Anti-Inflammatory Effect of Immature Sword Bean Pod (Canavalia gladiata) in Lipopolysaccharide-Induced RAW264.7 Cells.

Sword bean has been known as a traditional medicinal plant to treat cancer, sinus infection, and suppurative disease. It also possesses hypertension-relieving, antioxidation, and antibacterial effects. However, studies on the efficacy of sword bean are limited to mature beans. Few studies have focused on immature sword bean pod (ISBP). Therefore, this study aimed to investigate the anti-inflammatory effect of ISBP in RAW264.7 cells stimulated with lipopolysaccharide (LPS). After LPS-induced RAW264.7 cells were treated with ISBP at concentrations (0.5, 1, 2, and 5 mg/mL), levels of nitrite oxide (NO) and prostaglandin E2 (PGE2) production, protein, and mRNA levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), inflammatory cytokine secretion level, and nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) activity were determined. Under inflammatory conditions induced by LPS, ISBP reduced levels of inflammatory mediators NO and PGE2 by 60% and 23%, respectively. It also decreased protein and mRNA expression levels of iNOS and COX-2 known to synthesize inflammatory mediators. Inflammatory cytokines, interleukin (IL)-6, and IL-1ß, levels were decreased, while interferon gamma level was increased by ISBP based on enzyme-linked immunosorbent assay (ELISA) and real time-polymerase chain reaction results. Finally, ISBP showed the ability to inhibit NF-κB activity. In conclusion, ISBP can alleviate inflammation by controlling inflammation-related substances, and may have efficacy as a healthful functional food and natural anti-inflammatory drug.

Depsidomycins B and C: New Cyclic Peptides from a Ginseng Farm Soil-Derived Actinomycete.

LC/MS-based chemical profiling of a ginseng farm soil-derived actinomycete strain, Streptomyces sp. BYK1371, enabled the discovery of two new cyclic heptapeptides, depsidomycins B and C (1 and 2), each containing two piperazic acid units and a formyl group at their N-terminus. The structures of 1 and 2 were elucidated by a combination of spectroscopic and chemical analyses. These new compounds were determined to possess d-leucine, d-threonine, d-valine, and S-piperazic acid based on the advanced Marfey's method and a GITC (2,3,4,6-tetra-O-acetyl-ß-d-glucopyranosyl isothiocyanate) derivatization of their hydrolysates, followed by LC/MS analysis. Depsidomycins B and C displayed significant antimetastatic activities against metastatic breast cancer cells (MDA-MB-231).

New flavonolignan glycosides from the aerial parts of Zizania latifolia.

Two new flavonolignan glycosides, tricin-4'-O-(threo-ß-guaiacylglyceryl) ether 7''-O-ß-D-glucopyranose (4) and tricin-4'-O-(erythro-ß-guaiacylglyceryl) ether 7''-O-ß-D-glucopyranose (5) were isolated from the roots of Zizania latifolia, together with tricin-7-O-ß-D-glucopyranose (1), tricin-4'-O-(threo-ß-guaiacylglyceryl) ether 7-O-ß-D-glucopyranose (2), and tricin-4'-O-(erythro-ß-guaiacylglyceryl) ether 7-O-ß-D-glucopyranose (3). Their structures were identified on the basis of spectroscopic techniques, including HR-ESI/MS, 1D-NMR (1H, 13C, DEPT), 2D-NMR (gCOSY, gHSQC, gHMBC), and IR spectroscopy.

Microbial biosynthesis of medicinally important plant secondary metabolites.

Secondary metabolites derived from plants are a valuable source of pharmaceuticals, nutraceuticals, and cosmetics. To harness the potential of these natural products, reliable methods must be developed for their rapid and sustainable resupply. Microbial production of plant secondary metabolites through the heterologous expression of plant biosynthetic genes represents one such solution. This highlight focuses on recent advances in the microbial biosynthesis of plant secondary metabolites including terpenoids, flavonoids, and alkaloids as well as providing a brief insight into the current limitations and future prospects.

