Wonsik Jeong

Bioactive triterpenoids from Callistemon lanceolatus.

A new triterpenoid, 30-hydroxyalphitolic acid 1, and eight known triterpenoids, alphitolic acid 2, lupenol 3, 3-acetoxy-olean-18-en-28-oic acid 4, betulinic acid 5, ursolic acid 6, betulinic acid 3-O-caffeate 7, morolic acid 3-O-caffeate 8, and ursolic acid 3-O-caffeate 9, were isolated from Callistemon lanceolatus. Their structures were determined using spectroscopic techniques, which included 1D- and 2D-NMR. All compounds were evaluated for the inhibition of LPS-induced nitric oxide production in murine macrophage RAW264.7 cells. Betulinic acid 3-O-caffeate 7 showed a moderate inhibitory effect on nitric oxide production with IC50 value of 15.4 μM.

Acetylenic acid analogues from the edible mushroom Chanterelle (Cantharellus cibarius) and their effects on the gene expression of peroxisome proliferator-activated receptor-gamma target genes.

A new acetylenic acid, (10E,14Z)-9-oxooctadeca-10,14-dien-12-ynoic acid (1), was isolated from the edible mushroom Chanterelle (Cantharellus cibarius), together with a known acetylenic acid, (10E,14Z)-9-hydroxyoctadeca-10,14-dien-12-ynoic acid (2) and their structures were determined through analysis of NMR and mass data. The new acetylenic acid (1) specifically activated peroxisome proliferator-activated receptor (PPAR)-γ with an EC(50) value of 1.88 μM as measured by a reporter gene assay. Expression of PPAR-γ target genes were significantly altered as well, supporting the hypothesis that compound 1 is a PPAR-γ potential agonist that regulates transcription of the PPAR-γ target genes.

Ulmus davidiana Nakai induces apoptosis and autophagy on non-small cell lung cancer cells ☆

ETHNOPHARMACOLOGICAL RELEVANCE Ulmus davidiana Nakai (UDN) is frequently used in the treatment of cancer in traditional oriental medicine. Although several reports indicate that UDN has inhibitory effects in some cancers, there has been no report on the inhibitory effects of UDN via both autophagy and apoptosis. MATERIALS AND METHODS Cytotoxicity induced by UDN in human non-small cell lung cancer (NSCLC) H-1299 and H-460 cell lines was evaluated using the 2, 3-Bis (2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide inner salt (XTT) assay and trypan blue exclusion assay. Induction of apoptosis was also investigated using Hoechst staining and annexin-V binding assay and was confirmed with western blot analysis. Induction of autophagy was investigated through observation of autophagy vacuoles under inverted phase-contrast microscopy and was confirmed by observing the formation of autophagy vacuoles under a fluorescence microscope using monodansylcadaverine (MDC) staining and western blot analysis. The in vivo anti-tumorigenic effect of UDN was investigated in an athymic nude mouse xenograft model using H-1299 NSCLC cells. RESULTS UDN exhibited a marked inhibitory effect on cell growth in H-1299 and H-460 human NSCLC cell lines in a dose- and time-dependent manner in vitro and in vivo. It induced not only apoptosis, but also autophagy in both H-1299 and H-460 cells in a dose-dependent manner. UDN-mediated autophagy led to the accumulation of autophagosome, resulting in apoptosis induction and cell death. CONCLUSIONS From our current knowledge, we are the first to demonstrate that UDN has the potential to induce both autophagy and apoptosis in H-1299 and H-460 human NSCLC cell lines. We suggest that UDN can be considered a potential candidate for lung cancer-specific chemotherapy with efficacy as a cytotoxic agent.

Caragasinin C: a new oligostilbene from the roots of Caragana sinica

Abstract A new oligostilbene, caragasinin C (1), and seven known compounds, betulinic acid (2), 4-hydroxybenzaldehyde (3), (‒)-medicarpin (4), wistin (5), (2E,4S)-4-hydroxy-2-nonenoic acid (6), pallidol (7), and (+)-α-viniferin (8), were isolated from the roots of Caragana sinica. The structure of caragasinin C was established on the basis of spectroscopic techniques, including HRESIMS, 1D and 2D-NMR.

Inhibition of Antigen-Induced Degranulation by Flavonoids Isolated from the Leaves of Quercus Acuta in RBL-2H3 Cells

The genus Quercus has been taxonomically included in the Fagaceae with over 500 species from all corners of the globe. Q. acuta is distributed only in Korea, Japan, China s Guizhou Province, and Guangdong Province and grows in warmtemperate evergreen broadleaf forests [1]. The stems of Q. acuta have been used as a medicinal source for the treatment of various disorders such as diarrhea, dermatitis, arteriosclerosis, and haemorrhagia in Korea [2]. Previous phytochemical studies on this plant have reported the isolation of various types of phenolic compounds such as tannins, proanthocyanidins, lignans, and flavonoids, which possess various pharmacological effects such as anti-inflammatory, antibacterial, and antioxidant activities [2, 3]. In our research program on plant-derived inhibitors of the release of -hexosaminidase, the ethanolic extract of the leaves of Q. acuta was found to suppress antigen-mediated degranulation of rat basophilic leukemia (RBL-2H3) cells. A polyacylated flavonol glucoside (1), three flavone derivatives (2, 5, and 9), and seven flavonol derivatives (3, 4, 6, 7, 8, 10, and 11) were isolated from the ethanol extract using bioassay-guided fractionation. Compounds 1–11 were identified as kaempferol 3-(3 ,4 -diacetyl-2 ,6 -di-E-p-coumaryl)-glucoside (1), luteolin (2), guiajaverin (3), avicularoside (4), cynaroside (5), quercitrin (6), hyperoside (7), isoquercitrin (8), apigenin (9), quercetin (10), and kaempferol (11), by spectroscopic analysis (MS, 1D, and 2D NMR) and comparisons with literature data. This is the first time that the isolation of compounds 1–11 has been reported from Q. acuta species. We tested the antiallergic activity monitored by the enzyme -hexosaminidase: the compounds 1, 2, 9, 10, and 11 showed a good antiallergic potential (Table 1).