17—4PHMo钢的热处理与电化学腐蚀关系的研究

本文讨论了17—4PHMo(OCr17Ni4Cu4Mo2Nb)钢在含1.8％H_2SO_4和4.5％NaCl的溶液中电化学腐蚀行为。试验表明:经正常热处理的试样,在含Cl~-和H~+的溶液中能生成稳定的钝化膜,这种钝化膜只有当金属阳极电位高于20毫伏时才能被击穿。同时,由于Epp值相对较正,即使钝化膜被击穿而产生局部的点蚀,也能重新钝化,恢复完整的钝化膜。本文还讨论了钢热处理后的显微组织,也讨论了热处理工艺与电化学性能之间的关系,从而阐明该钢在较高NaCl含量的酸性溶液中不易产生点腐蚀破坏。     

INTRAMOLECULAR CROSS-LINKING OF PROTEINS BY FORMATION OF LYSINOALANINE OR LANTHIONINE Modification of Disulfides in Ovomucoids

The disulfide bonds of ovomucoids were cleaved and new sulfur-containing cross-links were introduced by two separate chemical modification methods: (1) alkali treatment, and (2) cyanolysis. Alkali and cyanolytic treatments were used to cleave disulfide bonds and to introduce new synthetic nonreducible cross-links consisting of residues of lysinoalanine (N-(dl -2-amino-2-carboxyethyl)-l -lysine) and lanthionine (bis(2-amino-2-carboxyethyl)sulfide). The two ovomucoids studied were turkey and penguin ovomucoids, which are “double-headed” inhibitors of proteolytic enzymes with one inhibitory site for bovine trypsin and another for bovine α-chymotrypsin or subtilisin. Trypsin does not compete with either α-chymotrypsin or subtilisin, but the latter compete with one another, apparently for the same inhibitory site. The stability of inhibitory activities as a function of disulfide bond scission and the formation of new nondisulfide cross-links was studied. In both methods of disulfide modification of turkey ovomucoid, inhibitory activity against trypsin was more stable with respect to the extent of modification than was inhibitory activity against chymotrypsin or subtilisin. With penguin ovomucoid, inhibitory activity against subtilisin was always more stable than activity against trypsin or chymotrypsin with both methods. With both ovomucoids it was thus possible to produce single-headed inhibitors from the double-headed inhibitors. The formation of the nonreducible cross-links of lanthionine from cystines, and of lysinoalanines from cystines and lysines, with retention of a biochemical activity, suggests that such a procedure may have at least limited use as a cross-linking method.     

Heat stable protein with anticoagulant and smooth muscle contractile actions isolated from Habu (Trimeresurus flavoviridis) venom

The biological activity of a Habu (Trimeresurus flavoiridis) venom fraction with drug-metabolizing enzyme inhibitory action was studied. The venom fraction, which was isolated through Sephadex G-100 gel filtration and cation exchange chromatography on Amberlite CG50, caused an increase of vascular permeability and hemorrhage, but these actions were lost after heating at 70 degrees C for 5 min. The fraction showed anticoagulant activity on citrated blood, and this activity remained after heating of the venom. Guinea pig ileum was contracted by treatment with nonheated or heated venom fraction, and these contractions were inhibited with atropine and potentiated with physostigmine. These results suggest that the drug-metabolizing enzyme inhibitor isolated from Habu venom involves the heat stable component with anticoagulant activity and smooth muscle contractile action.     

