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1.
Molecules ; 26(7)2021 Mar 26.
Artículo en Inglés | MEDLINE | ID: mdl-33810416

RESUMEN

The current COronaVIrus Disease 19 (COVID-19) pandemic caused by SARS-CoV-2 infection is enormously affecting the worldwide health and economy. In the wait for an effective global immunization, the development of a specific therapeutic protocol to treat COVID-19 patients is clearly necessary as a short-term solution of the problem. Drug repurposing and herbal medicine represent two of the most explored strategies for an anti-COVID-19 drug discovery. Clove (Syzygium aromaticum L.) is a well-known culinary spice that has been used for centuries in folk medicine in many disorders. Interestingly, traditional medicines have used clove since ancient times to treat respiratory ailments, whilst clove ingredients show antiviral and anti-inflammatory properties. Other interesting features are the clove antithrombotic, immunostimulatory, and antibacterial effects. Thus, in this review, we discuss the potential role of clove in the frame of anti-COVID-19 therapy, focusing on the antiviral, anti-inflammatory, and antithrombotic effects of clove and its molecular constituents described in the scientific literature.


Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Antivirales/farmacología , Fibrinolíticos/farmacología , Syzygium/química , Adyuvantes Inmunológicos/química , Adyuvantes Inmunológicos/farmacología , Antiinflamatorios no Esteroideos/química , Antivirales/química , /prevención & control , Medicina de Hierbas/métodos , Humanos , Fitoquímicos/química , Fitoquímicos/farmacología , Plantas Medicinales/química
2.
Adv Exp Med Biol ; 1308: 309-352, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33861453

RESUMEN

Today, there is an increased tendency to use herbal remedies. Rhubarb refers to several species of the genus Rheum L. in the Polygonaceae family. This species-rich genus is mainly distributed in Asian countries. Several medicinal effects have been attributed to the Rheum spp. in the traditional and modern medicine such as healing lungs, liver, kidney, womb and bladder diseases, cancer, diabetes, insect bites, relapsing fevers, diarrhea and constipation. Various in vitro, in vivo and clinical studies have investigated the therapeutic effect of extracts, fractions and pure compounds isolated from different species of this genus. Considering the positive findings, several pharmaceutical formulations containing rhubarb extract like capsules, drops, mouthwashes and different topical formulations are now present in the market. However, there are other traditional therapeutic effects of rhubarb that have not been studied yet and it is of great importance to perform confirmatory experiments or clinical investigations. The current review summarizes general information regarding botany, phytochemistry, ethnobotany and pharmacological aspects of Rheum spp. It is hoped that the present review could motivate subsequent research on the other medicinal properties of these plants that have been neglected until today.


Asunto(s)
Polygonaceae , Rheum , Asia , Etnobotánica , Etnofarmacología , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Fitoterapia , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
3.
Adv Exp Med Biol ; 1308: 501-546, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33861457

RESUMEN

Cichorium species have been used widely in traditional medicine universally. It is reported as a treatment for various respiratory and gastrointestinal disorders, as well as diabetes and rheumatism. A range of constituents including phenolic and poly phenolic compounds, fatty and organic acids and essential oils comprise the chemical composition of Cichorium species. Furthermore, modern investigations on these species has shown different pharmacological activities such as antioxidant, antiproliferative, anti-inflammation, antibacterial, anti-hyperglycemic, antidiabetic and hepatoprotective effects which are associated with divers molecular pathways and mechanisms. In this chapter, we have summarized comprehensive information regarding traditional and ethnomedicinal uses, phytochemical analysis and pharmacological aspects of Cichorium species.


Asunto(s)
Asteraceae , Etnofarmacología , Medicina Tradicional , Fitoquímicos/farmacología , Fitoterapia , Extractos Vegetales/farmacología
4.
Phytochemistry ; 186: 112736, 2021 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-33799193

RESUMEN

Euphorbia ebracteolata Hayata, as a traditional medicine, is widely distributed in China, Korea and Japan. In China, the dried root of this plant is named 'langdu'. It is traditionally used to treat oedema, skin ulcers, abdominal distension, cough, asthma, tuberculosis swelling and other diseases. Previous studies have found that the chemical constituents of E. ebracteolata are mainly concentrated in terpenoids, acetophenones, and flavonoids. Both extracts and pure compounds from E. ebracteolata were found to possess many pharmacological activities, such as anticancer, anti-inflammatory, antiviral, and antimicrobial effects. In addition, it was reported that E. ebracteolata shows toxicity. To provide inspiration for further in-depth studies on this plant, this review will provide a timely and systematic summary of E. ebracteolata in traditional uses, phytochemistry, pharmacology toxicology, and quality control.


