Identification of involatile chemical components from Moutai-flavored distiller’s grains / 中国药科大学学报

@#In order to study the involatile chemical components in Moutai-flavored distiller’s grains, the Moutai-flavored distiller’s grains were extracted with 75% ethanol, followed by extraction with petroleum ether, ethyl acetate, and n-butanol. Silica gel, ODS, sephadex LH-20, and preparative HPLC were used to separate and identify the petroleum ether and ethyl acetate layers.ESI-MS and NMR were used to identify the compounds, which were respectively identified as pentadecanoic acid (1), palmitic acid (2), trans-2-decenoic acid (3), n-nonyl octadecanoate (4), ethyl octadecanoate (5), ethyl linoleate (6), luric acid (7), 1, 3-dicaprylyl-2-linoleylglycerin (8), cyclic (phenylalanine-proline) (9), cyclo-(proline-leucine) (10), 3, 6-bis-(2-methylpropyl)-2,5-dione piperazine (11), 4-hydroxyphenethyl alcohol (12), 2,4-dihydroxybenzoic acid (13), stigmasterol (14), 2-furancarboxylic acid (15), valine (16), L-alanine acyl-L-proline (17), dihydroquercetin (18), 5, 7, 3'', 4''-tetrahydroxyflavonoids (19), quercetin (20), and naringenin (21). Compounds 1-21 were isolated from distiller’s grains for the first time.

Value of 3D printed polyether ether ketone prosthesis in the treatment of scapular tumors / 中华骨科杂志

Polyetheretherketone (PEEK) as a new type of thermoplastic engineering plastic, has good biological activity, elastic modulus close to human cortical bone and radiation permeability, and has been widely used in medical field. This study aims to explore the safety and clinical efficacy of using 3D printing personalized PEEK materials to repaire scapular bone defects after bone tumor resection. A total of 6 patients who underwent the implantation of 3D printed PEEK scapular prosthesis from January 2020 to December 2021 in Yunnan Cancer Hospital were retrospectively analyzed. There were 3 males and 3 females, with age ranged from 14 to 52 years. There were 1 case of synovial sarcoma, 1 of Ewing's sarcoma, and 4 of chondrosarcoma. PEEK prosthesis was designed and fabricated based on CT data before surgery. Tumor resection and prosthesis replacement were performed under the premise of ensuring safe surgical boundaries, including 2 cases of total scapular prosthesis replacement and 4 cases of partial scapular prosthesis replacement. The operation time was 90-170 min, and the intraoperative blood loss was 100-400 ml. All 6 patients received satisfactory follow-up, with a tumor progression free survival time of 16-28 months. No tumor recurrence or metastasis was observed, and all patients survived tumor free. At last follow-up, the Constant-Murley shoulder joint score was a minimum of 62 points and a maximum of 68 points. The Japanese Orthopaedic Association's shoulder joint score was 63 points minimum and 78 points maximum. Computer-aided design 3D printing PEEK material prosthesis has certain advantages in the treatment of scapular tumor limb salvage. It has light weight, well adapted, relatively simple installation, good histocompatibility, and can obtain a better appearance and function of the shoulder joint after operation. It can become one of the options for limb salvage treatment of scapular tumor.

Expression and significance of HERG protein in Cajal interstitial cells of gallbladder tissue in patients with gallbladder stones / 中华肝胆外科杂志

Objective:To investigate the expression and significance of human ether-a-go-go related gene (HERG) protein in interstitial cells of Cajal (ICC) in patients with gallbladder stones.Methods:The gallbladder tissues of 60 patients with gallbladder diseases who underwent cholecystectomy from January 2018 to December 2020 in the Faculty of Hepato-Pancreato-Biliary Surgery, Chinese PLA General Hospital were collected, including 36 males and 24 females, aged (46.0±14.0) years. They were divided into two groups according to whether there were gallstones: gallstone group and control group (patients with gallbladder polyps and gallbladder adenomyosis), with 30 cases in each group. Color ultrasound was used to detect and calculate the gallbladder contraction rate. The neck, body and bottom tissues of the gallbladder were excised and sectioned. The expression of HERG protein and CD117 ( marker of ICC) was detected by immunofluorescence staining, immunohistochemistry and Western blot.Results:The gallbladder contraction rate in the gallstone group was (65.8±4.1)%, lower than that in the control group (73.8±5.3)%, with a statistically significant difference ( t=4.14, P<0.001). Immunohistochemistry showed that HERG protein was mainly distributed in the mucosal layer of gallbladder tissue, which was pale brown. The relative expression of HERG protein at the bottom of gallbladder in the gallstone group was (0.293±0.102), lower than that in the control group (0.694±0.059), with a statistically significant difference ( t=3.38, P=0.027). Immunofluorescence staining showed that HERG protein was mainly distributed in ICC of gallbladder epithelium. HERG protein expression in ICC at the bottom of gallbladder in gallstone group was lower than that in control group, while HERG protein expression at the neck and body of gallbladder had no significant difference. Conclusion:There are ICC and HERG protein in gallbladder tissue of patients with gallstone. The decrease of gallbladder contraction rate may be related to the decrease of HERG protein expression in ICC in gallbladder bottom tissue.

