Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.

The NLRP3 inflammasome has been recognized as a promising therapeutic target in drug discovery for inflammatory diseases. Our initial research identified a natural sesquiterpene isoalantolactone (IAL) as the active scaffold targeting NLRP3 inflammasome. To improve its activity and metabolic stability, a total of 64 IAL derivatives were designed and synthesized.

Comparison of drug concentrations in blood and gastric lavage fluid before and after gastric lavage: A case report.

Background: Gastric lavage (GL) is one of the most important early therapies to remove unabsorbed toxins from the gastrointestinal tract. However, the details of performing gastric lavage remain to be established. There is controversy in clinical practice regarding individual choice of the timing of GL and its efficiency.

Synthesis and evaluation of new compounds bearing 3-(4-aminopiperidin-1-yl)methyl magnolol scaffold as anticancer agents for the treatment of non-small cell lung cancer via targeting autophagy.

Magnolol and honokiol are the two major active ingredients with similar structure and anticancer activity from traditional Chinese medicine Magnolia officinalis, and honokiol is now in a phase I clinical trial (CTR20170822) for advanced non-small cell lung cancer (NSCLC). In search of potent lead compounds with better activity, our previous study has demonstrated that magnolol derivative C2, 3-(4-aminopiperidin-1-yl)methyl magnolol, has better activity than honokiol. Here, based on the core of 3-(4-aminopiperidin-1-yl)methyl magnolol, we synthesized fifty-one magnolol derivatives.

Flavonoids with Inhibitory Effects on NLRP3 Inflammasome Activation from .

Eight new flavonoids, including two β-hydroxy/methoxychalcones, velutones A and B ( and ), two 1,3-diarylpropan-1-ols, velutols C and D ( and ), a dihydroxychalcone, velutone E (), a chalcone, velutone F (), a furanoflavanone, velutone G (), and a furanoflavonol, velutone H (), and 14 known compounds were isolated from . Their structures were determined by high-resolution electrospray ionisation mass spectrometry (HR-ESIMS) and spectroscopic data analyses and time-dependent density functional theory electronic circular dichroism (TD-DFT-ECD) calculations. Among the isolated constituents, compound exhibited the most potent inhibitory effect (IC: 1.

Chidamide based combination regimen for treatment of monomorphic epitheliotropic intestinal T cell lymphoma following radical operation: Two case reports.

Background: Monomorphic epitheliotropic intestinal T cell lymphoma (MEITL) is a rare extra-nodal T-cell lymphoma that has uniformly aggressive features with a poor prognosis. No standardized treatment protocols have been established. Previous experience has demonstrated favorable outcomes with combination chemotherapy followed by autologous hematopoietic stem cell transplant.

Modulation of LPS-induced inflammation in RAW264.7 murine cells by novel isoflavonoids from Millettia pulchra.

Millettia pulchra is a renowned anti-inflammatory herbal medicine in southeast provinces of China. However, the underlying anti-inflammation mechanism remained incompletely understood. Herein, four new isoflavones, pulvones A-D and eleven reported constituents were isolated from the stems of Millettia pulchra with their structures being elucidated by HRMS and NMR analysis.

Anti-inflammatory Ellagitannins from for the Treatment of Rheumatoid Arthritis.

Six new ellagitannins, brevipetins B-G ( and -), and a new phenolic glucoside, brevipetin A (), along with six known compounds were isolated from the traditional Chinese medicinal plant . Their structures and absolute configurations were determined by spectroscopic analyses, chemical methods, and TD-DFT-ECD calculations. Compounds - exhibited NO inhibitory effects with IC values of 1.

Design, synthesis and antibacterial evaluation of honokiol derivatives.

