Active, water-insoluble derivatives of D-glucose oxidase and alginic acid, chitin, and Celite

Treatment of 2-benzimidazolemethanol (4) with methanesulfonyl chloride and pyridine in chloroform afforded 2-(chloromethyl)-1-(methylsulfonyl)benzimidazole (6), which was also prepared by methanesulfonylation of 2-(chloromethyl)benzimidazole. Methanesulfonylation of α-(2-benzimidazolyl)benzyl alcohol (8) in chloroform yielded 2-(α-chlorobenzyl)-1-(methylsulfonyl)benzimidazole. 1-(Methylsulfonyl)-2-benzimidazolemethanol was obtained on methanesulfonylation of 4 pyridine at 0°, and α-[1-(methylsulfonyl)-2-benzimidazolyl]benzyl alcohol (12) was prepared from 8 by using the same reaction conditions. The reaction of 1-acetyl-2-(chloromethyl)-benzimidazole with silver methanesulfonate in benzene gave 1-acetyl-O-(methylsulfonyl)-2-benzimidazolemethanol. Compound 6 has some antitumor activity in the KB cell-culture system, and some antibacterial activity in the Staphylococcus aureus test-system; it is also active in preventing anaphylactic shock in a mouse test-system.     

Design,synthesis, and evaluation of anti-inflammatory,analgesic, ulcerogenicity,and nitric oxide releasing studies of novel indomethacin analogs as non-ulcerogenic derivatives

Most non-steroidal anti-inflammatory drugs (NSAIDs) suffer from the deadlier gastrointestinal (GI) toxicities. The free -COOH group is responsible for the GI toxicity associated with all traditional NSAIDs. In the present research work, the main objective was to develop new chemical entities as potential anti-inflammatory agents with no GI toxicities. The results of synthesis and pharmacological screening of a series of hybrid molecules having general formula 2-(5-(5-(substituted phenyl)-2-oxo-ethylthio)-1,3,4-oxadiazole-2-yl)-2-phenyl-1H-indol-1-yl)-2-oxoethyl nitrate are described. These compounds were tested in vivo for their anti-inflammatory, analgesic, and ulcerogenic properties, and subjected to histopathological studies. Compound 7c, 2-(5-(5-(3-hydroxyphenyl)-2-oxo-ethylthio)-1,3,4-oxadiazole-2-yl)-2-phenyl-1H-indol-1-yl)-2-oxoethyl nitrate, was the most potent in this series. The compounds that showed significantly reduced GI ulcerogenicity also showed promising results in histopathological studies, and they were found to cause no mucosal injury. All the synthesized compounds were found to exhibit significant nitric oxide releasing activity in an in vitro method. In conclusion, the designed hybrid molecules were found to be significantly promising.     

Roles of vasoconstrictor prostaglandins, COX-1 and -2, and AT1, AT2, and TP receptors in a rat model of early 2K,1C hypertension

