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Synthesis and anti-HIV properties of novel 6-phenylselenenyl-5-propyluracils

100%

Miazga A. , Felczak K. , Siwecka M. A. , Lipniacki A. , Piasek A. , Kulikowski T.

tom 54

nr 4

863-868

Novel 6-phenylselenenyl-5-propyluracils were synthesized from 5-propyluracil with the use of regioselective synthesis to give 1-[(2-hydroxyethoxy)-methyl]-6-phenylselenenyl-5-propyluracil (6), 1-ethoxymethyl-6-phenylselenenyl-5-propyluracil (9) and 1-benzyloxymethyl-6-phenylselenenyl-5-propyluracil (10). Interaction of these compounds with recombinant HIV-1 reverse transcriptase (RT) was evaluated using a non-isotopic colorimetric method. Compounds 9 and 10 exerted potent HIV RT inhibition (IC500.06 and 0.05 μM respectively) while compound 6 showed moderate inhibition (IC50=3.5 μM). Potent anti-HIV-1 activity in MT-2 cells inoculated by a syncythia-in-ducing HIV-1 (cat #3 strain) laboratory isolate was exerted by compounds 9 and 10 (EC500.62 μM and 0.025 μM, respectively), while compound 6 showed only moderate activity (IC50=4.1 μM). In addition, compound 10 showed very good in vitro therapeutic index (TI > 2046), indicating that it is a potential anti-HIV/AIDS drug.

The effect of volatile oil from Chinese mugwort leaf on human demodecid mites in vitro

100%

Du J. , Gao R. , Zhao J.

Acta Parasitologica

2021

tom 66

nr 2

Assessment of the efficiency of applying methisoprinol and vaccination of turkeys against the haemorrhagic enteritis virus using in ovo methods

100%

Koncicki A. , Tykalowski B. , Stenzel T. , Andrzejewski M.

nr 1

13-15

The aim of the research was to determine the efficiency of in ovo immunisation of turkeys against the haemorrhagic enteritis virus, while simultaneously applying a synthetic immunomodulator - methisoprinol - by the same route of administration. Dindoral SPF vaccine, in a dose of 0.1 ml of the solution prepared ex tempore after dissolving the vaccine in 100 ml of water for injection, and methisoprinol in a dose of 5 mg per egg, were administered in ovo on the 26th d of incubation. The control groups consisted of turkeys hatched from eggs into which only the methisoprinol or the vaccine was administered, as well as birds hatched from eggs that were not interfered with. The susceptibility of turkeys to HE virus infection was determined on the basis of the presence of HE antibodies in serum, the evaluation of a splenic index, and attempts to register the virus presence in the spleen 120 h after the control infections. The research proved the effectiveness of immunising turkeys against the haemorrhagic enteritis virus by administering Dindoral SPF vaccine in ovo. It was also demonstrated that the simultaneous application of methisoprinol, showing an antiviral effect, and the vaccine inhibited the development of post vaccinal immunity against this virus.

Antiviral activity of 2-chloro-2'-deoxyadenosine [2-CdA]

100%

Zahorska R. , Mazur N. , Skierski J. S. , Grieb P.

Archivum Immunologiae et Therapiae Experimentalis

1996

tom 44

nr 2-3

The influence of precursors and elicitor feeding on lignans accumulation in cultures of Taxus × media roots carrying a taxadiene synthase transgene

80%

Wencel A. , Syklowska-Baranek K. , Lysik K. , Pietrosiuk A.

2015

tom 96

nr 1

Morphological and chemical evaluation of St.John's wort [Hypericum perforatum L.] populations from Lithuania

80%

Bagdonaite E. , Zygmunt B. , Radusiene J.

2001

tom 47

nr 4

Przedstawiono wyniki testowania zmienności 27 populacji Hypericum perforatum występujących na terenie Litwy. Dotyczyły one 15 parametrów morfologicznych i wartości gospodarczej. Wyniki zostały poddane wielokierunkowej analizie statystycznej w celu oznaczenia ich zmienności między populacjami. Wyniki testu Scheffe pozwoliły wybrać spośród analizowanych populacji grupy podobne pod względem morfologicznym. Badania pokazały, że populacje istotnie różnią się w obrębie głównych cech. W badanych populacjach oznaczono zawartość ciał czynnych w kwiatach. Flawonoidy tj. rutynę, hyperozyd, kwercetynę i kemferol oraz hyperycynę i pseudohyperycynę oznaczono metodą HPLC. Metodą spektrofotometryczną oznaczono natomiast sumę wszystkich flawonoidów. Ilościowa zmienność substancji aktywnych w różnych populacjach pozwoliła na wyselekcjonowanie najlepszych roślin do uprawy i zachowania kolekcji polowej.

Results on testing the variability of 27 populations of H. perforatum L. in Lithuania concerning 15 morphological and productivity parameters are presented. The data were subjected to statistical analysis in order to determine the interpopulation variability. Results of Scheffe’s range tests allow the selection of morphologicaly homogenous groups within the analysed data set. The studies indicated that the populations significantly differentiated in the majority of characters. After the analysis of variance of the investigated parameters 3 morphologic types of H. perforatum were distinguished. The spectrophotometric and the high performance liquid chromatography (HPLC) were applied for the quantitative analysis of the active substances in H. perforatum. The flavonoids (rutin, hyperoside, quercetin, kaempferol) were identified under the UV waves of 360 nm and naphtodianthrones (hypericin, pseudohypericin) - under the waves of 590 nm. The total sum of flavonoids was determined under the UV waves of 425 nm. The quantitative variation of active substances in different populations allows the selection of the best plant accessions for their cultivation and conservation in field collections.

Inhibition of human immunodeficiency virus type 1 replication by human interferons alpha, beta and gamma

80%

Yamamoto J. K. , Kruzel M. L. , Louie H. , Georgiades J. A.

tom 41

nr 3-4