榆耳发酵液中新倍半萜——榆耳三醇的结构

从榆耳(Gloeostereum incarnatum S.Ito et Imai)的液体发酵物中经层析分离得一新倍半萜榆耳三醇(gloeosteretriol),根据红外光谱、核磁共振谱和质谱数据推定其结构为Ⅰ,并用X-射线晶体衍射进一步确证其结构和立体构型。     

榆耳多糖的分离纯化、结构鉴定及抗肿瘤活性研究

目的对榆耳粗多糖(GI)进行分离纯化,并对所得均一多糖进行结构鉴定及抗肿瘤活性的研究。方法 GI经Q-Sepharose F.F离子交换色谱,Sepharose CL-6B凝胶色谱分离得到均一多糖,采用凝胶色谱、薄层色谱、红外光谱、高碘酸氧化等方法测定相对分子质量(Mr)、单糖组成、糖苷键连接方式。采用MTT法对粗多糖和均一多糖的体外抗肿瘤活性进行测定。结果分离得到均一多糖GI1-3和GI1-4b,其Mr分别约为1.55×105和3.03×104。经薄层色谱法、红外光谱法、高碘酸氧化法确定GI1-3由半乳糖、葡萄糖、甘露糖、木糖组成,以β-(1,4)、β-(1,6)、β-(1,3)糖苷键连接。GI1-4b由葡萄糖、甘露糖和木糖组成,以β-(1,4)、β-(1,6)糖苷键连接。体外抗肿瘤实验表明,GI1-3的抑瘤活性较GI1-4b和GI高,GI的抑瘤活性在3种多糖组分中最低。结论 GI、GI1-3和GI1-4b对体外生长的肿瘤细胞具有不同的抑制作用,可能与其Mr及分子结构有关。     

槐榆片制备及临床疗效观察

目的探讨槐榆片制备及临床疗效。方法按现代工艺制备槐榆片,建立性状、鉴别与检查方法,以500例痔疮患者随机分为治疗组和对照组,治疗组250例口服槐榆片,对照组250例口服一清胶囊,治疗10 d后进行临床疗效对比。结果薄层图谱斑点清晰,阴性对照无干扰,片剂质量符合《中国药典》要求。临床治疗组总有效率98%;对照组总有效率80%,两组经统计学处理有显著性差异(P<0.05)。结论槐榆片组方合理,制备简单,对肛肠引起的内痔、外痔、混合痔、便血等疗效确切,无不良反应。     

槐榆片制备及临床疗效观察

目的 探讨槐榆片制备及临床疗效.方法 按现代工艺制备槐榆片,建立性状、鉴别与检查方法,以500例痔疮患者随机分为治疗组和对照组,治疗组250例口服槐榆片,对照组250例口服一清胶囊,治疗10 d后进行临床疗效对比.结果 薄层图谱斑点清晰,阴性对照无干扰,片剂质量符合《中国药典》要求.临床治疗组总有效率98%;对照组总有效率80%,两组经统计学处理有显著性差异(P＜0.05).结论 槐榆片组方合理,制备简单,对肛肠引起的内痔、外痔、混合痔、便血等疗效确切,无不良反应.     

榆栀止血颗粒联合富马酸亚铁治疗月经量过多所致贫血的疗效观察

目的 探究榆栀止血颗粒联合富马酸亚铁治疗月经量过多所致贫血的临床疗效。方法 选取曲靖市第一人民医院2018年4月-2019年1月收治的164例月经量过多所致贫血患者作为研究对象,根据治疗方案将患者分为对照组和观察组,每组82例。对照组患者口服富马酸亚铁咀嚼片,0.2 g/次,3次/d;观察组患者在对照组治疗的基础上口服榆栀止血颗粒,月经第1天开始服用,1袋/次,3次/d,经期服用,血止即停。观察两组患者的临床疗效,比较两组治疗前后的血红蛋白（Hb）、红细胞（RBC）、血浆白蛋白（PA）和红细胞压积（HCT）的水平。结果 治疗后,观察组总有效率为92.7%,显著高于对照组的82.9%,两组比较差异具有统计学意义（P<0.05）。治疗后,两组患者Hb、RBC、PA和HCT水平均显著升高（P<0.05）;治疗后,观察组患者治疗后Hb、RBC、PA和HCT显著高于对照组,差异具有统计学意义（P<0.05）。结论 榆栀止血颗粒联合富马酸亚铁治疗月经量过多所致贫血具有显著疗效,值得临床推广。     

