Palladium-Catalyzed Ring-Opening Reaction of Cyclopropenones with Vinyl Epoxides.

We report herein the Pd-catalyzed selective ring-opening reaction of cyclopropenones with vinyl epoxides. By using a commercially available Pd2(dba)3·CHCl3-BINAP catalyst, a wide range of conjugated alkadienyl carboxylates could be accessed in good yield and excellent regioselectivity. The new application of zwitterionic π-allyl palladium intermediates has been demonstrated in organic synthesis.

Molecular epidemiological characteristics of the virus in 96 children with acute diarrhea in Changdu of Tibet, China. / 西藏昌都地区96ä¾‹å„¿ç«¥æ€¥æ€§è ¹æ³»ç— æ¯’åˆ†å­æµè¡Œç— å­¦åˆ†æž.

OBJECTIVES: To study the molecular epidemiological characteristics of the virus in children with acute viral diarrhea in Changdu of Tibet, China. METHODS: Fecal specimens were collected from 96 children with acute diarrhea who visited the People's Hospital of Changdu, Tibet, from November 2018 to November 2020 and were tested for adenovirus, norovirus, astrovirus, sapovirus, and rotavirus. Gene sequencing was performed for the genotypes of these viruses. RESULTS: The overall positive rate of the five viruses was 39% (37/96), among which astrovirus had the highest positive rate of 17%, followed by norovirus (9%), rotavirus (8%), adenovirus (7%), and sapovirus (5%). There was no significant difference in the positive rate of the five viruses among different age groups (P>0.05). Only the positive rate of astrovirus was significantly different among the four seasons (P<0.05). For adenovirus, 6 children had F41 type and 1 had C2 type; for norovirus, 6 had GⅠ.3 type, 1 had GⅠ.7 type, 1 had GⅡ.3 type, and 2 had GⅡ.4 Sydney_2012 type; HAstrV-1 type was observed in all children with astrovirus infection; for sapovirus, 1 child each had sporadic GⅠ.2, GⅠ.6, and GⅡ.1 sapovirus and 2 children had unknown type; 6 children had rotavirus G9[P8]. CONCLUSIONS: Astrovirus and norovirus are important pathogens in children with acute diarrhea in Changdu, Tibet. The positive rate of adenovirus, norovirus, astrovirus, sapovirus, and rotavirus is not associated with age, and only the positive rate of astrovirus has obvious seasonality. F41 type is the dominant genotype of adenovirus; GⅠ.3 is the dominant genotype of norovirus; HAstrV-1 is the dominant genotype of astrovirus; sporadic GⅠ.2, GⅠ.6, and GⅡ.1 are the dominant genotypes of sapovirus; G9[P8] is the dominant genotype of rotavirus.

[Anisakis simplex larvae: infection status in marine fishes for sale in Shantou].

