RESUMEN
A pair of stilbenes with γ-lactam unit [(+)-1 and (-)-1], a new phenolic glucoside (2), and a new isoflavone glucoside (3), together with two known compounds (4-5) were isolated from the rhizomes of Belamcanda chinensis. The chemical structures of the undescribed compounds were elucidated on the basis of detailed spectroscopic analyses. Compounds 1, 4, and 5 (10 µM) exhibited anti-inflammatory activities with inhibition rates of 30.46%, 60.34%, and 37.91%, respectively, against the NF-κB signaling pathway.
Asunto(s)
Iridaceae , Género Iris , Estilbenos , Rizoma/química , Iridaceae/química , Estilbenos/farmacología , Estructura Molecular , Fenoles/farmacología , Fenoles/química , Glucósidos/farmacologíaRESUMEN
Belamcandaoids A-N (1-14), fourteen new triterpenoids were isolated from the seeds of Belamcanda chinensis. Their structures including absolute configurations were assigned by using spectroscopic, computational, and crystallographic methods. All the compounds except 1 and 2 are 3,4-seco-triterpenoids belonging to fernane type. Biological evaluation results indicated that 3 and 13 could reduce fibronectin and collagen I expression respectively in TGF-ß1 induced kidney proximal tubular cells.
Asunto(s)
Células Epiteliales/efectos de los fármacos , Matriz Extracelular/efectos de los fármacos , Iridaceae/química , Extractos Vegetales/farmacología , Factor de Crecimiento Transformador beta1/antagonistas & inhibidores , Triterpenos/farmacología , Animales , Línea Celular , Teoría Funcional de la Densidad , Relación Dosis-Respuesta a Droga , Células Epiteliales/metabolismo , Matriz Extracelular/metabolismo , Túbulos Renales Proximales/efectos de los fármacos , Túbulos Renales Proximales/metabolismo , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Ratas , Semillas/química , Relación Estructura-Actividad , Factor de Crecimiento Transformador beta1/metabolismo , Triterpenos/química , Triterpenos/aislamiento & purificaciónRESUMEN
Natural product is an excellent candidate for alternative medicine for disease management. The bulb of E. bulbosa is one of the notable Iridaceae family with a variety therapeutic potential that is widely cultivated in Southeast Asia. The bulb has been used traditionally among the Dayak community as a folk medicine to treat several diseases like diabetes, breast cancer, nasal congestion, and fertility problems. The bulb is exceptionally rich in phytochemicals like phenolic and flavonoid derivatives, naphthalene, anthraquinone, and naphthoquinone. The electronic database was searched using various keywords, i.e., E. bulbosa, E. americana, E. palmifolia, E. platifolia, and others due to the interchangeably used scientific names of different countries. Scientific investigations revealed that various pharmacological activities were recorded from the bulb of E. bulbosa including anti-cancer, anti-diabetic, anti-bacterial, anti-fungi, anti-viral, anti-inflammatory, dermatological problems, anti-oxidant, and anti-fertility. The potential application of the bulb in the food industry and in animal nutrition was also discussed to demonstrate its great versatility. This is a compact study and is the first study to review the extensive pharmacological activities of the E. bulbosa bulb and its potential applications. The development of innovative food and pharma products from the bulb of E. bulbosa is of great interest.
Asunto(s)
Antiinfecciosos/farmacología , Antiinflamatorios/farmacología , Antineoplásicos/farmacología , Iridaceae/química , Extractos Vegetales/farmacología , Animales , HumanosRESUMEN
Freesia hybrida is a group of cultivars in the genus Freesia with a strong floral scent composed of diverse volatile organic compounds (VOCs). In this study, the VOCs of 34 F. hybrida were extracted and analyzed by headspace solid phase microextraction and gas chromatography mass spectrometry (HS-SPME-GC-MS). A total of 164 VOCs whose relative contents were higher than 0.05% were detected. The numbers of VOCs in all germplasms differed between 11 to 38, and the relative contents ranged from 32.39% to 94.28%, in which most germplasms were higher than 80%. Terpenoids, especially monoterpenes, were the crucial type of VOCs in most germplasms, of which linalool and D-limonene were the most frequently occurring. Principal component analysis (PCA) clearly separated samples based on whether linalool was the main component, and hierarchical clustering analysis (HCA) clustered samples into 4 groups according to the preponderant compounds linalool and (E)-ß-ocimene. Comparison of parental species and hybrids showed heterosis in three hybrids, and the inherited and novel substances suggested that monoterpene played an important role in F. hybrida floral scent. This study established a foundation for the evaluation of Freesia genetic resources, breeding for the floral aroma and promoting commercial application.