美托洛尔注射剂稳定性的研究

对美托洛尔注射剂的稳定性进行了研究。应用紫外分光光度法对其进行含量测定，平均回收率为１００．３％（ＲＳＤ＝０．７％）。并用薄层色谱法进行检查，结果表明该药对热和光均相当稳定，暂定有效期为１年。     

Stability of high molecular weight anticancer agent SMANCS and its transfer from oil-phase to water-phase. Comparative study with neocarzinostatin

SMANCS is a conjugate protein of copolymer of styrene-maleic acid [SMA] (molecular weight: 1,500) and an antitumor protein neocarzinostatin [NCS] (molecular weight: 11,700). It has an approximate molecular weight of 15,000. We report here stability of SMANCS in oil and in water, and NCS in water, under various physical conditions such as exposure to heat, UV, pH, and ultrasonic treatment. Then, we carried out an experiment of transfer of SMANCS in lipid contrast medium [lipiodol] (oil phase) to water phase (blood and physiological saline) in vitro. Results are summarized as follows: In aqueous condition, SMANCS is far more stable than NCS against the exposure to heat and UV, though it is inactivated by excessive exposures. SMANCS in an oily medium was found much more stable even at higher temperatures than in the aqueous phase. Both SMANCS and NCS are the most stable at pH 4.9-6.0. SMANCS dissolved in oil transferred to water phase slowly, having T1/10 of 24 hours (in case of lipiodol). This helps maintaining the anticancer effect of the drug in vivo for a long period of time. SMANCS in lipiodol was found to exert its action against cultured tumor cells as in an aqueous solution.     

Fractionation of northern copperhead venom by ion-exchange chromatography: preliminary characterization of the primary lethal fraction

J. B. Moran, S. Y. Y. Pang, D. W. Martin and C. R. Geren. Fractionation of northern copperhead venom by ion-exchange chromatography: preliminary characterization of the primary lethal fraction. Toxicon17, 499–510, 1979.—Venom of the northern copperhead (Agkistrodon contortrix mokasen) has been fractionated by ion-exchange chromatography and the resulting fractions examined for lethal and enzymatic activities. Of the nine distinct fractions obtained by carboxymethyl cellulose chromatography, five were lethal to mice. One of these five accounted for 65–70% of the lethality of whole venom. This fraction, TII, under our experimental conditions appeared to be dissociated from enzymatic activities found both in the whole venom and in other carboxymethyl fractions. Phospholipase, protease and ester-hydrolytic activities appeared in significant quantities in both the fraction of the venom not retained by carboxymethyl cellulose and in various fractions which were retained. Re-chromatography of the non-retained fraction showed that these activities were distinct and not the result of a column overload. The non-retained fraction contained virtually all of the l-amino acid oxidase activity. This fraction also contained a component which caused hemorrhage in mice and a calcium-independent thrombin-like pro-coagulant activity. This fraction was further separated by diethylaminoethyl cellulose chromatography which revealed that the pro-coagulant activity consisted of at least two separate entities.TII had an ld₅₀ value in mice of 1–2 μg/g body weight, which is 10–20 times more potent than whole venom. This fraction has been shown to abolish the muscle response to indirect stimulation and acetylcholine, but not KCl in the chick biventer cervicis neuromuscular junction assay. Its lethality to mice is destroyed by incubation with proteases or at high pH. It is fairly heat stable with lethality being retained after 20 min at 100°C. Toxicity is lost when this fraction is dialyzed against 5 mM sodium acetate, but not when dialyzed against Tyrode's solution or 100 mM sodium acetate. Chemical modification studies have shown that the lethal activity of this fraction may have disulfide, tryptophan, histidine and possibly arginine dependency.     

Stability of extruded 17 beta-estradiol solid dispersions.

Recrystallization is one of the main problems concerning the stability of solid dispersions. Different analytical methods were applied showing that no recrystallization occurred after treating melt extruded solid dispersions with 17 beta-Estradiol as the model drug with heat or water vapor. A skillful choice of excipients--a combination of polymers and additives--could be the reason for improving the stability. The requirements of the USP 23 for Estradiol tablets of 75% dissolved drug after 60 min were fulfilled after storing the tablets for 6 months at 40 degrees C/75% RH. By observing the change in glass transition temperature, DSC analysis showed that the solid dispersions were stable against thermal stress. Isothermal microcalorimetry as well as moisture absorption gravimetry were methods to prove the stability of the solid dispersions against water vapor.     

