RESUMEN
CONTEXT: Ganoderma triterpenoids (GTs) have been recognised as an important bioactive ingredient in Ganoderma Lucidum (Leyss. ex Fr.) Karst. (Polyporaceae), widely used for treating and preventing chronic hepatopathy of various etiologies. OBJECTIVE: The objective of this study is to better understand the hepatoprotective effect of GTs and to enhance their use in food supplement pharmaceutical and medical industries. MATERIALS AND METHODS: HepG2 cells were pretreated in the presence or absence of GTs (50, 100 and 200 µg/ml) for 4 h, then exposed with 60 µmol/L of t-BHP for an additional 4 h. The cell viability was evaluated by MTT method. ALT, AST and LDH production in culture medium and intracellular MDA, GSH and SOD levels were determined. Moreover, the total triterpenoid content and chemical constituents in GTs were detected by ultraviolet spectrophotometry and HPLC/Q-TOF-MS, respectively. RESULTS: GTs (50, 100 and 200 µg/ml) significantly increased the relative cell viability by 4.66, 7.78 and 13.46%, respectively, and reduced the level of ALT by 11.44%, 33.41% and 51.24%, AST by 10.05%, 15.63% and 33.64%, and LDH by 16.03%, 23.4% and 24.07% in culture medium, respectively. GTs could also remarkably decrease the level of MDA and increase the content of GSH and SOD in HepG2 cells. Furthermore, the total triterpenoid content in GTs was 438 mg GAAEs/g GTs. And 16 triterpenoids in GTs were identified or tentatively characterised. DISCUSSION AND CONCLUSION: Our results showed that GTs had potent cytoprotective effect against oxidative damage induced by t-BHP in HepG2 cells, thus suggesting their potential use as liver protectant.
Asunto(s)
Antioxidantes/farmacología , Ganoderma , Hígado/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Triterpenos/farmacología , terc-Butilhidroperóxido/toxicidad , Antioxidantes/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Relación Dosis-Respuesta a Droga , Células Hep G2 , Humanos , Hígado/metabolismo , Estrés Oxidativo/fisiología , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología , Triterpenos/aislamiento & purificaciónRESUMEN
A simple and reliable method of high-performance liquid chromatography with photodiode array detection (HPLC-DAD) was developed to evaluate the quality of Receptaculum Nelumbinis (dried receptacle of Nelumbo nucifera) through establishing chromatographic fingerprint and simultaneous determination of five flavonol glycosides, including hyperoside, isoquercitrin, quercetin-3-O-ß-d-glucuronide, isorhamnetin-3-O-ß-d-galactoside and syringetin-3-O-ß-d-glucoside. In quantitative analysis, the five components showed good regression (R > 0.9998) within linear ranges, and their recoveries were in the range of 98.31%-100.32%. In the chromatographic fingerprint, twelve peaks were selected as the characteristic peaks to assess the similarities of different samples collected from different origins in China according to the State Food and Drug Administration (SFDA) requirements. Furthermore, hierarchical cluster analysis (HCA) was also applied to evaluate the variation of chemical components among different sources of Receptaculum Nelumbinis in China. This study indicated that the combination of quantitative and chromatographic fingerprint analysis can be readily utilized as a quality control method for Receptaculum Nelumbinis and its related traditional Chinese medicinal preparations.
Asunto(s)
Medicamentos Herbarios Chinos/análisis , Medicamentos Herbarios Chinos/química , Nelumbo/química , Cromatografía Líquida de Alta Presión/métodosRESUMEN
A new species of Anoectochilus (Orchidaceae) from Guangxi, China, A.zhongshanensis, is described here, which was identified based on phylogenetic studies adopting combined plastid markers (rbcL-matK-trnL-F), morphological observation and chemical analysis. Molecular phylogenetic results support the systematic status of A.zhongshanensis as a new species in Anoectochilus genus. Morphologically, this new species is similar to A.zhejiangensis and A.malipoensis, but differs by its characteristic labellum and column, including the hastate or scalpel-shaped lobes of epichile, forward curved and pinnately divided cristate lobes at both sides of the mesochile and inverted triangle column wings. Furthermore, HPLC-ELSD analysis of these three species revealed the interesting chemotaxonomic difference that the principle and characteristic lactone glycoside in this new species was kinsenoside, rather than its diastereoisomer, goodyeroside A, a major glycoside in A.zhejiangensis and A.malipoensis.
