Optimization of cellulase-assisted extraction process and antioxidant activities of polysaccharides from Tricholoma mongolicum Imai.

BACKGROUND: Tricholoma mongolicum Imai is a well-known edible and medicinal mushroom which in recent years has attracted increasing attention because of its bioactivities. In this study, water-soluble polysaccharides were extracted from T. mongolicum Imai by cellulase-assisted extraction and their antioxidant activities were investigated. RESULTS: In order to improve the yield of polysaccharides, four variables, cellulase amount (X1 ), pH (X2 ), temperature (X3 ) and extraction time (X4 ), were investigated with a Box-Behnken design. The optimal conditions were predicted to be cellulase amount of 20 g kg(-1) , pH of 4.0, temperature of 50 °C and extraction time of 127 min, with a predicted polysaccharide yield of 190.1 g kg(-1) . The actual yield of polysaccharides under these conditions was 189.6 g kg(-1) , which matched the predicted value well. The crude polysaccharides were purified to obtain four fractions, and characterization of each was carried out. In addition, antioxidant properties of four polysaccharides assessed by 1,1-diphenyl-2-picryldydrazyl (DPPH) and hydroxyl radical-scavenging assays indicated that polysaccharides from T. mongolicum Imai (TMIPs) possessed antioxidant activity in a dose-dependent manner. CONCLUSION: TMIPs show moderate antioxidant activities in vitro. Therefore it is suggested that TMIPs are potential natural antioxidants for use in functional foods. © 2016 Society of Chemical Industry.

Inhibition of UDP-Glucuronosyltransferases (UGTs) Activity by constituents of Schisandra chinensis.

Structure-activity relationship for the inhibition of Schisandra chinensis's ingredients toward (Uridine-Diphosphate) UDP-glucuronosyltransferases (UGTs) activity was performed in the present study. In vitro incubation system was employed to screen the inhibition capability of S. chinensis's ingredients, and in silico molecular docking method was carried out to explain possible mechanisms. At 100 µM of compounds, the activity of UGTs was inhibited by less than 90% by schisandrol A, schisandrol B, schisandrin, schisandrin C, schisantherin A, gomisin D, and gomisin G. Schisandrin A exerted strong inhibition toward UGT1A1 and UGT1A3, with the residual activity to be 7.9% and 0% of control activity. Schisanhenol exhibited strong inhibition toward UGT2B7, with the residual activity to be 7.9% of control activity. Gomisin J of 100 µM inhibited 91.8% and 93.1% of activity of UGT1A1 and UGT1A9, respectively. Molecular docking prediction indicated different hydrogen bonds interaction resulted in the different inhibition potential induced by subtle structure alteration among schisandrin A, schisandrin, and schisandrin C toward UGT1A1 and UGT1A3: schisandrin A > schisandrin > schisandrin C. The detailed inhibition kinetic evaluation showed the strong inhibition of gomisin J toward UGT1A9 with the inhibition kinetic parameter (Ki ) to be 0.7 µM. Based on the concentrations of gomisin J in the plasma of the rats given with S. chinensis, high herb-drug interaction existed between S. chinensis and drugs mainly undergoing UGT1A9-mediated metabolism. In conclusion, in silico-in vitro method was used to give the inhibition information and possible inhibition mechanism for S. chinensis's components toward UGTs, which guide the clinical application of S. chinensis.

Correlation between Antistress and Hepatoprotective Effects of Schisandra Lignans Was Related with Its Antioxidative Actions in Liver Cells.

The present study was conducted to investigate the relationship between the anti-stress and hepato-protective effects of Schisandra Lignans Extract (SLE) on stress-induced liver damage. Seven weeks old male mice were fixed in a restraint tube for 18 h to induce liver damage. SLE was orally administered to animals for 5 days at dosages of 100 and 200 mg/kg/day before exposed to restraint stress. Oral administration of SLE significantly reduced restraint-induced liver damage in experimental animal. SLE was further found to significantly alleviate the provocation of corticosterone in stressed mice. SLE also significantly decreased oxidative damage and increased anti-oxidative capability of liver cells by preventing the over production and accumulation of free radicals. In conclusion, the protective effects of SLE on stress-induced liver damage were confirmed, and the correlation between hepatoprotective and anti-stress effects of schisandra lignans was possible related to its alleviation on the malignant effects of stressors for bio-homeostasis, such as balance of oxidation and reduction in cells.

[Arnebia root oil promotes histological change and up-regulates bFGF and it's mRNA expression in the raw surface of the rabbits].

