Facile construction of dibenzodioxo[3.3.1]nonanes bearing spirocyclohexadienones domino [4 + 2] cycloaddition/C(sp)-H oxidative dehydrogenation coupling reactions.

A novel palladium catalyzed homodimerization of -hydroxyphenyl substituted -QMs has been developed [4 + 2] cycloaddition/oxidative dehydrogenation coupling domino reactions. An interesting palladium catalyzed intramolecular benzyl C-H oxidation dehydrogenation to form a transannular C(sp)-O bond was found. This protocol provided an efficient method to construct various dibenzodioxo[3.

Divergent oxidative dearomatization coupling reactions to construct polycyclic cyclohexadienones.

Highly selective divergent oxidative dearomatization coupling reactions, in which the chemoselectivity is controlled by catalysts and bases, are reported herein. Three different kinds of polycyclic cyclohexadienones are produced from the same reactants (41 examples, 85-99% yield). Our method marks a novel copper- and palladium-catalyzed C-H oxidative dearomatization of phenolic derivatives.

A double-blind, randomized, placebo- and positive-controlled phase III trial of 1% benvitimod cream in mild-to-moderate plaque psoriasis.

Background: Benvitimod cream, a novel synthetic small molecule, was effective in treating mild-to-moderate plaque psoriasis. We conducted a phase III clinical trial to assess the efficacy and safety of benvitimod cream in patients with mild-to-moderate plaque psoriasis.

Methods: We randomly assigned 686 patients (2:1:1) to receive 1% benvitimod cream, 0.

The Therapeutic and Pathogenic Role of Autophagy in Autoimmune Diseases.

Autophagy is a complicated cellular mechanism that maintains cellular and tissue homeostasis and integrity degradation of senescent, defective subcellular organelles, infectious agents, and misfolded proteins. Accumulating evidence has shown that autophagy is involved in numerous immune processes, such as removal of intracellular bacteria, cytokine production, autoantigen presentation, and survival of lymphocytes, indicating an apparent and important role in innate and adaptive immune responses. Indeed, in genome-wide association studies, autophagy-related gene polymorphisms have been suggested to be associated with the pathogenesis of several autoimmune and inflammatory disorders, such as systemic lupus erythematosus, psoriasis, rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis.

A comprehensive review of immune-mediated dermatopathology in systemic lupus erythematosus.

Lupus erythematosus (LE) is an autoimmune disease with a broad clinical spectrum ranging from cutaneous lesions to severe systemic manifestations. The pathogenesis of the disease and the immunological mechanisms for the heterogeneities in lupus remain unclear. The LE-specific cutaneous manifestations are generally divided into three categories: acute cutaneous LE (ACLE), subacute cutaneous LE (SCLE) and chronic cutaneous lupus erythematosus (CCLE).

Use of a dose-response model to guide future clinical trial of benvitimod cream to treat mild and moderate psoriasis.

Objective: To investigate the time-dose-response relationship of benvitimod cream after topical administration in patients with mild and moderate psoriasis vulgaris for dosage regimen exploring.

Methods: 36 patients with mild and moderate psoriasis vulgaris were randomly assigned to receive 0.5%, 1.

The antioxidants dimethylsulfoxide and dimethylthiourea affect the immediate adhesion responses of larval haemocytes from 3 lepidopteran insect species.

Antioxidants, dimethylsulfoxide (DMSO) and dimethylthiourea (DMTU), at concentrations not affecting the viability of blood cells (haemocytes) from the larval stage of 3 lepidopteran insects - Galleria mellonella, Lymantria dispar, and Malacosoma disstria - differed in their influence on the innate binding of haemocytes to glass, bacteria to haemocytes, and on humoral responses to alien materials. In vitro DMSO had little effect, whereas DMTU substantially impaired the adhesion of the haemocyte types, the plasmatocytes and granular cells, to slides as well as the attachment of Bacillus subtilis to these haemocytes. Although both antioxidants increased lysozyme and phenoloxidase activities, there was no correlation of enzyme activity and haemocyte adhesion responses, possibly reflecting sequestered radicals.

Substituted 6-amino-4H-[1,2]dithiolo[4,3-b]pyrrol-5-ones: synthesis, structure-activity relationships, and cytotoxic activity on selected human cancer cell lines.

An efficient synthesis and the cytotoxic activity of a series of substituted 6-amino-4H-[1,2]dithiolo[4,3-b]pyrrol-5-ones 1a-q is described. The synthesis was accomplished in an expedient manner (seven-steps) from commercially available starting materials. Several of the derivatives tested demonstrated significant in vitro cytotoxic activity against the human cancer cell lines H460 (7nM) and LCC6 (> or =28nM).

A novel antimicrobial epoxide isolated from larval Galleria mellonella infected by the nematode symbiont, Photorhabdus luminescens (Enterobacteriaceae).

A novel antimicrobial epoxide, 2-isopropyl-5-(3-phenyl-oxiranyl)-benzene-1,3-diol (1), was identified from larval Galleria mellonella infected by a symbiotically associated bacterium-nematode complex (Photorhabdus luminescens C9-Heterorhabditis megidis 90). Its structure was determined with spectroscopic analysis and confirmed by chemical synthesis starting from a known antibiotic, 2-isopropyl-5-(2-phenylethenyl)-benzene-1,3-diol (2). Epoxide 1 was active against Bacillus subtilis, Escherichia coli, Streptococcus pyogenes, and a drug-resistant, clinical strain of Staphylococcus aureus (RN4220) with minimum inhibitory concentrations in the range of 6.