Discovery of a New Anti-Inflammatory Agent from Anemoside B4 Derivatives and Its Therapeutic Effect on Colitis by Targeting Pyruvate Carboxylase.

Anemoside B4 (AB4), a triterpenoidal saponin from , shows significant anti-inflammatory activity, and may be used for treating inflammatory bowel disease (IBD). Nevertheless, its application is limited due to its high molecular weight and pronounced water solubility. To discover new effective agents for treating IBD, we synthesized 28 AB4 derivatives and evaluated their cytotoxic and anti-inflammatory activities .

Rosamultin ameliorates radiation injury via promoting DNA injury repair and suppressing oxidative stress in vitro and in vivo.

Radiotherapy remains the preferred treatment option for cancer patients with the advantages of broad indications and significant therapeutic effects. However, ionizing radiation can also damage normal tissues. Unfortunately, there are few anti-radiation damage drugs available on the market for radiotherapy patients.

Anemoside B4 inhibits SARS-CoV-2 replication and .

Objective: Anemoside B4 (AB4), the most abundant triterpenoidal saponin isolated from , inhibited influenza virus FM1 or -induced pneumonia. However, the anti-SARS-CoV-2 effect of AB4 has not been unraveled. Therefore, this study aimed to determine the antiviral activity and potential mechanism of AB4 in inhibiting human coronavirus SARS-CoV-2 and .

Anemoside B4, a new pyruvate carboxylase inhibitor, alleviates colitis by reprogramming macrophage function.

Objectives: Colitis is a global disease usually accompanied by intestinal epithelial damage and intestinal inflammation, and an increasing number of studies have found natural products to be highly effective in treating colitis. Anemoside B4 (AB4), an abundant saponin isolated from Pulsatilla chinensis (Bunge), which was found to have strong anti-inflammatory activity. However, the exact molecular mechanisms and direct targets of AB4 in the treatment of colitis remain to be discovered.

Ephrin B3 exacerbates colitis and colitis-associated colorectal cancer.

Ephrin B3, a member of Eph/ephrin family, contributes to embryogenesis and carcinogenesis, but few studies have suggested whether this ligand has regulatory effect on colitis. This study was to determine whether ephrin B3 played a role in colitis and colonic carcinogenesis. Dextran sodium sulfate (DSS)-induced colitis and azoxymethane (AOM)/DSS-induced colitis-associated carcinogenesis model was established in Efnb3-deficient (Efnb3) mice.

Pedunculoside inhibits epithelial-mesenchymal transition and overcomes Gefitinib-resistant non-small cell lung cancer through regulating MAPK and Nrf2 pathways.

Background: Lung cancer is the primary cause of cancer-related mortality worldwide owing to its strong metastatic ability. EGFR-TKI (Gefitinib) has demonstrated efficacy in metastatic lung cancer therapy, but most patients ultimately develop resistance to Gefitinib, leading to a poor prognosis. Pedunculoside (PE), a triterpene saponin extracted from Ilex rotunda Thunb.

Hederacoside C ameliorates colitis via restoring impaired intestinal barrier through moderating S100A9/MAPK and neutrophil recruitment inactivation.

Hederacoside C (HSC) has attracted much attention as a novel modulator of inflammation, but its anti-inflammatory mechanism remains elusive. In the present study, we investigated how HSC attenuated intestinal inflammation in vivo and in vitro. HSC injection significantly alleviated TNBS-induced colitis by inhibiting pro-inflammatory cytokine production and colonic epithelial cell apoptosis, and partially restored colonic epithelial cell proliferation.

Silencing Tautomerization to Isolate Unstable Physalins from .

The inherent structural instability of some physalins has hampered the isolation and identification of these compounds for approximately 50 years, and an effective method to overcome these challenges remains unavailable. In the present study, the unprecedented tautomerization mechanism of unstable physalins was elucidated by performing isotopic labeling experiments and DFT calculations, which led to the successful separation of tautomers and isolation of highly pure products for the first time. As a result, 15 new physalins, physaminins A-O (-), as well as 17 known analogues (-), were isolated from the whole plants of L.

Activation of spinal ephrin-B3/EphBs signaling induces hyperalgesia through a PLP-mediated mechanism.

