Acute lung injury (ALI) and the acute respiratory distress syndrome (ARDS) are high-mortality and life-threatening diseases that are associated with neutrophil activation and accumulation within lung tissue. Emerging evidence indicates that neutrophil-platelet aggregates (NPAs) at sites of injury increase acute inflammation and contribute to the development of ALI. Although numerous studies have increased our understanding of the pathophysiology of ALI, there is still a lack of innovative and useful treatments that reduce mortality, emphasizing that there is an urgent need for novel treatment strategies. In this study, a new series of small compounds of β-nitrostyrene derivatives (BNSDs) were synthesized, and their anti-inflammatory bioactivities on neutrophils and platelets were evaluated. The new small compound C7 modulates neutrophil function by inhibiting superoxide generation and elastase release. Compound C7 elicits protective effects on LPS-induced paw edema and acute lung injury via the inhibition of neutrophil accumulation, proinflammatory mediator release, platelet aggregation, myeloperoxidase activity, and neutrophil extracellular trap (NET) release. NET formation was identified as the bridge for the critical interactions between neutrophils and platelets by confocal microscopy and flow cytometry. This research provides new insights for elucidating the complicated regulation of neutrophils and platelets in ALI and sheds further light on future drug development strategies for ALI/ARDS and acute inflammatory diseases.

Muntingia calabura (Tiliaceae) is commercially used in healthcare for the improvement of hypertension, myocardial infarction, spasm, and inflammatory conditions. Its fruits can be processed into jam and the leaves can be used for making tea. In the work reported herein a new biflavan, 4'-hydroxy-7,8,3',5'-tetramethoxyflavone (2), and a new dihydrochalcone, (R)-2',β-dihydroxy-3',4'-dimethoxydihydrochalcone (3), have been isolated from the stem wood of M. calabura, together with 12 known compounds (4-15). The structures of these new compounds were elucidated by the interpretations of extensive spectroscopic data. Among the isolated compounds, 5-hydroxy-7-methoxyflavone (5), quercetin (6), and (2S)-7-hydroxyflavanone (10) exhibited potent inhibition of fMLP-induced superoxide anion generation by human neutrophils, with IC50 values of 1.77 ± 0.70, 3.82 ± 0.46, and 4.92 ± 1.71 μM, respectively.

Abstract:A new limonoid, swietemacrophin (1), was isolated from the seeds of Swietenia macrophylla, together with five known compounds 2-6. The structure of 1 was determined through extensive 1D/2D-NMR and mass-spectrometric analyses. Swietemacrophin (1)

Three new and rare chromone derivatives, epiremisporine C (1), epiremisporine D (2), and epiremisporine E (3), were isolated from marine-derived Penicillium citrinum, together with four known compounds, epiremisporine B (4), penicitrinone A (5), 8-hydroxy-1-methoxycarbonyl-6-methylxanthone (6), and isoconiochaetone C (7). Among the isolated compounds, compounds 2–5 significantly decreased fMLP-induced superoxide anion generation by human neutrophils, with IC50 values of 6.39 ± 0.40, 8.28 ± 0.29, 3.62 ± 0.61, and 2.67 ± 0.10 μM, respectively. Compounds 3 and 4 exhibited cytotoxic activities with IC50 values of 43.82 ± 6.33 and 32.29 ± 4.83 μM, respectively, against non-small lung cancer cell (A549), and Western blot assay confirmed that compounds 3 and 4 markedly induced apoptosis of A549 cells, through Bcl-2, Bax, and caspase 3 signaling cascades.

Abstract:Two new sesquiterpenoids-13-hydroxycurzerenone (1) and 1-oxocurzerenone (2)-have been isolated from the rhizomes of Curcuma zedoaria, together with 13 known compounds (3-15). The structures of two new compounds were determined through spectroscopic and MS analyses. Among the isolated compounds, 13-hydroxycurzerenone (1), 1-oxocurzerenone (2), curzerenone (3), germacrone (4), curcolone (5), procurcumenol (6), ermanin (7), curcumin (8), and a mixture of stigmast-4-en-3,6-dione (12) and stigmasta-4,22-dien-3,6-dione (13) exhibited inhibition (with inhibition % in the range of 21.28%-67.58%) against collagen-induced platelet aggregation at 100 µM. Compounds 1, 5, 7, 8, and the mixture of 12 and 13 inhibited arachidonic acid (AA)-induced platelet aggregation at 100 µM with inhibition % in the range of 23.44%-95.36%.

