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1.
J Org Chem ; 89(12): 8871-8877, 2024 Jun 21.
Artículo en Inglés | MEDLINE | ID: mdl-38837353

RESUMEN

Magterpenes A-C (1-3), three unprecedented meroterpenoids featuring a unique 6/6/6/6/6 polycyclic skeleton, were isolated from the ethanol extract of Magnolia officinalis Rehd. et Wils. The compounds were obtained as racemic mixtures that were completely resolved through chiral columns. Their structures were elucidated by extensive analyses of one-dimensional (1D) and 2D nuclear magnetic resonance, high-resolution electrospray ionization mass spectrometry, chemical calculations of 1H/13C NMR, and electronic circular dichroism calculations. The compounds were constructed via two Diels-Alder reactions in the proposed biosynthetic pathway. All isolates were evaluated for their nephroprotective and hepatoprotective activities. The results demonstrated that (+)-1 and (-)-1 possessed promising nephroprotective activities in a dose-dependent manner, while (-)-2 and (+)-3 exhibited moderate hepatoprotective activities.


Asunto(s)
Magnolia , Terpenos , Magnolia/química , Terpenos/química , Terpenos/farmacología , Terpenos/aislamiento & purificación , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación
2.
Phytochemistry ; 224: 114148, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38763311

RESUMEN

Seven previously undescribed triterpenes (1-7), as well as one triterpene (8) previously described as a synthetic product, were isolated from the antler-shaped fruiting body of Ganoderma lucidum. Their structures were established based on comprehensive spectroscopy analysis. At a concentration of 10 µM, (24E)-3-oxo-15α-acetoxy-lanosta-7,9(11),24-trien-26-al (3) and (24R,25S)-3-oxo-lanosta-7,9(11)-dien-25-ethoxyl-24,26-diol (5) provided significant protection against acetaminophen-induced necrosis in human HepG2 liver cancer cells, and the cell survival rates were 69.7 and 76.1% respectively, similar to that of the positive control (glutathione, 72.1%). Based on the present results, these compounds could be potential hepatoprotective agents.


Asunto(s)
Cuerpos Fructíferos de los Hongos , Sustancias Protectoras , Reishi , Triterpenos , Triterpenos/farmacología , Triterpenos/química , Triterpenos/aislamiento & purificación , Humanos , Células Hep G2 , Cuerpos Fructíferos de los Hongos/química , Reishi/química , Sustancias Protectoras/farmacología , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Estructura Molecular , Supervivencia Celular/efectos de los fármacos , Acetaminofén/farmacología , Relación Estructura-Actividad , Hígado/efectos de los fármacos , Relación Dosis-Respuesta a Droga
3.
Bioorg Chem ; 148: 107461, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38788363

RESUMEN

Stachybatranones A-F (1a/1b and 2-6) and three known analogues, namely methylatranones A and B (7 and 8) and atranone B (9), were isolated and identified from a toxigenic fungus Stachybotrys chartarum. Their structures and absolute configurations were elucidated via the extensive spectroscopic data, comparison of the experimental electronic circular dichroism (ECD) data, and single-crystal X-ray diffraction analyses. Structurally, compounds 2-6 belonged to a rare class of C-alkylated dolabellanes, featuring a unique five-membered hemiketal ring and a γ-butyrolactone moiety both fused to an 11-membered carbocyclic system, while compound 1 (1a/1b) represented the first example of a 5-11-6-fused atranone possessing a 2,3-butanediol moiety. The cardiomyocyte protective activity assay revealed that compounds 1-9 ameliorated cold ischemic injury at 24 h post cold ischemia (CI), with compounds 1 and 4 acting in a dose-dependent manner. Moreover, compound 1 prevented cold ischemia induced dephosphorylation of PI3K and AKT acting in a dose-dependent manner. In this study, a new class of natural products were found to protect cardiomyocytes against cold ischemic injury, providing a potential option for the development of novel cardioprotectants in heart transplant medicine.