Asunto(s)
Monoterpenos Acíclicos/química , Alquenos/química , Flores/química , Iridaceae/química , Compuestos Orgánicos Volátiles/química , Monoterpenos Acíclicos/metabolismo , Alquenos/metabolismo , Flores/genética , Flores/metabolismo , Iridaceae/genética , Iridaceae/metabolismo , Fitomejoramiento , Compuestos Orgánicos Volátiles/metabolismoRESUMEN
The aim of this study is to explore anti-inflammatory phytochemicals from B. chinensis based on the inhibition of pro-inflammatory enzyme, human neutrophil elastase (HNE) and anti-inflammatory activities in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage. Three stereoisomers of iridal-type triterpenoids (1-3) were isolated from the roots of B. chinensis and their stereochemistries were completely identified by NOESY spectra. These compounds were confirmed as reversible noncompetitive inhibitors against HNE with IC50 values of 6.8-27.0 µM. The binding affinity experiment proved that iridal-type triterpenoids had only a single binding site to the HNE enzyme. Among them, isoiridogermanal (1) and iridobelamal A (2) displayed significant anti-inflammatory effects by suppressing the expressions of pro-inflammatory cytokines, such as iNOS, IL-1ß, and TNF-α through the NF-κB pathway in LPS-stimulated RAW264.7 cells. This is the first report that iridal-type triterpenoids are considered responsible phytochemicals for anti-inflammatory effects of B. chinensis.
Asunto(s)
Antiinflamatorios/farmacología , Iridaceae/química , Elastasa de Leucocito/antagonistas & inhibidores , Extractos Vegetales/farmacología , Triterpenos/farmacología , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Humanos , Elastasa de Leucocito/metabolismo , Lipopolisacáridos/antagonistas & inhibidores , Lipopolisacáridos/farmacología , Ratones , Conformación Molecular , FN-kappa B/antagonistas & inhibidores , FN-kappa B/metabolismo , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Células RAW 264.7 , Triterpenos/química , Triterpenos/aislamiento & purificaciónRESUMEN
Type 2 diabetes (T2D) affects over 320 million people worldwide. Healthy lifestyles, improved drugs and effective nutraceuticals are different components of a response against the growing T2D epidemic. The specialized metabolite montbretin A (MbA) is being developed for treatment of T2D and obesity due to its unique pharmacological activity as a highly effective and selective inhibitor of the human pancreatic α-amylase. MbA is an acylated flavonol glycoside found in small amounts in montbretia (Crocosmia × crocosmiiflora) corms. MbA cannot be obtained in sufficient quantities for drug development from its natural source or by chemical synthesis. To overcome these limitations through metabolic engineering, we are investigating the genes and enzymes of MbA biosynthesis. We previously reported the first three steps of MbA biosynthesis from myricetin to myricetin 3-O-(6'-O-caffeoyl)-glucosyl rhamnoside (mini-MbA). Here, we describe the sequence of reactions from mini-MbA to MbA, and the discovery and characterization of the gene and enzyme responsible for the glucosylation of mini-MbA. The UDP-dependent glucosyltransferase CcUGT3 (UGT703E1) catalyzes the 1,2-glucosylation of mini-MbA to produce myricetin 3-O-(glucosyl-6'-O-caffeoyl)-glucosyl rhamnoside. Co-expression of CcUGT3 with genes for myricetin and mini-MbA biosynthesis in Nicotiana benthamiana validated its biological function and expanded the set of genes available for metabolic engineering of MbA.