Asunto(s)
Botánica , Euphorbia , Euphorbiaceae , China , Etnofarmacología , Japón , Fitoquímicos/farmacología , Fitoterapia , Extractos Vegetales/toxicidad , Control de Calidad , República de Corea
5.
Chem Biol Interact ; 341: 109449, 2021 May 25.
Artículo en Inglés | MEDLINE | ID: mdl-33798507

RESUMEN

BACKGROUND: COVID-19, a severe global pandemic caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has emerged as one of the most threatening transmissible disease. As a great threat to global public health, the development of treatment options has become vital, and a rush to find a cure has mobilized researchers globally from all areas. SCOPE AND APPROACH: This review focuses on deciphering the potential of different secondary metabolites from medicinal plants as therapeutic options either as inhibitors of therapeutic targets of SARS-CoV-2 or as blockers of viral particles entry through host cell receptors. The use of medicinal plants containing specific phytomoieties could be seen in providing a safer and long-term solution for the population with lesser side effects. Key Findings and Conclusions: Considering the high cost and time-consuming drug discovery process, therapeutic repositioning of existing drugs was explored as treatment option in COVID-19, however several molecules have been retracted as therapeutics either due to no positive outcomes or the severe side effects. These effects call for exploring the alternate treatment options which are therapeutically effective as well as safe. Keeping this in mind, phytopharmaceuticals derived from medicinal plants could be explored as important resources in the development of COVID-19 treatment, as their role in the past for treatment of viral diseases like HIV, MERS-CoV, and influenza has been well reported. Considering this fact, different phytoconstituents such as flavonoids, alkaloids, tannins and glycosides etc. Possessing antiviral properties against coronaviruses and possessing potential against SARS-CoV-2 have been reviewed in the present work.


Asunto(s)
Antivirales/farmacología , Fitoquímicos/farmacología , Alcaloides/química , Alcaloides/farmacología , Antraquinonas/química , Antraquinonas/farmacología , Antivirales/química , Flavonoides/química , Flavonoides/farmacología , Humanos , Aceites Volátiles/química , Aceites Volátiles/farmacología , Fitoquímicos/química , Plantas Medicinales/química , Plantas Medicinales/metabolismo , Saponinas/química , Saponinas/farmacología , Metabolismo Secundario
6.
Molecules ; 26(6)2021 Mar 22.
Artículo en Inglés | MEDLINE | ID: mdl-33809963

RESUMEN

The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome corona virus-2 (SARS-CoV-2), is the most important health issue, internationally. With no specific and effective antiviral therapy for COVID-19, new or repurposed antiviral are urgently needed. Phytochemicals pose a ray of hope for human health during this pandemic, and a great deal of research is concentrated on it. Phytochemicals have been used as antiviral agents against several viruses since they could inhibit several viruses via different mechanisms of direct inhibition either at the viral entry point or the replication stages and via immunomodulation potentials. Recent evidence also suggests that some plants and its components have shown promising antiviral properties against SARS-CoV-2. This review summarizes certain phytochemical agents along with their mode of actions and potential antiviral activities against important viral pathogens. A special focus has been given on medicinal plants and their extracts as well as herbs which have shown promising results to combat SARS-CoV-2 infection and can be useful in treating patients with COVID-19 as alternatives for treatment under phytotherapy approaches during this devastating pandemic situation.


Asunto(s)
Antivirales/farmacología , Fitoquímicos/farmacología , Plantas Medicinales/química , /patogenicidad , Antivirales/química , Humanos , India , Fitoquímicos/química , Extractos Vegetales/farmacología , /química
7.
Int J Mol Sci ; 22(4)2021 Feb 21.
Artículo en Inglés | MEDLINE | ID: mdl-33670070