Asunto(s)
Miocitos Cardíacos , Stachybotrys , Stachybotrys/química , Animales , Miocitos Cardíacos/efectos de los fármacos , Estructura Molecular , Relación Estructura-Actividad , Relación Dosis-Respuesta a Droga , Ratas , Descubrimiento de Drogas , Productos Biológicos/farmacología , Productos Biológicos/química , Productos Biológicos/aislamiento & purificación , Sustancias Protectoras/farmacología , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación
4.
Chem Biodivers ; 21(6): e202400251, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38606482

RESUMEN

Idiopathic pulmonary fibrosis (IPF) is a chronic interstitial pneumonia that leads to acute lung damage, deterioration of lung function, and increased mortality risk. In this study, we investigated the effects of the orange coproduct extract (OCE) and the combination of pure hesperidin and oleuropein (HO) on an experimental model of pulmonary fibrosis induced by bleomycin (BLM) in Wistar rats. Rats were divided into six groups: the control group (G1), the BLM group (G2), three groups (G3, G4, G5) receiving a single dose of BLM combined with OCE extract at 100, 200, and 300 mg/kg, and group 6 (G6) receiving a single dose of BLM combined with HO: both pure major phenolic compounds of OCE (hesperidin at 50 mg/kg) and olive leaves (oleuropein at 2.5 mg/kg). Oxidative stress in lung tissues was investigated using catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPX) assays and the measurement of malondialdehyde (MDA) and lactate dehydrogenase (LDH) levels. Treatment with OCE and HO normalized the disturbance in oxidative markers' levels and showed a significant reduction in fibrosis score with no renal or hepatic toxic effects. In conclusion, OCE and HO exhibit antifibrotic effects on a rat model of pulmonary fibrosis.


Asunto(s)
Bleomicina , Hesperidina , Glucósidos Iridoides , Extractos Vegetales , Fibrosis Pulmonar , Ratas Wistar , Animales , Glucósidos Iridoides/farmacología , Glucósidos Iridoides/química , Ratas , Fibrosis Pulmonar/inducido químicamente , Fibrosis Pulmonar/tratamiento farmacológico , Fibrosis Pulmonar/metabolismo , Fibrosis Pulmonar/patología , Hesperidina/farmacología , Hesperidina/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Masculino , Citrus sinensis/química , Estrés Oxidativo/efectos de los fármacos , Pulmón/efectos de los fármacos , Pulmón/patología , Pulmón/metabolismo , Sustancias Protectoras/farmacología , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Antioxidantes/farmacología , Antioxidantes/química
5.
Arch Pharm (Weinheim) ; 357(7): e2400055, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38607964

RESUMEN

The study explored the hepatoprotective activity and metabolic profile of Verbena bonariensis L. methanol extract (VBM) and fractions using isoniazid as well as rifampicin-triggered liver toxicity in Wistar albino rats. Metabolite profiling of VBM using HPLC-PDA-ESI-MS identified 12 compounds, mainly iridoids, phenylpropanoids, and flavonoids, where verbascoside represents the major compound. Different biochemical parameters such as aspartate transaminase (AST), alanine transaminase (ALT), and alkaline phosphatase (ALP), bilirubin, and total protein levels were used to assess liver functions. All the evaluated samples exhibited hepatoprotective potential, but VBM exhibited maximum activity and a notable decline in ALP (p < 0.05, significant), even better than the standard drug (silymarin). VBM significantly reduced the elevated ALT, AST, ALP, and total bilirubin. It also triggered a significant elevation in total proteins compared with diseased animals. This was further consolidated by histopathological studies. Verbena bonariensis L. could serve as a potent hepatoprotective agent and may alleviate liver ailments.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas , Isoniazida , Extractos Vegetales , Ratas Wistar , Rifampin , Verbena , Animales , Extractos Vegetales/farmacología , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Rifampin/farmacología , Isoniazida/farmacología , Ratas , Masculino , Verbena/química , Cromatografía Líquida de Alta Presión , Hígado/efectos de los fármacos , Hígado/patología , Hígado/metabolismo , Sustancias Protectoras/farmacología , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación
6.
Fitoterapia ; 175: 105899, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38471575

RESUMEN

Limonin is a natural tetracyclic triterpenoid compound in citrus seeds that presents hepatoprotective effects but is often discarded as agricultural waste because of its low content and low solubility. Herein, limonin with high purity (98.11%) from citrus seeds was obtained via purification by high-speed counter-current chromatography (HSCCC) and recrystallization. Limonin-loaded liposomes (Lip-LM) prepared by thin film hydration and high pressure homogenization method to enhance its solubility and hepatoprotective effect on APAP-induced liver injury (AILI). Lip-LM appeared as lipid nanoparticles under a transmission electron microscope, and showed well dispersed nano-scale size (69.04 ± 0.42 nm), high encapsulation efficiency (93.67% ± 2.51%), sustained release, fine stability. Lip-LM also exhibited significantly better hepatoprotective activity on AILI than free limonin in vivo. In summary, Lip-LM might be used as a potential hepatoprotective agent in the form of dietary supplement and provide an effective strategy to improve the potential value of citrus seeds.