Angiotensin (ANG) II activating type 1 receptors (AT(1)Rs) enhances superoxide anion (O(2)*(-)) and arachidonate (AA) formation. AA is metabolized by cyclooxygenases (COXs) to PGH(2), which is metabolized by thromboxane (Tx)A(2) synthase to TxA(2) or oxidized to 8-isoprostane PGF(2alpha) (8-Iso) by O(2)*(-). PGH(2), TxA(2), and 8-Iso activate thromboxane-prostanoid receptors (TPRs). We investigated whether blood pressure in a rat model of early (3 wk) two-kidney, one-clip (2K,1C) Goldblatt hypertension is maintained by AT(1)Rs or AT(2)Rs, driving COX-1 or -2-dependent products that activate TPRs. Compared with sham-operated rats, 2K,1C Goldblatt rats had increased mean arterial pressure (MAP; 120 +/- 4 vs. 155 +/- 3 mmHg; P < 0.001), plasma renin activity (PRA; 22 +/- 7 vs. 48 +/- 5 ng x ml(-1) x h(-1); P < 0.01), plasma malondialdehyde (1.07 +/- 0.05 vs. 1.58 +/- 0.16 nmol/l; P < 0.01), and TxB(2) excretion (26 +/- 4 vs. 51 +/- 7 ng/24 h; P < 0.01). Acute graded intravenous doses of benazeprilat (angiotensin-converting enzyme inhibitor) reduced MAP at 20 min (-36 +/- 5 mmHg; P < 0.001) and excretion of TxA(2) metabolites. Indomethacin (nonselective COX antagonist) or SC-560 (COX-1 antagonist) reduced MAP at 20 min (-25 +/- 5 and -28 +/- 7 mmHg; P < 0.001), whereas valdecoxib (COX-2 antagonist) was ineffective (-9 +/- 5 mmHg; not significant). Losartan (AT(1)R antagonist) or SQ-29548 (TPR antagonist) reduced MAP at 150 min (-24 +/- 6 and -22 +/- 3 mmHg; P < 0.001), whereas PD-123319 (AT(2)R antagonist) was ineffective. Acute blockade of TPRs, COX-1, or COX-2 did not change PRA, but TxB(2) generation by the clipped kidney was reduced by blockade of COX-1 and increased by blockade of COX-2. 2K,1C hypertension in rats activates renin, O(2)*(-), and vasoconstrictor PGs. Hypertension is maintained by AT(1)Rs and by COX-1, but not COX-2, products that activate TPRs.     

Prolamellar bodies of oat,wheat, and rye: Structure,lipid composition,and adsorption of saponins

Summary Soybean seedlings (Glycine max) were incubated in narrow temperature regimes to study the effects of heat shock on cell structures. The incubation temperatures used were as follows: 1. 28 °C (2h); 2. 40 °C (2h); 3. 45 °C (2h); 4. 40 °C (2h)45 °C (2h); 5. 47. 5 °C (10 min); 6. 40 °C (2h)47. 5 °C (10 min). Both optical and electron micrographs were taken of the different tissues of root meristems as they responded to heat shock. Cells of roots heated to 45 °C (2h) or 47.5 °C (10 min) with lethal treatment showed drastic heat injuries:e.g., membrane damage, coagulated plasmolysis, protoplasmic contraction, and leakage of cell content. Nucleolar segregation occurred in cells treated at both lethal and supraoptimal temperatures. Seedlings preincubated at 40 °C (2 h) became thermo-tolerant to lethal temperature treatment of 45 °C (2 h) or 47.5 °C (10 min), by protecting the plasmalemma, mitochondria, plastids and nuclei from heat damage. Without preincubation, however, these structures were destroyed.Abbreviations CC Central cylinder - CR Cortex - M Mitochondria - N Nuclei - Nu Nucleoli - P Plastids - RC Root cap - RE Region of elongation - RM Region of meristem     

Thermodynamics of hydrolysis of disaccharides. Lactulose, alpha-D-melibiose, palatinose, D-trehalose, D-turanose and 3-o-beta-D-galactopyranosyl-D-arabinose