OBJECTIVE: To explore the molecular biological mechanism of arnebia root oil in promoting wound surface healing by observing histological change and basic fibroblast growth factor(bFGF) mRNA expression in the wound surface tissues of 2 groups, as well as the wound surface healing rate. METHOD: Experimental model of incised-wound was produced on the back of 18 New Zealand albino rabbits. The wound surfaces were randomly divided into two groups, namely, experimental group and control group. The wound surfaces in the experimental group were treated by arnebia root oil and those in control group were treated by petrolatum gauze. Then raw surfaces were evaluated by the techniques of histology, histochemistry and electron microscope and the healing rates of the raw surfaces were compared between the two groups. Content of bFGF and it's mRNA expression in wound surface tissue was also measured by means of Western-blot and RT-PCR. RESULT: The wound surface healing rate in experimental group was higher than that in control group( P < 0.05). The fibroblast, collagen and blood capillaries were comparatively richer in experimental group as compared with those in control group, and similarly, the expression of bFGF mRNA was also significantly enhanced in the experimental group as compared with control group during the various periods of treatment. In addition, the changes in the expressions of bFGF and it's mRNA paralleled the changes of healing rates in the two groups. CONCLUSION: the present results showed that amebia root oil significantly can promote the healing of raw surfaces, which may be mediated by up-regulation of bFGF expression.

[Arnebia root oil promotes wound healing and expression of basic fibroblast growth factor on the wound surface in rabbits].

OBJECTIVE: To observe the promoting effect of arnebia root oils on expression of basic fibroblast growth factor (bFGF) in skin wound of rabbits and the histomorphological changes in the wound surface, and to discuss its mechanism. METHODS: Bilateral round skin wounds were made on the back of 15 rabbits. The three wounds on one side of the back of each rabbit were treated with arnebia root oils, while the three wounds on the other side were treated with vaseline in order to promote the wound healing. The histomorphology and ultrastructure under electron microscopy of the wounds, and the rate of wound healing were examined at different time. Western blotting assay was used to detect the expression of bFGF in the wound surface. RESULTS: The healing rate of the arnebia root oils-treated wounds was evidently higher than that of the vaseline-treated wounds (P<0.05). The quantities of fibroblast, collagen and capillary in the arnebia root oils-treated wounds were much more than those in the vaseline-treated wounds, and the expression of endogenous bFGF in the arnebia root oils-treated wounds was enhanced obviously as compared with that in the vaseline-treated wounds in different period of wound healing. There existed a parallel correlation between the expression level of bFGF and the rate of wound healing. CONCLUSION: The promoting effect of arnebia root oils on wound healing may be related to increasing the expression level of basic fibroblast growth factor in the skin wound.

Comprehensive treatment for old patients with hip fractures.

OBJECTIVE: To observe the effect of comprehensive treatment for hip fracture in old people. METHODS: Three hundred and seventy-two old patients with hip fractures were randomly divided into two groups, Group A and Group B. Cases in Group A were treated only by operations. Cases in Group B received comprehensive treatment. The Singh Indexes of both uninjured and injured femoral necks were used to judge the osteoporosis levels before operation and one year after the operation. The function of injured hip joints was evaluated one year postoperatively. RESULTS: Complications occurred in 36.56% of the cases in Group A and 5.91% of Group B. One year postoperatively, the Singh Index degree distributions of both uninjured and injured femoral necks in Group A had no significant difference compared with those before the operation (P>0.05). In Group B, there was significant difference between one year postoperatively and before operation, and the Singh Index one year after the operation showed better result than that before operation (P<0.05). One year after operation, there was significant difference in the function of injured hip joints between Group A and Group B (P<0.05). CONCLUSIONS: Hip fracture in old people should be treated comprehensively according to its internal characteristics, osteoporosis.

Alkaloids from Lycoris aurea and their cytotoxicities against the head and neck squamous cell carcinoma.

Phytochemical investigation of the 80% EtOH extract of the bulbs of Lycoris aurea led to the isolation of six new alkaloids, 2-demethyl-isocorydione (1), 8-demethyl-dehydrocrebanine (2), 1-hydroxy-anhydrolycorin-7-one (3), (+)-1,2-dihydroxy-anhydrolycorine N-oxide (4), 5,6-dihydro-5-methyl-2-hydroxyphenanthridine (5), and (+)-8-hydroxy-homolycorine-α-N-oxide (6), and together with two known compounds, isocorydione (7) and anhydrolycorin-7-one (8). Structural elucidation of all the compounds was performed by spectral methods such as 1D and 2D ((1)H-(1)H COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. All the alkaloids were in vitro evaluated for their cytotoxic activities against seven tumor cell lines of the head and neck squamous cell carcinoma and anti-inflammatory activities. Compounds 1, 2, 6, and 7 exhibited significant cytotoxicities against all the tested cell lines. Moreover, alkaloids 1, 2, and 7 possessed selective inhibition of Cox-2 (>85%).

Glucuronidation of the broad-spectrum antiviral drug arbidol by UGT isoforms.