OBJECTIVE: To investigate the infection status of Anisakis simplex larvae in marine fishes for sale in Shantou. METHODS: Marine fishes were randomly collected from markets in Shantou City from February to December 2013, and then classified. The viscera and muscle of each fish were carefully dissected and thoroughly examined for anisakids. The larvae were examined under a light microscope. The infection rate and intensity of Anisakis simplex larvae were calculated. RESULTS: A total of 382 fish specimens belonging to 52 species were examined. 42 out of 52 species (80.8%) were found infected by A. simplex larvae. The overall infection rate reached 47.4% (181/382), and average 5.5 larvae parasitized per infected fish (995/181). The survival rate of larvae was 100%. The highest infection rate observed was 100% in Scomber australasicus (4/4), Trachurus japonicus (9/9), Decapterus maruadsi (8/8), Lutjanus lutjanus (9/9), Argyrosomus argentatus (4/4), Nibea albiflora (4/4), Nemipterus bathybius (12/12), Trachinocephalus myops (7/7) and Mene maculata (9/9), followed by 16/18 in Pneumatophorus japonicus, 6/7 in Lutjanus ophuysenii and 5/6 in Lutjanus fulvus. A. simplex larvae were not detected in 10 fish species, namely, Megalaspis cordyla, Lutjanus argentimaculatus, Lutjanus fulviflamma, Acanthopagrus australis, Acanthopagrus latus, Plectorhinchus nigrus, Dentex tumifrons, Psenopsis anomala, Scatophagus argus, and Seriola lalandi. The infection intensity was the highest in Lutjanus fulvus (21.0 per fish), followed by Trachinocephalus myops (16.7 per fish), Saurida filamentosa (14.0 per fish) and Mene maculate (10.1 per fish). The lowest infection intensity was found in Rastrelliger kanagurta, Kaiwarinus equula, Atule mate, Lutjanus russellii, Plectorhinchus cinctus, Priacanthus tayenus, Branchiostegus argentatus, Branchiostegus albus, Sphyraena pinguis, Formio niger, Trachinotus blochii, Siganus fuscescens and Choerodon azurio (less than 2 per fish). The highest infection rate (34.3%, 131/382) was found in the mesentery. The infection intensity was highest in pyloric appendage (3.5 per fish). A. simplex larvae were not found in muscle. The highest infection rate (60.2%, 74/123) was found in fishes with body weight of 100-200 g. The infection intensity was highest in fish with body weight of 301-400 g (7.8 per fish). CONCLUSION: The infection rate of A. simplex larvae is high in marine fishes from Shantou markets.

Treatment for papillary thyroid microcarcinoma.

AIM OF THE STUDY: The treatment for papillary thyroid microcarcinoma (PTMC), which is a tumor measuring less than 1 cm, is still a subject of controversy. The aim of this study is to retrospectively evaluate the patients diagnosed with PTMC in terms of their clinical and histopathological features. MATERIAL AND METHODS: A total of 153 consecutive patients with PTMC were treated, and their clinical and histopathological characteristics were reviewed. The tumor diameter was observed to range from 1.0 mm to 10 mm (mean of 5.8 mm). Histologically, 138 (90.2%) cases of classical papillary carcinoma and 15 (9.8%) cases of the follicular variant were noted. Multicentric tumors were found in 37 (24.2%) patients, of whom 12 (7.8%) had more than one PTMC on the same side and 25 (16.3%) displayed bilateral PTMC. RESULTS: The proportions of capsular invasion and lymph node metastasis were 11.8% (18/153) and 48.1% (39/81), respectively. One patient showed distant metastasis during follow-up and died fifteen months after the operation. PTMC showed a high incidence of multifocality and lymph node metastasis in the level VI central compartment. The optimal surgical strategy for PTMC was total thyroidectomy and central compartment node dissection. CONCLUSIONS: Frozen tissue sections should be made for the prompt diagnosis of PTMC in all the thyroid nodules, except when the malignant diagnosis was already confirmed by cytology.

2-[(3-Bromo-anilino)meth-yl]-1,2-benzo-thia-zol-3(2H)-one.

The title compound, C(14)H(11)BrN(2)OS, was synthesized by the reaction of 1,2-benzothia-zol-3(2H)-one with formalin and 3-bromo-aniline in ethanol. The 1,2-benzothia-zolone ring system is approximately planar [maximum deviation = 0.0142 (s.u.?) Å] and forms a dihedral angle of 79.19 (5)° with the benzene ring. In the crystal, molecules are linked by N-H⋯O, C-H⋯O and C-H⋯Br interactions.

Surgical strategies for Mirizzi syndrome: A ten-year single center experience.

