Cryptotanshinone and dihydrotanshinone I exhibit strong inhibition towards human liver microsome (HLM)-catalyzed propofol glucuronidation.

Danshen is one of the most famous herbs in the world, and more and more danshen-prescribed drugs interactions have been reported in recent years. Evaluation of inhibition potential of danshen's major ingredients towards UDP-glucuronosyltransferases (UGTs) will be helpful for understanding detailed mechanisms for danshen-drugs interaction. Therefore, the aim of the present study is to investigate the inhibitory situation of cryptotanshinone and dihydrotanshinone I towards UGT enzyme-catalyzed propofol glucuronidation. In vitro the human liver microsome (HLM) incubation system was used, and the results showed that cryptotanshinone and dihydrotanshinone I exhibited dose-dependent inhibition towards HLM-catalyzed propofol glucuronidation. Dixon plot and Lineweaver-Burk plot showed that the inhibition type was best fit to competitive inhibition type for both cryptotanshinone and dihydrotanshinone I. The second plot using the slopes from the Lineweaver-Burk plot versus the concentrations of cryptotanshinone or dihydrotanshinone I was employed to calculate the inhibition parameters (Ki) to be 0.4 and 1.7µM, respectively. Using the reported maximum plasma concentration (Cmax), the altered in vivo exposure of propofol increased by 10% and 8.2% for the co-administration of dihydrotanshinone I and cryptotanshinone, respectively. All these results indicated the possible danshen-propofol interaction due to the inhibition of dihydrotanshinone I and cryptotanshinone towards the glucuronidation reaction of propofol.

Correlation between Antistress and Hepatoprotective Effects of Schisandra Lignans Was Related with Its Antioxidative Actions in Liver Cells.

The present study was conducted to investigate the relationship between the anti-stress and hepato-protective effects of Schisandra Lignans Extract (SLE) on stress-induced liver damage. Seven weeks old male mice were fixed in a restraint tube for 18 h to induce liver damage. SLE was orally administered to animals for 5 days at dosages of 100 and 200 mg/kg/day before exposed to restraint stress. Oral administration of SLE significantly reduced restraint-induced liver damage in experimental animal. SLE was further found to significantly alleviate the provocation of corticosterone in stressed mice. SLE also significantly decreased oxidative damage and increased anti-oxidative capability of liver cells by preventing the over production and accumulation of free radicals. In conclusion, the protective effects of SLE on stress-induced liver damage were confirmed, and the correlation between hepatoprotective and anti-stress effects of schisandra lignans was possible related to its alleviation on the malignant effects of stressors for bio-homeostasis, such as balance of oxidation and reduction in cells.

The protective effect of Schisandra lignans on stress-evoked hepatic metastases of P815 tumor cells in restraint mice.

AIM OF THE STUDY: The present study was conducted to investigate the effects of schisandra lignans extract (SLE) on stress-evoked hepatic metastases of mastocytoma P815 tumor cells, which was closely related with immune function. MATERIALS AND METHODS: The high-performance liquid chromatography (HPLC) fingerprint of SLE was recorded and the percentage composition of schisandra lignans was determined as 82.63%. The contributions of the immunomodulatory properties of SLE to the protective effects on stress-induced hepatic metastases were studied. RESULTS: Our results found that restraint stress significantly promoted hepatic metastases of P815 tumor cells. However, oral administration of SLE (100 and 200mg/kg/d, 14d) significantly reduced the number of metastatic colonies in liver of restrained mice. SLE was further found to be significantly improving T lymphocyte proportions and increasing cytotoxic T lymphocyte (CTL) activity of immunized spleen cells in stressed mice. CONCLUSION: These results indicated that the protective effects of SLE on hepatic metastases were related to its alleviation of the adverse effects of stressors for bio-homeostasis and immunoprotection. The obtained data provided evidences to elucidate the traditional use of Fructus schisandrae as a tonic or sedative.

Biocompatibility study of theophylline/chitosan/beta-cyclodextrin microspheres as pulmonary delivery carriers.

To evaluate the biocompatibility of the theophylline/chitosan/beta-cyclodextrin microspheres, which has a potential application in pulmonary delivery system. The detection of LDH and protein in BALF was examined acute cell toxicity, hemolysis test was carried out to estimate blood toxicity; Micronucleus Test was reckoned to identify genotoxicity, MTT assay was used to evaluate in vitro cytotoxicity, and muscle implantation investigated the tissue biocompatibility. The results demonstrated that the total contents of protein and LDH in BALF were not significantly different from that of normal group. The experiments showed that the cytotoxicity was depended on the concentration and had no cytoxicity at low concentration and no hemolysis activity. The micronucleus frequency of MS B was 0.99 per thousand, which showed no genotoxic effects either. The results of implantation showed that the microspheres had no effect on hemoglobin and no toxicity in the liver and kidney. The inflammations of muscle tissue were not significantly different from that of operative suture, therefore, the MS B possess high good biocompatibility and can be applied in pulmonary sustained release systems.

1,2-Bis(p-tolyl-sulfon-yl)hydrazine.

In the title compound, C(14)H(16)N(2)O(4)S(2), the dihedral angle between the aromatic ring planes is 76.8 (3)° and the S-N-N-S torsion angle is 122.5 (3)°. In the crystal structure, mol-ecules form a chain structure by way of N-H⋯O hydrogen bonds.