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In the present study we describe the synthesis and some pharmacological properties of eight new analogues of bradykinin (BK). Two peptides were designed by substitution of position 7 or 8 of the known [d-Arg0,Hyp3,Thi5,8,d-Phe7]BK antagonist (Stewart's antagonist) with l-pipecolic acid (l-Pip). The next two analogues were obtained by replacement of the d-Phe residue in position 7 of the Stewart's peptide with l-β2-isoproline (l-β2-iPro) or l-β3-homoproline (l-β3-hPro). The four analogues mentioned above were also prepared in N-acylated form with 1-adamantaneacetic acid (Aaa). Biological activity of the compounds was assessed by isolated rat uterus and rat blood pressure tests. Our results showed that l-Pip in position 7 slightly increased antagonistic potency in the blood pressure test, but it turned the analogue into an agonist in the rat uterus test. Replacement of Thi by l-Pip in position 8 also enhanced antagonism in the rat pressure test but preserved the antagonism in the rat uterus test. l-β2-iPro or l-β3-hPro in position 7 decreased the potencies in both tests. We also demonstrated that acylation of the N-terminus did not increase, as was claimed previously, the antagonistic potencies of the resulting peptides. The results thus support the hypothesis about the existence of different types of BK receptors in the rat uterus and blood vessels. Our studies provide new information about the structure-activity relationship of BK antagonists which may help in designing more potent BK receptor blockers.
 Biotransformation of deuterated-4'-O-methylnorbelladine into alkaloids galanthamine and lycorine in tissue cultures of Leucojum aestivum was demonstrated using HPLC coupled to mass spectrometry. GC-MS screening was also carried to investigate other native and deuterated alkaloids. A total of six labeled alkaloids were identified indicating that 4'-O-methyl-d3-norbelladine is incorporated into three different groups of Amaryllidaceae alkaloids that are biosynthesized by three modes of intramolecular oxidative phenol coupling.
W pracy omówiono aktualny stan wiedzy dotyczący mechanizmów działania genotoksycznego 2-podstawionych pochodnych 5-nitrofuranu. Omówiono główne tory metaboliczne prowadzące do powstawania aktywnych metabolitów tych związków.
Mangiferin, a C-glucopyranoside of 1, 3, 6, 7-tetrahydroxyxanthone, has been isolated from various parts of Mangifera indica (Anacardiaceae). The conclusive structure of mangiferin has been established by various researchers using a wide range of chemical and spectral analytical techniques. Mangiferin has been traditionally used in some parts of world as anti-inflammatory, analgesic, antipyretic, antioxidant, immunomodulator, antitumor, antiviral, and anthelminthic and in obesity treatment. The present article is an attempt to encompass various aspects and details related to the characterization of mangiferin and its subsequent pharmacological screening. The literature data on mangiferin has been comprehensively reviewed and evaluated by the authors and hence, the article contains brief description of phytochemical and pharmacological investigations conducted on mangiferin till now and thus may prove as a guiding force for further research in this particular area.
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