Polarographic activity of the antitumor drug cis-dichlorodiammineplatinum (II). The effect of hydrolysis and trans-isomerization of the drug

Summary Electrochemical activities of cis-dichlorodiammineplatinum(II) (cis-DDP) and its trans isomer were studied by classical and differential pulse polarography (d.p.p.). It was shown that both isomers yielded a polarographic step or peak at about –1.6V (vs. Ag/AgCl), which corresponded to electroreduction of the complex and to catalytic hydrogen evolution. This signal was easily measurable with the aid of d.p.p. and was suitable for investigation of the extent of hydrolysis and trans-isomerization of cis-DDP leading to the formation of toxic products. The detection limit for determination of cis-DDP and its trans isomer by d.p.p. was 1×10^–6 mol/l.Acknowledgment. This work was supported in part by Lachema n.e., Brno (Czechoslovakia).     

The specificity of reactions of polycyclic aromatics II. Polarographic reductions

Zusammenfassung Die polarographische Reduktion polyzyklischer are matischer Verbindungen kann als 1,2-, 1,4- oder 1,6 Addition erfolgen. Der Verlauf der Reaktionen lässt sic aus der Abnahme der Resonanzenergie ableiten.

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F. T. Wallenberger, Tetrahedron Letters9, 5–9 (1959).     

The cytogenetic efficiency of the antitumor agents bleomycin and peplomycin is enhanced by the heart drug verapamil (isoptin)

Summary The induction of 2-break chromosome aberrations (dicentrics and ring chromosomes) in human lymphocytes by the antitumor agents bleomycin and peplomycin is strongly enhanced when those agents are applied together with the heart drug verapamil (isoptin).We thank Heinrich Mack Nachf./Illertissen (Germany) for generously supplying both the bleomycin and the peplomycin and Dr P. Engel, Illertissen, for valuable informations.     

The cytogenetic efficiency of the antitumor agents bleomycin and peplomycin is enhanced by the heart drug verapamil (isoptin)

The induction of 2-break chromosome aberrations (dicentrics and ring chromosomes) in human lymphocytes by the antitumor agents bleomycin and peplomycin is strongly enhanced when those agents are applied together with the heart drug verapamil (isoptin).     

Studies on the hydrolysis of bradykinin by angiotensin-converting enzyme (kininase II)

Summary Arg-Pro-Pro-Gly-Phe, the N-terminal pentapeptide of bradykinin, is not an inhibitor of angiotensin-converting enzyme and is not hydrolyzed by the enzyme. Arg-Pro-Pro, the N-terminal tripeptide is a relatively potent (IC₅₀=2.3×10⁶ M) inhibitor but its higher homolog, Gly-Arg-Met-Lys-Arg-Pro-Pro is not an inhibitor of angiotensin-converting enzyme.This work was supported in part by grants from the US Public Health Service (HL 18415, HL 15691, HL 19764) and the John A. Hartford Foundation, Inc., and by the Medical Research Service of the Veterans Administration.     

A histochemical demonstration of the Na+ + K+-ATPase activity in the thyroid and the effect of cyclic adenosine monophosphate (c-AMP).

With a suitable modification of the Farquhar and Palade technique the Na+ + K+-ATPase activity in guinea-pig thyroid is demonstrated. The addition of c-AMP (5 X 10(-6) M or 1.5 X 10(-5) M) to the incubation media produced an apparent intensification of the Na+ + K+ -ATPase activity in the thyroid.     

Administration of the antitumor drug mitoguazone protects normal thymocytes against spontaneous and etoposide-induced apoptosis

The suggestion has been made that polyamines may be involved in the control of cell death, since exceedingly high or low levels induce apoptosis in different cell systems. For a deeper insight into the relationship between apoptosis and polyamine metabolism, we investigated in vitro the effect on rat thymocytes of mitoguazone (MGBG, which inhibits S-adenosylmethionine decarboxylase, i.e. a key enzyme in the polyamine biosynthetic pathway). Thymocytes were selected as an especially suitable model system, since they undergo spontaneous apoptosis in vivo and can be easily induced to apoptose in vitro by etoposide, used here as an apoptogenic agent. MGBG protected thymocytes from both spontaneous and drug-induced apoptosis, and this protective effect was associated with a decrease in polyamine oxidase activity and total polyamine levels.Received 7 July 2004; received after revision 2 September 2004; accepted 9 September 2004     

The effect ofp-benzoquinone and quinol on the IAA-oxidase activity

Zusammenfassung Bei Prüfung des Einflusses vonp-Benzochinon auf die Aktivität der partiell gereinigten IES-Oxidase aus Wurzeln von Maiskeimlingen wurde bei Konzentrationen von 5×10^–6 bis 5×10^–4 M eine 50-bzw. 100%ige Hemmung beobachtet.     