Staphylococcus aureus is a major and dangerous human pathogen that causes a range of clinical manifestations of varying severity, and is the most commonly isolated pathogen in the setting of skin and soft tissue infections, pneumonia, suppurative arthritis, endovascular infections, foreign-body associated infections, septicemia, osteomyelitis, and toxic shocksyndrome. Honokiol, a pharmacologically active natural compound derived from the bark of Magnolia officinalis, has antibacterial activity against Staphylococcus aureus which provides a great inspiration for the discovery of potential antibacterial agents. Herein, honokiol derivatives were designed, synthesized and evaluated for their antibacterial activity by determining the minimum inhibitory concentration (MIC) against S.

Separation of caffeoylquinic acids and flavonoids from Asteris souliei by high-performance counter-current chromatography and their anti-inflammatory activity in vitro.

Eleven compounds were successfully separated from Asteris souliei by using a two-step high-performance counter-current chromatography method. The first step involved a reversed phase isocratic counter-current chromatography separation using hexane/ethyl acetate/methanol/water (1:0.8:1:1 v/v/v/v), which produced three fractions, the first two of which were mixtures.

Flavonoids and biphenylneolignans with anti-inflammatory activity from the stems of Millettia griffithii.

Five new flavonoids, griffinones A-E (1-5), a new biphenylneolignan, griffilignan A (6) and ten known compounds were isolated from the n-hexane and EtOAc extracts of Millettia griffithii. The structures of the new compounds were determined by 1D and 2D NMR, and by HRMS. The anti-inflammatory activity of the isolated compounds was evaluated on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.

Synthesis and antiangiogenic activity of novel gambogic acid derivatives.

Gambogic acid (GA) is in a phase II clinical trial as an antitumor and antiangiogenesis agent. In this study, 36 GA derivatives were synthesized and screened in a zebrafish model to evaluate their antiangiogenic activity and toxicity. Derivatives 4, 32, 35, 36 effectively suppressed the formation of newly grown blood vessels and showed lower toxicities than GA as evaluated by zebrafish heart rates and mortalities.

[The clinical features, chemotherapy responses and survival of 223 patients with newly diagnosed multiple myeloma].

Objective: To explore the proportion, clinical and laboratory features, chemotherapy responses and long term survival of different kinds of newly diagnosed multiple myeloma (MM) in China.

Methods: The clinical data of 223 cases of newly diagnosed MM patients were gathered in the First Affiliated Hospital of Sun Yat-sen University from Jan, 2000 to Seb, 2007 were retrospectively analyzed.

Results: The proportions of each kind of MM including IgG, IgA, light chain, IgD, IgM and biclonal MM were 48.

[Efficacy of bortezomib combined dexamethasone in 24 patients with multiple myeloma].

Background & Objective: Bortezomib, a potent and reversible proteasome inhibitor, induces apoptosis of myeloma cells, resulting in durable responses in patients with multiple myeloma (MM). This study was to explore the medical effects and side effects of bortezomib combined dexamethasone in treating newly diagnosed and relapsed or refractory MM, and evaluate the safety of this regimen in the patients with renal impairment.

Methods: Twenty-four MM patients were treated with bortezomib and dexamethasone in a 21-day cycle.

Bis(μ-N,N'-di-4-pyridylpyridine-2,6-diamine)bis[dimethacrylatocobalt(II)] dihydrate.

The Co(II) ion in the title complex, [Co(2)(C(4)H(5)O(2))(4)(C(15)H(13)N(5))(2)]·2H(2)O, has a distorted square-planar coordination formed by the bridging bidentate N,N'-di-4-pyridylpyrid-ine-2,6-diamine (dapmp) ligands and two monodentate carboxyl-ate groups from methacrylates. Two dapmp ligands bridge two Co atoms, forming a dinuclear complex arranged around an inversion centre. N-H⋯O and O-H⋯O hydrogen bonds involving the solvent water mol-ecule result in the formation of a three-dimensional network.

[Efficacy and toxicity of intravenous busulfan-based conditioning before allogeneic peripheral blood stem cell transplantation for leukemia].

