Eucommia ulmoides staminate flowers (EUF), a newly approved functional food in China, have great potential for hormonal regulation. Herein, we aim to demonstrate the chemical composition and pharmacological activity of EUF in testosterone production and hormonal regulation. EUF extract and its components, kaempferol and geniposidic acid, exhibited a strong stimulating effect by increasing testosterone secretion, reducing ROS production, or promoting viability in Leydig cells. Meanwhile, the increased testosterone production was related to the upregulation of mRNA and protein expression of the steroidogenic pathway, such as steroidogenic acute-regulatory protein (StAR), 3β -hydroxysteroid dehydrogenase type 1 (HSD3B1), 17α-hydroxylase/17,20-lyase (CYP17A1), and nuclear receptor subfamily 5 group A member 1 (NR5A1). However, PKA inhibitor H89 or adenylyl cyclase inhibitor SQ22536 could block their effect. The results of transgenic yeast models showed the androgenic agonistic effects of kaempferol and naringenin and the estrogenic agonistic effects of rutin. These results indicated that the testosterone promotional effect of EUF was related to the activation of the steroidogenic pathway and potential hormonal regulation. Kaempferol and geniposidic acid might be the key active ingredients.

In this paper, the polysaccharides fingerprints of Polygonatum cyrtonema Hua. were constructed, combined with various chemometric methods, to evaluate the differences of P. cyrtonema polysaccharides from different origins. The 1-pheny-3-methyl-5-pyrazolone (PMP) pre-column derivatization-HPLC method was applied to analyze the monosaccharide composition and total polysaccharide content of P. cyrtonema. Furthermore, the fingerprints were further evaluated by chemometric methods, including similarity analysis (SA), cluster analysis (HCA), and principal component analysis (PCA). The results showed that the composition of monosaccharides was galacturonic acid, glucuronic acid, galactose, glucose, and xylose. The similarities were ranged from 0.781 to 0.945. In addition, the content of total polysaccharides was in the range of 7.18% to 16.27%. HCA and PCA all divided P. cyrtonema polysaccharides from different origins into two categories, the samples collected in Cili County, Hunan Province were a separate one. These results indicated that the polysaccharide fingerprints of P. cyrtonema were quite different. Establishing the standardized cultivation technology system of P. cyrtonema is necessary to ensure clinical efficacy and safety.

γ-氨基丁酸是一种非蛋白质氨基酸,广泛分布于微生物和动植物中,具有多种生物活性.γ-氨基丁酸具有抗糖尿病、抗高血压、保护肝肾、促进睡眠等活性.对γ-氨基丁酸的生物活性进行了总结,以期为后续γ-氨基丁酸的深入研究提供科学的依据.

目的 分离纯化滇黄精Polygonatum kingianum中的均一多糖,并阐释其理化性质和抗氧化活性.方法 通过水提醇沉、分级醇沉得滇黄精总多糖(PKS)的50％和70％醇沉部位,再经DEAE-琼脂糖凝胶FF离子交换柱和SephadexG-100柱色谱法分离纯化得到均一多糖,并利用柱前衍生化HPLC、高效凝胶渗透色谱法和红外光谱法分别对其单糖组成、相对分子质量和结构进行研究;同时采用总还原力实验、1-二苯基-2-三硝基苯肼(DPPH)和羟基自由基(·OH)清除法对其抗氧化活性进行评价.结果 从50％和70％醇沉部位分离纯化得到3个均一多糖(PKS-1、PKS-2和PKS-3),其单糖组成均含有D-甘露糖、D-半乳糖醛酸、D-葡萄糖醛酸、D-半乳糖、D邛可拉伯糖和L-岩藻糖,其中PKS-1及PKS-3还分别含有D-核糖和L-鼠李糖;相对分子质量分别为85017.83、266084.76和474799.22;PKS、PKS-1和PKS-2的总还原能力、·OH及DPPH自由基的清除能力为PKS＞ PKS-2 ＞PKS-1.结论 从滇黄精50％和70％醇沉部位分离到3个均一多糖,均为含有β构型的吡喃环酸性多糖,其单糖组成相似,PKS、PKS-1和PKS-2均有一定的抗氧化活性,为滇黄精抗氧化活性成分的研究及抗衰老药物和功能性食品的开发利用奠定了科学基础.

