Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 20 de 46
Filter
1.
Acta amaz ; 49(4): 257-267, out. - dez. 2019.
Article in English | LILACS | ID: biblio-1118924

ABSTRACT

Brazil nut is a very important nontimber forest product in the Amazon region. Propagation of this tree still represents a challenge due to slow and uneven seed germination. In this context, plant growth-promoting bacteria can facilitate the process of propagation. The aims of this study were to isolate and characterize endophytic bacteria from the roots of Brazil nut trees in native terra firme forest and cultivation areas in northern Brazil, and to identify mechanisms by which bacteria act in plant growth promotion. Overall, 90 bacterial isolates were obtained from the roots of Brazil nut trees in monoculture, agroforestry and native forest areas by using different semisolid media. The isolates were characterized by sequencing the 16S rRNA gene. Plant growth-promoting characteristics were evaluated by the presence of the nifH gene, aluminum phosphate solubilization and the production of indole compounds. The isolates were affiliated with 18 genera belonging to 5 different classes (α-Proteobacteria, ß-Proteobacteria, γ-Proteobacteria, Bacilli and Actinobacteria). The genus Bacillus was predominant in the forest and monoculture areas. Fourteen isolates presented the nifH gene. Most of the bacteria were able to solubilize aluminum phosphate and synthetize indole compounds. The results indicated high diversity of endophytic bacteria present among the roots of Brazil nut trees, mainly in the agroforestry area, which could be related to soil attributes. Among the 90 isolates, the 22 that presented the best results regarding plant growth promotion traits were good candidates for testing in seedling production of Brazil nut trees. (AU)


Subject(s)
RNA, Ribosomal, 16S , Amazonian Ecosystem , Indole Alkaloids , Bertholletia , Nitrogen Fixation
2.
Bol. latinoam. Caribe plantas med. aromát ; 18(5): 527-532, sept. 2019. ilus, tab
Article in English | LILACS | ID: biblio-1008292

ABSTRACT

Chemical constituents and biological activities of the aerial parts of Piper erecticaule C.DC. have been studied for the first time. Fractionation and purification of the extracts afforded aristolactam AII (1), aristolactam BII (2), piperolactam A (3), piperolactam C (4), piperolactam D (5), together with terpenoids of ß-sitosterol, ß-sitostenone, taraxerol, and lupeol. The structures of these compounds were obtained by analysis of their spectroscopic data, as well as the comparison with that of reported data. Acetylcholinesterase inhibitory activity revealed that compounds 1 and 3 showed strong AChE inhibitory effects with the percentage inhibition of 75.8% and 74.8%, respectively.


Se estudiaron por primera vez los constituyentes químicos y actividad biológica de las partes aéreas de Piper erecticaule C.DC. El fraccionamiento y la purificación de los extractos proporcionaron aristolactama AII (1), aristolactama BII (2), piperolactama A (3), piperolactama C (4), piperolactama D (5), junto con terpenoides de ß-sitosterol, ß-sitostenona, taraxerol, y el lupeol. Las estructuras de estos compuestos se obtuvieron mediante el análisis de sus datos espectroscópicos, así como mediante la comparación con datos ya informados. La actividad inhibidora de la acetilcolinesterasa reveló que los compuestos 1 y 3 mostraron un potente efecto inhibidor de la AChE con un porcentaje de inhibición del 75.8% y 74.8%, respectivamente.


Subject(s)
Aporphines/pharmacology , Acetylcholinesterase/drug effects , Plant Extracts/chemistry , Cholinesterase Inhibitors/pharmacology , Piper/chemistry , Alkaloids/pharmacology , Aporphines/chemistry , Terpenes/isolation & purification , Cholinesterase Inhibitors/chemistry , Indole Alkaloids/chemistry , Alkaloids/chemistry , Lactams/chemistry
3.
Article in Chinese | WPRIM | ID: wpr-776537

