Synergistic bioassay-guided isolation of the extracts of Artemisia rupestris L, which belongs to the family Asteraceae, afforded two acetylenic spiroketal enol ethers, namely rupesdiynes A (1) and B (2). Their structures were determined based on spectroscopic analysis and experimental and calculated ECD investigations. The two compounds exhibited synergistic activity and were able to reduce the minimum inhibitory concentration (MIC) of oxacillin four-fold, with a fractional inhibitory concentration index (FICI) of 0.5 in combination with oxacillin against the oxacillin-resistant EMRSA-16. Biofilm formation inhibitory and Ethidium bromide (EtBr) efflux assay were further employed to verify the possible mechanism of the synergistic antibacterial effect. Additionally, molecular docking studies were conducted to investigate the binding affinities of the two compounds with penicillin-binding protein 2a (PBP2a) of EMRSA-16. Taken together, rupesdiynes A (1) and rupesdiyne B (2) showed moderate synergistic activity against EMRSA-16 with oxacillin via inhibiting biofilm formation and efflux pump activity, respectively.

This study aimed to explore the correlation between rhizosphere soil microorganisms of wild Arnebia euchroma and the content of medicinal components to provide guidance for the selection of the ecological planting base. The total DNA of rhizosphere soil microorganisms of wild A. euchroma was extracted, and the microbial community structure of rhizosphere soil microorganisms was analyzed by IlluminaMiseq high-throughput sequencing technology. The content of total hydroxynaphthoquinone pigment and β,β'-dimethylacrylalkannin in medicinal materials was determined by high-performance liquid chromatography(HPLC). The physicochemical pro-perties of rhizosphere soil of wild A. euchroma in main producing areas were determined, and the correlation of soil microbial abundance with index component content and soil physicochemical properties was analyzed by SPSS software. The results showed that the species composition of rhizosphere fungi and bacteria in A. euchroma from different habitats was similar at the phylum and genus levels, but their relative abundance, richness index(Chao1), and community diversity(Simpson) index were different. Correlation analysis showed that the content of available phosphorus in soil was positively correlated with the content of total hydroxynaphthoquinone pigment and β,β'-dimethylacrylalkannin, and the abundance of five fungal genera such as Solicoccozyma and six bacterial genera such as Pseudo-nocardia and Bradyrhizobium was positively correlated with the content of medicinal components in medicinal materials. The abundance of Bradyrhizobium was significantly positively correlated with the content of β,β'-dimethylacrylalkanin. The abundance of fungi such as Archaeorhizomyces was significantly positively correlated with the content of available phosphorus in rhizosphere soil, and Bradyrhizobium was significantly negatively correlated with soil pH. Therefore, the abundance of fungi and bacteria in the rhizosphere of A. euchroma has a certain correlation with the medicinal components and the physicochemical properties of the rhizosphere soil, which can provide a scientific basis for the selection of ecological planting bases in the later stage.

目的 采用HPLC法同时测定大苞荆芥中齐墩果酸和熊果酸的含量,并分析不同产地大苞荆芥质量的差别.方法 采用JADE-PAKODS-AQ色谱柱(250mmx4.6mm,5μm),流动相为甲醇-0.05mol·L-1乙酸钱(85:15),检测波长210 nm,柱温30℃.结果 齐墩果酸和熊果酸的线性范围分别为0.108～4.32μg(r2=0.9993,n=6)、0.212～8.48μg(r2=0.9994,n=6),加样回收率与RSD均符合要求.大苞荆芥中齐墩果酸和熊果酸的平均含量分别为0.0686％、0.1186％.结论 所用方法简便、准确、稳定、可靠,可用于大苞荆芥的质量评价.

Imported medicinal materials are an important part of Chinese medicinal resources. To be specific, about 10% of the around 600 commonly used Chinese medicinal materials are from abroad, and the introduction of foreign medicinal materials has promoted the development of Chinese medicine. Amid the advancement of reform and opening up and the "Belt and Road" Initiative, major headway has been made in the cross-border trade in China, bringing opportunities for the import of medicinal materials from border ports. However, for a long time, there is a lack of systematic investigation on the types of exotic medicinal materials at border ports. In the fourth national census of traditional Chinese medicine resources, National Resource Center for Chinese Materia Medica, China Academy of Chinese Medical Sciences, together with several organizations, investigated the nearly 40 border ports, Chinese medicinal material markets, and border trade markets in 6 provinces/autonomous regions in China for the first time and recorded the types, sources, circulation, and the transaction characteristics of imported medicinal materials. Moreover, they invited experts to identify the origins of the collected 237 medicinal materials. In addition, the status quo and the problems of the medicinal materials were summarized. This study is expected to lay a basis for clarifying the market and origins of imported medicinal materials as well as the scientific research on and supervision of them.

