Combined spectroscopy methods and molecular simulations for the binding properties of trametinib to human serum albumin

Trametinib is a novel anticancer drug for treating metastatic cutaneous melanoma. The present study probed into the binding of trametinib to human serum albumin (HSA) through spectroscopy methods and molecular simulations. Trametinib could quench the fluorescence of HSA through static quenching which could be probed via fluorescence spectroscopy and time-resolved fluorescence. Thermodynamic parameters and docking results indicated that hydrogen bonds and van der Waals forces play crucial roles in this binding process, which exerts almost no effect on the HSA conformation under synchronous fluorescence, three-dimensional fluorescence, circular dichroism spectra, and molecular dynamics simulations. Site marker displacement experiments and molecular docking reveal that trametinib primarily binds to Sudlow site I of HSA. In addition, the trametinib–HSA interaction was hardly influenced by varying amino acid (glutamine, alanine, glycine, and valine) concentrations. This study can provide useful information for the pharmacokinetic properties of trametinib.

Probing the binding properties of trametinib to human serum albumin.     

骨代谢指标测定在骨质疏松诊治中的应用价值

目的 比较妇女绝经前后骨代谢指标的变化，研究各指标在骨质疏松症治疗后的变化率，对各指标在骨质疏松症诊治中的应用作出初步评价。方法 48例绝经前妇女、48例绝经后妇女测定10项骨代谢指标．45例绝经后骨质疏松症患者．治疗前、治疗6个月后分别测定10项骨代谢指标，观察其变化率。12名绝经后妇女，每两个月测定10项骨代谢指标。共观察一年。结果 绝经后妇女骨代谢指标明显升高，绝经后骨质疏松症患者经抗吸收治疗后．大部分骨代谢指标明显降低，血清骨形成指标比尿骨吸收指标长期个体内的变异要小。结论 绝经后骨质疏松症患者骨转换加快，部分血清骨代谢指标优于尿骨代谢指标，尤以血清骨形成指标N—mid骨钙素和血清骨吸收指标CTX为优。     

Rhizovagine A,an unusual dibenzo-α-pyrone alkaloid from the endophytic fungus Rhizopycnis vagum Nitaf22

Rhizovagine A (1), a novel dibenzo-α-pyrone alkaloid with an unprecedented 5/5/6/6/6 fused pentacyclic skeleton, was isolated from the endophytic fungus Rhizopycnis vagum Nitaf22. The structure was elucidated by comprehensive spectroscopic analysis, in combination with quantum chemical ¹³C NMR and electronic circular dichroism (ECD) calculations for configurational assignment. A plausible biosynthetic pathway for 1 was proposed. Compound 1 displayed acetylcholinesterase inhibitory activity.

Rhizovagine A (1), a dibenzo-α-pyrone alkaloid with a 5/5/6/6/6 fused pentacyclic skeleton and acetylcholinesterase inhibitory activity, was isolated from the endophytic fungus Rhizopycnis vagum Nitaf22.     

Multi-scale GCN-assisted two-stage network for joint segmentation of retinal layers and discs in peripapillary OCT images

An accurate and automated tissue segmentation algorithm for retinal optical coherence tomography (OCT) images is crucial for the diagnosis of glaucoma. However, due to the presence of the optic disc, the anatomical structure of the peripapillary region of the retina is complicated and is challenging for segmentation. To address this issue, we develop a novel graph convolutional network (GCN)-assisted two-stage framework to simultaneously label the nine retinal layers and the optic disc. Specifically, a multi-scale global reasoning module is inserted between the encoder and decoder of a U-shape neural network to exploit anatomical prior knowledge and perform spatial reasoning. We conduct experiments on human peripapillary retinal OCT images. We also provide public access to the collected dataset, which might contribute to the research in the field of biomedical image processing. The Dice score of the proposed segmentation network is 0.820 ± 0.001 and the pixel accuracy is 0.830 ± 0.002, both of which outperform those from other state-of-the-art techniques.     

促红细胞生成素长效化技术的研究与应用

<正>促红细胞生成素(erythropoietin,EPO)是最早通过基因工程技术研制的蛋白类药物之一(1989年由Amgen公司研制成功并上市的重组人EPO),二十多年来一直是基因工程药物中的常青树。由于EPO应用范围广、市场规模大,从而促使生物技术的革新不断应用于该品种,增强其生物学活性并延长其体内作用时间。本文将着重总结近年来EPO药物长效化的各种理论和实践的成果,展望未来长效EPO药物的发展趋势。     

Paratesticular solitary fibrous tumor: a case report and review of literature

Solitary fibrous tumor (SFT) is a rare spindle cell neoplasm that usually arising from the pleura, but has been reported in diverse extrapleural sites. Urogenital localization is rare, and only several cases of paratesticular SFT have been reported. In the present report, we present the case of a 61-year-old male suffering from a paratesticular SFT. A surgical excision of the lesion was performed. The tumor was well circumscribed and consisted of a mixture of bland spindle cells and dense collagen bands. Immunohistochemical studies showed positive reactivity for CD34, CD99 and vimentin, but stained negative for CD117, S100, SMA, HMB45, Desmin and CD68. All these clinicopathologic features are suggestive of the diagnosis of paratesticular SFT.