尼泊尔菊三七的离体快繁技术研究

目的依据尼泊尔菊三七野生资源开发利用情况,以尼泊尔菊三七的茎段为外植体,建立其离体快繁体系。方法通过正交设计法,添加不同浓度激素[6-苄氨基嘌呤(6-BA)和萘乙酸(NAA)]、无机元素和活性炭,建立包括丛生芽诱导、生根、壮苗以及移栽的离体快繁体系。结果用75%乙醇和0.1%升汞对外植体消毒的时间分别为20 s,6 min;尼泊尔菊三七离体快繁的最佳增殖培养条件为MS+萘乙酸0.5 mg/L+6-苄氨基嘌呤1.0 mg/L+蔗糖30 g/L+琼脂5.0 g/L,pH=6.0;壮苗生根的最佳培养条件是1/2 MS+萘乙酸0.5 mg/L+6-苄氨基嘌呤1.0 mg/L+蔗糖30 g/L+活性炭2.0 g/L+琼脂5.0 g/L,pH=6.0;移栽期间的最佳基质是腐殖土∶木炭土=3∶2。结论成功建立尼泊尔菊三七离体快繁体系,为将来大规模生产奠定了基础。     

人胎儿球结膜成纤维细胞的离体培养

为使离体成纤维细胞培养条件更符合正常人眼组织生物学特点，笔者取材人胎儿球结膜培养成纤维细胞获得成功。本文介绍了培养的方法。     

西洋参组织细胞培养及其代谢产物研究概况

对西洋参试管苗的再生、组织细胞的几种培养方法、细胞生长及人参皂苷合成的影响因素做了全面的综述。指出利用西洋参组织细胞培养技术进行人参皂苷工业化生产具有可行性     

太子参保健酒对小鼠离体肠平滑肌的研究

目的：观察太子参保健酒对小鼠离体肠平滑肌收缩活动的影响,并探讨其可能的作用机制。方法通过小鼠离体肠段实验,观察不同浓度的太子参保健酒对小鼠正常离体肠收缩活动的影响和对乙酰胆碱（ Ach）引起离体肠兴奋以及阿托品（ Atr）致肠管抑制等方面来考察太子参保健酒对小鼠离体小肠平滑肌的影响。结果与空白组比较,太子参保健酒增加正常小鼠小肠的张力、频率、活力;协同性作用于Ach 致小鼠离体小肠平滑肌;拮抗Atr 致小鼠离体小肠平滑肌抑制作用。结论提示太子参保健酒对肠管有一定的兴奋作用。     

阿司匹林对在体及离体气管平滑肌的影响

目的 研究阿司匹林对在体及离体气管平滑肌的影响.方法 本次研究对象为2013年~2016年之间接受治疗的80例患者,随机分成观察组(n=25)、实验组(n=25)和对照组(n=30),采用不同剂量的阿司匹林进行治疗,即对照组使用剂量为100mg,观察组使用剂量为200mg,试验组使用剂量为300mg,比较不同剂量的阿司匹林对在体及离体气管平滑肌的影响.结果 对照组与观察组和实验组哮喘持续时间比较呈逐渐缩短趋势,差异有统计学意义P<0.05;对照组与观察组和实验组哮喘恢复时间比较呈逐渐延长趋势,差异有统计学意义P<0.05.对照组与观察组和实验组的张力值比较呈逐渐增长趋势,差异有统计学意义P<0.05;对照组与观察组和实验组的抑制率比较呈逐渐下降趋势,差异有统计学意义P<0.05.阿司匹林的剂量增加,对抗气管平滑肌收缩的作用随之减弱.结论 较为适量的阿司匹林对气管平滑肌的扩张具有较好的作用功效.     

培养条件对三叶青愈伤组织生长及总黄酮含量的影响

研究培养条件对三叶青愈伤组织生长及黄酮积累的影响,建立用愈伤组织生产三叶青黄酮的方法。以三叶青的叶诱导产生的愈伤组织为材料,分别采用单因素实验、正交实验的方法比较了不同光照周期、不同有机添加物、不同前体、3种基础培养基、不同6-BA与NAA浓度的培养条件下愈伤组织生长的情况及黄酮含量。用愈伤组织生产三叶青黄酮可采用两步培养法来进行:先在促进愈伤组织生长的最佳处理组合条件:12 h/d间断性光照、MS+3.0 mg/L6-BA+2.0 mg/L NAA+2 g/L蛋白胨下培养30 d,再转入最利于黄酮积累的处理组合:连续光照、B5+4.0 mg/L 6-BA+2.0 mg/L NAA+40 mg/L苯丙氨酸下培养20 d。采用该方法培养的愈伤组织中总黄酮最大浓度可以达到28.4±3.9 mg/g DW。采用愈伤组织培养方式生产三叶青黄酮,不仅可以大大地缩短生产周期,而且培养物中的总黄酮含量也明显高于原植株叶片,接近于根茎中的黄酮含量,具有较大的可行性。     