RESUMEN

The present study aimed to investigate the enzymatic potential of Silybum marianum leaves to bioconvert phenolic acids produced in S. marianum callus into silymarin derivatives as chemopreventive agent. Here we demonstrate that despite the fact that leaves of S. marianum did not accumulate silymarin themselves, expanding leaves had the full capacity to convert di-caffeoylquinic acid to silymarin complex. This was proven by HPLC separations coupled with electrospray ionization mass spectrometry (ESI-MS) analysis. Soaking the leaf discs with S. marianum callus extract for different times revealed that silymarin derivatives had been formed at high yield after 16 h. Bioconverted products displayed the same retention time and the same mass spectra (MS or MS/MS) as standard silymarin. Bioconversion was achieved only when using leaves of a specific age, as both very young and old leaves failed to produce silymarin from callus extract. Only medium leaves had the metabolic capacity to convert callus components into silymarin. The results revealed higher activities of enzymes of the phenylpropanoid pathway in medium leaves than in young and old leaves. It is concluded that cotyledon-derived callus efficiently produces compounds that can be bio-converted to flavonolignans in leaves tissue of S. marianum.


Asunto(s)
Cardo Lechoso/química , Fitoquímicos/farmacología , Hojas de la Planta/química , Silimarina/farmacología , Extractos Vegetales/química , Hojas de la Planta/enzimología , Espectrometría de Masa por Ionización de Electrospray , Temperatura
9.
Int J Nanomedicine ; 16: 1663-1680, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33688184

RESUMEN

Background: Intracellular tension plays a crucial role in the destruction of the blood-brain barrier (BBB) in response to lesion stimuli. Tight junction structure could be primarily affected by tension activity. In this study, we aimed to determine the effects of extracellular BBB damage on intracellular tension activity, and elucidate the mechanism underlying the effects of intracellular protein nanoparticle-related osmotic pressure on BBB permeability. Methods: The intracellular tension for tight junction proteins occludin and ZO1 was evaluated using the fluorescence resonance energy transfer (FRET)-based tension probes and cpstFRET analysis. The changes in mobility ratios of occludin were evaluated via the fluorescence recovery after photobleaching (FRAP) test. The cytoplasmic osmotic pressure (OP) was measured using Osmometer. The count rate of cytoplasmic nanoparticles was detected by Nanosight NS300. The activation of cofilin and stathmin was examined by Western blot analysis. The BBB permeability in vivo was determined via the changes of Evans Blue (EB) injected into SD rats. The tight junction formation was assessed by the measurement of transendothelial electrical resistance (TEER). Intracellular calcium or chloride ions were measured using Fluo-4 AM or MQAE dyes. Results: BBB lesions were accompanied by changes in occludin/ZO1 tension. Increases in intracellular osmotic pressure were involved in alteration of BBB permeability, possibly through the depolymerization of microfilaments or microtubules and mass production of protein nanoparticles according to the Donnan effect. Recovery of protein nanoparticle-related osmotic pressure could effectively reverse the effects of changes in occludin/ZO1 tension under BBB lesions. Outward tension of intracellular osmotic potential also caused upregulation of membrane fluidity, which promoted nonselective drug influx. Conclusion: Our results suggest a crucial mechanical mechanism underlying BBB lesions, and protein nanoparticle-related osmotic pressure could be a novel therapeutic target for BBB lesion-related brain diseases.


Asunto(s)
Barrera Hematoencefálica/metabolismo , Fluidez de la Membrana , Nanopartículas/química , Presión Osmótica , Proteínas/química , Citoesqueleto de Actina/efectos de los fármacos , Citoesqueleto de Actina/metabolismo , Animales , Barrera Hematoencefálica/efectos de los fármacos , Línea Celular , Azul de Evans/metabolismo , Humanos , Masculino , Fluidez de la Membrana/efectos de los fármacos , Microtúbulos/efectos de los fármacos , Microtúbulos/metabolismo , Ocludina/metabolismo , Presión Osmótica/efectos de los fármacos , Permeabilidad , Fitoquímicos/farmacología , Polimerizacion , Ratas Sprague-Dawley , Uniones Estrechas/efectos de los fármacos , Uniones Estrechas/metabolismo , Proteína de la Zonula Occludens-1/metabolismo
10.
Biol Res ; 54(1): 7, 2021 Mar 02.
Artículo en Inglés | MEDLINE | ID: mdl-33653412