目的:基于网络药理学分析金钗石斛治疗神经系统疾病的药效物质基础及作用机制.方法:检索Si-noMed、中国知网、万方等数据库获取金钗石斛中的化学成分,将成分录入TargetNet数据库以获取潜在靶点,再将靶点导入CTD数据库检索相关疾病,导入DAVID数据库获取靶点的基因功能及作用通路.用Cytoscape软件构建"成分-靶点"及"靶点-疾病"网络等进一步可视化整合分析.并采用AutoDock Vina软件对关键成分与靶点进行分子对接验证.结果:本研究共收集到金钗石斛中47个成分,可作用于88个靶点,进一步分析可知Nobilin D、Nobliomethylene、decumbic acid B、(+)-dendrolactone、(-)-denobilone A和Nobilin等成分是金钗石斛治疗神经系统疾病的主要药效物质基础,可作用于MIF、ERS2、CYP19A1、ABCG2、TLR9和DRD5等关键靶点,通过调节Sphingolipid signaling pathway、Cocaine addiction及Serotonergic synapse等信号通路来发挥治疗神经系统疾病的作用.结论:本研究揭示了金钗石斛多成分、多靶点、多途径的作用规律,为深入开展金钗石斛治疗神经系统疾病的作用机制研究提供新的依据.

Hypertensive kidney injury (Hki) is one of the most common complications of hypertension. Early prevention and treatment of renal injury in patients with hypertension is great significance. The study, which used an integrated ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS) analysis, network pharmacology approach, and plasma metabolomics, aimed to discover the active ingredients and therapeutic mechanisms of Eucommiae folium (Ef) in treating Hki. The chemical components of Ef were analyzed by UPLC-quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS), and the "compound-target-disease" network was constructed by screening the closely related drug targets from the drug-target database, then the signaling pathways related to Hki were analyzed. Finally, the enzyme-linked immunosorbent assay (ELISA) and real-time quantitative reverse-transcription polymerase chain reaction were used to test and verify the key targets in the common pathways of metabolomics and network pharmacology. The results indicated that Eucommiae folium might play an excellent role in treating Hki, likely through regulating the vascular endothelial growth factor signaling pathway, hypoxia inducible factor 1 (HIF-1) signaling pathway, and glycerophospholipid metabolism pathway, which were validated by increasing levels of nitric oxide, endothelial nitric oxide synthase and reducing levels of endothelin 1, angiotensin II, renin, cyclic guanosine monophosphate, blood urea nitrogen, and serum creatinine, as well as the reduced gene expression of Ache, Ddah2, Egfr, Lcat, Pla2g2a, Stat3 and Vegfa. The study systematically explored the protective mechanisms of Ef against Hki and also provided the practical treatment strategies of Hki from the Chinese herb.

BACKGROUND:The tuber of Pinellia ternata has been used for a thousand years in China. P. ternata possessed the activities of anti-emetic, sedative-hypnotic, anti-cancer, anti-asthmatic, anti-tussive, and anti-inflammatory. It is the representative of expectorant medicines in Traditional Chinese Medicine (TCM). Phlegm is the pathological product and a new pathogenic factor of the metabolite, which is analogous to the damage of oxidative stress.PURPOSE:The objectives of the study were to investigate the protective activity and mechanism of ethanol extract of P. ternata tubers (PTE) and its main constituents on oxidative stress-induced cell senescence.METHODS:H2O2 and AAPH were used to establish cellular senescence models. The anti-aging effects of PTE and its components were evaluated by SA-β-gal staining, flow cytometry, scanning electron microscope (SEM), and multiple microplate reader, the molecular mechanisms of them were investigated by qRT-PCR and Western Blot.RESULTS:We found PTE exhibited the apparent effect on cell senescence, evidenced by inhibiting senescence β-Galactosidase (SA-β-gal) expression, lipofuscin accumulation, cell cycle arrest at the G2/M phase, oxidative damage and apoptosis, and increasing telomerase activity. Their mechanisms were related to increase expressions of SIRT1, forkhead box 3a (Foxo3a), Bcl-2, active regulator of SIRT1, RPS19BP1 (AROS), and Hu antigen R (HuR), but decrease Bax, p53 and deleted in breast cancer 1 (DBC1) levels. Furthermore, adenosine, and succinic acid, as the critical substances in PTE, could also inhibit SA-β-gal expression and cell cycle arrest, down-regulate the expression of Bax, and up-regulate Bcl-2, SirT1, and Foxo3a.CONCLUSIONS:We have demonstrated that PTE slows down oxidative stress-induced cell senescence, and adenosine and succinic acid are the key active components.

