A nanostructured liquid crystalline formulation of 20(S)-protopanaxadiol with improved oral absorption

As with many other anti-cancer agents, 20(S)-protopanaxadiol (PPD) has a low oral absorption. In this study, in order to improve the oral bioavailability of PPD, the cubic nanoparticles that it contains were used to enhance absorption. Therefore, the cubic nanoparticle loaded PPD were prepared through the fragmentation of the glyceryl monoolein (GMO)/poloxamer 407 bulk cubic gel and were verified by transmission electron microscope, small angle X-ray scattering and differential scanning calorimetry. The in vitro release of 20(S)-protopanaxadiol from these nanoparticles was less than 5% at 12 h. And then Caco-2 cell monolayer model was used to evaluate the absorption of PPD in vitro. Meanwhile the rat intestinal perfusion model and bioavailability were also estimated in vivo. The results showed that, in the Caco-2 cell model, the PPD-cubosome could increase the permeability values from the apical (AP) to the basolateral (BL) of PPD at 53%. The result showed that the four-site rat intestinal perfusion model was consistent with the Caco-2 cell model. And the result of a pharmacokinetic study in rats showed that the relative bioavailability of the PPD-cubosome (AUC_0–∞) compared with the raw PPD (AUC_0–∞) was 169%. All the results showed that the PPD-cubosome enhanced bioavailability was likely due to the increased absorption by the cubic nanoparticles rather than by the improved release. Hence, the cubic nanoparticles may be a promising oral carrier for the drugs that have a poor oral absorption.     

黑曲霉全细胞生物催化制备没食子酸丙酯的研究

利用黑曲霉(Aspergillus niger)细胞作为全细胞生物催化剂,研究了催化没食子酸生成没食子酸丙酯的条件,探讨了有机溶剂、细胞预处理、底物浓度、反应时间和水分含量等因素在酶催化没食子酸丙酯合成中的影响,结果表明,苯是最佳溶剂,而菌丝体的含水量在80％时得率最高.在此基础上,选择菌丝量、没食子酸浓度、正丙醇体积分数和反应时间进行了正交试验,在200 r/min、40℃的转化条件下得到的较佳催化组合为:25 mL锥形瓶中加入10 mL苯、0.5g菌丝、7 mmol(0.012 7 g)没食子酸、7.3 ％(0.73 mL)正丙醇组成的有机催化体系中,反应18h,没食子酸丙酯得率达到36.4％.该过程无需要纯化或者固定化酶,实现了没食子酸丙酯低成本、高得率的催化.     

N~+注入诱变黑曲霉选育单宁酶生产菌株

以黑曲霉为出发菌株,经多次N+注入诱变,得到突变高产单宁酶菌株黑曲霉ANO2。该突变菌株其产单宁酶酶活为670.2 U/mL,较出发菌株的单宁酶酶活442.3 U/mL提高51.4%以上,突变菌株经传10代培养,产酶特性稳定,是一株比较理想的单宁酶生产菌株。     

葛根渣固态发酵产异黄酮的研究

葛粉提取工艺中形成的废弃物葛根渣含有一定量的异黄酮。以葛根渣为主要原料,通过黑曲霉菌株的固态发酵,利用微生物产生的木聚糖酶和内切-β-葡聚糖酶（CMC酶）破坏细胞壁的纤维结构,促进异黄酮的溶出。优化后的固态发酵培养基由70％葛根渣和30％麸皮组成,含水量70％。在30℃下发酵120h,总异黄酮提取得率为常规醇提法的1．82倍。HPLC图谱显示：固态发酵后大豆苷元的含量下降,而糖苷型异黄酮的含量明显增加,其中葛根素含量为每克葛根渣含3．97mg,比常规醇提法提高了70％。     

20%龙卷风水剂防除猕猴桃园杂草药效试验

20%龙卷风水剂防除猕猴桃园杂草药效试验结果表明：在杂草株高10~15 cm时每667 m2喷施20%龙卷风水剂200 ml,施药后7 d,对杂草防效达到89.7%;施施后20 d,对杂草株数防效达到93.9%,杂草鲜重防效达到96.1%,其药效显著优于每667 m2喷施150 ml处理,与20%克无踪水剂200 ml的药效相当,且药效能持续20~25 d,对苗木安全,可大面积应用推广。     

Sulfated derivatives of 20(S)-ginsenoside Rh2 and their inhibitory effects on LPS-induced inflammatory cytokines and mediators

Ginsenoside Rh2 is one of the most important ginsenosides in ginseng with antitumor, antidiabetic, antiallergic, and anti-inflammatory effects. However, the extremely poor oral bioavailability induced by its low water solubility greatly limits the potency of Rh2 in clinical use. Therefore, in this study we sulfated 20(S)-ginsenoside Rh2 with chlorosulfonic acid and pyridine method, and got two new sulfated derivatives, Rh2-B1 and Rh2-B2, with higher water solubility. Their chemical structures were characterized by spectroscopic methods (IR, MS and NMR). Additionally, Rh2-B1 and Rh2-B2 had the greater anti-inflammatory effects than Rh2 through inhibiting inflammatory cytokines and mediators in LPS-induced mouse RAW264.7 macrophages cells. These results suggested that the sulfated modification of Rh2 improved its water solubility and the sulfated derivatives could be more potential candidates for developing as anti-inflammatory agents.     

