MITA oligomerization upon viral infection is dependent on its N-glycosylation mediated by DDOST.

The mediator of IRF3 activation (MITA, also named STING) is critical for immune responses to abnormal cytosolic DNA and has been considered an important drug target in the clinical therapy of tumors and autoimmune diseases. In the present study, we report that MITA undergoes DDOST-mediated N-glycosylation in the endoplasmic reticulum (ER) upon DNA viral infection. Selective mutation of DDOST-dependent N-glycosylated residues abolished MITA oligomerization and thereby its immune functions.

Bioassay-guided isolation of saikosaponins with agonistic activity on 5-hydroxytryptamine 2C receptor from Bupleurum chinense and their potential use for the treatment of obesity.

5-Hydroxytryptamine 2C (5-HT) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtOH extract of the roots of Bupleurum chinense was revealed to have agonistic activity on 5-HT receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT receptor agonistic activity in vitro and anti-obesity activity in vivo. The new compound, 22-oxosaikosaponin d (1), was determined by extensive spectroscopic analyses (HR-ESI-MS, IR, and 1D and 2D NMR).

Bioactivity-guided synthesis of gramine derivatives as new MT and 5-HT receptors agonists.

Twenty-four gramine derivatives were synthesized and evaluated on MT and 5-HT receptors in vitro. Among them, seven derivatives (7, 8, 16, 19, 20, 21, and 24) exhibited higher agonisting activities on MT or 5-HT receptors. Compared with gramine, derivatives 7, 8, 16, 19, 20, 21, and 24 displayed 1.

Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives.

Sixteen tropinone derivatives were prepared, and their antitumor activities against five human cancer cells (HL-60, A-549, SMMC-7721, MCF-7 and SW480) were evaluated with MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxy methoxyphenyl)-2-(4-sulfopheny)-2H-tetrazolium] assay. Most of the derivatives exhibited better activities compared with tropinone at the concentration of 40 μM. Particularly, derivative 6 showed significant activities with IC values of 3.

Catalytic Asymmetric Total Synthesis of (+)- and (-)-Paeoveitol via a Hetero-Diels-Alder Reaction.

The first catalytic asymmetric total synthesis of (+)- and (-)-paeoveitol has been accomplished in 42% overall yield via a biomimetic hetero-Diels-Alder reaction. The chiral phosphoric acid catalyzed hetero-Diels-Alder reaction showed excellent diastereo- and enantioselectivity (>99:1 dr and 90% ee); two rings and three stereocenters were constructed in a single step to produce (-)-paeoveitol on a scale of 452 mg. This strategy enabled us to selectively synthesize both paeoveitol enantiomers from the same substrates by simply changing the enantiomer of the catalyst.

LC-MS guided isolation of ent-kaurane diterpenoids from Nouelia insignis.

The preliminary LC-MS investigation on the stems of Nouelia insignis manifested the existence of diterpenoids. As a result, 15 ent-kaurane diterpenoids, including 7 new glycosides (nouelosides A-G, 1-7), were isolated under the direction of LC-MS analysis. The new compounds were determined by extensive spectroscopic analysis including HRESIMS, 1D and 2D NMR data and chemical methods.

Natural products as antidepressants documented in Chinese patents from 1992 to 2013.

Depressive disorder is a severe psychiatric problem all over the world. Clinical therapeutic agents for the treatment of depression in the market targeting on monoamine neurotransmitters are far from satisfaction due to their adverse effects. Novel classes of antidepressant agents with different mechanisms and low toxicity are needed.

(E)-4-(β-d-Allopyran-os-yloxy)cinnamyl 4-bromo-phenyl ketone ethanol solvate.

The title compound, C(21)H(21)BrO(7)·C(2)H(6)O, was synthesized by the Claisen-Schimidt reaction of helicid (systematic name: 4-formyl-phenyl-β-d-allopyran-oside) with 4-bromo-aceto-phenone in ethanol. The pyran ring adopts a chair conformation. In the crystal structure, mol-ecules are linked into a three-dimensional network by inter-molecular O-H⋯O hydrogen bonds.

1-[4-(2,3,4,6-Tetra-O-acetyl-β-d-allo-pyranos-yloxy)benzyl-idene]thio-semi-carbazide.

The title compound, C(22)H(27)N(3)O(10)S, was synthesized by reaction of an ethanol solution of helicid (systematic name: 4-formylphenl-β-d-allopyranoside), thio-semicarbazide and acetic acid. The mol-ecule exhibits a trans conformation with respect to the C=N double bond. The pyran ring adopts a chair conformation.

E-[4-(β-d-Allopyranos-yloxy)phen-yl]-1-(4-chloro-phen-yl)prop-2-enone ethanol solvate.

The title compound, C(21)H(21)ClO(7)·C(2)H(5)OH was synthesized by the condensation reaction between helicid [systematic name: 4-(β-d-allopyranos-yloxy)benzaldehyde] and 4-chloro-aceto-phen-one in ethanol. In the mol-ecular structure, the pyran-oside ring adopts a chair conformation. In the crystal structure, the molecules are linked by inter-molecular O-H⋯O hydrogen bonds involving the OH groups from the pyran-oside unit and from the ethanol solvent mol-ecule.

N,N-Dimethyl-4-[(E)-phenyl-imino-meth-yl]aniline.

The title compound, C(15)H(16)N(2), contains two aromatic rings linked through an imino group. The mol-ecule exhibits an E configuration with respect to the C=N bond. The dihedral angle between the aromatic rings is 61.