茶黄素是一类具有苯骈卓酚酮环结构的天然化合物,具有抗氧化、调血脂、降血糖、抗病毒、抗炎、降尿酸、抗菌、抗肿瘤、抗骨质疏松等药理作用.茶黄素是茶叶天然活性成分的研究重点之一,其在保健食品、医药、化妆品、动物饲料、植物农药等终端产品的开发上越来越广泛.通过查阅近年来有关茶黄素的文献资料,以茶黄素结构的认识为出发点,综述茶黄素的生物活性,关注茶黄素在保健食品、医药等领域中的科学研发与应用,以期为茶黄素的应用开发提供参考.

神秘果中含有的神秘果素,使人在品尝酸味食物时感受到甜味,而不是酸味.近年来,国内外学者研究发现神秘果中含有多种对健康有益的生物活性物质.该文对神秘果的化学成分及其生物活性的研究进展进行总结,以期对神秘果的进一步研究提供参考.

目的:基于网络药理学探究心脑宁胶囊治疗心脑血管疾病(Cardiovascular and cerebrovascular disease,CCVD)的作用机制.方法:本研究依托中药系统药理学平台及文献检索收集心脑宁胶囊所含化合物,通过类药五原则和生物利用度筛选活性化合物,采用Targetnet数据库及CTD数据库获得相关靶点及对应疾病.利用Cytoscape3.5.1网络可视化工具构建网络图.最终通过生物学信息注释库对关键靶点进行生物通路分析.结果:经筛选得到心脑宁胶囊中175个活性化合物,可通过作用于NOS2、NOS3、PTGS2及PTGS1等关键靶点调控VEGF、cAMP及PI3K-Akt等信号通路,对心肌梗塞、心力衰竭、动脉粥样硬化及脑缺血等疾病发挥作用,表明心脑宁胶囊的多成分、多通路共同作用于CCVD的治疗.结论:本研究有助于揭示心脑宁胶囊活性化合物的作用机制.

建立气相色谱内标法测定米糠脂肪烷醇中二十八烷醇和三十烷醇的含量.以三苯基苯为内标物,采用HP-5毛细管色谱柱.二十八烷醇和三十烷醇的加标回收率分别为99.41％和99.48％,相对标准偏差(relative standard deviation,RSD)分别为3.28％和3.17％.该方法适用于米糠脂肪烷醇中高级醇含量分析,为其产品质量的判定提供参考.

目的 基于网络药理学探索甘麦大枣汤改善睡眠障碍的主要活性成分及作用机制.方法 以OB≥20％和DL≥0.18为筛选条件获取活性成分,从TCMSP数据库筛选甘麦大枣汤中各味药的化合物和活性成分相互作用的靶点,并利用Cytoscape软件绘制甘麦大枣汤的C-T网络图,在DrugBank数据库中获得与睡眠障碍相关的靶点,并利用Cytoscape软件构建“成分-靶标-通路”网络图,采用DAVID数据库对靶点基因进行KEGG分析.结果 共获得127个化合物,174个与睡眠障碍相关的靶点,这些靶点主要作用于HIF-1、ErbB、雌激素等10条信号通路.结论 体现了中药多成分-多靶点-多通路特点,为进一步开发甘麦大枣汤为基础的功能产品奠定了基础.