RESUMEN

BACKGROUND: Leaves of the natural plant lotus are used in traditional Chinese medicine and tea production. They are rich in flavonoids. METHODS: In this study, lotus leaf flavonoids (LLF) were applied to human lung cancer A549 cells and human small cell lung cancer cells H446 in vitro to verify the effect of LLF on apoptosis in these cells through the ROS/p38 MAPK pathway. RESULTS: LLF had no toxic effect on normal cells at concentrations up to 500 µg/mL, but could significantly inhibit the proliferation of A549 cells and H446 cells. Flow cytometry showed that LLF could induce growth in A549 cells. We also found that LLF could increase ROS and MDA levels, and decrease SOD activity in A549 cells. Furthermore, qRT-PCR and western blot analyses showed that LLF could upregulate the expression of p38 MAPK (p-p38 MAPK), caspase-3, caspase-9, cleaved caspase-3, cleaved caspase-9 and Bax and downregulate the expression of Cu/Zn SOD, CAT, Nrf2, NQO1, HO-1, and Bcl-2 in A549 cells. Results of HPLC showed that LLF mainly contain five active substances: kaempferitrin, hyperoside, astragalin, phloridzin, and quercetin. The apoptosis-inducing effect of LLF on A549 cells came from these naturally active compounds. CONCLUSIONS: We have shown in this study that LLF is a bioactive substance that can induce apoptosis in A549 cells in vitro, and merits further research and development.


Asunto(s)
Apoptosis/efectos de los fármacos , Flavonoides/farmacología , Lotus/química , Neoplasias Pulmonares/patología , Especies Reactivas de Oxígeno/metabolismo , Proteínas Quinasas p38 Activadas por Mitógenos/metabolismo , Células A549 , Proliferación Celular , Humanos , Neoplasias Pulmonares/tratamiento farmacológico , Fitoquímicos/farmacología , Hojas de la Planta/química , Transducción de Señal/efectos de los fármacos
11.
Int J Mol Sci ; 22(5)2021 Feb 25.
Artículo en Inglés | MEDLINE | ID: mdl-33669060

RESUMEN

Chinese chive (Allium tuberosum) is a medicinal food that is cultivated and consumed mainly in Asian countries. Its various phytochemicals and physiological effects have been reported, but only a few phytochemicals are available for skeletal muscle cell proliferation. Herein, we isolated a new compound, kaempferol-3-O-(6″-feruloyl)-sophoroside (1), along with one known flavonoid glycoside (2) and six amino acid (3-8) compounds from the water-soluble fraction of the shoot of the Chinese chive. The isolated compounds were identified using extensive spectroscopic methods, including 1D and 2D NMR, and evaluated for their proliferation activity on skeletal muscle cells. Among the tested compounds, newly isolated flavonoid (1) and 5-aminouridine (7) up-regulated PI3K/Akt/mTOR pathways, which implies a positive effect on skeletal muscle growth and differentiation. In particular, compound 1 down-regulated the Smad pathways, which are negative regulators of skeletal muscle growth. Collectively, we suggest that major constituents of Chinese chive, flavonoids and amino acids, might be used in dietary supplements that aid skeletal muscle growth.


Asunto(s)
Proliferación Celular/efectos de los fármacos , Cebollino/química , Músculo Esquelético/efectos de los fármacos , Fosfatidilinositol 3-Quinasas/metabolismo , Fitoquímicos/farmacología , Proteínas Proto-Oncogénicas c-akt/metabolismo , Serina-Treonina Quinasas TOR/metabolismo , Aminoácidos/análisis , Aminoácidos/química , Aminoácidos/farmacología , Animales , Diferenciación Celular/efectos de los fármacos , Línea Celular , Cromatografía Liquida , Suplementos Dietéticos/análisis , Flavonoides/análisis , Flavonoides/química , Flavonoides/farmacología , Quempferoles/análisis , Quempferoles/química , Quempferoles/farmacología , Espectrometría de Masas , Ratones , Fitoquímicos/análisis , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/análisis , Extractos Vegetales/farmacología , Transducción de Señal/efectos de los fármacos , Análisis Espectral
12.
Molecules ; 26(4)2021 Feb 14.
Artículo en Inglés | MEDLINE | ID: mdl-33672916