Screening and isolation of a natural dopamine D1 receptor antagonist using cell-based assays.

To develop a cell-based assay to screen for human dopamine D(1) receptor agonists or antagonists from medicinal plant extracts, a stable Chinese hamster ovary (CHO) cell line (CHO-D1R) expressing the human dopamine D(1) receptor was established using an expression vector containing a scaffold attachment region (SAR) element. CHO-D1R cells showed specific binding to [(3)H]-SCH23390 with high affinity (K(d)=1.47+/-0.17 nM) and dose-dependent responses for the dopamine-mediated stimulation of cAMP concentrations (EC(50)=20.6+/-1.44 nM). The screening of medicinal plant extracts using cell-based cAMP assays revealed that an extract of Gleditsia sinensis Lam., which is known to be rich in saponin, had strong antagonist activity for the D(1) receptor. From the activity-guided fractionation and chemical structural analysis of the G. sinensis extract, a compound called gleditsioside F was isolated and was identified to have antagonist activity for the D(1) receptor. Gleditsioside F showed very effective D(1) antagonist activity by inhibiting ligand binding to the D(1) receptor as well as by inhibiting dopamine-mediated increases in cAMP concentration.

A cytotoxic and apoptosis-inducing sesquiterpenoid isolated from the aerial parts of Artemisia princeps PAMPANINI (Sajabalssuk).

Repeated silica gel and octadecyl silica gel (ODS) column chromatography of the aerial parts of Artemisia princeps PAMPANINI (Sajabalssuk) led to the isolation of a new sesquiterpenoid, 3-((S)-2-methylbutyryloxy)-costu-1(10),4(5)-dien-12,6 alpha-olide (2), along with two previously reported sesquiterpenoids: 8 alpha-angeloyloxy-3beta,4 beta-epoxy-6 beta H,7 alpha H,8 beta H-guaia-1(10),11(13)-dien-12,6 alpha-olide (1, carlaolide B) and 3beta,4 beta-epoxy-8 alpha-isobutyryloxy-6 beta H,7 alpha H,8 beta H-guaia-1(10),11(13)-dien-12,6 alpha-olide (3, carlaolide A). The structure of compound 2 was elucidated by spectroscopic data analysis, including one dimensional (1D) and two dimensional (2D) nuclear magnetic resonance (NMR) experiments. Of the isolates, compound 2 exhibited potent cytotoxicity against human cervix adenocarcinoma cells and induced apoptosis.

Heterocyclic compounds from Chrysanthemum coronarium L. and their inhibitory activity on hACAT-1, hACAT-2, and LDL-oxidation.

The aerial parts of Chrysanthemum coronarium L. were extracted with MeOH, and the concentrated extract was partitioned using EtOAc, n-BuOH, and H(2)O, successively. Repeated column chromatography of the EtOAc and n-BuOH fractions gave a new heterocycle, 5,5'-dibuthoxy-2,2'-bifuran (1) along with five known compounds: methyl trans-ferulate (2), prunasin (3), sambunigrin (4), pterolactam (5), and adenosine (6), which were identified by several spectroscopic methods including NMR and MS. This paper is the first report on the isolation of these compounds from C. coronarium L. The IC(50) values of compound 1 for human Acyl-CoA:cholesterol acyltransferase (hACAT)-1 and hACAT-2 were 0.16 mM and 0.19 mM, respectively. Compound 2 inhibited low-density lipoprotein (LDL) oxidation with an IC(50) value of 7.7 microM.

Identification of campesterol from Chrysanthemum coronarium L. and its antiangiogenic activities.