目的:通过对新疆紫草进行生态适宜性评价,为优质新疆紫草生产基地选址提供参考.方法:选取第四次全国中药普查新疆普查空间数据中129份新疆紫草的基本信息,利用最大熵(MaxEnt)模型和ArcGIS软件分析评价.结果:影响新疆紫草分布的主要生态因子为海拔、土壤类型、植被类型、6月降水量、12月降水量、10月平均气温、等温性;新疆紫草潜在分布区为和静县、尼勒克县、博乐市、温泉县、昭苏县、霍城县、精河县、伊宁市、伊宁县、裕民县、奎屯市、阿克陶县、巩留县、乌鲁木齐县、乌恰县等;MaxEnt模型预测结果经受试者工作特征(ROC)曲线评价曲线下面积(AUC)>0.9.结论:新疆紫草的生态适宜性分布区主要集中在天山山脉中段的和静县、尼勒克县、博乐市、温泉县、昭苏县,建议优先选择上述区域开展新疆紫草人工栽培.

Four undescribed sulfoxide-containing derivatives, sinkiangenoxides A and B, (2 Z , 4 E )-sinkiangenoxide C, and (2 E , 4 E )-sinkiangenoxide C ( 1 - 4 ), and one known compound, 1-(methylthio)propyl ( E )-1-propenyl disulfide ( 5 ), were isolated from the resin of Ferula sinkiangensis . Their structures were determined based on spectroscopic methods, including IR, UV, HRESIMS, NMR, and CD analysis. Compounds 2 - 4 showed moderate cytotoxic activities against four human cancer cell lines with IC (50) values ranging from 15.0 to 40.3 mu M. Sinkiangenoxide B ( 2 ) was shown to induce apoptosis in HepG2 cells. In addition, compound 5 effectively attenuated lipopolysaccharide-induced nitric oxide release and TNF- alpha , IL-1 beta , IL-6, and IL-10 expression.

目的:评价新疆阿魏内生真菌提取物体外抗肿瘤细胞增殖活性,并筛选具有抗肿瘤细胞增殖活性的菌株,为进一步研究其抗肿瘤作用提供依据.方法:采用四甲基偶氮唑盐(MTT)法测定117株新疆阿魏内生真菌菌液提取物和菌丝体提取物对人宫颈癌HeLa细胞和胃癌AGS细胞增殖的影响.结果:有43株链格孢属菌株的49份提取物在质量浓度为100μg·mL–1时,对肿瘤细胞抑制率达50％以上;其中15份对HeLa细胞、AGS细胞的增殖均具有显著抑制作用,且1938/TL168菌株提取物对HeLa细胞增殖的半数抑制浓度(IC50)低至(25.95±3.39)μg·mL–1.结论:阿魏内生真菌提取物可有效抑制肿瘤细胞增殖,具备抗肿瘤药物研发潜质.

目的 为揭示新疆啤酒花Humulus lupulus野生与栽培个体间的遗传关系、遗传结构及野生资源的遗传潜力.方法 利用SLAF-seq简化基因组测序技术,对新疆20个野生个体和18个栽培个体的SNP位点进行了开发与鉴定.利用系统发育分析、群体遗传结构分析和主成分分析(principal component analysis,PCA)等方法,从基因组水平揭示了野生种与栽培种之间的遗传结构.结果 结果表明,通过SLAF-seq测序共获得863228个SLAF标签,其中多态性SLAF标签有443922个,共获得2867140个SNP位点.系统发育分析表明,野生个体和栽培个体整体上可各自分为2个聚类簇.总的Shanon-Wiener指数平均为0.397,其中野生个体为0.455,栽培个体为0.398;总的Nei多样性指数平均为0.249,其中野生个体为0.293,栽培个体为0.250.AMOVA分析表明,啤酒花的主要遗传变异主要来源于群体间,野生个体与栽培个体之间具有较大的遗传分化.结论 新疆分布的野生啤酒花个体与栽培个体之间存在较大的遗传分化,但是野生啤酒花个体具有较高的遗传多样性,说明新疆啤酒花的野生资源具有较高的遗传育种潜力.