RESUMEN
The antioxidant activities of ethanolic crude extract (ECE) and its four different solvent sub-fractions (namely, petroleum ether fraction (PEF), ethyl acetate fraction (EAF), n-butanol fraction (BF) and the aqueous fraction (AF) from the receptacles of Nelumbo nucifera Gaertn. (Receptaculum Nelumbinis) were investigated using two in vitro antioxidant assays. BF showed the highest total phenolic content (607.6 mg/g gallic acid equivalents), total flavonoid content (862.7 mg/g rutin equivalents) and total proanthocyanidin content (331.0 mg/g catechin equivalents), accompanied with the highest antioxidant activity compared to other fractions through 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical scavenging assays. Five flavonol glycosides, namely hyperoside (1), isoquercitrin (2), quercetin-3-O-ß-d-glucuronide (3), isorhamnetin-3-O-ß-d-galactoside (4) and syringetin-3-O-ß-d-glucoside (5) were isolated from the Receptaculum Nelumbinis. Compounds 2-5 were isolated for the first time from the Receptaculum Nelumbinis. The five isolated flavone glycosides, particularly compounds 1-3, demonstrated significant DPPH and ABTS radical scavenging activity, with IC(50) values of 8.9 ± 0.2, 5.2 ± 0.2, 7.5 ± 0.1 for DPPH and 114.2 ± 1.7, 112.8 ± 0.8, 172.5 ± 0.7 µg/mL for ABTS, respectively. These results suggest that Receptaculum Nelumbinis has strong antioxidant potential and may be potentially used as a safe and inexpensive bioactive source of natural antioxidants.
Asunto(s)
Antioxidantes/química , Medicamentos Herbarios Chinos/química , Flavonoles/química , Glicósidos/química , Nelumbo/química , Extractos Vegetales/química , 1-Butanol/química , Benzotiazoles/química , Compuestos de Bifenilo/química , Flavonoides/química , Depuradores de Radicales Libres/química , Concentración 50 Inhibidora , Fenol/química , Picratos/química , Ácidos Sulfónicos/químicaRESUMEN
[This corrects the article DOI: 10.1016/j.chmed.2020.07.002.].
RESUMEN
Eclipta prostrata, an aromatic plant, is known in Chinese herbal medicine for the treatment of various kidney diseases. In the present study, the volatile components were isolated from the aerial parts of this plant by hydrodistillation and analysed by GC-MS. A total of 55 compounds, which were the major part (91.7%) of the volatiles, were identified by matching mass spectra with a mass spectrum library (NIST 05.L). The main components were as follows: heptadecane (14.78%), 6,10,14-trimethyl-2-pentadecanone (12.80%), n-hexadecanoic acid (8.98%), pentadecane (8.68%), eudesma-4(14),11-diene (5.86%), phytol (3.77%), octadec-9-enoic acid (3.35%), 1,2-benzenedicarboxylic acid diisooctyl ester (2.74%), (Z,Z)-9,12-octadecadienoic acid (2.36%), (Z)-7,11-dimethyl-3-methylene-1,6,10-dodecatriene (2.08%) and (Z,Z,Z)-1,5,9,9-tetramethyl-1,4,7-cycloundecatriene (2.07%). The effects of volatile components and ethanolic extract from the aerial parts of this plant on the proliferation and differentiation of primary osteoblasts were evaluated by the MTT method and measuring the activity of alkaline phosphatase (ALP activity). Both volatile components and ethanolic extract (1 microg/mL to 100 microg/mL) significantly (p < 0.01) stimulated the proliferation and increased the ALP activity of primary osteoblasts. These results propose that E. prostrata can play an important role in osteoblastic bone formation, and may possibly lead to the development of bone-forming drugs.