Study on nephrotoxicity of the extracts from different parts of Miao medicine Wikstroemia indica / 中国药房

OBJECTIVE To study the nephrotoxicity of the extracts from different parts o f Miao medicine Wikstroemia indica in healthy rats ，and to provide reference for the study of its toxicity mechanism and clinical drug use. METHODS Using 70％ ethanol as solvent ，total ethanol extract of W. indica was extracted with diacolation method. After dispersing the above extract with water，the fractions of corresponding fractions were obtained with petroleum ether ，ethyl acetate and n-butanol，and the rest was the extract of water fraction. SD rats were randomly divided into total ethanol extract group ，petroleum ether fraction group ，ethyl acetate fraction group ，n-butanol fraction group ，water fraction group and blank group ，with 12 rats in each group （half male and half female ）. The rats in the administration groups were given the corresponding dose of drug solution intragastrically （total ethanol extract 317.520 mg/kg，petroleum ether fraction 7.875 mg/kg，ethyl acetate fraction 78.435 mg/kg，n-butanol fraction 53.865 mg/kg and water fraction 76.545 mg/kg），once a day ，for conse- cutive 2 weeks，and then stopped taking drug for 2 weeks； rats in the blank group were given equal volume of 1.0％ . sodium carboxymethyl cellulose solution intragastrically. Duringthe experiment ，the general conditions of rats were observed. The samples of urine （on the 14th and 28th day ），serum and bilateral renal tissues （on the 15th and 29th day ）were taken respectively，the renal index was calculated ，the levels of @qq.com renal function indexes in serum and urine were detected ，and the pathomorphological changes of renal tissues were observed. RESULTS During administration ，compared with blank group ，the rats in the total ethanol extract group and ethyl acetate fraction group showed poisoning behavior and activity characteristics such as mental depression ，decreased activity and diet ，thin stool and decreased body mass. The mental state of the rats in the petroleum ether fraction group ，n-butanol fraction group and water fraction group were slightly worse than that in blank group，and slightly decreased activity and diet as well as thin stool ，and slowly increased body mass were found ；however，there was no significant difference in anal temperature in each group. After 2 weeks of administration ，the renal index in total ethanol extract group ，the serum levels of N-acetylglucosaminidase（NAG），urea nitrogen （BUN）and creatinine （Cr）in total ethanol extract group and ethyl acetate fraction group ，serum level of NAG in n-butanol fraction group and serum level of Cr in water fraction group ，as while as NAG levels in urine of rats in total ethanol extract group and petroleum ether fraction group ，NAG and urinary protein levels in urine of rats in ethyl acetate fraction group were increased significantly （P＜0.05 or P＜0.01）. In the pathomorphological observation ，renal tubules showed different degrees of unclear structure ，cell swelling and a few cell necrosis in the total ethanol extract group ，petroleum ether fraction group and ethyl acetate fraction group ，accompanying by glomerular pyknosis，renal tubular sclerosis and inflammatory cell infiltration ，compared with blank group. After drug withdrawal ，the mental state of rats in the administration groups were significantly improved ，the amount of activity and diet increased ，and the stool tended to be normal. Two weeks after drug withdrawal and recovery ，the levels of above indexes in serum and urine of rats in administration groups returned to be close to that in blank group （P＞0.05）；the glomerular structure of rats in each administration group gradually recovered clearly ，and cell swelling and inflammatory cell infiltration were rare in total ethanol extract group ， petroleum ether fraction group and ethyl acetate fraction group. CONCLUSIONS The total ethanol extract ，petroleum ether fraction and ethyl acetate fraction of Miao medicine W. indica have certain nephrotoxicity and reversibility. The toxic component may

Anti-tumor Effect of Draconis Sanguis Petroleum Ether Fraction on Human Gastric Cancer HGC-27 and MGC-803 Cells / 中国实验方剂学杂志

