The chemical constituents from the roots of Gentiana crassicaulis and their inhibitory effects on inflammatory mediators NO and TNF-α

Chemical study on the roots of Gentiana crassicaulis Duthie ex Burk(Gentianaceae)afforded 15 compounds,including two new iridoid glycosides,qinjiaosides B(1)and C(2).Their structures were elucidated by spectroscopic methods and chemical evidence.The isolated iridoid glycosides 1,4-6 and 8-11 were tested for their anti-inflammatory activity by the inhibitory effects on LPS-induced NO and TNF-αproduction in macrophage RAW264.7 cells.All of them showed inhibitory effects on inflammatory mediators NO at a concentration of 15μM,while 5 and 9 displayed the most potential inhibitory effects on TNF-awith IC50 of 0.06 and 0.05μM,respectively.The structure-activity relationships(SARs)of these iridoid derivatives were discussed.

中国内蒙古龙胆属一新种——兴安龙胆(Gentiana hsinganica)

描述了龙胆科龙胆属一新种——兴安龙胆(Gentiana hsinganica),绘制了形态图并与近缘种条叶龙胆(G.manshurica)、三花龙胆(G.triflora)和朝鲜龙胆(G.uchiyamai)做了比较,主要区别特征为:茎生叶3枚轮生,花萼裂片极小并呈三角形,每朵花下的苞片明显长于花萼。

Gentiana manshurica Kitagawa prevents acetaminophen-induced acute hepatic injury in mice via inhibiting JNK/ERK MAPK pathway

AIM:To investigate the in vivo hepatoprotective effects and mechanisms of Gentiana manshurica Kitagawa (GM) in acetaminophen (APAP)-induced liver injury in mice.METHODS: GM (200, 150 or 50 mg/kg body weight) or N-acetyl-L-cysteine (NAC; 300 mg/kg body weight) was administrated orally with a single dose 2 h prior to APAP (300 mg/kg body weight) injection in mice.RESULTS: APAP treatment significantly depleted hepatic glutathione (GSH), increased serum aspartate aminot ransferase (AST), alanine aminotransferase (ALT) and malonyldialdehyde (MDA) and 4-hydroxynonenal levels, and decreased hepatic activity of glutathione peroxidase (GSH-px) and superoxide dismutase (SOD). However, the pretreatment of GM signif icantly alleviated APAP-induced oxidative stress by increasing GSH content, decreasing serum ALT, AST and MDA, and retaining the activity of GSH-px and SOD in the liver. Furthermore, GM pretreatment can inhibit caspase-3 activation and phosphorylation of c-Jun-NH2-terminal protein kinase 2 (JNK1/2) and extracellular signalregulated kinase (ERK). GM also remarkably attenuated hepatocyte apoptosis confirmed by the terminal deoxynucleotidyl transferase mediated dUTP nick end-labeling method.CONCLUSION: Hepatoprotective effects of GM against APAP-induced acute toxicity are mediated either by preventing the decline of hepatic antioxidant status or its direct anti-apoptosis capacity. These results support that GM is a potent hepatoprotective agent.

Minor antifungal aromatic glycosides from the roots of Gentiana rigescens(Gentianaceae)

Two new phenolic glycosides, 2,3-dihydroxybenzoic acid methyl ester 3-O-β-o-glucopyranosyl-（1-6）-β-D-glucopyranoside （1） and 2,5-dihydroxylbenzofuran 5-O-β-D-xylopyranosyl-（1-6）-O-β-D-glucopyranoside （2）, were isolated as the minor chemical constituents from the roots of Gentiana rigescens, along with 15 known compounds. Their structures were elucidated by detailed spectroscopic analysis, including 1D, 2D NMR and chemical method. All of these compounds were isolated for the first time from the title plant. Moreover, compounds 1 and 2 were tested for the antifungal activities on three plant pathogens Peronophythora litchi, Glomerella cingulata, and Glorosprium musarum.