To investigate the pharmacological function localization and action mechanism of persimmon fruit based on network pharmacology, compounds in persimmon fruits were obtained by searching domestic and foreign literatures.The potential targets were predicted by Swiss target prediction database. Species were screened as potential targets for human beings. Compound-target network, target-disease name-disease classification network and PPI network of target protein were constructed by Cytoscape software. Pathway enrichment analysis of target was carried out using DAVID data-base. A total of 16 compounds were collected from persimmon fruits, which could act on 68 targets. Disease types are mainly related to cardiovascular diseases, neuropsychiatric diseases, and other diseases. Protein-protein interaction net-work (PPI) network graph contains 84 nodes and 226 edges. The top 10 degree values of proteins are ERS1, PGS2, MMP2, TIMP1, MMP9, MMP1, AR, SLC6 A3, PRKCB and CYP19 A1. Persimmon fruits may have therapeutic ef-fects on cardiovascular diseases, neuropsychiatric diseases by nitrogen metabolism, serotonergic synapse and inflammatory mediator regulation of TRP channel pathways. This study provides a reliable basis for elucidating the pharmacological function localization and action mechanism of action of persimmon fruits.

目的:整合多元网络分析柿蒂治疗顽固性呃逆的药效物质基础及作用机制.方法:检索中国知网、万方、PubMed和TCMSP等数据库获取柿蒂中的化合物,采用Targetnet数据库对化合物进行潜在靶点预测,将靶点导入CTD数据库获得对应疾病,采用在线分析数据库DAVID对靶点进行基因功能及通路富集分析.最后以Cyto-scape软件构建化合物-靶点网络,靶点-疾病网络.提取度值较高的靶点和化合物及通路,构建“核心化合物-核心靶点-信号通路”核心网络.结果:本研究共收集柿蒂中22个化合物,可作用于77个靶点.通过多元及核心网络分析,柿蒂中的化合物可通过作用于PTPN1、ALOX15、BCL2A1、MIF、ESR2、DNMT1、TLR9等关键靶点,进一步调节Bile secretion pathway、Ovarian steroidogenesis pathway,Steroid hormone biosynthesis pathway等信号通路来发挥治疗各种疾病引起的顽固性呃逆.结论:本研究体现了柿蒂多化合物、多靶点、多途径的作用规律,为深入开展柿蒂治疗顽固性呃逆的作用机制研究提供新的依据.

目的 基于网络药理学分析柿叶治疗心血管疾病的药效物质基础及作用机制.方法 检索Si-noMed、中国知网、万方等数据库获取柿叶中的化学成分,成分录入Targetnet数据库进行潜在靶点钓取,再将靶点导入CTD数据库获得关联疾病,采用DAVID数据库对靶点进行基因功能及通路富集分析.以Cytoscape软件构建成分-靶点网络,靶点-疾病网络,提取核心成分和靶点,构建"核心成分-核心靶点-信号通路"核心网络.结果 共收集到柿叶中54个成分,可作用于43个靶点.多元及核心网络分析结果显示,山奈酚(Kaempferol)、槲皮素(Quercetin)、白花蛇床子素(Droserone)等成分是治疗心血管疾病的主要物质基础,柿叶中的成分主要作用于酪氨酸蛋白磷酸酶非受体1型(PTPN1)、花生四烯酸-15-脂加氧酶(ALOX15)、雌激素受体2(ESR2)、雌激素受体1(ESR1)、前列腺素G/H合成酶1(PTGS1)等关键靶点,进一步调节催乳素信号通路(Prolactin signaling pathway)、血管内皮生长因子信号通路(VEGF signaling pathway)以及花生四烯酸代谢(Arachidonic acid metabolism)等信号通路来发挥治疗心血管疾病的作用.结论 本研究揭示了柿叶多成分、多靶点、多途径的作用规律,为深入开展柿叶治疗心血管疾病的作用机制研究提供了新的依据.