ObjectiveTo investigate the effect of Draconis Sanguis petroleum ether fraction （DSPEF） on the proliferation， apoptosis， migration， and autophagy of human gastric cancer HGC-27 and MGC-803 cells， and preliminarily elucidate its molecular mechanism. MethodCell counting kit-8 （CCK-8） assay was used to detect the effect of DSPEF at different concentrations （0， 20， 40， 60， 80 mg·L-1） on the proliferation of HGC-27 and MGC-803 cells after 24， 48， 72 h. Hoechst staining and flow cytometry were used to explore the effects of DSPEF at different concentrations on the apoptosis and apoptosis rate of HGC-27 and MGC-803 cells after 48 h treatment， respectively. The wound healing assay and acridine orange staining were used to investigate the effects of DSPEF on the migration and autophagy of HGC-27 and MGC-803 cells， respectively. Western blot was used to detect the expression levels of signaling pathway-related proteins in HGC-27 and MGC-803 cells treated with DSPEF for 48 h. ResultCompared with the control group， DSPEF（30 mg·L-1） inhibited the proliferation and migration of HGC-27 and MGC-803 cells in a concentration- and time-dependent manner （P<0.05）， and induced the apoptosis （P<0.01） and autophagy of HGC-27 and MGC-803 cells. DSPEF （60 mg·L-1） down-regulated the protein levels of phosphorylated mammalian target of rapamycin （p-mTOR） （P<0.05， P<0.01） and down-regulated phospho-signal transducer and activator of transcription 3 （p-STAT3） in HGC-27 and MGC-803 cells （P<0.01）， suggesting that DSPEF presumedly inhibited the proliferation and migration of human gastric cancer HGC-27 and MGC-803 cells and induced their apoptosis and autophagy by inhibiting the mTOR/STAT3 signaling pathway. ConclusionThe down-regulation of the mTOR/STAT3 signaling pathway may be involved in the anti-gastric cancer effect of DSPEF. This study is expected to provide a reference for the investigation of the anti-tumor effect of Draconis Sanguis.

Four new diphenyl ether derivatives from a mangrove endophytic fungus Epicoccum sorghinum / 中国天然药物

Four new diphenyl ethers, named epicoccethers K-N (1-4), were purified from the fermentation medium of a fungus Epicoccum sorghinum derived from Myoporum bontioides, and identified through HR-ESI-MS and NMR spectral analysis. Except that compound 1 showed moderate antifungal activity against Penicillium italicum and Fusarium graminearum, the other three compounds showed stronger activity against them than triadimefon. All of them showed moderate or weak antibacterial activity towards Staphylococcus aureus and Escherichia coli with O6 and O78 serotypes except that 3 was inactive to E. coli O6.

Protective effects of active compounds from on heart and brain of mice at simulated high altitude / 浙江大学学报·医学版

To investigate the active compounds from on the heart and brain of mice at simulated high altitude.Fifty healthy male adult BALB/c mice were randomly divided into normal control group, hypoxic model group, acetazolamide group, petroleum ether extract of (PESI) group and octacosan group with 10 mice in each group. Acetazolamide group, PESI group and octacosan group were treated with acetazolamide PESI (200 mg/kg) or octacosan by single tail vein injection, respectively. Except normal control group, the mice were exposed to a simulated high altitude of for in an animal decompression chamber. After the mice were sacrificed by cervical dislocation, the heart and brain were histologically observed by HE staining; superoxide dismutase (SOD) activity, total anti-oxidant capacity (T-AOC) and the content of malondialdehyde (MDA) in plasma, heart and brain tissues were detected by WST-1 method, ABTS method and TBA method, respectively; lactic acid and lactate dehydrogenase (LDH) activity in plasma, heart and brain tissues were detected by colorimetric method and microwell plate method, respectively; ATP content and ATPase activity in heart and brain tissues were detected by colorimetric method. PESI and octacosane significantly attenuated the pathological damages of heart and brain tissue at simulated high altitude; increased SOD activity, T-AOC and LDH activity, and decreased the contents of MDA and lactic acid in plasma, heart and brain tissues; increased the content of ATP in heart and brain tissues; increased the activities of Na-K ATPase, Mg ATPase, Ca ATPase and Ca-Mg ATPase in myocardial tissue; and increased the activities of Mg ATPase, Ca-Mg ATPase in brain tissue. PESI and octacosan exert anti-hypoxic activity by improving the antioxidant capacity, reducing the free radical levels, promoting the anaerobic fermentation, and alleviating the energy deficiency and metabolic disorders caused by hypoxia in mice.

