Strontium ranelate (SR) is the first generation of a new class of medication for osteoporosis, which is capable of inducing bone formation and, to a certain extent, inhibiting bone resorption. The aim of this study was to evaluate the in vitro effects of SR on osteoblastic cell cultures. MC3TE-E...

We have developed a new class of PDE10A inhibitor, a pyrazolo[1,5-a]pyrimidine derivative MT-3014 (1). A previous compound introduced was deprioritized due to concerns for E/Z-isomerization and glutathione-adduct formation at the core stilbene structure. We discovered pyrazolo [1,5-a] pyrimidine...

The cyclic dodecapeptide, cycloleonurinin, cyclo(-Gly-Pro-Thr-Gln-Tyr-Pro-Pro-Tyr-Tyr-Thr-Pro-Ala-), isolated from the fruits of Leonurus heterophyllus, showed potent immunosuppressive effect on human peripheral blood lymphocytes. The solution state conformation of cycloleonurinin was examined b...

In hydra, head activator (HA) acts as positive signal for nerve-cell determination and differentiation. For both events, HA uses cAMP as the second messenger. Evidence is presented that the cAMP agonist, Sp-cAMPS, is able to mimick the effect of HA on nerve-cell determination and differentiation...

The human neuroendocrine cell line BON was used to study second messengers involved in signal transduction for entry into mitosis. BON cells produce the neuropeptide head activator (HA) and use it as autocrine growth factor. HA stimulates BON cell proliferation by triggering entry into mitosis. ...

In NH15-CA2 cells head activator (HA) stimulates cell proliferation by acting in the G2M transition. Cells in mitosis were analyzed by flow cytometry 2–4 h after HA application. HA in a dose-dependent manner stimulated mitosis. Mitosis was prevented by preincubation of cells with pertussis toxi...

Glial cell line-derived neurotrophic factor (GDNF) is a potential therapeutic protein on a variety of central nervous system diseases including ischemic stroke. However, GDNF is a large molecule that cannot cross the blood–brain barrier (BBB), which is still intact in the early hours after stro...

Food processing technology such as protein hydrolysis using proteases has been receiving a lot of attention, and it is important to accurately understand the cleavage specificity of each protease for selecting a protease suited to aims. Although numerous methods have been reported to reveal the ...

Parkinson's disease (PD) is an oxidative stress-mediated neurodegenerative disorder caused by selective dopaminergic neuronal death in the midbrain substantia nigra. Paraoxonase 1 (PON1) is a potent inhibitor of low-density lipoprotein (LDL) and high-density lipoprotein (HDL) against oxidat...

Neuroinflammation and oxidative stress are involved in cerebral ischemia-reperfusion, in which Interleukin 1 (IL-1), as an effective intervention target, is implicated. Interleukin-1 receptor antagonist (IL-1RA) is the natural inhibitor of IL-1, but blood-brain barrier (BBB) limits the brain pen...

Phosphoprotein enriched in astrocytes 15 (PEA15) plays a multi-functional role in neuronal cell survival, however the effects of PEA15 against inflammation have not been investigated yet. To examine the effects of PEP-1-PEA15 protein against lipopolysaccharide (LPS)-induced inflammatory response...

Upon nitrogen step-down, Anabaena sp. PCC 7120 produces semi-regularly spaced heterocysts along filaments. HetR, the master regulator of heterocyst differentiation, has been shown to up-regulate hetP and hetZ in differentiating heterocysts via specific recognition sites. HetR is also predicted t...

Vibrio parahaemolyticus is a major seafood-borne pathogen that causes life-threatening gastroenteric diseases in humans through the consumption of contaminated seafoods. V. parahaemolyticus produces different kinds of toxins, including thermostable direct hemolysin (TDH), TDH-related hemolysin (...

Different concentrations of copolymer of (N-(4-chlorophenyl) acrylamide) (CA) with methyl methacrylate (MMA) were prepared and the reactivity ratio values of copolymerization were calculated using 1H NMR technique. Thermal analysis of the copolymers showed that the thermal stability is intermedi...

Publisher SummaryThis chapter discusses the syntheses of folic acid, aminopterin, and methotrexate analogs in which an intact L-glutamic acid side-chain is present while simultaneously varying the pteridine ring moiety, the C-9, N- 10 bridge and/or the benzoyl group. Several analogs of folic aci...

Hexamethyleneimine (HMI) is used as the structure-directing agent (SDA) in the conventional synthesis method of MCM-49 zeolite. Cyclohexanine (CA) is less toxic and cheaper than HMI. Hence, in this paper, MCM-49 zeolite was successfully synthesized by using CA as a sole SDA with the aid of seeds...

This study designs an alternative transdermal delivery system for 10,11-methylenedioxycamptothecin(MD-CPT) to inhibit keloid. Hyaluronic acid nanoemulsions (HANs) with nano size, negative charge and good stability were prepared as transdermal carriers. The MD-CPT loaded HANs performed desirable ...

A synthesis of 5′-(2H3)-(−)-11-nor-9-carboxy-Δ9-tetrahydrocannabinol methyl ester methyl ether (4) has been accomplished from α-bromoenone 10. The key steps are the stereocontrolled cyclobutane ring opening of the cuprate adduct 18 and the cyclization of the cyclohexenyl triflate 21 with exce...

Mandelic acid (MA) is generally used as a biomarker of the exposure of styrene, which is classified as a class of hazardous environmental pollutants, and also used as an important chiral intermediate in pharmaceutical industry. The previous studies have found the excretion of phenylglyoxylic aci...

To search for new drugs for intervention of drug-resistant lung cancer, a series of hybrids 4-15 from 2-cyano-3,12-dioxooleana-9-dien-28-oic acid (CDDO) and O2-(2,4-dinitrophenyl) diazeniumdiolate were designed, synthesized and biologically evaluated. The most active compound 7 produced relative...