Modulation of drug-metabolizing enzymes and transporters under hypoxia environment / 生理学报

Drug metabolism is significantly affected under hypoxia environment with changes of pharmacokinetics, expression and function of drug-metabolizing enzymes and transporters. Studies have shown that hypoxia increases the release of a series of inflammatory cytokines which can modulate drug metabolism. Besides, both hypoxia inducible factor 1α (HIF-1α) and microRNA-mediated pathways play a role in regulating drug metabolism. This article reviewed the impact and single-factor modulating mechanisms of drug metabolism under hypoxia, and put forward the speculation and prospects of multi-factor modulating mechanisms.

Spectrum-effect relationship between HPLC fingerprints and bioactive components of Radix Hedysari on increasing the peak bone mass of rat / 药物分析学报

The traditional Chinese medicine of Radix Hedysari plays an important role in invigorating gas for as-cending, benefiting blood for promoting production of fluid, and promoting circulation for removing obstruction in collaterals, which is consistent with the principle of treatment for osteoporosis. This study is designed to investigate the bioactive components on increasing peak bone mass (PBM) by exploring the spectrum-effect relationship between chromatography fingerprints and effect. Multiple indicators are selected to evaluate the pharmacological activity. In fingerprints, 21 common peaks are obtained, five of which are identified. Furthermore, gray relational analysis (GRA) is a quantitative method of gray system theory and is used to describe the correlation degree of common peaks and pharmacological activities with relational value. 21 components are then divided into three different regions, of which ononin and calycosin play an extremely significant role in increasing PBM. In addition, factor analysis and hierarchical cluster analysis (HCA) are used to screen the optimal producing area for Radix Hedysari. This provides a comprehensive and efficient method to improve the quality evaluation of Radix Hedysari, confirming the bioactive components for PBM-enhancement and further develop its medicinal value.

Complex enzyme combined with ultrasound extraction technology, physicochemical properties and antioxidant activity of Hedysarum polysaccharides / 中国中药杂志

In this study, complex enzymes combined with ultrasonic extraction technology（MC） were used, to select optimal extraction combinations by single factor and orthogonal test, with Hedysarum polysaccharides yield and content as the comprehensive indexes. The components, physicochemical properties and antioxidant activity of Hedysarum polysaccharides from complex enzyme combined with ultrasonic extraction（HPS-MC）and the Hedysarum polysaccharides from hot water extraction（HPS-R）were analyzed. The results showed that：complex enzymes had significant effect on the yield and content of Hedysarum polysaccharides, and the ultrasonic power could significantly improve the content of Hedysarum polysaccharides. The optimum technological parameters were as follows: complex enzyme ratio 1:1, ultrasonic power 105 W, ultrasonic time 60 min, and enzymatic hydrolysis pH 5, achieving （14.01±0.64）% and （92.45±1.47）% respectively for the yield and content of Polysaccharides. As compared with HPS-R, the molecular weight, absolute viscosity and protein content of HPS-MC were decreased, while the content of uronic acid was increased. In the antioxidant system, the concentration of polysaccharide was within the range of 1-7 g·L⁻¹; the antioxidant activity of HPS-MC was higher than that of HPS-R, and HPS-MC (80%) with the lowest molecular weight showed a significant dose effect relationship with the increase of the experimental concentration. In conclusion, MC is a simple, convenient, economical and environmentally friendly extraction technology, and the Hedysarum polysaccharides extracted by this method have obvious antioxidant activity.

Multi-index integrated evaluation of spectrum-effect relationship on immunocompetence of Radix Astragali / 药学学报

The study was aimed to investigate the correlation between the immunocompetence and the fingerprints of supernatant extracts from Radix Astragali by multi-index integrated evaluation, and reveal the material basis of Radix Astragali improving the immunological function. After oral administration 10 batch of supernatant extracts from Radix Astragali on immunosuppressed mice, phagocytic index, delayed type hypersensitivity (DTH) degree, organs index and the level of cytokines IFN-γ, IL-4 (ELISAs) were measured, and each common peak from HPLC-DAD/HPLC-ELSD fingerprints were correlated with the above data. A number of components in supernatant extracts of Radix Astragali display a substantial correlation with the immunocompetence. Supernatant extracts of Radix Astragali can significantly enhance immunological function on mice, which is related to various components in Radix Astragali.

Determination of eight active components in Radix Hedysari by HPLC and its cluster analysis / 药学学报

An HPLC method was established for the determination of adenosine, γ-aminobutyric acid (GABA) and six flavonoids (calycosin-7-glucoside, ononin, calycosin, isoliquiritigenin, formononetin and medicarpin) in Radix Hedysari. The samples were extracted with methanol by refluxing for 4 h. The HPLCDAD was performed on a Diamonsil C18 column (250 mm×4.6 mm, 5 μm) with acetonitrile-water as the mobile phase. The column temperature was at 40℃ and the flow rate was 1.0 mL·min-1, while the temperature of drift tube was 110.5℃ and the nebulizing gas flow was 3.1 L·min-1 for the ELSD system. The results showed all the eight components had good linear relationships (r2=0.992 8-1.000 0) in the range of the test concentration. The RSD of precision, stability and repeatability were less than 2%. The average recovery rates were 96.78%-103.45%, and RSD were 0.29%-1.61%. The index component contents of Radix Hedysari form 24 different origins were determined and used as variable factors in clustering analysis. The results were classified into 2 groups basically in accordance with the regional cluster. And the consequence was in consistent with the results of principal component analysis. This HPLC method is simple, shows good sensitive and accurate, and provides the experimental basis for multi-index control of Radix Hedysari. Clustering analysis for Radix Hedysari quality control has a certain reliability and objectivity.