林蛙油榆黄蘑胶囊抗小鼠疲劳的实验研究

目的 研究林蛙油榆黄蘑胶囊的抗疲劳作用.方法 在小鼠抗疲劳试验中,将小鼠分为空白组、林蛙油组、榆黄蘑组和3个不同剂量的林蛙油榆黄蘑胶囊组(0.7、1.4、2.1 g·Kg-1),分别ig蒸馏水和相应药物,每天1次,连续30 d.记录小鼠负重力竭游泳时间,在小鼠游泳实验中检测小鼠血乳酸、血清尿素氮(BUN)、肝糖原含量各...     

耳复康口服液对庆大霉素致豚鼠耳聋模型听觉耳动反射及瞬态诱发耳声发射的影响

目的 探究耳复康口服液对庆大霉素致豚鼠耳聋模型听觉耳动反射及瞬态诱发耳声发射（transient evoked otoacoustic emission,TEOAE）的影响。方法 将豚鼠随机分为正常对照组,模型组,耳聋左慈丸组（2.7 g·kg^-1）,高、中、低剂量耳复康口服液组（18,9,4.5 mL·kg^-1）。除空白对照组每天肌肉注射生理盐水2 mL·kg^-1,其余各组每天肌肉注射硫酸庆大霉素80 mg·kg^-1,同时给予相应的药物进行灌胃14 d,分别于第7天、第14天给药后进行听觉耳动反射的测试,第15天时每只豚鼠进行TEOAE测试。结果 对庆大霉素致豚鼠耳聋模型听觉耳动反射的影响：与模型组比,第7天耳复康口服液低剂量组可显著改善豚鼠听觉障碍（P<0.01）;第14天耳复康口服液高、中、低剂量组均可显著改善豚鼠听觉障碍（P<0.01）。对庆大霉素致豚鼠耳聋模型TEOAE的影响：与模型组比,耳复康口服液各剂量组总反应能量显著降低（P<0.05或P<0.01）;耳复康口服液各剂量组总相关度显著降低（P<0.01或P<0.05）。结论 耳复康口服液均对庆大霉素致聋豚鼠的听力障碍有改善作用。     

榆黄喷雾剂质量标准的建立

目的：本研究旨在建立榆黄喷雾剂的质量标准。方法：采用薄层色谱法与紫外分光光度法对榆黄喷雾剂中的盐酸小檗碱进行定性鉴别及含量测定,通过香草醛硫酸法测定缩合鞣质。结果：榆黄喷雾剂中盐酸小檗碱的薄层色谱显示,在与对照品色谱相应的位置上,显相同颜色的斑点,阴性无干扰;紫外分光光度法测定盐酸小檗碱,盐酸小檗碱在1.13-13.60μg·m^l-1之间呈良好线性关系（r=0.999 9）,平均回收率为99.68%,RSD=1.53%（n=9）;香草醛硫酸法测定榆黄喷雾剂中缩合鞣质含量,儿茶素对照品浓度在0.03-0.30 mg·ml^-1范围内与吸收度具有很好的线性关系r=0.999 3,平均回收率为99.6%,RSD为1.76%（n=9）。结论：研究证明,该方法可用于榆黄喷雾剂的质量控制。     

槐榆丸质量标准的研究

目的 研究槐榆丸的质量标准。方法 采用薄层色谱法对槐榆丸进行定性鉴别；采用高效液相色谱法（HPLC）对槐榆丸中芦丁的含量进行测定。结果 芦丁的线性范围115．2—1152ng，其回归方程为Y=1．00504X-2．92048；r=0．9999，平均回收率为98．16％，RSD为0．54％。结论 该方法简便、灵敏、准确，可作为制订槐榆丸质量标准的主要依据。     

