Glycogen synthase kinase-3 beta (GSK-3β) regulates glycogen metabolism and many different cellulars, including apoptosis, signaling, and neural. It is a crucial therapeutic receptor in heart disease, type 2 diabetes, and Alzheimer's. In this study, using computational methods, flavonoid compounds were investigated for potential inhibitors against GSK-3β. Virtual screening was utilized to investigate flavonoid compounds obtained from the PubChem database. Structure of human heart mitochondria of GSK-3β receptor constructed by homology modeling. Best binding poses were discovered via in silico molecular docking simulation. We surveyed noncovalent interactions among amino acid residues involved in the active site of the modeled Protein and compounds via molecular docking and molecular dynamics (MD). Moreover, ADMET characteristics of best docking conformers have been investigated. The obtained results revealed that compound 1 containing chromenone moiety with binding energy H-bond −11.4 kcal/mol inhibited effectively binding pocket of the GSK-3β receptor. Moreover, MD simulation analysis (RMSD and radius of gyration indicated complex of the compound and GSK-3β receptor remained stable throughout 100 ns MD simulation, and also analysis of ADMET profiles revealed that selected compounds had good drug-likeness and pharmacokinetic properties. Hence, it was suggested that compounds with chromenone scaffold could potentially inhibit GSK-3β. Structural modification of the chromenone derivatives may result in the discovery of promising candidates for identifying novel drugs as GSK-3β inhibitors.
American ginseng (Panax quinquefolius L.) has been cultivated in many locations in China, and we have noticed that its phenological performance and quality characteristics varied from location to location. However, the exogenous factors driving this process are still poorly understood, and this reduces the successful introduction of American ginseng for quality ensuring. Here, we conducted field and cabinet experiments to explore the relationship among environmental factors, phenological development, and ginsenoside accumulation in American ginseng. In the field experiments, we found that American ginseng from different original locations showed different phenological rhythms and different ginsenoside accumulation. Especially, those from higher latitude locations (e.g., Wuchang, 44.55°N) presented delayed spring phenology and advanced autumn phenology, but higher ginsenoside contents along with higher gene expression levels of ginsenoside biosynthesis than those from lower latitude locations (e.g., Wendeng, 37.23°N). Data analysis indicated that the phenological rhythm of American ginseng is closely related to the seasonal change in environmental factors, especially winter chilling duration, spring warming, and autumn day-length shortening. In the cabinet experiments, results further proved that temperature interaction with photoperiod plays a decisive role in the phenological development and ginsenoside accumulation of American ginseng in the absence of water and nutrient limitation. Both field and cabinet experiments indicated that sufficient winter cold exposure coupled with spring long day-length photoperiod is a beneficial environmental factor for normal spring phenology development, while shortening autumn day-length coupled with autumn cooling is a beneficial environmental factor for normal autumn phenology development of American ginseng. Results also indicated that insufficient cold exposure and unsuitable day-length photoperiod are detrimental factors to both spring and autumn phenology, and are not good for ginsenoside accumulation in American ginseng. An understanding of the environmental factors influencing phenological development along with ginsenoside accumulation can provide guidance for predicting suitable cultivation locations and improving planting techniques for high yield and good quality of American ginseng.
Background: Ginsenosides accumulation responses to temperature are critical to quality formation in cold-dependent American ginseng. However, the studies on cold requirement mechanism relevant to ginsenosides have been limited in this species. Methods: Two experiments were carried out: one was a multivariate linear regression analysis between the ginsenosides accumulation and the environmental conditions of American ginseng from different sites of China and the other was a synchronous determination of ginsenosides accumulation, overall DNA methylation, and relative gene expression in different tissues during different developmental stages of American ginseng after experiencing different cold exposure duration treatments. Results: Results showed that the variation of the contents as well as the yields of total and individual ginsenosides Rg1, Re, and Rb1 in the roots were closely associated with environmental temperature conditions which implied that the cold environment plays a decisive role in the ginsenoside accumulation of American ginseng. Further results showed that there is a cyclically reversible dynamism between methylation and demethylation of DNA in the perennial American ginseng in response to temperature seasonality. And sufficient cold exposure duration in winter caused sufficient DNA demethylation in tender leaves in early spring and then accompanied the high expression of flowering gene PqFT in flowering stages and ginsenosides biosynthesis gene PqDDS in green berry stages successively, and finally, maximum ginsenosides accumulation occurred in the roots of American ginseng. Conclusion: We, therefore, hypothesized that cold-induced DNA methylation changes might regulate relative gene expression involving both plant development and plant secondary metabolites in such cold-dependent perennial plant species. (C) 2019 The Korean Society of Ginseng. Publishing services by Elsevier B.V.