This study seeks to discover flavonoids from a traditional Chinese herb, Artemisia rupestris L., with synergistic antibacterial effects against multidrug-resistant Staphylococcus aureus. Five flavonoids, artemetin (1), chrysosplenetin (2), pachypodol (3), penduletin (4) and chrysoeriol (5) were obtained by various column chromatographic methods. Their chemical structures were determined on the basis of comprehensive spectroscopic analysis and comparison with literature data. Three of the compounds (2, 4 and 5) exhibited synergistic activity when combined with norfloxacin against SA1199B, an effluxing fluoroquinolone-resistant strain. The fractional inhibitory concentration indices (FICIs) of 2, 4 and 5 in combination with norfloxacin were 0.375, 0.079 and 0.266 respectively, suggesting synergy. Compound 5 also showed synergistic effects against EMRSA-15 and EMRSA-16 when combined with ciprofloxacin and oxacillin exhibiting FICIs of 0.024 and 0.375 respectively. Real time ethidium bromide (EtBr) efflux assay, qRT-PCR and molecular docking were employed to explore the mechanisms of the synergistic effects.

建立新疆不同产地罗布麻Apocynum venetum和白麻A.pictum药材的HPLC指纹图谱,结合相似度分析、含量测定、聚类分析和主成分分析对收集药材的化学成分差异进行分析.采用Phenomenex Kinetex C18(4.6 mn× 100 mm,2.6 μm)色谱柱,以乙腈-0.01％三氟乙酸水溶液为流动相,梯度洗脱,流速0.6 mL·min-1,检测波长281 nm,柱温25℃.建立31批药材的HPLC分析方法,并完成绿原酸、金丝桃苷、异槲皮苷、三叶豆苷、紫云英苷、芦丁和白麻苷的含量测定,分别利用《中药色谱指纹图谱相似度评价系统(2004A版)》和SPSS 21.0软件进行指纹图谱研究和化学计量学分析.结果 显示,罗布麻和白麻的HPLC指纹图谱标定了21个共有峰,并指认了绿原酸、金丝桃苷、异槲皮苷、三叶豆苷和紫云英苷5个共有峰.除了3批药材,其余28批药材的相似度均高于0.83,相似度总体上良好.基于含量测定结果进行聚类分析,当欧式距离为15时,可将药材分为南疆和北疆药材两大类,表明新疆罗布麻和白麻药材的差异与产地有一定关系.以主成分分析对药材质量进行排名,结果前15名均为北疆药材.综合相似度评价、聚类分析及主成分分析结果,认为新疆罗布麻和白麻药材在相似中存在差异,且差异与产地有一定相关性.该结果可为分析评价不同产地罗布麻和白麻药材差异及二者引种栽培产地的选择提供参考.

Ferula sinkiangensis K. M. Shen is a valuable traditional Chinese medicine historically used to treat stomachache and rheumatoid arthritis. The chloroplast genome of Ferula genus plant has not been previously reported. This study reported the complete chloroplast genome sequence of F. sinkiangensis based on high-throughput sequencing. The genome was 166,583 bp in length, containing a small single-copy (SSC) region of 17,595 bp and a large single-copy (LSC) region of 85,242 bp, separated by two inverted repeats (IRs) of 31,873 bp, each. The genome contained 114 unique genes, including 80 protein-coding genes (PCGs), four rRNA genes, and 30 tRNA genes. In addition, 17 genes contained one or two introns, including nine PCG genes with a single intron, two PCG genes harboring two introns, and six tRNA genes harboring a single intron. In this study, F. sinkiangensis K. M. had the closest genetic relationship with Torilis scabra and clustered with the Umbelliferae family species.

目的 探讨啤酒花改善β-淀粉样蛋白(Aβ)损伤成骨细胞的骨形成作用及其机制.方法 以新生24 h Wistar大鼠所分离的成骨细胞为研究对象,用Aβ1-42寡聚体对成骨细胞进行损伤,并用啤酒花提取物进行药物干预.分别采用MTT法、碱性磷酸酶(ALP)活性检测以及茜素红染色法评价成骨细胞的增殖、分化及骨矿化水平,流式细胞仪检测成骨细胞凋亡.采用蛋白质印迹法检测骨形成相关蛋白及氧化应激Nrf2、FoxO1通路蛋白的表达水平,并用免疫荧光检测FoxO1蛋白的入核表达.结果 啤酒花提取物可显著促进Aβ损伤成骨细胞的增殖,提高ALP活性及骨矿化结节水平,抑制细胞凋亡率,并促进骨形成相关蛋白I型胶原酶(COL-I)及骨桥蛋白(OPN)的表达.此外,啤酒花提取物可显著激活Aβ损伤成骨细胞的Nrf2和FoxO1信号通路,促进该氧化应激信号通路相关蛋白的表达,通过抗氧化维持骨代谢平衡.结论 本研究表明啤酒花具有减轻Aβ损伤成骨细胞的作用,初步阐明其作用机制与抗氧化有关,为抗骨质疏松作用机制及药物研发提供了新思路.

