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PubMed1995

Efficacy of peripheral kappa agonist fedotozine versus placebo in treatment of irritable bowel syndrome. A multicenter dose-response study.

The efficacy and safety of the peripheral kappa agonist fedotozine was evaluated in a double-blind, multicenter study involving 238 patients with the irritable bowel syndrome. After a two-week washout, patients were assigned to one of four groups to receive either placebo or fedotozine three times a day at doses of 3.5, 15, or 30 mg for six weeks. Patient assessment of mean symptom intensity indicated that the 30-mg dose of fedotozine was superior to placebo in relieving maximal daily abdominal pain (P = 0.01), mean daily pain (P = 0.007), and abdominal bloating (P = 0.02). Changes in bowel function and defecation disorders could not be evaluated reliably. According to the investigators, the highest dose of fedotozine markedly reduced overall disease severity (P = 0.003) and the pain component of the symptomatic profile (P = 0.009). Clinical and laboratory safety was very good. Fedotozine 30 mg three times a day therefore appears to be effective and safe in the treatment of the abdominal pain and bloating associated with IBS.

Adult↗
PubMed1990

Biophysical basis of growth promotion in primary leaves of Phaseolus vulgaris L. by hormones versus light: solute accumulation and the growth potential.

Rapid cell enlargement in primary leaves of bean is induced by bright white light (WL), gibberellic acid (GA3) or the cytokinin N6-benzyladenine (BA). In previous studies it has been show that all three agents cause an increase in wall extensibility, although by different mechanisms. Here we examine the effects of the three growth promoters on the osmotic potential difference (delta Psi), the accumulation of solutes (delta TSC), the wall yield threshold (Y) and the growth potential (delta Psi -Y). With GA3 and BA, but not WL, there was a rapid decline in delta Psi as measured by the osmotic concentration of expressed sap. Unlike WL, neither GA3 nor BA promoted the accumulation of osmotic solutes. The decline in delta Psi, however, was apparently counteracted by a decline in Y since the growth potential, as measured by the external-osmoticum method, remained unchanged. It is concluded that WL, GA3 and BA all promote cell enlargement of bean leaves by increasing one cellular growth parameter, wall extensibility. Only WL, however, promotes osmotic adjustment during growth.

Adenine↗
PubMed1994

Isolation of a cDNA clone for a cytokinin-repressed gene in excised cucumber cotyledons.

Rapid changes in gene expression were studied during incubation of cucumber (Cucumis sativus L.) cotyledons with cytokinins in darkness. Complementary-DNA clones for mRNAs whose levels decreased within 4 h of treatment with N6-benzyladenine (BA) were isolated by differential hybridization. One of them (CR9) was sequenced. It is 588 bp long, and would encode a protein consisting of 137 amino-acid residues and having a molecular mass of 15 kDa. The sequence shows a high homology with a light-induced gene from rice. Northern blot analysis of the CR9 transcript showed the level of the mRNA (0.7 kb) to decrease tenfold within 4 h of BA treatment, i.e. well before BA-induced cotyledon expansion was observed. The repression became greater with increasing concentration of BA (10(-8)-10(-5) M). The expression of the CR9 gene was repressed specifically by cytokinins (BA, isopentenyladenine and t-zeatin), but not by adenine or 2,4-dichlorophenoxyacetic acid (auxin). The results are discussed in relation to the primary action of cytokinin.

Adenine↗
PubMed1977

[Correlation of cyanogenic glycosides with content of benzyl alcohol in cherry brandies (author's transl)].

A clear correlation between cyanogenic glycosides and the content of benzyl alcohol in fermented mash of cherries was indicated by model experiments with amygdalin and fermenting yeast, cherry-stones with and without fermenting yeasts as well as bitter and sweet almonds. These correlations proofed that benzyl alcohol has to be regarded as a metabolic product of mandelonitrileglycosides.

Alcoholic Beverages↗
PubMed1975

Inhibition of enzymatic reduction of delta 14-double bond of 5 alpha-cholesta-8,14-dien-3 beta-ol and 5 alpha-cholesta-7,14-dien-3 beta-ol by AY-9944.

AY-994 (trans-1,4-bis-(2-chlorobenzyl-aminomethyl) cyclohexane dihydrochloride), a potent inhibitor of the enzymatic reduction of the delta 7-double bond of delta 5,7-sterols, has been shown to inhibit, at higher concentrations (10-4 M), the enzymatic reduction of the delta 14-double bond of cholesta-8,14-dien-3 beta-ol and cholesta-7,14-dien-3 beta-ol.

Animals↗
PubMed2000

Synthesis and characterization of oligonucleotides containing site-specific bulky N2-aralkylated guanines and N6-aralkylated adenines.