Chemical constituents from the stem of Callerya nitida Benth.var.hirsutissima Z.Wei / 中国药科大学学报

@#The chemical constituents from 70% ethanol petroleum ether and n-butanol extractions of Callerya nitita Benth.var.hirsutissima.Z.Wei. were separated by preparative high-performance liquid chromatographic techniques, including repeated column chromatography over macroporous adsorption resin, silica gel, ODS, Sephadex LH-20. The structures of the compounds were identified by their physicochemical properties, spectral data, and mass spectrometry data, in comparison with literature. In our research, one triterpenoids, taraxerone (1), and twenty flavonoids, including genistein-4′-O-β-glucoside (2), 5-hydroxy-4′-methoxyisoflavone-7-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (3), biochanin A 7-O-β-D-apiofuranosyl-(1→5)-β-D-apiofuranosyl- (1→6)-β-D-glucopyranoside (4), formononetin-7-O-β-D-galactopyranoside (5), 5,7-dihydroxy-3′,4′-dimethoxyisoflavone (6), biochanin A-7-O-β-D-apiofuranosyl-(1→2)-β-D-glucopyranoside (7), 5, 7-dihydroxyisoflavone-4′-O-α-L-rhamnopyranosyl-(1→2)-O-β-D-glucopyranoside (8), formononetin-7-O-D-apio-β-D-furanosyl(l→2)-β-D-glucopyranoside (9), 4′-hydroxy-3′-methoxyisoflavone-7-O-β-D-apiofuranosyl-(1→6)-β-D-glucopyranoside (10), prunetin (11), prunetin 4′-O-β-D-glucopyranoside (12), pratensein7-O-β-D-glucoside (13), 8-methoxyisoformononetin (14), genistein (15), 3′-hydroxybiochanin A (16), biochanin A (17), 5,7-dihydroxy-3′,5′-dimethoxyisoflavone (18), ononin (19), isoformononetin (20), 5,7,3′,4′-tetrahydroxyflavone (21) were isolated from the two extract parts.Compounds 1-10, 12-14, 16-18, 20 were obtained from this plant, and it is the first time to investigate the plant for the first time.

Effects of 2,2',4,4' -tetrabromodiphenyl ether on differentiation of mouse 3T3-L1 cells / 预防医学

Objective@#To investigate the effects of 2, 2', 4, 4'-tetrabromodiphenyl ether ( BDE-47 ) on the differentiation of mouse embryonic fibroblasts-3T3-L1, so as to provide the basis for revealing the mechanism of environmental obesity factors. @*Methods@#The 3T3-L1 cells were divided into five BDE-47 intervention groups ( 25, 18.75, 12.5, 7.5 and 2.5 µmol/L ), a positive control group (1 µmol/L 2, 4-thiazolidinedione) and a negative control group ( 0.1% dimethyl sulfoxide ) for the induction of differentiation. The lipid droplet accumulation in adipocytes was observed by oil red O staining treatment and detection of optical desity ( OD ) on the eighth day of differentiation. Triglyceride ( TG ) content was measured using the histiocyte TG enzymatic assay kit. The mRNA expression of adiponectin and peroxisome proliferator activated receptor-γ ( PPARγ ) was measured by RT-PCR.@*Results@#The positive areas of oil red O staining, OD values, TG content and mRNA expression of adiponectin and PPARγ in 3T3-L1 cells were significantly different among seven groups ( P<0.05 ). The positive areas of oil red O staining and OD values in the BDE-47 groups with different concentrations were higher than those in the negative control group ( P<0.05 ). The 18.75 µmol/L BDE-47 group had higher TG levels than the negative control group ( P<0.05 ). The mRNA expression of PPARγ in the 25, 18.75, 12.5, and 7.5 µmol/L BDE-47 groups and the positive control group was higher than that in the negative control group ( P<0.05 ). The mRNA expression of PPARγ in the 12.5 µmol/L BDE-47 group was higher than that in the 25, 18.75, 7.5, 2.5 µmol/L BDE-47 group and the positive control group ( P<0.05 ). The mRNA expression of adiponectin in the 12.5, 7.5 µmol/L BDE-47 group and the positive control group was higher than that in the negative control group ( P<0.05 ). The mRNA expression of adiponectin in the 12.5 µmol/L BDE-47 group was higher than that in the 25, 18.75, 2.5 µmol/L BDE-47 group ( P<0.05 ). The mRNA expression of PPARγ and adiponectin in the different concentration groups of BDE-47 distributed like inverted "U" shape.@*Conclusion@#BDE-47 can promote the differentiation of 3T3-L1 preadipocytes. Low concentration of BDE-47 may induce adipocyte differentiation by activating PPARγ.

