Study on metabolic dynamics,metabolic enzyme phenotype and species difference of hepatic and intestinal microsome of psoralidin / 中国中药杂志

This study aims to investigate metabolic activities of psoralidin in human liver microsomes( HLM) and intestinal microsomes( HIM),and to identify cytochrome P450 enzymes( CYPs) and UDP-glucuronosyl transferases( UGTs) involved in psoralidin metabolism as well as species differences in the in vitro metabolism of psoralen. First,after incubation serial of psoralidin solutions with nicotinamide adenine dinucleotide phosphate( NADPH) or uridine 5'-diphosphate-glucuronic acid( UDPGA)-supplemented HLM or HIM,two oxidic products( M1 and M2) and two conjugated glucuronides( G1 and G2) were produced in HLM-mediated incubation system,while only M1 and G1 were detected in HIM-supplemented system. The CLintfor M1 in HLM and HIM were 104. 3,and57. 6 μL·min~(-1)·mg~(-1),respectively,while those for G1 were 543. 3,and 75. 9 μL·min~(-1)·mg~(-1),respectively. Furthermore,reaction phenotyping was performed to identify the main contributors to psoralidin metabolism after incubation of psoralidin with NADPH-supplemented twelve CYP isozymes( or UDPGA-supplemented twelve UGT enzymes),respectively. The results showed that CYP1 A1( 39. 5 μL·min~(-1)·mg~(-1)),CYP2 C8( 88. 0 μL·min~(-1)·mg~(-1)),CYP2 C19( 166. 7 μL·min~(-1)·mg~(-1)),and CYP2 D6( 9. 1 μL·min~(-1)·mg~(-1)) were identified as the main CYP isoforms for M1,whereas CYP2 C19( 42. 0 μL·min~(-1)·mg~(-1)) participated more in producing M2. In addition,UGT1 A1( 1 184. 4 μL·min~(-1)·mg~(-1)),UGT1 A7( 922. 8 μL·min~(-1)·mg~(-1)),UGT1 A8( 133. 0 μL·min~(-1)·mg~(-1)),UGT1 A9( 348. 6 μL·min~(-1)·mg~(-1)) and UGT2 B7( 118. 7 μL·min~(-1)·mg~(-1)) played important roles in the generation of G1,while UGT1 A9( 111. 3 μL·min~(-1)·mg~(-1)) was regarded as the key UGT isozyme for G2. Moreover,different concentrations of psoralidin were incubated with monkey liver microsomes( MkLM),rat liver microsomes( RLM),mice liver microsomes( MLM),dog liver microsomes( DLM) and mini-pig liver microsomes( MpLM),respectively. The obtained CLintwere used to evaluate the species differences.Phase Ⅰ metabolism and glucuronidation of psoralidinby liver microsomes showed significant species differences. In general,psoralidin underwent efficient hepatic and intestinal metabolisms. CYP1 A1,CYP2 C8,CYP2 C19,CYP2 D6 and UGT1 A1,UGT1 A7,UGT1 A8,UGT1 A9,UGT2 B7 were identified as the main contributors responsible for phase Ⅰ metabolism and glucuronidation,respectively. Rat and mini-pig were considered as the appropriate model animals to investigate phase Ⅰ metabolism and glucuronidation,respectively.

IVOS Ⅱ versus Sperm Class Analyzer in the results of semen analysis / 中华男科学杂志

Objective@#To compare the results obtained from the computer-aided sperm analysis (CASA) systems of the two fully-automated commercial sperm quality analyzers, Hamilton-Thorn IVOS Ⅱ (IVOS Ⅱ) and Spanish Sperm Class Analyzer (SCA).@*METHODS@#A total of 99 semen samples were collected in the Center of Reproduction of Shenzhen Zhongshan Urology Hospital from September 2018 to October 2018 and, according to the sperm concentration, divided into groups A (50 ×10⁶/ml). IVOS Ⅱ, SCA and manual microscopy were used for the examination of each sample, followed by comparison of the sperm concentration, sperm motility and percentage of progressively motile sperm (PMS) obtained from IVOS Ⅱ and SCA.@*RESULTS@#The sperm concentrations derived from IVOS Ⅱ and SCA were significantly higher than that from manual microscopy in group A (［10.24 ± 4.60］ and ［10.20 ± 5.11］ vs ［8.45 ± 4.15］ ×10⁶/ml, P 0.05) or C (［102.14 ± 45.97］ and ［109.48 ± 46.32］ vs ［104.74 ± 41.87］ ×10⁶/ml, P > 0.05). Significant differences were not observed between IVOS Ⅱ and SCA in the percentage of PMS (［24.21 ± 14.62］% vs ［23.92 ± 15.42］%, P > 0.05) or sperm motility (［37.48 ± 19.34］% vs ［37.69 ± 16.61］%, P > 0.05) in group B, nor in group C (PMS: ［30.80 ± 12.06］% vs ［32.98 ± 16.10］%, P > 0.05; sperm motility: ［44.50 ± 15.62］% vs ［47.26 ± 17.46］%, P > 0.05). Both the percentage of PMS and sperm motility obtained from IVOS Ⅱ were remarkably lower than those derived from SCA in group A (PMS: ［18.54 ± 12.96］% vs ［22.90 ± 12.88］%, P < 0.05; sperm motility: ［26.97 ± 14.05］% vs ［34.90 ± 15.18］%, P < 0.05). IVOS Ⅱ and SCA both showed a high repeatability (CV <15%), and the former exhibited an even higher one than the latter, in detection of sperm concentration, sperm motility and the percentage of PMS.@*CONCLUSIONS@#IVOS Ⅱ and SCA both had a good consistency in the results of sperm concentration, motility and progressive motility, but showed a poor comparability with low-concentration semen samples.

