Bioactive A-ring rearranged limonoids from the root barks of Walsura robusta

Screening active natural products, rapid identification, and accurate isolation are of great important for modern natural lead compounds discovery¹. We hereby reported the isolation of seven new neotecleanin-type limonoids (17), seven new limonoids with 5-oxatricyclo[5.4.0.11., 4.]hendecane ring system (814), and two new precursors (1516) together with four known limonoids (1720) from the root barks of Walsura robusta. Their structures, including their absolute configurations, were elucidated based on analyses of HR-ESI-MS, 1D/2D NMR, ECD spectrum calculations and single-crystal X-ray diffraction techniques. Compounds 2, 8, 9, 11, 13, 14, 18 showed significant anti-inflammatory activities in LPS-induced RAW 264.7 cell line, BV2 microglial cells, and Propionibacterium acnes-stimulated THP-1 human monocytic cells. Walrobsin M (11) exhibited anti-inflammatory activity with IC₅₀ value of 7.96±0.36 μmol/L, and down-regulated phosphorylation levels of ERK and p38 in a dose-dependent manner.     

Lessons on health promotion from Japanese early childhood development

Early childhood development (ECD) has received increasing attention in both developed and developing countries since the 1990s. In Japan, ECD facilities have pursued integrated practices of education and health care to provide appropriate services to promote children’s welfare. This ECD approach appears to embody objectives of health promotion in young children. Therefore, information about Japanese practices may help to support ECD in other countries, especially developing countries. In this context, the present study discussed the potential application of health‐related ECD practices in Japan for developing countries by reviewing an outline of Japanese ECD, along with a case study describing practices in ECD facilities in Japan. We identified four main points: (i) distinct legal grounds including a legal basis for allocating health specialists; (ii) outlines of activities based on national standards and flexible practices at the facility level; (iii) teachers’ attitudes that respect children’s initiative, and explicit and independent activities embedded in children’s daily lives that reflect the child’s developmental status; and (iv) various useful practices to enhance the effect of health‐related activities, such as cooperation with parents, lesson study and hoiku‐ (teachers) conference. As these practices are based on the Japanese context, it is essential to consider both the Japanese context and potential risks of transplanting such concepts, to enable optimum use of these lessons in other countries.     

唾液中氰离子的五氟苄基溴衍生气相色谱法测定

目的 建立用五氟苄基溴(PFB-Br)衍生气相色谱法,电子捕获检测器(ECD)定量测定唾液中氰离子(CN^-)的方法。方法 取微量唾液,加入缓冲溶液后用乙腈稀释定容,加入定量的PFB-Br摇匀,沸水浴30.0 min进行衍生反应,冷却后直接进样入气相色谱仪分离,以ECD检测器检测。结果 唾液中CN^-的质量浓度在0.25~200.0 mg/L呈线性关系,线性相关系数为0.999 4;以100.0 μl唾液量计算,方法最低检出浓度为0.07 mg/L,最低定量浓度为0.25 mg/L;方法的批间精密度为2.4%~5.3%(n=6),批内精密度为1.1%~3.8%(n=6),加标回收率为100.7%~102.1%。唾液常见的无机离子Cl^-、F^-和SCN^-对测定结果均无干扰。样品可在4 ℃保存至少15 d。结论 该方法适用于唾液中氰离子测定,对氰化物中毒的应急检测有应用价值。     

High levels of soluble GPR56/ADGRG1 are associated with positive rheumatoid factor and elevated tumor necrosis factor in patients with rheumatoid arthritis

Background

GPR56/ADGRG1 is a member of the adhesion-class G protein-coupled receptor (aGPCR) family important in brain development, oncogenesis and tumor metastasis. Like other aGPCRs, GPR56 is cleaved at the GPCR proteolysis site (GPS) motif into an N-terminal fragment (NTF) and a C-terminal fragment (CTF). Existence of soluble GPR56 (sGPR56) has been shown in vitro, however the underlying mechanism and its pathophysiologic role remains undetermined.

An evaluation of kurtosis beamforming in magnetoencephalography to localize the epileptogenic zone in drug resistant epilepsy patients

Objective

Kurtosis beamforming is a useful technique for analysing magnetoencephalograpy (MEG) data containing epileptic spikes. However, the implementation varies and few studies measure concordance with subsequently resected areas. We evaluated kurtosis beamforming as a means of localizing spikes in drug-resistant epilepsy patients.

Fifteen-Year Follow-up After Anterior Chamber Phakic Intraocular Lens Implantation in One and LASIK in the Fellow Eye

Purpose: To report a patient fifteen years after anterior chamber phakic intraocular lens (AC-PIOL) implantation in one and laser in situ keratomileusis (LASIK) in the fellow eye.

