Brusatol, a biologically active natural product, was modified in four distinct positions through the covalent attachment of furoxan moiety, which acts as nitric oxide (NO) donor. Forty derivatives were synthesized and evaluated for their inhibitory effects on excess NO biosynthesis activated macrophages. Among them, compound 75 demonstrated inhibition (IC50 = 0.067 μM) comparable to that brusatol but less cytotoxic. More importantly, even at very low doses (2 μmol/kg/day), also showed...

Ceramide functions as an important second messenger in apoptosis signaling pathways. In this report, we show that treatment of NT-2 neuronal precursor cells with hypoxia/reoxygenation (H/R) resulted ceramide up-regulation. This elevation was primarily due to the actions acid sphingomyelinase and synthase LASS 5, demonstrating action salvage pathway. Hypoxia/reoxygenation led Bax translocation from cytoplasm mitochondria cytochrome c release mitochondria. Down-regulation either or...

Although the Chinese herb Gnetum cleistostachyum has been used as a remedy for cancers hundred years, active compounds and molecular mechanisms underlying its anti-cancer activity have not explored. Recently new derivative of stilbene compound, isorhapontigenin (ISO), was isolated from this herb. In present study, we examined potential ISO in involved human cancer cell lines. We found that exhibited significant inhibitory effects on bladder growth accompanied by marked apoptotic induction...

Epoxyeicosatrienoic acids (EETs) are metabolic products of free arachidonic acid, which produced through cytochrome P-450 (CYP) epoxygenases. EETs have anti-inflammatory, antiapoptotic, and antioxidative activities. However, the effect on cigarette smoke-induced lung inflammation is not clear. Autophagy believed to be involved in pathogenesis chronic obstructive pulmonary disease. In addition, nuclear erythroid-related factor 2 (Nrf2), a transcription that regulates many antioxidant genes,...

Twelve new dihydroagarofuran sesquiterpene polyol esters, triptersinines A–L (1–12), and eight known pyridine alkaloids were isolated from the leaves of Tripterygium wilfordii. Their structures elucidated on basis spectroscopic analyses, including UV, IR, NMR experiments (1H–1H COSY, NOESY, HSQC, HMBC). Furthermore, in an vitro bioassay, compounds 1, 9, 11, 13, 14, 18 showed moderate inhibitory effects nitric oxide production LPS-induced macrophages at 5 μM; all inactive when tested against...

Cigarette smoke (CS) increases the risk of chronic obstructive pulmonary disease (COPD) by causing inflammation, emphysema, and reduced lung function. Additionally, CS can induce autophagy which contributes to COPD. Arachidonic acid-derived epoxyeicosatrienoic acids (EETs) have promising anti-inflammatory properties that may protect heart liver regulating autophagy. For this reason, effect decreased soluble epoxide hydrolase (sEH, Ephx2)-mediated EET hydrolysis on function, was here studied...

Background/Aims: Epoxyeicosatrienoic acids (EETs), a type of lipid mediators produced by cytochrome P450 epoxygenases, exert anti-inflammatory, angiogenic, anti-oxidative and anti-apoptotic effects. However, the role EETs in cigarette smoke-induced lung injury underlying mechanisms are not fully known. The aim this study was to explore effects CYP2J2-EETs on smoke extracts (CSE)-induced apoptosis human bronchial epithelial cell line (Beas-2B) possible involved. Methods: Cytochrome...

Ginsenoside Rg1 (GR), a major bioactive compound of traditional Chinese medicine, such as Panax ginseng or Radix Notoginseng, has been shown to exert neuroprotective effects against ischemic stroke. However, pharmacokinetic studies have suggested that GR could not be efficiently transported through the blood-brain barrier. The mechanism by which attenuates cerebral injury in vivo remains largely unknown. Therefore, this study explored potential neuro-protective its systemic metabolic...

