药物对福氏志贺氏菌代谢抑制的微量热法研究

药物抑制细菌生长的热化学研究是当今热化学法研究的一个活跃领域．在这项研究中，Boling[1]、Nordmark[2]、屈松生[3]等人已做了不少有意义的工作．在前人工作的基础上，我们用热活性检测系统测定了福氏志贺氏菌属中五株细菌在药物抑制下生长的完整的热谱曲线．按指数生长模型计算出细菌代谢抑制下的生长速车常数，并用计算机拟会出生长速率常数与不同浓度药物之间的关系式，进一步得到生长速率常数为零（临界生长参数[4]）时的用药物浓度．此项研究工作的开展对于深入研究药物对细菌的抑制作用，筛选对某细菌抑制的特效药提供了一种新的…     

微量量热法筛选抑菌特效药的研究

用微量最热计连续测定细菌代谢过程中的热显变化，可获得反映细菌代谢规律的完整的热谱图以按指数生长模型对指数生长期进行处理，可计算出细菌正常代谢的生长速率常数L’．若在培养基中加入合成药物，使细菌在药物抑制作用下生长，也可获得完整的热谱图，从而计算出在药物抑制作用下细菌的生长速率常数．本义对福氏志贺氏Zb菌和金黄色葡萄球莉在四种合成药物抑制作用下的热谱进行了测定，并计算了生长速率常数，找出了细菌生长速率常数与所用药物浓度之间的定量关系，可为筛选抑菌药物和确定用药显提供定量依据’1基本原理设细菌在代谢过…     

葡萄糖氧化酶光敏氧化反应过程的毛细管电泳法监测

生物学研究表明，叶琳和酞著衍生物对癌变组织具有亲和性[1]．此类物质在吸收特定波长的光之后产生活性氧，可光敏氧化生物分子，并杀死癌细胞．光动力疗法对脑癌、颈癌和服癌等浅层癌具有明显的疗效[2]，研究各种光敏剂与生物大分子的作用机理[3，4]，对筛选新型光疗药物，改进光疗效果具有重要价值．癌细胞中葡萄糖的代谢非常旺盛，若阻断这种代谢，有可能实现对癌细胞进行代谢调控的目的．因此，本文选用葡萄糖氧化酶为模型化合物，用毛细管电泳法监测了4种新型光敏剂[ZnPcS4，ZnPc（NHCH2COOH）4，C1A1PcS，Por－Phyrine－like]…     

3，5-二氟-4-碘-苯甲醚的合成

生物活性含氟化合物作为活性强、选择性高的药物[1]及农药[2]已广泛应用;生物活性含氟化合物可以作为标记化合物模拟体内代谢过程[3],在酪氨酸分子的一定位置上氟代后,用电子能量损耗光谱可以对酪氨酸及其代谢产物进行分子水平的跟踪,而且酪氨酸分子中某些特定位置上的氢原子被     

[CuCl3CPZ(O)H]络合物的合成及电化学行为的研究

盐酸氯丙嗪目前在精神病治疗中作为首选药物之一，在临床上应用于精神分裂症、狂躁症、焦虑症及更年期精神病等症．该药物吩唾咪环比较容易被氧化；1982年Geary等[1]合成了该药物的钯络合物，并对其进行了X-今线结构分析．Kawazura等[2,3]研究了该药物与体内微量元素之间的相互作用；Holbrok山研究表明用盐酸氯丙埃后脑内铜的浓度上升．而服用后药物先与蛋白质结合，与金属离子反应的可能性较小；为此本文制备了该药物的主要代谢产物之一的CPZ（0）HCI，并与体内微量元素铜（11）络合得到KUQa＊Pz问仰，对该络合物进行了元素分析和电…     

细菌生长的热动力学研究进展

本文简单介绍了绝热式和热导式量热计及理论模型,细菌生长的动力学模型,着重介绍了近五年中热动力学在研究细菌生长代谢过程中的应用;通过测定不同条件下细菌生长代谢过程的产热曲线,求得细菌生长代谢的热力学和动力学参数,研究细菌的生长条件和药物的抑制作用。     