Asunto(s)
Acetaminofén , Enfermedad Hepática Inducida por Sustancias y Drogas , Citrus , Limoninas , Liposomas , Sustancias Protectoras , Semillas , Limoninas/aislamiento & purificación , Limoninas/farmacología , Citrus/química , Semillas/química , Animales , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Ratones , Sustancias Protectoras/farmacología , Sustancias Protectoras/aislamiento & purificación , Masculino , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología
7.
Chem Biodivers ; 21(5): e202400300, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38430215

RESUMEN

Sea buckthorn, a traditional medicinal plant, has been used for several years in China for the prevention and treatment of various diseases, a practice closely associated with its significant antioxidant activity. The aim of this study was to investigate the protective effects of sea buckthorn flavonoids on vascular endothelial cells in an oxidative stress environment. We isolated and extracted active compounds from sea buckthorn and investigated their impact on endothelial nitric oxide synthase (eNOS) activity through the PI3K/AKT-eNOS signaling pathway through a combination of network pharmacology and cellular experiments, elucidating the regulatory effects of these compounds on endothelial cell functions. Three flavonoids, named Fr.4-2-1, Fr.4-2-2 and Fr.4-2-3, were obtained from sea buckthorn. The results of network pharmacology indicated that they might exert their effects by regulating the PI3K-AKT signaling pathway. In vitro results showed that all three flavonoids were effective in alleviating the degree of oxidative stress in cells, among which Fr.4-2-1 exerted its antioxidant effects by modulating the PI3K/AKT-eNOS pathway. Flavonoids in sea buckthorn can effectively inhibit oxidative stress-induced cellular damage, preserving the integrity and functionality of endothelial cells, which is crucial for maintaining vascular health and function.


Asunto(s)
Flavonoides , Hippophae , Óxido Nítrico Sintasa de Tipo III , Estrés Oxidativo , Fosfatidilinositol 3-Quinasas , Proteínas Proto-Oncogénicas c-akt , Transducción de Señal , Hippophae/química , Óxido Nítrico Sintasa de Tipo III/metabolismo , Flavonoides/farmacología , Flavonoides/aislamiento & purificación , Flavonoides/química , Proteínas Proto-Oncogénicas c-akt/metabolismo , Estrés Oxidativo/efectos de los fármacos , Fosfatidilinositol 3-Quinasas/metabolismo , Transducción de Señal/efectos de los fármacos , Humanos , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Células Endoteliales/efectos de los fármacos , Células Endoteliales/metabolismo , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Células Endoteliales de la Vena Umbilical Humana/metabolismo , Supervivencia Celular/efectos de los fármacos , Sustancias Protectoras/farmacología , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación
8.
Mar Drugs ; 20(2)2022 Jan 20.
Artículo en Inglés | MEDLINE | ID: mdl-35200617

RESUMEN

This study aimed to investigate the protective effect of the metabolites produced by a new Lactiplantibacillus plantarum strain BF1-13, isolated from deep seawater (DSW), on the intestinal epithelial barrier against the dysfunction induced by hydrogen peroxide (H2O2) and to elucidate the mechanism underlying the effect. Protective effect of the metabolites by strain BF1-13 on the barrier function of the intestinal epithelial model treated with H2O2 was investigated by the transepithelial electrical resistance (TEER). The metabolites enhanced the Claudin-4 (CLDN-4) expression, including at the transcription level, indicated by immunofluorescence staining and quantitative RT-PCR. The metabolites also showed a suppression of aquaporin3 (AQP3) expression. Lactic acid (LA) produced by this strain of homofermentative lactic acid bacteria (LAB) had a similar enhancement on CLDN-4 expression. The metabolites of L. plantarum strain BF1-13 alleviated the dysfunction of intestinal epithelial barrier owing to its enhancement on the tight junctions (TJs) by LA, along with its suppression on AQP3-facilitating H2O2 intracellular invasion into Caco-2 cells. This is the first report on the enhancement of TJs by LA produced by LAB.


