Sulforaphane decreases oxidative stress and inhibits NLRP3 inflammasome activation in a mouse model of ulcerative colitis.

Excessive oxidative stress and NLRP3 inflammasome activation are considered the main drivers of inflammatory bowel disease (IBD), and inhibition of inflammasomes ameliorates clinical symptoms and morphological manifestations of IBD. Herein, we examined the roles of NLRP3 activation in IBD and modulation of NLRP3 by sulforaphane (SFN), a compound with multiple pharmacological activities that is extracted from cruciferous plants. To simulate human IBD, we established a mouse colitis model by administering dextran sodium sulfate in the drinking water.

Luteolin and its analog luteolin-7-methylether from Leonurus japonicus Houtt suppress aromatase-mediated estrogen biosynthesis to alleviate polycystic ovary syndrome by the inhibition of tumor progression locus 2.

Ethnopharmacological Relevance: Leonurus japonicus Houtt (L. japonicus, Chinese motherwort), known as Yi Mu Cao which means "good for women", has long been widely used in China and other Asian countries to alleviate gynecological disorders, often characterized by estrogen dysregulation. It has been used for the treatment of polycystic ovary syndrome (PCOS), a common endocrine disorder in women but the underlying mechanism remains unknown.

Chaetomadramines A-E, a class of siderophores with potent neuroprotective activity from the fungus Chaetomium madrasense cib-1.

Five hydroxamate siderophores, chaetomadramines A-E (1-5), along with seven known compounds were isolated from the fermented rice culture of the fungus Chaetomium madrasense cib-1. Compounds 1-5 were structurally elucidated on the basis of spectroscopic data, which were a group of unusual hydroxamate siderophores, bearing a long fatty acyl on the α-NH of the N-hydroxylated ornithine. Compounds 2-5 were new.

Chaetonigrisins A-L, a group of 3-Indole-1,2-Propanediol derived alkaloids from Chaetomium nigricolor YT-2.

Thirteen new alkaloids (1-13) as well as ten known compounds were isolated from the solid-state fermented rice medium of the fungus Chaetomium nigricolor YT-2. Their structures were elucidated on the basis of spectroscopic data, quantum calculations, and single crystal X-ray crystallographic analysis. Chaetonigrisin A (1) represents an unprecedented carbon skeleton featuring a polycyclic 1H-pyrano[3,2:3,4-]​furo[2,​3-​b]​indole.

Hexachlorophene, a selective SHP2 inhibitor, suppresses proliferation and metastasis of KRAS-mutant NSCLC cells by inhibiting RAS/MEK/ERK and PI3K/AKT signaling pathways.

Kirsten rat sarcoma viral oncogene homolog (KRAS) mutations account for 35% of the genetic alterations in non-small cell lung cancer (NSCLC). The Src-homology region 2-containing protein tyrosine phosphatase 2 (SHP2), encoded by PTPN11, is closely involved in RAS downstream pathways and development of many tumors by affecting cell proliferation, differentiation, and immunity. Targeting SHP2 with small molecules may be a promising avenue for the treatment of KRAS-mutant (mut) NSCLC.

A small molecule inhibitor of caspase-1 inhibits NLRP3 inflammasome activation and pyroptosis to alleviate gouty inflammation.

Caspase-1 is an integral regulator of innate immunity, which plays a key role in inflammasome activation and the release of pro-inflammatory cytokines. The development of novel non-peptidic small molecule caspase-1 inhibitors is an important strategy for antagonizing excessively activated caspase-1 induced by inflammatory diseases, including gouty arthritis. In the present study, we identified 63 caspase-1 inhibitors, with different structures and potencies, from bioactive compound libraries.

Reduced inspiratory muscle strength increases pneumonia in patients with acute myocardial infarction.

Background: Inspiratory muscle strength is associated with pneumonia in patients after surgery or those with subacute stroke. However, inspiratory muscle strength in patients with acute myocardial infarction (AMI) has not been studied.

Objective: To evaluate the predictive value of inspiratory muscle strength for pneumonia in patients with AMI.

Steroidal alkaloids from the bulbs of Fritillaria pallidiflora Schrenk and their anti-inflammatory activity.

