[Advance in modern studies on compatibility of Coptidis Rhizoma and Evodiae Fructus].

In traditional clinical application, Coptidis Rhizome and Evodiae Fructus have been combined to treat various stomach heat and cold syndromes, gastritis, gastric ulcer and the like. With the application of modem instruments and the development of molecular pharmacologic theory, their chemical constituents and pharmacological effects have been sufficiently studied. In this paper, literatures from Pubmed were adopted, with particular emphasis on findings of international counterparts and studies on compatibility of main chemical components in Coptidis Rhizoma and Evodiae Fructus, in order to elaborate on the scientific comparability of Coptidis Rhizoma and Evodiae Fructus through chemical analysis, and pharmacological and biopharmaceutics studies and introduce the future development trend of the studies.

Comparative studies of paeoniflorin and albiflorin from Paeonia lactiflora on anti-inflammatory activities.

CONTEXT: Paeonia lactiflora Pall. (Ranunculaceae) has been used for more than 1000 years in traditional Chinese medicine for the treatment of gynecological problems, cramp, pain, giddiness, and congestion. Paeoniflorin, monoterpene glycosides isolated from P. lactiflora, possesses a variety of pharmacological activities. However, the pharmacological activity of the pharmacological activity of albiflorin, another main monoterpene glycoside, has not been well studied. OBJECTIVES: The present study investigated the anti-inflammatory activities of paeoniflorin and albiflorin using models of lipopolysaccharides (LPS) induced RAW 264.7 cells. MATERIALS AND METHODS: Production of nitric oxide (NO) was measured by the Griess colorimetric method. In addition, prostaglandin E2 (PGE2), interleukin 6 (IL-6) and tumor necrosis factor alpha (TNF-α) synthesis were analyzed using an enzyme-linked immunosorbent assay (ELISA). The protein expression of cyclooxygenase-2 (COX-2) was detected by a cell-based ELISA. The gene expression levels of inducible nitric oxide synthase (iNOS), COX-2, TNF-α, and IL-6 were detected by quantitative real-time reverse-transcription polymerase chain reaction (real-time RT-PCR). RESULTS: Compared with the LPS-induced group, the inhibition rates of NO, PGE2, TNF-α, and IL-6 production were 17.61, 27.56, 20.57, and 29.01% by paeoniflorin and 17.35, 12.94, 15.29, and 10.78% by albiflorin. The IC50 values of paeoniflorin and albiflorin on NO production were 2.2 × 10(-4 )mol/L and 1.3 × 10(-2 )mol/L, respectively. The protein expression of COX-2 was reduced by 50.98% with paeoniflorin and 17.21% with albiflorin. The inhibition rates of gene expression of iNOS, COX-2, IL-6, and TNF-α were 35.65, 38.08, 19.72, and 45.19% by paeoniflorin and 58.36, 47.64, 50.70, and 12.43% by albiflorin, respectively. CONCLUSION: These results show that albiflorin has similar anti-inflammatory effects to paeoniflorin, which provides new evidence that albiflorin can serve as a new chemical marker for the quality control of Paeoniae Radix and the Chinese Pharmacopoeia can be updated.

Protective effects of alginate-chitosan microspheres loaded with alkaloids from Coptis chinensis Franch. and Evodia rutaecarpa (Juss.) Benth. (Zuojin Pill) against ethanol-induced acute gastric mucosal injury in rats.

Zuojin Pill (ZJP), a traditional Chinese medicine formula, consists of Coptis chinensis Franch. and Evodia rutaecarpa (Juss.) Benth. in a ratio of 6:1 (w/w) and was first recorded in "Danxi's experiential therapy" for treating gastrointestinal disorders in the 15th century. However, the poor solubility of alkaloids from ZJP restricted the protective effect in treating gastritis and gastric ulcer. The aim of the study was to investigate the protective mechanism of mucoadhesive microspheres loaded with alkaloids from C. chinensis Franch. and E. rutaecarpa (Juss.) Benth. on ethanol-induced acute gastric mucosal injury in rats. Surface morphology, particle size, drug loading, encapsulation efficiency, in vitro drug release, mucoadhesiveness, and fluorescent imaging of the microspheres in gastrointestinal tract were studied. The results showed that the mucoadhesive microspheres loaded with alkaloids could sustain the release of drugs beyond 12 hours and had gastric mucoadhesive property with 82.63% retention rate in vitro. The fluorescence tracer indicated high retention of mucoadhesive microspheres within 12 hours in vivo. The mucoadhesive microspheres loaded with alkaloids could reduce the gastric injury by decreasing the mucosal lesion index, increasing the percentage of inhibition and increasing the amount of mucus in the gastric mucosa in an ethanol-induced gastric mucosal injury rat model. Moreover, the mucoadhesive microspheres loaded with alkaloids reduce the inflammatory response by decreasing the levels of tumor necrosis factor-α (TNF-α), interleukin 1ß (IL-1ß), downregulating the mRNA expression of inducible nitric oxide synthase, TNF-α, and IL-1ß in gastric mucosa. All the results indicate that mucoadhesive microspheres loaded with alkaloids could not only increase the residence time of alkaloids in rat stomach, but also exert gastroprotective effects through reducing the inflammatory response on ethanol-induced gastric mucosal damage. Thus, these microspheres could be developed as a potential controlled release drug for treatment of gastric ulcer.

Protective effect of danhong injection on acute hepatic failure induced by lipopolysaccharide and d-galactosamine in mice.

Acute hepatic failure (AHF), which leads to an extremely high mortality rate, has become the focus of attention in clinic. In this study, Danhong injection (DHI) was investigated to evaluate the preventive and protective effect on AHF induced by lipopolysaccharide (LPS) and D-galactosamine (GalN) in mice. For AHF induction, ICR mice were intraperitoneally injected with D-GalN (700 mg/kg) and LPS (20 µ g/kg). DHI was administrated twice, at 12 and 1 h, respectively, before D-GalN/LPS injection. After stimulation with D-GalN/LPS for 1 and 6 h, serum and livers were collected for analysis. We found that mice administrated with DHI displayed a higher survival rate, lower serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (TBil), glutathione S-transferase (GST), and tumor necrosis factor (TNF)- α . DHI inhibited the elevations of hepatic lipid peroxidation (malondialdehyde), caspase-8 activity, and mRNA expression levels of inflammatory cytokines (interleukin-1 ß and interleukin-6) increased by D-GalN/LPS in the liver. Furthermore, liver histopathological analysis indicated that the DHI group showed markedly fewer apoptotic (TUNEL positive) cells and less pathological changes than those in the AHF model group. These results provide a novel insight into the pharmacological actions of DHI as a potential candidate for treating AHF.

Effects of ß-cyclodextrin on the intestinal absorption of berberine hydrochloride, a P-glycoprotein substrate.

The major objective of this work is to investigate the enhancing effect of ß-cyclodextrin on the intestinal absorption of berberine hydrochloride, a P-glycoprotein (Pgp) substrate. The inclusion complexation behavior of BBH with ß-CD was investigated by phase-solubility diagram, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffractometry, NMR spectroscopy, and molecular modeling studies. Results indicated that the 1,3-benzodioxole of BBH was included into the cavity of ß-CD to form an inclusion complex which exhibited higher dissolution rate than BBH in vitro. The intestinal absorption of the inclusion complex in rats was significantly higher than the free drug due to its solubilizing effect and Pgp modulatory activity. The mechanisms of ß-CD on Pgp modulation were demonstrated by modifying the Pgp ATPase activity, the Pgp mRNA level and the Pgp expression.