Recent Progress on Natural α-glucosidase Inhibitors Derived from the Plants and Microorganisms.

α-Glucosidase inhibitors (AGIs) showcase versatile biochemical activities with respect to antidiabetic, anticancerous, antiobese and antiviral effects. They have drawn a great deal of attention from the scientific community. While α-glucosidase inhibitors are mostly discovered from plants and microorganisms, the recent advance in natural αglucosidase inhibitors over the past five years has been reviewed in this article, and 139 distinct α-glucosidase inhibitors from the plants and microorganisms were classified into ten groups based on their chemical structures, including flavonoids (34), xanthones (6), alkaloids (8), benzopyrones / benzofuranones (8), terpenes (23), saponins (8), phenols / alcohols (25), esters (18), chalcone (5) and other compounds (4).

Study on Manufacturing Technology of Ag-8.5Au-3.5Pd Fine Alloy Wire.

The performance of Ag-8.5Au-3.5Pd alloy wire after cold deformation and annealing were analyzed by SEM (scanning electron microscope), strength tester and resistivity tester.

New organoselenides (NSAIDs-Se derivatives) as potential anticancer agents: Synthesis, biological evaluation and in silico calculations.

Herein we reported the synthesis of twenty new organoselenium compounds (2a-2j and 3a-3j) based on the hybridization of nonsteroidal antiinflammatory drugs (NSAIDs) skeleton and organoselenium motif (-SeCN and -SeCF), the anticancer activity was evaluated against four types of cancer cell lines, Caco-2 (human colon adenocarcinoma cells), BGC-823 (human gastric cancer cells), MCF-7 (human breast adenocarcinoma cells), PC-3 (human prostatic cancer cells). Interestingly, the introduction of the -SeCN or -SeCF moiety in corresponding parent NSAIDs results in the significant effect on cancer cell lines. Moreover, the most active compound 3a showed IC values lower than 5 μM against the four cancer cell lines, particularly to BGC-823 and MCF-7 with IC values of 2.

Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF) derivatives as potential anticancer agents.

A series of organoselenium compounds based on the hybridization of nonsteroidal antiinflammatory drugs (NSAIDs) scaffolds and Se functionalities (-SeCN and -SeCF) were synthesized and characterized, and evaluated against four types of cancer cell lines, SW480 (human colon adenocarcinoma cells), HeLa (human cervical cancer cells), A549 (human lung carcinoma cells), MCF-7 (human breast adenocarcinoma cells). Interestingly, most of the investigated compounds showed active in reducing the viability of different cancer cell lines. The most active compound 3h showed IC values lower than 20 μM against the four cancer cell lines, particularly to SW480 and MCF-7 with IC 50 values of 4.

Synthesis and Toxicity of Halogenated Bisphenol Monosubstituted-Ethers: Establishing a Library for Potential Environmental Transformation Products of Emerging Contaminant.

As an important branch of halogenated bisphenol compounds, the halogenated bisphenol monosubstituted-ether compounds have received a lot of attention in environmental health science because of their toxicity and variability. In this study, a synthetic method for bisphenol monosubstituted-ether byproduct libraries was developed. By using the versatile and efficient method, tetrachlorobisphenol A, tetrabromobisphenol A, and tetrabromobisphenol S monosubstituted alkyl-ether compounds were accessed in 39-82 % yield.

Design, synthesis and biological evaluation of acridone glycosides as selective BChE inhibitors.

Based on structure analyses of butyrylcholinesterase (BChE), a series of 21 acridone glycosides were designed, synthesized and evaluated in vitro for their BChE and acetylcholinesterase (AChE) inhibitory activities. d-ribose derivative 6f exhibited the greatest inhibitory activity on BChE (IC = 6.95 μM), and was the most selective inhibitor of BChE with the IC ratio of AChE/BChE was 20.

Total Synthesis of the Proposed Structure of Penasulfate A: l-Arabinose as a Source of Chirality.

The total synthesis of putative penasulfate A was effectively achieved by a convergent strategy with a longest linear sequence of 14 steps and overall yield of 8.6%. The highlights of our strategy involved an -selective olefin cross-metathesis, Suzuki cross-coupling, and a copper(I)-catalyzed coupling reaction.

Recent Advances of Chitosan and its Derivatives in Biomedical Applications.

Chitosan is the second-most abundant natural polysaccharide. It has unique characteristics, such as biodegradability, biocompatibility, and non-toxicity. Due to the existence of its free amine group and hydroxyl groups on its backbone chain, chitosan can undergo further chemical modifications to generate Chitosan Derivatives (CDs) that permit additional biomedical functionality.

Theranostic Applications of Antibody-Based Systems in Human Diseases.

Since antibodies are one of the most successful classes of biopharmaceuticals for cancer treatment, it is very important to discuss the functionality and biological activity of endogenous antibodies in the diagnosis and treatment of the diseases. Antibodies act on tumor cells in diverse ways, including engaging in antibody-dependent effector mechanisms, internalizing to deliver toxins, and displaying direct effects on cells. In this review, we outline three kinds of antibody-based therapeutic systems, namely Antibody-based Drug Conjugates (Ab-DCs), Antibody-based Recruiting Small Molecules (Ab-RSMs) and Carbohydrate Epitopes Recruiting Natural Antibodies (CERNA) for human disease treatment and imaging.

Recent progresses in biomedical applications of aptamer-functionalized systems.

Aptamers, known as "chemical antibodies" are screened via a combinational technology of systematic evolution of ligands by exponential enrichment (SELEX). Due to their specific targeting ability, high binding affinity, low immunogenicity and easy modification, aptamer-functionalized systems have been extensively applied in various fields and exhibit favorable results. However, there is still a long way for them to be commercialized, and few aptamer-functionalized systems have yet successfully entered clinical and industrial use.

The first convergent total synthesis of penarolide sulfate A2, a novel α-glucosidase inhibitor.

Penarolide sulfate A2, a 31-membered macrolide encompassing a proline residue and three sulfate groups, was firstly synthesized in 16 linear steps with 4.8% overall yield. Three consecutive stereogenic centers in penarolide sulfate A2 were efficiently derived from natural chiral template l-arabinose.

Total synthesis of (-)-orthodiffenes A and C.

The efficient and concise synthesis of (-)-orthodiffenes A and C has been accomplished for the first time in eight steps from readily available chiral synthons, D-mannose and D-ethyl lactate. Our work confirmed the complete structure of orthodiffenes A and C, including their absolute stereochemistry. The key steps of our total synthesis involved cis-fused tetrahydrofuran cyclization, one-pot deprotection-lactonization, and intramolecular benzoyl migration according to a biosynthetic hypothesis of orthodiffenes.