A novel peptide, H-Gly-Phe-Trp-Asn-Lys-OH, was isolated from eel guts. This peptide, termed eel intestinal pentapeptide (EIPP), enhanced the frequency of the spontaneous contractions and increased the basal tone of the circular muscle of the esophagogastric junction. Furthermore, EIPP enhanced t...

In vitro effects of pantethine on adipose tissue lipolysis and on both hepatic and intestinal cholesterol and fatty acid synthesis in normolipidemic rats are determined and related to their respective in vivo hypolipidemic effects after acute oral administration. At 3, 5, 7 and 24 h after a sing...

The ability of pantetheine/pantethine to modulate the activity of HMG-CoA reductase (EC 1.1.1.34) was determined in vitro with rat liver microsomes. The decay of the activity was obtained with pantethine in the 10 −5-10 −4 M range, whereas stimulation by pantetheine occurred at 10 −3-10 −2 M, as...

The effects of pantethine on LDL peroxidation in vitro are reported. LDL isolation by density gradient ultracentrifugation from 12 normal subjects were dialyzed 48 h under conditions allowing oxidation. The LDL peroxides were assayed for the presence of malondialdehyde (MDA) on the lipoprotein. ...

During the course of studies of the effects of pantethine, a cysteamine precursor known to deplete tissue concentration of immunoreactive somatostatin, we observed that the subject rats continued to eat despite marked distension of the stomach. To determine whether this effect was caused by drug...

Recent human studies suggest rapid in vivo hydrolysis of the lipid-lowering drug, pantethine, to the vitamin pantothenic acid and the small aminothiol compound, cysteamine. To test whether the active agent is a hydrolysis product, we repeated three experimental models of pantethine's effect...

In several animal models, preliminary studies have indicated that pantethine may inhibit cataract formation. Therefore, preclinical trials need to be conducted to study the pharmacology of pantethine in the ocular lens and to establish its efficacy. Since pantethine, which is a disulfide, can un...

The purpose of this review was to investigate the effectiveness and tolerability of pantethine in the treatment of hyperlipoproteinemia using all published literature to date. Using Medline (January 1966 through December 2002), all published studies involving human subjects, which examined the e...

BackgroundNew, safer, and more effective agents to treat hyperlipidemia and thereby prevent cardiovascular events are under research.

Some abnormalities of gastrointestinal function are presumed to result from changes in levels of stress-related hormones from the hypothalamic-pituitary-adrenal (HPA) axis and sympathetic nervous system (SNS), represented by adrenocorticotropic hormone (ACTH) and neuropeptide Y (NPY), respective...

Bombesin and its mammalian equivalent, gastrin-releasing peptide (GRP), stimulate cell proliferation and are involved in the pathogenesis of several types of human cancer. Bombesin-like peptides also display neuroendocrine activities and regulate neural function. In the present study, we evaluat...

Several lines of evidence have implicated bombesin and its mammalian analogue, gastrin-releasing peptide (GRP), in the mediation and/or modulation of the stress response. However, the physiological role of GRP in mediating conditioned fear responses remains to be elucidated. The objective of the...

The mitochondrial Mg2+-activated adenosine triphosphatase (ATPase; EC 3.6.1.4) from the insect flagellate Crithidia fasciculata ATCC 11745 has been extracted from the membrane by chloroform treatment and purified to electrophoretic homogeneity by a method involving ammonium sulphate fractionatio...

Efrapeptins, peptides isolated from the fungus Tolypocladium niveum, showed toxic activity, as a crude mixture of five closely related compounds, against twospotted spider mite, Colorado potato beetle,southern armyworm, and tobacco budworm. The insecticidal activity of pure efrapeptins was chara...

Steady-state velocity studies using a substrate regenerating system showed that efrapeptin, citreoviridin and aurovertin inhibit both membrane-bound and soluble mitochondrial ATPase (coupling factor F1 from Trypanosoma cruzi. Maximal inhibitions of ATP hydrolysis produced by efrapeptin and citre...

The brush border membrane of the insect midgut is an initial site for interaction of insecticidal proteins. We have investigated the possibility that it may contain a target site for two insecticidal fungal toxins, destruxin and efrapeptin, both of which are ATPase inhibitors. We have studied th...

This study shows for the first time that Tolypocladium species produce efrapeptins, a group of toxic peptides, in vivo but the quantities are too small to account for insect death, suggesting that these insecticidal compounds work in concert with other pathogenicity determinants. There is inter-...

The reactions of a range of aromatic primary amines with pyridine-2-carboxaldehyde were reported, highlighting the effect of the substituents of the amine on the outcomes of the Schiff base reactions. The variant products of the Schiff base reactions were reacted with cis-[PtCl2(DMSO)2], generat...

Monomers and polymers containing 3-arylcarbazol-9-yl fragments were synthesized. The materials were examined by various techniques including differential scanning calorimetry, thermogravimetry, electron photoemission spectrometry and xerographic time of flight technique. The electron photoemissi...

Isoform-selective inhibition of PI3K-α has been identified as one of the important strategy to discover effective and safer anticancer agents. Herein, we report discovery of ‘quinazoline’ as a new chemotype for isoform-selective PI3K-α inhibitors. The indolyl substituted quinazoline 9u displ...