RESUMEN

The in vitro activity of L. donovani (promastigotes, axenic amastigotes and intracellular amastigotes in THP1 cells) and T. brucei, from the fractions obtained from the hydroalcoholic extract of the aerial part of Hypericum afrum and the isolated compounds, has been evaluated. The chloroform, ethyl acetate and n-butanol extracts showed significant antitrypanosomal activity towards T. brucei, with IC50 values of 12.35, 13.53 and 12.93 µg/mL and with IC90 values of 14.94, 19.31 and 18.67 µg/mL, respectively. The phytochemical investigation of the fractions led to the isolation and identification of quercetin (1), myricitrin (2), biapigenin (3), myricetin (4), hyperoside (5), myricetin-3-O-ß-d-galactopyranoside (6) and myricetin-3'-O-ß-d-glucopyranoside (7). Myricetin-3'-O-ß-d-glucopyranoside (7) has been isolated for the first time from this genus. The chemical structures were elucidated by using comprehensive one- and two-dimensional nuclear magnetic resonance (1D and 2D NMR) spectroscopic data, as well as high-resolution electrospray ionization mass spectrometry (HR-ESI-MS). These compounds have also been evaluated for their antiprotozoal activity. Quercetin (1) and myricetin (4) showed noteworthy activity against T. brucei, with IC50 and IC90 values of 7.52 and 5.71 µM, and 9.76 and 7.97 µM, respectively. The T. brucei hexokinase (TbHK1) enzyme was further explored as a potential target of quercetin and myricetin, using molecular modeling studies. This proposed mechanism assists in the exploration of new candidates for novel antitrypanosomal drugs.


Asunto(s)
Antiprotozoarios/farmacología , Flavonoides/farmacología , Hypericum/química , Modelos Moleculares , Fitoquímicos/farmacología , Quercetina/farmacología , Trypanosoma/efectos de los fármacos , Secuencia de Aminoácidos , Antiprotozoarios/química , Sitios de Unión , Muerte Celular/efectos de los fármacos , Secuencia Conservada , Flavonoides/química , Flavonoides/aislamiento & purificación , Ligandos , Simulación de Dinámica Molecular , Fitoquímicos/química , Estructura Secundaria de Proteína , Proteínas Protozoarias/química , Quercetina/química , Quercetina/aislamiento & purificación , Agua/química
13.
Molecules ; 26(4)2021 Feb 20.
Artículo en Inglés | MEDLINE | ID: mdl-33672486

RESUMEN

Medicinal plants and their derived compounds have drawn the attention of researchers due to their considerable impact on human health. Among medicinal plants, mint (Mentha species) exhibits multiple health beneficial properties, such as prevention from cancer development and anti-obesity, antimicrobial, anti-inflammatory, anti-diabetic, and cardioprotective effects, as a result of its antioxidant potential, combined with low toxicity and high efficacy. Mentha species are widely used in savory dishes, food, beverages, and confectionary products. Phytochemicals derived from mint also showed anticancer activity against different types of human cancers such as cervix, lung, breast and many others. Mint essential oils show a great cytotoxicity potential, by modulating MAPK and PI3k/Akt pathways; they also induce apoptosis, suppress invasion and migration potential of cancer cells lines along with cell cycle arrest, upregulation of Bax and p53 genes, modulation of TNF, IL-6, IFN-γ, IL-8, and induction of senescence phenotype. Essential oils from mint have also been found to exert antibacterial activities against Bacillus subtilis, Streptococcus aureus, Pseudomonas aeruginosa, and many others. The current review highlights the antimicrobial role of mint-derived compounds and essential oils with a special emphasis on anticancer activities, clinical data and adverse effects displayed by such versatile plants.


Asunto(s)
Antibacterianos/farmacología , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Mentha/química , Aceites Volátiles/farmacología , Fitoquímicos/farmacología , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Bacterias/efectos de los fármacos , Compuestos de Bifenilo/antagonistas & inhibidores , Proliferación Celular/efectos de los fármacos , Humanos , Aceites Volátiles/química , Aceites Volátiles/aislamiento & purificación , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Picratos/antagonistas & inhibidores
14.
Molecules ; 26(4)2021 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-33671866

RESUMEN

Oxidative stress, which refers to unbalanced accumulation of reactive oxygen species (ROS) levels in cells, has been linked to acute and chronic diseases. Nuclear factor erythroid 2-related factor 2/antioxidant response element (Nrf2/ARE) pathway plays a vital role in regulating cytoprotective genes and enzymes in response to oxidative stress. Therefore, pharmacological regulation of Nrf2/ARE pathway is an effective method to treat several diseases that are mainly characterized by oxidative stress and inflammation. Natural products that counteract oxidative stress by modulating Nrf2 have contributed significantly to disease treatment. In this review, we focus on bioactive compounds derived from food that are Nrf2/ARE pathway regulators and describe the molecular mechanisms for regulating Nrf2 to exert favorable effects in experimental models of diseases.


