黔产莪术精油的化学成分研究

为了解黔产莪术药材的品质,用GC／MS从黔产获术精油中共检出67个成分,鉴定了其中37个化合物,主要成分为莪术酮（curzerenon）45．02％,莪术烯醇（curcumenol）8．31％,β-榄香烯（β-elemene）5．79％,异莪术烯醇（iso-curcumenol）4．05％,黔产莪术精油抗肿瘤活性成分较高。     

温莪术药渣再提取工艺及其美白活性研究CSCD

以活性成分总姜黄素得率为指标,响应面法优化温莪术药渣的最佳提取工艺,采用DPPH法和ABTS法评价温莪术药渣提取物的抗氧化活性,并考察其对小鼠黑色素瘤B16细胞存活率、黑色素合成及其细胞内酪氨酸酶活性的影响。实验结果表明,温莪术药渣提取物的最佳工艺条件为乙醇浓度82%,超声时间55 min,液料比22 mL/g,总姜黄素平均提取得率为6.38 mg/g;此外,温莪术药渣提取物对DPPH、ABTS自由基具有一定的清除作用,IC_(50)值分别为24.99、49.72μg/mL;并且能有效抑制B16细胞黑色素合成及酪氨酸酶活性,与正常组相比均具有显著性差异(P<0.05)。本研究为温莪术提油后药渣二次开发利用提供了依据。     

广西莪术关键采收月份挥发性成分的差异及动态变化研究北大核心CSCD

为探究4个采收月份(即2018年的12月和2019年的1月、2月、3月)广西莪术挥发性成分的差异性及动态变化规律,该研究利用气相色谱-质谱联用仪(GC-MS)对挥发性成分进行分析鉴定,并运用化学计量学方法对相对含量在1%以上的挥发性成分进行数据分析。结果表明:经GC-MS分析均鉴定出34种挥发性成分,不同采收月份广西莪术挥发性成分相对含量存在差异性;主成分聚类分析均分为4类,采用偏最小二乘法判别分析发现7个差异性化合物,其中莪术呋喃二烯酮的含量在1月份达到峰值,吉马酮和humulene 2,3-epoxide两个化合物的相对含量均在2月份达到最高,莪术烯、萜品油烯、异龙脑和表莪术呋喃烯酮在3月份达到峰值。该研究结果为广西莪术的质量控制、生长过程控制以及其他开发研究提供了参考依据。     

基于薄层色谱-生物自显影-MSn法表征枸骨叶中的脂肪酶抑制活性成分CSCD

为寻找枸骨叶的降脂减肥活性成分,本文采用薄层色谱-生物自显影法,筛选其具有脂肪酶抑制活性的成分,再通过原位TLC-EFISI-MSn技术,对具有脂肪酶抑制活性的成分进行快速结构解析。通过对10个具有脂肪酶抑制活性的薄层色谱-生物自显影斑点进行快速解析,初步鉴定出15个可能的成分,包括9个熊果烷型三萜、1个齐墩果烷型三萜,以及5个18,19-裂环型三萜,其中有7个活性斑点所包含的12个化合物通过对照品比对得到验证。该方法能够快速从枸骨叶中筛选、表征出具有脂肪酶抑制活性成分,从而为确定枸骨叶活性成分的筛选和鉴定提供依据。     

蝉花抗真菌活性成分的分离纯化研究

通过抗真菌实验进行活性跟踪,采用NKA大孔吸附树脂和硅胶两步柱色谱对蝉花中抗真菌活性成分进行分离纯化;并通过红外、质谱进行结构鉴定。结果表明,分离得到的抗真菌活性成分为多球壳菌素,对真菌的最小抑制浓度为0.02 mg/mL。本研究为进一步研究蝉花及制备医药工业所需的多球壳菌素提供了依据。     

黄皮属植物中香豆素成分及其药理活性研究进展

本文在前期对黄皮属植物中香豆素成分研究的基础上,结合系统的文献调研,对芸香科黄皮属植物中香豆素成分结构类型、检测、提取分离、结构鉴定及其药理活性的研究进展进行了归纳和总结。     

