Visible light-induced metal-free cascade denitrogenative borylation and iodination of nitroarenes.

An efficient method was developed for the one-pot construction of C-B and C-I via visible light-induced transformation of nitroarenes. This protocol relies on the photochemical properties of nitroarenes under visible light, followed by reduction with B2pin2 and diazotization with tBuONO. An array of arylboronates and iodobenzenes were constructed smoothly after excitation with purple LEDs at room temperature. In addition, the synthetic utility of this method was further demonstrated in the late-stage modification of a drug molecule. The advantages of this strategy include metal-free system, mild reaction conditions and acceptable substrate scope.

Enzymatic activity of 38 CYP2C9 genotypes on ibuprofen.

BACKGROUND AND OBJECTIVE: Ibuprofen, a common non-steroidal anti-inflammatory drug, is used clinically for pain relief and antipyretic treatment worldwide. However, regular or long-term use of ibuprofen may lead to a series of adverse reactions, including gastrointestinal bleeding, hypertension and kidney injury. Previous studies have shown that CYP2C9 gene polymorphism plays an important role in the elimination of various drugs, which leads to the variation in drug efficacy. This study aimed to evaluate the effect of 38 CYP2C9 genotypes on ibuprofen metabolism. METHODS: Thirty-eight recombinant human CYP2C9 microsomal enzymes were obtained using a frugiperda 21 insect expression system according to a previously described method. Assessment of the catalytic function of these variants was completed via a mature incubation system: 5 pmol CYP2C9*1 and 38 CYP2C9 variants recombinant human microsomes, 5 µL cytochrome B5, ibuprofen (5-1000 µM), and Tris-HCl buffer (pH 7.4). The ibuprofen metabolite contents were determined using HPLC analysis. HPLC analysis included a UV detector, Plus-C18 column, and mobile phase [50% acetonitrile and 50% water (containing 0.05% trifluoroacetic acid)]. The kinetic parameters of the CYP2C9 genotypes were obtained by Michaelis-Menten curve fitting. RESULTS: The intrinsic clearance (CLint) of eight variants was not significantly different from CYP2C9*1; four CYP2C9 variants (CYP2C9*38, *44, *53 and *59) showed significantly higher CLint (increase by 35%-230%) than that of the wild-type; the remaining twenty-six variants exhibited significantly reduced CLint (reduced by 30%-99%) compared to that of the wild-type. CONCLUSION: This is the first systematic evaluation of the catalytic characteristics of 38 CYP2C9 genotypes involved ibuprofen metabolism. Our results provide a corresponding supplement to studies on CYP2C9 gene polymorphisms and kinetic characteristics of different variants. We need to focus on poor metabolizers (PMs) with severely abnormal metabolic functions, because they are more susceptible to drug exposure.

Bis (2-butoxyethyl) Phthalate Delays Puberty Onset by Increasing Oxidative Stress and Apoptosis in Leydig Cells in Rats.

Objective: This study investigated the effects of bis (2-butoxyethyl) phthalate (BBOP) on the onset of male puberty by affecting Leydig cell development in rats. Methods: Thirty 35-day-old male Sprague-Dawley rats were randomly allocated to five groups mg/kg bw per day that were gavaged for 21 days with BBOP at 0, 10, 100, 250, or 500 mg/kg bw per day. The hormone profiles; Leydig cell morphological metrics; mRNA and protein levels; oxidative stress; and AKT, mTOR, ERK1/2, and GSK3ß pathways were assessed. Results: BBOP at 250 and/or 500 mg/kg bw per day decreased serum testosterone, luteinizing hormone, and follicle-stimulating hormone levels mg/kg bw per day (P < 0.05). BBOP at 500 mg/kg bw per day decreased Leydig cell number mg/kg bw per day and downregulated Cyp11a1, Insl3, Hsd11b1, and Dhh in the testes, and Lhb and Fshb mRNAs in the pituitary gland (P < 0.05). The malondialdehyde content in the testis significantly increased, while Sod1 and Sod2 mRNAs were markedly down-regulated, by BBOP treatment at 250-500 mg/kg bw per day (P < 0.05). Furthermore, BBOP at 500 mg/kg bw per day decreased AKT1/AKT2, mTOR, and ERK1/2 phosphorylation, and GSK3ß and SIRT1 levels mg/kg bw per day (P < 0.05). Finally, BBOP at 100 or 500 µmol/L induced ROS and apoptosis in Leydig cells after 24 h of treatment in vitro (P < 0.05). Conclusion: BBOP delays puberty onset by increasing oxidative stress and apoptosis in Leydig cells in rats.The graphical abstract is available on the website www.besjournal.com.