Asunto(s)
Diferenciación Celular/efectos de los fármacos , Eclipta/química , Etanol/química , Aceites Volátiles/farmacología , Osteoblastos/citología , Osteoblastos/efectos de los fármacos , Extractos Vegetales/farmacología , Fosfatasa Alcalina/metabolismo , Animales , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Aceites Volátiles/análisis , Osteoblastos/enzimología , Ratas , Ratas Sprague-DawleyRESUMEN
Total polysaccharide (i.e., GLP-UCE) was effectively isolated from the crude polysaccharide extract powder of Ganoderma lucidum by ultrasonic-circulating extraction, which was separated into three fractions (i.e., GLP-U40, GLP-U60, and GLP-U80) by ethanol fractional precipitation. The detection of antioxidant enzymes (GSH-Px, SOD) and oxidation metabolites (MDA, LF); liver function test of ALT, AST, and LDH; and western blot for antioxidant proteins of GSH-Px and MMP-2 showed that the GLP-UCE displayed a favorable in vivo antioxidant and hepatoprotective activities for reducing the oxidative damage in CCl4-hepatopathy SD rats. The GLP-UCE and its fractions were analyzed and compared by Fourier transform infrared (FT-IR), high-performance liquid chromatography, high-performance gel permeation chromatography, and antioxidant activity in vitro assay. These studies revealed that the fraction GLP-U80 exhibited stronger antioxidant activities in vitro than that of GLP-UCE and other fractions (pAsunto(s)
Antioxidantes
, Riñón/efectos de los fármacos
, Polisacáridos
, Reishi
, Agaricales/química
, Animales
, Antioxidantes/química
, Antioxidantes/aislamiento & purificación
, Antioxidantes/farmacología
, Fraccionamiento Químico/métodos
, Cromatografía Liquida
, Mezclas Complejas/química
, Carbohidratos de la Dieta/farmacología
, Riñón/patología
, Pruebas de Función Hepática
, Polisacáridos/química
, Polisacáridos/aislamiento & purificación
, Polisacáridos/farmacología
, Ratas
, Ratas Sprague-Dawley
, Reishi/química
, Espectroscopía Infrarroja por Transformada de Fourier
RESUMEN
Objective: To establish multi-class bioactive constituents' determination of ten Anoectochilus, four Goodyera and one Ludisia species, and provide reference for the improvement of their quality control. Methods: HPLC-ELSD and phenol-sulphuric acid methods were used for the quantitative determination of lactone glycosides (kinsenoside and its diastereoisomer, goodyeroside A) and polysaccharides, respectively, while an efficient iHPLC-MS/MS method was established for rapid determination of other minor constituents in ten Anoectochilus species and five related species. Results: The contents of kinsenoside, goodyeroside A, polysaccharides and flavonoids varied notably almost in all tested samples, including both wild plants and tissue cultures. In particular, kinsenoside was the major lactone glycoside in A. roxburghii, A. formosanus, A. xingrenensis, A. nandanensis, A. brevilabris and A. burmannicus, whereas goodyeroside A was the predominant constituent in A. lylei, A. longilobus, A. elatus, A. zhejiangensis, G. schlechtendaliana, G. biflora, G. yangmeishanensi, G. repens and Ludisia discolor. Conclusion: Our present study suggested that A. lylei, A. longilobus, A. elatus, A. zhejiangensis, Ludisia discolor and Goodyera species cannot be used as alternatives for A. roxburghii, and goodyeroside A may be reasonably used as a diagnostic marker for distinguishing A. roxburghii from A. lylei, A. longilobus, A. elatus and A. zhejiangensis, Goodyera and Ludisia species. The established method thus could be potentially used for the quality evaluation and control of Anoectochilus and some related species.