Biomechanical Study of PEEK Condyle Prosthesis Printed by Fused Deposition Modeling and Selective Laser Sintering / 医用生物力学

Objective To make finite element analysis and compressive performance test on three-dimensional (3D) printed personalized poly-ether-ether-ketone (PEEK) condyle prosthesis, so as to analyze stress distribution characteristics and mechanical properties of the prosthesis, and to evaluate its clinical value and prospect. Methods The finite element models of PEEK condyle prosthesis, mandible and fixation screw were established by software such as CBCT, Mimics, Geomagic Studio, SolidWorks and ANSYS Workbench. The maximum mastication force was applied, and the maximum stress of the condyle prosthesis and screw, as well as the stress and strain of the mandible were recorded. In order to simulate the actual clinical situation, a special fixture was designed to test compression performance of the condyle prosthesis prepared by the fused deposition modeling (FDM) and selective laser sintering (SLS) at the rate of 1 mm/min. Results The peak stress of the PEEK condyle prosthesis was 10.733 MPa, which was located at the back of the condyle neck. The peak stress of 5 fixing screws was 9.707 5 MPa, which appeared on the 2# and 5# screws near the trailing edge of the mandibular ascending branch. The peak stress of both the prosthesis and the screw was smaller than its yield strength. The maximum pressure of the condyle prosthesis prepared by FDM and SLS was (3 814.7±442.6) N and (1 193.970±260.350) N, respectively. Compared with the SLS preparation, the FDM prepared prosthesis not only had higher compression strength but also better toughness. Conclusions The 3D printed personalized PEEK condyle prosthesis shows uniform stress distributions and good mechanical properties, which can provide the theoretical basis for PEEK as reconstruction material for repairing temporomandibular joint.

Research progress on rutin derivatives / 中国中药杂志

Compounds derived from natural products present satisfactory efficacy in disease prevention and treatment. The use of chemical substances in plants to promote healthhas increasingly attracted people's attention. Rutin, a typical flavonoid, is mainly found in various vegetables, fruits and Chinese herbal medicines. As a natural antioxidant, it features many pharmacological activities, such as anti-inflammation, anti-virus, anti-tumor, and prevention and treatment of cardiovascular and cerebrovascular diseases. However, the low bioavailability and poor water solubility limit its clinical application. In view of this, its structure is optimized and modified to afford rutin derivatives with good solubility, high bioavailability, stable metabolism and small toxic side effects. So far, a large number of rutin ethers, esters, and complexes have been synthesized and undergone activity testing. This paper reviews the structural modification of rutin in recent years, and the obtained derivatives have excellent properties and significant biological activity.

Comparing the Effect of Methods of Rat Euthanasia on the Brain of Wistar Rats: Cervical Dislocation, Chloroform Inhalation, Diethyl Ether Inhalation and Formalin Inhalation

Contentions still exist as to the most humane method of sacrificing experimental animals. Beyond humaneness, there is also the issue of appropriateness of a method of sacrifice with regards to organ safety. This study compared four common methods of rodent sacrifice used in Nigeria and their effects on the brain. Twenty male Wistar rats weighing 150 to 180g were randomly separated into four groups of five rats each. After a two week period of acclimatization,the animals were sacrificed; Group A by Cervical dislocation (CD) which also served as control, Group B by chloroform inhalation (CI), Group C by diethyl ether inhalation (DEI) and group D by Formalin inhalation (FI). The time taken for the animals to pass out was documented and the brains were harvested. Four of the brains from rats in each group were homogenized in phosphate buffer solution and centrifuged at 10000rpm. The supernatant were used for antioxidant studies. The remaining one brain from each group were fixed in 10% formal saline and after 48 hours, the cerebellum (CB) and hippocampus (Hp) were used for histological studies using the H & E method. Our results show although CD was the quickest, it gave the least quantity of blood. Meanwhile CI was the most humane, gave the most blood and saved time compared to DEI and FI. None of the methods of sacrifice showed adverse effect on the antioxidant parameters of the rats. However, histological studies showed that while CD and CI showed no adverse effects on the hippocampus, only CD was completely safe for the CB. The other methods showed various levels of cell death. It is therefore expedient to consider these factors in making the choice of an appropriate method of sacrifice and to use the most humane and safest method with reference to the organ studied