Studies by the newt test on the possible importance of conjugated double-bonds and trans-isomerization for carcinogenic properties of lipids

Zusammenfassung Mittels der Salamander-Schnell-methode für Karzinogen-Prüfung wurde eine Reihe von Fettprodukten und verwandten Verbindungen untersucht. Äthylelaidat erwies sich als unwirksam, während Vitamin A, Ergosterol, Holzöl und konjugiertes Äthyllinoleat wirksam waren. Die Ergebnisse weisen auf eine grössere Bedeutung der konjugierten Doppelbindungen hin, während der quantitative Vergleich zeigt, dass auch andere Aspekte der chemischen Struktur von Bedeutung sein können.

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This work was supported by a grant from the Danish Anti-Cancer League.     

Zeitgeber induced modulation of activity patterns in nocturnal mammals (Chiroptera).

Changing the L:D intensity ratio of a synchronizing dark regime leads to characteristic modulations of the activity pattern of Chiroptera species. These modulations fit the predictions of WEVER'S oscillator model.     

Class I and class II ribonuclease H activities in Crithidia fasciculata (Protozoa).

The protozoan Crithidia fasciculata contains two different ribonuclease H activities. These enzymes display similar physical and biochemical characteristics to their homologues in higher eukaryotes, for instance calf thymus class I and class II ribonuclease H. Class I ribonuclease H of lower and higher eukaryotes can be activated by Mg2(+)- and Mn2(+)-ions. However, the presence of Mn2(+)-ions is inhibitory for the Mg2(+)-dependent class II ribonuclease H activity of Crithidia fasciculata and calf thymus. The protozoan class I-homologue enzyme appears to be serologically related to the class I ribonuclease H of calf thymus.     

Complexes of enkephalins with zinc (II). Study by nuclear magnetic resonance

Structural modifications of enkephalins obtained by complexation of Zn++ are brought out by high resolution 1 H N M R spectroscopy. For one of the two enkephalins studied, the conformational equilibrium is greatly shifted by the introduction of the metal ion.     

The effect of levamisole on phosphodiesterase activity

Summary Phosphodiesterase activity of mouse liver homogenates was estimated in presence and absence of levamisole. The enzyme activity was 1394 and 1399 nmoles/mg protein/30 min respectively. Our data show that levamisole does not affect the phosphodiesterase activity.     

Continued in vitro and in vivo release of an antitumor drug from albumin microspheres

Heated albumin microspheres with an average diameter of 45 +/- 8 microns and containing mitomycin C, released, in vitro, about 20% of this antibiotic over a 3-day period. VX-2 tumors were implanted into the hind leg of rabbits and the drug-containing microspheres were injected into the femoral artery of these animals. High levels of the drug were maintained for several hours in the tumor and growth of the tumor was inhibited considerably, compared to findings in control rabbits given the conventional mitomycin C. Half the number of the rabbits treated with our new method are alive with no evidence of tumor.     

The effect of head heating on the flight activity of the cockroach

Summary Internal head heating restricted the flight activity in the cockroachPeriplaneta americana. Heating the metathoracic ganglion did not have any pronounced effect on the flight. It is concluded that in the cockroach the head nervous centers are very heat-susceptible and might be the coordinating center for temperature responses.     

The effect of bradykinin on the electrical activity of rat jejunum

Summary Bradykinin increased the potential difference across both the jejunum and colon of the rat. This effect was significantly reduced by indomethacin, suggesting that it was mediated by prostaglandins. The possibility that bradykinin may contribute to the diarrhoea of the carcinoid syndrome by inducing a net secretory state in the intestine is discussed.