从红树林内源真菌2526#分离到Sterigmatocystin

从海洋资源中寻找药物已越来越受到重视 ,已有的研究表明海洋资源有可能成为治疗人类疑难病症和延年益寿药物的丰富源泉[1] 。本研究组在从海洋微生物筛选新药的过程中 ,已发现多种结构奇特而具有强生理活性的化合物[2～ 4 ] 。Ｓｔｅｒｉｇｍａｔｏｃｙｓｔｉｎ最早分离自陆生真菌Ａｓｐｅｒｇｉｌｌｕｓｖｅｒｓｉｃｏｌｏｒ的代谢产物[5] ,随后人们对其结构、生源合成及药理活性进行了广泛的研究。结果表明 ,ｓｔｅｒｉｇｍａｔｏｃｙｓｔｉｎ是细胞毒性更强的化合物ＡｆｌａｔｏｘｉｎＢ1的生源合成前体。本文报道从采自香港红树Ａｖｉ…     

红树林真菌Penicillium sp．No．ZZF33发酵液化学成分的研究

海洋微生物是寻找药物先导化合物的一个新的源泉,人类已从海洋微生物的次级代谢产物中发现了许多有生物活性的结构新颖的化合物[1]。近几年,本研究组对来自南中国海红树林的海洋真菌的代谢产物进行了系统的研究,从中发现大量有生物活性的化合物,揭示了红树林真菌的巨大应用潜力     

锗—132对体外幼鼠胰岛细胞的作用

自1968年浅井等人[1]首次合成了乙基锗倍半氧化物（即Ge-132）以来，对Ge-132生物活性的研究已有诸多报道[2]．近年来，日本学者[3]在研究Ge-132药物活性作用机理时认为，Ge-132有可能成为防治糖尿病及其并发症的有效药物．但还没能从分子水平来阐明有机锗的作用机理．为揭示上述作用的细胞学机制，我们观察了Ge-132及Ge2。对体外培养的幼鼠胰岛细胞结构和功能的影响，比较了两者的差异．认为一定浓度的Ge-132对体外培养的幼鼠胰岛细胞分泌胰岛素具有明显的促进作用，为开发利用有机锗药物治疗糖尿病及其并发症提供了重要的依据．一周龄…     

抗癌药物阿克拉霉素-A的氧化还原代谢机理研究

大多数化疗药物因很强的毒副作用在临床应用中受到很大的限制,阿克拉霉素为蒽环药物家族新成员,因其抗癌活性高和毒副作用低在抗肿瘤药物中占有重要地位．本论文将药物置于代谢模型内,以光谱技术现场监测药物的代谢过程,研究了阿克拉霉素-A的氧化还原代谢机理．阿克拉霉素．A在体内的代谢过程为先通过一步二电子过程还原生成阿克拉氢醌．A,再脱去糖．其脱糖反应与介质的pH密切相关．脱糖、异构化后的产物7-去氧阿克拉霉醌经缔合后可生成双分子缔合物．整个代谢过程中并不产生半醌自由基,因而对心脏和细胞的毒性较小．研究结果同时也表明药物分子中的糖环结构与药物代谢及药物的毒副作用密切相关．研究成果有助于深入探讨药物的构效关系,对药物的临床应用有着重要的实际意义．     

人参连作土壤对不同生育期人参生长发育及抗氧化系统的影响

人参产业是吉林省的特色支柱健康产业,但由于人参连作障碍的限制,使得人参产业面临着资源枯竭。通过探究人参连作土壤对正常人参生长发育的影响,研究破解人参连作障碍。以正常生长的盆栽人参样本为对照组（Control Check, CK）,以连作土壤种植人参样本为模型组（Continuous Crop obstacles, CCO）,从植物组织形态、生理生化水平和组织内抗氧化水平等3个方面,系统分析了不同生长时期连作土壤对正常人参生长发育的影响。结果表明,CCO组人参植株的株高、主根长、须根数在采收期较CK组相比具有显著差异（P<0.05）。在果实期和采收期,CCO组样本组织内过氧化氢酶（CAT）活性显著降低,丙二醛（MDA）含量显著增加（P<0.05）;在采收期,与CK组比较,CCO组人参过氧化物酶（POD）的活性显著增加（P<0.05）,超氧化物歧化酶（SOD）活性显著降低（P<0.05）,表明人参连作土壤可显著影响对正常人参植株的氧化应激水平与生长发育两个方面,如果能够通过土壤改良的方法,破解连作难题,则将有效解决吉林省的人参种植领域瓶颈问题。     