RESUMEN
Bioactivity-guided fractionation led to the successful isolation of antiosteoporotic components, i.e. physicion (1), rubiadin-1-methyl ether (2), 2-hydroxy-1-methoxy- anthraquinone (3), 1,2-dihydroxy-3-methylanthraquinone (4), 1,3,8-trihydroxy-2-methoxy- anthraquinone (5), 2-hydroxymethyl-3-hydroxyanthraquinone (6), 2-methoxyanthraquinone (7) and scopoletin (8) from an ethanolic extract of the roots of Morinda officinalis. Compounds 4-8 are isolated for the first time from M. officinalis. Among them, compounds 2 and 3 promoted osteoblast proliferation, while compounds 4, 5 increased osteoblast ALP activity. All of the isolated compounds inhibited osteoclast TRAP activity and bone resorption, and the inhibitory effects on osteoclastic bone resorption of compounds 1 and 5 were stronger than that of other compounds. Taken together, antiosteoporotic activity of M. officinalis and its anthraquinones suggest therapeutic potential against osteoporosis.
Asunto(s)
Antraquinonas/química , Antraquinonas/farmacología , Conservadores de la Densidad Ósea/química , Conservadores de la Densidad Ósea/farmacología , Morinda/química , Osteoblastos/efectos de los fármacos , Osteoclastos/efectos de los fármacos , Fosfatasa Alcalina/metabolismo , Animales , Antraquinonas/uso terapéutico , Conservadores de la Densidad Ósea/uso terapéutico , Resorción Ósea/tratamiento farmacológico , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Estructura Molecular , Osteoblastos/citología , Osteoclastos/citología , Ratas , Ratas WistarRESUMEN
BACKGROUND: Bone formation and resorption is a balanced and continuous process. When osteoclastic bone resorption exceeds osteoblastic bone formation, bone density decreases, which can lead to osteoporosis. Er-Zhi-Wan (EZW), a famous traditional Chinese formulation, has been developed as a restorative formula for hundreds of years, which contains two herbs viz. Herba Ecliptae and Fructus Ligustri Lucidi. EZW is widely used to prevent and treat various kidney diseases for its actions of nourishing the kidney yin and strengthening tendon and bone. The objective of current study was to investigate the effects of EZW on proliferation and differentiation of osteoblasts and osteoclasts in vitro using a serum pharmacological method. METHODS: The rats were orally administered EZW (0.45, 1.8 and 7.2gkg(-1)) for total seven doses and twice a day, and then the different concentrations of EZW-containing serum were prepared. The proliferation of primary cultural osteoblasts, UMR106 and RAW264.7 cells and differentiation of osteoclasts were determined after these cells were treated with different concentrations of EZW-containing serum for a period of time. RESULTS: The serum from rats treated with EZW for 4 days did not facilitate proliferation of primary cultural osteoblasts and UMR106 cells, but evidently inhibited both proliferation of RAW264.7 cells and differentiation of osteoclasts from RAW264.7 cells induced by receptor activator of nuclear factor kappaB ligand (RANK-L) and macrophage-colony stimulating factor (M-CSF). CONCLUSION: Antiosteoporotic activity of EZW is carried out mainly via restraint of osteoclastic bone resorption, which is in accordance with the traditional Chinese medicine theory on nourishing the kidney yin. Therefore EZW has favorable potency to develop a new anti-osteoporotic agent in clinic.
