing the amounts of substrate (L-arginine, and endothelial nitric oxide synthase activation and stabilisation) as well as decreasing the generation of reactive species (formed by uncoupledendothelial nitric oxide synthase). This review summarises several topics regarding arginase inhibition by natural substances as well as indicating this pathway as an emergent strategy to elevate nitric oxide levels in disorders involving endothelial dysfunction. In addition, some aspects regarding structural activity and future perspectives are discussed.


Asunto(s)
Arginasa/antagonistas & inhibidores , Productos Biológicos/farmacología , Óxido Nítrico/metabolismo , Plantas/química , Polifenoles/farmacología , Enfermedades Vasculares/tratamiento farmacológico , Arginasa/metabolismo , Productos Biológicos/química , Endotelio Vascular/efectos de los fármacos , Endotelio Vascular/fisiopatología , Estructura Molecular , Óxido Nítrico Sintasa/metabolismo , Óxido Nítrico Sintasa de Tipo III/efectos de los fármacos , Óxido Nítrico Sintasa de Tipo III/fisiología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Polifenoles/química , Relación Estructura-Actividad , Enfermedades Vasculares/fisiopatología
20.
J Ethnopharmacol ; 191: 29-40, 2016 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-27301616

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Euphorbia umbellata (leitosinha) is used in southern Brazilian folk medicine to treat gastric problems, as well as for its analgesic and anti-inflammatory properties. AIM OF STUDY: To evaluate the anti-ulcer effects of methanolic bark fraction (MF) against in vivo and in vitro assays, as well as an antioxidant, antibacterial and chromatographic study of this fraction. MATERIALS AND METHODS: In vivo anti-ulcer activity was performed using ethanol and indomethacin models with different MF concentrations (50, 100 or 200mg/Kg). The stomachs of the animals were applied to histological evaluation, and the serum to evaluate the ABTS(•+) radical capture. The 200mg/Kg dose was used to analyze the mechanisms involved in antiulcerogenic properties of methanolic fraction. The in vitro activity was performed using several different antioxidant assays, in addition to anti-Helicobacter pylori and anti-urease experiments. The chromatographic study was carried out by LC-MS analysis. RESULTS: Pharmacological investigation of the MF showed an anti-ulcer potential in ethanol and indomethacin in vivo assays. The material presented a high antioxidant activity for several oxidant in vitro systems (DPPH(•), ABTS(•+), O2(•-), HOCl, TauCl and HRP), as well as an ABTS(•+) capture increasing (7.5%) by the treated animals serum (when compared to the negative control). Prostaglandins, nitric oxide/ cyclic guanosine monophosphate pathway and involvement of the protein components of the glutathione complex are some of the mechanisms related with this potential anti-ulcer action. The histological examination of the stomachs of the animals showed that the MF also prevents local action of offensive agents. Chemical analysis using LC-QTOF-MS revealed the presence of ellagic and gallic acid derivatives and flavonols. CONCLUSION: The findings provide scientific basis to the ethnopharmacological purpose of the studied plant and the biological activities of MF of E. umbellata stem bark may be due to the presence of phenolic compounds.


Asunto(s)
Antiulcerosos/farmacología , Euphorbia/química , Extractos Vegetales/farmacología , Polifenoles/farmacología , Úlcera Gástrica/prevención & control , Estómago/efectos de los fármacos , Animales , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Antiulcerosos/química , Antiulcerosos/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Benzotiazoles/química , Cromatografía Líquida de Alta Presión , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Ácido Elágico/aislamiento & purificación , Ácido Elágico/farmacología , Etanol , Etnofarmacología , Femenino , Flavonoles/aislamiento & purificación , Flavonoles/farmacología , Ácido Gálico/aislamiento & purificación , Ácido Gálico/farmacología , Mucosa Gástrica/metabolismo , Helicobacter pylori/efectos de los fármacos , Indometacina , Metanol/química , Fitoterapia , Corteza de la Planta/química , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Plantas Medicinales , Polifenoles/química , Polifenoles/aislamiento & purificación , Ratas Wistar , Transducción de Señal/efectos de los fármacos , Solventes/química , Espectrometría de Masa por Ionización de Electrospray , Estómago/patología , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patología , Ácidos Sulfónicos/química
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