OBJECTIVES Xanthohumol (XAN) is a unique component of Humulus lupulus L. and is known for its diverse biological activities. In this study, we investigated whether Xanthohumol could ameliorate memory impairment of APP/PS1 mice, and explored its potential mechanism of action. METHODS APP/PS1 mice were used for in vivo test and were treated with N-acetylcysteine and Xanthohumol for 2 months. Learning and memory levels were evaluated by the Morris water maze. Inflammatory and oxidative markers in serum and hippocampus and the deposition of Aβ in the hippocampus were determined. Moreover, the expression of autophagy and apoptosis proteins was also evaluated by western blot. KEY FINDINGS Xanthohumol significantly reduced the latency and increased the residence time of mice in the target quadrant. Additionally, Xanthohumol increased superoxide dismutase level and reduced Interleukin-6 and Interleukin-1β levels both in serum and hippocampus. Xanthohumol also significantly reduced Aβ deposition in the hippocampus and activated autophagy and anti-apoptotic signals. CONCLUSIONS Xanthohumol effectively ameliorates memory impairment of APP/PS1 mice by activating mTOR/LC3 and Bax/Bcl-2 signalling pathways, which provides new insight into the neuroprotective effects of Xanthohumol.

Objective To explore the effects of Humulus lupulus L. extract (HLE) and xanthohumol (XN) on preventing glucocorticoid-induced osteoporosis (GIOP). Methods The GIOP model was established by intraperitoneal injection of dexamethasone (DEX). Bone microstructure, bone mineral density and serum biochemical indexes were evaluated by Micro-CT and ELISA kits. The levels of cells proliferation and ALP activity, and the expression of bone formation related proteins were assayed with primary osteoblasts injured by DEX. Results HLE and XN significantly alleviated the bone microstructure damage, enhanced the bone mineral density, and improved the trabecular parameters in GIOP mice. In vitro experiments showed that HLE and XN can prevent bone loss not only by improving cell proliferation and ALP activity, but also through increasing the expression of bone γ-glutamic acid-containing proteins (BGP), bone morphogenetic protein 2 (BMP-2) and runt-related transcription factor 2 (Runx-2). Conclusion This study confirmed that HLE and XN had anti-GIOP effects for the first time. It provides a new resource for the development of anti-osteoporosis medications.

建立高效液相色谱法,分别测定不同采收期的新疆产罗布麻和白麻药材中绿原酸、金丝桃苷、异槲皮苷、三叶豆苷、紫云英苷、芦丁和白麻苷的含量,进而分析2种药材的最佳采收期.发现不同采收期的新疆产罗布麻和白麻药材中绿原酸、金丝桃苷、异槲皮苷、三叶豆苷、紫云英苷、芦丁和白麻苷的含量存在一定差异,并且罗布麻和白麻呈现出不同特点.以《中国药典》中罗布麻含量测定项下的金丝桃苷为指标,罗布麻和白麻的最佳采收期都是6、7月;但是,以7个成分的总含量和6个黄酮的总含量为指标,罗布麻的最佳采收期是8、9月,白麻的最佳采收期仍是6、7月.该结果可为确定罗布麻和白麻药材的采收时间提供一定参考.