干耳和湿耳状态的慢性化脓性中耳炎行耳内镜下Ⅰ型鼓室成形术的临床疗效

目的 观察干耳和湿耳状态的慢性化脓性中耳炎患者行耳内镜下Ⅰ型鼓室成形术的临床疗效。方法 128例行耳内镜下Ⅰ型鼓室成形术的慢性化脓性中耳炎患者中，湿耳状态患者41例(湿耳组),干耳状态患者87例(干耳组)。记录术前以及术后1、3个月时气导听阈(PTA)和气骨导差(ABG),记录术后1、3个月时干耳率、鼓膜愈合率和听力改善率，并观察术后3个月内并发症发生情况。结果 与术前相比，两组术后1、3个月时PTA和ABG降低(P<0.05),术后3个月时降低更明显(P<0.05);干耳组术后1个月时ABG低于湿耳组(P<0.05)。湿耳组与干耳组术后1、3个月时干耳率、鼓膜愈合率和听力改善率差异均无统计学意义(P>0.05)。两组术后并发症发生率相仿(P>0.05)。结论 耳内镜下Ⅰ型鼓室成形术能安全、有效治疗不同状态慢性化脓性中耳炎，干耳或湿耳状态不会影响术后疗效。     

蜜环菌菌丝体化学成分的研究——Ⅵ.蜜环菌癸素(armillaripin)的分离与结构

从人工发酵培养的蜜环菌[Armillaria mellea(Vahl.ex Fr.)Quel.属白蘑科(Tricholometaceae)真菌]菌丝体的石油醚提取物中,经硅胶层析分离得到一新的倍半萜醇芳香酸酯类化合物,命名为蜜环菌癸素(armillaripin)。根据光谱(UV,IR,¹HNMR,¹³CNMR和MS)分析推测其化学结构,并进一步用X-线衍射晶体解析法确证其结构和其相对构型。     

温敏性吲哚美辛/β-环糊精包合物的制备及体外评价

目的合成兼具温敏性及药物包合能力的新型药物载体聚(N-异丙基丙烯酰胺)-β-环糊精(PNIPA-β-CD)，以吲哚美辛为模型药物，考察该载体的释药行为。方法末端带羧基的PNIPA与改性后的环糊精衍生物在1-(3-二甲氨基丙基)-3-乙基-碳二亚胺(EDC)的作用下缩合，得到PNIPA-β-CD，采用冻干法制备吲哚美辛/PNIPA-β-CD包合物。红外、¹H NMR和DSC表征载体的结构及包合物的形成；用分光光度法测定载体材料的LCST，并进行包合物体外释药研究。结果PNIPA-β-CD在35 ℃发生相转变，吲哚美辛/PNIPA-β-CD包合物的载药量为5.8％，药物与载体摩尔比为0.97∶1。体外释放研究表明吲哚美辛/PNIPA-β-CD包合物在37 ℃的释药比其在25 ℃的释放要慢，在LCST以上具有一定的缓释作用。结论该载体既具有温敏性，又具有药物包合作用，并且在体温条件下具有缓释作用，是一种新型的温敏性药物载体。     

Identification and characterization of nitric oxide synthase inSalmonella typhimurium

The presence of the nitric oxide synthase (NOS) enzyme from Salmonella typhimurium (S. typhimurium) was identified by measuring radiolabeled L-[3H]citrulline and NO, and Western blot analysis. NOS was partially purified by both Mono Q ion exchange and Superose 12HR size exclusion column chromatography, sequentially. The molecular weight of NOS was estimated to be 93.3 kDa by Western blot analysis. The enzyme showed a significant dependency on the typical NOS cofactors; an apparent Km for L-arginine of 34.7 mM and maximum activity between 37 degrees C and 43 degrees C. The activity was inhibited by NOS inhibitors such as aminoguanidine and N(G),N(G)-dimethyl-L-arginine. Taken together, partially purified NOS in S. typhimurium is assumed to be a different isoform of mammalian NOSs.     

