Anti-tumor alkaloids from Peganum harmala.

Six alkaloids peharmalines F-K, along with 14 known ones, were isolated from the aerial part of Peganum harmala L.. The structures of the isolated compounds were determined based on their HR-ESI-MS data, extensive NMR spectroscopic analyses, and ECD calculations. 3-(4-Hydroxyphenyl)quinoline exhibited potent antiproliferative activity against the HepG-2 cell lines with an IC50 value of 3.05 µM. Norharmane displayed a moderate inhibition against A549 and HepG-2 cells with IC50 values of 16.45 µM and 17.27 µM, respectively.

Moutan cortex extract exerts protective effects in a rat model of cardiac ischemia/reperfusion.

Moutan cortex (MC) is a traditional Chinese medicine with diverse biological effects. The present study was performed to investigate the effects of MC on myocardial ischemia/reperfusion (I/R) in rats and to explore its possible mechanisms. Sprague-Dawley rats were administered MC extract (1.98 g/kg, i.g.) for 14 days and underwent a subsequent open-chest procedure involving 30 min of myocardial ischemia and 60 min of reperfusion. The cardioprotective effect of MC was demonstrated by reduced infarct size and marked improvement in the histopathological examination. The increase in the activity of superoxide dismutase (SOD) and glutathione (GSH) as well as the reduction of malondialdehyde (MDA) indicated that MC effectively promoted the anti-oxidative defense system. Increased anti-oxidative defense was accompanied by decreased release of lactate dehydrogenase (LDH) and creatine kinase (CK). The reduction in TUNEL-positive myocytes demonstrated that MC decreased myocardial apoptosis. The mRNA expression of B cell leukemia-2 (Bcl-2) was upregulated by MC and the ratio of Bcl-2/Bcl-2-associated X protein (Bax) mRNA expression was increased. MC pretreatment decreased the mRNA expression of inducible nitric oxide synthase (iNOS). The data from this study suggest that MC exerted protective effects on acute myocardial I/R injury via anti-oxidative and anti-apoptotic activities.

Juglone prevents metabolic endotoxemia-induced hepatitis and neuroinflammation via suppressing TLR4/NF-κB signaling pathway in high-fat diet rats.

Juglone as a natural production mainly extracted from green walnut husks of Juglans mandshurica has been defined as the functional composition among a series of compounds. It showed powerful protective effect in various diseases by inhibiting inflammation and tumor cells growth. However, studies on its anti-inflammatory effect based on high-fat diet-induced hepatitis and neuroinflammation are still not available. In this regard, we first investigated whether juglone suppresses high-fat diet-stimulated liver injury, hypothalamus inflammation and underlying mechanisms by which they may recover them. SD rats were orally treated with or without high-fat diet, 0.25 mg/kg or 1 mg/kg juglone for 70 days. Subsequently, blood, hypothalamus and liver tissue were collected for different analysis. Also, the primary astrocytes were isolated and used to analyze the inhibitory effect of juglone in vitro. Analysis of inflammatory cytokines declared that the inhibition of TNF-α, IL-1ß and IL-6 could be carried by juglone in response to high-fat diet rats. Meanwhile, TLR4 expression and NF-kappa activity also have been confirmed to be the key link in the development of hepatitis and nerve inflammation. The activation was significantly suppressed in treatment group as compared with model. These results indicated that juglone prevents high-fat diet-induced liver injury and nerve inflammation in mice through inhibition of inflammatory cytokine secretion, NF-kappa B activation and endotoxin production.

Anti-hyperglycemic effect of Potentilla discolor decoction on obese-diabetic (Ob-db) mice and its chemical composition.

Potentilla discolor is used as an ethnomedicine in treatments of diabetes mellitus in China for years. In the present study, the anti-hyperglycemic effects of a clinical active extract (decoction) from P. discolor were investigated in Ob-db mice. Four week's treatment of P. discolor decoction ameliorated the development of hyperlipidemia, lipid peroxidation and hyperglycemia associated with hyperphagia and polydypsia in Ob-db mice. P. discolor significantly attenuated the increase of blood glucose and cholesterol levels in Ob-db mice. These findings clearly provided evidences regarding the anti-hyperglycemic potentials of P. discolor decoction. High-resolution liquid chromatography-mass spectrometry/mass spectrometry (HR-LC-MS/MS) was used to analyze the phytochemicals in P. discolor decoction. In an comprehensive analysis of phytochemicals in P. discolor, thirty-five components were identified or characterized in P. discolor decoction and only sixteen of them have been reported in P. discolor previously. There are five major components identified in P. discolor decoction. One of the major components is a flavonoid sulfate, and this is the first evidence for the presences of sulfated flavonoid in P. discolor. Sulfated flavonoids have been reported to improve the complications of diabetes mellitus by inhibition of the aldose reductase in both experimental animals and clinical trials. Therefore, the sulfated flavonoid in P. discolor decoction may in part contribute to the anti-hyperglycemic effect of P. discolor.