ABSTRACT

OBJECTIVE@#To investigate the effects of rutaecarpine on high glucose-induced Alzheimer's disease-like pathological and cognitive dysfunction and its mechanism in rats.@*METHODS@#Adult male SD rats were randomly divided into three groups (n=20): control group, high glucose group and rutaecarpine group. Rats in the control group were fed with conventional feed and tap water. The rats in the high glucose group were fed with conventional feed and 20% sucrose water. The rutaecarpine group was fed with fodder contain 0.01% rutaecarpine and 20% sucrose water. Morris water maze test was used to detect learning and memory and cognitive function of three groups rats after 24 weeks of feeding. Western blot analysis was used to detect tau protein at Thr205 and Ser214 sites in each group. Phosphorylation levels of GSK-3β in serine 9 site (S9-GSK-3β) and PP2A at cycline 307 site (Y307-PP2AC) were also detected. Immunohistochemistry further confirmed tau protein at Thr205 site in each group both in hippocampus and cortex.@*RESULTS@#Compared with the control group, Morris water maze results showed that the latency of finding the hidden platform of the rats in high glucose group was increased significantly and the number of crossing platforms and the target quadrant residence time were significantly decreased (all P<0.05). Immunohistochemistry showed that the phosphorylation level of tau protein at Thr205 site was significantly increased in the high glucose group compared with the control group, and the phosphorylation level of tau protein at Thr205 site in the rutaecarpine group was higher than that in the high glucose group. Western blot analysis showed that the phosphorylation level of tau protein in the high glucose group was significantly increased at Thr205 and Ser214 site compared with the control group, but the phosphorylation level of pS9-GSK-3β was significantly decreased (all P <0.05). Compared with the high glucose group, the latency of finding the hidden platform of the rats in rutaecarpine group was significantly decreased, and the number of crossing platforms and the target quadrant residence time were significantly increased (both P<0.05). Compared with the high glucose group, the phosphorylation levels of tau protein at Thr205 and Ser214 sites showed a significant decrease, but the phosphorylation level of pS9-GSK-3β was significantly increased (all P<0.05).@*CONCLUSION@#Rutaecarpine can alleviate AD-like cognitive dysfunction induced by high glucose, possibly by enhancing pS9-GSK-3β phosphorylation, down-regulating GSK-3β activity, and thus reducing hyperphosphorylation of tau-associated sites.


Subject(s)
Alzheimer Disease , Drug Therapy , Animals , Cognitive Dysfunction , Drug Therapy , Glucose , Glycogen Synthase Kinase 3 beta , Chemistry , Indole Alkaloids , Pharmacology , Male , Maze Learning , Phosphorylation , Quinazolines , Pharmacology , Random Allocation , Rats , Rats, Sprague-Dawley , tau Proteins , Chemistry
4.
Article in Chinese | WPRIM | ID: wpr-777507

ABSTRACT

Uncaria genus( Rubiaceae) contains 34 species all over the world,of which 11 species and one variant are present in China. Five species,namely U. rhynchophylla,U. macrophylla,U. hirsuta,U. sinensis and U. sessilifructus,are documented in Chinese Pharmacopoeia as the raw materials of Uncariae Ramulus Cum Uncis. Indole alkaloids are the characteristic constituents of Uncaria plants,in addition to triterpenes,lignans and flavones. This paper reviews the progress of indole alkaloids and their distribution within the five Uncaria species documented in Chinese Pharmacopoeia for better understanding the active constituents of Uncariae Ramulus Cum Uncis.


Subject(s)
Alkaloids , China , Drugs, Chinese Herbal , Indole Alkaloids , Medicine, Chinese Traditional , Uncaria
5.
Article in English | WPRIM | ID: wpr-691364

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect and potential mechanisms of rutaecarpine (Rut) in a rat artery balloon-injury model.</p><p><b>METHODS</b>The intimal hyperplasia model was established by rubbing the endothelia with a balloon catheter in the common carotid artery (CCA) of rats. Fifty rats were randomly divided into five groups, ie. sham, model, Rut (25, 50 and 75 mg/kg) with 10 rats of each group. The rats were treated with or without Rut (25, 50, 75 mg/kg) by intragastric administration for 14 consecutive days following injury. The morphological changes of the intima were evaluated by hematoxylin-eosin staining. The expressions of proliferating cell nuclear antigen (PCNA) and smooth muscle (SM) α-actin in the ateries were assayed by immunohistochemical staining. The mRNA expressions of c-myc, extracellular signal-regulated kinase 2 (ERK2), MAPK phosphatase-1 (MKP-1) and endothelial nitric oxide synthase (eNOS) were determined by real-time reverse transcription-polymerase chain reaction. The protein expressions of MKP-1 and phosphorylated ERK2 (p-ERK2) were examined by Western blotting. The plasma contents of nitric oxide (NO) and cyclic guanosine 3',5'-monophosphate (cGMP) were also determined.</p><p><b>RESULTS</b>Compared with the model group, Rut treatment significantly decreased intimal thickening and ameliorated endothelial injury (P<0.05 or P<0.01). The positive expression rate of PCNA was decreased, while the expression rate of SM α-actin obviously increased in the vascular wall after Rut (50 and 75 mg/kg) administration (P<0.05 or P<0.01). Furthermore, the mRNA expressions of c-myc, ERK2 and PCNA were downregulated while the expressions of eNOS and MKP-1 were upregulated (P<0.05 or P<0.01). The protein expressions of MKP-1 and the phosphorylation of ERK2 were upregulated and downregulated after Rut (50 and 75 mg/kg) administration (P<0.05 or P<0.01), respectively. In addition, Rut dramatically reversed balloon injury-induced decrease of NO and cGMP in the plasma (P<0.05 or P<0.01).</p><p><b>CONCLUSION</b>Rut could inhibit the balloon injury-induced carotid intimal hyperplasia in rats, possibly mediated by promotion of NO production and inhibiting ERK2 signal transduction pathways.</p>