Asunto(s)
Diabetes Mellitus Tipo 2/tratamiento farmacológico , Flavonas/biosíntesis , Glucosiltransferasas/metabolismo , Hipoglucemiantes/metabolismo , Ingeniería Metabólica/métodos , Trisacáridos/biosíntesis , Ácidos Cafeicos/química , Ácidos Cafeicos/metabolismo , Flavonas/química , Flavonas/farmacología , Flavonas/uso terapéutico , Flavonoides/química , Flavonoides/metabolismo , Flavonoles/química , Flavonoles/metabolismo , Perfilación de la Expresión Génica , Regulación de la Expresión Génica de las Plantas/genética , Glucosa/química , Glucosa/metabolismo , Glicósidos/química , Glicósidos/metabolismo , Glicosilación , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Iridaceae/química , Iridaceae/enzimología , Filogenia , Proteínas de Plantas/metabolismo , Tallos de la Planta/química , Tallos de la Planta/metabolismo , Plantas Modificadas Genéticamente , Ramnosa/química , Ramnosa/metabolismo , Metabolismo Secundario , Biología Sintética/métodos , Nicotiana/metabolismo , Transcriptoma/genética , Trisacáridos/química , Trisacáridos/farmacología , Trisacáridos/uso terapéutico , Xilosa/química , Xilosa/metabolismoRESUMEN
This study investigated the influence of Eleutherine bulbosa (Mill.) Urb. on the immune responses, bacterial population in the intestines, and resistance of white shrimp, Litopenaeus vannamei, against infection with Vibrio parahaemolyticus. Shrimp were fed with three dosages of powder, at 6.25 g kg-1 (P6.25), 12.5 g kg-1 (P12.5), and 25 g kg-1 (P25). One dosage of the crude extract was provided, 1.25 g kg-1 (E1.25), and the controls without administration of E. bulbosa consisted of a positive control (PC) and a negative control (NC). Feed supplementation was carried out for 30 days; then shrimp from all treatments were challenged by intramuscular injection with V. parahaemolyticus (106 cfu/mL), except for the NC. The results showed that supplementation with the powder and extract of E. bulbosa for 30 days resulted in significantly higher (P < 0.05) immune responses (total hemocyte count (THC), phenoloxidase activity (PO), respiratory bursts (RBs)), gene expression (prophenoloxidase (proPO), lipopolysaccharide- and ß-1,3-glucan-binding protein (LGBP)), and total bacterial count (TBC) compared to PC/NC. In post challenge testing, there were significantly higher levels for THC, PO, RBs, proPO, LGBP, and PE (peroxinetin), and the treatments were able to suppress V. parahaemolyticus in the intestines, hepatopancreas, and muscles and to reduce damage to the muscles and hepatopancreas. The survival rate with P12.5 was significantly higher compared to the other treatments. It was concluded that the shrimp receiving supplementation with the powder and extract of E. bulbosa had increased immunity and resistance against V. parahaemolyticus infection, with the best dosage being the P12.5 treatment.
Asunto(s)
Adyuvantes Inmunológicos/farmacología , Expresión Génica/inmunología , Inmunidad Innata/genética , Iridaceae/química , Penaeidae/inmunología , Extractos Vegetales/farmacología , Vibrio parahaemolyticus/fisiología , Animales , Expresión Génica/efectos de los fármacos , Inmunidad Innata/efectos de los fármacos , Penaeidae/efectos de los fármacos , Penaeidae/microbiología , Extractos Vegetales/química , Polvos/química , Polvos/farmacologíaRESUMEN
Ten new iridal-type triterpenoid derivatives, polycycloiridals K-T (1-10), with a cyclopentane moiety originating from the cyclization of the homofarnesyl side chain were isolated from the rhizomes of Belamcanda chinensis. Their structures were established by spectroscopic data, a single-crystal X-ray diffraction analysis, TDDFT quantum mechanical calculations, and chemical derivatization. Compounds 2 and 10 exhibited 33.4% and 32.9% inhibitory activities, respectively, against PTP1b (protein tyrosine phosphatase) at a concentration of 10 µM. A putative biosynthetic pathway is proposed.