The anticoagulant fraction from the leaves ofDiospyros kaki L. has an antithrombotic activity

The leaves of Persimmon (Diospyros kaki L.) has long been used for tea in Korea since it was thought to be effective against hypertension. An anticoagulant fraction was purified through gel filtration G-100, hydrophobic, gel filtration G-150, and FPLC, Phenyl superpose column chromatographies. The purified fraction was homogenous and its Mr was estimated 10,000 Da by gel filtration and SDS-PAGE. The purified fraction was sensitive to treatment of subtilisin B, but not to heat and its activity was not changed after periodate oxidation, indicating that the activity was not due to carbohydrates. It delayed thrombin time (TT), activated partial thromboplastin time (APTT), and prothrombin time (PT) using human plasma. TT was more sensitive than APTT and PT, suggesting that the anticoagulant activity may be caused by a degradation or a defect of fibrin or thrombin. It did not cause the hydrolysis of fibrin after incubation. However, it inhibited thrombin-catalyzed fibrin formation with a competitive inhibition pattern. These results indicate that it may be an antithrombotic agent and that it is bound to fibrinogen binding sites of thrombin.     

黄連及厚樸抗菌作用的研究(一)黄連及厚樸在試管內的抗菌作用

在广大之农区及牧区中,中獸医较西獸医为多,而中药之获得,亦较西药为易,无论中药或中獸医,均具有千年以上之经验,其中不乏良药良方。就中药之抗菌作用而言.过去研究者亦不乏人。例如著者曾作六十二种中药抗菌性之初步探讨,发现其中以厚樸及广木香对白色葡萄球菌及枯草桿菌之抗菌作用较强:又如苏联李彼德夫之研究报告,发现四十五种中药中,黄连等六种中药对金色葡萄球菌有抗生作用,及小回回蒜、百部对大肠桿菌有抗生作用;刘国聲亦谓     

Isolation of an anticomplement factor from the venom of the Mojave rattlesnake (Crotalus scutulatus scutulatus)

The venom of the Mojave rattlesnake was fractionated by DEAE-Sephadex column chromatography. A venom fraction, F5, inactivated both human and guinea pig complement. Both serum and purified C3 were partially converted to a protein of faster electrophoretic mobility, indicating that F5 had a direct proteolytic effect on C3. This product was capable of passively lysing guinea pig red blood cells. F5 very effectively inactivated the classical pathway, but only partially inactivated the alternative pathway. The venom fraction worked in a dose-dependent fashion, was heat labile but not lethal to mice at concentrations as high as 10 μg/g mouse weight. Antibodies were produced by immunizing rabbits with F5. The antibodies formed one precipitin line in gels against F5 and also neutralized the complement inactivating activity. The antibodies recognized the venom of the western diamondback rattlesnake, Crotalus atrox, but did not, however, recognize the crude venom of the Mojave rattlesnake.     

Stability of Extruded 17β-Estradiol Solid Dispersions

Recrystallization is one of the main problems concerning the stability of solid dispersions. Different analytical methods were applied showing that no recrystallization occurred after treating melt extruded solid dispersions with 17β-Estradiol as the model drug with heat or water vapor. A skillful choice of excipients—a combination of polymers and additives—could be the reason for improving the stability. The requirements of the USP 23 for Estradiol tablets of 75% dissolved drug after 60 min were fulfilled after storing the tablets for 6 months at 40°C/75% RH. By observing the change in glass transition temperature, DSC analysis showed that the solid dispersions were stable against thermal stress. Isothermal microcalorimetry as well as moisture absorption gravimetry were methods to prove the stability of the solid dispersions against water vapor.     

