[Purification of polyphenols from Sabina vulgaris antoine and its antioxidant properties].

OBJECTIVE: To purify polyphenols from Sabina vulgaris and to investigate its antioxidant properties. METHODS: Polyphenols were purified from Sabina vulgaris Antoine with macroporous resin HPD-700, and the quantity of polyphenols was determined by Folin-Ciocalteu colorimetry. The antioxidant properties of polyphenols were evaluated by total antioxidant capacity (T-AOC) and its activities of scavenging DPPH (1,1 diphenyl-2-picry-hydrazyl) radicals, superoxide anion (O2·-), hydroxyl free radicals (OH·) and ferric reducing antioxidant power (FRAP). RESULTS: After purification, the purity of polyphenols increased from 0.053% to 0.995%.The antioxidant properties study showed that its inhibition rate of scavenging DPPH radicals and FRAP was 151.83 U/ml and 204.59 U/ml. Its scavenging capacity for superoxide anion (O2·-) and hydroxyl free radicals (OH·) was 151.83 U/ml and 204.59 U/ml. The total antioxidant capacity was 72.68 U/ml. CONCLUSION: Polyphenols from Sabina vulgaris Antoine have high antioxidant properties, suggesting that it worth further study of its pharmacological effects.

[Influence of isoliensinine on activity of CYP3A in rats].

OBJECTIVE: To investigate the influence of isoliensinine (IL) on CYP3A enzyme activity. METHODS: A mixture metabolic system of liver microsome enzymes in vitro was developed. A HPLC method to test the metabolic activity of CYP3A was established with testosterone as a probe. The activities of CYP3A enzymes were measured with different IL concentrations and incubation time with testosterone. RESULTS: In mixture metabolic system of liver microsome enzymes, the best incubation concentration of testosterone was 200 µmol/L, the best incubation time was 210 min, in this condition the IC50 of IL for CYP3A inhibition was >1 000 µmol/L. CONCLUSION: No significant interaction between IL and CYP3A is detected, which indicates that IL might be used with CYP 3A enzyme substrates.

The compound losartan cream inhibits scar formation via TGF-ß/Smad pathway.

The role of angiotensin receptor blocker in wound healing and cutaneous fibrosis has become a hotspot in recent years. We have developed a losartan cream that is comparable to triamcinolone ointment in inhibiting scarring. Considering the effects of chitosan and asiaticoside on wound healing and scarring, we added them to the losartan cream this time and improved the formula, expecting to get a better anti-scarring effect. The effects of creams were investigated on mouse scar model with triamcinolone ointment, onion extract gel, and commercial asiaticoside cream set as positive controls. A preliminary exploration of the mechanism involved in TGF-ß/Smad pathway was performed in vivo and in vitro. With all results of anti-scarring, the compound losartan cream (containing chitosan, asiaticoside, and losartan) shows the best effect, followed by the chitosan asiaticoside cream. The treatment of the compound losartan cream inhibited expression of TGF-ß1, collagen, and Smads, and decreased phosphorylation of Smad in vivo. These inhibitory effects were also confirmed in vitro. Our findings indicated that the compound losartan cream could inhibit scarring via TGF-ß/Smad pathway. This cream might be an effective option for scar treatment.

[Study on determination and pharmacokinetics of metabolites from Folium Mori extract in rats].