目的:系统评价新鲜土豆片外敷在防治化疗性静脉炎中的应用价值.方法:通过检索中国期刊全文数据库(CNKI)、维普中文科技期刊数据库(VIP)、万方数据库及中国生物医学文献数据库(CBM)从建库到2017年12月公开发表的应用新鲜土豆片外敷和50%硫酸镁常规湿敷防治化疗性静脉炎的随机对照研究,按纳入标准对文献进行资料提取和质量评价后,选用Cochrane协作网提供的RevMan 5.3软件进行Meta分析.结果:共纳入276篇关于化疗性静脉炎防治文献,共涉及临床病例964例.新鲜土豆片组(试验组)486例,50% 硫酸镁组(对照组)共478例.新鲜土豆片组防治化疗性静脉炎总有效率高于50% 硫酸镁组(P<0.05).结论:新鲜土豆片外敷能有效防治化疗性静脉炎,治疗效果优于50% 硫酸镁常规湿敷,在化疗性静脉炎预防与治疗方面具有应用价值.
Diabetes is one of the most concerned metabolic diseases worldwide and threaten public health. In the present work, two polysaccharide-rich extracts from Apocynum venetum leaves were extracted using distilled water and alkaline solution (0.05 M NaOH), and fully characterized. Hypoglycemic and hypolipidemic effects of two polysaccharide-rich extracts on high-fat diet and streptozocin-induced type 2 diabetic mice were investigated. Treatment of alkaline extracted polysaccharide-rich products significantly decreased the levels of fasting blood glucose, serum insulin, glycated serum protein, as well as serum lipids profiles including total cholesterol, triacylglycerols, low-density lipoprotein cholesterol, and nonesterified fatty acid. Meanwhile, the reduced glycogen contents in liver were prominently improved, and the oxidative damage were markedly ameliorated by alkaline extracted polysaccharide products in diabetic mice. Furthermore, both polysaccharide-rich extracts could reverse the gut microbiota dysbiosis in diabetic mice by increasing the abundance of genera Odoribacter, Anaeroplasma, Parasutterella, and Muribaculum; while by decreasing the abundance of genera Enterococcus, Klebsiella, and Aerococcus. This study provides new sights for exploitation of Apocynum venetum extracts as a promising anti-diabetic nutraceutical for the treatment of type 2 diabetes and metabolic syndrome.
目的 建立同时测定金羚感冒片中绿原酸、马钱苷和蒙花苷含量的高效液相色谱(HPLC)方法.方法 色谱柱为Inertsil ODS-SP(4.6 mm×250 mm,5μm);流动相为甲醇-0.6%冰醋酸溶液,梯度洗脱,柱温为30℃,流速为1.0 ml/min,检测波长为236 nm.结果 3种成分的峰面积与浓度呈的线性关系良好,加样回收率分别为102.1%,103.3%,102.4%,RSD均低于2.0%.结论 该方法简单、分离度好,可作为金羚感冒片的中绿原酸、马钱苷和蒙花苷的含量测定方法.
野生大豆在我国黄河三角洲地区种植面积较大,其含有丰富的氨基酸、矿物质元素等营养物质,还富有大豆异黄酮、皂苷、花青素、不饱和脂肪酸等功能成分,在食品及医药领域具有十分重要的应用前景.为了明确野生大豆中主要营养成分和生物活性因子的种类和具体功效,进一步促进野生大豆的开发利用,综述了野生大豆中各种营养成分和功能因子的研究进展,为野生大豆的合理开发利用提供一定的依据,并对其发展应用前景进行了展望.