Campesterol, a plant sterol in nature, is known to have cholesterol lowering and anticarcinogenic effects. Since angiogenesis is essential for cancer, it was surmised that an antiangiogenic effect may be involved in the anticancer action of this compound. This study investigated the effect of campesterol on basic fibroblast growth factor (bFGF)-induced angiogenesis in vitro in human umbilical vein endothelial cells (HUVECs) and an in vivo chorioallantoic membrane (CAM) model. Campesterol isolated from an ethylacetate fraction of Chrysanthemum coronarium L. showed a weak cytotoxicity in non-proliferating HUVECs. Within the non-cytotoxic concentration range, campesterol significantly inhibited the bFGF-induced proliferation and tube formation of HUVECs in a concentration-dependent manner, while it did not affect the motility of HUVECs. Furthermore, campesterol effectively disrupted the bFGF-induced neovascularization in chick chorioallantoic membrane (CAM) in vivo. Taken together, these results support a potential antiangiogenic action of campesterol via an inhibition of endothelial cell proliferation and capillary differentiation.

Phenolic compounds from the roots of Lindera fruticosa.

The phenolic compounds isolated from the roots of Lindera fruticosa included four new compounds, 2-methoxy-3,4-methylenedioxybenzophenone (1), (S)-2-methoxy-3,4-methylenedioxybenzhydryl alcohol (2), 3-hydroxy-5-methoxybiphenyl (3), and 1-methoxy-2,5,7-trihydroxyxanthone (4). Three previously identified phenolics were also identified, namely, 3,5-dimethoxybiphenyl (5), benzyl 2-hydroxy-6-methoxybenzoate (6), and 1,7-dihydroxyxanthone (7). These compounds were evaluated for their inhibitory effects on human acyl-CoA:cholesterol acyltransferase activity and on the in vitro oxidation of low-density lipoprotein.

In vitro GABA-transaminase inhibitory compounds from the root of Angelica dahurica.

The 80% aqueous MeOH extracts from the root of Angelica dahurica, found to inhibit the activities of GABA degradative enzymes GABA transaminase (GABA-T) and succinic semialdehyde dehydrogenase (SSADH), were fractionated using EtOAc, n-BuOH and H2O. Repeated column chromatography for the EtOAc and n-BuOH fractions led to the isolation of two new coumarins, oxypeucedanin hydrate-3''-butyl ether and isopraeroside IV along with six known coumarins, isoimperatorin, imperatorin, phellopterin, oxypeucedanin hydrate, nodakenin and 3'-hydroxymarmesinin, and two polyacetylenes, falcarindiol and octadeca-1,9-dien-4,6-diyn-3,8,18-triol. Of the isolated pure compounds, imperatorin and falcarindiol inactivated the GABA-T activities in both time- and concentration-dependent manners. The kinetic studies showed that imperatorin and falcarindiol reacted with the GABA-T with a second-order rate constant of 2.3 +/- 0.2 mm(-1) min(-1) and 1.5 +/- 0.1 mm(-1) min(-1), respectively. It is postulated that imperatorin and falcarindiol are able to elevate the neurotransmitter GABA levels in the central nervous system by an inhibitory action on the GABA degradative enzyme GABA-T.

5-Hydroxy-7-(4'-hydroxy-3'-methoxyphenyl)-1-phenyl-3-heptanone: a pancreatic lipase inhibitor isolated from Alpinia officinarum.

A pancreatic lipase inhibitor, 5-hydroxy-7-(4'-hydroxy-3'-methoxyphenyl)-1-phenyl-3-heptanone (HPH), from the rhizome of Alpinia officinarum (AO) was isolated and its antihyperlipidemic activity was measured. HPH inhibited a pancreatic lipase with an IC(50) value of 1.5 mg/ml (triolein as a substrate). HPH significantly lowered the serum TG level in corn oil feeding-induced triglyceridemic mice, and reduced serum triglyceride (TG) and cholesterol in Triton WR-1339-induced hyperlipidemic mice. However, HPH did not show hypolipidemic activity in high cholesterol diet-induced hyperlipidemic mice. Based on these findings, we propose that PL inhibitors may be effective as hypolipidemic agents.