BACKGROUND: Mirizzi syndrome (MS) remains a challenging biliary disease, and its low rate of preoperative diagnosis should be resolved. Moreover, technological advances have not resulted in decisive improvements in the surgical treatment of MS. Complex bile duct lesions due to MS make surgery difficult, especially when the laparoscopic approach is adopted. The safety and long-term effect of MS treatment need to be guaranteed in terms of preoperative diagnosis and surgical strategy. AIM: To analyze preoperative diagnostic methods and the safety, effectiveness, prognosis and related factors of surgical strategies for different types of MS. METHODS: The clinical data of MS patients who received surgical treatment from January 1, 2010 to December 31, 2020 were retrospectively reviewed. Patients with malignancies, choledochojejunal fistula, lack of data and lost to follow-up were excluded. According to preoperative imaging examination records and documented intraoperative findings, the clinical types of MS were determined using the Csendes classification. The safety, effectiveness and long-term prognosis of surgical treatment in different types of MS, and their interactions with the clinical characteristics of patients were summarized. RESULTS: Sixty-six patients with MS were included (34 males and 32 females). Magnetic resonance imaging/magnetic resonance cholangiopancreatography (MRI/MRCP) showed specific imaging features of MS in 58 cases (87.9%), which was superior to ultrasound scan (USS) in the diagnosis of MS and more sensitive to subtle biliary lesions than USS. The overall laparoscopic surgery completion rate was 53.03% (35/66), where the completion rates of MS type I, II and III were 69.05% (29/42), 42.86% (6/14) and zero (0/10), respectively. Thirty-one patients (46.97%) underwent laparotomy or conversion to laparotomy including 11 cases of iatrogenic bile duct injury which occurred in type I patients, and 25 of these patients underwent bile duct exploration, repair and T-tube drainage. In addition, 25 patients underwent intraoperative choledochoscopy and T-tube cholangiography. Overall, 21 cases (31.8%) were repaired by simple suturing, and 14 cases (21.2%) were repaired using the remaining gallbladder wall patch in the subtotal cholecystectomy. The ascendant of the Csendes classification types led to an increase in surgical complexity reflected by increased operation time, bleeding volume and cost. Gender, acute abdominal pain and measurable stone size had no effect on Csendes type of MS or final surgical approach. Age had no effect on the classification of MS, but it influenced the final surgical approach, hospital stay and cost. A total of 66 patients obtained a relatively high preoperative diagnostic rate and underwent surgery safely without serious complications, and no mortality was observed during the follow-up period of 36.5 ± 26.5 mo (range 13-76, median 22 mo). CONCLUSION: MRI/MRCP can improve the preoperative diagnosis of MS. The Csendes classification can reflect the difficulty of treatment. The surgical strategies including laparoscopic surgery for MS should be formulated based on full evaluation and selection.

Electroacupuncture improves learning and memory functions in a rat cerebral ischemia/reperfusion injury model through PI3K/Akt signaling pathway activation.

Electroacupuncture has been widely used to treat cognitive impairment after cerebral ischemia, but the underlying mechanism has not yet been fully elucidated. Studies have shown that autophagy plays an important role in the formation and development of cognitive impairment, and the phosphoinositide 3-kinase (PI3K)/Akt signaling pathway plays an important role in autophagy regulation. To investigate the role played by the PI3K/Akt signaling pathway in the electroacupuncture treatment of cerebral ischemia/reperfusion rat models, we first established a rat model of cerebral ischemia/reperfusion through the occlusion of the middle cerebral artery using the suture method. Starting at 2 hours after modeling, electroacupuncture was delivered at the Shenting (GV24) and Baihui (GV20) acupoints, with a dilatational wave (1-20 Hz frequency, 2 mA intensity, 6 V peak voltage), for 30 minutes/day over 8 consecutive days. Our results showed that electroacupuncture reduced the infarct volume in a rat model of cerebral ischemia/reperfusion injury, increased the mRNA expression levels of the PI3K/Akt signaling pathway-related factors Beclin-1, mammalian target of rapamycin (mTOR), and PI3K, increased the protein expression levels of phosphorylated Akt, Beclin-1, PI3K, and mTOR in the ischemic cerebral cortex, and simultaneously reduced p53 mRNA and protein expression levels. In the Morris water maze test, the latency to find the hidden platform was significantly shortened among rats subjected to electroacupuncture stimulation compared with rats without electroacupuncture stimulation. In the spatial probe test, the number of times that a rat crossed the target quadrant was increased in rats subjected to electroacupuncture stimulation compared with rats without electroacupuncture stimulation. Electroacupuncture stimulation applied to the Shenting (GV24) and Baihui (GV20) acupoints activated the PI3K/Akt signaling pathway and improved rat learning and memory impairment. This study was approved by the Animal Ethics Committee of the First Affiliated Hospital of Henan University of Traditional Chinese Medicine, China (approval No. 8150150901) on March 10, 2016.

Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro.

AIM: To design and synthese a novel class of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors, featuring the (phenylsulfonamido-methyl)pyridine and (phenylsulfonamido-methyl)thiazole framework. METHODS: Our initial lead 4-(phenylsulfonamido-methyl)benzamides were modified. Inhibition of human and mouse 11beta-HSD1 enzymatic activities by the new compounds was determined by a scintillation proximity assay (SPA) using microsomes containing 11beta-HSD1. RESULTS: Sixteen new compounds (6a-6h, 7a-7h) were designed, synthesized and bioassayed. In dose-response studies, several compounds showed strong inhibitory activities with IC50 values at nanomolar or low nanomolar concentrations. Structure-activity relationships are also discussed with respect to molecular docking results. CONCLUSION: This study provides two promising new templates for 11beta-HSD1 inhibitors.

4-Methyl-3-[4-(3-pyrid-yl)pyrimidin-2-yl-oxy]aniline.

In the title compound, C(16)H(14)N(4)O, there are inter-molecular N-H⋯N hydrogen bonds which may be effective in stabilizing the crystal. The title compound is an important medicament and is used in the synthesis of anti-tumour drugs.

The choose of different surgical therapies of hepatic alveolar echinococcosis: A single-center retrospective case-control study.

The aim of this study was to evaluate different surgical therapies for hepatic alveolar echinococcosis in different clinical stages.We analyze the clinical data of 115 patients who received surgical treatment in West China Hospital from January 2004 to June 2016. Among these patients, 77 cases underwent radical hepatic resection (group A, n = 77); 17 cases underwent palliative resection (group B, n = 17), and 21 cases underwent liver transplantation (group C, n = 21) with 12 cases of orthotopic liver transplantation and 9 cases of liver autotransplantation.The postoperative complication rate of radical hepatic resection group was 13.0% (10/77), which is statistically significant (P < .05) than the rate of palliative resection group 29.4% (5/17) or liver transplantation group 23.8% (5/21). The follow-up period ranged from 1 to 72 months. The overall median survival rate of radical resection was 72/77, higher than the rate of palliative group (12/17) or transplantation group (17/21), which was also statistically significant (P < .01).In our study, we believe in that all stages of hepatic alveolar echinococcosis should take active surgical interventions, and radical hepatic resection should be considered as the first-choice treatment for early stage of alveolar echinococcosis, while palliative surgery is still helpful to relieve symptoms and improve the life quality for advanced patients. Liver transplantation might also be an alternative option for the late-stage hepatic alveolar echinococcosis.

Influences of the Three Gorges Project on seismic activities in the reservoir area.

Reservoir-induced earthquakes related with the construction of the Three Gorges Project have attracted great concerns of the public. Since the first water impoundment on May 25, 2003, a number of earthquakes have occurred during the water storage stages, in which the largest was the Badong M5.1 earthquake on December 16, 2013. In this paper, the relationships between seismic activities, b value, seismic parameters, and reservoir water level fluctuations are studied. In addition, based on the digital seismic waveform data obtained since 2000, the focal depth changes and focal mechanism characteristics before and after the water impoundment are studied as well. These provide us important information to understand the earthquake mechanisms. The results show that these earthquakes are typical reservoir-induced earthquakes, which are closely related to water infiltration, pore pressure, and water level fluctuations. The majority of the micro and small earthquakes are caused by karst collapse, mine collapse, bank reformation, superficial unloading, and so on. The larger earthquakes are related to the fault structures to some extent. Due to the persistent effects of water impoundment on the seismic and geological environments around the reservoir and water infiltration into the rocks, the influences on the crustal deformation field, gravity field, seepage field, and fault medium-softening action may vary gradually from a higher strength to a weaker one. Therefore, it is possible that small earthquakes and few medium earthquakes (M≤5.5) will occur in the reservoir area in the future.