Enhanced secondary metabolite biosynthesis by elicitation in transformed plant root system

Plants generally produce secondary metabolites in nature as a defense mechanism against pathogenic and insect attack. In this study, we applied several abiotic elicitors in order to enhance growth and ginseng saponin biosynthesis in the hairy roots of Panax ginseng. Generally, elicitor treatments were found to inhibit the growth of the hairy roots, although simultaneously enhancing ginseng saponin biosynthesis. Tannic acid profoundly inhibited the hairy root growth during growth period. Also, ginseng saponin content was not significantly different from that of the control. The addition of selenium at inoculum time did not significantly affect ginseng saponin biosynthesis. However, when 0.5 mM selenium was added as an elicitor after 21 d of culture, ginseng saponin content and productivity increased to about 1.31 and 1.33 times control levels, respectively. Also, the addition of 20μM NiSO₄ resulted in an increase in ginseng saponin content and productivity, to about 1.20 and 1.23 times control levels, respectively, and also did not inhibit the growth of the roots. Sodium chloride treatment inhibited hairy root growth, except at a concentration of 0.3% (w/v). Increases in the amounts of synthesized ginseng saponin were observed at all concentrations of added sodium chloride. At 0.1% (w/v) sodium chloride, ginseng saponin content and productivity were increased to approx, 1.15 and 1.13 times control values, respectively. These results suggest that processing time for the generation of ginseng saponin in a hairy root culture can be reduced via the application of an elicitor.     

Ultra-performance LC/TOF MS analysis of medicinal Panax herbs for metabolomic research

In this study, metabolite profiling of five medicinal Panax herbs including Panax ginseng (Chinese ginseng), Panax notoginseng (Sanchi), Panax japonicus (Rhizoma Panacis Majoris), Panax quinquefolium L. (American ginseng), and P. ginseng (Korean ginseng) were performed using ultra-performance LC-quadrupole TOF MS (UPLC-QTOFMS) and multivariate statistical analysis technique. Principal component analysis (PCA) of the analytical data showed that the five Panax herbs could be separated into five different groups of phytochemicals. The chemical markers such as ginsenoside Rf, 20(S)-pseudoginsenoside F11, malonyl gisenoside Rb1, and gisenoside Rb2 accountable for such variations were identified through the loadings plot of PCA, and were identified tentatively by the accurate mass of TOFMS and partially verified by the available reference standards. Results from this study indicate that the proposed method is reliable for the rapid analysis of a group of metabolites present in herbal medicines and other natural products and applicable in the differentiation of complex samples that share similar chemical ingredients.     

Translational Enhancer of Tobacco mosaic virus Enhancing Expression of Hepatitis B Surface Antigen in Transgenic Panax ginseng C. A. Meyer Callus

The 5＇-nontranslated leader（omega sequence） of Tobacco mosaic virus（TMV） was used as a translational enhancer sequence in the expression of the hepatitis B surface antigen（HBsAg） gene in transgenic ginseng callus cultures. The adr subtype HBsAg gene was placed under the control of the Cauliflower mosaic virus（CaMV） 35S promoter linking to the TMV leader sequence. The antisense omega sequence was used in a control construct. The resulting constructs cloned in the binary vector pBI121 were used to transform the ginseng callus tissue via the Agrobacterium-mediated procedure. The integration and expression of the HBsAg gene were evaluated by PCR and western blot, respectively. Enzyme-linked immunoassays（ELISA） using a monoclonal antibody directed against human serum-derived HBsAg revealed a three to four-fold enhanced expression of HBsAg in ginseng cells conferred by the TMV omega element.     

Determination of power-time curves of Staphylococcus aureus growth and study of promoter action of a ginseng

The powervs. time curves ofStaphylococcus aureus were determined by using a 2277 Thermal Activity Monitor (Sweden). By means of a new model of microorganism growth, the growth rate constants at different concentrations of ginseng and the minimum concentration were calculated from these curves.     

