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R1128 B (1,3,6-trihydroxy-8-n-butylanthraquinone), a new antibiotic produced by Streptomyces sp. No. 1128, inhibited estrogen binding to its receptor. The IC50 value of R1128 B for partially purified rat uterine cytosol receptor was 1.2 x 10(-7) M. However, the IC50 value of R1128 B against androgen-receptor binding was about 50-fold greater than that against estrogen-receptor binding. R1128 B was a competitive inhibitor against estrogen-receptor binding. R1128 B inhibited the growth of estrogen-responsive human mammary adenocarcinoma MCF-7 cells in soft agar. This inhibition, however, was reversed when estradiol was added to the culture medium. R1128 B showed antitumor activities against MCF-7 both xenografted to nude mice and implanted in subrenal capsule of mice (SRC assay). The potency of R1128 B was about 8-fold lower than that of tamoxifen both in vitro and in vivo.

Tobacco BY-2 cells were synchronized by an aphidicolin treatment, and their beta-tubulin isoforms and their mRNA were analyzed by Western, Northern and dot blottings. The relative ratio of the beta-tubulin isoforms changed with the progress of cell cycle stage. By Northern blot hybridization of poly(A)+RNAs with a cloned carrot beta-tubulin cDNA probe, a single band of about 1.6 kb was detected throughout the cell cycle. Dot blot hybridization showed that beta-tubulin mRNA existed in all stages in the cell cycle at a relatively constant level, though it accumulated slightly more than average at M phase and decreased during G1 phase.

The bronchodilating effect and other related pharmacological properties of SN-408 were studied in comparison with those of isoproterenol, salbutamol and procaterol. SN-408 caused concentration-dependent relaxation of isolated guinea pig trachea via the beta 2-adrenoceptor. The order of relaxation potency was: procaterol greater than SN-408 greater than or equal to isoproterenol greater than salbutamol, but the duration of the action of SN-408 was far longer than those of other beta-agonists. Positive chronotropic and inotropic actions of SN-408 in isolated guinea pig right atria and left atria were less potent than those of other beta-agonists. In isolated guinea pig lung tissues, SN-408 increased cyclic AMP contents. Also in vivo, SN-408 showed dose-dependent bronchodilating action by i.v. administration in anesthetized guinea pigs and by inhalation in conscious guinea pigs. Bronchodilating actions of SN-408 were less potent than those of procaterol and isoproterenol, but the duration of action of SN-408 was far longer than those of other beta-agonists. SN-408 showed no evidence of the development of tolerance to the bronchodilating action. SN-408 caused small tachycardia in guinea pigs by i.v. and inhalation. SN-408 given i.v. suppressed vascular permeability in mice. These results indicate that SN-408 is a long-acting and selective beta 2-stimulant bronchodilator.

Successful En-Bloc Resection of 6 Cases of Large Superficial Esophageal Cancer Using Sodium Hyaluronate and Needle-Knife Makoto Nishimura, Hironori Yamamoto, Kentaro Sugano Background: En-bloc resection by endoscopic submucosal dissection (ESD) is desirable to facilitate accurate histopathological assessment of tissue specimens, and is indispensable in treating the superficially-spreading type of esophageal cancer. A new ESD method using sodium hyaluronate has been developed at our institution for use in endoscopic en-bloc resection of large superficial gastric and colonic lesions. We developed and improved this method for application to large superficial esophageal cancer. This study evaluated the safety and reliability of this newly developed method of performing ESD for esophageal cancer. Methods: Between March 2003 and November 2005, we treated 6 large superficial esophageal cancers over 30 mm in diameter. In all patients, ESD was performed using sodium hyaluronate and a needle-knife. Sodium hyaluronate was used for injection into the submucosa, and mucosal incisions were made with a needle-knife. Results: All lesions were successfully treated by ESD using sodium hyaluronate and a needleknife without significant complications. Only one minor air leakage into the mediastinum occured. The en-bloc resection rate was 100% (6/6). The mean surgical duration was 253 min (range 90-480 min). The mean size of the resected specimen was 39.2 mm in diameter (range 35-50 mm). Histopathological assessment demonstrated that 50% (3/6) of lesions were intramucosal squamous cell carcinoma (m1-m2), and 50% (3/6) of lesions seemed to show submucosal invasion (sm1-sm2). Lateral cut margin was positive in 17% (1/6), and vertical cut margin was positive in 33% (2/6). Therefore, radiation was administered to these two patients. During follow-up (median 10.5 months, range 1-32 months), there were no further residual or recurrent lesions found. Discussion: Injection of sodium hyaluronate creates prolonged submucosal thickening. In addition, carefully cutting only the submucosal layer by needle-knife in combination with pre-coagulation by an electrocoagulator, we could complete en-bloc resection of large esophageal cancer without perforation or severe bleeding, then perform radiation based on a accurate histopathological assessment. Based on our experience in these 6 cases, we conclude that this new method is safe and useful for large superficially-spreading esophageal cancers.