建立高效液相色谱法同时测定木姜叶柯中三叶苷、根皮苷和根皮素的含量.采用C18色谱柱;检测波长285 nm,流动相为乙腈-0.04％甲酸,梯度洗脱;流速0.8 mL/min;柱温40℃.三叶苷、根皮苷和根皮素的加标回收率分别为102.54％、102.01％和102.12％,RSD分别为1.66％、2.21％和2.38％.该方法适用于木姜叶柯中根皮苷、三叶苷和根皮素的含量分析,为其药材质量的判定提供数据参考.

[目的]研究复合红酒素固体饮料(复红固饮)对葡聚糖硫酸钠(dextran sulphate sodium,DSS)诱导的溃疡性结肠炎的预防作用及机制.[方法]本实验采用2.5％ DSS对小鼠进行溃疡性结肠炎造模,将小鼠随机分为正常对照组、模型对照组、阳性药组(0.5 g/kg奥沙拉嗪)、低剂量复红固饮组(2.5 g/kg)及高剂量复红固饮组(5 g/kg).连续灌胃给药7d,记录小鼠体质量并观察结肠炎的症状,第8天断头取血,截取结肠并测定长度,将部分结肠用多聚甲醛固定.测定小鼠血清中肿瘤坏死因子α(tumor necrosis factor-α,TNF-α)及白介素10(interleukin-10,IL-10)的含量.[结果]复红固饮组小鼠急性结肠炎的症状有所缓解,体质量减轻得到抑制,结肠萎缩程度有明显改善,且复红固饮组的血清TNF-α浓度降低,血清IL-10浓度明显升高.复红固饮对结肠黏膜上皮细胞中COX-2的表达也有抑制作用.[结论]复红固饮有明显的预防溃疡性结肠炎的作用,其机制可能与调节体内细胞因子的水平和抑制炎症反应有关.

目的:分析九香虫及相似品的多糖组成.方法:采用水提醇沉法提取多糖,利用苯酚-硫酸法测定多糖含量,通过柱前衍生化HPLC分析单糖组成,使用SIMCA-P软件进行主成分分析(PCA).结果:小皱蝽的多糖含量相对偏高,其次为无刺蝽;九香虫等的多糖主要由甘露糖、鼠李糖、葡萄糖、半乳糖等单糖组成,而小皱蝽的多糖主要由葡萄糖组成;从主成分分析来看,除九香虫外,其他品种能聚合为一类.结论:九香虫及相似品多糖含量、单糖组成存在明显差异.

So far, more than 20 species of Ganoderma (Lingzhi) fungi have been studied, including G. lucidum, G. sinense, G. japonicum, G. capense, G. australe, G. tsugae, G. applanatum, G. tropicus, G. boniense, G. duropora, G. resinaceum, G. theaecolum, G. cochlear, G. atrum, G. formosanum, G. boninense, G. colossum, G. concinna, G. amboinense, G. pfeifferi, and G. orbiforme. Over 600 compounds were isolated and identified from the genus Ganoderma. The components in Ganoderma contained triterpenes, meroterpenoids, steroids, alkaloids, nucleosides, nucleobases, and polysaccharides, in which triterpenes were the main compounds, and more than 300 triterpenes obtained from it. With the use of new technology of separation and purification, the other types of compounds, such as meroterpenoids, alkaloids, nucleosides, and polysaccharides were reported in recent years. Herein, the structural classifications and characteristics and separation methods were summarized.

以白树(Suregada glomerulata)中分离得到的五个氮杂糖成分为底物,在其N上衍生合成,分析N上衍生基团对α-葡萄糖苷酶抑制活性的影响.分别合成了N-甲基化、N,N-二甲基化、N-丁基化和N-氧化衍生物,体外测试化合物的α-葡萄糖苷酶抑制活性.合成了7个未见文献报道的目标化合物,结构经1H NMR、13C NMR和MS确证.初步药理结果显示,所有衍生物均未见增强α-葡萄糖苷酶抑制活性.N-取代基对活性的影响较大;化合物5属于N,N-二取代衍生物,仍具有一定的α-葡萄糖苷酶抑制活性,值得进一步研究.