Subject(s)
Actins , Metabolism , Animals , Carotid Arteries , Metabolism , Pathology , Carotid Artery Injuries , Drug Therapy , Genetics , Pathology , Cyclic GMP , Blood , Disease Models, Animal , Gene Expression Regulation , Hyperplasia , Indole Alkaloids , Pharmacology , Therapeutic Uses , Male , Nitric Oxide , Blood , Phosphorylation , Proliferating Cell Nuclear Antigen , Metabolism , Quinazolines , Pharmacology , Therapeutic Uses , RNA, Messenger , Genetics , Metabolism , Rats, Sprague-Dawley , Tunica Intima , Pathology
6.
Braz. j. microbiol ; 48(3): 410-418, July-Sept. 2017. tab, graf
Article in English | LILACS | ID: biblio-889127

ABSTRACT

Abstract Chaetoglobosin A is an antibacterial compound produced by Chaetomium globosum, with potential application as a biopesticide and cancer treatment drug. The aim of this study was to evaluate the feasibility of utilizing cornstalks to produce chaetoglobosin A by C. globosum W7 in solid-batch fermentation and to determine an optimal method for purification of the products. The output of chaetoglobosin A from the cornstalks was 0.34 mg/g, and its content in the crude extract was 4.80%. Purification conditions were optimized to increase the content of chaetoglobosin A in the crude extract, including the extract solvent, temperature, and pH value. The optimum process conditions were found to be acetone as the extractant, under room temperature, and at a pH value of 13. Under these conditions, a production process of the antifungal chaetoglobosin A was established, and the content reached 19.17%. Through further verification, cornstalks could replace crops for the production of chaetoglobosin A using this new production process. Moreover, the purified products showed great inhibition against Rhizoctonia solani, with chaetoglobosin A confirmed as the main effective constituent (IC50 = 3.88 µg/mL). Collectively, these results demonstrate the feasibility of using cornstalks to synthesize chaetoglobosin A and that the production process established in this study was effective.


Subject(s)
Industrial Microbiology/methods , Callosities/microbiology , Chaetomium/metabolism , Indole Alkaloids/metabolism , Antifungal Agents/metabolism , Waste Products/analysis , Industrial Microbiology/instrumentation , Callosities/metabolism , Molecular Structure , Plant Stems/metabolism , Plant Stems/microbiology , Indole Alkaloids/isolation & purification , Indole Alkaloids/chemistry , Antifungal Agents/isolation & purification , Antifungal Agents/chemistry
7.
Acta Physiologica Sinica ; (6): 249-254, 2016.
Article in Chinese | WPRIM | ID: wpr-331659

ABSTRACT

The aim of this study was to investigate the relationship between the acetylcholine concentration in the blood and gelsenicine-induced death in mice. Kunming mice were given intraperitoneal injections of normal saline, gelsenicine or different doses of acetylcholine chloride. Atropine was given to the mice which received gelsenicine or medium dose acetylcholine chloride injection. The blood was sampled immediately when the mice died or survived for 20 min after injection. The acetylcholine concentration and acetylcholinesterase activity in the blood were measured by the testing kits, and the mortality was calculated and analyzed. The results showed that half lethal dose of gelsenicine (0.15 mg/kg) reduced the acetylcholinesterase activity and increased the blood acetylcholine concentration. The blood acetylcholine concentration of the dead mice in the gelsenicine group was increased to 43.0 μg/mL (from 31.1 μg/mL in the control), which was lower than that (53.9 μg/mL) of the dead mice in the medium dose acetylcholine chloride group, but almost equal to that (42.7 μg/mL) of the survival mice in the medium dose acetylcholine chloride group. Atropine could successfully rescue the mice from acetylcholine poisoning, but its efficiency of rescuing the mice from gelsenicine intoxication was weak. These results suggest that gelsenicine can inhibit acetylcholinesterase activity and increase blood acetylcholine concentration, but the accumulation of acetylcholine may not be the only or main cause of the death induced by gelsenicine in mice.


Subject(s)
Acetylcholine , Animals , Death , Indole Alkaloids , Mice
8.
Natural Product Sciences ; : 278-281, 2015.
Article in English | WPRIM | ID: wpr-7746

ABSTRACT

Chemical investigation on a colonial marine tunicate, Didemnum sp. led to the isolation of a series of indole alkaloids including a new (1) and two known metabolites (2-3). Based on the spectroscopic analysis including 1D and 2D NMR along with MS spectra, the structure of 1 (16-epi-18-acetyl herdmanine D) was elucidated as a new amino acid derivative. The absolute configuration of 1 was determined by comparison of specific rotation with the known compound. The structures of compounds 2 and 3 were also identified as bromoindole containing compounds N-(6-bromo-1H-indole-3-carbonyl)-L-arginine and (6-bromo-1H-indol-3-yl) oxoacetamide, respectively, based on 1H and 13C NMR data, MS data and specific rotation value. Their pharmacological potentials as antibacterial agents and FXR antagonists were investigated, but no significant activity was found. However, the structural similarity of compound 1 to compound 4 suggested the antiinflammatory potential of compound 1.