Asunto(s)
Mucosa Intestinal/efectos de los fármacos , Lactobacillus plantarum/metabolismo , Sustancias Protectoras/farmacología , Acuaporina 3/genética , Células CACO-2 , Humanos , Peróxido de Hidrógeno/toxicidad , Mucosa Intestinal/patología , Ácido Láctico/metabolismo , Lactobacillus plantarum/aislamiento & purificación , Sustancias Protectoras/aislamiento & purificación , Agua de Mar , Uniones Estrechas/efectos de los fármacos
9.
Anal Biochem ; 641: 114566, 2022 03 15.
Artículo en Inglés | MEDLINE | ID: mdl-35085547

RESUMEN

Fungi can be used as a potent chemotherapeutic agent to treat various cancers. In current study acetone and methanol extracts of Terfezia claveryi, Terfezia boudieri, Terfezia olbiensis, Picoa lefebvrei, Picoa juniperi were used to assess total phenolic contents, antioxidant activity, ion-chelating impact, antimicrobial activity, the cytotoxic and protective effects. Both methanol and acetone extracts of T. boudieri had the highest FRAP and DPPH scavenging abilities. Dose-dependent increased ion-chelating impact of all tested truffles species was found. Extracts of T. boudieri, T. claveryi, and T. albiensis exhibited higher antimicrobial activities. T. claveryi and T. boudieri showed the highest protective effects against H2O2-induced genotoxicity (P < 0.05), in S. cerevisiae BY4741. The least protective effect was showed by the acetone extracts of T. olbiensis (144 ± 8); methanol extracts of P. lefebvrei (140 ± 8) and P. juniperi (140 ± 10). MCF 7 cells showed more sensitivity against to methanol extracts of T. boudieri at 10-100 µg/mL concentrations. HepG2 cells showed more sensitivity against the methanolic extracts of T. boudieri at both doses. Overall, P. lefebvrei and P. juniperi extracts had the least cytotoxic effects. The species of Terfezia exhibit significant protective effects against DNA damage and also have the potential of cytotoxicity effects.


Asunto(s)
Antibacterianos/farmacología , Antineoplásicos/farmacología , Antioxidantes/farmacología , Ascomicetos/química , Sustancias Protectoras/farmacología , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Compuestos de Bifenilo/antagonistas & inhibidores , Proliferación Celular/efectos de los fármacos , Supervivencia Celular , Ensayos de Selección de Medicamentos Antitumorales , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Humanos , Peróxido de Hidrógeno/antagonistas & inhibidores , Pruebas de Sensibilidad Microbiana , Picratos/antagonistas & inhibidores , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Células Tumorales Cultivadas
10.
Drug Des Devel Ther ; 15: 4615-4632, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34785890

RESUMEN

Andrographolide is the major compound found in the medicinal plant, Andrographis paniculata (Burm.f.) Nees, which accounts for its medicinal properties. Both the plant extract and compound have been reported to exhibit potential cardiovascular activities. This review summarises related studies describing the biological activities and target mechanisms of A. paniculata and andrographolide in vivo and in vitro. The current evidence unambiguously indicated the protective effects provided by A. paniculata and andrographolide administration against myocardial injury. The intervention ameliorates the symptoms of myocardial injury by interfering with the inductive phase of a) inflammatory response mediated by nuclear factor-kappa B (NF-κB), phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt), mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription 3 (STAT3) signalling molecules; b) oxidative stress via activation of nuclear factor erythroid 2-related factor (Nrf-2) and reduction of enzymes responsible for generating reactive oxygen and nitrogen species; c) intrinsic and extrinsic mechanisms in apoptosis regulated by upstream insulin-like growth factor-1 receptor (IGF-1R) and peroxisome proliferator-activated receptor-alpha (PPAR-α); d) profibrotic growth factors thus reducing cardiac fibrosis, improving endothelial function and fibrinolytic function. In conclusion, A. paniculata and andrographolide possess therapeutic potential in the management of myocardial injury, which requires further validation in human clinical trials.