Adaptations of the floral characteristics and biomass allocation patterns of Gentiana hexaphylla to the altitudinal gradient of the eastern Qinghai-Tibet Plateau

This study addressed the floral component traits and biomass allocation patterns of Gentiana hexaphylla as well as the relationships of these parameters along an elevation gradient(approximately 3700 m, 3800 m, 3900 m, and 4000 m) on the eastern Qinghai-Tibet Plateau. The plant height, floral characteristics, and biomass allocation of G. hexaphylla were measured at different altitudes after field sampling, sorting, and drying. Plant height was significantly greater at 3700 m than that at other elevations. Flower length was significantly greater at 4000 m than that at other elevations, whereas the flower length at low elevations showed no significant differences. Corolla diameter increased with altitude, although the difference was not significant between 3800 m and 3900 m. Variations in biomass accumulation, including the aboveground, photosynthetic organ, flower and belowground biomasses, showed non-linear responses to changes in altitude. The aboveground and photosynthetic organ biomasses reached their lowest values at 4000 m, whereas the belowground and flower biomassreached minimum values at 3700 m. The sexual reproductive allocation of G. hexaphylla also increased with altitude, with a maximum observed at 4000 m. These results suggest that external environmental factors and altitudinal gradients as well as the biomass accumulation and allocation of G. hexaphylla play crucial roles in plant traits and significantly affect the ability of this species to adapt to harsh environments. The decreased number of flowers observed at higher altitudes may indicate a compensatory response for the lack of pollinators at high elevations, which is also suggested by the deformed flower shapes at high altitudes. In addition, the individual plant biomass(i.e., plant size) had significantly effect on flower length and corolla diameter. Based on the organ biomass results, the optimal altitude for G. hexaphylla in the eastern Qinghai-Tibet Plateau is 3800 m, where the plant exhibits minimum propagule biomass and asexual reproductive allocation.

Immunomodulatory activity of butanol fraction of Gentiana olivieri Griseb. on Balb/C mice

Objective:To explore the immunomodulatory properties of 80% ethanol extract and butanol fraction of Gentiana olivieri(G. olivieri) Griseb on Balb/C mice.Methods:The study was performed with basic models of immunomodulation such as the humoral antibody response(hemoglutination antibody titres), cell mediated immune response(delayed type hypersensitivity and in vivocarbon clearance or phagocytosis). Ethanol(80%) extract of flowering aerial parts of G.olivieriand its butanol fraction were administered p.o.(orally) to the mice. Levamisole, 2.5 mg/kg was used as standard drug.Results:There was a potentiation of immune response to sheep red blood cells by cellular and humoral mediated mechanisms comparable to levamisole(2.5 mg/kg) by both 80% ethanol extract and the butanol fraction at doses of 50-200 mg/kg in male Balb/C mice. Both significantly(P<0.01) potentiated the humoral immune response in cyclophosphamide(250 mg/kg)immunosupressed mice at 100 and 200 mg/kg of each extract and fraction as compared to control.The potentiation of delayed type hypersensitivity response was statistically significant(P<0.01) at200 mg/kg of ethanol extract and 100, 200 mg/kg of butanol fraction as compared to control. The phagocytosis was significant at 200 mg/kg with butanol fraction ofG. olivieri.Conclusions:The results reveal the immunostimulant effects of plantG. olivieriin mice by acting through cellular and humoral immunity in experimental models of immunity in mice. Butanol fraction is the most effective at a dose level of 200 mg/kg.

Effects of gentiana scabra bage on expression of hepatic type Ⅰ,Ⅲ collagen proteins in Paragonimus skrjabini rats with liver fibrosis

Objective:To exploit- the effects of gentiana scabra bage on the expression of hepatic collagen proteins in Paragonimus skrjabini rats with liver fibrosis.Methods:Immunohistochemical technique was used to observe the changes of content of hepatic type Ⅰ,Ⅲ collagen proteins in Paragonimus skrjabini rats with Liver fibrosis before and after the gentiana scabra bage treatmeat.Results:Comparing with the model group,changes of hepatic tvpe Ⅰ and type Ⅲ collagen proteins in gentiana scabra bage treated group were significantly weakened.Conclusions:Gentiana scabra bage treatment can reduce the content of hepatic type Ⅲ and type Ⅰ collagen protein significantly in Paragonimus skrjabini rats with liver fibrosis,thereby,playing the role against hepatic fibrosis.