异叶梁王茶甙Ⅲ和Ⅳ的结构

继前报后,又从异叶梁王茶[Nothopanax davidii(France)Harms]树皮中分离得到两种五环三萜皂甙。经化学和波谱(IR,¹HNMR,~(13)CHMR,¹H-¹HCOSY,¹³C-¹H COSY,MS)分析,分别鉴定为3-O-α-(2’,4’-O-二乙酰基)-L-吡喃阿拉伯糖-3β-羟基齐墩果-12-烯-28,29-双羧酸-28-O-[α-L-吡喃鼠李糖(1-4)-β-D-吡喃葡萄糖(1—6)-β-D-吡喃葡萄糖]酯甙(Ⅲ),命名为异叶梁王茶甙Ⅲ和3-O-β-(2-O-乙酰基)-D-吡喃木糖-3β-羟齐墩果-12-烯-28,29-双羧酸甙(Ⅳ),命名为异叶梁王茶甙Ⅳ。这两种皂甙均系首次从植物中分出的新化合物。     

湖北贝母属植物化学成分的研究*——ⅩⅢ湖贝甙的分离与结构解析

从湖北贝母Fritillaria hupehensis Hsiao et K.C.Hsia经干燥的鳞茎中分离出Ⅰ～Ⅳ4个生物碱,经理化常数测定和波谱分析,并与标准品对照,鉴定碱Ⅰ,Ⅱ和Ⅲ分别为浙贝甲素(veimine)、浙贝乙素(Peiminine)和鄂贝新(ebeiensine),其中鄂贝新咱湖北贝母中首次得到.碱Ⅳ是一种微量生物碱甙,C₃₃H₅₃NO₈,mp206～208℃,定名为湖贝甙(hupehemonoside),经IR,MS,¹HNMR和¹³CNMR解析,推定其结构为5α,14α,17β,22β-cevanine-20β-hydroxyl-6-oxo-3β-O-β-D-glucoside。     

Characterization and Modulation of the Transferrin Receptor on Brain Capillary Endothelial Cells

PURPOSE: The expression level of the transferrin receptor (TfR) on brain capillary endothelial cells (BCECs) and the endocytosis of 125I-transferrin (125I-Tf) by this receptor was investigated. Furthermore, the influence of iron, the iron scavenger deferoxamine mesylate (DFO), astrocytic factors, a GTP-ase inhibitor (tyrphostin-A8, T8), lipopolysaccharide (LPS), and the radical scavenger N-acetyl-L-cysteine (NAC) on the TfR expression was studied to gain insight in the use and optimization of the TfR for drug targeting to the brain. METHODS: Experiments were performed with primary cultured bovine BCECs that were incubated with 125I-Tf at 4 degrees C (to determine binding) or at 37 degrees C (to determine endocytosis) in the absence or presence of the modulators. For full saturation curves in the absence or presence of iron or DFO, analysis was performed with a population approach using NONMEM, allowing us to estimate a single value for affinity (Kd, concentration of 50% receptor occupancy) and separate values for maximum receptor occupancy (B(max). RESULTS: On BCECs, the TfR is expressed extracellularly (B(max) of 0.13 fmol/microg cell protein), but also has a large intracellular pool (total B(max) of 1.37 fmol/microg cell protein), and is actively endocytosing Tf via clathrin-coated vesicles. At 4 degrees C, a Kd of 2.38 microg/ml was found, whereas the Kd at 37 degrees C was 5.03 microg/ml. Furthermore, DFO is able to increase both the extracellular as well as the total binding capacity to 0.63 and 3.67 fmol/microg cell protein, respectively, whereas it had no influence on Kd. B(max) at 37 degrees C after DFO preincubation was also increased from 0.90 to 2.31 fmol/microg cell protein. Other modulators had no significant influence on the TfR expression levels, though LPS increased cellular protein concentrations after 2-h preincubation. CONCLUSIONS: The TfR is expressed on BCECs and actively endocytoses Tf, making it a suitable target for drug delivery to the bloodbrain barrier and the CNS. DFO up-regulates the TfR expression level, which may influence targeting efficiency.     