产纤维素酶微生物发酵转化虎杖提高白藜芦醇收率的研究

用微生物发酵法酶解虎杖,可以提高从虎杖中获取白藜芦醇的得率。通过从传统发酵食品中筛选含纤维素酶菌株,获得一株可以直接作用于虎杖的优良菌株。分别对固体堆积发酵条件:菌龄、温度、接种量、湿度进行单因素优化,与植物虎杖中白藜芦醇含量相比,发酵后白藜芦醇提取率提高至1.45%。     

Biotransformation of ursolic acid by Syncephalastrum racemosum CGMCC 3.2500 and anti-HCV activity

Microbial transformation of ursolic acid (UA, 3β-hydroxy-urs-12-en-28-oic acid, 1) by filamentous fungus Syncephalastrum racemosum CGMCC 3.2500 was conducted. Five metabolites 3β, 7β, 21β-trihydroxy-urs-12-en-28-oic acid (2); 3β, 21β-dihydroxy-urs-11-en-28-oic acid-13-lactone (3); 1β, 3β, 21β-trihydroxy-urs-12-en-28-oic acid (4); 3β, 7β, 21β-trihydroxy-urs-1-en-28-oic acid-13-lactone (5); and 21-oxo-1β, 3β-dihydroxy-urs-12-en-28-oic acid (6) were afforded. Elucidation of the structures of these metabolites was primarily based on 1D and 2D NMR and HR-MS data. Metabolite 2 was a new compound. In addition, the anti-HCV activity of compounds 1–6 was evaluated.     

中籼型水稻光（温）敏核不育系佳丰20S 的选育及初步利用

指出了籼型水稻光温敏核不育系佳丰20S是利用8077S与丰两优1号杂交，然后再与蜀恢527和扬稻6号复交选育而成。它属于无花粉类型，不育期间败育彻底，不育性稳定，其不育株率、花粉不育度和自交套袋不实率均为100％。在12．5h短日下，不育临界温度低于23．0℃。开花习性和稻米品质性状较好，配合力强，容易繁殖制种。利用该不育系育成的苗头组合正在参加各级区试。     

虎杖固体发酵生产白藜芦醇工艺条件优化研究

应用黑曲霉固体发酵法酶解虎杖中的虎杖苷,以提高从虎杖中获取白藜芦醇的得率.分别对固体堆积发酵条件:菌龄、温度、接种量、水料比进行单因素分析,并采用正交法对4因素进行组合优化,实验结果表明,最优工艺条件为:温度40℃,水料比2∶1(g∶g),接种量1％,菌龄40h;此条件下,发酵48 h,虎杖中白藜芦醇得率提高到1.48...     

Optimization of the selective preparation of 20(R)-ginsenoside Rg3 catalyzed by d,l-tartaric acid using response surface methodology

The optimization of the selective preparation of 20(R)-ginsenoside Rg3 converting protopanaxadiol type saponins (PPD saponins) by the commercially available d, l-tartaric acid was carried out using response surface methodology (RSM) based on a three-factor and six-level central composite design. The optimal 20(R)-ginsenoside Rg3 de% was predicted to be 94.52% in the combination of the factors (d, l-tartaric acid concentration 1.19 mol/L, temperature 107.9 °C and time 2.79 h) through the canonical analysis with maximum responses. Under the optimum reaction conditions, the actual 20(R)-ginsenoside Rg3 de% was 96.49%. 20(R)-ginsenoside Rg3 (1) and 20(S)-ginsenoside Rg3 (2) were separated and identified by ¹H-NMR and ¹³C-NMR. Therefore, the RSM was effective to optimize the preparation of 20(R)-ginsenoside Rg3 by converting PPD saponins using d, l-tartaric acid.     

Influence of (22S,23S)-homobrassinolide on rooting capacity and survival of adult Norway spruce cuttings

To determine whether brassinosteroids promote clonal propagation of mature coniferous trees, cuttings of adult Norway spruce (Picea abies (L.) Karst.) trees were harvested in late March, treated with (22S,23S)-28-homobrassinolide (SSHB), and stored at 2 degrees C in darkness until they were planted in May. Treatment of the cuttings with SSHB significantly enhanced the formation of adventitious roots by increasing percent rooting from 50% in the control cuttings to 92% in the 60 ppm SSHB treatment. N(6)-Benzyladenine (BA) stimulated rooting slightly although not significantly, but it counteracted the stimulative effect of SSHB when cuttings were treated with both compounds together. In a second study, the above-ground parts of medium-sized mature clonal Norway spruce trees were pretreated from the end of June till August with SSHB or BA or both. Needle retention of cuttings taken from the pretreated trees the following spring was prolonged until September and the cuttings flushed, but did not root, whereas cuttings from untreated stock plants died before September. No interaction between BA and SSHB was observed. When these pretreatments were repeated the following year on the same mature clonal trees rooting of cuttings was significantly improved in the 5 ppm SSHB treatment.     