Ephrin B/EphB signaling pathway is involved in the regulation of pain caused by spinal cord injury. However, the role of ephrin-B3/EphBs signaling in regulation of nociceptive information is poorly understood. In the present study, formalin-induced inflammatory pain, mechanical allodynia and thermal hyperalgesia, was measured using Efnb3 mutant mice (Efnb3 ) and wild-type (Efnb3 ) mice.

Rosamultin from Potentilla anserine L. exhibits nephroprotection and antioxidant activity by regulating the reactive oxygen species/C/EBP homologous protein signaling pathway.

Rosamultin, a major bioactive constituent from Potentilla anserine L., has antioxidative and hepatoprotective activities. However, its protective effects on cisplatin-induced acute renal injury and the underlying mechanisms remain elusive.

Naturally occurring physalins from the genus Physalis: A review.

Physalins, including physalins and neophysalins, are a class of highly oxygenated ergostane-type steroids. They are commonly known by the name of 16,24-cyclo-13,14-seco steroids, in which the disconnection of C-13 and C-14 produces an eight or nine-membered ring and the carbocyclization of C-16 and C-24 generates a new six-membered ring. Meanwhile, the oxidation of C-18 methyl to carboxyl group forms a 18,20-lactone, and the oxidation of C-14 and C-17 gets a heterocyclic oxygen acrossing rings C and D.

Anemoside B4 inhibits enterovirus 71 propagation in mice through upregulating 14-3-3 expression and type I interferon responses.

Enterovirus 71 (EV71) is the major pathogens of human hand, foot, and mouth disease (HFMD). EV71 efficiently escapes innate immunity responses of the host to cause infection. At present, no effective antiviral drugs for EV71 are available.

Rotundic acid reduces LPS-induced acute lung injury in vitro and in vivo through regulating TLR4 dimer.

Acute lung injury (ALI) is a serious clinical disease. Rotundic acid (RA), a natural ingredient isolated from Ilex rotunda Thunb, exhibits multiple pharmacological activities. However, RA's therapeutic effect and mechanism on ALI remain to be elucidated.

Anemoside B4 ameliorates TNBS-induced colitis through S100A9/MAPK/NF-κB signaling pathway.

Background: Despite the increased morbidity of ulcerative colitis (UC) in the developing countries, available treatments remain unsatisfactory. Therefore, it is urgent to discover more effective therapeutic strategies. Pulsatilla chinensis was widely used for the treatment of inflamed intestinal diseases including UC for thousands of years in China.

Anemoside B4 Protects against Acute Lung Injury by Attenuating Inflammation through Blocking NLRP3 Inflammasome Activation and TLR4 Dimerization.

Acute lung injury (ALI) is an acute inflammatory process in the lung parenchyma. Anemoside B4 (B4) was isolated from Pulsatilla, a plant-based drug against inflammation and commonly applied in traditional Chinese medicine. However, the anti-inflammatory effect and the mechanisms of B4 are not clear.

Triterpenoid saponins from Ilex cornuta protect H9c2 cardiomyocytes against H2O2-induced apoptosis by modulating Ezh2 phosphorylation.

Ethnopharmacological Relevance: Ilex cornuta Lindl. et Paxt. (Aquifoliaceae family) belongs to the Ilex genus.

Ginsenoside Rb1 is an immune-stimulatory agent with antiviral activity against enterovirus 71.

Ethnopharmacological Relevance: According to the theory of traditional Chinese medicine, the main pathogenesis of severe hand, foot and mouth disease (HFMD) is that the heat and wet poisons are deeply trapped in the viscera, which causes the deficiency of Qi and Yin in the patient's body. Ginsenoside Rb1 (Rb1) is the most abundant triterpenoid saponin in Panax quinquefolius L., which has the function of Qi-invigorating and Yin-nourishing.

Anemoside B4 protects against - and influenza virus FM1-induced pneumonia via the TLR4/Myd88 signaling pathway in mice.

Background: Pneumonia refers to the inflammation of the terminal airway, alveoli and pulmonary interstitium, which can be caused by pathogenic microorganisms, physical and chemical factors, immune damage, and drugs. Anemoside B4, the major ingredient of (Bunge) Regel, exhibited anti-inflammatory activity. However, the therapeutic effect of anemoside B4 on pneumonia has not been unraveled.

