Preparation, characterization, antioxidant, and antifungal activity of phenyl/indolyl-acyl chitooligosaccharides.

In this study, carboxylic acids compounds were grafted onto chitooligosaccharides to prepare seven phenyl/indolyl-acyl chitooligosaccharides derivatives. The structures of the derivatives were characterized by IR spectroscopy, C NMR and elemental analysis. Meanwhile, antioxidant activities in vitro of the novel derivatives were analyzed.

Iron-Catalyzed C(sp)-C(sp) Coupling to Construct Quaternary Carbon Centers.

The construction of quaternary carbon centers via C-C coupling protocols remains challenging. The coupling of tertiary C(sp) with secondary or tertiary C(sp) counterparts has been hindered by pronounced steric clashes and many side reactions. Herein, we have successfully developed a type of bisphosphine ligand iron complex-catalyzed coupling reactions of tertiary alkyl halides with secondary alkyl zinc reagents and efficiently realized the coupling reaction between tertiary C(sp) and secondary C(sp) with high selectivity for the initial instance, which provided an efficient method for the construction of quaternary carbon centers with high steric hindrance.

HIF-1α-mediated augmentation of miRNA-18b-5p facilitates proliferation and metastasis in osteosarcoma through attenuation PHF2.

Extensive evidence has explored the involvement of microRNAs (miRNAs) in osteosarcoma (OS). Limitedly, the concrete function of microRNA-18b-5p (miR-18b-5p) in OS remains unexplored and largely elusive. Here, we validated that miR-18b-5p significantly elevated in OS via analyzing the data from GEO database.

Luteolin attenuates doxorubicin-induced cardiotoxicity by modulating the PHLPP1/AKT/Bcl-2 signalling pathway.

Background: Luteolin (LUT) is a flavonoid found in vegetables and fruits that has diverse functions. Doxorubicin (DOX) is an anthracycline antibiotic that is frequently used for the treatment of various cancers. Unfortunately, the clinical efficacy of DOX is limited by its dose-related cardiotoxicity.

microRNA-96 promotes osteoblast differentiation and bone formation in ankylosing spondylitis mice through activating the Wnt signaling pathway by binding to SOST.

Ankylosing spondylitis (AS) refers to a type of arthritis manifested with chronic inflammation of spine joints. microRNAs (MiRNAs) have been identified as new therapeutic targets for inflammatory diseases. In this study, we evaluated the influence of microRNA-96 (miR-96) on osteoblast differentiation together with bone formation in a murine model of AS.

Effects of Digeda-4 Decoction on the CYP450 Activities in Rats Using a Cocktail Method by HPLC.

Digeda-4 decoction is a traditional Mongolian medicine; its effects on cytochrome (CYP) enzymes are still unclear. CYP450 isoenzymes are the main drug metabolic enzymes, and their activities may be induced or inhibited by certain drugs, which lead to drug interactions in clinical use. Effects of Digeda-4 decoction on the activities of CYP450 subtype enzymes CYP1A2, CYP2C9, CYP2E1, CYP2C19, and CYP3A4 in rats were studied by cocktail method, and the pharmacokinetic parameters of five specific probe drugs (theophylline, tolbutamide, chlorzoxazone, omeprazole, and midazolam) were calculated by DAS software; changes of parameters can be used to evaluate the effects of Digeda-4 decoction on enzyme activities.

Water-Soluble Hypervalent Iodine(III) Having an I-N Bond. A Reagent for the Synthesis of Indoles.

A readily accessible and bench-stable water-soluble hypervalent iodine(III) reagent ( phenyl iodonio) sulfam ate (PISA) with an I-N bond was synthesized, and its structure was characterized by X-ray crystallography. With PISA, various indoles were synthesized via C-H amination of 2-alkenylanilines involving an aryl migration/intramolecular cyclization cascade with excellent regioselectivity in aqueous CHCN. Notably, using this new method as the key step, not only two drug molecules, indometacin and zidometacin, but also another bioactive molecule, pravadoline, were synthesized.

Hypervalent-Iodine-Mediated Ring-Contraction Monofluorination Affording Monofluorinated Five-Membered Ring-Fused Oxazolines.