Background & Objective: Busulfan (Bu) is commonly used as a component of conditioning regimens for hematopoietic stem cell transplantation. Erratic gastrointestinal absorption as a result of oral administration of Bu not only affects the efficacy, but also increases the risk of toxicity. This study was to analyze the efficacy and toxicity of intravenous Bu and cyclophosphamide (Cy) conditioning before allogeneic peripheral blood stem cell transplantation (allo-PBSCT) for leukemia.

[Effects and prognostic factors of HLA-matched sibling donor allogeneic hematopoietic stem cell transplantation for chronic myelogenous leukemia].

Objective: To retrospectively analyze the curative effects and prognostic factors of HLA-matched sibling donor allogeneic hematopoietic stem cell transplantation (allo-HSCT) for chronic myelogenous leukemia patients (CML).

Methods: Of the 35 CML patients, 26 were males and 9 were females, with a median age of 32 (12 - 50) years. 30 patients were in chronic phase of CML, 5 patients were in accelerated phase.

[Study of TRAIL receptors expression on the mononuclear cells from multiple myeloma patients and KM3 cells].

Objective: To study the differential expression of four TRAIL receptors on bone marrow mononuclear cells (BMMNC) from multiple myeloma (MM) patients and myeloma cell line KM3 cells, to compare their altered expressions after chemotherapy and to explore the mechanisms by which TRAIL selectively kills tumor cells.

Methods: Semi-quantitative reverse transcriptase-polymerase chain reaction (RT-PCR) and flow cytometry were used to investigate the expression of four TRAIL receptors on BMMNCs in 23 MM patients, KM3 cells and 15 controls, and the changes of their expression pattern after chemotherapy and after incubation of KM3 cells with sub-clinical concentration of doxorubicin.

Results: DR4 and DR5 were highly expressed on KM3 cells with no expression of DcR1 and DcR2.

[Efficacy of imatinib mesylate, a specific inhibitor of BCR/ABL tyrosine kinase, on chronic myeloid leukemia in blast phase].

Background & Objective: Chronic myeloid leukemia (CML) in blast phase is refractory with a poor prognosis. This study was to evaluate efficacy of imatinib mesylate, a specific inhibitor of BCR/ABL tyrosine kinase, on CML in blast phase.

Methods: Nineteen patients with CML in blast phase (imatinib treatment group) received induction of cytarabine-based standard chemotherapy for 2 cycles, and 400 mg/d of imatinib mesylate for 4 weeks.

[Effects of combination therapy with all-trans retinoic acid and arsenic trioxide on acute promyelocytic leukemia].

Background & Objective: The mechanism of effect of arsenic trioxide on promyelocytic leukemia is different from that of all-trans retinoic acid. Arsenic trioxide exerts its action by accelerating cell apoptosis, while all-trans retinoic acid by inducing cell differentiation. However, both drugs can inhibit the transcription of tissue factor (TF) mRNA in acute promyelocytic leukemia, and decrease TF level and coagulative activity to normalize coagulopathy.

[Comparison of two conditioning regimens in treatment of leukemia by allogeneic hematopoietic stem cell transplantation].

Background & Objective: The conditioning regimens are the critical factors in the allogeneic hematopoietic stem cell transplantation. This study was conducted to compare the effectiveness and side-effects of two conditioning regimens in allogeneic hematopoietic stem cell transplantation (allo-HSCT).

Methods: Twenty-one cases received busulfan(BU) 16 mg/kg plus cyclophosphamide(CY) 120 mg/kg,the other 23 cases received total body irradiation(TBI) 7.

[Values of soluble thrombomodulin and von Willebrand factor judging reject reaction in liver transplantation].

Objective: To find sensitive and specific laboratory examination items for early diagnosing and monitoring liver transplantation reject reaction.

Methods: Randomly investigate 41 liver transplantation patients, among them there were 16 patients with reject reaction (including 12 with acute rejection, 4 with chronic rejection). Plasma soluble thrombomodulin (STM) and von Willebrand factor (vWF) levels were measured before operation and every other day after operation.