Asunto(s)
Andrographis paniculata/química , Diterpenos/farmacología , Infarto del Miocardio/tratamiento farmacológico , Sustancias Protectoras/farmacología , Diterpenos/química , Diterpenos/aislamiento & purificación , Humanos , Conformación Molecular , Infarto del Miocardio/metabolismo , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación
11.
Molecules ; 26(21)2021 Oct 25.
Artículo en Inglés | MEDLINE | ID: mdl-34770840

RESUMEN

The acid fruit of the "xoconostle" cactus belongs to the genus Opuntia family of cacti. It is used as a functional food for its bioactive compounds. Several studies reported that xoconostle fruits have a high amount of ascorbic acid, betalains, phenols, tannins, and flavonoids. These compounds confer antioxidant, antibacterial, anti-inflammatory, and hepatoprotective gastroprotective activity. Xoconostle fruit extracts were tested by in vitro assays where the digestion conditions were simulated to measure their stability. At the same time, the extracts were protected by encapsulation (microencapsulation, multiple emulsions, and nanoemulsions). Applications of encapsulated extracts were probed in various food matrices (edible films, meat products, dairy, and fruit coatings). The xoconostle is a natural source of nutraceutical compounds, and the use of this fruit in the new food could help improve consumers' health.


Asunto(s)
Suplementos Dietéticos , Frutas/química , Alimentos Funcionales , Opuntia/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Antiinfecciosos/química , Antiinfecciosos/aislamiento & purificación , Antiinfecciosos/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Fraccionamiento Químico/métodos , Emulsiones , Fitoquímicos/química , Extractos Vegetales/aislamiento & purificación , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología
12.
Molecules ; 26(21)2021 Oct 26.
Artículo en Inglés | MEDLINE | ID: mdl-34770868

RESUMEN

Polyphenols are bioactive compounds found naturally in fruits and vegetables; they are widely used in disease prevention and health maintenance. Polyphenol-rich blackcurrant extract (BCE) exerts beneficial effects on vascular health in menopausal model animals. However, the vasculoprotective effects in diabetes mellitus (DM) and atherosclerotic vascular disease secondary to DM are unknown. Therefore, we investigated whether BCE is effective in preventing atherosclerosis using KK-Ay mice as a diabetes model. The mice were divided into three groups and fed a high-fat diet supplemented with 1% BCE (BCE1), 3% BCE (BCE2), or Control for 9 weeks. The mice in the BCE2 group showed a considerable reduction in the disturbance of elastic lamina, foam cell formation, and vascular remodeling compared to those in the BCE1 and Control groups. Immunohistochemical staining indicated that the score of endothelial nitric oxide synthase staining intensity was significantly higher in both BCE2 (2.9) and BCE1 (1.9) compared to that in the Control (1.1). Furthermore, the score for the percentage of alpha-smooth muscle actin was significantly lower in the BCE2 (2.9%) than in the Control (2.1%). Our results suggest that the intake of anthocyanin-rich BCE could have beneficial effects on the blood vessels of diabetic patients.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/uso terapéutico , Extractos Vegetales/uso terapéutico , Polifenoles/uso terapéutico , Sustancias Protectoras/uso terapéutico , Ribes/química , Animales , Diabetes Mellitus Experimental/inducido químicamente , Dieta Alta en Grasa/efectos adversos , Modelos Animales de Enfermedad , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Ratones , Ratones Mutantes , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Polifenoles/química , Polifenoles/aislamiento & purificación , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación
13.
Molecules ; 26(21)2021 Oct 29.
Artículo en Inglés | MEDLINE | ID: mdl-34770962

RESUMEN

To scientifically clarify the hepatoprotective constituents of Fructus Schizandrae chinensis, eleven batches samples of total dibenzocyclooctadiene lignans (TDL) from Schisandra chinensis were prepared by using the optimum extraction technique. Characteristic high-performance liquid chromatography (HPLC) chromatograms were obtained through HPLC analysis technology, and the hepatoprotective effects of the eleven batches of TDL were evaluated by MTT assay. Based on the chemical and biological activity results, the spectrum-effect relationship between the characteristic HPLC fingerprints and the hepatoprotective effect of TDL was established using Minitab 16.0 data analysis software. On the basis of the spectrum-effect relationship, thirteen compounds (1-13) were obtained from the TDL by chemical natural product chemical separation and purification technology, and their structures were identified on the basis of the spectral data and the literature. Based on these compounds, thirteen common peaks among the thirty-three chromatographic peaks in the above HPLC fingerprints were identified. Our findings showed that some components, including, schisandrin B (2), schisandrin A (3), and schisandrol B (7) had significant roles in promoting hepatoprotective activity. Preliminary verification of the spectrum-effect relationship of TDL from S. chinensis was carried out, and the results confirmed that the activity of a composite of these three key components in optimal ratios was better than that of any individual compound, which potentially confirmed the reliability of the spectrum-effect relationship and the synergistic effects of traditional Chinese medicine.