[Penile cancer with perineural invasion is more prone to postoperative recurrence].

OBJECTIVE: To explore the correlation between perineural invasion and postoperative recurrence in patients surgically treated for penile cancer. METHODS: We conducted a retrospective analysis of the clinical data on 18 penile cancer patients surgically treated in our hospital from January 2018 to December 2021, 8 with postoperative recurrence (the recurrence group) and the other 10 without (the non-recurrence control group). We compared the two groups of patients in the age of onset, tumor-node-metastasis (TNM) stages, American Joint Committee on Cancer (AJCC) prognosis stages, surgical methods, perineural invasion and recurrence time. We analyzed the differences in postoperative recurrence using the Kaplan Meier plotted survival curve and in independent risk factors in predicting postoperative recurrence using the ROC curve. RESULTS: Compared with the non-recurrence controls, the patients in the recurrence group had a significantly older age of onset (P=0.0411) and severer perineural invasion (P<0.001), and those with perineural invasion had a shorter recurrence time (P<0.001), which was an independent risk factor for postoperative recurrence. The areas under the ROC curves for perineural invasion and age were 0.885 and 0.213, respectively. CONCLUSION: Penile cancer with perineural invasion is more prone to and perineural invasion is an independent risk factor for postoperative recurrence of the malignancy.

A Strong Correlation Between the Severity of Flatfoot and Symptoms of Knee Osteoarthritis in 95 Patients.

Objective: The purpose of this study is to assess the association between the presence and severity of flatfoot and symptoms of knee OA. Methods: 95 participants with knee OA were recruited from a patient cohort at a regional hospital. Symptoms of knee OA, including knee degeneration, femorotibial alignment, pain, stiffness and dysfunction were assessed using the Kellgren-Lawrence (K-L) grading system, femoral-tibial angle (FTA), and Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC). Participants were divided into groups with flatfoot (mild, moderate and severe) and without flatfoot based on the Clarke's angle. Linear regression and ordinal logistic regression were used for statistical analysis, as appropriate. Results: Having flatfoot was associated with a significantly increased risk of having a higher K-L grade (OR: 20.03; 95% CI, 5.88, 68.27; p < 0.001), smaller FTA (Beta: -2.96; 95% CI, -4.41, -1.50; p < 0.001), higher pain score (Beta: 0.47; 95% CI, 0.24, 0.69; p < 0.001) and greater loss of function (Beta: 0.25; 95% CI, 0.02, 0.48; p = 0.03). Severe grades of flat feet were associated with a higher K-L grade (OR: 0.19; 95% CI, 0.08, 0.44; p < 0.001), smaller FTA (Beta: 1.51; 95% CI, 0.66, 2.35; p = 0.001), higher pain score (Beta: -0.25; 95% CI, -0.39, -0.11; p = 0.001), greater stiffness (Beta: -0.24; 95% CI, -0.38, -0.09; p = 0.002) and greater loss of function (Beta: -0.27; 95% CI, -0.41, -0.14; p < 0.001). Conclusion: The results indicated that the severity of flattening is significantly associated with symptoms of knee OA. For the conservative management of knee OA, both flatfoot and its severity should be carefully considered.

Data Mining and Systems Pharmacology to Elucidate Effectiveness and Mechanisms of Chinese Medicine in Treating Primary Liver Cancer.