Apocynum venetum has a long history as a Chinese traditional tea. As one of the major components, polysaccharides from Apocynum venetum leaves were extracted with acid (HCl), distilled water and alkaline (NaOH) to study the effect of the extraction solvents on their chemical composition and biological activities in this work. Monosaccharide composition revealed that polysaccharides from acidic and distilled water extraction were pectic polysaccharides, while those from alkaline extraction consisted of pectin and hemicellulose. Chemical analysis and FT-IR spectra indicated the co-extraction of protein and polyphenol contents in alkaline extracted polysaccharides, which exhibited strongest antioxidant and digestive enzyme inhibition activities. The antioxidant capacities were 185.26–286.30 mg TE/g for DPPH radical scavenging, 409.06–502.00 mg TE/g for ABTS radical scavenging, and 152.12–260.70 mg TE/g sample for reducing power assay, respectively. The lowest IC50 for α-glucosidase and lipase inhibition activities were 16.75 μg/mL and 820 μg/mL, respectively. Further purification of alkaline extracts was carried out and characterized. The results showed that acid hydrolysis could successfully reduce polyphenol and protein contents, and purified polysaccharides showed even higher antioxidant activities and α-glucosidase inhibition activity. These results provide a scientific support for functional application and extraction of polysaccharides from Apocynum venetum leaves.
目的:研究水分和肥料因素对远志皂苷积累的效应,为远志的栽培技术提供参考.方法:采用盆栽试验,设置一系列水分和肥料处理,取材测定远志根皮的细叶远志皂苷含量及产量.结果:(1)适当灌溉促进远志根皮增产但水分过多却显著降低其皂苷含量,其中70%的土壤持水量处理条件下细叶远志皂苷单株产量最高;(2)氮、磷、钾肥均对远志根皮有增产效应,也都促进根皮中皂苷的积累,但三者对细叶远志皂苷单株产量的贡献率不同,表现为:磷量>氮量>钾量,磷肥在远志药材的品质形成中起重要作用.结论:控制适量的灌溉水分和合理施肥有助于兼顾远志药材的产量和质量.
Objective To investigate the chemical constituents from the ethanol extract of Ulva pertusa.Methods The compounds were isolated and purified by chromatography on silica gel,ODS,Diaion HP-20,Sephadex LH-20,and preparative HPLC methods.Their structures were elucidated on the basis of spectral data.Results Eighteen compounds were isolated and identified as isophitol (1),indole-3-carboxylic acid (2),1-O-palmitoyl-3-O-(6'-sulfo-α-D-quinovopyranosyl) glycerol (3),(2S)-l-O-palmitoyl-3-O-[α-D-galactopyranosyl-(1→2)-β-D-galactopyranosyl] glycerol (4),3-methylsulfoxypropionic acid (5),3-chloropropionic acid (6),tyrosol (7),4-hydroxybenzoic acid (8),4-hydroxyphenylacetic acid (9),6-vinyl hexanolide (10),loliolide (11),armuionone D (12),azelaic acid (13),succinic acid (14),8-hydroxy-(6E)-octenoic acid (15),3-ethoxypropionic acid (16),n-butyl β-D-fructopyranoside (17),and n-butyl pyroglutamate (18).Conclusion Compounds 1-16 are isolated from this alga for the first time,and compounds 5,6,10,15,and 16 are obtained from natural products for the first time.Compounds 17 and 18 are artifacts of isolation from β-D-fructopyranoside and pyroglutamic acid.
Two new monoterpene glycosides, perillanolides A and B, together with a known compound reported from the genus Perilla for the first time were isolated and characterized from the leaves of Perilla frutescens (L.) Britton, Lamiaceae, a garnish and colorant for foods as well as commonly used for traditional medicine. The structures of the isolated compounds were elucidated on the basis of extensive spectroscopic evidences derived from nuclear magnetic resonance experiments, mass spectrometry and by comparing their physical and spectroscopic data of literature. These compounds, together with the previously isolated secondary metabolites of this species, were investigated for their inhibitory effects on xanthine oxidase in vitro. Of the compounds, luteolin showed the strongest inhibitory activity with an IC50 value of 2.18μM. Esculetin and scutellarein moderately inhibited the enzyme, while perillanolides A and B, and 4-(3,4-dihydroxybenzoyloxymethyl)phenyl-O-β-d-glucopyranoside exerted weak activities.