7-Bromomethylbenz[a]anthracene is a known mutagen and carcinogen. The two major DNA adducts produced by this carcinogen, i.e., N2-(benz[a]anthracen-7-ylmethyl)-2'-deoxyguanosine (2, b[a]a2G) and N6-(benz[a]anthracen-7-ylmethyl)-2'-deoxyadenosine (4, b[a]a6A), as well as the simpler benzylated analogs, N2-benzyl-2'-deoxyguanosine (1, bn2G) and N6-benzyl-2'-deoxyadenosine (3, bn6A), were prepared by direct aralkylation of 2'-deoxyguanosine and 2'-deoxyadenosine. To determine the site-specific mutagenicity of these bulky exocyclic amino-substituted adducts, the suitably protected nucleosides were incorporated into 16-base oligodeoxyribonucleotides in place of a normal guanine or adenine residues which respectively are part of the ATG initiation codon for the lac Z' alpha-complementation gene by using an in situ activation approach and automated phosphite triester synthetic methods. The base composition and the incorporation of the bulky adducts into synthetic oligonucleotides were characterized after purification of the modified oligonucleotides by enzymatic digestion and HPLC analysis.

Adenine↗
PubMed2005

Synthesis of decapeptide of L-aspartic acid and benzyl-L-aspartic acid by solid phase peptide synthesis.

Polyene macrolide amphotericin B (AmB) is the drug of choice for the treatment of disseminated fungal infections. However, because of its pronounced side effects, the drug has limited applicability. There are few interesting reports, which state that co-administration of the drug with homo-peptide of polyaspartic acid reduces the side effects of the drug. In our present study, an approach has been made to systematically synthesize low molecular weight heteropeptides consisting of L-aspartic acid and its derivative. It was hypothesized that such heteropeptides will reduce the toxic side effects of the drug by facile hydrophobic binding between the polymer and the drug. We have employed the strategy of solid phase peptide synthesis (SPPS) to synthesize low molecular weight hetero-peptides by using L-aspartic acid and benzyl-L-aspartic acid to induce the hydrophobic binding between the peptide and the drug. In future, the proposed methodology can be employed to tailor other polypeptides substituted with benzyl groups to reduce the nephrotoxicity of AmB.

Aspartic Acid↗
PubMed1994

Computer assisted recognition and quantitation of the effects of airborne chemicals acting at different areas of the respiratory tract in mice.

The pattern and timing of a normal breath in unanesthetized mice was analyzed from measurement of inspiratory and expiratory airflows (VI and VE). Airflow was measured via a differential pressure transducer, attached to a pneumotachograph, which itself was attached to a body plethysmograph into which a mouse was placed. The analog voltage from the differential pressure transducer was digitized and stored for analysis on a microcomputer. Criteria were developed to classify each breath as normal (N) or belonging into one of seven abnormal categories. The abnormal categories were arrived at by computer analysis, recognizing specific modifications of the normal pattern into patterns of: sensory irritation of the upper respiratory tract (S), airflow limitation within the conducting airways of the lungs (A) or pulmonary irritation at the alveolar level (P). Combinations of these effects, i.e., S+A, P+A, P+S and P+S+A were also recognized. Computer analysis of each breath also permitted quantitative evaluation of the degree of S, A or P abnormalities. To induce each type of effect we used inhalation exposures to 2-chlorobenzylchloride, carbamylcholine or propranolol. We propose that this approach will permit rapid evaluation of the possible effects of airborne chemicals at three levels of the respiratory tract, with the classification of the type of effect easily obtained in an objective way using well defined criteria, followed by quantitation of the degree of each effect.

Administration, Inhalation↗
PubMed1998

Computer-based bioassay for evaluation of sensory irritation of airborne chemicals and its limit of detection.

We expanded a previously described rule-based computerized method to recognize the sensory irritating effect of airborne chemicals. Using 2-chlorobenzylchloride (CBC) as a sensory irritant, characteristic modifications of the normal breathing pattern of exposed mice were evaluated by measuring the duration of braking (TB) after inspiration and the resulting decrease in breathing frequency. From the measurement of TB, each breath was then classified as normal (N) or sensory irritation (S). Using increasing exposure concentrations, the classification S increased from < or = 2% (equivalent to sham-exposure) to 100% within a narrow exposure concentration range. The potency of CBC was then evaluated by calculating the concentration necessary to produce 50% of the breaths classified as S, i.e., S50. This approach is easier to use than obtaining RD50 (decrease in respiratory frequency by 50%) when high exposure concentrations are difficult to achieve. Detection limits were also established for this bioassay and experiments were conducted to obtain a level of response just around these limits, in order to delineate the practicality of using this bioassay at low exposure concentrations. Using this approach, sensory irritation was the only effect induced by CBC at low exposure concentrations. However, bronchoconstriction and pulmonary irritation were superimposed on this effect at higher exposure concentrations.