High-pressure liquid chromatography and microcalorimetry have been used to study the thermodynamics of the hydrolysis reactions of a series of disaccharides. The enzymes used to bring about the hydrolyses were: beta-galactosidase for lactulose and 3-o-beta-D-galactopyranosyl-D-arabinose; beta-glucosidase for alpha-D-melibiose; beta-amylase for D-trehalose; isomaltase for palatinose; and alpha-glucosidase for D-turanose. The buffer used was sodium acetate (0.02-0.10 M and pH 4.44-5.65). For the following processes at 298.15 K: lactulose(aq) + H2O(liq) = D-galactose(aq) + D-fructose(aq), K0 = 128 +/- 10 and delta H0 = 2.21 +/- 0.10 kJ mol-1; alpha-D-melibiose(aq) + H2O(liq) = D-galactose(aq) + D-glucose(aq), K0 = 123 +/- 42 and delta H0 = -0.88 +/- 0.50 kJ mol-1; palatinose(aq) + H2O(liq) = D-glucose(aq) + D-fructose(aq), delta H0 = -4.44 +/- 1.1 kJ mol-1; D-trehalose(aq) + H2O(liq) = 2 D-glucose(aq), K0 = 119 +/- 10 and delta H0 = 4.73 +/- 0.41 kJ mol-1; D-turanose(aq) + H2O(liq) = D-glucose(aq) + D-fructose(aq), delta H0 = -2.68 +/- 0.75 kJ mol-1; and 3-o-beta-D-galactopyranosyl-D-arabinose(aq) + H2O(liq) = D-galactose(aq) + D- arabinose(aq),0H0 = 107 +/- 10 and delta H0 = 2.97 +/- 0.10 kJ mol-1.(ABSTRACT TRUNCATED AT 250 WORDS)     

Synthesis of carbohydrate analogs (positional,configurational, and optical) of N-acetylmuramoyl-l-alanyl-d-isoglutamine,and their immunoadjuvant activities

2-Acetamido-2-deoxy-4- and -6-O-(d-2-propanoyl-l-alanyl-d-isoglutamine)-d-glucopyranose, 2-acetamido-2-deoxy-3-O-(d-2-propanoyl-l-alanyl-d-isoglutamine)-d-allopyranose, -d-gulopyranose, -d-galactopyranose, -d-mannopyranose, and -l-idopyranose, and 3-O-(d-2-propanoyl-l-alanyl-d-isoglutamine)-d- and -l-glucopyranose were synthesized, in order to clarify the structural requirements for the immunoadjuvant activity of the carbohydrate moiety in N-acetylmuramoyl-l-alanyl-d-isoglutamine. Immunoadjuvant activity of the N-acetylmuramoyl-dipeptide analogs was examined in guinea-pigs.     

Bacteriochlorophyll c monomers,dimers, and higher aggregates in dichloromethane,chloroform, and carbon tetrachloride

Bacteriochlorophyll c in vivo is a mixture of at least 5 homologs, all of which form aggregates in CH₂Cl₂, CHCl₃ and CCl₄. Three homologs exist mainly in the 2-R-(1-hydroxyethyl) configuration, whereas the other two homologs, 4-isobutyl-5-ethyl and 4-isobutyl-5-methyl farnesyl bacteriochlorophyll c, exist mainly in the 2-S-(1-hydroxyethyl) configuration (Smith KM, Craig GW, Kehres LA and Pfennig N (1983) J. Chromatograph. 281: 209–223). In CCl₄ the S-homologs form an aggregate of 2–3 molecules whose absorption (747 nm maximum) and circular dichroism spectra resemble those of the chlorosome. In CH₂Cl₂, CHCl₃ and CCl₄ the 4-n-propyl homolog (R-configuration) forms dimers absorbing at ca. 680 nm and higher aggregates absorbing at 705–710 nm. In CCl₄ the dimerization constant is approx. 10 µM^–1 (1000 times that for chlorophyll a). The difference between the types of aggregates formed by the 4-n-propyl and 4-isobutyl homologs is attributed to the difference between the R- and S-configurations of the 2-(1-hydroxyethyl) groups in each chlorophyll.Abbreviations BChl bacteriochlorophyll - CD circular dichroism - Chl chlorophyll - DNS data not shown - EEF 4-ethyl-5-ethyl farnesyl - iBM/EF 4-isobutyl-5-methyl/ethyl farnesyl - MEF 4-methyl-5-ethyl farnesyl - PEP 4-n-propyl-5-ethyl farnesyl     

Chemoenzymatic synthesis of 2-azidoethyl-ganglio-oligosaccharides GD3, GT3, GM2, GD2, GT2, GM1, and GD1a