Cyclin D1 antisense oligodexoyneucleotides inhibits growth and enhances chemosensitivity in gastric carcinoma cells.

AIM: To examine the effects of cyclin D1 antisense oligodexoyneucleotides (ASODN) on growth and chemosensitivity of gastric carcinoma cell lines SGC7901 and its mechanism. METHODS: Phosphorothioate modified cyclin D1 ASODN was encapsulated by LipofectAMINE2000 (LF2000) and transfected into cells, the dose-effect curves and growth curves were observed. 5-FU, MTX, CDDP of different concentrations were given after transfecting cells with cyclin D1 ASODN for 24 h the dose-effect responses were observed and IC50s were calculated. The mRNA expression of cyclin D1, thymidylate synthase (TS), thymidine phosphorylase (TP) and dihydrofolate reductase (DHFR) was detected by reverse transcription-PCR (RT-PCR) at 24 h and 48 h after transfection. RESULTS: Dose-dependent inhibitory effect was caused by cyclin D1 ASODN in SGC7901 cells. Transfecting gastric carcinoma cells with 0.2 micromol/L cyclin D1 ASODN for 24 h could inhibit growth significantly and reduce expression of cyclin D1 mRNA. Cyclin D1 ASODN could increase the chemosensitivity to 5-FU, MTX, CDDP in cells. The IC50s of different chemotherapeutic agents in ASODN plus chemotherapy groups were significantly lower than those in controls. Transfection with cyclin D1 ASODN leaded to an increase in TS and DHFR mRNA and a decrease in TP mRNA as determined by RT-PCR at 24 h, the alterations were more significant at 48 h. CONCLUSIONS: Cyclin D1 ASODN can decrease mRNA expression of cyclin D1, inhibit growth and enhance the chemosensitivity by changing the expression of enzymes related to metabolism of chemotherapeutic agents in SGC7901 gastric carcinoma cells.

Development of a double-monoclonal antibody sandwich ELISA: Tool for chicken interferon-γ detection ex vivo.

The aim of the present work was to develop reagents to set up a chicken interferon-γ (ChIFN-γ) assay. Four monoclonal antibodies (mAbs) specific for ChIFN-γ were generated to establish sandwich ELISA based on 2 different mAbs. To improve the detection sensitivity of ChIFN-γ, a double-monoclonal antibody sandwich ELISA was developed using mAb 3E5 as capture antibody and biotinylated mAb 3E3 as a detection reagent. The results revealed that this ELISA has high sensitivity, allowing for the detection of 125 to 500 pg/mL of recombinant ChIFN-γ, and also has an excellent capacity for detecting native ChIFN-γ. This ELISA was then used to detect ChIFN-γ level in chickens immunized with a Newcastle disease virus (NDV) vaccine, the immunized chicken splenocytes were stimulated by NDV F protein as recall antigen. From our results, it appears that the sensitivity range of this sandwich ELISA test is adequate to measure the ex vivo release of ChIFN-γ.

L'objectif de la présente étude était de développer des réactifs afin de mettre au point une épreuve de détection de l'interféron-γ de poulet (ChIFN-γ). Quatre anticorps monoclonaux (AcMo) spécifiques pour ChIFN-γ ont été produits afin d'avoir un ELISA sandwich reposant sur deux AcMo différents. Afin d'améliorer la sensibilité de détection de ChIFN-γ, un test ELISA sandwich a deux anticorps monoclonaux a été développé utilisant l'AcMo 3E5 comme anticorps de capture et l'AcMo 3E3 biotinylé comme réactif de détection. Les résultats ont démontré que ce test ELISA possède une sensibilité élevée, permettant la détection de 125 à 500 pg/mL de ChIFN-γ recombinant, et ayant également une excellente capacité à détecter le ChIFN-γ original. Ce test ELISA a par la suite été utilisé pour détecter les quantités de ChIFN-γ chez des poulets immunisés avec un vaccin contre la maladie de Newcastle (NDV), les cellules de la rate des poulets immunisés ont été stimulées par la protéine F du NDV comme antigène de rappel. À partir de nos résultats, il semble que la plage de sensibilité de ce test ELISA sandwich est adéquate pour mesurer la libération ex vivo de ChIFN-γ.(Traduit par Docteur Serge Messier).