OBJECTIVE: To establish a RP-HPLC method for simultaneous determination of total quercetin, kaempferol and isorhamnetin in rat plasma after oral administration of Folium Mori extract (FME). METHODS: After a single dose of FME (110 mg/kg) was taken, rat plasma samples were collected. The samples were hydrolyzed with hydrochloric acid (c=3.0 mol/L), the mixed solution was extracted with ether acetone mixture. The total quercetin, kaempferol and isorhamnetin in plasma samples were determined by HPLC, pharmacokinetic parameters were calculated by DAS 3.0 software. RESULTS: The method was linear over the concentration ranges of 0.0545-8.70, 0.0954-14.7 and 0.0545-8.55 µg/ml for quercetin, kaempferol and isorhamnetin, respectively (r=0.9979, 0.9993, 0.9981). The absolute recoveries were 85.3%-86.1%, 79.4%-86.7% and 62.8%-89.7%, respectively and the assay recoveries were all from 94.7% to 107%. The relative standard deviation (RSD) of intra-and inter-day were less than 9.5% and 9.8%, respectively. The main pharmacokinetic parameters were as follows: T(1/2z) was 92.7, 67.9 and 54.2 h; Tmax was 0.400, 0.400 and 3.87 h; AUC(0-∞) was 68.0, 67.5 and 32.8 mg/h/L; MRT(0-∞) was 128, 85.2 and 72.0 h for quercetin, kaempferol and isorhamnetin, respectively. CONCLUSION: The method established in this study is accurate, reliable and reproducible, and can be applied for determination of total quercetin, kaempferol and isorhamnetin in rat plasma after oral administration of FME; the pharmacokinetic studies showed that the distribution of drugs is rapid and elimination is very slow.

Nanomedicine Fabricated from A Boron-dipyrromethene (BODIPY)-Embedded Amphiphilic Copolymer for Photothermal-Enhanced Chemotherapy.

To overcome the shortcomings of chemotherapy including side effects and uncontrollable release, as well as to increase the therapeutic efficacy, a diblock copolymer (mPEG-b-PLA-BODIPY) was constructed containing a NIR absorbing boron-dipyrromethene (BODIPY) tail, a hydrophobic polylactide (PLA) segment, and a hydrophilic poly(ethylene glycol) (PEG) segment. The nanoparticles self-assembled from mPEG-b-PLA-BODIPY with a core-shell structure were utilized to load docetaxel (DTX) in the core through hydrophobic interaction. Tailored drug release and high tumor penetration of the nanomedicine were realized by fully taking advantage of photothermal effect and the enhanced penetration and retention effect, facilitating enhanced therapeutic performance and reducing undesirable side effects. In vivo antitumor studies demonstrate that photothermal-enhanced chemotherapy effectively suppresses tumor progression, while systemic toxicity and side effects of DTX are remarkably decreased benefiting from rational design. This pioneering example provides a blueprint for the next generation of polymeric delivery vehicles integrating novel theranostic functions.

Effect of p-amino-diphenyl ethers on hepatic microsomal cytochrome P450.

The present paper aims to investigate whether p-amino-2',4'-dichlorodiphenyl ether and p-amino-4'-methyldiphenyl ether are inhibitors as well as inducers of P450. Mice were given daily intraperitoneal (ip) injections of p-amino-2',4'-dichlorodiphenyl ether (0.25 mmol/kg) or p-amino-4'-methyldiphenyl ether (0.25 mmol/kg) for 4 days and tested at 24 h and 48 h after the last dose injection. The results showed the mice pentobarbital sleeping time was shorter and the P450 content of hepatic microsome increased significantly in the group pretreated with p-amino-4'-methyldiphenyl ether when compared with the control group, while in mice pretreated with p-amino-2',4'-dichlorodiphenyl ether the hepatic microsome P450 content increased but the pentobarbital sleeping time was extended in clear contrast to the control group. The sleeping time of the phenobarbital group (80 mg/kg daily ip injection for 4 days) was shortened at 24 h after the last injection with increased P450 content of hepatic microsome, but it showed no difference at 48 h. The zoxazolamine-paralysis times of mice treated with p-amino-2',4'-dichlorodiphenyl ether were longer than those of the control mice, while the same dose of zoxazolamine did not lead to paralysis in mice pretreated with BNF. p-Amino-2',4'-dichlorodiphenyl ether and p-amino-4'-methyldiphenyl ether inhibited the activity of 7-ethoxyresorufin O-deethylase from rat hepatic microsome induced by BNF in vitro by 70.0% and 50.1% respectively. These results suggest that p-amino-2',4'-dichlorodiphenyl ether and p-amino-4'-methyldiphenyl ether are inhibitors as well as inducers of P450.