枸橼酸西地非尔对兔海绵体组织作用及其机制的离体研究

目的　研究枸橼酸西地非尔对兔海绵体组织舒张功能的影响及其作用机制。方法　 37℃温孵兔海绵体组织(RCC) ,用放射免疫方法监测在硝普钠存在下 ,西地非尔10、10 0、10 0 0nmol·L-1对cGMP水平的影响 ;采用离体器官水浴技术 ,将RCC用苯丙肾上腺素 (PE)收缩 ,观察西地非尔对NO供体硝普钠 (SNP)及促内皮依赖性NO释放剂氯化乙酰甲基胆碱介导RCC舒张作用的影响。结果　SNP可提高RCC中cGMP水平 ,西地非尔 10、10 0、10 0 0nmol·L-1可剂量依赖性使之升至更高水平。西地非尔使SNP、氯化乙酰甲基胆碱 (MCH)作用IC50 显著减小。结论　以上结果表明枸橼酸西地非尔通过NO/cGMP呈剂量依赖性增强MCH和SNP对RCC的舒张作用 ,对动物阴茎海绵体组织舒张功能有显著性改善作用 ,从而大大提高动物性功能。     

离体兔晶状体上皮细胞的体外培养

后发性白内障的发生是白内障囊外除术后残留在前囊膜下的晶状体上皮细胞迁移、黏附在后囊膜并不断增殖、纤维化的过程,而白内障术后血-房水屏障的破坏,细胞外基质（extra cellular matrix,ECM）中一些成分在后囊膜上的沉积为晶状体上皮细胞在后囊膜黏附、增殖提供了适宜的内环境.通过探讨离体兔晶体上皮细胞的体外培养方法,为下一步研究后发性白内障的发病机制提供研究基础.     

丹参酮对离体肺的保护作用研究

目的观察丹参酮对离体肺的保护作用。方法24只新西兰免随机平均分为两组，对照组用LPD液行肺动脉灌注和保存，实验组用丹参酮加LPD液以同样方法灌注和保存。18h后观察形态学改变。结果光镜下两组肺泡、支气管及毛细血管结构完整，高倍视野下对照组较实验组肺泡上皮及毛细血管上皮细胞肿胀、肥大，少部分组织可见肺泡内有红细胞渗出、间隔增宽等。结论在LPD液中加入丹参酮，能够对离体肺起到更好的保护作用。     

Antibacterial properties of compounds isolated from Carpobrotus edulis

Several compounds isolated from the plant Carpobrotus edulis were evaluated for their activity against multidrug-resistant (MDR) bacteria and their efflux pump systems. Amongst the compounds isolated, six compounds were tested, namely uvaol, β-amyrin, oleanolic acid, catechin, epicatechin and monogalactosyldiacylglycerol. Oleanolic acid presented high antibacterial activity against a large number of bacterial strains. The triterpene uvaol was the most active compound for modulation of efflux activity by MDR Gram-positive strains.     

In vitro mutagenicity of valepotriates

Valepotriates are epoxide-bearing triesters of the monoterpene alcohol 4,7-dimethylcyclopenta-(c)-pyrane isolated from the roots of several Valerianacae species. They are regarded as the main tranquilizing constituents of these drugs.Although the valepotriates valtrate/isovaltrate (VAL) and dihydrovaltrate (DH-VAL) showed a strong alkylating activity against the nucleophilic agent 4-(p-nitrobenzyl)-pyridine (NBP), they were not clearly mutagenic for the strains TA98, TA100, TA1535, and TA1537 of Salmonella typhimurium or for the strains WP2 and WP2 uvrA^– of Escherichia coli in the absence of a metabolic activation system (S9-mix). However, the valepotriates were mutagenic for TA100, WP2 and WP2 uvrA^– at concentrations up to about 1.0 mole/plate when S9-mix was added to the test system. With more than 1 mole/plate the valepotriates were toxic in the presence of a metabolic activation system for all strains tested. The mutagenicity of the valepotriates was inversely related to the protein content of the S9-mix used. The mutagenicity and toxicity of the valepotriates could be inhibited when the S9-mix was preincubated with the esterase inhibitor paraoxon (1 mM) for 5 min before the test compounds and bacteria were added. Therefore, bioactivation of the valepotriates by an enzymatic hydrolysis of their ester groups is considered. This could be proven by activating the valepotriates with purified esterase.Parts of this paper were presented at the Congress, Fortschritte in der Arzneimittelforschung, April 17–20, 1983 in Munich     

In vitro Metabolism of Bumetanide

A new metabolite of the diuretic drug bumetanide, the 4-[(4-hydroxy)-phenoxy] analog (7), was identified in incubation mixtures of rat liver microsomes. Phenobarbital and clofibrate pretreatment to induce microsomal enzymes changed the relative amounts of the six metabolites formed. Compound 7was the most prevalent metabolite after clofibrate pretreatment.     