Asunto(s)
Medicamentos Herbarios Chinos/administración & dosificación , Osteoblastos/efectos de los fármacos , Osteoclastos/efectos de los fármacos , Osteoporosis/tratamiento farmacológico , Administración Oral , Animales , Diferenciación Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Masculino , Osteoporosis/patología , Ratas , Ratas Sprague-DawleyRESUMEN
An endophytic fungus Chaetomium fusiforme was obtained from a liverwort, Scapania verrucosa. A comparison of the constituents of the ether extracts between S. verrucosa and the C. fusiforme culture was investigated by gas chromatography-mass spectrometry (GC/MS). The yield of ether extract based on dried plant material was 0.6% and 59 compounds were found in S. verrucosa. (+)-Aromadendrene (9.12%), hexadecanoic acid (6.92%), 6-isopropenyl-4,8a-dimethyl-1,2,3,5,6,7,8,8a-octahydro-naphthalen-2-ol (5.97%), s-tetrachloroethane (5.61%) and acetic acid (5.30%) were found to be the most abundant components among the 49 characterized compounds in S. verrucosa, which represented 84.64% of the total extract. However, the constituents of the cultured endophyte extract contained mainly acetic acid (35.05%), valeric acid, 3-methyl-, methyl ester (21.25%), and butane-2, 3-diol (12.24%). Although the extracts of S. verrucosa and its endophyte showed little chemical composition correlation, both of them demonstrated antifungal and antitumor activities. Furthermore, C. fusiforme has displayed a wider range of antimicrobial and antitumor activities, which were better than the host plant. These results could support the suggestion of endophytes as an alternative of the host for medicinal activity.
Asunto(s)
Antifúngicos/química , Antineoplásicos/química , Chaetomium/química , Hepatophyta/química , Antifúngicos/aislamiento & purificación , Antineoplásicos/aislamiento & purificación , Aspergillus fumigatus/efectos de los fármacos , Candida albicans/efectos de los fármacos , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Cryptococcus neoformans/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Éter/química , Cromatografía de Gases y Espectrometría de Masas , Células HL-60 , Hepatophyta/microbiología , Humanos , Concentración 50 Inhibidora , Pruebas de Sensibilidad MicrobianaRESUMEN
We recently proposed, and successfully applied, a novel and efficient technique-ultrasonic-circulating extraction (UCE) integrating superfine pulverization-to extract and prepare antioxidant crude polysaccharides other natural active substances from Ganoderma lucidum. The aim of this study was to evaluate the antioxidant and hepatoprotective activities and active ingredients in the powder from UCE (UCEP) through comparison with powder from hot water extraction (HWEP). The DPPH radical, ABTS radical, superoxide anion, total antioxidant activity, and ferric-reducing antioxidant power assay results showed that the UCEP exhibited stronger (P < 0.01) in vitro antioxidant activity than the HWEP. The hepatoprotective activity of the extracts was evaluated against CCl4-induced oxidative damage in the liver. Measurements of reduced glutathione, superoxide dismutase, and malondialdehyde in rat liver; measurements of alanine transaminase, aspartate transaminase, and lactate dehydrogenase in rat blood; and Western blotting for antioxidant proteins of transforming growth factor-ß1, heme-oxygenase 1, and glutathione per-oxidase showed that the UCEP had antioxidant activity in vivo either similar to or slightly stronger than (P < 0.1) the HWEP. Further analysis of the active ingredients revealed that the UCEP and HWEP have similar mean yield and total triterpenoid content, but the former has significantly higher (P < 0.05) mean yield and total polysaccharide content than the latter. Our results suggest that the UCEP displays stronger antioxidant activities because of the larger amount of total polysaccharides; the UCEP may be able to be used as an antioxidant and liver protectant.