Asunto(s)
Ciclopentanos/química , Iridaceae/química , Rizoma/química , Triterpenos/aislamiento & purificación , Espectroscopía de Resonancia Magnética con Carbono-13 , Cristalografía por Rayos X , Estructura Molecular , Espectroscopía de Protones por Resonancia Magnética , Espectrometría de Masa por Ionización de Electrospray , Triterpenos/químicaRESUMEN
Eight new iridal-type triterpenoid derivatives, including two noriridals with ether bridge (1-2); two iridals lactone (3-4), four monocyclic iridals (5-8), together with five known iridals (9-14) were identified from the rhizome of Belamcanda chinensis. Their structures were elucidated on the basis of comprehensive spectroscopic methods and electronic circular dichroism (ECD) calculations. Bioassay results showed that belamcanoxide B (1) exhibited moderated cytotoxic activities against HCT-116 and MCF-7 cell lines with IC50 values of 5.58 and 3.35⯵M.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Iridaceae/química , Triterpenos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Relación Estructura-Actividad , Triterpenos/química , Triterpenos/aislamiento & purificaciónRESUMEN
Bio-guided fractionation of the 70% ethanol extract of Belamcanda chinensis (L.) DC. revealed four new compounds, including 6â³-O-acetylembinin (5), 3â³-O-acetylembinin (6), irigenin 3'-O-ß-glucopyranoside (8), and 2'-acetyl-1,3-O-diferuloylsucrose (9), along with five known compounds (1-4, 7). Their chemical structures were determined using extensive NMR data, mass spectroscopy, and comparison with published literature. Among the isolates, compounds 1 and 4-7 achieved good regulation of the growth and proliferation of vascular smooth muscle cells.
Asunto(s)
Iridaceae/química , Isoflavonas/farmacología , Músculo Liso Vascular/citología , Músculo Liso Vascular/efectos de los fármacos , Componentes Aéreos de las Plantas/química , Extractos Vegetales/farmacología , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Relación Dosis-Respuesta a Droga , Humanos , Isoflavonas/química , Isoflavonas/aislamiento & purificación , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Relación Estructura-ActividadRESUMEN
Dietes bicolor (Iridaceae) is an ornamental plant used by African local healers to treat diarrhea and dysentery. A new dihydroflavonol, (2R,3R)-3,5,7-trihydroxy-8-methoxyflavanone (1); two known dihydroflavonols, trans-3-hydroxy-5-methoxy-6,7-methylenedioxyflavanone (2) and trans-3-hydroxy-5,7-dimethoxyflavanone (3); the known isoflavone orobol 7,3'-di-O-methyl ether (4); the known biflavones lanaroflavone (5), robustaflavone (6), and amentoflavone (7); and ß-sitosterol (8) were isolated from the CH2Cl2 fraction of D. bicolor leaves. The extract showed potent activity in antiallergic and anti-inflammatory assays. The structures of the isolates were identified by spectroscopic and spectrometric methods. Compounds 6 and 7 (400 µM) exhibited antiallergic activity by inhibiting antigen-induced ß-hexosaminidase release at 45.7% and 46.3%, respectively. Moreover, 6 and 7 exerted anti-inflammatory activity as demonstrated by the inhibition of superoxide anion generation with an IC50 value of 1.0 µM as well as the inhibition of elastase release with IC50 values of 0.45 and 0.75 µM, respectively. The anti-inflammatory activity was further explained by the virtual docking of the isolated compounds to the binding sites in the human neutrophil elastase (HNE) crystal structure using Discovery Studio 2.5. It was concluded that the biflavonoids bind directly to HNE and inhibit its enzymatic activity based on the CDOCKER algorithm. The data provided evidence for the potential use of D. bicolor against certain diseases related to allergy and inflammation.
