This study aimed to investigate the influence of combinating Huangqi with Fuzi on the pharmacokinetics of six Aconitum alkaloids, i.e. aconitine (AC), hypaconitine (HA), mesaconitine (MA), benzoylaconine (BAC), benzoylhypaconine (BHA) and benzoylmesaconine (BMA). The plasma concentrations of the drugs were determined by LC-MS for dose response and time dependent curves. The pharmacokinetic parameters were calculated by DAS 3.3, and SPSS 12.0 was used to analyze the differences of main pharmacokinetic parameters between the two groups. Comparing with Fuzi group, the AUC_0-t and AUC_0-∞ of six alkaloids in Fuzi-Huangqi group was significantly decreased, the CL_z/Fof six alkaloids except HA was significantly increased; the C_max was decreased and the t_max was prolonged in 3 monoester alkaloids, and the apparent volume of distribution of BMA and MA (V_z/F) increases. These data indicated that Huangqi can inhibit the absorption of aconite alkaloids, induce the distribution of aconite alkaloids to the whole body, and accelerate the elimination of aconite alkaloids. The animal experiment scheme in this study has been approved by the Experimental Animal Ethics Committee of Jiangxi University of Traditional Chinese Medicine.

OBJECTIVE: To investigate the relationship of the function and gene polymorphism of insulin receptor substrate (IRS) with type 2 diabetes mellitus (T2DM), and to provide a new perspective for T2DM drug development. METHODS: Relevant literatures included in CNKI, Wanfang, VIP, PubMed, SpringerLink and other databases from Jan. 1991 to Nov. 2017 were retrieved by using "Insulin receptor substrate" "Type 2 diabetes" "Insulin resistance" "Polymorphism" as Chinese keywords, and "Insulin receptor substrate" "IRS" "Type 2 diabetes" "Insulin resistance" "Polymorphism" as English keywords. The relationship of the function and gene polymorphism of IRS family with T2DM was reviewed. RESULTS & CONCLUSIONS: A total of 328 literatures were retrieved, of which there were 38 valid literatures. At present, IRS family has six members (IRS-1 to IRS-6). The dysfunction of IRS-1 and IRS-2 will lead to insulin resistance and induce T2DM. The relationship of IRS-3 and IRS-4 with T2DM remains controversial. IRS-5 and IRS-6 were newly found and their functions are not clear. The Gly972Arg mutation of IRS-1 is positively correlated with the pathogenesis of T2DM. Gly1057Asp mutation of IRS-2 combined with obesity can induce insulin resistance, but there is controversy. The mutation types of IRS family other members include Ala94Thr, Ala512Pro and Ser892Gly mutation of IRS-1, ACC, Ala157Thr and Leu647Val mutation of IRS-2. The relationship between these types of mutation and T2DM has not yet been fully supported. Multiracial and large-scale studies are required. Some achievements have been made in the present study, but the study is not yet comprehensive. Relationship of IRS family members and their mutation sites with T2DM still needs to be further tested in the expanded population.

The purpose of this study was to investigate the effect of key physical properties of hawthorn leaf granule on its dissolution behavior. Hawthorn leaves extract was utilized as a model drug. The extract was mixed with microcrystalline cellulose or starch with the same ratio by using different methods. Appropriate amount of lubricant and disintegrating agent was added into part of the mixed powder, and then the granules were prepared by using extrusion granulation and high shear granulation. The granules dissolution behavior was evaluated by using equilibrium dissolution quantity and dissolution rate constant of the hypericin as the indicators. Then the effect of physical properties on dissolution behavior was analyzed through the stepwise regression analysis method. The equilibrium dissolution quantity of hypericin and adsorption heat constant in hawthorn leaves were positively correlated with the monolayer adsorption capacity and negatively correlated with the moisture absorption rate constant. The dissolution rate constants were decreased with the increase of Hausner rate, monolayer adsorption capacity and adsorption heat constant, and were increased with the increase of Carr index and specific surface area. Adsorption heat constant, monolayer adsorption capacity, moisture absorption rate constant, Carr index and specific surface area were the key physical properties of hawthorn leaf granule to affect its dissolution behavior.

Objective To observe the expression of NOD-like receptor pyrin domain-3 (NLRP3) inflammasome and interleukin-1 beta (IL-1b) in pterygium and normal conjunctiva specimens,and clarify the role of NLRP3 in the development of pterygium.Methods Specimens from 20 cases of pterygium and 6 cases of normal eonjunctival were analyzed for establishing the expression of NLRP3 and IL-1b by immune-histochemistry.The level of caspase-1 and pro-caspase-1 protein were analyzed by Westernblot,gene expression of interleukin-18 (IL-18) was detected by RT-PCR.Results NLRP3 was not expressed in normal conjunctival epithelial cells,but was positive in the basal part of pterygium;IL-1was not expressed in normal conjunctival tissues,but was positive in pterygium.There was no significant difference about the expression of Procaspase-1 in normal conjunctiva and pterygium (P ＞ 0.05),However,caspase-1,also known as the active form of pro-caspase-1 expressed in pterygiun was higher than that in normal conjunctiva(P ＜ 0.05).The average level of IL-18 in 20 cases of pterygium was significantly higher than that in normal conjunctiva (P ＜ 0.05).Conclusion After NLRP3 signaling pathway activating in pterygium tissue,caspase-1,IL-1β and IL-18 are high expression abnormally,suggest that NLRP3 inflammasome and the related signaling pathways may play a role in the progression of pterygium.

To study the improvement of powder flowability and hygroscopicity of traditional Chinese medicine extract by surface coating modification technology. The 1% hydrophobic silica nanoparticles were used as surface modifier, and andrographis extract powder was taken as a model drug. Three different techniques were used for coating model drugs, with angle of repose, compressibility, flat angle and cohesion as the comprehensive evaluation indexes for the powder flowability. The powder particle size and the size distribution were measured by Mastersizer 2000. FEI scanning electron microscope was used to observe the surface morphology and structure of the powder. The percentage of Si element on the powder surface was measured by energy dispersive spectrometer. The hygroscopicity of powder was determined by Chinese pharmacopoeia method. All of the three techniques can improve the flowability of powder extract. In particular, hygroscopicity of extract powder can also be improved by dispersion and then high-speed mixing, which can produce a higher percentage of Si element on the powder surface. The improvement principle may be correlated with a modifier adhered to the powder surface.

Objective To observe the relationship between injury of corticospinal cord tract (CST) in basal ganglia and upper limb func-tion after stroke using diffusion tensor imaging (DTI). Methods 18 stroke inpatients hospitalized from January, 2013 to July, 2015 accepted DTI, and their upper limb function was evaluated with simple Fugl-Meyer Assessment and Japan Upper Limb Function Test. The fractional anisotropy (FA) of CST in basal ganglia of affected and unaffected sides were compared, and the correlation between FA of affected CST and upper limb motor function were analyzed. Results The FA was significantly less in the affected CST than in the unaffected CST (t=-21.09, P<0.001). The FA of the affected CST correlated with the scores of simple Fugl-Meyer Assessment (r=0.570, P<0.05) and Japan Upper Limb Function Test (r=0.509, P<0.05). Conclusion CST is injured after stroke, which may related to the upper limbs motor function impairment.