Asunto(s)
Antioxidantes/farmacología , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Polisacáridos/farmacología , Sustancias Protectoras/farmacología , Reishi/química , Alanina Transaminasa/sangre , Animales , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/metabolismo , Aspartato Aminotransferasas/análisis , Tetracloruro de Carbono/administración & dosificación , Glutatión/metabolismo , L-Lactato Deshidrogenasa/sangre , Hígado/efectos de los fármacos , Hígado/patología , Masculino , Malondialdehído/metabolismo , Oxidación-Reducción , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Ratas , Ratas Sprague-Dawley , Organismos Libres de Patógenos Específicos , Superóxido Dismutasa/sangre , Triterpenos/química , Triterpenos/aislamiento & purificación , Triterpenos/farmacología , Ondas UltrasónicasRESUMEN
The n-butanol fraction of the MeOH extract from Paederia scandens was evaluated for antinociceptive activity in mice using chemical and thermal models of nociception. The n-butanol fraction, given orally at doses of 150, 300 and 600 mg/kg produced significant inhibition of chemical nociception induced by intraperitoneal acetic acid and subplantar formalin or capsaicin injections, and of thermal nociception in the tail-flick test and in the hot plate test. More significant inhibition of nociception was observed at a dose of 600 mg/kg. In the pentobarbital sodium-induced sleeping time test and the open-field test, the n-butanol fraction neither significantly enhanced pentobarbital sodium-induced sleeping time nor impaired motor performance, indicating that the observed anti-nociception was unlikely to be due to sedation or motor abnormality. Moreover, the n-butanol fraction-induced anti-nociception in both the capsaicin and formalin tests was insensitive to naloxone or glibenclamide but was significantly antagonized by nimodipine. These results suggest that the n-butanol fraction produced anti-nociception possibly related to nimodipine-sensitive L-type Ca2+ channels, which merits further studies regarding the precise site and mechanism of action. Furthermore, four iridoid glycosides isolated from the n-butanol fraction might be related to its antinociceptive action fraction. Therefore, the effect on analgesic activity of each chemical compound in large quantity might well be considered in a further study.
Asunto(s)
Analgésicos/farmacología , Rubiaceae/química , 1-Butanol , Ácido Acético , Analgésicos Opioides/farmacología , Animales , Capsaicina , Constricción Patológica/inducido químicamente , Constricción Patológica/prevención & control , Formaldehído , Calor , Hipnóticos y Sedantes/farmacología , Metanol , Ratones , Ratones Endogámicos ICR , Morfina/farmacología , Actividad Motora/efectos de los fármacos , Dimensión del Dolor/efectos de los fármacos , Pentobarbital/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Tiempo de Reacción/efectos de los fármacos , Sueño/efectos de los fármacos , SolventesRESUMEN
The 3,440 open reading frames (ORFs) of Ralstonia solanacearum GMI1000 were used for predicting signal peptides by comprehensive analyses with SignalP 3.0, TMHMM 2.0, TargetP 1.01, LipoP 1.0 and PSORTb, and screening based on L value. Total 186 signal peptides with conserved amino acid residues are found and among them, 134 are secretary types, 22 are RR-motif types and 30 are lipoprotein signal peptides. The length distribution of signal peptide and its domains were analyzed systemically. No type pilin-like signal peptides and bacteriocins and pheronones signal peptides are found in the database of deduced proteins encoded by the genome of R. solanacearum GMI1000.
Asunto(s)
Proteínas Bacterianas/metabolismo , Señales de Clasificación de Proteína/fisiología , Ralstonia solanacearum/metabolismo , Proteínas Bacterianas/química , Valor Predictivo de las Pruebas , Señales de Clasificación de Proteína/genética , Ralstonia solanacearum/química , Ralstonia solanacearum/clasificación , Análisis de Secuencia de ProteínaRESUMEN
OBJECTIVE: To provide DNA molecular marker for identification of Nelumbo nucifera by exploring the differences of nrDNA-ITS sequence of N. nucifera originated from different habitats. METHOD: To compare nrDNA-ITS base sequence using specific PCR-ITS. RESULT: The completed sequence of ITS and 5.8 S rDNA, and the partial sequences of 18S rDNA and 26S rDNA, totally 750 bp, from N. nucifera were obtained. The differences among N. nucifera from different habitats and from different cultivars were found. CONCLUSION: The method can be used to identify N. nucifera among different species and to distinguish their fakes. It provided the basis for identifying N. nucifera from different geographical regions by comparison of their ITS sequences.