Cytomorphology of Gentiana kurroo: an important endangered bitter plant of temperate Himalaya

Gentiana kurroo, a potent bitter drug plant of Indian subcon- tinent, is under threat due to over exploitation and destruction of natural habitat. We studied the murphophenology and chromosomes of G. kurtoo on both wild and field grown plants, which is very important for proper identification, conservation and domestication. Results reveal that G. kurroo is a perennial herb, and its shoot is represented by flowering branches only. Stem is modified to rhizome. The older rhizomes split into four parts at collar region appearing to fuse together at the ends and is an important diagnostic feature for crude raw materials. Two types of leaves i.e. radical leaves at the base of the plant and canline leaves on flowering shoot are present. Flowering occurs during September to October with 1-9 inflorescences per plant. Inflorescence is terminal monoca- sial cysome type. Mowers are protrandus. Anthesis starts around 7.30 am and continued till 10.0 am. Ovary is bicarpillary syncarpous unilocular. Fruit is Capsule and takes 18-20 days to mature after fertilization. Seeds are very small elliptical and 1 000 seeds weigh to 0.1275 g. Chromosomal studies made by usual squash method reveals the species is a genomic allotetreploid with n = 13. The anaphase-I segregation was normal and in none of the cells at Anaphase-I or Telophase-I could any abnor- mality like laggards, bridges, micronuclei etc. be observed.

Technical Specifications for Seed Breeding of Gentiana macrophylla Pall.

This paper elaborates on the seedling technology,field cultivation technology,field management technology,seed harvesting and seed processing technology in the propagation process of Gentiana macrophylla to provide technical support for artificial breeding of G. macrophylla.

Pharmacokinetic Analysis of Four Bioactive Iridoid and Secoiridoid Glycoside Components of Radix Gentianae Macrophyllae and Their Synergistic Excretion by HPLC-DAD Combined with Second-Order Calibration

An HPLC-DAD method combined with second-order calibration based on the alternating trilinear decomposition(ATLD)algorithm with the aid of region selection was developed to simultaneously and quantitatively characterize the synergistic relationships and cumulative excretion of the four bioactive ingredients of Radix Gentianae Macrophyllae in vivo.Although the analytes spectra substantially overlapped with that of the biological matrix,the overlapping profiles between analytes and co-eluting interferences can be successfully separated and accurately quantified by the ATLD method on the basis of the strength of region selection.The proposed approach not only determined the content change but also revealed the synergistic relationships and the cumulative excretion in vivo of the four ingredients in urine and feces samples collected at different excretion time intervals.In addition,several statistical parameters were employed to evaluate the accuracy and precision of the method.Quantitative results were confirmed by HPLC-mass spectrometry.Satisfactory results indicated that the proposed approach can be utilized to investigate the pharmacokinetics of Radix Gentianae Macrophyllae excretion in vivo.

Exploring the anti-hepatoma effect and potential targets of the active components from Gentiana rhodantha Franch ex Hemsl

The screening of lead compounds in plants is an important way to develop new drugs.Gentiana rhodantha Franch ex Hemsl,belonging to genus Gentiana of Gentianaceae family,has the functions of clearing heat and drying dampness,detoxifying and purging fire,relieving cough and so on.Previous studies have shown that many compounds in G.rhodantha have antitumor activities,but the mechanism is still unclear.The purpose of this study was to investigate the anti-hepatoma activity of the compounds in G.rhodantha by using the knowledge of network pharmacology.A compound-cancer target network with 57 candidate molecules and 38 potential targets was constructed.Analysis of the models showed that the most effective compound in this plant might be compound 47(rhyncoside D)ether,and the most potential target might be GMP synthase(2vxo).We believe that the present study can provide important clues for the study of anti-hepatoma activity.

A review of phytochemistry and pharmacology perspectives of Gentiana rhodantha Franch.ex Hemsl.

Gentiana rhodantha Franch.ex Hemsl.(G.rhodantha)is a perennial herb distributed in southwest China,belonging to the Gentiana genus of Gentianaceae family.Previous research indicated that G.rhodantha contains flavonoids,anthraquinones,terpenes and other compounds,which possess the effects of antioxidant,antibacterial,and antitumor.Besides,its dry herb is used as antiphlogistic and antitussive remedy for the treatment of lung,liver,and gallbladder diseases.This review outlines the chemical constituents and biological activities of G.rhodantha,which will be useful for the further research on this plant.