We have synthesized several ganglio-oligosaccharide structures using glycosyltransferases from Campylobacter jejuni. The enzymes, alpha-(2-->3/8)-sialyltransferase (Cst-II), beta-(1-->4)-N-acetylgalactosaminyltransferase (CgtA), and beta-(1-->3)-galactosyltransferase (CgtB), were produced in large-scale fermentation from Escherichia coli and further characterized based on their acceptor specificities. 2-Azidoethyl-glycosides corresponding to the oligosaccharides of GD3 (alpha-D-Neup5Ac-(2-->8)-alpha-D-Neup5Ac-(2-->3)-beta-D-Galp-(1-->4)-beta-D-Glcp-), GT3 (alpha-D-Neup5Ac-(2-->8)-alpha-D-Neup5Ac-(2-->8)-alpha-D-Neup5Ac-(2-->3)-beta-D-Galp-(1-->4)-beta-D-Glcp-), GM2 (beta-D-GalpNAc-(1-->4)-[alpha-D-Neup5Ac-(2-->3)]-beta-D-Galp-(1-->4)-beta-D-Glcp-), GD2 (beta-D-GalpNAc-(1-->4)-[alpha-D-Neup5Ac-(2-->8)-alpha-D-Neup5Ac-(2-->3)]-beta-D-Galp-(1-->4)-beta-D-Glcp-), GT2 (beta-D-GalpNAc-(1-->4)-[alpha-D-Neup5Ac-(2-->8)-alpha-D-Neup5Ac-(2-->8)-alpha-D-Neup5Ac-(2-->3)]-beta-D-Galp-(1-->4)-beta-D-Glcp-), and GM1 (beta-D-Galp-(1-->3)-beta-D-GalpNAc-(1-->4)-[alpha-D-Neup5Ac-(2-->3)]-beta-D-Galp-(1-->4)-beta-D-Glcp-) were synthesized in high yields (gram-scale). In addition, a mammalian alpha-(2-->3)-sialyltransferase (ST3Gal I) was used to sialylate GM1 and generate GD1a (alpha-D-Neup5Ac-(2-->3)-beta-D-Galp-(1-->3)-beta-D-GalpNAc-(1-->4)-[alpha-D-Neup5Ac-(2-->3)]-beta-D-Galp-(1-->4)-beta-D-Glcp-) oligosaccharide. We also cloned and expressed a rat UDP-N-acetylglucosamine-4'epimerase (GalNAcE) in E. coli AD202 cells for cost saving in situ conversion of less expensive UDP-GlcNAc to UDP-GalNAc.     

Synthesis and Biological Evaluation of 1,3-Oxathiolane 5-Azapyrimidine, 6-Azapyrimidine,and Fluorosubstituted 3-Deazapyrimidine Nucleosides

Abstract

(2R,5S)-5-Amino-2-[2-(hydroxymethyl)-1,3-oxathiolan-5-y1]-1,2,4-triazine-3(2H)-one (8) and (2R,5R)-5-amino-2-[2-(hydroxymethyl)-1,3-oxathiolan-5-y1]-1,2,4-triazine-3(2H)-one (9) have been synthesized via a multi-step procedure from 6-azauridine. (2R,5S)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-y1]-1,3,5-triazine-2(1H)-one (11) and (2R,5R)-4-amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-y1]-1,3,5-triazine-2(1H)-one (12), and the fluorosubstituted 3-deazanucleosides (19–24) have been synthesized by the transglycosylation of (2R,5S)-1-{2-[[(tert-butyldiphenylsilyl) oxy]methyl]-1,3-oxathiolan-5-y1} cytosine (2) with silylated 5-azacytosine and the corresponding silylated fluorosubstituted 3-deazacytosines, respectively, in the presence of trimethylsilyl trifluoromethanesulfonate as the catalyst in anhydrous dichloroethane, followed by deprotection of the blocking groups. These compounds were tested in vitro for cytotoxicity against L1210, B₁₆F₁₀, and CCRF-CEM tumor cell lines and for antiviral activity against HIV-1 and HBV.     