Subject(s)
Anti-Bacterial Agents , Indole Alkaloids , Urochordata
9.
Article in English | WPRIM | ID: wpr-812509

ABSTRACT

The ocean continues to provide a plethora of unique scaffolds capable of remarkable biological applications. A large number of pyrroloiminoquinone alkaloids, including discorhabdins, epinardins, batzellines, makaluvamines, and veiutamine, have been isolated from various marine organisms. A class of pyrroloiminoquinone-related alkaloids, known as bispyrroloquinones, is the focus of this review article. This family of marine alkaloids, which contain an aryl substituted bispyrroloquinone ring system, includes three subclasses of alkaloids namely, wakayin, tsitsikammamines A-B, and zyzzyanones A-D. Both wakayin and the tsitsikammamines contain a tetracyclic fused bispyrroloiminoquinone ring system, while zyzzyanones contain a fused tricyclic bispyrroloquinone ring system. The unique chemical structures of these marine natural products and their diverse biological properties, including antifungal and antimicrobial activity, as well as the potent, albeit generally nonspecific and universal cytotoxicities, have attracted great interest of synthetic chemists over the past three decades. Tsitsikammamines, wakayin, and several of their analogs show inhibition of topoisomerases. One additional possible mechanism of anticancer activity of tsitsikammamines analogs that has been discovered recently is through the inhibition of indoleamine 2, 3-dioxygenase, an enzyme involved in tumoral immune resistance. This review discusses the isolation, synthesis, and evaluation of bioactivities of bispyrroloquinone alkaloids and their analogs.


Subject(s)
Alkaloids , Chemistry , Pharmacology , Animals , Anti-Infective Agents , Chemistry , Pharmacology , Antineoplastic Agents , Chemistry , Pharmacology , Biological Products , Chemistry , Pharmacology , Humans , Indole Alkaloids , Chemistry , Pharmacology , Indoles , Chemistry , Pharmacology , Pyrroles , Chemistry , Pharmacology , Quinolines , Chemistry , Pharmacology , Quinones , Chemistry , Pharmacology
10.
Pesqui. vet. bras ; 34(9): 837-844, set. 2014. ilus, tab
Article in Portuguese | LILACS | ID: lil-728820

ABSTRACT

Amorimia exotropica é um arbusto escandente que pertence à família Malpighiacea, cujo princípio tóxico é o monofluoracetato de sódio e possui ação cardiotóxica em bovinos. Ela é a única representante, na região Sul do país, do grupo de plantas que causam morte súbita associada ao exercício. Este trabalho identificou e mapeou as lesões cardíacas observadas em bovinos intoxicados naturalmente por A. exotropica. Selecionaram-se nove corações bovinos, provenientes de um surto de intoxicação natural pela planta em uma propriedade de gado de corte do Rio Grande do Sul e procedeu-se o mapeamento de oito regiões topográficas distintas (ápice, ventrículos direito e esquerdo, septo interventricular, músculos papilares direito e esquerdo e átrios direito e esquerdo). À avaliação macroscópica quatro bovinos apresentaram lesão focal e bem delimitada no músculo papilar esquerdo. Estas áreas na histologia correspondiam à necrose de coagulação em diferentes estágios de evolução, similares a infartos. Todos os bovinos apresentavam necrose de cardiomiócitos, caracterizadas por retração e hipereosinofilia citoplasmática e fragmentação celular em todas as áreas amostradas. A severidade da injúria celular foi avaliada pela imuno-histoquímica anti-troponina C, a qual demonstrou acentuada perda e/ou diminuição de marcação citoplasmática em células necróticas. O músculo papilar esquerdo foi a região mais acometida nos casos de intoxicação por Amorimia exotropica...


Amorimia exotropica is a shrub of the Malpighiacea family that contains sodium monofluoroacetate as the toxic principle, which has a cardiotoxic action in cattle. In Southern Brazil it is the only species of the group of plants that causes "sudden death during exercise". This study has identified and mapped cardiac lesions observed in cattle naturally poisoned by A. exotropica. An outbreak of poisoning by the plant occurred in a beef cattle herd in Rio Grande do Sul, where nine bovine hearts were selected for examination and mapping of eight distinct topographical regions (apex, right and left ventricles, interventricular septum, right and left papillary muscles , right and left atrium). At gross examination, four cattle showed focal and well-defined lesions in the left papillary muscle. This corresponds to areas of coagulation necrosis in different stages of evolution on histology, similar to infarcts. All hearts showed cardiomyocytes necrosis, characterized by shrinkage and hypereosinophilic cytoplasm and cellular fragmentation in all sampled areas. The severity of cellular injury was evaluated by immunohistochemistry anti-troponin C, which showed marked decrease of cytoplasm staining in necrotic cells. The left papillary muscle was the most affected region in cases of poisoning by A. exotropica...