黄褐毛忍冬化学成分的研究

从我省商品药材金银花的主要品种之一,黄褐毛忍冬(Lonicera fulvotomentosa Hsu et S.C.Cheng)的花蕾中分离到五种以常春藤皂甙元构成甙元的皂甙(Ⅰ～Ⅴ),本文报道化合物Ⅰ,Ⅱ和Ⅴ的结构测定。Ⅴ为新的三萜酸双糖链甙,命名为黄褐毛忍冬皂甙甲(fulvotomentoside A),Ⅰ和Ⅱ为已知化合物,分别被鉴定为α-常春藤皂甙(α-hederin)和无患子皂甙B(sapindoside B)。     

Ambient temperature effects on 3,4-methylenedioxymethamphetamine-induced thermodysregulation and pharmacokinetics in male monkeys.

Changes in ambient temperature are known to alter both the hyperthermic and the serotonergic consequences of 3,4-methylenedioxymethamphetamine (MDMA). Metabolism of MDMA has been suggested to be a requisite for these neurotoxic effects, whereas the hyperthermic response is an important contributing variable. The aim of the present study was to investigate the interaction between ambient temperature, MDMA-induced thermodysregulation, and its metabolic disposition in monkeys. MDMA (1.5 mg/kg i.v.) was administered noncontingently at cool (18 degrees C; n = 5), room (24 degrees C; n = 7), and warm (31 degrees C; n = 7) ambient temperatures. For 240 min following MDMA administration, core temperature was recorded and blood samples were collected for analysis of MDMA and its metabolites 3,4-dihydroxymethamphetamine (HHMA), 3,4-dihydroxyamphetamine, and 3,4-methylenedioxyamphetamine (MDA). A dose of 1.5 mg/kg MDMA induced a hypothermic response at 18 degrees C, a hyperthermic response at 31 degrees C, and did not significantly change core temperature at 24 degrees C. Regardless of ambient temperature, plasma MDMA concentrations reached maximum within 5 min, and HHMA was a major metabolite. Curiously, the approximate elimination half-life (t(1/2)) of MDMA at 18 degrees C (136 min) and 31 degrees C (144 min) was increased compared with 24 degrees C (90 min) and is most likely because of volume of distribution changes induced by core temperature alterations. At 18 degrees C, there was a significantly higher MDA area under the concentration-time curve (AUC) and a trend for a lower HHMA AUC compared with 24 degrees C and 31 degrees C, suggesting that MDMA disposition was altered. Overall, induction of hypothermia in a cool environment by MDMA may alter its disposition. These results could have implications for MDMA-induced serotonergic consequences.     

Characteristics of chitosanases from<Emphasis Type="Italic">Aspergillus fumigatus</Emphasis> KB-1

Two chitosanases produced by Aspergillus fumigatus KB-1 were purified by ion exchange and size exclusion chromatographies. Molecular weights of chitosanases were 111.23 kDa (chitosanase I) and 23.38 kDa (chitosanase II). The N-terminal amino acid sequence of chitosanase II was determined as follows: YNLPNNLKQIYDKHKGKXSXVLAKGFTN. The optimum pH of the chitosanase I and II was 6.5 and 5.5, respectively. The optimum temperatures were 60 degrees C for chitosanase land 70 degrees C for chitosanase II. Hydrolysis products of two chitosanases were analyzed by HPLC and GPC. Chitosanase I hydrolyzed substrate to glucosamine. Chitosanase II produced chitooligosaccharides.     

Effect of storage on the plasma concentration of chlorpromazine and six of its metabolites.

The concentrations of chlorpromazine (CPZ) and six of its metabolites in patient plasma samples that had been stored for 24 h at -20 degrees C, for 1 week at -20 degrees C, and for 4 weeks at -70 degrees C were compared. The concentrations of CPZ and six of its metabolites in human plasma spiked with known concentrations and stored at -70 degrees C for either 3 or 12 months were also compared. No significant difference was seen in the concentrations after storage under nitrogen and analysis by a high-performance liquid chromatography technique.