基于高通量测序分析青藏高原特有植物蓝玉簪龙胆(Gentiana veitchiorum)的SSR和SNP特征

利用Illumina HiSeq ^(TM)2500平台对青海省库泽县的蓝玉簪龙胆(Gentiana veitchiorum)进行高通量测序,共得到SSR序列8 588条,对其SSR重复类型进行分析;三核苷酸重复类型所占的比例最大占54.7%(4696);其次是二核苷酸重复类型占41.3%(3543);四核苷酸重复类型,五核苷酸重复类型和六核苷酸重复类型所占的比例较少(共占4%)。在二核苷酸重复类型中AT/TA重复类型所占的比例最大分别为9.85%和9.5%。在微卫星中重复单元的长度大小和重复次数成负相关,并且微卫星的总长度与重复单元的长度成正相关。在蓝玉簪龙胆的花(GP-F)和叶(GP-L)中分别得到253 789和249 417个SNP位点,其中在非编码区上的比例为51.29%和51.96%。分析发现蓝玉簪龙胆SNP位点在编码区中同义转换所占的比例(48.63%和47.96%)要远远高于非同义转换的比例(0.08%和0.08%),可能与功能基因序列相对稳定有关。

A New Species of <i>Gentiana, Gentiana ciliolata</i>and It’s Two Subspecies of subsp. ciliolata and subsp. <i>longiloba</i>of Yunnan &Sichuan Provinces

A new species of Gentiana (Gentianaceae), Gentiana ciliolata is described and illustrated;it has a spectacular characteristics of calyx lobe ciliolate, distributed in Yunnan and Sichuan Provinces on the two sides of Jinsha River, and then two subspecies have been further re-classified as Gentiana ciliolata subsp. ciliolata and Gentiana ciliolata subsp. longiloba respectively. The subsp. ciliolata idistributes on the right side of Jinsha River in Yiliang County, Yunnan Province and the subsp. longiloba distributes itself on the southwest and west part of Sichuan Province, such as Leibo County, Wenchuan County and Mabian Yi Autonomous Prefacture, in the grassland under forests and moist rock slopes at an altitude of 1300 - 3200 m.

线叶龙胆(Gentiana lawrencei var.farreri)ITS序列杂合性与遗传分化分析

线叶龙胆(Gentiana lawrencei var.farreri)是龙胆属的常见种之一,分布于青藏高原地区,具有药用与观赏价值。ITS是重要的分子标记之一,可用于植物群体遗传与进化研究;然而由于其杂合性较高,为后续分析带来一定困难。以线叶龙胆7个居群共39个个体为对象,通过基因克隆与测序,共得到81条序列,鉴定出76个单倍型。结果表明ITS序列在线叶龙胆中存在很高的杂合性,居群遗传多样性高;且遗传变异的87.61%来自居群内,仅有12.39%来自于居群间。在鉴定的单倍型中,97.36%为单个个体所特有,个体间很少共享同一种单倍型;进一步的系统发育分析表明这些单倍型无法聚成高支持率的支系。研究揭示了线叶龙胆ITS序列存在高度杂合性,可为龙胆属的进化研究提供参考。

中国龙胆属(Gentiana L.)秦艽组(Sect.Aptera Kusnez.)的分类研究

龙胆属(Gentiana L.)秦艽组(Sect.Aptera Kusnez.)所属的种类大多数是治疗风湿性关节炎常用中药之一,除供国内广泛应用外,还有一定量的出口。此组在我国种类多,产量高,分布广,且有不少特有种。现在市场上商品秦艽和原植物的关系存在着一定的混乱现象,影响医疗效果。秦艽组在我国究竟有多少种,分布情况怎样,都不很清楚,为此作者对秦艽组进行了分类研究。

Gentiopicroside, originated from Gentiana macrophylla Pall, possesses antiarthritic efficacy in adjuvant-induced arthritis rats