OBJECTIVE: To identify specific Chinese medicines (CM) that may benefit patients with primary liver cancer (PLC), and to explore the mechanism of action of these medicines. METHODS: In this retrospective, singlecenter study, prescription information from PLC patients was used in combination with Traditional Chinese Medicine Inheritance Supports System to identify the specific core drugs. A system pharmacology approach was employed to explore the mechanism of action of these medicines. RESULTS: Taking CM more than 6 months was significantly associated with improved survival outcomes. In total, 77 putative targets and 116 bioactive ingredients of the core drugs were identified and included in the analysis (P<0.05). A total of 1,036 gene ontology terms were found to be enriched in PLC. A total of 75 pathways identified from Kyoto Encyclopedia of Genes and Genomes were also enriched in this disease, including fluid shear stress, interleukin-17 signaling, signaling between advanced glycan end products and their receptors, cellular senescence, tumor necrosis factor signaling, p53 signaling, cell cycle signaling, steroid hormone biosynthesis, T-helper 17 cell differentiation, and metabolism of xenobiotics by cytochrome. Docking studies suggested that the ingredients in the core drugs exert therapeutic effects in PLC by modulating c-Jun and interleukin-6. CONCLUSIONS: Receiving CM for 6 months or more improves survival for the patients with PLC. The core drugs that really benefit for PLC patients likely regulates the tumor microenvironment and tumor itself.

Nimodipine Improves Cognitive Impairment After Subarachnoid Hemorrhage in Rats Through IncRNA NEAT1/miR-27a/MAPT Axis.

BACKGROUND: Subarachnoid hemorrhage (SAH) is a cerebral hemorrhage disease that severely damages the brain and causes cognitive impairment (CI). Therefore, accurate and appropriate treatment strategies are urgently needed. The application of nimodipine can not only improve blood circulation in patients with SAH but also repair ischemic neuron injury. PURPOSE: To investigate the effects of nimodipine and lncRNA nuclear paraspeckle assembly transcript 1 (NEAT1)/miR-27a/microtubule-associated protein tau (MAPT) axis on CI after SAH. METHODS: One hundred and twenty healthy male rats were selected and equally divided into control group, sham operation group, model group, PBS group, nimodipine group (drug group), NC siRNA group, NC mimics group, NEAT1 siRNA, miR-27a mimics, MAPT siRNA, drug + NEAT1-ad, and drug + NC-ad groups by random number table. Rats in the model group were constructed by double-hemorrhage model, and expression vectors were injected into the tail to regulate the expression of lncRNA NEAT1, miR-27a and MAPT. In addition, Western blot was employed to detect brain tissue protein, flow cytometry was applied to measure brain tissue apoptosis, and MTT was utilized to determine cell activity, so as to evaluate brain damage and cognitive function in each group. RESULTS: Nimodipine, down-regulated lncRNA NEAT1, up-regulated miR-27a and down-regulated MAPT all improved brain damage and CI, inhibited brain tissue cell apoptosis, and enhanced brain cell activity. The common binding sites of lncRNA NEAT1 and MAPT were found on the miR-27a sequence fragment, and miR-27a could be paired with the former two. Nimodipine was found to cause the down-regulation of lncRNA NEAT1 and MAPT, as well as the up-regulation of miR-27a. CONCLUSION: Nimodipine can improve CI after SAH in rats through the lncRNA NEAT1/miR-27a/MAPT axis.

Comparative analysis of the biomechanics of the adjacent segments after minimally invasive cervical surgeries versus anterior cervical discectomy and fusion: A finite element study.