Biotransformation on the flavonolignan constituents of Silybi Fructus by an intestinal bacterial strain Eubacterium limosum ZL-II

Eubacterium limosum ZL-II is an anaerobic bacterium with demethylated activity, which was isolated from human intestinal bacteria in our previous work. In this study, the flavonolignan constituents of Silybi Fructus were biotransformed by E. limosum¹ ZL-II, producing four new transformation products — demethylisosilybin B (T1), demethylisosilybin A (T2), demethylsilybin B (T3) and demethylsilybin A (T4), among which T1 and T2 were new compounds. Their chemical structures were identified by ESI-TOF/MS, ¹H NMR, ¹³C NMR, HMBC and CD spectroscopic data. The bioassay results showed that the transformation products T1–T4 exhibited significant inhibitory activities on Alzheimer's amyloid-β 42 (Aβ₄₂²) aggregation with IC₅₀ values at 7.49 μM–10.46 μM, which were comparable with that of the positive control (epigallocatechin gallate, EGCG³, at 9.01 μM) and much lower than those of their parent compounds (at not less than 145.10 μM). The method of biotransformation by E. limosum ZL-II explored a way to develop the new and active lead compounds in Alzheimer's disease from Silybi Fructus. However, the transformation products T1–T4 exhibited decreased inhibitory activities against human tumor cell lines comparing with their parent compounds.     

关于KZ──D系统调速指标D和S定义的探讨

本文通过对现有书籍和文献中有关直流调速系统的调速范围Ｄ和静差率Ｓ各种定义的分析，研究了ＫＺ—Ｄ系统，指出原有定义中的不尽合理之处．并在此基础上，避开非线性区，对调速范围Ｄ和静差率Ｓ的原有定义进行了扩展、引申和部分修正．对如何测试、分析或设计一个实际的ＫＺ—Ｄ调速系统，具有理论指导意义和实用参考价值．     

METHOD FOR FAST TEST OF PRESTRESSED CONCRETE VOIDED SLAB (V.S)

Withadvantagesofsimpleshape,conven-ientconstruction,lowbuildingdepthetC,pre-stressedconcreteV.Sisusedwidelyinbulld-ingbridge.Forevaluatequalityofdesignandconstruction,dead1oadtestinbuildingsiteoflenisconductedtoanalyzeanddeteforbearingcapaclty'anduseconditionofpre-strcssedconcreteV.S.However.accuratedateiscommonl\'influencedbvsuchconditionasonthesitecondition,increasingofdataerrorbytemPeratUreandhumidity,concretemateri-als,anditoftencostmorethantWodaystoprepareoneprcstrCssedconcreteV.Sonth…     

SZW(S)10-2.5-M型废料锅炉的研制

木材加工生产过程中产生大量的废弃物(树皮、腐朽木、碎木块、砂光粉、刨花等),利用废弃物作为生产锅炉的供热燃料节省了燃煤,降低了生产成本。 根据吉林森工集团股份公司红石中密度纤维板厂废料量的状况及生产工艺对锅炉参数的要求,确定研制SZW(S)10-2.5-M型废料锅炉的设计参数,研制废料锅炉。     

20%氟硅唑·咪鲜胺热雾剂防治橡胶树白粉病试验初报

2007年3月在云南河口进行的20%氟硅唑·咪鲜胺热雾剂防治橡胶树白粉病的田间试验结果:常规硫磺粉处理的效果极显著(P=0.01)优于氟硅唑·咪鲜胺的每带、隔一带、隔二带胶树施烟雾等3个处理;而氟硅唑·咪鲜胺的每带施烟雾处理防效极显著(P=0.01)和显著优于其它二种处理,防效可达80%以上,可进一步作应用技术研究。     

Rindenkrebs der Eßkastanie (Cryphonectria parasitica) in Südwestdeutschland

Chestnut blight (Cryphonectria parasitica) in South-west Germany . In 1992 and 1993, chestnut blight (Cryphonectria parasitica) was found in three stands in the south-west of Germany. Each of the three stands has only one compatibility group (vc-group). Two of them (97 and 75 Isolates) belong to the vc-group I. They are compatible with the Swiss vc-group I. The 43 Isolates from the third stand were not compatible with the most common Swiss vc-groups (vc-group I-V). In the German vc-group I, one hypovirulent strain was found.