Ameliorating Effect of Crassocephalum rabens (Asteraceae) Extract on Skin Aging: A Randomized, Parallel, Double-Blind, and Placebo-Controlled Study.

Crassocephalum rabens (Asteraceae) is a common herb used in Taiwanese folk medicine to treat inflammation-related syndromes. Pharmacological studies have revealed that galactolipids exhibit anti-oxidative, anti-inflammatory, and anti-hyaluronidase activities and improve skin wrinkles, moisture, and elasticity in healthy subjects. However, the anti-aging effects of C. rabens and its primary active compound, 1,2-di-O-linolenoyl-3-O-ß-galactopyranosyl-sn-glycerol (dLGG), remain elusive. Here, we investigated whether C. rabens can improve skin conditions in healthy individuals using a double-blind approach. Forty enrolled volunteers were randomly and equally assigned to the control or treatment group and were required to take either a placebo or a C. rabens extract capsule daily for one month. Skin parameters were measured before and after the study. The results showed significant differences in skin elasticity, wrinkles, collagen content, brightness, and hydration between the baseline and week 4 in the treatment group. Particularly, compared with those in the placebo group, skin wrinkles (p < 0.05), brightness (p < 0.001), collagen content (p < 0.01), and UV spots (p < 0.05) were notably improved after treatment with the C. rabens extract. Our study successfully demonstrated the application of C. rabens in preventing skin aging. Further investigations will be conducted to study the underlying anti-aging mechanism of dLGG.

Effect of floral sources on the antioxidant, antimicrobial, and anti-inflammatory activities of honeys in Taiwan.

We evaluated the antioxidant, antibacterial, and anti-inflammatory activities of honey made from different floral sources, including the medicinal herb Bidens pilosa, fruit trees, Dimocarpus longan, Litchi chinensis, and Citrus maxima, the Taiwanese endemic plant Aglaia formosana, and a multifloral forest. The total phenolic and flavonoid contents of the honey made from B. pilosa were significantly higher than those of the other honeys. The honey from B. pilosa also had significantly greater scavenging activities for 1,1-diphenyl-2-picrylhydrazyl (DPPH·) and hydroxyl radical, and substantially more reducing power. In addition, the honey from B. pilosa showed greater antibacterial activity against gram-positive and gram-negative bacteria. However, B. pilosa honey showed little inhibitory activity against IL-8 secretion, whereas the other honeys did. These findings suggest that the levels of antioxidant and antibacterial activities are attributable to the total phenolic and flavonoid contents of honeys, while the IL-8 inhibition is attributable to components other than phenols.

Distinguishing between R- and S-antcin C and their cytotoxicity.

Antcin C is a bioactive compound isolated from Antrodia cinnamomea, a rare and expensive medicinal fungus endemic to Taiwan. Up to date, the absolute structure of antcin C has not been solved. In this study, the phenylglycine methyl ester (PGME) derivatives of antcin C were prepared. From NMR analysis the absolute configuration of(S)-antcin C (1) and (R)-antcin C (2) were determined. By MTT assay, (S)-antcin C presented cytotoxicity against Hep G2 and MCF-7 cells, with IC50 values of 14.5 and 12.8 microg/mL, respectively. However, (R)-antcin C did not show significant cytotoxicity. Our results showed that the configuration at C25 for antcin C is very important for its cytotoxicity. From a quality control point of view, it is necessary to identify and quantify the R- and S- enantiomers in the A. cinnamomea products.

Metabolite profiles for Antrodia cinnamomea fruiting bodies harvested at different culture ages and from different wood substrates.