Asunto(s)
ADN de Plantas/genética , ADN Espaciador Ribosómico/genética , Nelumbo/genética , Plantas Medicinales/genética , Secuencia de Bases , China , ADN de Plantas/química , ADN de Plantas/metabolismo , ADN Espaciador Ribosómico/clasificación , Desoxirribonucleasa EcoRI/metabolismo , Desoxirribonucleasas de Localización Especificada Tipo II/metabolismo , Contaminación de Medicamentos/prevención & control , Geografía , Nelumbo/clasificación , Filogenia , Plantas Medicinales/clasificación , Reacción en Cadena de la Polimerasa , ARN Ribosómico/genética , ARN Ribosómico 18S/genética , ARN Ribosómico 5.8S/genética , Análisis de Secuencia de ADN , Especificidad de la EspecieRESUMEN
OBJECTIVE: To investigate the anti-inflammatory effect of casticin of Fructus Viticis. METHODS: Observations were made on the anti-inflammatory effect of casticin in the models of acute inflammation in vivo. RESULTS: Casticin inhibited significantly xylene-induced mouse ear edema, egg albumen-induced rat paw edema and acetic acid-induced mouse vascular permeability. CONCLUSION: Casticin has significant anti-inflammatory effect on acute inflammation, which is probably related to the inhibition of the inflammation factors. Casticin is the effective constituent contributing to the anti-inflammatory effect of Fructus Viticis.
Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Flavonoides/farmacología , Inflamación/tratamiento farmacológico , Animales , Permeabilidad Capilar/efectos de los fármacos , Edema/metabolismo , Inflamación/metabolismo , Ratones , Ratones Endogámicos ICR , Ratas , Ratas Sprague-DawleyRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: The roots of Actinidia eriantha Benth (AER) are commonly used traditional folk medicine for the treatment of gastric carcinoma, nasopharyngeal carcinoma, and breast carcinoma. Besides, the anti-proliferative and immunomodulatory effects of AER polysaccharides on tumor-bearing mice have been reported previously. AIM OF THE STUDY: This work was carried out to investigate the anticancer and anti-angiogenic activities of AER. MATERIALS AND METHODS: The growth inhibitory effects of ethanol extracts from the leaves (EEL), stems (EES) and roots (EER) of A. eriantha on human gastric carcinoma SGC7901 cells, human nasopharyngeal carcinoma CNE2 cells, human breast carcinoma MCF7 cells and human umbilical vein endothelial cells (HUVECs) were evaluated by MTT assay. The ethyl acetate fraction from EER (EA-EER) was further investigated for the anticancer activity against SGC7901 cells and the anti-angiogenic activity in HUVECs in vitro. The apoptosis in SGC7901 cells and HUVECs was confirmed by DAPI nuclear staining and flow cytometry analysis, the effect on cellular DNA fragmentation was detected in SGC7901 cells. And the cell cycle-arresting activity in HUVECs was determined by flow cytometry. Moreover, the inhibitory effect of EA-EER on cell migration in HUVECs was observed by both wound-healing and Transwell migration assays. RT-PCR and Western-blotting were performed to determine the mRNA and protein expression levels, respectively, including Bax, Bcl-2 and caspase-3 in SGC7901 cells, as well as VEGF-A and VEGFR-2 in HUVECs. Furthermore, the in vivo anti-angiogenic activity of EA-EER was evaluated by using chick embryo chorioallantoic membrane (CAM) assay. Ultimately, the chemical components in EA-EER were isolated and purified by repeated column chromatography followed by structure characterization using 1H and 13C nuclear magnetic resonance and mass spectroscopy. RESULTS: Compared with EEL and EES, EER displayed the strongest growth inhibitory effect on SGC7901 cells, CNE2 cells and HUVECs. Among the EER fractions, EA-EER exhibited the most potent growth inhibitory activity against