Production of antioxidant compounds by culture of Panax ginseng C.A. Meyer hairy roots

Ginseng (Panax ginseng C.A. Meyer) hairy root cultures, established by infecting ginseng root discs with Agrobacterium rhizogenes, were used for secondary metabolite production. In this study, several elicitors [salicylic acid (SA), acetylsalicylic acid (ASA), yeast elicitor, and bacterial elicitor] were used to improve the productivity of useful metabolite in P. ginseng hairy root cultures. In SA elicitation, total ginseng saponin content increased slightly at lower elicitor dosages (0.1 to 0.5 mM). Also, the use of ASA as an elicitor resulted in the inhibition of biomass growth and an increase in total ginseng saponin content at every elicitor dosage (0.1 to 1.0 mM) by about 1.1 times. With yeast elicitor addition, hairy root growth was inhibited about 0.8-fold on a dry weight basis compared to the control, but total ginseng saponin content increased by about 1.17 times when compared to the control. The bacterial elicitor showed a slight inhibition of biomass growth, but total ginseng saponin content increased by about 1.23 times upon the addition of 1 mL.     

Research Progress on the Continuous Cropping Obstacles of Ginseng from Soil Improvement北大核心CSCD

The unique black soil resources and natural environment of Jilin province provide the proper conditions for the growth of ginseng-the king of herb. Ginseng industry has effectively promoted the development of medical and health industry，and brought considerable economic income for ginseng farmers. However，long-term continuous cropping of ginseng causes the chemical，biological，and physical properties deterioration of soil，which influences the yield and the quanlity of ginseng，and results in the occurrence of replant obstacle. Identifying the malignant soil factors in continuous cropping obstacles，then analyzing the evolution process，and putting forward the improvement strategies is the primary task of ginseng research at present. This paper reviews the influence of ginseng cultivation on the physicochemical property，nutrient， enzyme activity，microecology and ecotoxicity of the soil，and the achievements of improving ginseng soil by chemical and biological techniques and methods in recent 10 years. © 2022, Science Press (China). All rights reserved.     

气相色谱-三重四极杆质谱分析人参炮制品中的挥发性成分

人参炮制的化学成分变化研究主要集中在皂苷和糖类,本文首次从挥发性成分角度阐释了人参不同炮制品的物质基础。利用气相色谱-质谱联用(GC-MS/MS)方法,对鲜参、生晒参和红参中挥发性成分及其衍生规律进行研究。采用TG-5SILMS非极性气相色谱柱,以He为载气,通过NIST MS Spectral Database对挥发性成分进行检测并鉴定。鲜参、生晒参、红参中分别检出30、33和34种挥发性成分,其中生晒参中(-)-斯巴醇含量为鲜参含量的31.98倍,辛醛等8种挥发性成分为鲜参中含量的3倍以上,红参中有环癸等10种挥发性成分为鲜参中含量的3倍以上。生晒参和红参中各有4种挥发性成分在鲜参中未检出。     

Sensitive high-performance liquid chromatography method of non-polar ginsenosides by alkaline-enhanced pulsed amperometric detection

We determined the minute amount of non-polar ginsenosides in red ginseng with a reversed-phase high-performance liquid chromatography-pulsed amperometric detection (RP-HPLC-PAD) method. Non-polar ginsenosides efficiently extracted by ethyl acetate were well separated in 40 min using a water–acetonitrile gradient eluent and detected by PAD under NaOH alkaline conditions. The ginsenoside detection limits (S/N = 3) were 0.03–0.10 ng. The coefficients of linear regression were 0.9972–0.9990. Intra- and inter-day precision (RSDs) was less than 8.34% and average recovery was 98.06–102.73%. The total amount of non-polar ginsenosides in hairy root of red ginseng was slightly higher than in the main root.     

A new compound with cytotoxic activities from the leaves of Panax ginseng C.A. Meyer

A new compound, 3,6,20（S）-trihydroxy- 12,23-epoxydammar-24-ene,6,20-di-O-β-D-glucopyranoside （1）, was isolated from the leaves of Panax ginseng C.A. Meyer, whose structural elucidation was carried out by means of spectral analysis （including IR, HR- FAB-MS and NMR）. This compound showed the moderate cytotoxic activities against U937 and HeLa cells by using the MTT method.