Effects of purified fruit bromelain fractions on intestinal inflammatory diseases

OBJECTIVE To investigate the effects of purified fruit bromelain fractions on mice colitis, to determine the potential mechanisms underlying the bromelain fractions-induced protect against intestinal inflammation.METHODS The purified fruit bromelain fractions were obtained from pineapple fruit. Mice colitis was established by freely drinking water contained 2.5% dextran sodium sulfate(DSS). After the establishment of colitis model, the four purified bromelain fractions and total bromelain extracts were used to treat colitis. Intestinal Caco-2 cells incubated with LPS were used to establish the barrier dysfunction cellular model in vitro to test whether the purified bromelain fractions can restore intestinal barrier function. Intestinal barrier function was represented by tran-sepithelial electrical resistance(TER) using an epithelial voltohmmeter. We use IEC-6 epithelial cel s and RAW264.7 mouse macrophage to test the drug toxicity and cell viability, use Western blotting to test anti-inflammation and anti-apoptotic effect. RESULTS Gavage administration of purified bromelain fraction one and four have antiinflammation effects. The fraction one and four significantly decreased colitis symptoms which were indicated by HE-staining, macroscopic damage scores, inflammatory response, recovery of intestinal barrier function, as well as attenuated neutrophil infiltration and cytokine profiles;the fraction two and three have some pro-apoptotic effects compared with the fraction one and four. The detail mechanisms underlying the fraction one and four induced treatment effects needs further study. CONCLUSION In this study, purified bromelain fractions are obtained from pineapple fruit, which may be beneficial for the treatment and prevention of intestinal inflammation. The purified bromelain fraction one and four aleviated inflammation and epithelial barrier dysfunction respectively. This study may supply new insights into both the prevention and protection of intestinal inflammation diseases.     

Study of the Effects of Dispase in the Chemotherapy of Multicellular Tumour Spheroids of Small-cell Lung Carcinoma in Man

Multicellular tumour spheroids (MTS), diameter 650 μm, from PC-6, SBC-1 and NCL-H60 small-cell lung carcinoma cell-lines in man were prepared by the liquid overlay culture method and used to study the influence of treatment with dispase (bacterial neutral protease from Bacillus polymyxa, 1000 units mL^?1) on the effectiveness of carboplatin, as determined by colony-forming assay. When carboplatin alone was used on monolayers the curve of survival fraction against concentration was exponential in shape, indicating that the drug was active against the monolayer. When MTS were treated with medium concentrations (10^?5 and 10^?4 m ) of carboplatin alone the survival fraction–concentration curve showed that the effectiveness of the treatment was less than that against the monolayer. On treatment of MTS with carboplatin and dispase the survival fraction–concentration curve was similar to that obtained for the monolayer and the survival fraction of the core of the MTS was also less than when carboplatin alone was used. These results imply that dispase dissolves the intercellular matrix of the MTS enabling enhanced infiltration of carboplatin into the core of the MTS. Dispase thus indirectly increases the effectiveness of carboplatin.     

Arsenic toxicity in a sediment-dwelling polychaete: detoxification and arsenic metabolism

The accumulation, subcellular distribution and speciation of arsenic in the polychaete Arenicola marina were investigated under different laboratory exposure conditions representing a range of metal bioavailabilities, to gain an insight into the physiological mechanisms of how A. marina handles bioaccumulated arsenic and to improve our understanding of the potential ecotoxicological significance of bioaccumulated arsenic in this deposit-feeder. The exposure conditions included exposure to sublethal concentrations of dissolved arsenate, exposure to sublethal concentrations of sediment-bound metal mining mixtures, and exposure to lethal concentrations of sediment-bound metal mining mixtures and arsenic- and multiple metal-spiked sediments. The sub-lethal exposures indicate that arsenic bioaccumulated by the deposit-feeding polychaete A. marina is stored in the cytosol as heat stable proteins (~50%) including metallothioneins, possibly as As (III)-thiol complexes. The remaining arsenic is mainly accumulated in the fraction containing cellular debris (~20%), with decreasing proportions accumulated in the metal-rich granules, organelles and heat-sensitive proteins fractions. A biological detoxified metal compartment including heat stable proteins and the fraction containing metal-rich granules is capable of binding arsenic coming into the cells at a constant rate under sublethal arsenic bioavailabilities. The remaining arsenic entering the cell is bound loosely into the cellular debris fraction, which can be subsequently released and diverted to an expanding detoxified pool. Our results suggest that a metal sensitive compartment comprising the cellular debris, enzymes and organelles fractions may be more representative of the toxic effects observed.     