PURPOSE: Percutaneous full-endoscopic anterior cervical discectomy (PEACD) and posterior cervical foraminotomy (PCF) as alternatives to anterior cervical discectomy and fusion (ACDF) are extensively used in the treatment of patients with cervical spondylotic radiculopathy. The possibility of avoiding the risk of accelerated degeneration of the adjacent segments caused by fusion is claimed to be the theoretical advantage of these approaches; however, there is a paucity of supportive evidence from biomechanical data. Therefore, this study investigated and compared the effects of PCF, PEACD, and ACDF on the adjacent segments and operative segments of the cervical spine from a biomechanical standpoint. METHOD: A normal and intact three-dimensional finite element digital model of C4-C7 was constructed and validated, and the finite element models of PEACD, PCF, and ACDF were obtained by modifying the C4-C7 model. All models were exposed to identical conditions of load during flexion, extension, axial rotation, and lateral bending. We calculated the range of motion (ROM), intervertebral disc pressure (IDP), and facet joint contact force (FJCF) of the operative segment and the adjacent segment in different motion conditions. RESULT: The conventional ACDF had a remarkable influence on the ROM and IDP of the operative segment and the adjacent segments. In the PEACD model, the change of ROM was not noticeable; the IDP of the operative segment was significantly smaller, whereas the change of IDP of the adjacent segment was insignificant. In the PCF model, the ROM and IDP of all segments remained unaffected.During extension, the facet joint contact force changed significantly after ACDF, and it changed slightly after PECAD and PCF. CONCLUSION: By comparatively analyzing the biomechanical changes of the cervical spine after PCF, PEACD, and ACDF using the finite element method, we suggested that PCF and PEACD were more suitable for surgical intervention of cervical spondylotic radiculopathy than ACDF from a biomechanical point of view and PCF may outperform PEACD.

Prognostic value of programmed cell death ligand 1 (PD-L1) for hepatocellular carcinoma: a meta-analysis.

The prognostic role of programmed death ligand-1 (PD-L1) expression in hepatocellular carcinoma (HCC) has been widely studied but the results are controversial. In this comprehensive meta-analysis, we elucidated the clinical value of PD-L1 in HCC. Relevant studies were systematically searched in the Cochrane Library, EMBASE, and PubMed until June 27, 2019. Eligible studies were validated for the prognostic effect of PD-L1 on the overall survival (OS), disease-free survival (DFS), and relapse-free survival (RFS) in HCC using a hazard ratio (HR) and its 95% confidence interval (95% CI). Twenty-three studies with 3529 patients were involved in this meta-analysis. The pooled results revealed that high membrane-bound PD-L1 (mPD-L1) expression was associated with poor OS (HR: 1.42; 95% CI: 1.12-1.80; P = 0.004) and had no significant correlation with RFS (HR: 1.14; 95% CI: 0.85-1.54; P = 0.39), and DFS (HR: 1.36; 95% CI: 0.81-2.28; P = 0.25). The results also indicated that high soluble PD-L1 (sPD-L1) levels were associated with worse OS (HR: 2.93; 95% CI: 2.20-3.91; P < 0.00001). In addition, high mPD-L1 expression was associated with high alpha-fetoprotein levels (AFP; OR = 1.46; 95% CI: 1.16-1.84; P = 0.001), hepatitis (OR = 0.72; 95% CI: 0.54-0.98; P = 0.03), poor tumor differentiation (OR = 0.68; 95% CI: 0.55-0.84; P = 0.03), and tumor-infiltrating lymphocytes (OR = 3.39; 95% CI: 1.06-10.91; P = 0.04). The mPD-L1 expression had no significant correlation with age, number of tumors, gender, tumor size, liver cirrhosis, vascular invasion, tumor encapsulation, or TNM stage. The study revealed that high mPD-L1 expression in the tumor tissue and high sPD-L1 levels were associated with shorter OS in HCC. Moreover, overexpression of mPD-L1 was significantly associated with poor tumor differentiation, hepatitis, AFP elevation, and tumor-infiltrating lymphocytes.

The complete chloroplast genome sequence of Brasenia schreberi (Cabombaceae).

Brasenia schreberi is a perennial aquatic herb. We determined the complete chloroplast genome sequence for B. schreberi using Illumina sequencing data. The complete chloroplast sequence is 158,993 bp, include large single-copy (LSC) region of 88,779 bp, small single-copy (SSC) region of 21,665 bp, a pair of invert repeats (IR) regions of 21,078 bp. Plastid genome contains 132 genes, 87 protein-coding genes, 37 tRNA genes, and 8 rRNA genes. Phylogenetic analysis base on 12 chloroplast genomes indicates that B. schreberi is sister to Cabomba spp. in Cabombaceae.

Complete chloroplast genome sequence of Bougainvillea Spectabilis (Nyctaginaceae).