Exercise hyperventilation, dyspnea sensation, and ergoreflex activation in lone atrial fibrillation

Lone atrial fibrillation may be associated with daily life disability and exercise limitation. The extracardiac pathophysiology of these effects is poorly explored. In 35 subjects with lone atrial fibrillation (mean age 67 +/- 7 yr), we investigated pulmonary function, symptom-limited cardiopulmonary exercise performance, muscle ergoreflex (handgrip exercise) contribution to ventilation, and brachial artery flow-mediated dilation (as a measure of endothelial function) before and after (average interval 20 +/- 5 days) restoring sinus rhythm with external cardioversion. Respiratory volumes and lung diffusing capacity at rest were within normal limits during both atrial fibrillation and after restoring sinus rhythm. Cardioversion was associated with the following changes: a decrease of the slope of exercise ventilation vs. CO2 production (from 35 +/- 5 to 29 +/- 3; P <0.01) and of dyspnea sensation (Borg score from 4 to 2) and an increase of peak oxygen uptake (Vo2; from 16 +/- 4 to 20 +/- 5 ml.min(-1).kg(-1); P <0.01), Vo2 at anaerobic threshold (from 11 +/- 2 to 13 +/- 2 ml.min(-1).kg(-1); P <0.05), and O2 pulse (from 8 +/- 3 to 11 +/- 3 ml/beat; P <0.01). After cardioversion, the observed improvement in ventilatory efficiency was accompanied by a significant peak end-tidal CO2 increase (from 33 +/- 2 to 37 +/- 2 mmHg; P <0.01) and no changes in dead space-to-tidal volume ratio (from 0.23 +/- 0.03 to 0.23 +/- 0.02; P=not significant). In addition, the ergoreflex contribution to ventilation was remarkably attenuated, and the brachial artery flow-mediated dilatation was significantly augmented (from 0.32 +/- 0.07 to 0.42 +/- 0.08 mm; P <0.01). Ten patients had atrial fibrillation relapse and, compared with values after restoration of regular sinus rhythm, invariably showed worsening of endothelial function, exercise ventilatory efficiency, and muscle ergoreflex contribution to ventilation. In subjects with lone atrial fibrillation, an impairment in ventilatory efficiency appears to be involved in the pathophysiology of exercise limitation, and to be primarily related with a demodulated peripheral control of ventilation.     

Design,Synthesis, and Insecticidal Activities of Novel meta-Diamide Compounds Containing Ethyl Acetate and Their Derivatives

In this study, a series of meta-diamide compounds containing ethyl acetate group and their derivatives were designed and synthesized. Their insecticidal activities against Plutella xylostella, Spodoptera frugiperda and Alfalfa sprouts were evaluated. Preliminary bioassays showed that some of the title compounds exhibited excellent insecticidal activities. Especially compound ethyl N-(3-((2-bromo-4-(perfluoropropan-2-yl)-6-(trifluoromethyl)phenyl)carbamoyl)-2-fluorophenyl)-N-(4-cyanobenzoyl)glycinate and ethyl N-(3-((2-bromo-4-(perfluoropropan-2-yl)-6-(trifluoromethyl)phenyl)carbamoyl)-2-fluorophenyl)-N-(6-fluoronicotinoyl)glycinate showed 100 % mortality at 0.1 mg/L against Plutella xylostella and Spodoptera frugiperda, same to broflanilide. Their LC₅₀ against Plutella xylostella is 0.286 mg/L and 0.0218 mg/L, respectively. Moreover, compound ethyl N-(3-((2-bromo-4-(perfluoropropan-2-yl)-6-(trifluoromethyl)phenyl)carbamoyl)-2-fluorophenyl)-N-(6-fluoronicotinoyl)glycinate displayed faster control efficacy than broflanilide at 0.1 mg/L. The results indicated that meta-diamide compounds containing ethyl acetate group could be developed as novel and promising insecticides.     