Asunto(s)
Antialérgicos/química , Antiinflamatorios/química , Biflavonoides/química , Iridaceae/química , Antialérgicos/farmacología , Antiinflamatorios/farmacología , Biflavonoides/farmacología , Línea Celular Tumoral , Humanos , Mastocitos , Extractos Vegetales/química , Hojas de la Planta/química , Sitoesteroles/químicaRESUMEN
BACKGROUND: Inflammatory bowel disease (IBD) [including Crohn's disease (CD) and ulcerative colitis (UC)] constitutes an important clinical problem. The pathogenesis of IBD remains unclear. It is believed that immune dysfunction, inflammatory mediators and oxidative damage play crucial roles in development of IBD. The condition is clinically associated with symptoms ranging from mild to severe during relapses, depending on the affected segment of the gastrointestinal tract. Bloody diarrhea with mucus, abdominal pain, weight loss and anemia are initial symptoms of both CD and UC. Differences between diseases become more evident in time, along with the development of intestinal and extraintestinal complications. Mangiferin (1,3,6,7-tetrahydroxyxanthone-C-2-ß-D-glucoside), a natural polyphenol in plants, exerts antioxidant and anti-inflammatory effects making it an interesting option for the treatment of inflammatory pathologies associated with oxidative stress in humans, such as IBD. PURPOSE: The aim of the current study was to elucidate the impact of mangiferin on colon tissues in 2,4,6-trinitrobenzensulfonic acid (TNBS)-induced colitis in rats. METHODS: Mangiferin was obtained from Belamcanda chinensis rhizomes by a multistage process. Groups of rats were pre-treated with 10, 30 or 100 mg/kg of mangiferin, or with distilled water administered intragastrically for 16 days. An ethanol solution of TNBS or saline was given rectally on the day 15 of the experiment. The experiment was terminated on the day 17. The colon was removed, cleaned, weighed and examined macro- and microscopically. Determination of tumor necrosis factor α (TNF-α), interleukin 17 (IL-17), malondialdehyde (MDA) levels and superoxide dismutase (SOD) activity were performed spectrophotometrically in homogenates of colon tissues. RESULTS: Rats in the TNBS group developed symptoms of colitis, including: body weight loss, colon mass index increase and damage of intestinal tissues with concomitant increase in TNF-α, IL-17, MDA levels and decreased SOD activity. In non-TNBS-treated rats mangiferin did not cause any changes of studied parameters. Pre-treatment with mangiferin exerted a protective effect, reducing the intensity of damage caused by TNBS. Mangiferin at the doses of 30 and 100 mg/kg reduced the macro- and microscopic damage score and the MDA level in colon tissues. Only at the dose of 100 mg/kg, mangiferin decreased TNF-α and IL-17 concentrations, and SOD activity in colon tissues. CONCLUSION: Mangiferin attenuates inflammatory changes of colon tissues in experimental, TNBS-induced colitis in rats. Protective effect exerted by mangiferin depends primarily on its anti-inflammatory activity and secondarily on its antioxidant properties.
Asunto(s)
Colitis/tratamiento farmacológico , Iridaceae/química , Extractos Vegetales/farmacología , Xantonas/farmacología , Animales , Antiinflamatorios/farmacología , Antioxidantes/metabolismo , Colitis/metabolismo , Citocinas/metabolismo , Modelos Animales de Enfermedad , Mediadores de Inflamación/metabolismo , Enfermedades Inflamatorias del Intestino/tratamiento farmacológico , Enfermedades Inflamatorias del Intestino/metabolismo , Masculino , Malondialdehído/metabolismo , Estrés Oxidativo/efectos de los fármacos , Ratas , Ratas Wistar , Factor de Necrosis Tumoral alfa/metabolismoRESUMEN
A new naphthalene derivative and three known compounds were isolated from the petroleum ether extract of the bulbs of Eleutherine americana by using various chromatographic techniques, such as column chromatography over silica gel and semi-preparative HPLC. Their structures were elucidated by spectroscopic date (MS, UV, IR, NMR), which were identified as eleutherol B (1), 4,8-dihydroxy-3-methoxy-1-methylanthraquinone-2-carboxylic acid methyl ester (2), 8-hydroxy-3,4-dimethoxy-1-methylanthraquinone-2-carboxylic acid methyl ester (3), and isoeleutherine (4). Compound 1 is a new compound. The diastolic blood vessels activity of compound 1 and 2 were potent, reaching 82.5% and 85.3% at the concentration of 10 µmol·L⻹, which were basically the same as that of the positive drug tanshinone â ¡A.