The seeds of Cassia obtusifolia L. are widely used in traditional Chinese medicine and health tea. The objective of this study was to investigate the effect of water availability on plant growth, seed yield, and seed quality in C. obtusifolia for improving its cultivation. Pot and field irrigation experiments were conducted in Qingdao of China in 2013 and 2014, respectively. Seven water irrigation treatments including 100%, 90%, 80%, 70%, 60%, 50% and 40% of field capacity (FC) in pot experiments while five water irrigation treatments including 100%, 85%, 70%, 55% and 40% of field capacity (FC) in field experiments were applied on the plant of C. obtusifolia, respectively. In both experiments, the results showed that different drought stress significantly resulted in different reduction in plant growth and seed yield attributes of C obtusifolia, and more pronounced with the severity of drought. However, as for the seed quality attributes, both results showed that weak and moderate drought stress significantly increased the content of anthraquinones (plant secondary metabolites) while significantly decreased the content of protein (plant primary metabolites) in the seeds of C obtusifolia, except that strong drought stress significantly decreased both of them. Notably, the weak drought stress (70% FC in pot and in field) did not decrease the seed yield significantly which resulted in a biggest harvest index among other treatments and thus resulted in the highest anthraquinones yields per plant. In addition, results showed that strong and moderate drought stress affected the proportion between hydrophilic and lipophilic anthraquinones in seed of C. obtusifolia significantly. Our study suggested that a certain of deficit irrigation has the potential to compromise seed yield and seed quality of C. obtusifolia, which can be used as a practical irrigation strategy for cultivation improving of C. obtusifolia as a medicinal plant. (C) 2017 Published by Elsevier B.V.
To investigate the chemical constituents from the ethyl acetate extract of Rabdosia excise,in this paper,the compounds were isolated by ODS(octadecyl-binded silica gel) column chromatography and preparative HPLC(High Performance Liquid Chromatography),their structures were elucidated on the basis of chemical and spectroscopic methods including MS,1D and 2D NMR spectra techniques.Seven triterpenes were isolated from the ethyl acetate extract of Rabdosia excise,and were identified as 2α,3β,19α-thihydroxy-28-norurs-12-ene,2α,3β,24-trihydroxy-olean-12-en-28-oic acid,hyptadienic acid,2α,3α-dihydroxyurs-12-en -28-oic acid,3-epimaslinic acid,maslinic acid,and oleanic acid.Compounds 2α,3β,19α-thihydroxy-28-norurs-12-ene and 2α,3β,24-trihydroxy-olean-12-en-28-oicacid are firstly isolated from the genus of Rabdosia.
Method of multi-enzyme was used to optimize the extraction process of polysaccharide from Ploygonatum sibiricum,phenol-sulfuric acid colorimetric method was applied to determine the content of polysaccharide,defined the polysaccharide extraction rate as the index to choice the kind and ratio of enzymes,the experimental factors were selected by single factor trials such as enzymatic hydrolysis temperature,pH,the rate of material to solvent,the amount of enzyme concentration,the important ones of which would be chosen to optimize by orthogonal test. Results showed that multi-enzyme extraction was better than extraction by single-enzyme or water. The rate of cellulose to papain was 3 to 7. The optimum enzymolysis conditions were as following:pH value of 5.0,temperature of 50 ℃,the rate of material to solvent was 1 to 20,the amount of enzyme concentration was 1.5%,which was 0.45% of cellulose and 1.05% of papain,2 hour-hot water extraction after 2 hour-enzymatic hydrolysis. In this condition,the maximum polysaccharide rate was 21.55%,which was 2.75 times as high as water,and had 12.6%higher than that of single factor
Objective To observe the effect ofCodonopsis lanceolata Radix from four origins on milk yield and prolactin (PRL) level in rats with puerperal hypogalactia and analyze the action mechanism.Methods The rat model of puerperal hypogalactia was induced by bromocriptine. The effect of extract ofCodonopsis lanceolata Radix from four origins on the milk yield and PRL level of maternal rats was determined.Results Compared with the animals in model group, the milk yield and PRL level of rats with puerperal hypogalactia treated with extract ofCodonopsis lanceolata Radix from four different regions increased.ConclusionCodonopsis lanceolata Radix can unblock the lactation channel, increase milk yield and increase the PRL level in the rats with puerperal hypogalactia.