Morphology of juvenile stages of Birsteinius clavatus (Acari, Oribatida, Liacaridae)

The morphology of the juvenile stages of the mite Birsteinius clavatus (Oribatida, Liacaridae) is described and illustrated. The body and legs possess a granular cerotegument. The nymphs possess exuviae (this fact is mentioned for Liacaridae for the first time). Sensilla are well developed, possessing elongate spindle-shaped hairs, with noticeable swelling and flagellate tip. Interlamellar setae are long, setiform in larva, and small thornshaped in nymphs. Gastronotic setae are long, barbed, possessing flagellate tips. Setal formulae of the body (larva to tritonymph) are the following: genital (0-1-2-4), aggenital (0-0-1-1), anal (0-0-0-2), adanal (0-0-3-3), gastronotic (11-12-12-12) and epimeral setae (3-1-2, 3-1-2-1, 3-1-2-2, 3-1-3-3). Palpal tarsus possesses 8 setae and a single solenidion; the solenidion is not fused with any seta. Femora I and IV possess very long seta. Juvenile stages of B. clavatus combine morphological features of Liacarus (Liacaridae) and Gustavia (Gustaviidae). Norton’s hypothesis (1983) on phylogenetic relations in Gustavioidea is discussed.     

Mucronustyrene,mucronulastyrene and villostyrene,cinnamylphenols from Machaerium mucronulatum and M. villosum

The wood of Machaerium mucronulatum contains, in addition to chalcones and isoflavonoids, the cinnamylphenols mucronustyrene[E-1-(4-hydroxy-2,3-dimethoxybenzyl)-2-phenylethylene], mucronulastyrene[Z-1-(4-hydroxy-2,3-dimethoxybenzyl)-2-phenylethylene] and villostyrene [Z-I-(4-hydroxy-2,3-dimethoxybenzyl)-2-(2-methoxyphenyl)-ethylene. Isoflavonoids and villostyrene were also found in the heartwood of M. villosum. The structural determination of the cinnamylphenols relied on spectra, degradations and syntheses.     

基质金属蛋白酶-2、-9及其组织抑制因子(TIMPs)在动情周期大鼠子宫中的表达(英文)

基质金属蛋白酶（ＭＭＰｓ）家族的作用是降解所有细胞外基质,其活性受其特异性组织抑制因子（ＴＩＭＰｓ）的抑制。细胞外基质成分的降解与重组在动物生殖生长过程中起重要作用,其变化可以通过ＭＭＰｓ和ＴＩＭＰｓ两者表达水平的变化进行监测。大鼠虽然没有月经形成,但是在其子宫内膜也出现类似灵长类的生殖生物学变化。本文从ＭＭＰｓ和ＴＩＭＰｓ两者的表达水平,对大鼠子宫内膜的这些变化进行了研究。于大鼠动情周期的不同时期,将其处死、取子宫制备酶粗提液和组织切片,采用酶谱法（ｚｙｍｏｙｒａｎｈｎ）和原位杂交方法研究动情周期大鼠子宫中ＭＭＰ－２和－９的活性变化以及ＭＭＰ－２、－９和ＴＩＭＰ－１、－２、－３ｍＲＮＡ的表达。并通过光密度扫描方法对酶谱结果进行半定量分析。所用杂交探针见Ｔａｂｌｅ１。酶谱结果显示：在动情周期大鼠子宫中只检测到６７ｋＤａ的ＭＭＰ－２活性,而没有检测到ＭＭＰ－９的活性（Ｆｉｇ．１）。ＭＭＰ－２的活性在动情前期最高,动情期和动情后期次之,间情期最低（Ｆｉｇ．２）。原位杂交结果显示：ＭＭＰ－２、－９、ＴＩＭＰ－１、－２、－３ｍＲＮＡ主要在子宫内膜基底部的基质细胞中表达。ＭＭＰ－２和－９ｍＲＮＡ在动情前期、动情期和动     