OBJECTIVE This work aimed to investigate the anti-rheumatoid arthritic effect of gentio.picroside from Gentiana macrophylla Pall using an animal model of adjuvant induced arthritis.METH.ODS Adjuvant arthritis was induced in fifty SD male rats,which were randomly divided into five groups(n=10):control(0.5% CMC-Na) group,AIA(rats with CFA) group,dexamethasone(1 mg·kg^(-1)) group,gentiopicroside(50 mg·kg^(-1)) group,and gentiopicroside(100 mg·kg^(-1)) group.Rats were administered intragastrically with drugs or CMC-Na once a day for a period of 2 weeks.Paw swelling,arthritic index,histological changes were assessed to evaluate the anti-arthritic effect.Weight growth,spleen and thymus indexes were also investigated in.RESULTS Gentiopicroside at dose of 100 mg·kg^(-1) significantly inhibited the secondary paw swelling(P<0.05) and arthritis index(P<0.05),decreased synovial inflammatory infil.tration,synovial hyperplasia and bone erosion.Furthermore,gentiopicroside showed no immunosup.pressive adverse effects in body weight,index of spleen and thyums compared with dexamethasone administration(P<0.05,P<0.01).CONCLUSION Gentiopicroside possessed anti-arthritic efficacy in AIA rats without immunosuppressive effects.

滇龙胆的本草考证

目的:研究历代典籍对滇龙胆的文献记载,对滇龙胆进行本草考证,以期为滇龙胆的开发利用提供参考。方法:通过查阅历代本草典籍,结合现代研究文献,对滇龙胆的名称、基原、产地变迁、采收加工以及品质评价进行系统的梳理、考证。结果:经考证,滇龙胆始载于《滇南本草》,别名坚龙胆、龙胆草、苦草等,为龙胆科龙胆属植物,基原植物为滇龙胆,是《中华人民共和国药典》龙胆药材的基原植物之一;主产于云南,临沧是其道地产区;滇龙胆一般于秋冬两季采收;加工多以产地初加工为主,即将滇龙胆清洗后阴干或晒干;历代本草典籍中对其质量评价的记载非常少,以“形如枯骨”“根肥长”“脂润”“味苦”“粘牙”作为质量好坏的评价标准,现代主要以龙胆苦苷含量作为龙胆药材质量评价的主要手段之一,辅助以外观性状等的观测。结论:考证结果将为今后滇龙胆的开发利用提供参考。

Cryptic diversity and rampant hybridization in annual gentians on the Qinghai-Tibet Plateau revealed by population genomic analysis

Understanding the evolutionary and ecological processes involved in population differentiation and speciation provides critical insights into biodiversity formation. In this study, we employed 29,865 single nucleotide polymorphisms(SNPs) and complete plastomes to examine genomic divergence and hybridization in Gentiana aristata, which is endemic to the Qinghai-Tibet Plateau(QTP) region. Genetic clustering revealed that G. aristata is characterized by geographic genetic structures with five clusters(West, East, Central, South and North). The West cluster has a specific morphological character(i.e., blue corolla) and higher values of FSTcompared to the remaining clusters, likely the result of the geological barrier formed by the Yangtze River. The West cluster diverged from the other clusters in the Early Pliocene;these remaining clusters diverged from one another in the Early Quaternary. Phylogenetic reconstructions based on SNPs and plastid data revealed substantial cyto-nuclear conflicts. Genetic clustering and D-statistics demonstrated rampant hybridization between the Central and North clusters,along the Bayankala Mountains, which form the geological barrier between the Central and North clusters. Species distribution modeling demonstrated the range of G. aristata expanded since the Last Interglacial period. Our findings provide genetic and morphological evidence of cryptic diversity in G. aristata, and identified rampant hybridization between genetic clusters along a geological barrier.These findings suggest that geological barriers and climatic fluctuations have an important role in triggering diversification as well as hybridization, indicating that cryptic diversity and hybridization are essential factors in biodiversity formation within the QTP region.

辽东山区龙胆草栽培技术

本文简介了龙胆草的生物学特性,并从播种育苗、移栽、田间管理、病害防治、采收与加工等方面详细介绍了在辽东山区其栽培技术。