A new amide, beilschamide (1), has been isolated from the stem of Beilschmiedia erythrophloia, together with seven known compounds, N-trans-feruloyltyramine (2), N-trans-feruloyloctopamine (3), vanillin (4), D-tocopheryl quinone (5), E-sitostenone (6), E-sitosterol (7), and 6D-hydroxystigmast-4-en-3-one (8). The structure of the new compound 1 was determined through spectroscopic and MS analyses. N-trans-Feruloyloctopamine (3) and beilschamide (1) exhibited cytotoxic effects with IC 50 values of 10.3 and 21.2 Pg/mL, respectively, against CCRF-CEM cell line. Beilschmiedia erythrophloia Hay. (Lauraceae) is an evergreen tree, distributed throughout South Mainland China, Hainan Island, the Ryukyus, and Taiwan [1]. Alkaloids [2, 3], flavonoids [4], endiandric acids [5-7], lignans [8, 9], benzenoids [7, 8], steroids [6-9], triterpenoids [7,9], fatty acid esters [7,9], and their derivatives are widely distributed in plants of the genus Beilschmiedia. Many of these compounds exhibit diverse biological activities, including cytotoxic [8] and antitubercular [7,9] activities. In a preliminary screening, the methanolic extract of the root of this species showed cytotoxic activities in vitro. The current phytochemical investigation of the stem of this plant has led to the isolation of a new amide, beilschamide (1), along with seven known compounds. The structural elucidation of 1 and its cytotoxic property are described herein.Extensive fractionation of the EtOAc-soluble portion of a MeOH extract of leaves of Beilschmiedia erythrophloia using silica gel column chromatography (CC), MPLC, and preparative TLC afforded compounds 1-8.Compound 1 was isolated as a yellowish amorphous powder. The HR-ESI-MS gave an [M + Na] + ion at m/z 380.1470 (calcd for C 20 H 23 NO 5 Na, 380.1474), consistent with a molecular formula of C 20 H 23 NO 5 . IR absorptions for NH, OH (3355, 3265 cm -1 ), and carbonyl (1652 cm -1 ) functions were observed. The signals of the 1 H and 13 C NMR spectra of 1 were assigned to a 3,4-dimethoxyphenyl, a 4-hydroxyphenyl, a conjugated double bond, a methoxy, an oxymethine, and a methylene. Comparison of the 1 H and 13 C NMR data of 1 with those of 3-(4-hydroxy-3-methoxyphenyl)-N-[2-(4-hydroxyphenyl)-2-methoxyethyl]acrylamide [10] suggested that their structures were closely related, except for the 3,4-dimethoxyphenyl group [G H 3.87 (6H, s, 3, 4-OMe), 6.96 (1H, d, J = 8.5 Hz, H-5), 7.13 (1H, dd, J = 8.5, 2.0 Hz, H-6), 7.16 (1H, d, J = 2.0 Hz, H-2); at C-7 of 1 replacing the 4-hydroxy-3-methoxyphenyl group of 3-(4-hydroxy-3-methoxyphenyl)-N-[2-(4-hydroxyphenyl)-2-methoxyethyl]acrylamide [10].

Four new 2-(2-phenylethyl)-4-chromen-4-one derivatives, 6-hydroxy-5-methoxy-2-[2-(4'-methoxyphenyl)ethyl]chromone (1: ), 6,7-dimethoxy-2-[2-(2'-hydroxyphenyl)ethyl]chromone (2: ), 5-hydroxy-6-methoxy-2-[2-(3'-methoxyphenyl)ethyl]-chromone (3: ), and 7-chloro-8-hydroxy-2-[2-(4'-methoxyphenyl)ethyl]chromone (4: ), have been isolated from the resinous wood of , together with 16 known compounds (5: -20: ). Among these, 7-methoxy-2-[2-(4'-methoxyphenyl)ethyl]chromone (5: ) was isolated from a natural source for the first time. The structures of the new compounds were established by spectroscopic analyses (1D and 2D NMR, HR-ESI-MS, IR, UV). Nine compounds, including 1: showed more than 80% inhibition of superoxide anion generation by human neutrophils in response to formyl-L-methionyl-L-leucyl-L-phenylalanine at 50 µM.

Three new and uncommon chromone analogs, epiremisporine F (1), epiremisporine G (2), and epiremisporine H (3), were isolated from marine-origin Penicillium citrinum. Among the isolated compounds, compounds 2–3 remarkably suppressed fMLP-induced superoxide anion generation by human neutrophils, with IC50 values of 31.68 ± 2.53, and 33.52 ± 0.42 μM, respectively. Compound 3 exhibited cytotoxic activities against human colon carcinoma (HT-29) and non-small lung cancer cell (A549) with IC50 values of 21.17 ± 4.89 and 31.43 ± 3.01 μM, respectively, and Western blot assay confirmed that compound 3 obviously induced apoptosis of HT-29 cells, via Bcl-2, Bax, and caspase 3 signaling cascades.