Bougainvillea spectabilis is an important ornamental plant in tropical and subtropical regions, whose complex and diverse germplasm has brought great difficulties to variety selection and identification. Here, to provide data support for the identification of the relationship between cultivars of B. spectabilis, we sequenced the chloroplast genome of B. spectabilis. The chloroplast genome is 154,520 bp in length, including a large single-copy (LSC) region of 88,101 bp and small single-copy (SSC) region of 17,729 bp, and a pair of invert repeats (IR) regions of 24,171 bp. The chloroplast genome contains 129 genes, including 83 protein-coding genes, 37 tRNA genes, and 8 rRNA genes. The phylogenetic analysis based on 14 chloroplast genome demonstrated a close relationship between B. spectabilis and other plant species in Caryophyllales. The chloroplast genome will help for further of taxonomy research and provide data support for the identification of genetic relationship among different cultivars of B. spectabilis.

The complete chloroplast genome sequence of Eranthis stellate (Ranunculaceae).

Eranthis stellate belong to Ranunculaceae, which is interest in phylogenetic research because it has often been considered one of the most basal eudicots families. However, there are few chloroplastg enome data of Ranunculaceae available. Here, to provide available genomic data for the phylogenetic of Ranunculaceae, we determined the complete chloroplast genome of E. stellate. The complete chloroplast sequence is 158,817 bp, including a large single-copy (LSC) region of 87,137 bp, a small single-copy (SSC) region of 16,834 bp, a pair of invert repeats (IR) regions of 27,424 bp. Plastid genome contain129 genes, 84 protein-coding genes, 36 tRNA genes, and 8 rRNA genes. Phylogenetic analysis based on 14 chloroplast genomes indicates that E. stellata is sister to Aconitum austrokoreense clade in Ranunculaceae.

Microglial priming in Alzheimer's disease.

Alzheimer's disease (AD) is a chronic and progressive neurodegenerative disease of central nervous system (CNS). Nowadays, increasing evidence suggests that immune system plays a significant role in the mechanisms of AD's onset and progression. Microglia, the main participator in the immune system of CNS, is always regarded as a protector of our brain in a healthy state and also has a beneficial role in maintaining the homeostasis of CNS microenvironment. However, chronic and sustained stimulation can push microglia into the state termed priming. Primed microglia can induce the production of amyloid ß (Aß), tau pathology, neuroinflammation and reduce the release of neurotrophic factors, resulting in loss of normal neurons in quantity and function that has immense relationship with AD. The therapeutic strategies mainly aimed at modulating the microenvironment and microglial activity in CNS to delay progression and alleviate pathogenesis of AD. Overall, in this review, we highlight the mechanism of microglial priming, and discuss the profound relationship between microglial priming and AD. Besides, we also pay attention to the therapeutic strategies targeting at microglial priming.

Successful fertility following optimized perfusion and cryopreservation of whole ovary and allotransplantation in a premature ovarian insufficiency rat model.

BACKGROUND: Fertility preservation by whole ovary cryopreservation and transplantation (WOCP&TP) with vascular anastomosis requires successful cryopreservation. In this study, we investigated the possibility of restoring ovarian function and natural fertility after WOCP&TP in a premature ovarian insufficiency (POI) rat model. The influence of cryopreservation on the offspring of rats following WOCP&TP was also explored. METHOD: Rats aged 8-10 weeks were used as donors and recipients for allotransplantation. Fifteen rat whole ovaries were divided into three groups: the optimized group, the conventional group, and the fresh group. Different perfusion modes were used before cryopreservation and after thawing. Whole ovaries were observed by morphologic analysis, immunohistochemical staining, and transferase-mediated deoxyuridine triphosphate nick end-labeling assay. Ovarian function and fertility after WOCP&TP were then observed in 25 cyclophosphamide-induced POI rats for 8 months. Ovarian function was assessed by vaginal smears and blood hormone levels. Fertility restoration was quantified as the live birth rate after mating. The filial generation of rats was mated at 8-10 weeks of age. Offspring were observed for birth defect. RESULTS: Histological evaluation demonstrated intact morphology of follicles in all groups, with 77.6% of the total number of follicles identified as intact in the optimized group. The apoptotic rates of ovarian cells in the optimized group were significantly lower than that in the conventional group. Of the 20 live POI rats, 14 (70%) began to recover ovarian function after 2 weeks of transplantation, with normal hormone levels achieved 4 weeks after transplantation. Four of 14 rats were pregnant and delivered live offspring. One rat had a second pregnancy and delivered a second litter of live offspring. When the offspring matured, they were mated, and second and third generations of rats were born. All offspring had no abnormalities in appearance. CONCLUSIONS: High rates of restoration of ovarian function and natural fertility with multiple generations of offspring were obtained following WOCP&TP in a cyclophosphamide-induced POI rat model by utilizing optimized perfusion. Cryopreservation did not affect the viability of successive generations.