Chemical structural features and anti-complementary activity of polysaccharide HPS1-D from Hedysarum polybotrys / 中国中药杂志

HPS1-D, an active polysaccharide,was isolated and purified from Hedysarum polybotrys. HPS1-D was obtained after treated with Savage method and H2O2, and purified with DEAE-cellulose 52 and Sephadex G-100 gel filtration chromatography. Then physicochemical property analysis, GC, methylation, partial acid hydrolysis, and NMR method were used to study chemical structural of HPS1-D. The conformation was primarily analyzed with GPC-MALLS method and Congo red reaction. The anti-complementary activity of HPS1-D was evaluated with the hemolysis assay. HPS1-D was a heteropolysaccharide and consisted of D-glucose, L-arabinose, (7.2:1.3). HPS1-D proved to be a neutral sugar, with 1, 4-and 1, 4, 6-alpha-D-glucopyranosyl residues in backbone ,and 1, 5-and 1, 3, 5-alpha-L-arabinofuranosyl residues in branches. HPS1-D has a random coil state conformation with monodisperse mass distribution in 0.9% NaCl solution. And HPS1-D had triple-helix conformation in concentrate of NaOH solution. Anti-complementary activity of HPS1-D was closed to its positive control heparin.

Investigation on chromatogram-pharmacodynamics relationship of Angelica sinensis on effect of replenishing blood / 中国中药杂志

Blood deficiency model of mice was copied by subcutaneous injection with 200, 100 and 100 mg x kg(-1) (0.01 mL x g(-1)) acetyl phenylhydrazine (APH) at the frist, fourth, and seventh days. Mice in each group were perfused with different extracted parts of Angelica sinensis (drug dosage was 2.4 g x kg(-1)) at the tenth day, once a day for 10 days. Then compare the influence of different extracted parts of Angelica sinensis to RBC, Hb, PLT and thymus, spleen and weight changes of blood deficiency mice. The peak areas of each common peak from HPLC fingerprint were associated with the date of replenishing blood pharmacodynamics efficacy by using gray relation statistic, which was used to research the chromatogram-pharmacodynamics relationship. The results showed that the part of DSC has the better effect in replenishing blood. The contribution degree of the DSC to replenishing blood of each component were determined by correlation size, and ferulic acid made the largest contribution, but contribution of other components should not be ignored. In this paper, we research the relationship of the HPLC fingerprint and spectrum activity relationship, determine the material basis of the DSC for replenishing blood, and provide effective way to represent the spectral correlation effect.

Sulfated modification and anticoagulant activity in vitro of sulfated glucan isolated from the aqueous extract of Hedysarum polybotrys / 药学学报

SHG was sulfated by chlorosulfonic acid-pyridine method, and six samples which we got were prepared in different reaction conditions. There is a characteristic absorption peak near 260 nm in UV spectra and there are two characteristic absorption peaks near 1240 cm(-1) and 810 cm(-1) in the FT-IR. Degree of sulfation (DS) was calculated by elemental analysis and turbidimetry. Under the same conditions the absorption peaks become strong with the DS increase. The anticoagulant activity of SHG and sulfated modification samples was evaluated by the classic coagulant assays of prothrombin time (PT), activated partial thrombin time (APTT) live enzymes, and plasma thrombin time (TT). Results show that sulfated SHG has a good anticoagulant activity in vitro, and DS increased activity within a certain range.

Spectrum-effect relationship of reducing phlegm effect of Peucedanum harrysmithii var. subglabrum / 中国中药杂志

<p><b>OBJECTIVE</b>To analyze the relationship between high-performance liquid chromatography (HPLC) fingerprints of the chloroform extract fractions of Peucedanum harrysmithii var. subglabrum (PHS) and its phlegm-reducing effect, in order to establish "active component group for reducing phlegm".</p><p><b>METHOD</b>HPLC was adopted to determine and analyze HPLC fingerprints of chloroform extract fractions of PHS. Phenol red expectorant experiment was used to observe the phlegm-reducing effect in mice. Mice were administered intragastrically with chloroform extract fractions for 6 days (1.4 g x kg(-1)), with acute bronchitis syrup as the positive control drug (12 mL x kg(-1)). The phenol red secretion in mice was determined by spectrophotometer. Then the grey relational analysis was used to study the spectrum-effect relationship.</p><p><b>RESULT</b>The phlegm-reducing effect of the chloroform extract fractions of PHS were resulted from the combined effect of all of its chemical components. Its various characteristic peaks represented different chemical components, and the order of their contributions to the phlegm-reducing effect was (number of peaks) 13 > 12 > 16 > 18 > 19 > 6 > 20 > 14 > 1 > 11 > 15 > 10 > 17 > 2 > 5 > 4 > 7 > 3 > 8 > 9, in No. 1, 3, 4, 10, 13 and 16 characteristic peaks were identified as marmesin, psoralen, xanthotoxin, Pd-Ib, pteryxin and peuformosin.</p><p><b>CONCLUSION</b>The chloroform extract fractions of PHS show strongly phlegm-reducing effect. There may be certain relationship between their HPLC fingerprint and phlegm-reducing effect.</p>