The ability to monitor the estrus cycle in wild and captive marine species is important for identifying reproductive failures, ensuring a successful breeding program, and monitoring animal welfare. Minimally invasive sampling methods to monitor estrus in captive populations have been developed, ...
Hydroxyprolines (Hyp) are non-standard amino acids derived from the post-translational modification of proteins by prolyl hydroxylase enzymes. Some plants and bacteria produce Hyp, and the isomers trans-3-Hydroxy-l-proline (T3LHyp) and trans-4-Hydroxy-l-proline (T4LHyp) are major components of m...
The isopropyl (2R,3R)- and (2S,3S)-cis-2,3-epoxybutanoates were prepared in three steps from l- and d-threonine, respectively. The racemic isopropyl trans-2,3-epoxybutanoate was obtained in two steps from trans-crotonic acid. The previous esters (four stereoisomers) could be easily differentiate...
A synthetic gene encoding a Streptomyces l-proline-3-hydroxylase was constructed and used to produce the hydroxylase protein in recombinant Escherichia coli. A fermentation process for growth of this recombinant E. coli for enzyme production was scaled-up to 250 L. A biotransformation process wa...
Cis-3-hexen-1-ol (cis-HXO) is a green leaf volatile emitted from plants under stress and belongs to an important class of biogenic volatile organic compounds. In this study, we have investigated the potential formation of organosulfates (OSs) from the hydroxyl radical (OH)-initiated oxidation an...
A Pseudomonas sp. UW4 protein (UniProt K9NIA5) of unknown function was identified as similar to 4-oxalocrotonate tautomerase (4-OT)-like and cis-3-chloroacrylic acid dehalogenase (cis-CaaD)-like subgroups of the tautomerase superfamily (TSF). This protein lacks only Tyr-103 of the amino acids cr...
Isothermal vapor-liquid equilibrium (VLE) data were measured for the binary systems of nitrogen with 2-methyl-1-pentanol, 1-octanol, or 1-decanol at temperatures from 333.15 K to 453.15 K and pressures up to 100 bar. Henry's constants of nitrogen in these three alcohols were determined by u...
The privileged location of Santa Maria Island (Azores archipelago) in the middle of the North Atlantic makes the fossiliferous outcrops on this island of utmost importance to gain a better understanding of how coeval living communities relate to the broader evolutionary and biogeographic history...
Sea-level indicators dated to the Last Interglacial, or Marine Isotope Stage (MIS) 5e, have a twofold value. First, they can be used to constrain the melting of Greenland and Antarctic Ice Sheets in response to global warming scenarios. Second, they can be used to calculate the vertical crustal ...
The Last Interglacial (MIS 5e, 128–116 ka) is among the most studied past periods in Earth's history. The climate at that time was warmer than today, primarily due to different orbital conditions, with smaller ice sheets and higher sea-level. Field evidence for MIS 5e sea-level was reporte...
By presenting benthic foraminifera isotope profiles and bulk geochemical composition of core sediments, we offer a mutiproxy reconstruction of the central Okhotsk Sea oceanography between ∼130 to and ∼115 kyr, related to the marine isotopic stage 5e (MIS 5e). Sediments from the site MR0604-PC7...
We have developed a sensitive and specific LC–MS/MS method for the simultaneous determination of alisol A (A), alisol A 23-acetate (A23) and alisol A 24-acetate (A24), the major active components in Rhizoma Alismatis extract (RAE), in rat plasma. In brief, plasma samples were extracted by methy...
Alisol A 24-acetate (AA), a natural triterpenoid isolated from the traditional Chinese medicine Rhizoma Alismatis, has various therapeutic effects. We investigated the anti-nonalcoholic steatohepatitis (NASH) effect of AA and its underlying mechanisms in vitro and in vivo. C57BL/6 mice were fed ...
A series of 2,2-difluoro-2H-chromenes were synthesized from the tandem reactions of ethyl 3-bromo-3,3-difluoropropionate with salicylaldehyde derivatives in good yields under basic conditions. In acidic environment defluorination took place during the reaction. A plausible mechanism was proposed...
The synthesis, the antitumor activity, the SAR and, whenever described, the possible mode of action of 1,2,4-triazine derivatives, their N-oxides, N,N′-dioxides as well as the benzo- and hetero-fused systems are reported. Herein are treated derivatives disclosed to literature from the beginning...
IntroductionThe redox characteristics of 1,2,4-benzotriazine-1,4-dioxides (BTDOs) make them potential radiosensitizing agents for hypoxic cells in solid human cancers. Tirapazamine (TPZ) is the most clinically tested BTDO radiosensitizer, despite its toxicity at effective doses. To date, no BTDO...
The heterocyclic N-oxide, 3-amino-1,2,4-benzotriazine 1,4-dioxide (tirapazamine, 1), shows promising antitumor activity in preclinical studies, but there is a continuing need to explore new compounds in this general structural category. In the work described here, we examined the properties of 7...
New synthetic analogues of the chemotactic N-formyltripeptide HCO–Met–Leu–Phe–OMe have been synthesized. The reported new models, namely Boc–Met–β-Ala–Phe–OMe (1), HCO–Met–β-Ala–Phe–OMe (2), Boc–Met–Tau–Phe–OMe (3), HCO–Met–Tau–Phe–OMe (4) and HCl·Met–Tau–Phe–OMe (5), a...
A series of 17α-substituted estradiols was synthesized in which the stereochemical characteristics of carbons 20 and 21 were modified. It was found that the (Z)-isomer demonstrated more favorable receptor binding affinity than the corresponding (E)-isomer.
Pyridazinone derivatives have been investigated either pre-clinically or clinically in the treatment of various cardiovascular diseases. The main problems associated with these drugs are the poor aqueous solubility and toxicity. Therefore, in the current study, the solubility of pyridazinone der...
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