In-vitro antioxidant and in-vivo photoprotective effect of three lyophilized extracts of Sedum telephium L. leaves

Sedum telephium L. is a medicinal plant used in antiquity to cure many types of inflammatory skin diseases. The leaves (without the external cuticle), are used to promote healing and reduce skin inflammation and pain, and contain various components. We found two major components: flavonol glycosides and polysaccharides, with molecular weight between 13,000 and 13,500 Da. We evaluated the in-vitro antioxidant and in-vivo skin photoprotective effects of three lyophilized extracts obtained from the juice of S. telephium L. leaves: a total lyophilized juice, a lyophilized flavonolic fraction, and a lyophilized polysaccharidic fraction. Two in-vitro models were used: the bleaching of the stable 2,2-diphenyl-1-picrylhydrazyl (DPPH*) radical, and the protective effect against UV-induced peroxidation on phosphatidylcholine multilamellar vesicles, as model membranes. The antioxidant/radical scavenging activity of each lyophilized extract was also assessed in-vivo by determining their ability to reduce UVB-induced skin erythema (monitored by reflectance spectrophotometry) in healthy human volunteers. The findings of the in-vitro experiments clearly demonstrated that, unlike the lyophilized polysaccharidic fraction, the lyophilized flavonolic fraction and total lyophilized juice possess strong antioxidant/free radical scavenging properties, which are likely due to phenolic compounds. Consistent with these findings, gel formulations of both the total lyophilized juice and, to a greater degree, the lyophilized flavonolic fraction appeared to possess a strong protective effect against UV-induced skin erythema in-vivo, whereas the lyophilized polysaccharidic fraction was completely ineffective. The in-vitro and in-vivo results suggest that, both the total lyophilized juice and, in particular, the lyophilized flavonolic fraction, but not the lyophilized polysaccharidic fraction of S. telephium L. leaves, have photoprotective effects against UVB-induced skin damage.     

国产果糖二磷酸钠对42例冠心病心绞痛患者的作用

采用随机双官交叉对照法观察国产FDP对冠心病心绞痛患者的影响.42用心绞痛患者随机分为A、B组.A组给予安慰剂(5%GS100ml)iv gtt,bid×1od;继予FDP 10g iv gtt,bid×10d;B组治疗与A组相同而顺序相反.心绞痛患者分别在安慰剂和FDP治疗前和治疗的最后2d行ECG平板运动负荷试验,24h动态ECG及放射性核素门电路平衡法心血池造影.结果显示:JDP能延长运动持续时间,运动起始至心绞痛发作时间,运动起始至ST段下降1mm时间及运动起始至达到最大ST段下降时间;提高患者所耐受的最大运动负荷和运动起始至ST段下降1mm负荷.增加LVEF和PFR.对静息及运动HR和BP均无显著作用;FDP也能使无病性心肌缺血的时间总和及心肌缺血总负荷减小.提示FDP iv gtt后可在一定程度上改善也定型心绞痛患者的运动能力及左心室功能,减少无症状心肌缺血的发生.     

