A new polyoxygenated cyclohexane and other constituents from <i>Kaempferia rotunda</i> and their cytotoxic activity

<div><p>The isolation of secondary metabolites from a methanolic extract of <i>Kaempferia rotunda</i> yielded 12 compounds (<b>1</b>–<b>12</b>), including a new polyoxygenated cyclohexane compound, (–)-3-acetyl-4-benzoyl-1-benzoyloxymethyl-1,6-diepoxycyclohexan-2,3,4,5-tetrol (<b>1</b>). The structures of the isolated compounds were determined based on their spectroscopic data and comparison with references. All of the isolated compounds were tested for their cytotoxic activity against pancreatic (PSN-1) and breast (MDA-MB231) cancer cell lines. Compound <b>12</b> showed moderate cytotoxic activity against PSN-1 and MDA-MB231 without showing any cytotoxicity against the normal cell line, TIG-3.</p></div

Muchimangins G–J, Fully Substituted Xanthones with a Diphenylmethyl Substituent, from <i>Securidaca longepedunculata</i>

Four highly oxygenated xanthones, muchimangins G–J (<b>1</b>–<b>4</b>), have been isolated from the roots of <i>Securidaca longepedunculata</i> collected in Democratic Republic of Congo. Their structures were elucidated by analyses of spectroscopic data to be fully substituted xanthones with a diphenylmethyl substituent at C-2

Prenylation of a Nonaromatic Carbon of Indolylbutenone by a Fungal Indole Prenyltransferase

FtmPT1 from <i>Aspergillus fumigatus</i> is a fungal indole prenyltransferase (PT) that normally catalyzes the regiospecific prenylation of brevianamide F (cyclo-l-Trp-l-Pro) at the C-2 position of the indole ring with dimethylallyl diphosphate (DMAPP). Interestingly, FtmPT1 exhibited remarkable substrate tolerance and accepted (<i>E</i>)-4-(1<i>H</i>-indol-3-yl)but-3-en-2-one (<b>1</b>) as a substrate to produce an unnatural novel α-prenylindolylbutenone (<b>1a</b>). This is the first demonstration of the prenylation of a nonaromatic carbon of the acceptor substrate by a fungal indole PT

Kaempulchraols A–H, Diterpenoids from the Rhizomes of <i>Kaempferia pulchra</i> Collected in Myanmar

Eight new diterpenoids, kaempulchraols A–H (<b>1</b>–<b>8</b>), along with five known analogues were isolated from the CHCl₃-soluble extract of rhizomes of <i>Kaempferia pulchra</i> of Myanmar. The structures of these compounds were elucidated using extensive spectroscopic techniques including X-ray diffraction analysis. All the isolates were tested for their antiproliferative activity against a panel of five human cancer cell lines (A549, human lung cancer; HeLa, human cervix cancer; PANC-1 and PSN-1, human pancreatic cancer; MDA-MB-231, human breast cancer) and TIG-3, normal human primary fibroblast cells. Kaempulchraol F (<b>6</b>) exhibited weak activity against the human pancreatic PSN-1 cell line with an IC₅₀ value of 12.3 μM

A new sterol from the Vietnamese marine sponge <i>Xestospongia testudinaria</i> and its biological activities

<p>A new sterol, langcosterol A (<b>1</b>), together with two known sterols <b>2</b> and <b>3</b>, were isolated from the marine sponge <i>Xestospongia testudinaria</i> collected in Vietnam. Their chemical structures were elucidated on the basis of extensive spectroscopic analyses and comparisons with published data. The new compound <b>1</b> and the known compound <b>3</b> exhibited moderate cytotoxic activities against three human cancer cell lines (A549, lung cancer; MCF7, breast cancer; HeLa, cervical cancer) and a human normal cell line (WI-38 fibroblast), with IC₅₀ values ranging from 29.0 to 68.0 μM.</p

A kaempferol triglycoside from <i>Tephrosia preussii</i> Taub. (Fabaceae)