体積受熱型ソーラコレクタの集熱効率は層内自然対流を抑制することにより改善される.この抑制法として, 作動流体層を透明な仕切板によりマルチレイヤ化し, 対流が発生するゾーンを小さくすることが考えられる.本研究では, マルチレイヤ化した体積受熱型ソーラコレクタの集熱特性について検討するために, 1層および2層のコレクタを用い, 種々の流量において層内温度分布および集熱効率を測定した.また, 層内自然対流を考慮に入れた理論解析を行い, 実験結果と比較検討し, さらに, 種々の因子の影響について考察を行った.その結果, 作動流体層のマルチレイヤ化は層内自然対流の抑制に有効であることが認められ, また, 操作条件に対して最適な分割数が存在することが見い出された.

気泡塔に一部あるいは全部を多孔としたドラフトチューブを備えた場合の流動状態, 液の混合時間, ガスホールドアップおよび気液界面積について実験的に検討した. これらの流動特性にはドラフトチューブの径・長さ, 多孔部分の割合, 孔径, 開孔率により影響されることが認められた.多孔部分において気液の半径方向の流れが起こり, ガスが多孔部分を通過する際に微細化された. また, 環状部においては, 気液の下向流れとドラフトチューブ内部から出てきたガスが接触し, 気液が激しく混合した.多孔ドラフトチューブを用いた場合の液の混合時間は, 無孔ドラフトチューブを用いた場合あるいはドラフトチューブを用いない場合よりも著しく短くなり, 混合時間の減少度合は多孔部分の割合に強く依存した.同一通気速度においては, 多孔ドラフトチューブにすると, 無孔ドラフトチューブの場合より, ガスホールドアップは低くなるが, 気液界面積は高くなった.

The hydrocracking of coal extracts was performed using as catalysts (in the same weight as the extract used) three kinds of molten salts, ZnCl2, ZnCl2-CuCl (3:2mol), and ZnCl2-KCl (3:2mol) at 350°C under the initial hydrogen pressure of 100kg/cm2 for 3hr. The ZnCl2-KCl system was found to be the most satisfactory for achieving the highest yields of hexanesoluble fractions and suppressing the production of undesirable gases and benzene-insoluble fractions. The maximum yield of hexane soluble was obtained when the mol per cent of KCl was 20-40. Analyses of the resulting hexane solubles indicated that the oxygen percentage, fa, and the molecular weight decreased in the order: ZnCl2-KCl (4:6mol>5:5>6:4> 7:3>8:2)>ZnCl2>ZnCl2-CuCl. These findings could be rationalized in terms of the acid strengths of the molten salts. Further characterization of hexane solubles was made by using adsorption chromatography on Floridil which gives the oil and resin fractions. The elemental analyses of resin fractions coupled with their i.r. measurements showed that the increasing amount of ZnCl2 in the ZnCl2-KCl system could bring about the progressive deoxygenation reactions of hexane solubles. The hydrocracking of each extract from Big Ben coal and Indian Ridge coal was also undertaken; these results were compared with those of Taiheiyo coal extracts based on the average molecular structure of each extract deduced by using a computer-assisted method.