BACKGROUNDA Chinese folk medicine plant Pleurospermum lindleyanum possesses pharmacological activities of heat-clearing, detoxifying and preventing from hepatopathy, coronary heart disease, hypertension, and high altitude sickness. We isolated and characterized its constituents to investigate its synergistic effects against human hepatoma SMMC-7721 cells. Objective: The aim of this study was to explore the synergistic anti-cancer activities of isolates from P. lindleyanum with 5-FU on hepatoma SMMC-7721 cells in vitro and their primary mechanisms. Methods: Sequential chromatographic techniques were conducted for the isolation studies. The isolates structures were established by spectroscopic analysis as well as X-ray crystallographic diffraction. Growth inhibition was detected by MTT assay. The isobologram method was used to assess the effect of drug combinations. Flow cytometry and western blot were used to examine apoptosis and protein expression. Results: A new coumarin (16), along with sixteen known compounds, were isolated from the whole plant of P. lindleyanum and their structures were elucidated by spectroscopic methods. Four coumarins (2, 3, 5, and 16), two flavonoids (8 and 9) and three phytosterols and triterpenes (12-14) were found to synergistically enhance the inhibitory effect of 5-FU against SMMC-7721 cells. Among them, compounds 3 and 16 exhibited the best synergistic effects with IC50 of 5-FU reduced by 16-fold and 22-fold possessing the minimum Combination Index (CI) 0.34 and 0.27. The mechanism of action of combinations might be through synergistic arresting for the cell cycle at G1 phases and the induction of apoptosis. Moreover, western blotting and molecular docking revealed that compounds 3 or 5 might promote 5-FU-induced apoptosis by regulating the expression of Caspase 9 and PARP. Conclusion: Constituents from P. lindleyanum may improve the treatment effectiveness of 5-FU against hepatocellular carcinoma cells.

目的 建立测定清补通络丸中丹酚酸B含量的高效液相色谱法.方法 色谱柱为ACE 5 Super C18柱(250 mm×4.6 mm,5μm),流动相为乙腈-0.1％磷酸(22:78,V/V),检测波长为286 nm,流速为1.2 mL/min,柱温为25℃.结果 丹酚酸B质量浓度在30.62～306.20μg/mL范围内与峰面积线性关系良好,r=0.9975(n=6);平均加样回收率为99.55％,RSD为1.31％(n=6);供试品中丹酚酸B的平均含量为11.0305 mg/g.结论 该方法简便、准确,重复性好,可用于检测清补通络丸中丹酚酸B的含量.

[目的]研究不同地区梭梭种子性状及发芽能力的差异.[方法]对新疆22个不同地区的梭梭种子在室内进行发芽实验,并对种子表型粒径、粒厚和粒径粒厚比与种子地理、气候相关因子进行分析.[结果]1)粒径最大值为哈巴河县,最小值为巴里坤县;粒厚最大值为克拉玛依市,最小为福海县;粒径粒厚比最大值为福海县,最小为托里县.2)种子粒径、粒厚、粒径粒厚比、发芽率及发芽势之间差异均显著.变异系数表明,种子发芽率和发芽势变异幅度较大,粒径变异幅度较小.粒径、粒厚、粒径粒厚比、发芽率和发芽势在各地区间的变异系数分别为9.00%、11.72%、10.40%、16.00%和18.05%.3)地理、气象因子与梭梭种子萌发及性状呈现一定的相关性,种子发芽率和发芽势与年均温度呈显著正相关.[结论]通过对发芽率等指标选择评价,阜康市、托克逊县和托里县的梭梭种子发芽率最大,表现较优,可以考虑作为梭梭种子育苗推广.

Five undescribed sesquiterpene coumarins, one undescribed coumarin derivative, and twenty-five known analogues, were isolated from the resin of Ferula sinkiangensis K.M.Shen. The planar structures and relative configurations of the undescribed compounds were determined by NMR experiment and HRESIMS data. The absolute configurations were established by Electrostatic Circular Dichroism method. Among these analogues, Sinkiangenol E showed the best cytotoxic activity against HeLa cervical cancer cells. Annexin V-FITC/PI staining indicated that Sinkiangenol E induced apoptosis in HeLa cells. Cell cycle analysis showed Sinkiangenol E arrested cell cycle at G0/G1 phase. Western blot results proved that Sinkiangenol E affected apoptosis-related and cell cycle regulation-related protein expression by activating the MAPK pathway.

目的 研究新疆阿魏内生菌Alternaria sp.TA26-16的化学成分.方法 该真菌固体发酵物的甲醇提取物采用硅胶、凝胶和制备高效液相进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构.结果 从中分离得到10个化合物,分别鉴定为麦角甾-4,6,8 (14),22E-四烯-3-酮(1)、邻苯二甲酸二异丁酯(2)、油酸(3)、对甲基苯甲醛(4)、β-谷甾醇(5)、亚油酸(6)、2-oxabicyclo[3,2,2]nona-5,7,8-triene (7)、2-(4-羟基苯基)乙酸乙酯(8)、alternariol (9)、alternariol-4-methyl ether (10).结论 所有化合物均为首次从该内生菌中分离得到.