[Morphological and histological studies of Herpetospermum pedunculosum seeds and other substitutes].

OBJECTIVE: To provide new evidences for the identification of Herpetospermum pedunculosum seeds and other substitutes. METHOD: Microscopic examination of the cross sections and powers of the seeds of H. pedunculosum, Momordica charantia, Thladiantha setispina and M. cohinchinensis were made to characterize the drug materials. RESULT AND CONCLUSION: The external and internal structure of T. setispina and M. charantia were studied for the first time. Two types of different branched starry sclereids was found in M. cohinchinensis. Comparative studies on external and internal structure were carried out on seeds of the 4 species. As a result, they could be distinguished by external characteristics such as shape, size and color of their seeds, and by internal structure such as size and type of sclereid, epidermis and sub-epidermis cell of seed coat.

Prognosis of psychomotor and mental development in premature infants by early cranial ultrasound.

BACKGROUND: It is of high incidence of brain injuries in premature infants, so it is necessary to diagnose and treat the brain injury early for neonatal clinical practice. We are aimed to investigate the relationship between early postnatal cranial ultrasonography and psychomotor and mental development in prematrue infants at the age of 12 months. METHODS: Two-hundred and eight premature infants were selected and underwent follow-up from January, 2007 to November, 2012. Cranial ultrasonography was performed on them. The developmental outcomes of these premature infants at the age of 12 months were assessed by the psychomotor developmental index (PDI) scale and mental development index (MDI). The relationship between ultrasonic gray-scale value and PDI and MDI was analyzed. RESULTS: The worse prognosis for psychomotor and mental development was associated with the gestational age, Apgar score(1 min), gender, chorioamnionitis, duration of mechanical ventilation and duration of mechanic ventilation. The differences between the prognosis of psychomotor and mental development, and peri-intraventricular hemorrhage (PIVH) and periventricular white matter damage (PWMD), were statistically significant (P<0.05). There were also significant differences between the early postnatal ultrasonic gray-scale value and prognoses of both psychomotor development and mental development (P<0.05). There were negative correlations between ultrasonic gray-scale and both PDI and MDI (r=-0.753, P<0.05; r=-0.764, P<0.05). CONCLUSIONS: The early postnatal cranial ultrasonography can assist to predict the prognosis of psychomotor and mental development for premature infants. The higher grade of PIVH and PWMD was associated with the worse prognosis of psychomotor and mental development.

[Treatment of paraneoplastic pemphigus with Castleman's disease].

OBJECTIVE: To discuss the clinical findings and treatment of paraneoplastic pemphigus (PNP) with Castleman's disease. METHODS: To investigate the clinical, histopathologic and CT findings of 8 cases paraneoplastic pemphigus with Castleman's disease. RESULTS: All of 8 patients were diagnosed PNP first and were found Castleman's tumor incidently during routine examination. All 8 cases showed severe erosion or ulcer of the oral mucosa with various skin lesions. Histopathologically, there were intraepidermal acantholytic vesicle, basal cell liquefaction, necrotic keratinocytes in the epidermis and lymphocyte infiltration in the upper dermis. CT scan appeared solitary mass in these patients. Some of them were attacked by bronchiolitis obliterans. All 8 patients were failed by use of predisone. Obvious relief of PNP and pulmonary lesion occurred after tumor was rescted. CONCLUSIONS: Paraneoplastic pemphigus with Castleman's disease is a rare disease. The key step is to find and resect the tumor in abdomen. CT scan should be used to detect the tumor in patients with PNP, especially, when predisone was failed in treatment.