OBJECTIVES: The aim of this work was to identify the uridine glucuronosyltransferase (UGT) isoforms involved in the metabolism of the broad-spectrum antiviral drug arbidol. METHODS: A human liver microsome (HLM) incubation system was employed to catalyse the formation of arbidol glucuronide. The glucuronidation activity of commercially recombinant UGT isoforms towards arbidol was screened. A combination of kinetic analysis and chemical inhibition study was used to determine the UGT isoforms involved in arbidol's glucuronidation. KEY FINDINGS: The arbidol glucuronide was detected when arbidol was incubated with HLMs in the presence of UDP-glucuronic acid. The Eadie-Hofstee plot showed that glucuronidation of arbidol was best fit to the Michaelis-Menten kinetic model, and K(m) and apparent V(max) were calculated to be 8.0 ± 0.7 µm and 2.03 ± 0.05 nmol/min/mg protein, respectively. Assessment of a panel of recombinant UGT isoforms revealed that UGT1A1, UGT1A3 and UGT1A9 could catalyse the glucuronidation of arbidol. Kinetic analysis and chemical inhibition study demonstrated that UGT1A9 was the predominant UGT isoform involved in arbidol glucuronidation in HLMs. CONCLUSIONS: The major contribution of UGT1A9 towards arbidol glucuronidation was demonstrated in this study.

Inhibition of CYP3A4 and CYP2C9 by podophyllotoxin: implication for clinical drug-drug interactions.

Podophyllotoxin (PPT) and its derivatives exert significant anti-cancer activities, and one derivative etoposide is often utilized to treat various cancers in the clinic. The aim of the present study is to investigate the inhibitory effects of PPT on major cytochrome P450 (CYP) isoforms in human livers. Inhibition of CYP3A4, CYP2C9, CYP2C8, CYP2D6, CYP2E1 and CYP2A6 by PPT was investigated in the human liver microsomal system. Time-dependent inhibition of CYP3A4 by PPT was also evaluated. The results showed that PPT strongly exhibited inhibitory effects on CYP3A4 and CYP2C9 in a concentration-dependent manner. Half inhibition concentration (IC50) was 1.1 +/- 0.3 and 4.6 +/- 0.3 meu M for CYP3A4 and CYP2C9, respectively. Inhibition kinetic analysis showed that PPT exhibited competitive inhibition towards CYP3A4 and CYP2C9 with Ki of 1.6 and 2.0 meu M, respectively. Additionally, PPT exerted time-dependent inhibition towards CYP3A4 and the kinetic parameters were 4.4+/- 2.1 meu M and 0.06 +/- 0.01 min-1 for KI and kinact, respectively. Our experimental data indicate that potential drug-drug interaction (DDI) might exist when PPT is co-administered with the substrates which mainly undergo CYP3A4- or CYP2C9-mediated metabolism.

[Treatment of lumbar spondylolisthesis with AF device fixation system and PROSPACE interbody fusion cage].

OBJECTIVE: To discuss the clinical effect and the application of AF device fixation system and PROSPACE interbody fusion cage on treating lumbar spondylolisthesis. METHODS: Twenty-one cases of lumbar spondylolisthesis treated by operation from 1999 to 2002 were analyzed retrospectively (13 males and 8 females, 25-66 years old averaging 42 years). We had thorough decompression on the part of nerve compression and had replacement and fixation of the slippage vertebral body with the AF transpedicular screw/rod system so that the normal spine physiological curvature could be recovered, and then performed the posterolateral interbody fusion with implanting the PROSPACE filled with autograft bones. RESULTS: All the patients were followed up for 3 months to 3 years with an average of 15 months. The preoperation symptoms improved in 20 cases (95.2%). CONCLUSION: The combination of AF device fixation system and PROSPACE interbody fusion cage can relieve effectively nerve compression, recover the normal spinal physiological curvature, maintain the height of interbody and promote the nerve fusion. It is reliable and effective in the treatment of spondylolisthesis.

[Selection of the type in revision total hip replacement for failed hip arthroplasty].

OBJECTIVE: To evaluate the selection of the type of prosthesis in revision hip arthroplasty. METHODS: There were 33 hips in our study, male in 7 hips and female in 26 hips. The average age of the patients were 59 years. The reasons of the revision included aseptic loosing in 22 hips, infection in 8 hips (2 infection hips with discharging sinuses), and acetabular erosion in 3 hips. The operations for revision were 13 cemented and 12 cementless acetabular prosthesis with autograft in morselized form; the femoral revision were all selected in cemented prosthesis. The revision for infection hip were all cemented prosthesis of extensively porouse-coated. RESULTS: The average follow-up duartion was 3.9 years and 11 months. There was a radiolucency but no clinical instability accompanied in 2 hips and remaining moderate pain in 4 hips. No dislocation and fracture were seen in the series. Harris score were improved to 82.4 (68-88). CONCLUSION: The commonest reason of revision hip arthroplasty was aseptic loosing. The acetabular prosthesis in revision could select cemented or cementless components and femoral prosthesis could select extensively coated stem. The cemented components could yield good results in infection hips revision.