Preliminary Screening of Polybrominated Diphenyl Ethers (PBDEs); Decabromodiphenyl Ether (BDE-209) and Tetrabromobisphenol-A (TBBPA) Flame Retardants in Municipal Dumpsite in Delta State, Nigeria

Aims: This study is aimed at determining the concentration of two widely used BFRs; Decabromodiphenyl Ether (BDE-209) and Tetrabromo Bisphenol-A (TBBPA) in sediment and leachate samples. Place and Duration of Study: Field sampling were carried out from five major dumpsites around Warri Municipality, Delta State, Nigeria. Analyte extraction was done in 2017 at the Science laboratory, Federal University of Petroleum Resources, Effurun Delta State, Nigeria and quantification done in Switzerland by Bachema Analytical Laboratories in 2017. Methods: Three soil samples were collected from each site 15cm from the soil surface. Also, three leachate samples from three different trial pits done for each site. Collected soil samples were stored in glass bottles and labelled. While the leachate samples are stored using glass containers and labelled. The BFRs were extracted using Aceton and cyclohexane for each soil matrix and cyclohexane for the leachate samples, then the extract was analysed using GC coupled with an ECD supplied by Thermo Trace GC Ultra, Italy. Results: The results showed the average concentration for TBBPA in the sediments was 0.0234 g/kg and that of the BDE-209 was recorded as 0.1828 g/kg. Results from the leachate sample were below the detectable range of the analytical equipment, TBBPA (0.02 g/kg) and BDE (0.1 g/kg). There is no statistical difference between the mean concentration of TBBPA for the sediment in each of the locations (P>.05) and no difference (P>.05) for BDE-209 for the sediment in each of the locations (P>.05). Conclusion: Findings from this study holds that the concentration of TBBPA and BDE-209 in sediment is higher when compared with concentrations presented in other literatures studied in this report and this calls for immediate action due to the health risk associated with exposure in these municipalities.

G604S-HERG mutation in LQT2 leads to autophagy via the UPR-related pathway

Congenital long QT syndrome (LQTS) is a heart channel disease associated with fatal ventricular arrhythmiasor cardiac arrest. Human ether-a-go-go-related gene (HERG) mutation is one of the main causes in type 2LQTS since it may lead to abundant immature HERG channel protein accumulate in the endoplasmic reticulum(ER). In our study, we have successfully constructed the G604S-HERG mutation in HEK293 cells anddemonstrated that the immature HERG protein on ER via Western blot and immunofluorescence. Herein wefound that unfolded protein reaction (UPR) process has been activated in order to counter this endoplasmicreticulum stress (ERS) since the main sensors got upregulated. Meanwhile, autophagy was also observed inthis process and verified by Western blot and transmission electron microscopy. To explore the relationshipunderlying autophagy and UPR in the condition of ERS, we found that PERK-EIF2a-CHOP axis was activated. Our findings provides insight for G604S-HERG mutation in type 2 LQTS.

Anestesia de roedores sigmodontinos en condiciones de campo / Anesthesia in Sigmodontinae Rodents Living out in the Countryside

Resumen Algunas investigaciones de mamíferos silvestres requieren del uso de métodos que faciliten la manipulación de los individuos en condiciones de campo, sin afectar negativamente a los animales o a los investigadores. Dentro de estos métodos, se encuentra la inmovilización química, la cual no ha sido muy documentada en roedores silvestres de la subfamilia Sigmodontinae (Cricetidae). Por ello, en esta investigación se evaluó el uso de éter dietílico inhalado para manipular roedores sigmodontinos en campo, comparando el tiempo de inducción y el tiempo de recuperación de la anestesia entre especies, sexos y tipos de ambientes. Se capturaron y anestesiaron un total de 289 individuos de seis especies en el Parque Nacional Natural Chingaza. El tiempo de inducción de la anestesia fue diferente entre Microryzomys minutus, Neomicroxus bogotensis, Thomasomys laniger y Thomasomys niveipes (F3; 552 = 9,36; p < 0,05); de igual forma, el tiempo de recuperación de la anestesia fue diferente entre dichas especies (H = 9,59; p = 0,022). No se encontraron diferencias en los tiempos de inducción y recuperación de la anestesia entre sexos, ni entre ambientes. La mortalidad total fue de 4,5 %. No se observaron secreciones mucosas, vómito o complicaciones cardíacas o respiratorias en los individuos anestesiados. Los individuos fueron recapturados y no se evidenciaron alteraciones en su comportamiento o aspecto físico que indicaran una afectación por la anestesia o manipulación en capturas previas. La anestesia inhalada con éter dietílico puede ser una opción rápida y segura para inmovilizar y manipular sigmodontinos durante procedimientos cortos en campo dentro de estudios poblacionales o programas de monitoreo en vida silvestre.