[Analysis of malaria epidemic situation in Shantou City from 1992 to 2012].

OBJECTIVE: To understand the epidemic characteristics, regular pattern and trend of malaria in Shantou City, Guangdong Province. METHODS: The historical data of malaria were collected and analyzed by the descriptive epidemiological methods in Shantou City from 1992 to 2012. RESULTS: A total of 556 malaria cases were reported in Shantou City from 1992 to 2012, with the annually incidence of 0.056 cases per 10 thousand. After 2003, no secondary cases and local outbreak of malaria occurred. The ratio of male to female was 3.34: 1, and 82.73% of the patients were aged from 15 to 45 years. The peasants (including workers from the village) and factory workers most easily suffered from malaria with a proportion of 39.21% and 18.35%, respectively. Nevertheless there was an exception in some year. CONCLUSION: There is still some reported cases of malaria each year in Shantou City, therefore, we should continue to strengthen the preventive and monitoring measures.

[Dynamic characteristics of forest landscape in Chengdu City in last 20 years].

Based on the remote sensing data of Landsat TM (1985, 1995, and 2000) and CBERS (2006), and by using landscape pattern method and index model of regional land use change in combining with eco-function regionalization, this paper analyzed the dynamic characteristics of forest landscape in Chengdu City in 1985-2006. In the study period, over 17,000 hm2 of forest land lost, and the number and area of small- and medium-size patches changed significantly, indicating the apparent conversion and fragmentation of forest land. Forest land was mainly distributed in mountainous area, accounting for 70% of the total. In contrast, more number of patches was found in plain region, amounting to 70% of the total. The most rapid change of forest land area occurred in 1985-1995, especially in mountainous region. The relative change rate of forest land area in different eco-function regions also varied in different periods. Forest land, converted to or converted from, was mainly related to cropland and grassland. In 2000-2006, forest land was quite stable. Survival-oriented economic welfare, environmental security, and fast urbanization process were the main driving forces of the temporal dynamic change of forest landscape, whereas geographical division and socio-economic layout were the main constraints to the spatial dynamic change of forest landscape.

Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice.

BACKGROUND AND PURPOSE: 11beta-Hydroxysteroid dehydrogenase type 1 (11beta-HSD1) is an attractive therapeutic target of type 2 diabetes and metabolic syndrome. Emodin, a natural product and active ingredient of various Chinese herbs, has been demonstrated to possess multiple biological activities. Here, we investigated the effects of emodin on 11beta-HSD1 and its ability to ameliorate metabolic disorders in diet-induced obese (DIO) mice. EXPERIMENTAL APPROACH: Scintillation proximity assay was performed to evaluate inhibition of emodin against recombinant human and mouse 11beta-HSDs. The ability of emodin to inhibit prednisone- or dexamethasone-induced insulin resistance was investigated in C57BL/6J mice and its effect on metabolic abnormalities was observed in DIO mice. KEY RESULTS: Emodin is a potent and selective 11beta-HSD1 inhibitor with the IC(50) of 186 and 86 nM for human and mouse 11beta-HSD1, respectively. Single oral administration of emodin inhibited 11beta-HSD1 activity of liver and fat significantly in mice. Emodin reversed prednisone-induced insulin resistance in mice, whereas it did not affect dexamethasone-induced insulin resistance, which confirmed its inhibitory effect on 11beta-HSD1 in vivo. In DIO mice, oral administration of emodin improved insulin sensitivity and lipid metabolism, and lowered blood glucose and hepatic PEPCK, and glucose-6-phosphatase mRNA. CONCLUSIONS AND IMPLICATIONS: This study demonstrated a new role for emodin as a potent and selective inhibitor of 11beta-HSD1 and its beneficial effects on metabolic disorders in DIO mice. This highlights the potential value of analogues of emodin as a new class of compounds for the treatment of metabolic syndrome or type 2 diabetes.