杨小舟蛾雌蛾性信息素活性成分的鉴定

【目的】鉴定杨小舟蛾Micromelalopha sieversi雌蛾性信息素活性成分的结构信息。【方法】采用正己烷浸提的方法提取杨小舟蛾性成熟处女雌蛾性腺中的活性成分;利用气相色谱-触角电位联用(GC-EAD)技术对其活性成分进行定位;性腺提取物与4-甲基-1,2,4-三唑啉-3,5-二酮(MTAD)进行微量化学反应,获得衍生物;利用气相色谱-质谱联用(GC-MS)技术分别对性腺提取物及MTAD衍生物进行质谱特征离子分析。【结果】GC-EAD结果显示,杨小舟蛾雄蛾触角对雌蛾性信息素腺体提取物中的一种成分有较好的反应;GC-MS分析结果表明,能引起雄蛾触角电生理反应的成分为十八碳的不饱和醛;MTAD衍生物的GC-MS结果显示,该活性成分的两个双键分别位于碳链的13和15位。【结论】本研究鉴定出杨小舟蛾雌蛾性信息素活性成分的平面结构为13,15-十八碳二烯醛,但双键的立体构型有待合成标准化合物进一步鉴定。本研究为杨小舟蛾性信息素备选化合物的筛选提供了方向,为信息素的结构确证奠定了基础。     

甘草属植物化学和药理学研究进展

本文对近年发表的有关甘草属植物化学和药理学研究文献进行了综述,其中包括了得自本属植物的新的黄酮类、三萜类成分。文中以表格形式列出了各类成分的名称、结构、物理常数和植物来源,并对某些成分的生理活性作了归纳。     

化学工业出版社新书

天然活性成分生物技术制备方法杨文宇、牛锐、韩丽主编,ISBN978-7-122-00853-4,2007年8月出版本书以天然活性成分的类型为线索,系统阐述各种结构类型活性成分的生物技术制备方法以及最新的研究成果。本书涉及的天然活性成分类型较全,包括生物碱,黄酮,皂苷,一些结构简单的苷及苷     

菊科植物二萜类成分研究进展

二萜类是广泛存在于菊科植物中的一类特征成分,结构多样,一直备受植物化学家的关注。本文就菊科植物中该类成分的结构和主要活性进行综述,以期为它们的进一步开发利用提供依据和参考。     

杨树溃疡病生防菌株N6-34抗菌活性物质的分离纯化与结构鉴定

【背景】杨树溃疡病是一种主要由葡萄座腔菌引起的杨树枝干病害,危害严重。前期从杨树中分离到一株内生拮抗细菌N6-34,研究表明该菌株拮抗效果好,对多种植物病原菌均有较强的拮抗作用。【目的】对拮抗细菌N6-34产生的抗菌活性物质进行分离纯化,并鉴定了活性物质组分的结构。【方法】通过硫酸铵盐析、甲醇抽提、分子筛、高效液相色谱等方法分离纯化N6-34菌株的抗菌活性物质,并对其进行结构鉴定。【结果】N6-34菌株发酵液经多步分离纯化,共获得14个组分,其中有13个组分具有抗菌活性,经一级质谱分析,获得了13种抗菌活性组分的分子量;经二级质谱分析,将13种抗菌活性物质鉴定为Fengycin A或Fengycin B的同系物或同分异构体。【结论】从N6-34菌株发酵液中分离获得了13种抗菌成分,为杨树溃疡病的生物防治提供了理论依据。     

Prunella stica inhibits the proliferation but not the prostaglandin production of Ishikawa cells

Chinese herbs have been used to relieve dysmenorrhea associated with endometriosis. Active components in the herbs and their mechanisms of action remain unknown. Prunella stica, a Chinese herb commonly used to treat dysmenorrhea, was chosen for the present studies. Its effects were investigated on Ishikawa cells, an epithelial cell line derived from human endometrium. Cell proliferation and inhibition of interleukin 1beta (IL-1beta) induced prostaglandin (PG) production were examined. To learn more about the active components, 120 fractions were collected from the crude extract and each fraction was tested individually. To further characterize the active components, aliquots of fractions with activity were subject to mass spectrometry analysis. Crude extract of P. stica inhibited the proliferation of Ishikawa cells but not the IL-1beta induced PG production. Active components of P. stica clustered around fractions 64 and 92; they increased cell doubling time from 18.6 to 26.2 and 29.4h, respectively. Mass spectrometry analysis showed fractions 64 and 92 consisted of three components whose molecular weights were 337, 348 and 430 Daltons. The therapeutic effects of P. stica reside, in part, in inhibiting the proliferation of the epithelial cells derived from human endometrium. The active components are small molecules.     

Preventing sexual transmission of HIV: anti-HIV bioregulatory and homeostatic components of commercial sexual lubricants