Methods: Case report.

Results: A 56-year-old male underwent AC-PIOL implantation in one eye and LASIK in the fellow eye fifteen years ago. Preoperative uncorrected visual acuity (UCVA) was finger count in both eyes. Preoperative best spectacle-corrected visual acuity (BSCVA) was 20/25 (?16.75 ?0.50?×?40) in the LASIK eye and 20/32 (?24.50 ?0.50?×?90) in the AC-PIOL eye. Fifteen years postoperatively, UCVA was finger count in the LASIK eye and 20/200 in the AC-PIOL eye, while BSCVA was 20/32 and 20/25, respectively. Endothelial cell density (ECD) was 2020±47 in the LASIK eye and 945±22 in the AC-PIOL eye.

Conclusion: Both procedures had similar visual outcomes. Furthermore, lower ECD was found in the AC-PIOL eye in comparison to the LASIK eye.     

Synthesis of S‐thiomethyl DMSA and S‐thiomethyl ECD,radiolabelling with technetium‐99m and biological evaluation

Protection of the thiolate function of dimercaptosuccinic acid (DMSA) and ethylenedi‐l ‐cysteine diethyl ester (ECD) by S‐thiomethylation allowed automatic deprotection during technetium‐99m (^99mTc) radiolabelling by direct reduction with stannous chloride dihydrate. Protection of the free thiolate group increased the stability of the ligands as well as deprotection during complexation, which resulted in the desired radiopharmaceuticals. The complexes obtained from the protected ligands were chromatographically (HPLC) and biologically compared with the corresponding ^99mTc complexes of the unprotected ligands. The results suggest that the aforementioned method of protection by S‐thiomethylation could be utilized for the development of single‐vial DMSA and ECD kit. Copyright © 2012 John Wiley & Sons, Ltd.     

99mTc - ECD的正常脑分布模式

目的:探讨~(99)Tc-ECD在正常成人脑中的分布模式,这种分布在个体间的变异情况,在不同部位的分布与年龄、性别的关系以及目测分析与常用半定量分析方法的相关性。方法:对34例健康志愿者(年龄范围20～74岁,平均年龄35.03±11.81岁)行~(99)Tc-ECD SPECT脑血流灌注显像。选相应横断面图像分别在与左右小脑、下中额、下侧额、额颞部、颞枕部、下枕部、尾状核、壳核、中额部、中侧额、上额颞、上后颞、上枕部、距状裂、上中额、上侧额、感觉区、侧顶部及上距状裂相当的部位勾画38个感兴趣区(ROI),求出每个ROI内的每像素平均计数值。分别计算各ROI平均计数与双侧小脑平均计数比值和与脑皮质平均计数的比值。同时,采用7级评分法,分别由3位核医学医师对上述ROI部位的图像进行评分。然后,对各部位目测分析及半定量分析的数据进行统计比较。结果:~(99)Tc-ECD在脑不同部位中的分布差异较大,根据目测评分的结果,评分范围+3分～-1分。评为3分最多的部位依次为上距状裂、下距状裂和小脑,评为-1分最多的部位依次为壳核、上枕部、下枕部和颞枕部。但ECD在相同部位的个体间差异却较小,应用平均计数与小脑平均计数比值、平均计数与脑皮质总平均计数的比值及左右各对应部位平均计数的比值进行分析,其平均CV分别为9.06％、6.5     

脑膜瘤99Tcm-MIBI与99Tcm-ECD SPECT脑显像的对照研究

目的探讨脑膜瘤99Tcm-MIBI 和99Tcm-ECD SPECT 脑显像的影像特征,并评价其应用价值.方法对10例正常对照者及18例脑膜瘤患者进行99Tcm-MIBI和99Tcm-ECD SPECT脑显像;分析病灶的影像特征.结果正常对照者99Tcm-MIBI显像脑实质内均无核素浓聚;99Tcm-ECD 显像脑实质内放射性核素分布大致均匀,左右侧基本对称.18例脑膜瘤99Tcm-MIBI显像见肿瘤处均表现为均匀的圆形或卵圆形放射性核素浓聚,其阳性率为100%;而99Tcm-ECD显像18例中有17例示肿瘤处表现为形态规整、边缘整齐的圆形或卵圆形内凹缺损,其形态与99Tcm-MIBI显像所示的浓聚区相吻合,另1例为假阴性结果,其阳性率为94.4%.结论 99Tcm-MIBI结合99Tcm-ECD SPECT脑显像可用于脑膜瘤的辅助诊断.