Subject(s)
Animals , Cattle , Cattle , Cardiovascular Diseases/veterinary , Plant Poisoning/veterinary , Malpighiaceae/poisoning , Myocytes, Cardiac , Troponin/analysis , Indole Alkaloids/poisoning , Toxicological Symptoms/poisoning
11.
Article in Chinese | WPRIM | ID: wpr-243473

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the protective effects of rutaecarpine (Rut) on right ventricular remodeling in rats with monocrotaline-induced pulmonary hypertension (PH).</p><p><b>METHOD</b>Forty-eight SD rats were fed adaptively for 1 week and then were randomly divided into the following 4 groups (n = 12): normal control group, monocrotaline (MCT) treatment group, MCT treatment with Rut (20 mg/kg)group and MCT treatment with Rut (40 mg/kg) group. PH rats were induced by a single injection of monocrotaline (60 mg/kg, sc) and were administered with Rut (20 or 40 mg/kg/d) for 4 weeks. At the end of experiment, the right ventricular systolic pressure (RVSP) and mean pulmonary artery pressure (mPAP) were monitored via the right jugular vein catheterization into the right ventricle. The ratio of right ventricle (RV) to left ventricle (LV) + septum (S) and the ratio of RV to tibial length were calculated. Right ventricular morphological changes were deserved by HE staining. Masson's trichrome staining was used to display collagen deposition. The total antioxidative capacity (T-AOC) and malondialdehyde (MDA) levels in right ventricle were determined according to the manufacturer's instructions. mRNA and protein expression levels of NOX4, collagen I and collagen III were analyzed by immunohistochemisty, real-time PCR and Western blot.</p><p><b>RESULTS</b>The results showed that Rut treatment for 4 weeks attenuated RVSP, mPAP and right ventricular remodeling index (RV/LV + S and RV/Tibial length) of PH rats induced by monocrotaline. Furthermore, the right ventricular collagen deposition and collagen I and collagen I expression induced by MCT were both significantly suppressed by Rut. The expression levels of NOX4 and MDA were obviously decreased, while the T-AOC was significantly increased in right ventricular from PH rats treated with Rut.</p><p><b>CONCLUSION</b>These results suggested that Rut ameliorates the right ventricular remodeling in rats with PH induced by MCT through down-regulating of NOX4 expression and collagen accumulation.</p>


Subject(s)
Animals , Antioxidants , Metabolism , Heart Ventricles , Metabolism , Hypertension, Pulmonary , Drug Therapy , Indole Alkaloids , Pharmacology , Male , Malondialdehyde , Metabolism , Monocrotaline , NADPH Oxidase 4 , NADPH Oxidases , Metabolism , Quinazolines , Pharmacology , Rats , Ventricular Remodeling
12.
Acta Pharmaceutica Sinica ; (12): 849-853, 2014.
Article in Chinese | WPRIM | ID: wpr-245004

ABSTRACT

Hypoxia is a general characteristic of most solid malignancies and intimately related to cancer progression. Homeostatic response to hypoxia is primarily mediated by hypoxia inducible factor-1alpha (HIF-1alpha) that elicits transcriptional activity through recruitment P300 coactivator. Targeting the interaction of HIF- alpha and P300 would thus constitute a novel approach for cancer treatment by suppressing tumor angiogenesis and metastasis. Here, a screening assay was developed for inhibitors targeting the interaction between HIF-1alpha and P300. The nucleotide sequence of human HIF-1alpha and P300 were cloned into pBIND and pACT vectors, named pBIND-HIF1alpha and pACT-P300. The interaction of HIF-1alpha and P300 was identified in HEK293 cell using mammalian two-hybrid system. And compound chetomin decreased their interaction in this mammalian two-hybrid system. We further verified HIF-1 inhibition effect of chetomin in U251-HRE cells. Therefore, we established a screening assay combined HIF-1alpha and P300 mammalian two-hybrid system and U251-HRE reporter assay for HIF-1 selective inhibitors.


