A sensitive HPLC-ESI-MS method for the simultaneous determination of loureirin A (LA) and loureirin B (LB) in rat plasma and tissues was developed, and the pharmacokinetic and tissue distribution characteristics of LA and LB were investigated after gavage administration. The samples were pretrea...

Loureirin A is a flavonoid extracted from Dragon׳s Blood that has been used to promote blood circulation and remove stasis in Chinese traditional medicine. However, the mechanisms of these effects are not fully understood. We explored the anti-platelet activity and underlying mechanism of lourei...

The interactions of loureirin A (LA) and cochinchinenin C (CC) with human serum albumin (HSA) under simulated physiological conditions (pH = 7.4) have been studied with fluorescence, UV–vis absorption spectroscopic method and molecular docking technique. The results indicated that there was a s...

OBJECTIVETo investigate whether the effect of loureirin B plus capsaicin on tetrodotoxin-resistant (TTX-R) sodium channel.

11β-Hydroxysteroid dehydrogenase-1 (11β-HSD1) plays a key role in glucocorticoid receptor (GR) activation. Besides, it metabolizes some oxysterols and bile acids (BAs). The GR regulates BA homeostasis; however, the impact of impaired 11β-HSD1 activity remained unknown. We profiled plasma and ...

ObjectiveThe effects of diets high in refined grains on biliary and colonic bile acids have been investigated extensively. However, the effects of diets high in whole versus refined grains on circulating bile acids, which can influence glucose homeostasis and inflammation through activation of f...

Promising biomarkers were identified in adult male Crl:CD (SD) rats for the screening of new chemical entities for their potential to cause liver injury. We examined the serum biochemistry, liver histopathology, and bile acid profiles by LC-MS/MS, and the mRNA expression of transporters and CYPs...

BackgroundBile acids (BAs) are known mediators of glucose metabolism that are altered in type 2 diabetes mellitus (T2DM) and gestational diabetes mellitus (GDM). We hypothesised that post-prandial BA fractions are changed in women with Insulin resistance (IR) after recovery from GDM using homeos...

Compact fluorophores are desired for bioconjugation because they minimally perturb the native biological functions of proteins or organelles. However, their absorption and emission wavelengths are typically short and not ideal for practical applications. For example, coumarin is one of the small...

Melanoma skin cancer is the fastest growing cancer in the US [1]. A great need exists for improved formulations and mechanisms to prevent and protect human skin from cancers and other skin damage caused by sunlight exposure. Current efforts to prevent UV damage to human skin, which in many cases...

We have earlier postulated that the presence of a pyridazone ring fused with an anthracenedione moiety resulted in the analog’s ability to overcome multidrug resistance of tumor cells [J. Med. Chem. 1999, 42, 3494]. High cytotoxic activity of obtained anthrapyridazones [Bioorg. Med. Chem. 2003,...

New designer drugs such as K2, Spice, and “bath salts” present a formidable challenge for law enforcement and public health officials. The following report summarizes a three-year study of 1320 law enforcement cases involving over 3000 products described as vegetable material, powders, capsule...

A series of chiral derivatizing reagents (CDRs) was synthesized by nucleophilic replacement of one chlorine atom in cyanuric chloride (2,4,6-trichloro-1,3,5-triazine; s-triazine) by alkoxy (methoxy, butoxy, 1,1,1-trifluoroethoxy) or aryloxy groups (phenoxy, nitrophenoxy, phenylphenoxy, 4-methylc...

Fatty acid amide hydrolase is a key enzyme in the inactivation of the analgesic and anti-inflammatory endocannabinoid anandamide. Previously, the chiral compound 1-(1H-benzotriazol-1-yl)-3-(4-phenylphenoxy)butan-2-one was identified as a potent inhibitor of fatty acid amide hydrolase and is ther...

Mutations induced by substances formed during food cooking are a field of growing interest; for a better comprehension of the mechanism of action of these carcinogens, simple routes to their synthesis are needed. In this letter we describe an easy method for 2-amino-1-methyl-6-phenylimidazo[4,5-...

Hair follicle research is currently focused on the development of drug-loaded nanocarriers for the targeting of follicular structures in the treatment of skin and hair follicle-related disorders. In the present study, a dual-label nanocarrier system was implemented in which FITC-labeled BSA hydr...

3,5-O-Benzylidene-2-C-cyano-1,4-anhydro-l-xylitol 7 was synthesized stereoselectively from d-xylose in 7 steps. 2-C-(4-Aminocarbonyl-2-thiazoyl)-1,4-anhydro-l-xylitols and their fluoro derivatives were synthesized from the cyanohydrin 7. Fluorination of compound 9 proceeded with retention of con...

A highly enantio-selective ene reaction was developed on the bases of charility transfer. Under the influence of Me2AlCl, the reactions of various aldehydes with (S)-3-(tert-butyldimethylsiloxy)-2-(ethylthio)-1-butene which was easily prepared from (S)-ethyl lactate afforded the optically active...

A NHCs-mediated benzoates formation was developed by treatment of aromatic aldehydes with alkyl halides in the presence of oxygen. Corresponding benzoate derivatives were obtained in high yields up to 99%. The reaction mechanism was also discussed and a NHCs-mediated O-alkylation and subsequent ...

The male antifertility effect of a water–chloroform extract of Tripterygium wilfordii Hook. f. (GTW) and several monomers isolated from GTW has attracted worldwide interest. In the present study, the effects of two isolated monomers from GTW, demethylzeylasteral and celastrol, on the Ca2+ chann...