Asunto(s)
Elementos de Respuesta Antioxidante/genética , Enfermedad , Alimentos , Factor 2 Relacionado con NF-E2/metabolismo , Transducción de Señal , Animales , Humanos , Fitoquímicos/farmacología
15.
Molecules ; 26(4)2021 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-33672083

RESUMEN

Sweet pepper is one of the most important economic fruits with nutritional attributes. In this sense, the nutraceutical value of consumed products is a major concern nowadays so the content of some bioactive compounds and antioxidants (phenols, ascorbic acid, lycopene, carotenoids, chlorophylls, and antioxidant activity) was monitored in 18 sweet pepper landraces at two maturity stages (green and red). All the traits except chlorophylls significantly increased in red fruits (between 1.5- and 2.3-fold for phenols, ascorbic acid, and 2-2-diphenyl-1-picrylhydrazyl (DPPH) inhibition activity, 4.8-fold for carotenoid and 27.4-fold for lycopene content), which suggests that ripening is key for obtaining desired fruit quality. Among landraces, P-44 in green fruits is highlighted for its content in carotenoids, chlorophylls, phenols, and ascorbic acid, and P-46 for its antioxidant capacity and lycopene content. Upon maturity, P-48, P-44, and P-41 presented higher levels of phenols and lycopene, and P-39 of phenols, carotenoid, and DPPH. This work reflects a wide variability in the 18 pepper landraces at bioactive compounds concentration and in relation to fruit ripeness. The importance of traditional landraces in terms of organoleptic properties is emphasized as they are the main source of agricultural biodiversity today and could be helpful for breeders to develop new functional pepper varieties.


Asunto(s)
Antioxidantes/farmacología , Capsicum/química , Ecotipo , Fitoquímicos/farmacología , Ácido Ascórbico/análisis , Clorofila/análisis , Suplementos Dietéticos/análisis , Frutas/química , Licopeno/análisis , Fenoles/análisis , Pigmentación , Análisis de Componente Principal
16.
Int J Mol Sci ; 22(5)2021 Feb 24.
Artículo en Inglés | MEDLINE | ID: mdl-33668383

RESUMEN

Cyanidin 3-O-galactoside (Cy3Gal) is one of the most widespread anthocyanins that positively impacts the health of animals and humans. Since it is available from a wide range of natural sources, such as fruits (apples and berries in particular), substantial studies were performed to investigate its biosynthesis, chemical stability, natural occurrences and content, extraction methods, physiological functions, as well as potential applications. In this review, we focus on presenting the previous studies on the abovementioned aspects of Cy3Gal. As a conclusion, Cy3Gal shares a common biosynthesis pathway and analogous stability with other anthocyanins. Galactosyltransferase utilizing uridine diphosphate galactose (UDP-galactose) and cyanidin as substrates is unique for Cy3Gal biosynthesis. Extraction employing different methods reveals chokeberry as the most practical natural source for mass-production of this compound. The antioxidant properties and other health effects, including anti-inflammatory, anticancer, antidiabetic, anti-toxicity, cardiovascular, and nervous protective capacities, are highlighted in purified Cy3Gal and in its combination with other polyphenols. These unique properties of Cy3Gal are discussed and compared with other anthocyanins with related structure for an in-depth evaluation of its potential value as food additives or health supplement. Emphasis is laid on the description of its physiological functions confirmed via various approaches.