The overall quality control of xianling gubao capsules based on hplc-uvd-elsd fingerprint and simultaneous determination of main representative components / 中国药学杂志

OBJECTIVE: To establish the fingerprint of Xianling Gubao Capsules (XLGB) by multi-wavelength HPLC-UVD-ELSD and determine the main representative components simultaneously, in order to provide reference for the overall quality control of XLGB.METHODS: The separation was developed on Poroshell 120 EC-C18 column (4.6 mm×100 mm, 2.7 μm) by gradient elution with methanol-water at 240, 270 and 334 nm, the temperature of drift tube was maintained at 105 ℃ and the carrier gas flow rate was 2.0 L•min-1. An HPLC-UVD-ELSD fingerprint of XLGB was set up, and 15 batches of XLGB were evaluated by similarity assay. Furthermore, the contents of the main representative components were determined on the premise of small disparities between batches. RESULTS: The multi-wavelength HPLC-UVD-ELSD fingerprint of XLGB was established with good separation, and six chemical components were determined simultaneously. Thirty-one main characteristic peaks from six herbs of XLGB were chemically identified and 26 main characteristic peaks were assigned to individual herbs. The similarity of 15 batches of XLGB was about 0.943 to 0.997. Moreover, good linear relationships were found (r=0.999 0-0.999 6), and the average recovery rates were 98.5%-104.9%. CONCLUSION: The method can be used for the overall quality control of XLGB with good specificity and high efficiency and is close to the actual production, which is promising to be further improved to be used as an industry internal control standard.

Phytochemistry and pharmacology of Allii Macrostemonis Bulbus, a traditional Chinese medicine / 中国天然药物

Allii Macrostemonis Bulbus (Xiebai in Chinese), as a famous traditional Chinese medicine, has great medicinal and dietary values since ancient times. In China, the dry bulbs of Allium macrostemon and Allium chinense are both used as its original plants. Pharmacological studies have revealed that both of them could increase plasminogen activator activity and prolong the effect of coagulation to achieve antiplatelet aggregation which validates their traditional uses for the treatment of thoracic obstruction and cardialgia in clinics. Besides, several other significant activities, including lipid-lowering, anti-atherosclerosis, antitumor, antispasmodic, antibacterial, antioxidant, and insecticidal activities, have already been reported. The volatile oils, nitrogenous compounds, and steroidal saponins are the major beneficial compounds. Among them, steroidal saponins are considered as the characteristic constituents. In this review, the current information concerning the phytochemistry and pharmacology of Allii Macrostemonis Bulbus is summarized comprehensively. In addition, several research future perspectives are presented, especially the mechanism of bioactive components and fraction from the bulbs of Allium macrostemon and Allium chinense.

Determination of plasma protein binding rate of methyl protodioscin with ultrafiltration / 中国中药杂志

<p><b>OBJECTIVE</b>To study the plasma protein binding rate of methyl protodioscin.</p><p><b>METHOD</b>The ultrafiltration was employed to determine the plasma protein binding rate of methyl protodioscin. The plasma concentrations of methyl protodioscin were measured by HPLC-MS-MS.</p><p><b>RESULT</b>The plasma protein binding rate of methyl protodioscin with rat plasma at the concentration of 20.0, 100 and 200 microg x mL(-1) were (94.6 +/- 0.16)%, (91.6 +/- 0.35)% and (86.10 +/- 0.60)%, respectively, while the plasma protein binding rate of methyl protodioscin with normal human plasma at the above concentrations were (82.11 +/- 5.12)%, (84.54 +/- 0.32)% and (88.52 +/- 1.02)%, respectively.</p><p><b>CONCLUSION</b>The binding rate of methyl protodioscin with plasma protein is high.</p>

Applications of tree-shaped structure in DICOM based on XML / 中国医疗器械杂志

In order to improve the sharing of DICOM, a proposal is offered to introduce XML into DICOM on the SPIE 2005 and in this way, better readability and expansibility of DICOM files have been achieved. On this basis, the DICOM data structure is improved further by replacing the one-dimension linear data structure with multilayer tree-shaped data structure. And thus the nesting and dependence relationships between information object and data elements are much clearer and it is more convenient and easy to browse DICOM image files.