The first ring-contraction monofluorination reaction mediated by a hypervalent iodine reagent is reported, and the use of the reaction for the synthesis of monofluorinated five-membered ring-fused oxazolines is described. By means of this reaction, a fluorine atom can be selectively introduced either on the five-membered ring or external to it, depending on whether or not the substrate has C-4 alkyl substituents. The reaction was used for the further conversion of probenecid and isoxepac.

Diastereoselective total synthesis of (±)-schindilactone A, Part 1: Construction of the ABC and FGH ring systems and initial attempts to construct the CDEF ring system.

First-generation synthetic strategies for the diastereoselective total synthesis of schindilactone A (1) are presented and methods for the synthesis of the ABC, FGH, and CDEF moieties are explored. We have established a method for the synthesis of the ABC moiety, which included both a Diels-Alder reaction and a ring-closing metathesis as the key steps. We have also developed a method for the synthesis of the FGH moiety, which involved the use of a Pauson-Khand reaction and a carbonylative annulation reaction as the key steps.

[Facial paralysis induced by herpes simplex virus type 1 and the study of facial neurons apoptosis in mice].

Objective: To study the apoptosis of facial motor neurons and the expression of apoptosis-related genes, Bcl-2 and Bax, in the animal model of viral facial paralysis.

Methods: Total of 84 Balb/c mice were divided into viral inoculation group and nerve transaction group. The animals were executed 1, 3, 7, 10, 15, 20 and 30 days after being operated respectively.

[4, 8-disubstituted-8, 9-dihydro-pyrazine[2,3-g]quinazoline-7(6H)-ketones: a novel class of antitumor agents].

Objective: To evaluate the antitumor activity of a novel class of 4, 8-Disubstituted-8, 9-dihydropyrazine[2, 3-g]quinazoline-7(6H)-ketones in vitro, and to screen potential anticancer compounds for further study.

Methods: Seventeen compounds of 4, 8-Disubstituted-8, 9-dihydropyrazine[2, 3-g]quinazoline-7(6H)-ketones were synthesized with solid-phase method for biological evaluation of EGFR tyrosine kinase. MTT method was used to evaluate the cytotoxic activity in vitro against three human cancer cell lines (human lung carcinoma cell line A549, human leukemia cell lines K562 and human gastric carcinoma cell line SGC7901).

[Soil respiration in temperate secondary forest and Larix gmelinii plantation in Northeast China].

With Li-6400-09 chamber, the soil respiration rate in adjacent stands of temperate secondary forest and Larix gmelinii plantation in Maoershan Mountain of Heilongjiang Province was measured from May to October, 2006. The results showed that similar to the variation of soil temperature, the daily pattern of soil respiration could be expressed as a one-humped curve. Over the study period, soil respiration rate varied from 0.

Stereoselective construction of an unprecedented 7-8 fused ring system in micrandilactone a by [3,3]-sigmatropic rearrangement.

The 7-8 bicyclic ring system of micrandilactone A (1) with the required stereochemistry and functional groups was constructed by a Bu3Al-promoted Claisen rearrangement. Computational studies indicated that the exocyclic vinyl ether undergoes a [3,3] sigmatropic process via a chairlike transition state to afford exclusively the Z-double bond in the newly generated 8-membered ring with a high level of chirality transfer.

In vitro and in vivo antitumor effects of doxorubicin loaded with bacterial magnetosomes (DBMs) on H22 cells: the magnetic bio-nanoparticles as drug carriers.

Hepatocellular carcinoma (HCC) is the most common form of cancer although effective therapeutic strategy especially targeted therapy is lacking. We recently employed bacterial magnetosomes (BMs) as the magnetic-targeted drug carrier and found an antitumor effect of doxorubicin (DOX)-loaded BMs (DBMs) in EMT-6 and HL60 cell lines. The aim of this study was to evaluate the in vitro and in vivo anti-neoplastic effects of DBMs on hepatic cancer.

Total synthesis of wedelolactone.

The total synthesis of wedelolactone, a naturally occurring direct inhibitor of IKK complex that can suppress LPS-induced caspase-11 expression, using a convergent synthetic approach, is described. The key steps involved in this synthesis include the palladium-catalyzed Sonogashira reaction and the palladium-catalyzed carbonylative annulation reaction. This approach allows access to diversified analogues of wedelolactone.