Asunto(s)
Antocianinas/farmacología , Antiinflamatorios/farmacología , Antineoplásicos/farmacología , Productos Biológicos/farmacología , Galactósidos/farmacología , Hipoglucemiantes/farmacología , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Animales , Frutas/química , Humanos
17.
Braz J Biol ; 82: e236297, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33787716

RESUMEN

Plectranthus barbatus Andrews (Lamiaceae) is widely distributed in the world and has a range of popular therapeutic indications. This work aimed to evaluate the phytochemical characterization of two leaf extracts of P. barbatus, and their antimicrobial, antineoplastic and immunomodulatory potential. After collection, herborization and obtainment of the P. barbatus aqueous extract (PBA) and acetone:water 7:3 P. barbatus organic extract (PBO), the phytochemical characterization was performed by high-performance liquid chromatography (HPLC). The antimicrobial activity was performed to determine the minimum inhibitory concentration (MIC) against eight bacterial strains using the microdilution test and the fungus Trichophyton rubrum by disc diffusion assay and microdilution test. Cytotoxicity was assessed by MTT and trypan blue methods in normal peripheral blood mononuclear cells (PBMCs) at concentrations ranged between 0.1 to 100 µg.mL-1 and in neoplastic cell lines Toledo, K562, DU-145 and PANC-1 at 1, 10 and 100 µg.mL-1 . Immunomodulatory activity, was evaluated by sandwich ELISA of proinflammatory cytokines at BALB/c mice splenocytes cultures supernatant. Both extracts presented flavonoids, cinnamic derivatives, steroids and ellagic acid. PBO showed bacteriostatic activity against Acinetobacter baumannii (MIC = 250 µg.mL-1) clinical isolate and PBA fungistatic activity against Trichophyton rubrum (MIC = 800 µg.mL-1). The extracts did not exhibit toxicity to PBMCs and neoplastic cells (IC50 > 100 µg.mL-1). Additionally, PBO at 100 µg.mL-1 significantly inhibited IFN-γ and IL-17A cytokines (p = 0.03). Plectranthus barbatus is a potential candidate for therapeutic use due to its low toxicity in healthy human cells and exhibits biological activities of medical interest as bacteriostatic, fungistatic and immunomodulatory.


Asunto(s)
Plectranthus , Animales , Arthrodermataceae , Leucocitos Mononucleares , Ratones , Ratones Endogámicos BALB C , Pruebas de Sensibilidad Microbiana , Fitoquímicos/farmacología , Extractos Vegetales/farmacología
18.
Molecules ; 26(5)2021 Feb 24.
Artículo en Inglés | MEDLINE | ID: mdl-33668106

RESUMEN

Tagetes erecta L. is a popular ornamental plant of the Asteraceae family, which is widely cultivated not only for its decorative use, but also for the extraction of lutein. Besides carotenoid representatives, which have been extensively studied, other important classes of secondary metabolites present in the plant, such as polyphenols, could exhibit important biological activities. The phytochemical analysis of a methanolic extract obtained from T. erecta inflorescences was achieved using liquid chromatography-mass spectrometry (LC-MS) techniques. The extract was further subjected to a multistep purification process, which allowed the separation of different fractions. The total extract and its fractions contain several polyphenolic compounds, such as hydroxybenzoic and hydroxycinnamic acid derivatives, flavonols (especially quercetagetin glycosides), and several aglycons (e.g., quercetin, patuletin). One of the fractions, containing mostly quercetagitrin, was subjected to two different antioxidant assays (metal chelating activity and lipoxygenase inhibition) and to in vitro cytotoxicity assessment. Generally, the biological assays showed promising results for the investigated fraction compared to the initial extract. Given the encouraging outcome of the in vitro assays, further purification and structural analysis of compounds from T. erecta extracts, as well as further in vivo investigations are justified.


Asunto(s)
Antioxidantes/farmacología , Flores/química , Inhibidores de la Lipooxigenasa/farmacología , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Tagetes/química , Animales , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Fibroblastos/efectos de los fármacos , Lipooxigenasa/metabolismo , Inhibidores de la Lipooxigenasa/química , Inhibidores de la Lipooxigenasa/aislamiento & purificación , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Conejos , Relación Estructura-Actividad
19.
Molecules ; 26(5)2021 Feb 24.
Artículo en Inglés | MEDLINE | ID: mdl-33668293