Certain safe over-the-counter (OTC) sexual lubricants such as Astroglide, KY Liquid, Replens, Vagisil, ViAmor, and Wet Stuff inhibit both cell-free HIV and the production of HIV by infected leukocytes in vitro even in the presence of seminal fluid. To identify which components of the lubricants were active against HIV, we tested five components (glycerin, methylparaben, propylparaben, polyquaternium-32, and propylene glycol). The paraben preservatives and propylene glycol in the lubricants did not inhibit HIV, while the common natural homeostatic metabolite, glycerin, and the thickener polyquaternium-32 did strongly inactivate infectious HIV and HIV-infected leukocytes. Activity against HIV and HIV-infected cells by glycerin was stable through 24 hours at 37 degrees C. Glycerin and polyquaternium-32 were active at minimum concentrations of approximately 2% and 0.01%, respectively--well within the highest FDA safety guidelines. Both active components disrupted infected leukocytes within 5 minutes which resulted in inhibition of infectious HIV production by infected leukocytes of greater than 25 to 100-fold. These components do not disrupt vaginal epithelial cells in vivo.These components also rapidly inactivate cell-free HIV by 10- to 30-fold. Thus, we may conclude that the active components of the OTC lubricants are glycerin and polyquaternium-32. Using these components, OTC sexual lubricants could be reformulated to optimize their anti-HIV activity. Furthermore, clinical trials of these lubricants and components seem to be indicated because of their FDA safety level, wide availability, and low cost.     

Identification of a delta-Endotoxin Gene Product Specifically Active against Spodoptera littoralis Bdv. among Proteolysed Fractions of the Insecticidal Crystals of Bacillus thuringiensis subsp. aizawai 7.29

At least three different insecticidal crystal protein genes were shown to be expressed in Bacillus thuringiensis subsp. aizawai 7.29, a strain that is potentially active against the cotton leafworm Spodoptera littoralis Bdv. Among crude K-60 fractions (60- to 70-kilodalton [kDa] molecules) that were products of proteolysed crystals containing the active domains of the protoxin molecules, we were able to distinguish several distinct components on the basis of their antigenic relationship and their larvicidal properties. A purified fraction designated SF2 was a 61-kDa component specifically active against Pieris brassicae L. and homologous to the B. thuringiensis subsp. berliner 1715 plasmid-encoded crystal protein. A second fraction designated SF1 was composed of 63- and 65-kDa polypeptides and was specifically active against S. littoralis. The SF1 fraction and particularly the 65-kDa component were not antigenically related to the 61-kDa component. The purified fractions were compared with the products of three different crystal protein genes we previously cloned from total DNA of B. thuringiensis subsp. aizawai, among them a new type of crystal protein gene encoding a protein that is specifically active against S. littoralis and other insects of the Noctuidae family. This approach led us to consider the 65-kDa component as a minimum active part of a delta-endotoxin that is encoded by this new gene. Products of the two other cloned genes can be correlated with the 61- and 63-kDa components, respectively. Thus, in B. thuringiensis subsp. aizawai 7.29, multiple delta-endotoxin genes of different structural types direct the synthesis of several delta-endotoxins with different host specificities which were identified as components of the insecticidal crystals.     

抗肿瘤动物类中药的研究进展

动物类中药资源丰富,其在肿瘤治疗中取得的疗效引起医药领域广泛关注,已成为抗肿瘤药物的一个新的研究热点。然而,抗肿瘤动物类中药成分复杂,其有效成分和作用机制尚有待进一步明确。综述常用抗肿瘤动物类中药及其活性成分、抗肿瘤动物类中药作用机制与临床应用,以期为抗肿瘤动物类中药的深入研究与开发提供参考。     

Components of human complement system. Testing and isolation of C3 and C5

Modified reagents for testing the hemolytic activity of human complement components, C3 and C5, have been obtained. These reagents were obtained by treatment of human blood serum pools with a saturated solution of KBr (reagent R3) or 2 M KSCN and denaturated yeasts (reagent R5). These reagents were found to be rich in the serum factor obtained through the use of DEAE-cellulose DE-52 and containing the active component of the complement (C4). To test the sensitivity and specificity of the above reagents, components C3 and C5 were purified. After this procedure these components emerged as hemolytically active, electrophoretically and immunophoretically homogeneous components, C3 and C5. DEAE-cellulose DE-52, DEAE-Sephacel, Hydroxylapatite and Ultra-gel AcA-34 were used consecutively as purification agents. The activity yields of components C3 and C5 with regard to the initial serum levels were 31% and 18%, respectively.     

Active spice-derived components can inhibit inflammatory responses of adipose tissue in obesity by suppressing inflammatory actions of macrophages and release of monocyte chemoattractant protein-1 from adipocytes