Methylophiopogonanone A (MO-A), an active homoisoflavonoid of the Chinese herb Ophiopogon japonicus which has been shown to have protective effects on cerebral ischemia/reperfusion (I/R) injury, demonstrated anti-inflammatory and anti-oxidative properties. However, little is known about its role in I/R injury. Therefore, this study, by using a middle artery occlusion (MCAO) reperfusion rat model, effect MO-A injury was examined. The results showed that treatment reduced infarct volume brain...

Background Histone deacetylase 2 (HDAC2) is a class I histone family member that plays critical role in suppressing inflammatory gene expression the airways, lung parenchyma, and alveolar macrophages patients with chronic obstructive pulmonary disease (COPD). However, of HDAC2 peripheral blood monocytes (PBMCs), nuclear factor kappa B (NF-κB) p65, serum cytokine levels COPD patients, smokers, non-smokers remains unclear. Methods PBMCs were obtained from healthy nonsmokers. The NF-κB p65...

Anesthesia and analgesia are essential components for surgical procedures. While the neurotoxic effects of multiple anesthesia exposures during brain development well established, combined impact surgery with on neurodevelopmental remains unknown. In this study, neonatal mice underwent fentanyl sevoflurane (MSFS) postnatal days 6, 8, 10, resulting in attention deficit hyperactivity disorder (ADHD)-like hyperactivity, impulsive behavior, cognitive impairment, fine motor dysfunction adulthood....

Aplastic anemia (AA) is a refractory hematological disease with limited therapeutic effectiveness and serious treatment-related side effects. Cytotoxic T lymphocytes (CTLs) play key role in AA pathogenesis. In our previous study, sinomenine derivative 3a was obtained, which demonstrated potential anti-AA activity by targeting CTLs low toxicity. this novel metabolite, 3a-M1, identified optimized bioavailability from metabolism, exhibited more notable effect alleviating symptoms, suppressing...

Chronic obstructive pulmonary disease (COPD) is a complex and heterogeneous characterized by persistent airflow limitation but still lacking effective treatments. Perilla frutescens (L.) Britt., an important traditional medicinal plant with excellent antioxidant anti-inflammatory properties, widely used for the treatment of respiratory in China. However, its protective activity mechanism against COPD airway inflammation have not been fully studied. Here, effects PLE were investigated,...

Abstract The low‐grade, chronic inflammation initiated by TLR4‐triggered innate immune responses has a central role on early osteoarthritis. Amurensin H is resveratrol dimer with anti‐inflammatory and anti‐apoptotic effects, while its effects TLR‐4 signals to inhibit osteoarthritis are still unclear. In the present study, treatment amurensin for 2 weeks in monosodium iodoacetate‐induced mice significantly slows down cartilage degeneration using macroscopic evaluation, haematoxylin eosin (HE)...

Amurensin H, a resveratrol dimer derived from Vitis amurensis Rupr, has several biological effects, including anti-inflammatory and antioxidant activities. Studies have found that amurensin H attenuated asthma-like allergic airway inflammation. However, its protective activity on chronic obstructive pulmonary disease (COPD) inflammation is not fully explored. The present study used lipopolysaccharide (LPS)/cigarette smoke-induced mice model an LPS-stimulated THP-1-derived macrophages to...

Pirfenidone, a pyridone compound, is an effective and novel antifibrotic agent. In this article, we describe the design, synthesis activity evaluation of agents, 1-(substituted aryl)-5-trifluoromethyl-2(1H) pyridones modified with carbohydrate. Most title compounds exhibited comparable or better inhibitory than fluorofenidone. Notably, compound 19a demonstrated highest cell-based against NIH 3T3 (IC(50) = 0.17 mM).

Background Tamarixinin A, a natural tannin isolated from Myricaria bracteata, has been confirmed to have moderate anti-inflammatory effects in vitro and vivo. However, how it rheumatoid arthritis (RA) is still unknown. Therefore, the aim of this study investigate therapeutic tamarixinin A on experimental RA, explore underlying mechanism. Methods The anti-arthritic were evaluated collagen-induced (CIA) mice adjuvant-induced (AIA) rats. hind paw thickness, inflammatory cytokine levels serum,...