Subject(s)
Cell Hypoxia , Disulfides , Pharmacology , Drug Screening Assays, Antitumor , E1A-Associated p300 Protein , HEK293 Cells , Humans , Hypoxia-Inducible Factor 1, alpha Subunit , Indole Alkaloids , Pharmacology , Two-Hybrid System Techniques
13.
Article in English | WPRIM | ID: wpr-293260

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate the effects and possible mechanisms of rutaecarpine on angiotensin II (Ang II)-induced proliferation in cultured rat vascular smooth muscle cells (VSMCs).</p><p><b>METHODS</b>VSMCs were isolated from Male Sprague-Dawley rat aorta, and cultured by enzymic dispersion method. Experiments were performed with cells from passages 3-8. The cultured VSMCs were randomly divided into control, model (Ang II 0.1 μmol/L), and rutaecarpine (0.3-3.0 μmol/L) groups. VMSC proliferation was induced by Ang II, and was evaluated by the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay and cell counting. To examine the mechanisms involved in anti-proliferative effects of rutaecarpine, nitric oxide (NO) levels and NO synthetase (NOS) activity were determined. Expressions of VSMC proliferation-related genes including endothelial nitric oxide synthase (eNOS), and c-myc hypertension related gene-1 (HRG-1) were determined by real-time reverse transcription-polymerase chain reaction (RT-PCR).</p><p><b>RESULTS</b>Rutaecarpine (0.3-3.0 μmol/L) inhibited Ang II-induced VSMC proliferation and the best effects were achieved at 3.0 μmol/L. The Ang II-induced decreases in cellular NO contents and NOS activities were antagonized by rutaecarpine (P <0.05). Ang II administration suppressed the expressions of eNOS and HRG-1, while increased c-myc expression (P <0.05). All these effects were attenuated by 3.0 μmol/L rutaecarpine (P <0.05).</p><p><b>CONCLUSION</b>Rutaecarpine is effective against Ang II-induced rat VSMC proliferation, and this effect is due, at least in part, to NO production and the modulation of VMSC proliferation-related gene expressions.</p>


Subject(s)
Angiotensin II , Pharmacology , Animals , Base Sequence , Cell Proliferation , Cells, Cultured , DNA Primers , Hemeproteins , Metabolism , Indole Alkaloids , Pharmacology , Male , Muscle, Smooth, Vascular , Cell Biology , Nitric Oxide Synthase Type III , Metabolism , Proto-Oncogene Proteins c-myc , Metabolism , Quinazolines , Pharmacology , Rats , Rats, Sprague-Dawley , Real-Time Polymerase Chain Reaction , Reverse Transcriptase Polymerase Chain Reaction
14.
Acta Pharmaceutica Sinica ; (12): 225-229, 2014.
Article in Chinese | WPRIM | ID: wpr-297989

ABSTRACT

Eight compounds were isolated from the stems of Brucea mollis by various chromatographic techniques such as column chromatography on silica gel and Sephadex LH-20, and preparative HPLC, and their structures were elucidated as bruceolline O (1), 1-(1-beta-glucopyranosyl)-1H-indole-3-carbaldehyde (2), canthin-6-one (3), 11-hydroxycanthin-6-one (4), 9-methoxycanthin-6-one (5), 4-methoxycanthin-6-one (6), infractin (7), and beta-carboline-1-propionic acid (8). The cytotoxic activities of compounds 1-8 against HCT-8 and A549 human cell lines were determined, but none of them exhibited significant activity (IC 50 > 10 micromol x L(-1)). Among them, compound 1 is a new indole alkaloid, and compounds 2 and 5-7 were isolated from this plant for the first time.


Subject(s)
Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Brucea , Chemistry , Carbolines , Chemistry , Pharmacology , Cell Line, Tumor , Humans , Indole Alkaloids , Chemistry , Pharmacology , Molecular Structure , Plant Stems , Chemistry , Plants, Medicinal , Chemistry
15.
Article in Chinese | WPRIM | ID: wpr-327865

ABSTRACT

It is now well established that inflammation plays an important role in the development of numerous chronic metabolic diseases including insulin resistance (IR) and type 2 diabetes (T2DM). Skeletal muscle is responsible for 75% of total insulin-dependent glucose uptake; consequently, skeletal muscle IR is considered to be the primary defect of systemic IR development. Our pre- vious study has shown that rutaecarpine (Rut) can benefit blood lipid profile, mitigate inflammation, and improve kidney, liver, pan- creas pathology status of T2DM rats. However, the effects of Rut on inflammatory cytokines in the development of IR-skeletal muscle cells have not been studied. Thus, our objective was to investigate effects of Rut on inflammatory cytokines interleukiri (IL)-1, IL-6 and tumor necrosis factor (TNF)-α in insulin resistant primary skeletal muscle cells (IR-PSMC). Primary cultures of skeletal muscle cells were prepared from 5 neonate SD rats, and the primary rat skeletal muscle cells were identified by cell morphology, effect of ru- taecarpine on cell proliferation by MTT assay. IR-PSMC cells were induced by palmitic acid (PA), the glucose concentration was measured by glucose oxidase and peroxidase (GOD-POD) method. The effects of Rut on inflammatory cytokines IL-1, IL-6 and TNF-α in IR-PSMC cells were tested by enzyme-linked immunosorbent assay (ELISA) kit. The results show that the primary skeletal muscle cells from neonatal rat cultured for 2-4 days, parallel alignment regularly, and cultured for 7 days, cells fused and myotube formed. It was shown that Rut in concentration 0-180. 0 μmol x L(-1) possessed no cytotoxic effect towards cultured primary skeletal muscle cells. However, after 24 h exposure to 0.6 mmol x L(-1) PA, primary skeletal muscle cells were able to induce a state of insulin resistance. The results obtained indicated significant decrease (P < 0.05 to P < 0.001) IL-1, IL-6 and TNF-α production by cultured IR-PSMC cells when incubating 24 hours with Rut, beginning from 20 to 180.0 μmol x L(-1). IL-1, IL-6 and TNF-α in the Rut treated groups were dose-dependently decreased compared with that in the IR-PSMC control group. Our results demonstrated that the Rut promoted glucose consumption and improved insulin resistance possibly through suppression of inflammatory cytokines in the IR-PSMC cells.