半透過性PCM (相変化物質) 平板に直接太陽光をあて, 加熱融解するパッシブな太陽熱蓄熱システムに関して, 温度分布, 蓄熱効率に及ぼす光学的厚さの影響を検討した.PCMとしてパラフィンワックスを用い, 吸収係数を変化させるため黒色染料を添加した.PCMと保温層 (底背面断熱) とから成る試料平板について一定入射量の擬似太陽光の下で実験を行った.同時に, 総括比熱の概念に基づく理論解析を試みた.その結果, 本実験範囲では理論解析結果と実験結果はかなり良好な一致を示し, 理論解析の妥当性が確かめられた.また, PCMの光学的厚さの大きさによって温度分布, 蓄熱効率が大きく異なることが明らかになった.さらに, 光学的厚さが小さい場合, 内部融解 (back melting) となり, 蓄熱効率の面で有利であることがわかった.

Flow characteristics of the downflow bubble column with a simultaneous gas-liquid injection nozzle were experimentally investigated. The flow pattern was observed and ranges of stable cocurrent downflow operation were examined. Gas holdup and specific gas-liquid interfacial area were measured. When the simultaneous gas-liquid injection nozzle was used in the downflow bubble column, spouting and calm sections were observed to appear in the column. In the spouting section, gas holdup was higher and interfacial area was larger than those in the calm section. In comparison with the results for the perforated sparger, the bubble diameter was smaller and the range of stable cocurrent downflow operation was wider. In addition, it was found that, under a specified condition, the gas holdup was lower and the interfacial area was larger than those in the case of the perforated sparger, and that such differences became more marked with decreasing nozzle diameter and with increasing liquid velocity.

ガス吸込み式気液同時吹込みノズルを備えた気泡塔の流動特性について実験的に検討した.吸込みガス量およびガスホールドアップは, 液流量の増加につれて, 増大した.また, 前回報告したエアリフトと気液同時吹込みノズルを組合せた場合と比較した.本測定条件下では, 吸込みガス量についてのノズル部の最適寸法は次のようであった.ノズル長さ/ノズル径= 20 ～ 30オリフィス径/ノズル径 =0.5 ～ 0.6また, ノズル径 30mm以下では, ノズル径が大きいほど, 動力当たりの吸込みガス量は高くなった.一方, ガスホールドアップについては, 操作条件により最適ノズル径が変った.気泡塔内においては, エアリフトと組合せた場合と同様, 噴流部および斉流部が観察され, 気泡径は小さく, ガスホールドアップおよび気液界面積は高くなった.ガスホールドアップ, 気液界面積のエネルギー効率は本方式の方がエアリフト式よりも高かった.

気液同時吹込みノズルと外部循環式エアリフトを組合せた気泡塔における流動特性について実験的に検討した, 塔径0.164m, 塔高1.70, 2.70, 3.90mの気泡塔を用い, ノズル径を20, 25および40mmと変えて, 流動状態の観察およびガスホールドアップ, 循環液流量の測定を行った.また, 亜硫酸ナトリウム水溶液による酸素吸収量を測定し, 気液界面積についての考察を行った.その結果, 本組合せ方式により優れた気液接触効率の得られることが知られた.すなわち, ガス速度が高い場合には, 気泡塔内に噴流部および斉流部が観察され, ガスホールドアップおよび気液界面積は液流れのない場合よりも大きくなった.これらの増大効果はノズル径の影響を受け, 最適ノズル径の存在することが認められた.また, 本測定範囲においては塔高が高いほどガスホールドアップおよび気液界面積は大きくなった.ガスホールドアップおよび気液界面積の実験式を算出した。これらの実験式とエネルギ収支式に基づく計算値は, ±15%以内の誤差で実測値とほぼ一致した.