<p>A phytochemical investigation of the MeOH extract of twigs and leaves of <i>Tephrosia preussi</i> was carried out to give a new kaempferol triglycoside, named tephrokaempferoside (<b>1</b>), together with five known compounds: tephrosin (<b>2</b>), betulinic acid (<b>3</b>), lupeol (<b>4</b>), <i>β</i>-sitosterol (<b>5</b>) and 3-<i>O</i>-<i>β</i>-d-glucopyranoside of <i>β</i>-sitosterol (<b>6</b>). The structure of the new compound was characterised by analyses of NMR (1D and 2D) and MS data, and chemical conversion. Tephrokaempferoside (<b>1</b>) had weak antibacterial activity against <i>Klebsiella pneumoniae</i> with an MIC value of 150 μg/mL.</p

Additional file 1: of Spontaneous adrenocorticotropic hormone (ACTH) normalisation due to tumour regression induced by metyrapone in a patient with ectopic ACTH syndrome: case report and literature review

Figure S1. Enlargement of the lung tumour on day 14. (TIFF 48 kb

Decreased production of highly reactive oxygen species production induced by complement-mediated phagocytosis in Rab27a-knockdown cells.

<p>(A–D) Both Rab27a-knockdown HL60 cells (Rab27aKD; clone 1 and clone 2) and control-shRNA transferred HL60 cells (Control; clone 1 and clone 2) were treated with ATRA for 3 days and complement-mediated phagocytosis assay was performed using serum-opsonized Texas Red-labeled zymosan. (A) At 30 min after the onset of phagocytosis, uptake of zymosan particles in Rab27a-knockdown cells was analyzed by flow cytometry. In the presence of APF, (B) microscopic analysis and (C) flow cytometric analysis were performed at 30 min after the onset of phagocytosis. In (B) and the cytograms of (C), the results of Rab27aKD clone 1 and Control clone 1 are shown as representative data. In (B), hypochlorite appears green and Texas Red-labeled zymosan is red. Scale bars indicate 5 µm. (D) In the presence of HPF, flow cytometric analysis was performed at 30 min after the onset of phagocytosis. In (A), (C), (D), the data are the mean with SD from three independent experiments. Asterisks (*) mean that the difference is statistically significant (p values<0.01). NS means no statistical significance.</p

Effects of Rab27a-knockdown on neutrophil-like differentiaiton of HL60 cells.

<p>(A–C) HL60 cells, Rab27a-knockdown cells transfected with shRNA-Rab27a using a lentiviral system (Rab27aKD; clone 1 and clone 2) and control-shRNA transferred HL60 cells (Control; clone 1 and clone 2) were treated with ATRA for 3 days. (A) The expression of Rab27a in similarly treated cells were analyzed by immunoblotting analysis. (B) Morphology and (C) cell surface expression of CR3 were analyzed by May-Giemsa staining and flow cytometry, respectively. In (B), Rab27aKD clone 1 and Control clone 1 are shown as representative images. (D) Expression of myeloperoxidase (MPO) in whole cell lysates were analyzed by immunoblotting analysis. Scale bars indicate 10 µm.</p

The effects of Rab27a-knockdown on PMA-induced NET formation.

<p>(A–C) Neutrophil-like differentiated control HL60 cells (Control; clone 1 and clone 2) and Rab27a-knockdown cells (Rab27aKD; clone 1 and clone 2) were stimulated with PMA. (A) Both cells fixed with PFA were stained with Hoechst 33342 (left). Cell lysates were assesed by immunoblotting analysis using specific antibody against H4cit3 and histone H4 (middle). PFA-fixed cells were stained with antibody against H4cit3 in the presence of Hoechst 33342 (right). Scale bars indicate 10 µm. (B) Representative fluorescence images at 4 hours after PMA treatment in the presence of both Hoechst 33342 and Sytox Green. Scale bars indicate 10 µm. Blue and green colors show Hoechst 33342-positive and Sytox Green-positive, respectively (left). The results of Rab27aKD clone 1 and Control clone 1 are shown as representative data. Frequency of Sytox Green-positive cells at indicated time points after PMA treatment (middle). The percentage of the cells in the individual stages at 4 h after PMA treatment (right). (C) The mean fluorescence intensity (MFI) after PMA treatment in the presence of APF at 30 min (left) or CM-H₂DCFDA at 20min (right). The mean value of MFI of control cells was adjusted to 1. In (B) and (C), the data are the mean with SD from three independent experiments.</p