A novel tyrosine aminotransferase gene (designated as SmTAT) involved in rosmarinic acid biosynthesis pathway is cloned from Salvia miltiorrhiza Bung. The full-length cDNA of SmTAT is 1,603 bp long with an open reading frame (ORF) of 1,233 bp encoding a polypeptide of 411 amino acid residues. The deduced amino acid sequence of the SmTAT gene shared high homology with other known TATs. Analysis of SmTAT genomic DNA reveals that it contains 6 exons, 5 introns. The analysis of SmTAT promoter region and terminator region was also presented. Semi-quantitative RT-PCR analysis reveals that the constitutive expression of SmTAT in stem is much higher than that in root, leaf. Further expression analysis reveals that the signaling components of defense/stress pathways, such as methyl jasmonate (MeJA), abscisic acid (ABA), salicylic acid (SA) and ultraviolet-B radiation (UV-B), up-regulate the SmTAT transcript levels over the control. This study provides useful information for further studying this gene and its function in rosmarinic acid biosynthetic pathway in S. miltiorrhiza, the roots of which so-called ''Danshen'' possess many pharmaceutical properties for human health.
The synthesis and pharmacological activities of anthraquinone-ibuprofen prodrugs for finding new anti-inflammatory drugs specifically targeting osseous tissues were studied. Two hydrolytically activated anti-inflammatory prodrugs containing anthraquinone moiety and ibuprofen moiety were designed and synthesized. Rhein was chosen as bone-targeting agent and potentially active drug, which was linked chemically with ibuprofen through glycol ester as bone-targeting anti-inflammatory prodrugs. The chemical structures of the new compounds were confirmed by IR, 1H NMR, 13C NMR, MS and elemental analysis. The studies of bioactivities demonstrated that both prodrugs showed significant binding capability to hydroxyapatite (HAP), the major component of bone, and were hydrolytically activated under physiological conditions in vitro and better anti-inflammatory activity in vivo.
A highly efficient one-pot, two-step sequential process consisting of modified Jones oxidation of aqueous cyclovirobuxine D acetate followed by Ruschig degradation after pH regulation with saturated aqueous NaOH, provided cyclobuxophyllinine M in high yield and in a single geometrical isomeric form. 141 ing ketone, which further react with sodium hydroxide at 80°C to give cis-, -unsaturated cyclopentenone in a high yield. This efficient one-pot transformation, together with a relatively straightforward purification process, makes this protocol ideal for the synthesis of parallel compounds.
Angiotensin converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) are widely used in patients who are at high risk of cardiovascular events. A consensus has emerged that ACEIs can reduce the risk of stroke. This programme of overviews of randomized trials was established to investigate the effects of ARBs on the risk of stroke in patients at risk for cardio-cerebrovascular events. Electronic databases were searched up to January 2009, for randomized clinical trials comparing ARBs with other active treatments and placebo in patients at risk for cardio-cerebrovascular events. Data were extracted for patients' characteristics, interventions, quality of trials, and rates of stroke. The efficacy measures were the odds ratios of strokes. We did separate overviews of trials comparing ARBs with placebo, with ACEIs, and with calcium antagonists. The pooled effects were calculated using the random effects model. Twenty three with 1832 patients were included in the analysis. The overview of placebo-controlled trials (11 trials, 44961 patients) revealed ARBs was associated with a significant reduction in the risk of stroke, with a pooled odds ratio of 0.91 (0.84 to 0.98). In the overview of trials comparing ARBs with ACEIs (6 trials, 26537 patients), there were no significant reduced risks of stroke with ARBs (odds ratio 0.93, 0.84 to 1.03). In the overviews comparing ARBs with calcium antagonists (4 trials, 22446 patients), no significant difference was found, with a pooled ratio of 1.16 (0.91 to 1.48). Evidence of the benefits of ARBs on the risk of stroke is provided by the overviews of placebo-controlled trials. There was no evidence of differences when comparing ARBs with ACEIs, and with calcium antagonists. Therefore, ARBs should be regarded as suitable treatments for preventing stroke in patients who are at high risk of cardiovascular events.
In tricyclic fragment of the title molecule, C20H14ClNOS, the central 1,4-dihydropyridine ring adopts a boat conformation while the two benzene rings form a dihedral angle of 17.38 (5)°. In the crystal structure, weak intermolecular N—H⋯O hydrogen bonds link the molecules into chains propagating along the b axis.
Media. -The procedure consists of a modified Jones oxidation followed by Ruschig degradation at pH 9 and proceeds stereoselectively to the (E)-isomer (II) of the target compound. -(LIU, H.-F.; WU, X.-Q.; DUAN, Y.-B.; GU, B.; JI*, M.; Lett.
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