Abstract Some researches in wild mammals require methods that enable to handle the animals living in wild conditions, without affecting negatively the animals, or the researchers. These methods include the chemical immobilization, which has not been enough documented when handling wild rodents of the Sigmodontinae subfamily (Cricetidae). Therefore, this research evaluated the use of diethyl ether when handling Sigmodontinae rodents out in the countryside. It compared the induction time to the anesthesia recovery time between species, genders, and type of environments. A total of 289 animals were caught and anesthetized from six species in the Chingaza National Natural Park. The anesthesia induction times were different between Microryzomys minutus, Neomicroxus bogotensis, Thomasomys laniger y Thomasomys niveipes (F3; 552 = 9.36; p < 0.05). Likewise, the anesthesia recovery times were different between the same species (H = 9.59; p = 0.022). No difference was found in the induction times and the anesthesia recovery times between genders, neither for the types of environment. Total mortality was 4.5%. None mucosal secretions, vomit, or cardiac/respiratory complications were observed in the anesthetized animals. These subjects were caught again and they did not show any alterations in their behavior or physical aspect indicating affection derived either from the anesthesia or the previous handling under captivation. Anesthesia with diethyl ether can be a quick and safe choice when it comes to immobilize and handle Sigmodontinae rodents during short procedures out in the countryside, when carrying out population studies or wildlife monitoring programs.

Formulation Development, Characterization and In-vitro Evaluation of Tamoxifen Loaded Liposomes

Background: The study was aimed to prepare and evaluate tamoxifen loaded controlled release liposomes to reduce the side effects of tamoxifen during cancer treatment. Methods: Different tamoxifen loaded liposomes were prepared by modified ether injection (MEIM) and thin film hydration method (TFHM) under prescribed conditions. The prepared liposomes were characterized by using optical microscopy, evaluating encapsulation efficiency, in-vitro and ex-vivo diffusion studies by using dialysis membrane and chicken intestinal sac respectively.Results: The data revealed that all of the liposomes were spherical in shape and stable under three physical conditions i.e. 4, 25 and 37 ± 2°C temperatures and 60 ±5% relative humidity. Additionally most of the liposomes followed zero order and class II release kinetics. It was also observed that with the increase of phospholipids and cholesterol, entrapment efficiency of liposome vesicles increased thus giving a controlled release drug delivery system but further increase reduced this efficiency at a certain level.Conclusion: The formulated control release liposomes might be a good drug delivery system for target oriented drug delivery with minimum side effects of tamoxifen during cancer treatment

Design, synthesis and antitumor activities of chlorin p6 ether derivatives as photosensitizer for photodynamic therapy / 药学实践杂志

Objective To designe, synthesize a series of chlorin p6 ether photosensitizers and preliminarily investigate their photodynamic antitumor activity based on previous research results that alkoxyl ether derivatives of 3-vinyl on chlorin f exhibited stronger photosensitive antitumor activity than parent compound. Methods Purpurin-18 (4) was obtained by oxidative degradation with air and alkali on pheophorbide a (5) which was prepared through acid hydrolysis of chlorophyll a from crude chlorophyll extracts in Chinese traditional herb named Silkworm excrement. Then, chlorin p6 trimethylester (2) were formed via basic hydrolysis of internal anhydride ring for lead compound 3 and following immediately methylation with CH2N2. The intermediate 2 reacted with 33% HBr, following nucleophilic substitution with various alkoxyl alcohol to get six title compounds (1). All title compounds were subjected to photodynamic antitumor activity screening for melanoma B16-F10 cell in vitro. Results All title compounds showed much higher phototoxicity against melanoma B16-F10 cells than talaporfin and verteporfin. Their structures were confirmed by 1H-NMR, 13C-NMR, ESI-MS and ESI-HRMS spectra. Conclusion Chlorin p6 ether compounds were promising candidate photosensitizers for PDT applications due to theirs high dark toxicity/phototoxicity ratio and excellent phototoxicity, which were worthy of further research and development.