Synthesis, characterization, and antifungal activity of novel quaternary chitosan derivatives

Three novel quaternary chitosan derivatives were successfully synthesized by reaction of chloracetyl chitosan (CACS) with pyridine (PACS), 4-(5-chloro-2-hydroxybenzylideneamino)-pyridine (CHPACS), and 4-(5-bromo-2-hydroxybenzylideneamino)-pyridine (BHPACS). The chemical structure of the prepared chitosan derivatives was confirmed by Fourier transform infrared (FT-IR) and ¹³C nuclear magnetic resonance (¹³C NMR) and their antifungal activity against Cladosporium cucumerinum, Monilinia fructicola, Colletotrichum lagenarium, and Fusarium oxysporum was assessed. Comparing with the antifungal activity of chitosan, CACS, and PACS, CHPACS and BHPACS exhibited obviously better inhibitory effects, which should be related to the synergistic reaction of chitosan itself with the grafted 2-[4-(5-chloro-2-hydroxybenzylideneamino)-pyridyl]acetyl and 2-[4-(5-bromo-2-hydroxybenzylideneamino)-pyridyl]acetyl.     

Photochemical synthesis and anticancer activity of barbituric acid,thiobarbituric acid,thiosemicarbazide, and isoniazid linked to 2-phenyl indole derivatives

2-Phenyl-1H-indole-3-carbaldehyde-based barbituric acid, thiobarbituric acid, thiosemicarbazide, isoniazid, and malononitrile derivatives were synthesized under photochemical conditions. The antitumor activities of the synthesized compounds were evaluated on three different human cancer cell lines representing prostate cancer cell line DU145, Dwivedi (DWD) cancer cell lines, and breast cancer cell line MCF7. All the screened compounds possessed moderate anticancer activity, and out of all the screened compounds, 5-{1[2-(4-chloro-phenyl)2-oxo-ethyl]-2-phenyl-1H-indole-3-ylmethylene}-2-thioxo-dihydro-pyrimidine-4,6-dione (2b) and 5-{1[2-(4-methoxy-phenyl)2-oxo-ethyl]-2-phenyl-1H-indole-3-ylmethylene}-2-thioxo-dihydro-pyrimidine-4,6-dione (2d) exhibited marked antitumor activity against used cell lines. Additionally, barbituric acid derivatives were selective to inhibit cell line DWD and breast cancer cell lines.     

SEASONAL VARIATIONS OF PHOTOSYNTHETIC PIGMENTS, TOTAL C, N, AND P CONTENT, AND PHOTOSYNTHESIS IN PHYLLARIOPSIS PURPURASCENS: (PHAEOPHYTA) FROM THE STRAIT OF GIBRALTAR

Photosynthetic pigments, C, N, and P tissue composition, and photosynthetic rate were measured from April to October in the brown alga Phyllariopsis purpurascens (C. Agardh) Henry et South (Laminariales, Phaeophyta) growing at a 30-m depth in the Strait of Gibraltar. Ir-radiance reaching the population ranged from 13.5 to 27.5 mol.m^-2.mo^-1. The available light for this species, expressed as a percentage of the irradiance above the water, was 1.8%. Dissolved inorganic nitrogen forms, NO3-and NH₄+, were constant from April to October, whereas phosphate was depleted in August. Chlorophyll a decreased from 520.0 ± 165.0 to 199.6 ± 159.9 μg.g^-1 dry weight; in contrast, chlorophyll c and carotenoids did not change until September but increased threefold in October. C:N and N:P ratios changed in the same way and in the same range. They were constant until July but increased from 15–17 up to 42 (C:N) and from 14 to 40 (N:P) in October, suggesting a severe P limitation of growth of this species. The dark respiration rate and the light compensation point were constant from April to October (0.5 ± 0.1 μmol O₂. m^-2.s^-1 and 6.5 ± 0.2 μmol.m^-2. s^-1, respectively), whereas the maximum rate of apparent photosynthesis, light onset saturation parameter, and half saturation constant for light were maximum in April to May (3.7 μmol O₂. m^-2.s^-1and 40 and 41.5 μmol.m^-2. s^-1, respectively) and October (3.6 μmol O₂. m^-2.s^-1 and 50 and 53.7 μmol.m^-2. s^-1, respectively). They were minimum in August (1.2 μmol O₂.m^-2.s^-1 and 11.3 and 12 μmol.m^-2.s^-1, respectively). These minimum figures yielded a negative carbon budget in August and 0 in September, whereas it was positive the rest of the year. Photosynthetic efficiency, estimated by the ratio between maximum apparent photosynthesis and light half saturation constant, showed a strong agreement with productivity measured by means of an independent method. These results indicate that lamina expansion in this species is controlled by photosynthetic efficiency.     