The new families of aluminate glasses obtained by the present authors from their melts in the systems K2O–Ta2O5–Al2O3, Na2O–K2O–Ta2O5–Al2O3, K2O –Cs2O– Ta2O5–Al2O3, K2O–Nb2O5–Al2O3, Na2Oz.sbnd;K2O–TiO2–Al2O3, BaO–TiO2–Al2O3, BaO–ZrO2–TiO2–Al2O3 and Na2O–K2O–BaO–ZrO2–Ta2O5–TiO2 –Al2O3 showed high transmissions of visible and infrared (IR) radiation ranging from 0.4 to about 6 μm, as well as high refractive indices up to 2.0. Their physical and chemical properties such as glass-forming ability, softening temperature, hardness and hygroscopicity were comparable to conventional silicate glasses. These properties are useful for IR applications. The cause of the high IR transmission of the aluminate glasses was interpreted in terms of the masses of the constituent cations and the single bond strengths of the cations with oxygen ions.

The critical operation condition for complete countercurrent flow may be extended by enlarging the bottom of the bubble column. Several cylindrical enlarged sections of different diameter and length were examined and the critical liquid velocities were measured.It was found that the critical liquid velocity increased with increasing diameter or length of the enlarged section. An experimental equation for the critical liquid velocity was deduced.Higher gas holdup and liquid-phase overall mass transfer coefficient were obtained in the bubble column with enlarged bottom and correlating equations were derived.

The structure of FR900840, a new antitumor antibiotic produced by a strain of Streptomyces has been deduced as 1 on the basis of spectroscopic and chemical evidence and finally confirmed by synthesis from L-threonine and L-serine.

ドラフトチューブを挿入した内径0.164m, 高さ2.2mの三相流動層の流動特性について実験的に検討した.ガスには空気, 液には水, 固体には液より密度の高いナイロンまたは液より密度の低いポリプロピレンの径約3mmの粒子を用い, ドラフトチューブの内部あるいは環状部へ通気した三相流動層にて実験を行った.ある通気速度以上では, 安定した循環流が生じ固体は高さ方向に均一に分布したが, この条件下で以下のことが観察された.ガスホールドアップは通気速度の増加につれて増大し, ドラフトチューブ径が大きく固体がポリプロピレンの場合を除くと, 環状部通気の方が内部通気よりも高くなった.固体ホールドアップは通気速度が高くなると通気速度の影響を受けず, ほぼ一定となった.液の循環流量は通気速度の増加につれて増大した.また, 同一通気速度においては外塔径の約0.6倍のドラフトチューブ径にて最大値を示した.固体とガスの循環流量は液の循環流量に大きく支配された.

7種の気泡塔 (塔径50, 70, 94,114,164,200および280mm, 塔高5000mm) を用いて, 上向並流, 向流および下向並流操作にわたる気液速度において, 流動状態の観察およびガスホールドアップと気液界面積の測定を行った.ガスには空気, 液には水道水および硫酸ナトリウム水溶液を用いた.また, 気液界面積の測定には亜硫酸ナトリウムの酸化反応を利用した.流動状態の変わる気液速度は塔径および液種により異なり, その変移は気液相対速度により判定された.ガスホールドアップに関しては気泡流とチャーン乱流に大別して実験式を導出したが, 140mm以上の塔径では, いずれの気液流れ方向においてもガスホールドアップに及ぼす塔径の影響は現れなかった.気液界面積はガスホールドアップに大きく支配されるが, 気泡流とチャーン乱流ではガスホールドアップに対する傾向が異なった.