Objective To optimize the extraction process of total saponins from Polygonati Rhizoma produced in Mountain Lao. Methods The vanillin-perchloric acid chromogenic assay was applied to determine the content of total saponins. On the basis of single factor experiment, the impact of ethanol concentration, the rate of material to solvent, extraction temperature, time and frequency on extraction efficacy was observed by Box-Benhnken design combined with responsive surface analysis, using extraction rate of total saponins as index. Results The extraction process of total saponins from Polygonati Rhizoma produced in Mountain Lao was established. The optimized extraction process was as follows: ethanol concentration of 73 %, extraction temperature of 56 ℃, the rate of material to solvent of 1:15, extraction time of 45 min and the extraction was repeated for two times. The maximum yield of total saponins was 2.87 mg/g under these conditions, which was 6.3 % higher than that of single factor trial. Conclusion An optimum extraction method for total saponins was established, which van provide basis for further development and comprehensive utilization of Polygonati Rhizoma produced in Mountain Lao.
By methods of species investigation,specimen identification and literatures retrieving,the legumes species and medicinal plant resources were investigated,the chemical constituents and medicinal val-ue of legumes medicinal plants in Laoshan Mountain were analyzed.The results showed that the legumes me-dicinal plants in Laoshan Mountain belonged to 90 species,42 genera,accounting for 5.40%and 24.42%of the total species and genera in China respectively.Forty -three species belonging to 25 genera were the typi-cal medicinal plants,and 21 among them had been listed into “China Pharmacopoeia”(2010 Edition).The legumes medicinal plants in Laoshan Mountain had complicated pharmaceuticals such as flavonoids,steroidal, saponins and anthraquinones and various bioactivity.They were classified according to their different pharma-codynamic effects.
目的 系统调查青岛崂山抗癌药用植物状况,为抗癌植物资源的进一步开发利用提供依据.方法 行野外实地考察,采集标本并鉴定,同时查阅文献资料.结果 发现崂山重要抗癌药用植物有18种,包括:喜树、长春花、日本榧树、七叶一枝花、白花蛇舌草、白英、半枝莲、龙葵、白屈菜、枸橘、虎杖、苦参、农吉利、皂荚、异叶败酱、射干、马勃、苍耳.结论 青岛崂山蕴含着珍贵的具有抗癌功效的植物资源,可为抗癌新药开发提供重要资源.
Through the methods of species investigation , specimen identification and literatures retrie-ving, the species and medicinal plants belonging to Compositae family were investigated systematically in the Laoshan Mountain of Qingdao .Their chemical components and medicinal value were also analyzed .The re-sults showed that 145 species of this family were found belonging to 69 genera , accounting for 82 .9%and 88.5%of the total species and genera in Shandong Province , and 6.3%and 29.4%of the total species and genera in China , respectively .Thirty species were new found and not recorded in the Laoshan Flora .Among them, 106 species belonging to 51 genera were of typical medicinal value , which accounted for 42.5% and 21.2%of the total medicinal genera and species number in China; in which, 32 species were recorded in Chinese Pharmacopoeia .The medicinal plants in the Laoshan Mountain had complex chemical components such as volatile oil , flavonoid , polyacetylenes , triterpenoid saponin , lignans and alkaloid , so they were of multiple biological activities .Some suggestions were put forward to protect and utilize these medicinal plants of Compositae family in the Laoshan Mountain .