Steroidal alkaloids (1-11), including one new 24-hydroxylated cevanine-type steroidal alkaloid, named yibeinone F (1), were isolated from the bulbs of Fritillaria pallidiflora Schrenk. Their structures were elucidated by analyses of extensive spectroscopic data and comparison of the NMR data with those reported previously, and the structures of compounds 1, 7 and 11 were further confirmed by X-ray single crystal diffraction analyses. The anti-inflammatory effects of all the isolated alkaloids were evaluated in LPS-activated RAW264.

Inhibition of Phosphodiesterase 5 Promotes the Aromatase-Mediated Estrogen Biosynthesis in Osteoblastic Cells by Activation of cGMP/PKG/SHP2 Pathway.

Mechanical stimulation induces bone growth and remodeling by the secondary messenger, cyclic guanosine 3', 5'-monophosphate (cGMP), in osteoblasts. However, the role of cGMP in the regulation of estrogen biosynthesis, whose deficiency is a major cause of osteoporosis, remains unclear. Here, we found that the prenylated flavonoids, 3--methoxymethyl-7--benzylicaritin (13), 7--benzylicaritin (14), and 4'--methyl-8-isopentylkaempferol (15), which were synthesized using icariin analogs, promoted estrogen biosynthesis in osteoblastic UMR106 cells, with calculated EC values of 1.

The Safety and Efficacy of Inspiratory Muscle Training for Patients With Acute Myocardial Infarction Undergoing Percutaneous Coronary Intervention: Study Protocol for a Randomized Controlled Trial.

Uncommonly high rates of pneumonia in patients with acute myocardial infarction (AMI) undergoing primary percutaneous coronary intervention (PCI) have been observed during recent years. Inspiratory muscle training (IMT) could reduce pneumonia in patients undergoing coronary artery bypass grafting and other cardiac surgeries. The relationship between IMT and AMI is unknown.

Synthesis and antitumor activity of novel berbamine derivatives.

A series of new berbamine derivatives were synthesized, and their cytotoxic activity was evaluated against Human T-cell lymphoma cell line H9 and multiple myeloma cell line RPMI8226 . Compared with berbamine, the cytotoxicity of the modified derivatives was enhanced, especially simultaneously substituted at OH and 5-position. Compounds and exhibited high antitumor activity.

Luteolin-7-methylether from Leonurus japonicus inhibits estrogen biosynthesis in human ovarian granulosa cells by suppression of aromatase (CYP19).

Leonurus japonicus (motherwort) has been widely used to treat gynecological disorders, in which estrogen is often dysregulated, for a long time in China and other Asian countries. However, the chemical constituents and mechanisms underlying the activity of this medicinal plant are not fully understood. Seventeen of forty-six tested natural products from L.

Aloe-emodin induces hepatotoxicity by the inhibition of multidrug resistance protein 2.

Background: Aloe-emodin (AE) is among the primary bioactive anthraquinones present in traditional Chinese medicinal plants such as Rheum palmatum L. Multidrug resistance protein 2 (ABCC2/ MRP2) is an important efflux transporter of substances associated with cellular oxidative stress. However, the effects of traditional Chinese medicine on this protein remain unclear.

Three new diterpenes from and their NO production inhibitory activity.

Three new diterpenes were isolated from the stems of Merr and characterized on the basis of spectral data. Neoclerod-13-ene-3, 4, 15-triol () exhibited the inhibition of lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophages with an IC value of 25.

Inhibition of TPL2 by interferon-α suppresses bladder cancer through activation of PDE4D.

Background: Drugs that inhibit the MEK/ERK pathway have therapeutic benefit in bladder cancer treatment but responses vary with patients, for reasons that are still not very clear. Interferon-α (IFN-α) is also used as a therapeutic agent for bladder cancer treatment but the response rate is low. It was found that IFN-α could enhance the cytotoxic effect of MEK inhibition.

[Photosynthetic mechanism of tea yield and quality affected by different habitats].

To understand photosynthetic mechanism of tea yield and quality, an experiment was conducted with four different typical habitats, including three intercropping patterns (S:Osmanthus-Tea, S:Michelia-Tea, S:Osmanthus-Michelia-Tea) and a control (CK) at Changsha Agricutural Observation Station of Chinese Academy of Sciences. The photosynthetic physiological and ecological characteristics of tea yield and quality were examined. The results showed that the habitats S, S, S reduced the leaf temperature (TL), photosynthesis active radiation flux (PAR), net photosynthetic rate (P), transpiration rate (T), and stomatal conductance (g), as well as the tea polyphenol content.