SGC7901 cells, CNE2 cells and HUVECs. Moreover, EA-EER induced obvious apoptosis in SGC7901 and HUVECs, and significantly inhibited the proliferation of HUVECs via blockade of cell cycle G1 to S progression. Furthermore, EA-EER suppressed the expression of Bcl-2 and improved the expression Bax and caspase-3 in SGC7901 cells. EA-EER not only inhibited migration of HUVECs, but also down-regulated the expression of VEGF-A and VEGFR-2 in HUVECs. In vivo, EA-EER exposure reduced the formation of blood vessels in chick embryos. A bio-guided isolation of EA-EER led to the isolation of three compounds for the first time, namely (6R, 7E, 9S)-6, 9-hydroxy-megastigman-4, 7-dien-3-one-9-O-ß-D-glucopyranoside, Oleanolic acid-23-O-ß-D-glucopyranoside, 3ß, 23, 24-trihydroxyl-12-oleanen-28-oic acid. CONCLUSION: The present research demonstrated that the significant anticancer and anti-angiogenic effects of AER, providing the supportive evidence for its traditional use in the treatment for cancer. It was suggested that AER could be use as a potential source of cancer therapeutic drug.
Asunto(s)
Actinidia/química , Inhibidores de la Angiogénesis/farmacología , Antineoplásicos Fitogénicos/farmacología , Extractos Vegetales/farmacología , Inhibidores de la Angiogénesis/aislamiento & purificación , Animales , Antineoplásicos Fitogénicos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Embrión de Pollo , Membrana Corioalantoides/efectos de los fármacos , Células Endoteliales de la Vena Umbilical Humana , Humanos , Células MCF-7 , Ratones , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Hojas de la Planta , Raíces de Plantas , Tallos de la PlantaRESUMEN
OBJECTIVE: To promote its comprehensive utilization, the involatile constituents of Mentha haplocalyx were studied systematically. METHOD: The chemical components were isolated and purified by silca gel column chromatography and recrystallization. The chemical structures were elucidated on the basis of physico-chemical properties and spectral data. RESULT: Eight compounds were isolated and identified as: acacetin (I), tilianine (II), linarin (III), n-butyl-beta-D-fructopyranoside (IV), ursolic acid (V), oleanolic acid (VI), beta-sitosterol (VII), daucosterol (VIII). CONCLUSION: Compounds I approximately V were obtained from this plant for the first time.
Asunto(s)
Flavonas/aislamiento & purificación , Glicósidos/aislamiento & purificación , Mentha/química , Plantas Medicinales/química , Triterpenos/aislamiento & purificación , Flavonas/química , Glicósidos/química , Componentes Aéreos de las Plantas/química , Triterpenos/química , Ácido UrsólicoRESUMEN
BACKGROUND: Podocarpium podocarpum (DC.), an edible and medicinal plant popularly used for the treatment of bruises and fracture in Chinese folk medicine, has been proved to possess significant antiosteoporotic effect in our latest research. PURPOSE: Our study aimed to investigate the in vitro and in vivo antiosteoporotic effect of kaempfertrin (KN), a principal flavonoid in P. podocarpum obtained through bio-guided isolation. METHODS: An ovariectomized (OVX) rat model of osteoporosis as well as in vitro osteoblast and osteoclast cell lines were employed to evaluate the antiosteoporotic potency of KN. RESULTS: KN significantly improved the bone mass and microarchitecture in OVX rats, with little estrogen-like side effect compared with estradiol valerate. KN also exhibited stimulatory effect on osteoblastic cells and inhibitory action on osteoclastic cells, which down-regulated the phosphorylation level of I-κB. CONCLUSION: KN possessed significant antiosteoporotic activity. Combined with its limited estrogen-like side effect, KN can be regarded as an idealistic antiosteoporotic candidate for human osteoporosis diseases.