The vial kit formulation for preparation of no‐carrier‐added 131I‐MIBG

We have developed a new set of lyophilized kits, composed of 3 different kits, for the instant preparation of no‐carrier‐added ¹³¹I‐MIBG in the clinic. We here discussed the formulation of the kits, optimization of radiolabelling, quality control of radiolabeled ¹³¹I‐MIBG, and studies of animal biodistribution. The no‐carrier‐added (nca) ¹³¹I‐MIBG injection could be prepared within 30 minutes in the clinic with the help of the lyophilized kits. The radiochemical purity and specific activity (SA) could achieve above 98% and 6700 MBq/mg, respectively.     

基于抗菌药物分级管理的我院抗菌药物医嘱评价

摘 要 目的：明确我院三级抗菌药物（非限制使用级、限制使用级、特殊使用级）不合理使用情况的特点及差异,为临床规范使用抗菌药物提供理论依据。 方法：对我院736份出院病历的1 228条抗菌药物医嘱逐条进行合理性点评,并对三级抗菌药物医嘱不合理使用率、分布特点、类型进行比较。 结果：我院三级抗菌药物不合理使用率差异不全相同,以限制使用级为最高（25.0%）,特殊使用级最低（9.8%）,两者比较差异有统计学意义（P<0.01）。以头孢菌素为主的β内酰胺类抗菌药物的不合理医嘱最多。三级抗菌药物不合理用药类型差异有统计学意义（P<0.05）。“抗菌药物用法用量不适宜”、“围手术期预防性使用抗菌药物不合理”为非限制使用级及限制使用级抗菌药物的主要不合理医嘱构成。而“遴选抗菌药物不适宜”则为特殊使用级抗菌药物的主要不合理医嘱构成。结论：我院抗菌药物不合理使用情况较普遍。医院需针对各级抗菌药物使用中存在的主要问题加强抗菌药物的管理。     

Enzymatic glycosylation of oleanane-type triterpenoids

Abstract

Glycosylation is an effective approach to improve the druggability of natural products by increasing their water solubility. In this work, we report the glycosylation of oleanane-type triterpenoids by a recombinant microbial glycosyltransferase YjiC1. A preliminary screening test indicated YjiC1 exhibited robust capabilities for O-glycosylation of triterpenoids, based on LC/MS analysis. Among the products, two new compounds (2a and 3a), together with a known one (1a), were isolated and characterized. These products exhibited improved water solubility, and 3a showed moderate anti-HIV activities at 100 μM. This reaction provides a facile and efficient approach to synthesize the glucosides of triterpenoids.     

Enzymatic synthesis of glucuronidated metabolites of two neurological active agents using plant glucuronosyltransferases

Abstract

Glucuronidation is an important and popular metabolic reaction in vivo of drugs. The further evaluation of biological activity and toxicity of glucuronides is necessary in the course of the drug research and development. However, the synthesis of glucuronides is limited by the lack of efficient approach. Herein, we have developed a new glucuronide synthesis method using plant uridine diphosphate-dependent glucuronosyltransferases (UGTs), UGT88D4, UGT88D7, and EpGT8, enabling the convenient preparation for corresponding O-glucuronide metabolites (1a, 2a, 3a, and 3b) in milligram scale of two neurological active agents, IMM-H004 (1) and FLZ (2). Their structures were characterized by spectroscopic data analyses.     

Two new saponins from the leaves of Panax notoginseng

Two new saponins, notoginsenosides Ng1 (1) and Ng2 (2), together with seven known compounds (3–9), were isolated from the leaves of Panax notoginseng. Their structures were elucidated by UV, IR, HRESIMS, and NMR experiments. Compounds 6 and 7 showed moderate cytotoxic activities against HCT-116, with IC₅₀ values of 4.98 and 0.64 μmol/L, respectively.     

Homoisoflavanones with estrogenic activity from the rhizomes of Polygonatum sibiricum

A new homoisoflavanone, (3R)-5-hydroxy-7-methoxyl-3-(2′-hydroxy-4′- methoxybenzyl)-chroman-4-one (1), together with six known analogs, were isolated from the rhizomes of Polygonatum sibiricum. Their structures were elucidated on the basis of extensive spectroscopic analysis. All compounds were tested for their estrogenic activity using the MCF-7 estrogenresponsive human breast cancer cell lines. At a dose of 0.1 μmol/L, compounds 1–7 exhibited significant proliferative effects on MCF-7 cells compared with E₂. The molecular docking study results indicated that the activity of compounds 3, 5, 6, and 7 may be the binding with ERR.     

Chemical constituents from Canarium album Raeusch and their anti-influenza A virus activities

Journal of Natural Medicines - Two new dyhydrophaseic acid glucoside isomers, (1′S, 3′R, 5′S, 8′R, 2Z, 4E)-dihydrophaseic acid-3′-O-β-d-glucopyranoside (2) and...     

Two new secoiridoid glucosides and a new lignan from the roots of <Emphasis Type="Italic">Ilex pubescens</Emphasis>

Two new secoiridoid glucosides, ilexpublignoside (1), pubzenoside (2), and a new lignan, ilexlignan B (3), along with seven known compounds (4–10) were isolated from the roots of Ilex pubescens for the first time. Their chemical structures were elucidated on the basis of extensive spectroscopic methods, including IR, UV, HR-ESI–MS, CD, NMR experiments, as well as comparison with the reported data.