Asunto(s)
Iridaceae/química , Naftalenos/química , Raíces de Plantas/química , Cromatografía Líquida de Alta Presión , Estructura Molecular , Naftalenos/aislamiento & purificación , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/químicaRESUMEN
The separation of a compound of interest from its structurally similar homologues to produce high-purity natural products is a challenging problem. This work proposes a novel method for the separation of iristectorigenin A from its structurally similar homologues by ionic-liquid-based ultrasound-assisted extraction and the subsequent screening and isolation of potential α-glucosidase inhibitors via ultrafiltration and semipreparative high-performance liquid chromatography. Ionic-liquid-based ultrasound-assisted extraction was successfully applied to the extraction of tectorigenin, iristectorigenin A, irigenin, and irisflorentin from Belamcanda chinensis. The optimum conditions for the efficient extraction of isoflavones were determined as 1.0 M 1-ethyl-3-methylimidazolium tetrafluoroborate with extraction time of 30 min and a solvent to solid ratio of 30 mL/g. Ultrafiltration with liquid chromatography and mass spectrometry was applied to screen and identify α-glucosidase inhibitors from B. chinensis, followed by the application of semipreparative high-performance liquid chromatography to separate and isolate the active constituents. Four major compounds including tectorigenin, iristectorigenin A, irigenin, and irisflorentin were screened and identified as α-glucosidase inhibitors, and then the four active compounds abovementioned were subsequently isolated by semipreparative high-performance liquid chromatography (99.89, 88.97, 99.79, and 99.97% purity, respectively). The results demonstrate that ionic liquid extraction can be successfully applied to the extraction of isoflavones from B. chinensis.
Asunto(s)
Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Iridaceae/química , Isoflavonas/aislamiento & purificación , Cromatografía Líquida de Alta Presión , UltrafiltraciónRESUMEN
Stroke represents the fourth leading cause of death in the USA and the second leading cause of death worldwide. Lactate dehydrogenase inhibitors are widely used in the treatment of ischemic stroke and natural products are considered a promising source of novel lactate dehydrogenase inhibitors. In this study, we used PC12 cells to determine the protective effect of extracts from the herb Belamcanda chinensis following toxic challenge. Using ultrafiltration high-performance liquid chromatography coupled with photo-diode array detection and electrospray ionization mass spectrometry, we screened and identified isoflavonoids from Belamcanda chinensis extracts. Semi-preparative high-performance liquid chromatography was then applied to separate and isolate the active constituents. Using these methods, we identified six major compounds in Belamcanda chinensis as lactate dehydrogenase inhibitors: tectoridin, iristectorin A, iridin, tectorigenin, irigenin, and irisflorentin, which were then isolated to >92% purity. This is the first report that Belamcanda chinensis extracts contain potent lactate dehydrogenase inhibitors. Our results demonstrate that the systematic isolation of bioactive components from Belamcanda chinensis guided by ultrafiltration high-performance liquid chromatography coupled with photo-diode array detection and electrospray ionization mass spectrometry represents a feasible and efficient technique that could be extended for the identification and isolation of other enzyme inhibitors.
