Bone marrow genotoxicity of N-methyl, N-nitrosourea (NMU): n-alkanols as sister chromatid exchange (SCE) anti-inducers

The in vivo SCE test was used to demonstrate significant inhibition of NMU bone marrow genotoxicity by pretreatment of Chinese hamsters with n-alkanols. Our findings exclude a loss of intracellular DNA alkylation potential through a competitive direct reaction of NMU with the weakly nucleophilic polar end of the n-alkanols, but not through methylations of nucleophilic membrane sites possibly liberated by structural modifications which the membrane-active amphiphilics induce.     

Steady-state kinetic studies with the polysulfonate U-9843, an HIV reverse transcriptase inhibitor

The tetramer of ethylenesulfonic acid (U-9843) is a potent inhibitor of HIV-1 RT^* and possesses excellent antiviral activity at nontoxic doses in HIV-1 infected lymphocytes grown in tissue culture. Kinetic studies of the HIV-1 RT-catalyzed RNA-directed DNA polymerase activity were carried out in order to determine if the inhibitor interacts with the template: primer or the deoxyribonucleotide triphosphate (dNTP) binding sites of the polymerase. Michaelis-Menten kinetics, which are based on the establishment of a rapid equilibrium between the enzyme and its substrates, proved inadequate for the analysis of the experimental data. The data were thus analyzed using steady-state Briggs-Haldane kinetics assuming that the template:primer binds to the enzyme first, followed by the binding of the dNTP and that the polymerase is a processive enzyme. Based on these assumptions, a velocity equation was derived which allows the calculation of all the specific forward and backward rate constants for the reactions occurring between the enzyme, its substrates and the inhibitor. The calculated rate constants are in agreement with this model and the results indicated that U-9843 acts as a noncompetitive inhibitor with respect to both the template:primer and dNTP binding sites. Hence, U-9843 exhibits the same binding affinity for the free enzyme as for the enzyme-substrate complexes and must inhibit the RT polymerase by interacting with a site distinct from the substrate binding sites. Thus, U-9843 appears to impair an event occurring after the formation of the enzyme-substrate complexes, which involves either an event leading up to the formation of the phosphoester bond, the formation of the ester bond itself or translocation of the enzyme relative to its template:primer following the formation of the ester bond.     

古典几何的正弦定理和余弦定理

本主旨在以新的观点讨论非欧几何、球面几何和欧氏几何等三种古典几何体系的正弦定理和余弦定理的统一形式,并阐明它们的相互关系.     

On the pathway of the rectosphincteric reflex

In several rat models, including those with circular and semicircular rectal aganglionosis, the rectosphincteric reflex was examined. The reflex was confirmed to be essentially an intramural one and its route is considered to run mainly in the longitudinal and partly in the oblique directions.     

Antiviral activity of coralloid root ofCycas revoluta extract against some viruses of tomato plant

Summary Crude coralloid root extract ofCycas revoluta showed significant antiviral activity against viruses of the tomato plant (PVX, PVY, TMV, TAV and TRSV) when applied 24 h before virus inoculation, or when mixed with different virus inocula before virus inocultion, in hypersensitive and systemic hosts. No such inhibition was observed when extract was applied 24 h after virus inoculation. TAV did not show any inhibitory response in a systemic host.Authors are thankful to Dr S. N. Gupta and Dr (Smt.) K. Shukla for their valuable guidance and providing laboratory facilities and U.G.C. for financial assistance.     

Antibacterial activity in the egg mass of a sea hare

Summary The eggs of a sea hare,Aplysia kurodai, contained antibacterial factors which probably play a role in the defense of eggs against bacterial infection. The active factors were composed of several heat-labile proteins, unrelated to lysozyme, and were produced in the albumen gland.     

Accumulation of3H-dopamine by synaptic vesicles from rat striatum in an impermeant medium

Summary The accumulation of³H-dopamine by synaptic vesicles from rat striatum was significantly stabilized in a membrane impermeant medium. The characteristics of dopamine accumulation by striatal vesicles were quite similar to those reported for dopamine accumulation by a whole brain vesicle preparation in the same medium, and were siginificantly different from the characteristics previously reported for vesicular accumulation of norepinephrine.Acknowledgments. This work was supported by grant NS 18752 (NIH) of the United States Public Health Service. Reprint requests to J. A. R.     

Immunoactive TSH in the amniotic fluid of the rat

Summary Amniotic fluid was obtained from 19-day-old rat fetuses by aspiration. Pooled samples measured at 4 different dilutions demonstrated parallelism with standard rat TSH. It is concluded that rat amniotic fluid has TSH immunoactivity.This work was supported by Hong Kong University Research Grant No. 335/034/5727.The authors wish to acknowledge with thanks the gift of rat TSH RIA kit from Dr A. F. Parlow and the Rat Pituitary Programme of NIAMDD.     

Optically active benzo[c]phenanthrene diol epoxides bind extensively to adenine in DNA

Reactions of diol epoxide metabolites of carcinogenic polycyclic aromatic hydrocarbons with DNA are thought to initiate the carcinogenic process. Although formation of a benzo[a]pyrene (BaP) diol epoxide-deoxyguanosine adduct has been held responsible for biological activity, the more potent carcinogen, 7,12-dimethylbenz[a]anthracene (DMBA) binds extensively to deoxyadenosine residues in DNA, suggesting that hydrocarbon carcinogen-deoxyadenosine adducts may be instrumental in tumour initiation. Because the bay region diol epoxides of benzo[c]phenanthrene (BcPh) are very active tumour initiators, and the relative activities of the four configurationally isomeric 3,4-diol 1,2-epoxides (Fig. 1) are known, we examined their reactions with DNA. Each BcPh diol epoxide isomer exhibits a remarkable preference for covalent binding to DNA over hydrolysis, each yields a unique distribution of products with the nucleosides of DNA and each reacts extensively with deoxyadenosine residues in DNA. The relative tumour initiating activities of these stereoisomers is best reflected by the relative yields of one of the deoxyadenosine adducts formed.