In vitro maturation of oocytes

Only about 400 of the one million oocytes present at birth will be ovulated, while the rest will die by atresia. The ability to rescue oocytes destined to die and mature them in vitro would provide invaluable information about folliculogenesis and oocyte maturation, and could provide oocytes for infertile women. In vitro maturation (IVM) is challenging in the human because folliculogenesis is a lengthy process encompassing many complex cellular changes in the oocyte and its surrounding follicle cells. A few live births have resulted from the maturation and fertilization of immature human oocytes aspirated from small antral follicles. Furthermore, it is possible to grow primordial follicles to pre-antral stages in slices of ovarian tissue, and support antrum formation in isolated pre-antral follicles. However, we are still a considerable way from growing and maturing pre-antral follicles to pre-ovulatory stages in vitro. The importance of the follicular environment for producing a healthy and developmentally competent oocyte is illustrated by the oocyte's susceptibility to errors during meiosis. This counsels considerable caution in the development of IVM for clinical application.     

In vitro evaluation of lomefloxacin

Lomefloxacin (1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4- oxoquinoline-3-carboxylic acid monohydrochloride, SC-47111) is a broad-spectrum antibiotic of the 4-quinolone group. In this comparative study the antimicrobial in-vitro activity of lomefloxacin was tested against 863 gram-negative and 415 gram-positive strains from fresh clinical isolates. As comparative agents ciprofloxacin, norfloxacin and ofloxacin were used. The minimal inhibitory concentrations were determined by means of a serial dilution with the agar-dilution procedure. Lomefloxacin showed an antibacterial efficacy comparable to other quinolones. Ciprofloxacin in general was two-fold dilutions more active. No cross-resistance with beta-lactamase producing-methicillin resistant or aminoglycoside-, tetracycline-, chloramphenicol- and co-trimoxacol-resistant strains could be found. Lomefloxacin showed in this study a broad antimicrobial activity. The clinical utilities of this new fluoroquinolone will depend on the pharmacokinetic properties and the adverse event profile.     

西格列他钠的体外代谢

目的研究拟治疗2型糖尿病的创新化合物西格列他钠(chiglitazar)的体外代谢速率、代谢酶和代谢转化,为临床应用提供参考。方法采用高效液相-紫外检测(HPLC-UV)的方法测定肝微粒体孵育液中西格列他钠的浓度,用特异性抑制剂的方法分析化合物的代谢酶,用大鼠肝微粒体体外研究西格列他钠可能的代谢产物和代谢途径。结果建立了可靠的测定大鼠肝微粒体中西格列他钠的HPLC分析方法;体外半衰期方法求得西格列他钠的t1/2为27.2min,固有清除率(Clint)为50.9mL.min-1.g-1蛋白;代谢酶研究表明,西格列他钠主要被P450酶中的CYP3A亚型代谢;西格列他钠在大鼠肝微粒体中的代谢主要为羟基化和O-脱烷基化,采用LC/MSn分析共发现了8个代谢物。结论西格列他钠是代谢活跃的化合物,有必要研究代谢产物的活性及临床注意药物相互作用。     

In vitro dissolution of dapsone

Log normal samples of dapsone (DDS) were prepared in which the geometric mean diameter ranged from 20 to 50 μm while the geometric standard deviation was in the range 1·62 to 1·88. Using a simple in vitro flow-through dissolution cell at 37°C, the data obtained were found to fit the Hixson-Crowell cube root dissolution law up to a critical time, T_c, where a distinct break occurred. Such a biphasic phenomenon has been predicted by other workers and is related to the time at which the smallest particles present have undergone dissolution. The initial slopes of the cube root dissolution plots were shown to be directly related to the reciprocal of the geometric mean diameter.     

In vitro activity of pefloxacin

A broth dilution method was used to measure the minimal inhibitory concentrations of pefloxacin, a new quinolone derivative. Because this new agent could be used in systemic infections, mezlocillin, cefotaxime, ceftazidime and amikacin were used as comparative agents. Pefloxacin was found to be more active than mezlocillin and as active as or more active than cefotaxime, ceftazidime and amikacin. With the exception of Serratia marcescens, only 7% of Enterobacteriaceae strains were resistant to pefloxacin with a MIC greater than 8 micrograms/ml. Pefloxacin was also found to be the best agent against the non-fermenters Staphylococcus aureus and St. epidermidis. Resistance to ampicillin, carbenicillin and gentamicin did not affect the effectiveness of pefloxacin. However, pefloxacin appeared more susceptible to nalidixic acid resistance, with MICs four to sixfold higher.