Anti-neuroinflammatory effects of novel 5,6-dihydrobenzo[h]quinazolin-2-amine derivatives in lipopolysaccharide-stimulated BV2 microglial cells.

Neuroinflammation is an intricate process that is associated with both normal and pathological conditions. Microglia-mediated neuroinflammation is known to lead to various neurodegenerative and neurological disorders. A series of 3,4-dihydronaphthalen-1(2H)-one derivatives (1-15) and novel 5,6-dihydrobenzo[h]quinazolin-2-amine derivatives (16-30) were synthesized and characterized by various analytical methods, such as NMR and HRMS.

Characteristics influencing high-risk sexual behaviours in elderly men.

With the objective of investigating the characteristics influencing high-risk sexual behaviours in elderly men (60-74 years of age) in Chongqing, China, a total of 1433 healthy elderly men with sexual intercourse frequencies of one to six times/month who were willing to participate in the questionnaires were studied at four hospitals. We measured serum testosterone levels and performed follow-ups every six months, with a total of 1128 elderly men followed up after two years. We also investigated socio-economic and demographic characteristics (age, education, income, location, marital status and number of marriages), types of sexual partners, age differences with fixed sexual partners, frequency of sexual intercourse, combined basic age-related diseases, sexually transmitted infections (STIs) education, elderly self-care ability and high-risk sexual behaviours (frequency of sexual intercourse and number of sexual partners) using questionnaires.

Eis, a novel family of arylalkylamine N-acetyltransferase (EC 2.3.1.87).

Enhanced intracellular survival (Eis) proteins were found to enhance the intracellular survival of mycobacteria in macrophages by acetylating aminoglycoside antibiotics to confer resistance to these antibiotics and by acetylating DUSP16/MPK-7 to suppress host innate immune defenses. Eis homologs composing of two GCN5 N-acetyltransferase regions and a sterol carrier protein fold are found widely in gram-positive bacteria. In this study, we found that Eis proteins have an unprecedented ability to acetylate many arylalkylamines, are a novel type of arylalkylamine N-acetyltransferase AANAT (EC 2.

Synthesis and Antibacterial Evaluation of a Series of 11,12-Cyclic Carbonate Azithromycin-3-O-descladinosyl-3-O-carbamoyl Glycosyl Derivatives.

A novel series of 11,12-cyclic carbonate azithromycin-3--descladinosyl-3--carbamoyl glycosyl derivatives were designed, synthesized, and evaluated for their antibacterial activities in vitro. Most of these compounds had significant antibacterial activity against seven kinds of susceptible strains. In particular, compound exhibited the most potent activity against methicillin-resistant 943 (MIC: 1 μg/mL), 746 (MIC: 2 μg/mL), 447 (MIC: 8 μg/mL), and 236 (MIC: 32 μg/mL), which were two-, four-, four-, four-, and eight-fold stronger activity than azithromycin, respectively.

A genetically encoded biosensor for in vitro and in vivo detection of NADP(.).

NADP(+), the oxidized form of nicotinamide adenine dinucleotide phosphate, plays an essential role as a coenzyme in cellular electron transfer reactions. The concentration of NADP(+) in cytoplasm or organelles is dynamic due to its conversion to many important derivatives. To track the NADP(+) concentration in single living cells, we developed a genetically encoded NADP(+) biosensor by inserting a reporter element, ketopantoate reductase (KPR), between the Förster resonance energy transfer (FRET) pair, cyan fluorescent protein (CFP) and yellow fluorescent protein (YFP).

A novel, colorimetric method for biogenic amine detection based on arylalkylamine N-acetyltransferase.

We developed a novel colorimetric method for rapid detection of biogenic amines based on arylalkylamine N-acetyltransferase (aaNAT). The proposed method offers distinct advantages including simple handling, high speed, low cost, good sensitivity and selectivity.

[Study on stem-tip tissue culture of the traditional Chinese medicine Chrysanthemum morifolium].

Objective: To set up the optimums for the stem-tip tissue culture of Chrysanthemum morifolium cultivated in Anhui Province.

Method: Small sections (about 0.5 mm in length) from the stem-tips were isolated and inoculated with different media, and induced to form the whole plantlet formation.