Inflammation plays a key role in obesity-related pathologies such as cardiovascular disease, type II diabetes, and several types of cancer. Obesity-induced inflammation entails the enhancement of the recruitment of macrophages into adipose tissue and the release of various proinflammatory proteins from fat tissue. Therefore, the modulation of inflammatory responses in obesity may be useful for preventing or ameliorating obesity-related pathologies. Some spice-derived components, which are naturally occurring phytochemicals, elicit antiobesity and antiinflammatory properties. In this study, we investigated whether active spice-derived components can be applied to the suppression of obesity-induced inflammatory responses. Mesenteric adipose tissue was isolated from obese mice fed a high-fat diet and cultured to prepare an adipose tissue-conditioned medium. Raw 264.7 macrophages were treated with the adipose tissue-conditioned medium with or without active spice-derived components (i.e., diallyl disulfide, allyl isothiocyanate, piperine, zingerone and curcumin). Chemotaxis assay was performed to measure the degree of macrophage migration. Macrophage activation was estimated by measuring tumor necrosis factor-alpha (TNF-alpha), nitric oxide, and monocyte chemoattractant protein-1 (MCP-1) concentrations. The active spice-derived components markedly suppressed the migration of macrophages induced by the mesenteric adipose tissue-conditioned medium in a dose-dependent manner. Among the active spice-derived components studied, allyl isothiocyanate, zingerone, and curcumin significantly inhibited the cellular production of proinflammatory mediators such as TNF-alpha and nitric oxide, and significantly inhibited the release of MCP-1 from 3T3-L1 adipocytes. Our findings suggest that the spice-derived components can suppress obesity-induced inflammatory responses by suppressing adipose tissue macrophage accumulation or activation and inhibiting MCP-1 release from adipocytes. These spice-derived components may have a potential to improve chronic inflammatory conditions in obesity.     

In Vitro Incorporation of Molybdate into Demolybdoproteins in Escherichia coli

When Escherichia coli was grown in the presence of tungstate, inactive forms of two molybdoenzymes, nitrate reductase and formate dehydrogenase, accumulated and were converted to their active forms upon incubation of cell suspensions with molybdate and chloramphenicol. The conversion to the active enzymes did not occur in cell extracts. When incubated with [(99)Mo]molybdate and chloramphenicol, the tungstate-grown cells incorporated (99)Mo into protein components which were released from membranes by procedures used to release nitrate reductase and formate dehydrogenase and which migrated with these activities on polyacrylamide gels. Although neither activity was formed during incubation of the crude extract with molybdate, (99)Mo was incorporated into protein components which were released from the membrane fraction under the same conditions and were similar to the active enzymes in their electrophoretic properties. The in vitro incorporation of (99)Mo occurred specifically into these components and was equal to or greater than the amount incorporated in vivo under the same conditions. Molybdenum in preformed, active nitrate reductase and formate dehydrogenase did not exchange with [(99)Mo]molybdate, demonstrating that the observed incorporation depended on the demolybdo forms of the enzymes. We conclude that molybdate may be incorporated into the demolybdo forms both in vivo and in vitro; some unknown additional factor or step, required for active enzyme formation, occurs in vivo but not in vitro under the conditions employed.     

Effects of Growing Location on the Contents of Main Active Components and Antioxidant Activity of Dasiphora fruticosa (L.) Rydb. by Chemometric Methods

Traditional Chinese Medicine (TCM) is a very important raw material source for natural medicines in China. The content and activity of active component are main indexes that evaluate the quality of TCM, however, they may vary with environmental factors. In this study, the effects of environmental factors on the active component contents and antioxidant activity of Dasiphora fruticosa collected from the five main growing areas of China were investigated. The contents of tannin, total flavonoids and rutin were determined to be 7.65 – 10.69%, 2.30 – 5.39% and 0.18 – 0.81%, respectively. Antioxidant activity was determined by DPPH assay, with the DPPH IC₅₀ values ranged from 8.791 to 32.534 μg mL^?1. In order to further explore the cause of these significant geographical variations, the chemometric methods including correlation analysis, principal component analysis, gray correlation analysis and path analysis were applied. The results showed that environmental factors had significant effect on the contents of active components and antioxidant activity. Rapidly available phosphorus (RAP) and rapidly available nitrogen (RAN) were common dominant factors, and a significant positive action existed between RAP and active components and antioxidant activity (P < 0.05). Contributed by their high active components and strong antioxidant activity, Bange in Tibet and Geermu in Qinghai Province were selected as a favorable growing location, respectively.     

毛脉酸模不同器官中几种生物活性物质的含量及生长季节对其的影响

为确定毛脉酸模(Rumex gmelini)最佳药用部位和最佳采收期, 从而为新药源开发提供科学依据, 我们采用HPLC法和梯度洗脱, 研究了一年生和二年生毛脉酸模不同生长发育期、不同器官、组织中7种生物活性成分(白藜芦醇、白藜芦醇苷、大黄酚苷、酸模素、大黄素、大黄酚和大黄素甲醚)的动态分布规律。结果表明毛脉酸模根部含有生物活性成分的种类及含量均多于其他部位, 为最佳药用部 位。一年生毛脉酸模根部不含有酸模素。二年生毛脉酸模根部含有全部7种生物活性成分, 且在8~9月份含量最高, 为最佳采收期。