Asunto(s)
Ciclooctanos/farmacología , Lignanos/farmacología , Hígado/efectos de los fármacos , Sustancias Protectoras/farmacología , Schisandra/química , Animales , Tetracloruro de Carbono , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Análisis por Conglomerados , Ciclooctanos/química , Ciclooctanos/aislamiento & purificación , Análisis de los Mínimos Cuadrados , Lignanos/química , Lignanos/aislamiento & purificación , Ratones , Estructura Molecular , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación
14.
Cell Mol Biol (Noisy-le-grand) ; 67(1): 142-146, 2021 Jan 31.
Artículo en Inglés | MEDLINE | ID: mdl-34817355

RESUMEN

Present research project was an attempt to explore the functional/nutraceutical worth of guava leaves from two locally grown varieties (Ruby & Safeda). For the purpose, guava leaves extract was fed to experimental male Sprague Dawley rats to explore the nutraceutical potential of guava leaves against hepatotoxicity. Two studies were performed on two types of rats i.e. study I (normal rats), study II (hepatotoxic rats). In both studies, 250 mg/kg each of pink guava leaves extracts (T1) and white guava leaves extracts (T2) was added in the feed. Feed intake and body weights of the rats were recorded. At the end of the first and eighth week of study, the blood samples of the rats were analyzed to check the effect of guava leaves extracts on renal functioning (Alkaline Phosphatase, Alanine Transaminase and Aspartate Transaminase) as well as liver functioning parameters including urea and creatinine. In both studies, comparatively higher feed consumption was observed in the control group than the rest of the treatments. At the end of study I, the highest weight (207±9.21 g) was observed in T0 whereas, during study II, the maximum value (202±5.58 g) was found in T2 (rats consuming white guava leaves extract) that indicates its effectiveness against hepatotoxicity. Regarding renal functioning tests, pink guava leaves were more effective in decreasing urea and creatinine levels in rats as compared to the white guava leaves in both study plans. Likewise, in each of study trial, pink guava leaves were more effective in reducing AST, ALT and ALP than white guava leaves and control. From the present investigation, it is deduced that guava leaves were effective against hepatotoxicity.


Asunto(s)
Riñón/efectos de los fármacos , Hígado/efectos de los fármacos , Extractos Vegetales/farmacología , Hojas de la Planta/química , Psidium/química , Alanina Transaminasa/metabolismo , Fosfatasa Alcalina/metabolismo , Animales , Aspartato Aminotransferasas/metabolismo , Peso Corporal/efectos de los fármacos , Suplementos Dietéticos , Riñón/metabolismo , Riñón/fisiología , Hígado/metabolismo , Hígado/fisiología , Masculino , Extractos Vegetales/administración & dosificación , Extractos Vegetales/aislamiento & purificación , Sustancias Protectoras/administración & dosificación , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología , Psidium/clasificación , Ratas Sprague-Dawley , Especificidad de la Especie
15.
Fitoterapia ; 155: 105064, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-34656670

RESUMEN

Five undescribed cembranoid alcohols, boscartinols A-E (1-5) were discovered from the gum resin of Boswellia carterii. Their structures were elucidated by analyzing the spectroscopic data. Notably, all these five compounds preserved an isopropyl type cembranoid skeleton, featured the same groups of one epoxy ring at C1-C12 and one hydroxy group at C-11, as well as two double bonds migrating from C3 to C9 and one hydroxy group from C3 to C8 within the cembranoid structure. These cembranoids were evaluated for the hepatoprotective and anti-inflammatory activities using two cell models of APAP-induced HepG2 and LPS-induced RAW 264.7. For hepatoprotective activity, compounds 1 and 5 showed remarkable hepatoprotective activity (inhibition rate of 51.6% and 39.8%, respectively) at 10 µM, with the other three compounds of 2-4 showing less potently hepatoprotective. For anti-inflammatory activity, compounds 2-4 showed significant inhibitory effects on NO produced by LPS-induced RAW 264.7 cell (IC50 values of 13.40 µM, 7.08 µM and 14.26 µM), with the other two compounds of 1 and 5 showing less potently anti-inflammatory activities.


