Indoxyl derivatives of drug metabolites

Summary Indoxyl derivatives were detected as minor products among the urinary metabolites of two trial drugs, a benzodiazepine (GP 55 129) and a benzophenone (CGP 11 952). Their structures were elucidated by NMR and mass spectroscopy. Presumably, metabolites containing potential aldehyde functions react spontaneously with endogenous indoxyl. Such derivatives have not hitherto been encountered in drug metabolism.     

蒙药治疗药物流产后恶露不绝31例

目的：观察蒙药内服法治疗药流后恶露不绝的临床疗效．方法：选择我院诊治的药流后恶露不绝患者31例，用蒙药六味大黄散2次／日，3g／每次，2周为1疗程，结果：用药1～3d后，症状明显改善，7d后恶露基本排尽．31例中治愈23例，好转8例，结论：该方剂性温，为妇科血症及赫依症专方．具有促进子宫收缩、活血化瘀的功能，可用于药物流产后恶露不绝的治疗．     

Stimuli-responsive polymeric materials for human health applications

Stimuli-responsive polymers have the extraor- dinary ability to change their physical and/or chemical state after they ＂detect＂ a change in their environment; their response depends dramatically on their chemical compo- sition. This property has been used for a plethora of applications; this review highlights their utility for human health. Specifically, this review will highlight efforts in the areas of sensing and biosensing, antimicrobial/antifouling coatings, tissue engineering and regenerative medicine, and drug delivery. Specific examples are given in each of these areas, with some focus on our work engineering poly（N- isopropylacrylamide）-based microgels and other respon- sive systems.     

卫生部药品标准中药成方制剂中含反药药对成方制剂收载情况与分析

"十八反"、"十九畏"作为中医药领域传统的配伍禁忌,一直沿用至今,但由于临床不乏反药同用治疗某些疾病突显奇效的病案,其是否确属绝对配伍禁忌,是众多学者及临床医生关注的热点问题.<中华人民共和国卫生部药品标准·中药成方制剂>是卫生部为解决中药材品种混乱问题,保证人民用药安全有效,颁布的具有权威性的法定标准.据统计,其1～20册共收载成方制剂4052个品种,其中含反药配伍的成方制剂65个,包括含"十八反"药对的品种43个,含"十九畏"药对的品种25个,既含"十八反"又含"十九畏"药对的品种3个.经分析可知,该标准含反药药对的成方中以乌头类与半夏、官桂与赤石脂配伍使用为多;其临床应用特点,含"十八反"药对的成方主要用于风湿痹病、跌打损伤,剂型以丸剂、膏药、橡胶膏剂为主,口服与外用比例相当;含"十九畏"药对的成方主要用于月经不调,以丸剂口服为主.在处方药味数方面,含反药药对的成方以16～30味的处方较多.     

牙周炎病原菌的分离鉴定及药敏试验

从７例牙周炎患者病料中分离到６株专性厌氧菌和若干株兼性厌氧菌。通过形态学观察，微量生化试验以及用气相色谱分析其代谢产物等方法，已将６株厌氧菌鉴定到种。随后用江西中医学院研制的数种治疗牙周炎的药物对其中几株主要病原菌做了体外药敏试验，比较了５种药物成分对牙周炎病原菌的作用；测定了５种药物配方对５株厌氧菌的ＭＩＣ及ＭＬＣ。此外，还探索了药液的牛津杯法在厌氧菌抑菌试验中的应用。     

药材鳖甲的真伪鉴别

中药鳖甲是使用鳖的背甲。近来发现有以腹甲混入背甲充作药用。本文从鳖的背甲及腹甲形态特征进行比较,这样就改进了鳖甲的鉴别方法。     

Strategies for the design of inhibitors of aldose reductase, an enzyme showing pronounced induced-fit adaptations

Aldose reductase is involved in the polyol pathway, catalyzing the reduction of glucose to sorbitol. However, due to pronounced binding site adaptations, the enzyme can operate on a broad palette of structurally diverse substrates ranging from small aliphatic and aromatic aldehydes up to steroid-type ligands. A comparative analysis of the presently accessible crystal structures of aldose reductase complexes reveals four binding-competent protein conformations. Additional relevant conformers are detected through molecular dynamics simulations. They indicate an equilibrium of several conformers which is shifted towards the binding-competent geometries upon ligand binding. Such a manifold system with several alternative binding site conformers requires some tailored concepts in virtual screening. We followed two strategies, both successfully suggesting new micromolar inhibitors. In a first attempt, we concentrated on one preferred conformer and performed a virtual screening, assuming that the binding pocket of aldose reductase adopts only this conformation. In a second approach, we followed a ligand superpositioning method. Ligands were extracted in their bound conformations from three different crystal structures, all accommodating the ligands with different active site conformations. After merging these ligands into one supermolecule, mutual alignments were computed, taking candidate ligands from a screening database. The latter strategy also retrieved several structurally new inhibitors of micromolar potency.     

肿瘤侵袭和转移的规律及其药物防治策略

介绍了肿瘤侵袭和转移的规律及药物防治策略，提出了阻断肿瘤侵袭，转移过程的各个步骤是今后的研究方向。     

In vitro study of poly(ethylene carbonate) as a drug-eluting stent coating

An in vitro feasibility study of the use of poly(ethylene carbonate) (PEC) as a biodegradable coating material for drug-eluting stents is reported, and the performance of PEC is compared with that of poly(lactic-co-glycolic acid) (PLGA). Scanning electron microscopy (SEM) images of PEC and PLGA discs after treatment with an alkaline KO2 solution as a superoxide source showed that the PEC maintained its integrity whereas holes and small particles appeared during the treatment of PLGA. Sirolimus and paclitaxel were loaded into PEC and PLGA in order to study drug release performance. Attenuated total reflectance–infrared (ATR– FTIR) spectroscopy of sirolimus, PEC and the sirolimus-loaded PEC coating showed that no chemical reaction occurred between sirolimus and PEC. The results of atomic force microscopy (AFM) revealed that the mean roughness (Ra) values of the bare metal stent (BMS) and the drugeluting stent (DES) were 2.3 nm and 1.0 nm, respectively. After balloon expansion experiments, no delamination or destruction of the PEC coating was observed. The drug release profile of sirolimus was different from that of paclitaxel when PEC was employed as the drug carrier, and the release curves of sirolimus were different when PEC and PLGA were used as drug carriers. All the experimental results demonstrated that PEC was one of the best potential stent-coating materials.     

铜绿假单胞菌多重耐药性分子机制的研究

铜绿假单胞菌是重要的医院感染条件致病菌.由于各种抗生素的广泛使用,细菌耐药问题日趋严重,导致了铜绿假单胞菌产生了很强的耐药性而且多重耐药,铜绿假单胞菌通过多种途径产生耐药.而从分子水平对其耐药性机制进行研究具有重要意义.