Enhanced Stability and Oral Bioavailability of Folic Acid-Dextran-Coenzyme Q10 Nanopreparation by High-Pressure Homogenization.

The preparation of folic acid-dextran-coenzyme Q10 (FA-DEX-CoQ10) nanopreparation was optimized by high-pressure homogenization to improve the dissolution and oral bioavailability of CoQ10. The preparation conditions of FA-DEX-CoQ10 nanopreparation were optimized by single-factor and orthogonal experimental design. The properties of CoQ10 raw materials, CoQ10 physical mixtures, and FA-DEX-CoQ10 nanopreparation were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). The concentration of CoQ10 in rat plasma was determined by high-performance liquid chromatography, and the corresponding pharmacokinetic parameters were calculated. The optimal preparation method is as follows: mass ratio of CoQ10/FA-DEX of 1:18, mass ratio of stabilizer/CoQ10 of 0.4:1, 6 homogenization cycles, and homogenization pressure of 800 bar. These conditions resulted in a mean particle size of 87.6 nm. SEM showed that the particles was spherical. DSC and XRD analyses showed that the crystallinity of FA-DEX-CoQ10 nanopreparation decreased. FA-DEX-CoQ10 possesses long-term stability. By single-factor and orthogonal experiments, the dissolution rate, Cmax, and area under the curve (AUC) of the optimized FA-DEX-CoQ10 nanopreparation were 3.95, 2.7, and 2.4 times as much as those of the raw materials. The results showed that FA-DEX-CoQ10 nanopreparation had better oral bioavailability.

Antioxidant Properties of Phenolic Compounds in Renewable Parts of Crataegus pinnatifida inferred from Seasonal Variations.

In this study, the effect of seasonal variations on Crataegus pinnatifida, changes in antioxidant activity and active components in C. pinnatifida leaves, roots, twigs, and fruits from May to October were investigated. Through correlation analysis of climatic factors and 7 phenolic compounds yield, the phenolic compounds content was positively correlated with temperatures and daytime. The correlation coefficient of temperatures and daytime were 0.912 and 0.829, respectively. 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, 2,2'-azino-bis 3-ethylbenzothiazoline-6-sulphonic acid (ABTS) radical scavenging and reducing power tests were employed to evaluate the antioxidant activity of the C. pinnatifida. C. pinnatifida leaves exhibited significant advantages in terms of higher phenolic contents and excellent antioxidant activities. Principal component analysis (PCA) revealed that 2 main PC characterize the C. pinnatifida phenolic composition (82.1% of all variance). C. pinnatifida leaves in September possessed remarkable antioxidant activity. The results elucidate that C. pinnatifida leaves, as renewable parts, are suitable for application as antioxidant ingredients.

Aspidin BB, a phloroglucinol derivative, induces cell cycle arrest and apoptosis in human ovarian HO-8910 cells.

Aspidin BB, an effective phloroglucinol derivative from Dryopteris fragrans (L.) Schott, has been previously reported to exert high biological activities. In this study, we analyzed the underlying mechanisms of aspidin BB on human ovarian cancer cell line, HO-8910. Aspidin BB significantly inhibited HO-8910 cell proliferation in a dose- and time-dependent manner. The IC50 values were 15.02, 25.79 and 68.81µM after 72, 48 and 24h treatment, respectively. Meanwhile, aspidin BB markedly induced apoptosis evidenced by characteristic apoptotic morphological changes, nuclear DNA fragmentation, annexin V-FITC/propidium iodide (PI) double staining and S peak. Western blot analysis showed that aspidin BB suppressed Bcl-2 expression and enhanced Bax expression to desintegrate the outer mitochondrial membrane, then caused cytochrome c release which led to the activation of effector caspase-3, and further cleaved the poly ADP-ribose polymerase (PARP) in the nucleus, finally induced cell apoptosis. Furthermore, aspidin BB provoked S phase arrest in HO-8910 cells with up-regulation of pRb, E2F1, CDK2, cyclin E and cyclin A proteins. Taken together, these findings support the conclusion that aspidin BB exhibits cytotoxicity towards human ovarian cancer HO-8910 cells through induction of apoptosis via mitochondrial pathway and arresting cell cycle progression in S phase.

Negative-pressure cavitation extraction of four main vinca alkaloids from Catharanthus roseus leaves.

In the present study, an improved method termed negative-pressure cavitation extraction (NPCE) followed by reverse phase high-performance liquid chromatography (RP-HPLC) was developed for the extraction and quantification of vindoline (VDL), catharanthine (CTR), vincristine (VCR) and vinblastine (VLB) from Catharanthus roseus leaves. The optimized method employed 60-mesh particles, 80% ethanol, a negative pressure of -0.075 MPa, a solid to liquid ratio of 1:20, 30 min of extraction and three extraction cycles. Under these optimized conditions, the extraction yields of VDL, CTR, VCR and VLB are 0.5783, 0.2843, 0.018 and 0.126 mg/g DW, respectively. These extraction yields are equivalent to those from the well-known ultrasonic extraction method and higher than the yields from maceration extraction and heating reflux extraction. Our results suggest that NPCE-RP-HPLC represents an excellent alternative for the extraction and quantification of vinca alkaloids for pilot- and industrial-scale applications.