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OBJECTIVE To study the metabolites of four diterpenoids of Euphorbia fischeriana in liver microsomes of rats and to investigate its metabolic regularity. METHODS In vitro incubation system of liver microsomes of rats was built. The jolkinolide A，jolkinolide B ，17-hydroxyl jolkinolide A and 17-hydroxyl jolkinolide B were added into incubation system of liver microsomes in rats activated by reduced nicotinamide adenine dinucleotide phosphate ，incubated at 37 ℃ for 30 min，and then terminated the reaction with acetonitrile. Taking the negative group （adding acetonitrile firstly and then starting incubation for 30 min）as the reference，the ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry was used ；Anaylyst®TF 1.7.1、PeakView® 2.2，MetabolitePilot 1.5 and MasterView 1.2 software were used to speculate and identify the fragmentation law of mass spectrometry and metabolites. RESULTS Four diterpenoids were easy to lose neutral fragments such as H 2O and CO in secondary mass spectrometry. Jolkinolide A and 17-hydroxyl jolkinolide A showed similar metabolism pathway ，including dihydroxylation，dehydrogenation，and monohydroxylation ；six and five metabolites were identified respectively. Jolkinolide B and 17-hydroxyl jolkinolide B showed similar metabolism pathway ，including monohydroxylation ，hydration and isomerization. Five metabolites were identified. CONCLUSIONS Both jolkinolide A and 17-hydroxyl jolkinolide A produce the metabolites of hydroxylation and dehydrogenation in liver microsomes of rats ；both jolkinolide B and 17-hydroxyl jolkinolide B produce the metabolites of hydroxylation ，hydration and isomerization in liver microsomes of rats. The metabolites of four diterpenoids are phase Ⅰ metabolites.
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Objective@#To compare the biomechanical performance between the single- versus double-threaded cannulated screws in the treatment of femoral neck fractures of Pauwels type Ⅲ.@*Methods@#Models of femoral neck fracture of Pauwels type Ⅲ (70°) were made of the Sawbone synthetic composite femurs. All specimens were divided into 2 groups (n=12). Group A was fixated with single-threaded cannulated screws and group B with double-threaded cannulated screws, both in an inverted triangle configuration. The screws ranged from 90 to 95 mm in length and from 7.3 to 7.5 mm in diameter. All the specimens were subjected to axial stiffness and failure load tests with 7° valgus (simulating normal two-legged weight-bearing stance) and 25° valgus (simulating normal one-legged weight-bearing stance) and torsion test as well. The 2 groups were compared in the torques at axial stiffness angles of 1°, 2°, 3°, 5° and 7°.@*Results@#Group B had significantly greater axial stiffness at 7° valgus and 25° valgus (89±26 N/mm and 128±37 N/mm) and failure load (1,154±368 N) than group A did (36±12 N/mm and 47±16 N/mm; 688±94 N) (P< 0.05). The torques increased with the increase in rotation angle in both groups. However, the torques in group B (3.26±0.96, 4.16±1.23, 4.64±1.13, 5.59±1.26 and 6.53±1.47 N·m) were all significantly larger than in group A (1.44±0.19, 2.03±0.41, 2.33±0.62, 2.74±0.87 and 3.05±1.07 N·m) (P<0.05).@*Conclusion@#Double-threaded cannulated screws may provide better biomechanical stability than single-threaded ones, due to their substantial improvement in anti-compression and anti-rotation performance.
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Objective To compare the biomechanical performance between the single-versus double-threaded cannulated screws in the treatment of femoral neck fractures of Pauwels type Ⅲ.Methods Models of femoral neck fracture of Pauwels type Ⅲ (70°) were made of the Sawbone synthetic composite femurs.All specimens were divided into 2 groups (n =12).Group A was fixated with single-threaded cannulated screws and group B with double-threaded cannulated screws,both in an inverted triangle configuration.The screws ranged from 90 to 95 mm in length and from 7.3 to 7.5 mm in diameter.All the specimens were subjected to axial stiffness and failure load tests with 7° valgus (simulating normal two-legged weight-bearing stance) and 25° valgus (simulating normal one-legged weight-bearing stance) and torsion test as well.The 2 groups were compared in the torques at axial stiffness angles of 1°,2°,3°,5° and 7°.Results Group B had significantly greater axial stiffness at 7° valgus and 25° valgus (89 ± 26 N/mm and 128 ± 37 N/mm) and failure load (1,154 ±368 N) than groupAdid (36 ±12 N/mm and 47 ±16 N/mm;688 ±94 N) (P ＜0.05).The torques increased with the increase in rotation angle in both groups.However,the torques in groupB (3.26±0.96,4.16±1.23,4.64±1.13,5.59±l.26and6.53±l.47 N·m) were all significantly larger than in group A (1.44 ±0.19,2.03 ±0.41,2.33 ±0.62,2.74 ±0.87 and 3.05 ± 1.07 N · m)(P ＜ 0.05).Conclusion Double-threaded cannulated screws may provide better biomechanical stability than single-threaded ones,due to their substantial improvement in anti-compression and anti-rotation performance.
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OBJECTIVE： To analyze the metabolites of jolkinolide B in rats， and predict its metabolism pathway. METHODS： The rats were randomly divided into blank group （0.5％ CMC-Na， ig） and administration group （jolkinolide B， ig， 100 mg/kg）， with 8 rats in each group. The fecal samples were collected at ＞0-12， ＞12-24， ＞24-36 hours after administration； the urine samples were collected at ＞0-2， ＞2-8， ＞8-12， ＞12-24， ＞24-36， ＞36-48 hours after administration； the blood samples were collected at 1， 2， 8， 12， 24， 36 hours after administration. UPLC-Q-TOF/MS combined with Analyst® TF 1.7.1 and PeakView® 2.2 software were used to analyze and identify the metabolites in the samples after treated with ultrasonic extraction， solid phase extraction and protein precipitation. RESULTS & CONCLUSIONS： Prototype drugs and seven metabolites were detected in rat’s fecal samples， and one or two metabolites were detected in urine and blood samples， respectively. After intragastric administration， the metabolism of jolkinolide B in rats is mainly through ring opening， oxidation， dehydration， deoxygenation and hydrogenation of phase Ⅰ， but no phase Ⅱ metabolites were detected.
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<p><b>OBJECTIVE</b>To develop an UPLC method of determining the characteristic chromatographic profiles of Moutan Cortex for quality control of the medicine.</p><p><b>METHOD</b>The UPLC characteristic chromatographic profiles of fifteen batches of Moutan Cortex were determined on an HSS T3 column (2.1 mm x 100 mm, 1.8 microm) eluted with the mobile phase consisted of water containing 0.05% phosphoric acid and acetonitrile in gradient mode and the detection wavelength was set at 254 nm.</p><p><b>RESULT</b>The common mode of the UPLC characteristic chromatographic profile was set up under the established condition. There were 20 common peaks in the characteristic chromatographic profile of fifteen samples, ten of which were identified, and the similar degrees of the fifteen batches to the common mode were between 0.973-0.998.</p><p><b>CONCLUSION</b>The method was fast and accurate. The characteristic chromatographic profile of Moutan Cortex with high specificity can be used to control the quality of Moutan Cortex.</p>