Copper-Catalyzed Intermolecular Cross-dehydrogenative C-N Coupling at Room Temperature via Remote Activating Group Enabled Radical Relay Strategy.

Employing N-fluorobenzenesulfonimide (NFSI) as a nitrogen-centered radical (NCR) precursor, an intermolecular C(sp2)-N coupling on heteroarenes or substituted benzenes with remote activated aniline derivatives via copper catalyzed N-N radical relay strategy at room temperature is developed. Good to excellent yields are acquired, and no ligand or additive is required. Reaction scope investigation and preliminary mechanistic studies demonstrate that the remote activating strategy and delicate control on the reactivities of active NCR species are essential to guarantee satisfactory chemo- and site-selectivity.

Gelatin/alginate-based microspheres with sphere-in-capsule structure for spatiotemporal manipulative drug release in gastrointestinal tract.

Microsphere with sphere-in-capsule structure is a multi-drugs delivery system to achieve the purpose of combination therapy. In this paper, we have prepared gelatin/alginate-based microspheres with sphere-in-capsule structure by a relatively fast, simple, and easily large-scale industrialized emulsification method for spatiotemporal manipulative drug release in gastrointestinal tract. Calcium alginate microspheres encapsulated with bovine serum albumin (BSA) were first prepared as inner microspheres, and then inner microspheres and ranitidine hydrochloride (RH) were co-encapsulated by gelatin microspheres to form double-layer microspheres with sphere-in-capsule structure. The size and distribution of microspheres can be easily controlled by emulsifying conditions. The microspheres with sphere-in-capsule structure displayed desirable encapsulation efficiency of BSA (61.52 %) and RH (56.07 %). The in vitro simulated drug release showed the spatiotemporal release feature of microspheres with sphere-in-capsule structure. In the specific simulated fluid, the release behavior and cumulative release of RH (sustainedly released 95 % in simulated gastric fluid) and BSA (rapidly released 73 % in simulated intestinal fluid) were different. The drug release mechanisms were analyzed to determine RH and BSA's release behavior. Overall, the microspheres with sphere-in-capsule structure have the potential application of spatiotemporal manipulative drug delivery in the gastrointestinal tract.

Acupuncture and Related Therapies for Obesity: A Network Meta-Analysis.

Obesity is a worldwide public health problem. Currently, increasing evidence suggests acupuncture and related therapies are effective for obesity. This network meta-analysis (NMA) was performed to compare the effectiveness of different acupuncture and related therapies. We searched potential randomized controlled trials (RCTs) in three international databases. Thirty-four trials involving 2283 participants were included. Pairwise meta-analysis showed that acupuncture and related therapies were superior to lifestyle modification and placebo in reducing weight and body mass index (BMI). Based on decreases in body weight, results from NMA showed that acupoint catgut embedding (standard mean difference [SMD]: 1.26; 95% credible interval [95% CI], 0.46-2.06), acupuncture (SMD: 2.72; 95% CrI, 0.06-5.29), and combination of acupuncture and related theories (SMD: 3.65; 95% CrI, 0.96-6.94) were more effective than placebo. Another NMA result indicated that acupoint catgut embedding (SMD: 0.63; 95% CI, 0.25-1.11), acupuncture (SMD: 1.28; 95% CrI, 0.43-2.06), combination of acupuncture and related therapies (SMD: 1.44; 95% CrI, 0.64-2.38), and electroacupuncture (SMD: 0.60; 95% CrI, 0.03-1.22) were superior to lifestyle modification in decreasing BMI. Combination of acupuncture and related therapies was ranked the optimal method for both reducing weight and BMI. Further studies will clarify which combination of acupuncture and related therapies is better.