Asunto(s)
Inhibidores Enzimáticos/aislamiento & purificación , Iridaceae/química , L-Lactato Deshidrogenasa/antagonistas & inhibidores , Fitoquímicos/aislamiento & purificación , Animales , Isquemia Encefálica , Cromatografía Líquida de Alta Presión , Cromatografía Liquida , Células PC12 , Extractos Vegetales/química , Ratas , Espectrometría de Masa por Ionización de Electrospray , Accidente Cerebrovascular , Espectrometría de Masas en Tándem , UltrafiltraciónRESUMEN
CONTEXT: Cipura paludosa Aubl. (Iridaceae) is widely used in folk medicine to treat several ailments. Experimental studies have confirmed its anti-inflammatory, antinociceptive, and neuroprotective effects. OBJECTIVE: This study evaluates the possible antiproliferative potential of the crude methanol extract and three isolated compounds from the bulbs of C. paludosa. MATERIALS AND METHODS: Phytochemical analysis was carried out by conventional chromatographic techniques, and the resulting compounds were identified by NMR (1)H and (13)C. The antiproliferative activity was analysed using the sulforhodamine B assay. RESULTS: Crude methanol extract of C. paludosa bulbs showed GI50 values of between 1.6 and 30.8 µg/mL. The naphthoquinone derivatives (eleutherine, isoeleutherine, and eleutherol) isolated from the bulbs of C. paludosa exhibited promising cytotoxicity against several human tumour cell lines, especially the two main compounds, eleutherine and isoeleutherine, against glioma and breast cancer cell lines, with TGI values of between 2.6 and 13.8 µg/mL. CONCLUSION: Cipura paludosa bulbs produce active principles with relevant antiproliferative potential, such as naphthoquinone derivatives, identified as eleutherine, isoeleutherine, and eleutherol. This is the first report indicating C. paludosa with antiproliferative potential.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Proliferación Celular/efectos de los fármacos , Iridaceae/química , Naftoquinonas/farmacología , Extractos Vegetales/farmacología , Raíces de Plantas/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Furanos/aislamiento & purificación , Furanos/farmacología , Humanos , Concentración 50 Inhibidora , Medicina Tradicional , Estructura Molecular , Naftoquinonas/aislamiento & purificación , Extractos Vegetales/aislamiento & purificaciónRESUMEN
BACKGROUND: Bacterial resistance to antibiotics is becoming a serious problem worldwide. The discovery of new and effective antimicrobials and/or resistance modulators is necessary to tackle the spread of resistance or to reverse the multi-drug resistance. We investigated the antibacterial and antibiotic-resistance modifying activities of the methanol extracts from Allanblackia gabonensis, Gladiolus quartinianus and Combretum molle against 29 Gram-negative bacteria including multi-drug resistant (MDR) phenotypes. METHODS: The broth microdilution method was used to determine the minimal inhibitory concentrations (MIC) and minimal bactericidal concentrations (MBC) of the samples meanwhile the standard phytochemical methods were used for the preliminary phytochemical screening of the plant extracts. RESULTS: Phytochemical analysis showed the presence of alkaloids, flavonoids, phenols and tannins in all studied extracts. Other chemical classes of secondary metabolites were selectively presents. Extracts from A. gabonensis and C. molle displayed a broad spectrum of activity with MICs varying from 16 to 1024 µg/mL against about 72.41% of the tested bacteria. The extract from the fruits of A. gabonensis had the best activity, with MIC values below 100 µg/mL on 37.9% of tested bacteria. Percentages of antibiotic-modulating effects ranging from 67 to 100% were observed against tested MDR bacteria when combining the leaves extract from C. molle (at MIC/2 and MIC/4) with chloramphenicol, kanamycin, streptomycin and tetracycline. CONCLUSION: The overall results of the present study provide information for the possible use of the studied plant, especially Allanblackia gabonensis and Combretum molle in the control of Gram-negative bacterial infections including MDR species as antibacterials as well as resistance modulators.
Asunto(s)
Antibacterianos/farmacología , Clusiaceae/química , Combretum/química , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Iridaceae/química , Extractos Vegetales/farmacología , Pruebas de Sensibilidad MicrobianaRESUMEN
Six novel iridal-type triterpenoids with a previously unreported 3,6-dihydro-2H-pyran moiety, named spirioiridotectals A-F (1-6), were isolated from the ethanol extract of the rhizomes of Iris tectorum. Their structures were elucidated on the basis of extensive spectroscopic analysis. Furthermore, in in vitro bioactivity assays, compounds 1, 2, and 6 exhibited neuroprotective activities against serum-deprivation-induced PC12 cell damage.
Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Medicamentos Herbarios Chinos/aislamiento & purificación , Medicamentos Herbarios Chinos/farmacología , Iridaceae/química , Fármacos Neuroprotectores/aislamiento & purificación , Fármacos Neuroprotectores/farmacología , Triterpenos/aislamiento & purificación , Triterpenos/farmacología , Animales , Antineoplásicos Fitogénicos/química , Medicamentos Herbarios Chinos/química , Estructura Molecular , Fármacos Neuroprotectores/química , Resonancia Magnética Nuclear Biomolecular , Células PC12 , Ratas , Rizoma/química , Triterpenos/químicaRESUMEN
The study is aimed to provide the theoretical basis for exploiting and utilization of salt-alkaline soil and cultivating Belamcanda chinensis. In this study, we exerted exogenous substances SNP, Spd to relieve the damage of the mixing salt-alkaline stress on B. chinensis seedling which is NaCl, Na2SO4, NaHCO3 and Na2CO3 four kinds of salt molar ratio of 9: 1: 9: 1, salt concentration of 100 mmol x L(-1). The result illustrated that high pH stress is a major factor caused the salt-alkaline stress, the interaction between time and the concentration of each, treatment was observed, what is more, there are synergies between the salt and alkali stress. The content of B. chinensis seedling leaves' membrane peroxidation index (MDA, O2-*) and metabolites (soluble protein, soluble sugars, organic acids) are showing an upward trend in varying degrees under 100 mmol x L(-1) salt-alkaline stress. It is effective to reduce the content of MDA and O2-*. and improve the levels of metabolites, in which the SNP (0.05 mmol x L(-1)) and Spd (0.5 mmol x L(-1)) to alleviate damage effects is the best. Therefore we can hold the conclusion that SNP and Spd can effectively mitigate the damage of B. chinensis seedling on salt-alkaline stress, improve the resistance ability of B. chinensis seedling which can provide the scientific basis for the utilization of salt-alkaline soil, and the cultivation of B. chinensis.
Asunto(s)
Álcalis/metabolismo , Iridaceae/fisiología , Óxido Nítrico/farmacología , Cloruro de Sodio/metabolismo , Iridaceae/química , Iridaceae/efectos de los fármacos , Iridaceae/crecimiento & desarrollo , Hojas de la Planta/química , Hojas de la Planta/efectos de los fármacos , Hojas de la Planta/crecimiento & desarrollo , Hojas de la Planta/fisiología , Plantones/química , Plantones/efectos de los fármacos , Plantones/crecimiento & desarrollo , Plantones/fisiologíaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Belamcanda chinensis (L.) Redouté is widely distributed in East Asia, such as China, Russia and North Korea. Belamcandae Rhizoma is the sun-dried rhizome of B. chinensis and has a long history of traditional medicinal use. It was first recorded in the Shennong's Herbal Classic, and has the effects of clearing heat and detoxifying, eliminating phlegm and benefiting the pharynx. AIM OF THE STUDY: To systematically study the source of Belamcandae Rhizoma, summarize the evolution of its medicinal properties, efficacy and the application history of its prescriptions, summarize its biological activity, phytochemistry, synthetic metabolic pathway and toxicology, and screen the Quality-Markers of Belamcandae Rhizoma according to the screening principle of traditional Chinese medicine Quality-Markers. MATERIALS AND METHODS: All information available on Belamcandae Rhizoma was collected using electronic search engines, such as Pubmed, Web of Science, CNKI, WFO (www.worldfloraonline.org), MPNS (https://mpsn.kew.org), Changchun University of Traditional Chinese Medicine Library collections, Chinese Medical Classics. RESULTS: The source of Belamcandae Rhizoma is B. chinensis of Iridaceae. It has a long history of application in China. It has the effects of clearing heat and detoxifying, eliminating phlegm and promoting pharynx. Modern pharmacological studies have shown that it has anti-inflammatory, anti-oxidation, anti-tumor and other physiological activities, and is safe and non-toxic at normal application doses. At present, tectoridin, iridin, tectorigenin, irigenin and irisflorentin are identified as the Quality-Markers of Belamcandae Rhizoma. CONCLUSIONS: As a traditional Chinese medicine, Belamcandae Rhizoma has a long history of application, and multifaceted studies have demonstrated that Belamcandae Rhizoma is a promising Chinese medicine with good application prospects. By reviewing and identifying the Quality-Markers of Belamcandae Rhizoma, this study can help to establish the evaluation procedure of it on the one hand, and identify the shortcomings research on the other hand. Currently, there are few studies on the anabolism and toxicology of it, and future studies may focus on its in vivo processes, toxicology and adverse effects.