Dietary quercetin potentiates the antiproliferative effect of interferon-α in hepatocellular carcinoma cells through activation of JAK/STAT pathway signaling by inhibition of SHP2 phosphatase.

Type I interferons (IFN-α/β) have broad and potent immunoregulatory and antiproliferative activities, which are negatively regulated by Src homology domain 2 containing tyrosine phosphatase-2 (SHP-2). Inhibition of SHP2 by small molecules may be a new strategy to enhance the effcacy of type I IFNs. Using an screening assay for new inhibitors of SHP2 phosphatase, we found that quercetin was a potent inhibitor of SHP2.

Flavonoid glycosides and alkaloids from the embryos of Nelumbo nucifera seeds and their antioxidant activity.

Chemical investigation of the embryos of Nelumbo nucifera afforded four new flavone C-glycosides, named nelumbosides A-D (1-4), together with nine known ones, comprising five flavonoids (5-9) and four alkaloids (10-13). The chemical structures of the new compounds were elucidated by 1D, 2D-NMR and HR-ESI-MS techniques, together with chemical methods. Nelumbosides A-D (1-4) are rarely present in naturally occurring flavone C-glycosides featuring a 4-hydroxystyrene unit connected to the flavonoid skeleton.

Bioactive steroidal alkaloids from the fruits of Solanum nigrum.

The investigation of the fruits of Solanum nigrum led to the isolation of four previously undescribed steroidal alkaloids, named solanine A, 7α-OH khasianine, 7α-OH solamargine and 7α-OH solasonine, together with six known ones. The structures of the isolated compounds were elucidated unambiguously by spectroscopic data analyses and chemical methods. Solanine A represents an unusual steroidal alkaloid with an unprecedented 6/5/6/5/5/6 hexacyclic ring system, and its structure was confirmed by X-ray single crystal diffraction analysis.

6-Hydroxy-3-O-methyl-kaempferol 6-O-glucopyranoside potentiates the anti-proliferative effect of interferon α/β by promoting activation of the JAK/STAT signaling by inhibiting SOCS3 in hepatocellular carcinoma cells.

Suppressor of cytokine signaling 3 (SOCS3) is a key negative regulator of type I interferon (IFN α/β) signaling. Inhibition of SOCS3 by small molecules may be a new strategy to enhance the efficacy of type I IFN and reduce its side effects. We established a cell-based screening assay using human hepatoma HepG2 cells stably transfected with a plasmid wherein the luciferase reporter activity was propelled by interferon α-stimulated response element (ISRE), which is a motif specifically recognized by type I IFN-induced activation of Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway.

Nitric oxide production inhibition and mechanism of phenanthrene analogs in lipopolysaccharide-stimulated RAW264.7 macrophages.

Natural phenanthrene derivatives are considered to be important resource for the anti-inflammatory therapeutics, but their structure-activity relationship and mechanisms are still unknown. In this study we evaluated 20 synthesized phenanthrene analogs in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages.

Iridoid Glucosides and Diterpenoids from Caryopteris glutinosa.

Five new iridoid glucoside derivatives (1-5), three new diterpenoids (7, 12, and 15), and 11 known compounds were isolated from the aqueous EtOH extract of Caryopteris glutinosa. Cell-based estrogen biosynthesis assays indicated that caryopteriside C (3) and caryopterisoid B (12) promote the biosynthesis of estrogen E2, with EC50 values of 11.1 and 8.

Multistimuli-Responsive Luminescence of Naphthalazine Based on Aggregation-Induced Emission.

Stimuli-responsive luminescent materials, which are dependent on changes in physical molecular packing modes, have attracted more and more interest over the past ten years. In this study, 2,2-dihydroxy-1,1-naphthalazine was synthesized and shown to exhibit different fluorescence emission in solution and solid states with characteristic aggregation-induced emission (AIE) properties. A remarkable change in the fluorescence of 2,2-dihydroxy-1,1-naphthalazine occurred upon mechanical grinding, heating, or exposure to solvents.