Asunto(s)
Antiinflamatorios/farmacología , Boswellia/química , Sustancias Protectoras/farmacología , Animales , Antiinflamatorios/aislamiento & purificación , Células Hep G2 , Humanos , Ratones , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Gomas de Plantas/química , Sustancias Protectoras/aislamiento & purificación , Células RAW 264.7 , Resinas de Plantas/química
16.
Bioorg Chem ; 116: 105341, 2021 11.
Artículo en Inglés | MEDLINE | ID: mdl-34525394

RESUMEN

Five new dimeric phloroglucinol derivatives, agrimones A - E (1-5), were isolated from the whole plant of Agrimonia pilosa. Their structures including absolute configurations were determined by a series of spectroscopic data (UV, IR, HR-ESI-MS, 1D and 2D NMR), complemented with the comparison of the experimental and calculated ECD spectra, and gauge-independent atomic orbital (GIAO) NMR calculations. Notably, compounds 1 and 2 represent a highly oxidized 6/6/6 tricyclic ring skeleton based on the cis-fused paraquinone and chroman. Compounds 1a, 4, and 5 exhibited moderate hepatoprotective activities against APAP-induced HepG2 cell injury at 10 µM.


Asunto(s)
Agrimonia/química , Floroglucinol/farmacología , Sustancias Protectoras/farmacología , Acetaminofén , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Células Hep G2 , Humanos , Estructura Molecular , Floroglucinol/química , Floroglucinol/aislamiento & purificación , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Relación Estructura-Actividad
17.
Bioorg Chem ; 115: 105252, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-34390972

RESUMEN

Twelve tetrahydrofuran lignans (1-12), including six new compounds (1-6), were isolated from the 70% EtOH extract of the fruits of Leonurus japonicus. Spectroscopic analyses and ECD and OR calculations were used to determine their structures. Compounds 5 and 6 were unusual alkaloidal lignans with a butyrolactam unit. Based on the beneficial effects of the fruits of L. japonicus (Chongweizi in Chinese) on the liver in traditional Chinese medicine (TCM), the hepatocyte protective activities of the isolates were studied by MTT, Hoechst 33,342 staining, and western blotting. The MTT results revealed that compounds 1, 2, 7, and 8 significantly increased the survival rates of HL-7702 cells injured by acetaminophen, with EC50 values of 10.41 ± 0.90 µM, 19.86 ± 3.13 µM, 9.68 ± 1.93 µM, and 21.35 ± 3.58 µM, respectively. In the Hoechst 33,342 fluorescence staining, compounds 1 and 7 suppressed the apoptosis of the injured HL-7702 cells. Furthermore, the western blot analysis showed that compounds 1 and 7 increased the Bcl-2/Bax protein expression ratio and procaspase-3 protein expression, indicating that compounds 1 and 7 may exert hepatoprotective activity by regulating the mitochondrial apoptotic pathway.


Asunto(s)
Frutas/química , Hepatocitos/efectos de los fármacos , Leonurus/química , Lignanos/farmacología , Sustancias Protectoras/farmacología , Apoptosis/efectos de los fármacos , Línea Celular , Relación Dosis-Respuesta a Droga , Humanos , Lignanos/química , Lignanos/aislamiento & purificación , Estructura Molecular , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Relación Estructura-Actividad
18.
J Nat Prod ; 84(8): 2189-2199, 2021 08 27.
Artículo en Inglés | MEDLINE | ID: mdl-34383500

RESUMEN

Prunella vulgaris is a widely used edible Chinese medicinal plant. In the present study, two new abietane-type diterpenoids, abietoquinones A (1) and B (2), were isolated from this plant by an immunosuppressive bioassay-guided isolation procedure. Their structures were elucidated unambiguously by NMR spectroscopic analysis, single-crystal X-ray crystallography, and electronic circular dichroism calculations. Compounds 1 and 2 bear a cyclohex-2-ene-1,4-dione moiety, which is uncommon among abietane diterpenes. Also, abietoquinone A (1) suppressed murine splenocyte proliferation and decreased the production of proinflammatory cytokines induced by concanavalin A (Con A) in vitro. In Con A-challenged mice, preinjection with 1 significantly ameliorated liver injury. Additionally, abietoquinone A (1) exhibited inhibitory activities against the proliferation of murine splenocytes and human T cells induced by anti-CD3/anti-CD28 monoclonal antibodies (mAbs).