Determination of 1-methoxy-2-propanol in urine by headspace solid-phase microextraction coupled with gas chromatography / 中华劳动卫生职业病杂志

Objective@#To establish a method for the determination of 1-methoxy-2-propanol in urine using headspace solid phase micro-extraction coupled with gas chromatography.@*Methods@#The 1-methoxy-2-propanol was enriched by headspace solid phase micro-extraction fiber coated with carbene/polydimethylsiloxane (CAR/PDMS) . Single factor rotation method was used to optimize the conditions of extraction temperature, salt amount, and extraction time. The separation was performed on DB-5 (30 m×0.32 mm×0.25 μm) capillary column and detected with flame ionization detector. The quantification was based on the standard curve.@*Results@#The concentration of 1-methoxy-2-propanol in urine was linear in the range of 0.50-10.0 mg/L, and the linear correlation coefficient was 0.9993. The detection limit of the method was 0.14 mg/L, and the limit of quantification was 0.45 mg/L. The recovery was 85.8% to 104.7%, and the RSD of intra- and inter-batch precision were 3.25%-6.65% and 0.81%-3.96%, respectively.@*Conclusion@#The method is high sensitivity and simple operation, and is suitable for the determination of 1-methoxy-2-propanol in urine of occupational exposure population.

Anti-tumor Constituents from Rhizome of Euphorbia fischeriana / 中国实验方剂学杂志

Objective::To screen out active fraction from Euphorbia fischeriana, separate active components from E. fischeriana and explore structure-activity relationships, in order to analyze and identify chemical compositions of petroleum ether fraction from E. fischerian ethanol extract by ultra-performance liquid chromatography with quadrupole-time-of flight mass spectrometry (UPLC-Q-TOF-MS). Method::The anti-tumor activities of petroleum ether, ethyl acetate, n-butanol and water extracts from E. fischeriana were tested by methyl thiazolyl tetrazolium(MTT)method. A variety of modern chromatographic separation methods were used to separate active compounds from petroleum ether layer. Compounds were isolated. Their structures were identified by NMR technique. The structure-activity relationships between anti-tumor activities and structures of compounds were investigated. UPLC-Q-TOF-MS technique was used to identify the structures of petroleum ether extract from E. fischeriana. Mass spectrometry was performed in the positive ion mode using ESI ion sources. Result::Six compounds were isolated from petroleum ether fraction. They were jolkinolide A, jolkinolide B, 17-hydroxyjolkinolide A, 17-hydroxyjolkinolide B, euphopilolide and atis-16-en-13(s)-hydroxy-3, 14-dione. A total of 23 peaks were identified based on the comparison of retention times, accurate masses and fragmentation patterns with available standard compounds and literatures. Among them, there were 19 diterpenoids, 2 polyphenols, 1 fatty acid and 1 triterpenoid. Peaks No.18 and No.21 were tentatively identified as new compounds. Conclusion::The petroleum ether fraction showed a potential anti-tumor activity. The structure-activity relationships were discussed. UPLC-Q-TOF-MS technology can be used to quickly and accurately identify the structures, so as to provide a reference for its quality evaluation and active ingredient research.

Qualitative and quantitative analysis of trace element of terpenoid conjugated curcuminoid and curcuminoids in herbal medicine derived from different Curcuma species / 中草药

Objective: To qualitatively and quantitatively analyze the terpene-conjugated curcuminoid compound- Bisabolocurcumin ether (BCE) in Curcuma species. Methods: UPLC-Q-TOF-MS/MS was used to establish a qualitative analysis of BCE, and its distribution in Curcuma species was studied. UPLC was used to establish quantitative analysis of BCE and three main curcuminoids in three Curcuma species (Rhizoma Curcumae Longae, HuangsiYujin, Curcuma phaeocaulis), in order to study the difference of BCE content in different Curcuma species and its content difference with other curcuminoids. Results: In the qualitative analysis, by analyzing the primary, secondary pyrolysis fragments and the cracking law of BCE, it was found that only Jianghuang and HuangsiYujin contained it, but BCE could not be detected in the PengEzhu. In the quantitative analysis, BCE and the three main curcuminoids had good linear relationship in their linear range (r ≥ 0.999 3); The average recovery rates were in range of 99.407%-113.631%, and RSD < 4%. It was found that the content of three curcuminoids in Jianghuang were significantly higher than the other two herbs, and the content of BCE in the three herbs was very different. The BCE content in Jianghuang was four times than that of HuangsiYujin. Conclusion: The qualitative and quantitative analysis methods established in this study can provide reference for the discovery and analysis of more novel BCE structure’s compounds, and provide a basis for improving the quality standards of Curcuma species.