Copper-Catalyzed Trifluoromethylation/Cyclization of Alkynes for Synthesis of Dioxodibenzothiazepines.

A facile and efficient approach for the synthesis of the CF3-containing dioxodibenzothiazepines has been developed via copper-catalyzed trifluoromethylation/cyclization of alkynes utilizing a radical relay strategy. This method has demonstrated low catalyst loading, high regiocontrol, and broad scope under mild conditions. Good compatibility for the N-protecting group, gram-scale experiment, and further derivation of product prove the versatility of this transformation.

Remote azidation of C(sp3)-H bonds to synthesize δ-azido sulfonamides via iron-catalyzed radical relay.

With an iron catalyst playing dual roles as a radical initiator and terminator, we report a selective remote C-H functionalization to access δ-azido sulfonamides through a radical relay process. The reaction of N-fluorosulfonamide furnishes the corresponding products in excellent yields with high regioselective control. The key to success is the highly efficient iron-mediated redox azido transfer to the in situ generated carbon radical. The products provide incentives for drug discovery and ligand designs.

Effect of Danggui Shaoyaosan on Copper Ion-mediated Aβ Aggregation in AD Cell Model / 中国实验方剂学杂志

Objective:To investigate the effect of copper ion(Cu2+) on the aggregation and neurotoxicity of Aβ, and affirm the role of Danggui Shaoyaosan in vitro,the Neuroblastoma (SH-SY5Y) cells treated with β-amyloid 1-42 (Aβ1-42) and Cu2+ were used as a vitro models of Alzheimer's disease(AD). Method:Aβ 1-42 (20 μmol·L-1) was reacted with different concentrations of copper sulfate (CuSO4,20,40 μmol·L-1), and then the thioflavine T (ThT) staining method was used to detect the Aβ aggregation state. The Aβ aggregation status was also detected by ThT staining in the Aβ1-42-Cu2+ group(20+20 μmol·L-1), and Danggui Shaoyaosan groups(1.6,3.2,6.4 mg·L-1).The SH-SY5Y cells were cultured and incubated with different concentrations of Aβ1-42(1.25,2.5,5,10,20,40 μmol·L-1) and Danggui Shaoyaosan(1.6, 3.2, 6.4,12.8 mg·L-1) for 24 h. Subsequently, SH-SY5Y cells were incubated with Aβ1-42 (20 μmol·L-1) and CuSO4(20 μmol·L-1) in the Aβ1-42-Cu2+ group, and incubated with Aβ1-42 (20 μmol·L-1), Danggui Shaoyaosan (1.6 mg·L-1) and CuSO4 (20 μmol·L-1) in Danggui Shaoyaosan group. Control group was added with the medium. After 24 h of co-action, the cell viability was detected by the methylthiazolyl tetrazolium (MTT) assay. The morphology of the cells was photographed by microscopy. The intracellular extracellular Aβ1-42 aggregation was detected by Western blot. Result:Cu2+ and Aβ1-42 bound to more and larger Aβ aggregates compared with the Aβ1-42 group. Compared with the normal group, cell viability was significantly reduced (PPβ1-42 aggregation was increased(PPβ-Cu2+ (PPβ1-42 protein (PPConclusion:Cu2+ can increase the aggregation and toxicity of Aβ; Danggui Shaoyaosan can significantly reduce the damage of SH-SY5Y cells induced by Cu2+-mediated Aβ aggregation, promote Aβ endocytosis, reduce extracellular Aβ aggregation and increase cell viability.

[Study on porous starch as solid dispersion carrier of total Epimedium flavonoids].

In order to evaluate the characteristic of porous starch (PS) as the solid dispersions carrier of the total Epimedium flavonoids (TEF), the PS was used. The dissolution of icariin was selected as an indicator to analyze the differences of dissolution between TEF and its solid dispersion. TEF was characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). Solid dispersion was irregular block and no powder characteristics of TEF and PS could be seen in SEM, DSC and XRD analysis suggested that TEF may be present in solid dispersion as amorphous substance. The dissolution rate of icariin has been improved significantly when the proportion of TEF and PS was 1:2. PS as a traditional solid dispersion carrier is worthy of further study.

[Solidification of volatile oil with graphene oxide].

To evaluate the properties of solidifying volatile oil with graphene oxide, clove oil and zedoary turmeric oil were solidified by graphene oxide. The amount of graphene oxide was optimized with the eugenol yield and curcumol yield as criteria. Curing powder was characterized by differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). The effects of graphene oxide on dissolution in vitro and thermal stability of active components were studied. The optimum solidification ratio of graphene oxide to volatile oil was 1:1. Dissolution rate of active components had rare influence while their thermal stability improved after volatile oil was solidified. Solidifying herbal volatile oil with graphene oxide deserves further study.

[Endoscopic thyroidectomy with 150 cases].

OBJECTIVE: To discuss the method, the advantages and disadvantages of endoscopic thyroidectomy. METHODS: Endoscopic thyroidectomy via areola of breasts approach was performed in 150 patients, including 41 cases of thyroid adenoma, 64 cases of nodular goiter, 40 cases of Graves' disease, and 5 cases of thyroid carcinoma. RESULTS: The endoscopic thyroidectomy was successfully carried out in 144 cases, including tumor dissection in 32 cases, one lobe partial thyroidectomy in 54 cases, two lobe partial thyroidectomy in 19 cases, subtotal thyroidectomy in 37 cases of Graves' disease, and radical thyroidectomy in 2 cases of thyroid carcinoma. The operative time length ranged from 50 to 270 min (mean 80 min). There were no complications such as damage to recurrent laryngeal nerve or parathyroid glands. Postoperative hospital stay ranged from 3 to 7 days (mean 4 days). The post-operative following-up for 1 approximately 13 months indicated that all the patients were satisfied with the cosmetic results and the same curative effects as conventional surgery were obtained. However, the operations were converted into open surgery in 6 cases. CONCLUSIONS: Endoscopic thyroidectomy is a safe and effective method of thyroid surgery. Since all the minimal incisions are on concealed parts of the body, the obvious cosmetic effect of this method is guaranteed.

Laparoscopic vertical banded gastroplasty for morbid obesity.

OBJECTIVE: To evaluate the clinical application of laparoscopic vertical banded gastroplasty (LVBG) for morbid obesity. METHODS: Four patients undergoing LVBG were evaluated by comparison of the preoperative and postoperative morbidities and body weights. RESULTS: Laparoscopic surgery was successfully performed in all the 4 cases without laparotomy. The average operative time was 210 min without intraoperative or postoperative complications. In the 24-month follow-up, the body weight was reduced by over 50% of the excessive weight. CONCLUSION: LVBG is an effective and safe treatment for morbid obesity.