Asunto(s)
Abietanos/farmacología , Hepatitis Autoinmune/tratamiento farmacológico , Sustancias Protectoras/farmacología , Prunella/química , Abietanos/aislamiento & purificación , Animales , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Concanavalina A , Citocinas , Femenino , Humanos , Ratones , Ratones Endogámicos C57BL , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Plantas Medicinales/química , Sustancias Protectoras/aislamiento & purificación , Bazo/citología , Linfocitos T/efectos de los fármacos
19.
Chem Biodivers ; 18(10): e2000936, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-34432933

RESUMEN

The antioxidant and mutagenic/antimutagenic activities of the fixed oils from Nigella sativa (NSO) and Nigella damascena (NDO) seeds, obtained by cold press-extraction from the cultivar samples, were comparatively investigated for the first time. The antimutagenicity test was carried out using classical and modified Ames tests. The fatty acid composition of the fixed oils was characterized by gas chromatography-mass spectrometry (GC-MS) while the quantification of thymoquinone in the fixed oils was determined by UPC2 . The main components of the NSO and NDO were found to be linoleic acid, oleic acid, and palmitic acid. The results of the Ames test confirmed the safety of NSO and NDO from the viewpoint of mutagenicity. The results of the three antioxidant test methods were correlated with each other, indicating NDO as having a superior antioxidant activity, when compared to the NSO. Both NSO and NDO exhibited a significant protective effect against the mutagenicity induced by aflatoxin B1 in Salmonella typhimurium TA98 and TA100 strains. When microsomal metabolism was terminated after metabolic activation of the mycotoxin, a significant increase in antimutagenic activity was observed, suggesting that the degradation of aflatoxin B1 epoxides by these oils may be a possible antimutagenic mechanism. It is worthy to note that this is the first study to assess the mutagenicity of NSO and NDO according to the OECD 471 guideline and to investigate antimutagenicity of NDO in comparison to NSO against aflatoxin.


Asunto(s)
Antimutagênicos/farmacología , Antioxidantes/farmacología , Nigella damascena/química , Nigella sativa/química , Aceites de Plantas/farmacología , Sustancias Protectoras/farmacología , Aflatoxina B1/antagonistas & inhibidores , Antimutagênicos/química , Antimutagênicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Compuestos de Bifenilo/antagonistas & inhibidores , Picratos/antagonistas & inhibidores , Aceites de Plantas/química , Aceites de Plantas/aislamiento & purificación , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Salmonella typhimurium/química
20.
Drug Des Devel Ther ; 15: 2885-2897, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34262256

RESUMEN

PURPOSE: The polysaccharide of Anoectochilus roxburghii (wall.) Lindl. (ARPS) is one of its important active ingredients. Hepatoprotective effects of ARPS on rat liver injury induced by CCl4 were studied. METHODS: ARPS was extracted using the ultrasonic method and successfully purified by high-speed counter-current chromatography (HSCCC) with a two-phase aqueous system composed of 12.5% PEG 1000-20% K2HPO4:KH2PO4 (1:1). The HSCCC conditions were optimized, and the structure of ARPS was characterized. The hepatoprotective effects of ARPS against CCl4-induced chronic hepatic injury in SD rats were evaluated. RESULTS: The results showed that ARPS was a water-soluble polysaccharide with a molecular weight of 28,518 Da. It was composed of mannose, ribose, glucose, and arabian sugar; its monosaccharide molar ratio was glucose:ribose:arabinose:mannose = 54.24:13.20:1.09:1.00. The purity of ARPS was determined by HPLC to be 96.93%. The intervention effects of ARPS on CCl4-induced hepatic damage model in rats showed that ARPS could effectively reduce the activity of alanine amino transferase and aspartate amino transferase, decrease the content of malondialdehyde and nitric oxide synthesis, and increase the content of glutathione. Pathology revealed that liver plate order, liver cell degeneration, and edema were improved; inflammatory cell infiltration was not observed after ARPS intervention. CONCLUSION: ARPS had the function of antioxidant for protecting CCl4-induced injured liver, and the mechanisms were related to anti-lipid peroxidation, which could eliminate oxygen-free radicals and protect liver cells from attacks by free radicals.


Asunto(s)
Hepatopatías/prevención & control , Orchidaceae/química , Extractos Vegetales/farmacología , Polisacáridos/farmacología , Animales , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Tetracloruro de Carbono , Modelos Animales de Enfermedad , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Peroxidación de Lípido/efectos de los fármacos , Masculino , Polisacáridos/aislamiento & purificación , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología , Ratas , Ratas Sprague-Dawley
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