Subject(s)
Animals , Cell Proliferation , Cytokines , Metabolism , Female , Glucose , Metabolism , Indole Alkaloids , Pharmacology , Inflammation , Metabolism , Insulin Resistance , Male , Muscle, Skeletal , Cell Biology , Metabolism , Quinazolines , Pharmacology , Rats
16.
Article in Chinese | WPRIM | ID: wpr-300211

ABSTRACT

A RP-HPLC method was developed to evaluate the quality of Picrasmae Ramulus et Folium by simultaneous determination of five constituents including 1-hydroxymethyl-beta-carboline (1), 1-methoxicabony-beta-carboline (2), 4-methoxy-5-hydroxy-canthin-6-one (3), 4, 5-dimethoxy-canthin-6-one (4) and maackiain (5) in Picrasmae Ramulus et Folium. The samples were separated on a Kromasil RP-C18 (4.6 mm x 250 mm, 5 microm) column eluted with acetonitrile and 0.1% phosphoric acid as mobile phases in gradient mode. The detection wavelength was set at 254 nm. The calibration curves and linearity of the above five standards were determined as (1) Y = 6 525.6X + 37.25 (0.009-1.780 microg, r = 0.996 8), (2) Y = 3 662.3X + 41.55 (0.005-0.920 microg, r = 0.999 5), (3) Y = 3763.1X + 146.87 (0.015-3.060 microg, r = 0.999 0), (4) Y = 2 174.1X + 21.52 (0.003-0.620 microg, r = 0.999 5), and (5) Y = 276.25X + 7.65 (0.010-1.960 microg, r = 0.998 9), respectively. The method is simple and repeatable, and can be used for the quality assessment of Picrasmae Ramulus et Folium.


Subject(s)
Alkaloids , Calibration , Carbolines , Chromatography, High Pressure Liquid , Methods , Chromatography, Reverse-Phase , Methods , Flavonoids , Indole Alkaloids , Picrasma , Chemistry , Plant Leaves , Chemistry , Plant Stems , Chemistry , Pterocarpans , Reproducibility of Results
17.
Acta Pharmaceutica Sinica ; (12): 276-280, 2013.
Article in Chinese | WPRIM | ID: wpr-235672

ABSTRACT

In order to study the chemical constituents in the water extract of the stem of Nauclea officinalis, column chromatography over D101 macroporous resin and silica gel and an automatic purification system were used to isolate and purify the chemical constituents from the extract. Nine compounds were obtained. By analysis of the physicochemical properties and spectral data, their structures were identified as naucleamide G (1), 3, 4-dimethoxyphenol-beta-D-apiofuranosyl (1-->6)-beta-D-glucopyranoside (2), kelampayoside A (3), 3alpha, 5alpha-tetrahydrodeoxycordifoline lactam (4), naucleamide A-10-O-beta-D-glucopyranoside (5), pumiloside (6), 3-epi-pumiloside (7), strictosamide (8) and vincosamide (9), separately. Among them, compound 1 is a new compound, compound 2 was found in plants of the genus Nauclea for the first time, and compounds 3 and 4 were isolated from this plant for the first time.