Spirostanol saponins from Paris polyphylla,structures of polyphyllin C,D, E and F

The structures of four new saponins, polyphyllin C, D, E and F, isolated from the tubers of Paris polyphylla have been elucidated as diosgenin-3-O-α-l-rhamnopyranosyl(1→3)-β-d-glucopyranoside, diosgenin-3-O-α-l-rhamnopyranosyl(1→3)- [α-l-arabinofuranosyl(1→4)]-β-d-glucopyranoside, diosgenin-3-O-α-l-rhamnopyranosyl(1→2)-α-l-rhamnopyranosyl (1→4)[α-l-rhamnopyranosyl(1→3)]-β-d-glucopyranoside and diosgenin-3-O-α-l-rhamnopyranosyl(1→4)[α-l- rhamnopyranosyl(1→3)][β-d-glucopyranosyl(1→2)]-α-l-rhamnopyranoside, respectively, on the basis of chemical and spectral data.     

Cloning,expression, isolation,and properties of thymidine kinase from herpes simplex virus type 1, strain L2

Thymidine kinase UL23 gene (EC 2.7.1.145) from the L2 acyclovir-sensitive strain of herpes simplex virus type 1 was cloned and expressed in E. coli. The enzyme was purified by chromatography to the purity of 90% according to PAG electrophoresis data. The Michaelis constants for the reactions with thymidine and acyclovir were determined. The enzyme was found to phosphorylate modified nucleosides, particularly 3′-deoxythymidine, 3′-deoxy-2′,3′-didehydrothymidine, 2′,3′-dideoxycytidine, 9-[(hydroxyethyl)methyl]guanine, E-5-(2-bromovinyl-2′-deoxyuridine, 9-(1,3-dihydroxy-2-propoxymethyl)guanine, 2′,3′-dideoxydehydrothymidine, β-L-2′,3′-dideoxy-3′-thiacytidine, and 3′-fluoro-3′-deoxythymidine. Some properties of the purified enzyme were compared with those of thymidine kinases of other herpes simplex virus strains. It was shown that acyclovir H-phosphonate inhibited the enzyme.     

Mono- and bis-cobalt complexes with carbonyl, nitrosyl, and monocarbollide ligands

Reaction of [Co(CO)₃(NO)] with [2-NMe₃-closo-2-CB₁₀H₁₀] in refluxing CH₂Cl₂ affords the mono- and di-cobalt complexes [1-NMe₃-2-CO-2-NO-closo-2,1-CoCB₁₀H₁₀] (3) and [2,7-{Co(CO)(NO)}-7-(μ-H)-1-NMe₃-2-CO-2-NO-closo-2,1-CoCB₁₀H₉] (4), respectively, of which 4 contains formally both Co(I) and Co(-I) centers. Compound 4 reacts with CO to give 3, or with donor ligands L in the presence of Me₃NO to afford simple substituted species, [1-NMe₃-2-L-2-NO-closo-2,1-CoCB₁₀H₁₀] (compounds 5; L = PEt₃, PPh₃, CNBu^t).