Anti-inflammatory Withanolides from .

Five new withanolides () along with five known ones () were isolated from the whole plants of Linn. The chemical structures of the new compounds were identified as (20,22) 15-acetoxy-5β,6β-epoxy-4β,14,28-trihydroxy-3β-methoxy-1-oxowitha-16,24-dienolide (), (20,22) 15-acetoxy-5β,6β-epoxy-3β,4β,14β,17β,20β-pentahydroxy-1-oxowitha-24-enolide (), (20,22) 15α-acetoxy-4β,5α,6β,14α,20β-pentahydroxy-1-oxowitha-2,24-dienolide (), (20,22) 15α-acetoxy-5α,6β,14α,20β-tetrahydroxy-1-oxowitha-2,24-dienolide (), and (20,22) 5α,6β,14β-trihydroxy-1,15-dioxowitha-2,16,24-trienolide () on the basis of integration combining IR, UV, HR-ESI-MS, 1D-NMR, and 2D-NMR analyses. Biologically, compounds () were subjected to evaluate their anti-inflammatory activities inhibiting nitric oxide production in lipopolysaccharide-stimulated murine RAW 264.

Anticancer activity of oleiferoside B involving autophagy and apoptosis through increasing ROS release in MCF-7 cells and SMMC-7721 cells.

Oleiferoside B is a triterpenoid monomer compound, mainly isolated from roots of Abel, the underlying mechanism of its antitumour is not clear. In the present study, oleiferoside B potently inhibited SMMC-7721 and MCF-7 cells proliferation and cause cells apoptosis. In addition, it activated an autophagy-mediated cell death pathway, as indicated by the accumulated the ratio of LC3- II/LC3- I and inhibited apoptosis protein expression after pre-treatment with autophagy inhibitors 3-MA.

Cryptotanshinone from Bunge (Danshen) inhibited inflammatory responses via TLR4/MyD88 signaling pathway.

Background: Cryptotanshinone (CPT), as a major component of Bunge (Danshen), displays many pharmacological activities including anti-inflammatory effects. However, the exact cellular and molecular mechanisms of the anti-inflammatory activities of CPT remain to be elucidated. The present study was aimed to clarify its mechanisms on lipopolysaccharide (LPS)-induced inflammatory responses in mouse macrophages, RAW264.

Ginsenoside Rb1 exerts anti-inflammatory effects in vitro and in vivo by modulating toll-like receptor 4 dimerization and NF-kB/MAPKs signaling pathways.

Backgound: Ginsenoside Rb1, the main active constituent of Panax ginseng, displays significant anti-inflammatory activity, although the mechanism has not been clearly unraveled. In this study, Rb1's mechanism of anti-inflammatory effects were investigated.

Methods: The flow cytometry and enzyme-linked immunosorbent assay (ELISA) were empolyed to detect pro-inflammatory cytokines release.

Five new 5,6-β-epoxywithanolides from Physalis minima.

Five new 5,6-β-epoxywithanolides (1-5) were isolated from the whole plants of Physalis minima L. Their structural elucidations were achieved by the extensive spectroscopic analysis (IR, UV, HR-ESI-MS, 1D-NMR, and 2D-NMR). The isolates were evaluated for their anti-inflammatory activities on lipopolysaccharide-induced nitric oxide production in RAW 264.

Induction of an MLKL mediated non-canonical necroptosis through reactive oxygen species by tanshinol A in lung cancer cells.

Recent discoveries revealed several types of programmed necrosis, such as necroptosis, ferroptosis, pyroptosis, etc. Necroptosis is mediated by signaling complexes with receptor-interacting protein kinases (RIPs) and mixed lineage kinase domain-like protein (MLKL). Here, we described an MLKL mediated non-canonical necroptosis through reactive oxygen species (ROS) in lung cancer cells triggered by a natural compound, tanshinol A (TSA).

Anti-inflammatory and immune-modulatory properties of anemoside B4 isolated from Pulsatilla chinensis in vivo.

Background: Pulsatilla chinensis is commonly used for the treatment of cancers and inflammatory disorders in China. Our recent studies showed that anemoside B4, its major ingredient, possessed notable antioxidant and protected cisplatin-induced acute kidney injury in vivo. Furthermore, we found the protective effect might be involved its anti-inflammation activities.