In anesthetized dogs, pressor and hyperglycemic effects of Ephedra aqueous extract as well as its alkaloid fraction and adsorption of alkaloid from the digestive tract were studied in order to investigate how closely effects of the alkaloid fraction relate to those of the Ephedra extract itself. Blood pressure, heart rate, and blood glucose concentration were increased by intraduodenal administration of the extract and the alkaloid fraction on the bases of the same alkaloid content (20 mg/Kg). In respect to the pressor and hyperglycemic effects, changes in time course of the effects produced by these two drug preparations were similar and in either of the two physiological parameters the maximal value given by the extract was about a half that given by the alkaloid fraction. A maximal level of blood pressure and blood glucose concentration was reached 10-15 min after the administration of the two drug preparations, while the amount of alkaloid absorbed in the portal vein until this time was about 2-3 times as much under administration of the alkaloid fraction as under administration of the extract. Absorption of alkaloid in the extract occurred slowly and lasted longer compared with that of the alkaloid fraction itself. On the contrary, the alkaloid-free extract administered intraduodenally showed no virtual effects on blood pressure and blood glucose concentration except producing tachycardia. It seems that the effect of Ephedra extract on blood pressure and blood glucose concentration was mostly qualitatively and quantitatively represented by that of alkaloid contained and that effect of the extract mainly depended on that of alkaloid absorbed early after its application.

Twenty-one patients with cerebrovascular disease (5 with hemorrhage, 10 with infarction, 2 with TIA, 4 with motor disturbance of unknown cause) were studied using N-isopropyl-p-(123I)iodoamphetamine (123I-IMP) and single photon emission CT. In 3 of 5 cases with cerebral hemorrhage, perfusion defects were shown in and around the region of hematomas, furthermore, one of the cases with internal capsular hematoma, the perfusion defect extended to the cortical area corresponding to the neurological pathway. In one case with MCA infarction, the perfusion defect was greater and clearer than the low density area on X-ray computed tomography (CT). These results revealed the 123I-IMP study provides physiological information in contrast with X-ray CT which provides anatomical information. In 3 of 9 cases with multiple small deep hemispheric infarctions on X-ray CT, the perfusion to the basal ganglia was suspected to be decreased on 123I-IMP images. However, this visual findings was not definitive and, in fact, the diseased side was not always consistent with the clinical findings. For quantitative analysis, symmetrical regions of interest (ROIs) were constructed both basal ganglia and the ratio of average counts over the ROI to those over the whole slice was calculated. In the small infarction group, the mean +/- S.D. of the values was 0.89 +/- 0.09 in right and 0.89 +/- 0.08 in left. Although the values were not significantly different from those of normal subjects (0.99 +/- 0.02 in right, 0.97 +/- 0.03 in left), they distributed in the range less than normal in 5 of 9 cases. This method was thought to be useful and practical to evaluate the cerebral blood flow in basal ganglia of patients with deep hemispheric infarction.

A new antitumor antibiotic, FR900840, was isolated from a culture broth of Streptomyces strain No. 8727 as a pale yellowish prism and the molecular formula was determined to be C7H11N3O5. The antibiotic exhibited prominent antitumor effects on human tumor cell lines both in vitro and in vivo.

R&D of launch vehicles, satellites and the Japanese Experiment Module to be connected to the Space Station is traced with special emphasis on their tribological problems encountered on the way of space development in Japan. Lubrication, friction and wear of rolling bearings and seals applied to turbopumps of an LE-5, the first LOX/LH2 engine completed in Japan, are discussed. Performance on orbit of ball bearings supporting the scanning mirrors of the earth sensors launched ill 1981 is introduced including test results of candidate materials used for cages. Compared to conventional rolling bearings, magnetic bearings have the merit of no friction and wear. Results obtained from experiments of the magnetically supported flywheel brought into orbit in 1987 are described. Furthermore several tribological problems tribologists confront in designing the Japanese Experiment Module are refered.

Gas entrainment by liquid flowing downward into a downcomer was considered to be applicable as a method of gas transport. By using downcomer s of different diameter and length, the gas entrainment was experimentally examined.The flow pattern in the downcomer changed with increasing liquid flow rate : annular flow, slug flow, and mixed flow. The ratio of gas/liquid flow rates showed the maximum during liquid flow rate in the slug flow regime. Under the present experimental conditions, the maximum ratio of gas/ liquid flow rates increased with decreasing downcomer diameter.