We reported the preparation of a novel trehalose derivative based on enzymatic oxidation of trehalose by water-soluble glucose-3-dehydrogenase (G3DH) from marine bacterium Halomonas sp. α-15 cells. The product of G3DH enzymatic conversion was 3,3′-diketotrehalose (3,3′dkT), a novel trehalose ...

Here we report a high yielding, stereoselective synthesis of the naturally occurring 1,1′-disaccharide neotrehalosadiamine (NTD) and some related analogs. Following an eleven-step sequence, seven of which did not require chromatographic separation, NTD was generated in 60% overall yield from th...

Rubitecan (RFS2000, 9 nitrocamptothecin,) is a new oral topoisomerase I inhibitor. We report a phase II, single-arm, open-label study of RFS2000 as first line treatment for non-small cell lung cancer (NSCLC). Seventeen treatment-naïve patients with stage IIIB (9/17) and IV (8/17) NSCLC (11 male ...

A randomised, open label phase II study was performed in patients with advanced colorectal cancer to evaluate the safety, toxicity and antineoplastic activity of the topoisomerase I-inhibitor rubitecan. A cross-over design was chosen to determine the intrapatient variation of the bioavailability...

Pseudomonas cepacia lipase-catalyzed enantioselective hydrolysis of 2 in water afforded (3S,6R)-3. The antipode (3R,6S)-3 was prepared by enantioselective acylation of 4 using the same enzyme.

ProELH is the prohormone to the bag cell egg-laying peptide of Aplysia. In addition to containing the structure of the hormone (ELH) itself, proELH also contains several other secreted peptides: AP (acidic peptide) and α-, β-, and γ-bag cell peptides (BCPs). The BCPs, ranging in length from 5...

α-Bag cell peptide (α-BCP), one of several secreted peptides encoded in the precursor to the egg-laying hormone (proELH) of the neurosecretory bag cells of Aplysia, has been variously reported to have autoexcitatory or autoinhibitory effects on the cells which secrete it. Since we had found pr...

Double-label immunocytochemistry reveals that immunoreactivity for two putative peptide transmitters, egg-laying hormone and a-bag cell peptide1–9, co-exist in most bag cell somata and processes in the abdominal ganglion of the marine mollusc Aplysia. Together with previous physiological and bi...

Egg laying in the marine molluscan genus Aplysia is elicited by an egg-laying hormone (ELH) which induces ovulation and acts on central neurons to effect egg-laying behavior. ELH, isolated from the A. californica bag cells, and three ELH-related peptides, isolated from the A. californica atrial ...

The neurosecretory bag cells of the mollusk, Aplysia, generate a peptide egg-laying hormone (ELH) from a 29,000 Dalton precursor protein by proteolytic cleavage to a 6–9,000 Dalton intermediate, followed by cleavage of the intermediate. We report here the initial characterization of these cleav...

The caudodorsal cells of Lymnaea and the bag cells of Aplysia are neuroendocrine cells whose peptide products have homologous functions, i.e., regulation of egg deposition. One of the Lymnaea products, calfluxin, increases cytosolic and hence mitochondrial calcium concentrations in secretory cel...

Structure-activity relationships were determined for the natural bag cell peptides (BCPs) and for a series of synthetic analogues in terms of their ability to stimulate (at 30°C) and to inhibit (at 15°C) bag cell adenyl cyclase. We found that the core RLRF motif shared by all these peptides is...

Neuroendocrine secretion often requires prolonged voltage-gated Ca2+ entry; however, the ability of Ca2+ from intracellular stores, such as endoplasmic reticulum or mitochondria, to elicit secretion is less clear. We examined this using the bag cell neurons, which trigger ovulation in Aplysia by...

Targeting signalling molecules to ion channels can expedite regulation and assure the proper transition of changes to excitability. In the bag cell neurons of Aplysia, single-channel studies of excised patches have revealed that protein kinase C (PKC) gates a non-selective cation channel through...

The bag cell peptides (α-, β-, and γ-BCP) are secreted by the neuroendocrine bag cells of Aplysia, and provide feedback modulation of bag cell excitability and cAMP levels. We report here that if 200–500 mM NaCL is included in the assay buffer, the BCPs alter adenylate cyclase activity in a ...

We investigated the effects of shogaol, which has an α, β-unsaturated carbonyl group, and gingerol, which does not, on primary-cultured microglia to understand how the α, β-unsaturated carbonyl interacts with Kelch-like ECH-associated protein (Keap)1. Shogaol (1 μM) but not the same concent...

[6]-Shogaol, an alkylphenol compound purified from the root and stem of ginger (Zingiber officinale), has attracted considerable interest due to its potential anticancer, antioxidative and antirheumatic properties. However, the oral bioavailability of [6]-shogaol has been severely limited becaus...

Subcritical water extraction is an eco-friendly method for the extraction of less polar compounds without the use of organic solvents. This study determined the extraction conditions that maximize the contents of 6-gingerol and 6-shogaol obtained from ginger pulp and peel. The highest yields of ...

Disclosure of ultraviolet (UV) radiation is the key feature from environment to cause redness of the skin, inflammation, photoaging and skin cancer. 6-Shogaol, a spicy compound secluded from ginger, which shows anti-inflammatory effects. Present study was demonstrated the role of 6-Shogaol on UV...

The synthesis of 5-aryl-4-oxo-3,4,5,8-tetrahydropyrido[2,3-d]pyrimidine-7-carboxylic acids 3 from the reaction of 6-aminopyrimidines 1 with arylidene derivatives of pyruvic acid 2 under microwave and ultrasound irradiation is described. The orientation of cyclization process was determined by NM...