[Total knee arthroplasty with 3D printing technique versus conventional surgery: comparison of the outcomes].

OBJECTIVE: To compare the clinical outcomes of patients receiving total knee arthroplasty (TKA) using 3D printing technique and conventional surgical methods. METHODS: From October, 2015 to February, 2017, 17 patients (20 knees) underwent TKA with the assistance of individualized navigation template and 16 concurrent patients (18 knees) matched for age, gender and knee society score received conventional TKA. The operation time, blood loss, and osteotomy data of the femoral condyle and tibia plateau were recorded. The mean femorotibial angle (MFTA) and sagittal tibial component angle (STCA) after the operation and the KSS at the last follow-up were compared between the two groups. RESULTS: All the patients were followed up for 7-23 months, during which no infection or prosthesis loosening or motion was found. In patients receiving surgery with 3D printing technique, the osteotomy data of the femoral condyle and tibia plateau in the actual surgeries were consistent with those in surgical plans (P>0.05). The patients in the 3D group had a significantly shorter operation time and a higher KSS score than those in the conventional group (P<0.05). Significant differences were found between the two groups in postoperative MFTA and STCA (P<0.05). CONCLUSION: The application of 3D printing technique can simplify the surgical procedure and improve the surgical precision and efficacy of TKA.

One-stage Posterior Spinal Osteotomy in Severe Spinal Deformities: A Total of 147 Cases.

STUDY DESIGN: This is a retrospective study. OBJECTIVES: The treatment of severe spinal deformities is still a difficult surgical challenge. It is generally significant to identify the related complications performed to a consecutive series of patients with severe spinal deformity and managed by 1-stage posterior spinal osteotomy. SUMMARY OF BACKGROUND DATA: We investigated data from 147 consecutive patients (75 males and 72 females) with severe deformity and managed by Smith-Petersen osteotomy, pedicle subtraction osteotomy, or vertebral column resection between years 2006 and 2012 with >2-year follow-up. Mean age was 21.2 (range, 14-51 y) years at operation. MATERIALS AND METHODS: The patients underwent standing anteroposterior and lateral radiography before and after scoliosis surgery. Age, sex, diagnosis, surgical approach and centrum, all the related complications, treatment, and preoperative and postoperative Cobb angle in the coronal and sagittal planes were recorded at final follow-up. RESULTS: There were 17 (11.6%) cases with complications in 147 patients, including spinal cord-related complications in 7 cases (4.8%), superior mesenteric artery syndrome in 5 cases (3.4%), broken rod and unstable screw hat in 3 cases (2.0%), and infection in 2 cases (1.4%). Among the 17 cases, 15 cases recovered completely and 2 cases recovered partially. CONCLUSIONS: The total complication rate of severe spinal deformity after 1-stage posterior spinal osteotomy without fusion was about 11.6%. Except for the major complication of neurological deficit, spine surgeon should also pay more attention on other related complications, especially superior mesenteric artery syndrome. Large-scale and long-term follow-up was warranted to find out more subjective complication rates. LEVEL OF EVIDENCE: Level IV-prognostic study (see the guidelines for a complete description of levels of evidence).

Influence Analysis of Target Surface Emissivity on Infrared Radiation Polarization Characteristics.