Air Pollutants↗
PubMed2002

Regeneration of the Egyptian medicinal plant Artemisia judaica L.

An in vitro propagation system for Artemisia judaica L., a traditional Egyptian medicinal plant, has been developed. De novo shoot organogenesis was induced by culturing etiolated hypocotyls and intact seedlings on medium supplemented with thidiazuron [N-phenyl-N'-(1,2,3-thidiazol-yl) urea] via callusing at the cotyledonary notch region. Up to 16 shoots formed per seedling cultured on a medium containing 1 micro mol l(-1) thidiazuron for an optimal duration of exposure of 20 days. Regenerated shoots formed roots when subcultured onto a medium containing 1 micromol l(-1) indole-3-butyric acid. The regeneration protocol developed in this study provides a basis for germplasm conservation and for further investigation of medicinally active constituents of A. judaica.

Adenine↗
PubMed2002

Production of haploids of neem (Azadirachta indica A. Juss.) by anther culture.

Androgenic haploids of the neem tree (Azadirachta indica A. Juss.) were produced by anther culture at the early- to late-uninucleate stage of pollen. Haploid formation occurred via callusing. The best medium for inducing callusing in the anther cultures was Murashige and Skoog's basal medium (MS) (9% sucrose) supplemented with 1 microM 2,4-D, 1 microM NAA and 5 microM BAP, while anther callus multiplied best on MS medium supplemented with 1 microM 2,4-D and 10 microM Kn. These calli differentiated shoots when transferred to a medium containing BAP; 5 microM BAP was optimum for young calli (75% cultures differentiated shoots), but older calli showed the best regeneration with 7.5 microM BAP. Shoots elongated at a lower concentration of BAP-0.5 microM. These shoots were multiplied by forced axillary branching and rooted in vitro. The plants were subsequently established in soil. Of the plants that regenerated from anther callus 60% were haploid, 20% were diploid and 20% were aneuploid.

2,4-Dichlorophenoxyacetic Acid↗
PubMed2003

Adventitious shoot regeneration from in vitro cultured leaves of London plane tree (Platanus acerifolia Willd.).

Adventitious shoots were successfully regenerated from leaf explants of in vitro cultures of Platanus acerifolia Willd. The leaves of three clones (genotypes), designated as PH1, PH2 and PC, respectively, were wounded by three to four transverse cuts through the midvein and cultured on 26 media based on Murashige and Skoog (MS) basal medium, containing different concentrations of 6-benzylaminopurine (BAP) in combination with different concentrations of indole-3-butyric acid (IBA). The highest regeneration rate (>90%) and the largest number of shoot clumps per regenerating leaf (>4 shoot clumps/explant) were obtained with leaves of genotype PH2 cultured on MS basal medium supplemented with 17.76 microM BAP and 4.92 microM IBA. The other two genotypes, PH1 and PC, showed very low capability of shoot regeneration (<10%) on all the media tested. Shoots on leaf explants originated mainly from callus that developed around the cut end of petioles and along the cuts across the midvein. The regenerated shoots were micropropagated, rooted and transplanted to the soil successfully.

Adenine↗
PubMed2003

Enhanced bud and bulblet regeneration from bulbs of Nerine sarniensis cultured in vitro.

Nerine (Nerine sarniensis) cv. Salmon Supreme in vitro-grown bulblets, 7-9 mm in diameter, were cut in half longitudinally and used for adventitious bud initiation following dissection of the roots and two-thirds of the upper part of the bulblets. The terminal apex was injured with a hot, sterile microscope dissecting needle. The highest number of buds formed (seven to nine buds per halved bulblet) on a semi-solid Murashige and Skoog (MS) basal salts medium supplemented with 3% sucrose and either 1 microM 6-benzylaminopurine (BA) and 1 microM alpha-naphthaleneacetic acid (NAA) or 0.5 microM BA and 0.1 microM NAA. Bulblet halves were cultured in the dark for 11-13 weeks with one subculture after 6 weeks. Anatomical studies indicated that the initiation of adventitious buds on the abaxial side of the inner scales of the halved bulblet was adjacent to the basal plate and started from the leaf primordium and a meristematic bulge. Buds developed directly into small bulblets after they were transferred to semi-solid MS basal salts medium supplemented with 6% sucrose, 10 microM indole-3-butyric acid (IBA) and 0.25% activated charcoal. Small bulblets cultured in liquid MS medium supplemented with additional KH(2)PO(4 )(170 mg l(-1)), 6% sucrose and 0.1 microM NAA under a 16/8-h (light/dark) photoperiod for 8 weeks grew into larger bulbs faster than those cultured on semi-solid medium. The bulbs were rooted on a semi-solid medium after 4 weeks and then transferred to the soil. As many as 18 bulblets developed and rooted from one in vitro-grown bulb after 25-27 weeks.

Adenine↗