RESUMEN

Plant-based foods, like fruits, vegetables, whole grains, legumes, nuts, seeds and other foodstuffs, have been deemed as heart healthy. The chemicals within these plant-based foods, i.e., phytochemicals, are credited with protecting the heart. However, the mechanistic actions of phytochemicals, which prevent clinical endpoints, such as pathological cardiac hypertrophy, are still being elucidated. We sought to characterize the overlapping and divergent mechanisms by which 18 selected phytochemicals prevent phenylephrine- and phorbol 12-myristate 13-acetate-mediated cardiomyocyte enlargement. Of the tested 18 compounds, six attenuated PE- and PMA-mediated enlargement of neonatal rat ventricular myocytes. Cell viability assays showed that apigenin, baicalein, berberine hydrochloride, emodin, luteolin and quercetin dihydrate did not reduce cell size through cytotoxicity. Four of the six phytochemicals, apigenin, baicalein, berberine hydrochloride and emodin, robustly inhibited stress-induced hypertrophy and were analyzed further against intracellular signaling and genome-wide changes in mRNA expression. The four phytochemicals differentially regulated mitogen-activated protein kinases and protein kinase D. RNA-sequencing further showed divergence in gene regulation, while pathway analysis demonstrated overlap in the regulation of inflammatory pathways. Combined, this study provided a comprehensive analysis of cardioprotective phytochemicals. These data highlight two defining observations: (1) that these compounds predominantly target divergent gene pathways within cardiac myocytes and (2) that regulation of overlapping signaling and gene pathways may be of particular importance for the anti-hypertrophic actions of these phytochemicals. Despite these new findings, future works investigating rodent models of heart failure are still needed to understand the roles for these compounds in the heart.


Asunto(s)
Cardiomegalia/tratamiento farmacológico , Cardiotónicos/farmacología , Miocitos Cardíacos/efectos de los fármacos , Fitoquímicos/farmacología , Animales , Cardiomegalia/metabolismo , Cardiotónicos/química , Células Cultivadas , Miocitos Cardíacos/metabolismo , Fitoquímicos/química , Ratas , Ratas Sprague-Dawley
20.
Molecules ; 26(5)2021 Feb 25.
Artículo en Inglés | MEDLINE | ID: mdl-33668690

RESUMEN

The Mongolian rhubarb-Rheum undulatum L. (RU)-and Rumex crispus L. (RC)-a Taiwanese local rhubarb belonging to the family of Polygonaceae-are principal therapeutic materials in integrative medicine due to their rich quantities of bioactive compounds; however, their phytochemical and antioxidant properties, and anti-cancer activity is poorly investigated. Furthermore, the phytochemical characteristics of both species may be affected by their different geographical distribution and climatic variance. The current study aimed to compare RU with RC extracts in different polarity solvents (n-hexane, ethyl acetate, acetone, ethanol, and water) for their phytochemical contents including the total phenolic content (TPC), total anthraquinone content (TAC), total flavonoid content (TFC), antioxidant and free radical scavenging capacities, and anticancer ability on the HepG2 cell. Except for the n-hexane extract, all of the RU extracts had considerably higher TPCs than RC extracts, ranging from 8.39 to 11.16 mg gallic acid equivalent (GAE) per gram of dry weight, and the TPCs of each extract were also significantly correlated with their antioxidant capacities by ABTS, DPPH, and FRAP assays (p < 0.05). Moreover, there was no remarkable association between the antioxidant capacities and either TACs or TFCs in both the RU and RC extracts. Besides, high-performance liquid chromatography (HPLC) analysis revealed that both the RU and RC extracts contained chrysophanol, emodin, and physcion, and those bioactive compounds were relatively higher in the n-hexane solvent extracts. Additionally, we observed different levels of dose-dependent cytotoxic effects in all the extracts by cell viability assay. Notably, the ethanol extract of RU had a compelling cytotoxic effect with the lowest half-maximum inhibition concentration (IC50-171.94 ± 6.56 µg/mL at 48 h) among the RU extracts than the ethanol extract of RC. Interestingly, the ethanol extract of RU but not RC significantly induced apoptosis in the human liver cancer cell line, HepG2, with a distinct pattern in caspase-3 activation, resulting in increased PARP cleavage and DNA damage. In summary, Mongolian Rhubarb, RU, showed more phytochemical contents, as well as a higher antioxidant capacity and apoptotic effect to HepG2 than RC; thus, it can be exploited for the proper source of natural antioxidants and liver cancer treatment in further investigation.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Rheum/química , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Benzotiazoles/antagonistas & inhibidores , Compuestos de Bifenilo/antagonistas & inhibidores , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Células Hep G2 , Humanos , Mongolia , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Picratos/antagonistas & inhibidores , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Relación Estructura-Actividad , Ácidos Sulfónicos/antagonistas & inhibidores , Taiwán , Células Tumorales Cultivadas
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