Polarization imaging contains rich target parameters including spectrum, radiant intensity, polarization state, space geometry, etc. Polarization imaging can improve the target detection and recognition ability. The infrared polarization imaging is a new infrared detect technology in recent years. Infrared polarization imaging mainly aims to detect and identify the target with the difference of infrared radiation polarization characteristic between target and scene. But the state of polarization is affected by transmission medium in the transmission process of infrared radiation polarization information while the common method is to analyze the infrared radiation polarization characteristics of target that is not able to describe effects of all interrelated parameters and is difficult to estimate influence factors in the process of transmission. The equation of infrared polarized radiation is established through bidirectional reflectance distribution function based on micro-facet theory. And the mathematical model of the relationship between infrared radiation polarization degree and emissivity is derived in this paper. Result shows that the influence of target surface emissivity on the infrared degree can be ignored. On the basis of theoretical analysis, the infrared spectrum polarization imaging tests are unfolded, and the analysis of test data is consistent with the theoretical analysis. It is concluded that the correlation between the polarization degree of infrared and the emissivity of target surface can be neglected. The research production of this paper is conductive to increase of target detect efficiency, and it will provide new ways and means for camouflage target detect and identify. Therefore, the research production can be applied to detect and identify the camouflage target that is accomplished camouflage through change emissivity of camouflage target surface.

[Flavonoid glycosides from callus cultures of Dysosma versipellis].

Various chromatographic techniques, including silica gel column chromatography, Sephadex LH-20, preparative thin-layer chromatography, and preparative HPLC, were employed to isolate the chemical constituents from callus cultures of Dysosma versipellis. Structures of the compounds were elucidated based on UV, IR, MS and NMR spectroscopic data analysis. Totally, seven flavonoid glycosides were isolated from the 95% ethanol extract of the callus cultures and identified as kaempferol-3-O-[6″-(3″'-methoxy)-malonyl]-ß-D-glucopyranoside(1), kaempferol-3-O-(6″-O-acetyl)-ß-D-glucopyranoside(2), kaempferide-3-O-ß-D-glucopyranoside(3), kaempferol-3-O-ß-D-glucopyranoside(4), isoquercitrin(5), quercetin-4'-O-ß-D-glucopyranoside(6) and kaempferol-3-(6″-malonyl)-ß-D-glucopyranoside(7), respectively.All these compounds were isolated from callus cultures of D. versipellis for the first time.Compounds 1, 2, 3, 6 and 7 were firstly obtained from plant materials of D. versipellis, and compound 1 was a new compound.

Impact of CYP2C9 polymorphism found in the Chinese population on the metabolism of propofol in vitro.

The microsomal CYP2C9 alleles involved in the biotransformation of propofol, a widely used anesthetic agent, were investigated in vitro. To examine the enzymatic activity of the CYP2C9 alleles, kinetic parameters for propofol 4-hydroxylation were determined in recombinant human P450s CYP2C9 microsomes from Sf21 insects cells carrying CYP2C9*1 and other variants. Some of the variants showed decreased enzyme activity compared with the wild type, as previously reported. Two variants (CYP2C9*36 and *56) were found substantially to increase intrinsic clearance relative to the wild type variant. Most variants significantly (p<0.05) decreased intrinsic clearance of propofol compared with the wild type, except *11, *47, and *54. This study is the first to report these rare alleles for propofol metabolism, providing fundamental data for further clinical studies on CYP2C9 alleles for propofol metabolism in vivo.

Meroterpenoids and isoberkedienolactone from endophytic fungus Penicillium sp. associated with Dysosma versipellis.

Seven meroterpenoids and five small-molecular precursors were isolated from Penicillium sp., an endophytic fungus from Dysosma versipellis. The structures of new compounds, 11beta-acetoxyisoaustinone (1) and isoberkedienolactone (2) were elucidated based on analysis of the spectral data, and the absolute configuration of 2 was established by TDDFT ECD calculation with satisfactory match to its experimental ECD data. Meroterpenoids originated tetraketide and pentaketide precursors, resepectively, were found to be simultaneously produced in specific fungus of Penicillium species. These compounds showed weak cytotoxicity in vitro against HCT-116, HepG2, BGC-823, NCI-H1650, and A2780 cell lines with IC 50 > 10 micromol x L(-1).