阿片类戒断综合征中医辨证计量诊断的初步研究

目的 :探讨阿片类戒断综合征中医辨证计量诊断。方法 :在对 4 2 3例阿片依赖戒断者调查的基础上进行了阿片类戒断综合征计量诊断研究 ,采用最大似然法判别分析模型 ,建立阿片类戒断综合征中医辨证计量诊断的指数表。继而运用DME方法 ,对毒瘀内阻寒热错杂证、毒瘀热阻证和毒瘀寒阻证进行了诊断效能的评价。结果 :阿片类戒断综合征中医辨证计量诊断指数表具有良好的诊断效能。结论 :该方法有一定的推广使用价值。     

丹参酮的药理

丹参酮是中药丹参Salvia miltiorrhiza Bunge根的乙醚提取物。其所含十种成分中隐丹参酮、二氢丹参酮Ⅰ、羟基丹参酮Ⅱ-A、丹参酸甲酯及丹参酮Ⅱ-B有抗金黄色葡萄球菌作用。实验是以总丹参酮进行的。体外实验丹参酮对金黄色葡萄球菌,特别是对耐药菌株有抗菌作用,在相同浓度下抗菌作用比小蘖碱强。丹参酮对结核杆菌H37 Rv及两种毛发癣菌有抑制作用。丹参酮口服或皮下给小白鼠,能在组织脏器及尿中检出有抗菌作用的物质。对小白鼠及大白鼠都未见毒性。对三联菌苗致热家兔口服丹参酮有解热作用。实验治疗对金黄色葡萄球菌腹腔感染的小白鼠,口服给丹参酮未见保护作用,但全量的丹参酮与阈下治疗剂量的金霉素合并应用则有明显保护作用。对大白鼠感染性关节肿有治疗作用。对巴豆油引起的小白鼠耳部炎症,丹参酮有抗炎作用。丹参酮片口服及凡士林2%丹参酮油膏外用,在临床观察了455例各种以金葡感染为主的急性炎症,总有效率为90%,特别是对用抗菌素治疗无效的病例改用丹参酮治疗有效。本文对抗菌中药的作用及研究方法进行了初步讨论。     

N—取代—2—氨基—2—噻唑啉类化合物的合成

Ｎ┐取代┐２┐氨基┐２┐噻唑啉类化合物的合成ＰＲＥＰＡＲＡＴＩＯＮＯＦＮ┐ＳＵＢＳＴＩＴＵＴＥＤ┐２┐ＡＭＩＮＯ┐２┐ＴＨＩＡＺＯＬＩＮＥＳ刚典臣＊宋俊林ａ（武汉化工学院，湖北４３００７３；ａ湖北省化学研究所，武汉４３００７４）ＧＡＮＧＤｉａｎ－Ｃｈ...     

Effect of Loperamide on Mucosal Guanylyl Cyclase Activity in Rat Jejunum Following Escherichia coli Heat‐Stable Toxin‐Induced Fluid Accumulation

Abstract: Loperamide has antidiarrhoeal activities against secretagogues with different mechanisms of action. Besides its opioid‐like effect on intestinal motility and secretion it might exhibit additional antisecretory properties which may not be completely elucidated yet. Direct effects of loperamide on mucosal guanylyl cyclase have never been observed. We therefore investigated the effect of loperamide on intestinal fluid transport altered by heat‐stable Escherichia coli enterotoxin which acts by stimulating mucosal guanylyl cyclase. Net fluid movement was determined during a 1 hr incubation period in ligated jejunal loops of anaesthetised female Wistar rats. Transport rates of net fluid movement were calculated from the loop contents measured gravimetrically at the beginning and the end of the experiments. Addition of heat‐stable Escherichia coli enterotoxin to the luminal solution resulted in a net secretion of water which was significantly reversed into net absorption by loperamide. The specific activity of the particulate guanylyl cyclase was determined in mucosal scrapings of the jejunum without and with the addition of heat‐stable Escherichia coli enterotoxin and/or loperamide. Additions of loperamide of up to 10 μmol/l did not change guanylyl cyclase activity. We conclude that the effect of loperamide counteracting heat‐stable Escherichia coli enterotoxin induced changes of intestinal fluid transport does not involve a direct effect on guanylyl cyclase.