Subject(s)
Camptothecin , Chemistry , Carbolines , Chemistry , Glucosides , Chemistry , Indole Alkaloids , Chemistry , Molecular Structure , Plant Stems , Chemistry , Plants, Medicinal , Chemistry , Rubiaceae , Chemistry , Vinca Alkaloids , Chemistry
18.
Acta Pharmaceutica Sinica ; (12): 315-324, 2013.
Article in Chinese | WPRIM | ID: wpr-235666

ABSTRACT

Polo-box domain 1 (PBD1) is a characteristic domain of polo-like kinase 1 (PLK1), which locates in C-terminal and can influence the catalytic activity and specific subcellular locations of PLK1. At present, most PLK1 inhibitors are developed to occupy the ATP pocket or its close sites. However, this kind of PLK1 inhibitors is difficult to pursue target selectivity and may encounter cross drug resistance with other kinase inhibitors due to the conserved sequence of ATP pocket. Recently, PBD1, with aberrant specificity in sequence and structure, has attracted enormous interests as the alternative target to the discovery of corresponding inhibitors for anti-tumor drugs. The structure and function of PBD1 as well as the advances of its inhibitors are reviewed in this paper.


Subject(s)
Benzocycloheptenes , Chemistry , Pharmacology , Benzoquinones , Chemistry , Pharmacology , Cell Cycle Proteins , Chemistry , Cell Line, Tumor , Cell Proliferation , Humans , Indole Alkaloids , Chemistry , Pharmacology , Lactams , Chemistry , Pharmacology , Peptides, Cyclic , Chemistry , Pharmacology , Phosphopeptides , Chemistry , Pharmacology , Protein-Serine-Threonine Kinases , Chemistry , Proto-Oncogene Proteins , Chemistry
19.
Article in Chinese | WPRIM | ID: wpr-350698

ABSTRACT

<p><b>OBJECTIVE</b>To explore an HPLC method for determination of rhnchophylline and isorhnchophylline in Uncaria rhnchophylla.</p><p><b>METHOD</b>An HPLC method has been developed for determination of rhnchophylline and isorhnchophylline. The transformation of rhnchophylline and isorhnchophylline after heating was also studied by HPLC-ESI-MS.</p><p><b>RESULT</b>Good linearities of rhynchophylline and isorhynchophylline were 0.064-5.100, 0.064-5.110 mg, respectively. The average recoveries were from 87.51% to 88.83% for rhynchophylline and from 107.9% to 113.9% for isorhynchophylline. The recoveries of rhynchophylline and isorhnchophylline reference solutions after extraction were 12.60% and 40.00% in the reflux extraction procedure, respectively. While in the ultrasonic extraction procedure, the average recoveries of rhynchophylline and isorhynchophylline was from 99.48% to 103.2% and from 97.00% to 99.59%, resepectively. The recoveries of rhynchophylline and isorhnchophylline reference solutions after extraction were 47.08% and 51.03%, respectively. The unqualified recovery could be elucidated by HPLC-ESI-MS analysis, indicating that trhynchophylline could be transformed mostly into isorhynchophylline and a little amount of unkown composition, while isorhynchophylline could be transformed into rhynchophylline isocorynoxeine, corynoxeine and 22-O-beta-D-glucopyranosyl isocorynoxeinic acid during the extraction procedure.</p><p><b>CONCLUSION</b>Ultrasonic extraction procedure was more sutble for HPLC determination of the content of rhynchophylline and isorhynchophylline in U. rhnchophylla, however, the recovery problems should be paid attention to when it comes to the determination.</p>


Subject(s)
Chromatography, High Pressure Liquid , Indole Alkaloids , Chemistry , Reproducibility of Results , Spectrometry, Mass, Electrospray Ionization , Ultrasonics , Uncaria , Chemistry
20.
Acta Pharmaceutica Sinica ; (12): 764-768, 2012.
Article in Chinese | WPRIM | ID: wpr-276247

ABSTRACT

The study on the Rauvolfia verticillata (Lour.) Baill., which belongs to Apocynaceae, was carried out to look for its chemical constituents and pharmacological activity. The isolation and purification were performed by chromatography on silica gel, Sephadex LH-20 and ODS (octadecyl silane) open column. The structures of obtained compounds were elucidated on the basis of physicochemical properties and spectral analysis. Three indole alkaloids and one acridone alkaloid were isolated from chloroform layer extract and identified as ajmalicine B (1), sandwicine (2), raunescine (3) and 7-hydroxynoracronycine (4) separately. Ajmalicine B (1) is a new compound belonging to indole alkaloid. Compound 4 as an acridone alkaloid was a new type compound isolated from Rauvolfia genus for the first time. We also did some biological activity research on the new type compound (4) to explore other pharmacological activities in addition to antihypertensive activity.


Subject(s)
Animals , Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Cell Proliferation , Drugs, Chinese Herbal , Chemistry , Pharmacology , HL-60 Cells , Humans , Indole Alkaloids , Chemistry , Pharmacology , Inhibitory Concentration 50 , Intestine, Small , Physiology , MCF-7 Cells , Molecular Structure , Muscle Relaxation , Muscle, Smooth , Physiology , Plant Roots , Chemistry , Plant Stems , Chemistry , Plants, Medicinal , Chemistry , Rabbits , Rauwolfia , Chemistry
SELECTION OF CITATIONS
SEARCH DETAIL