Antrodia cinnamomea is a precious edible fungus endemic to Taiwan that has long been used as a folk remedy for health promotion and for treating various diseases. In this study, an index of 13 representative metabolites from the ethanol extract of A. cinnamomea fruiting body was established for use in quality evaluation. Most of the index compounds selected, particularly the ergostane-type triterpenoids and polyacetylenes, possess good anti-inflammation activity. A comparison of the metabolite profiles of different ethanol extracts from A. cinnamomea strains showed silmilar metabolites when the strains were grown on the original host wood (Cinnamomum kanehirai) and harvested after the same culture time period (9 months). Furthermore, the amounts of typical ergostane-type triterpenoids in A. cinnamomea increased with culture age. Culture substrates also influenced metabolite synthesis; with the same culture age, A. cinnamomea grown on the original host wood produced a richer array of metabolites than A. cinnamomea cultured on other wood species. We conclude that analysis of a fixed group of compounds including triterpenoids, benzolics, and polyacetylenes constitutes a suitable, reliable system to evaluate the quality of ethanol extract from A. cinnamomea fruiting bodies. The evaluation system established in this study may provide a platform for analysis of the products of A. cinnamomea.

Antidyslipidemic activity of hot-water extracts from leaves of Cinnamomum osmophloeum Kaneh.

The antidyslipidemic activity of hot-water extracts of Cinnamomum osmophloeum leaves (COE) were evaluated on hamsters fed a high-fat diet. Oral administration of COE to hyperlipidemic hamsters reduced the total cholesterol (TC), triglyceride (TG) and low-density lipoprotein (LDL-C) levels. Compared with hyperlipidemic hamsters, the plasma TC and TG levels of hamsters fed with COE at a dosage of 100 mg/kg body weight for 5 and 10 weeks were significantly reduced to 12.63% and 34.25%, and 33.88% and 36.88%, respectively. Plasma LDL-C was also reduced to 27.77% after 10 weeks feeding with the same regimen. Standard diagnostic tests indicated that the extracts did not cause damage to hamster liver or kidneys. Based on these results, it is concluded that COE possesses antidyslipidemic activity. The composition of COE was characterized. Two main compounds, kaempferol 3-O-ß-D-apiofuranosyl-(1 → 2)-α-L-arabinofuranosyl-7-O-α-L-rhamnopyranoside (1) and kaempferitrin (2) were identified in the hot-water extracts. Their contents were 7.56% and 9.95%, respectively.

Inhibitory effect of human breast cancer cell proliferation via p21-mediated G1 cell cycle arrest by araliadiol isolated from Aralia cordata Thunb.

A new polyacetylenic compound, araliadiol, was isolated from the leaves of Aralia cordata Thunb. (Araliaceae). The structure of araliadiol was determined to be 3( S),8( R)-pentadeca-1,9( Z)-diene-4,6-diyne-3,8-diol by MS, NMR, IR, and UV spectroscopic analysis as well as Mosher ester reaction. Araliadiol displayed a significant inhibitory effect on the growth of a human breast adenocarcinoma cell line (MCF-7), with an IC (50) value for cytotoxicity of 6.41 µg/mL. Cell cycle analysis revealed that the proportion of cells in the G (1) phase of the cell cycle increased in a dose-dependent manner (from 54.7 % to 72.0 %) after 48 h exposure to araliadiol at dosages ranging from 0 to 80 µM. The results suggest that araliadiol inhibits cell cycle progression of MCF-7 at the G (1)-S transition. After treatment with araliadiol, phosphorylation of retinoblastoma protein (Rb) in MCF-7 cells was inhibited, accompanied by a decrease in the levels of cyclin D (3) and cyclin-dependent kinase 4 (cdk4) and an increase in the expression of p21 (WAF-1/Cip1). However, the expression of phosphorylated p53 (Ser15) and Chk2 was not altered in MCF-7 cells. These findings indicate that araliadiol exhibits its growth-inhibitory effects on MCF-7 cells through downregulation of cdk4 and cyclin D (3), and upregulation of p21 (WAF-1/Cip1) by a p53-independent mechanism.

Involvement of caspases and apoptosis-inducing factor in bufotalin-induced apoptosis of Hep 3B cells.

Bufotalin is one of the bufadienolides isolated from Formosan Ch'an Su, which is made of the skin and parotid glands of toads. Ingestion of toad venom results in severe morbidity and high mortality. Although Ch'an Su is clinically toxic, it has been used as an important traditional Chinese medicine for heart failure and pains. In this study, bufotalin-induced apoptosis in human hepatocellular carcinoma Hep 3B cells was investigated. The results indicate that externalization of phosphatidylserine, accumulation of sub-G(1) cells, fragmentation of DNA, and formation of apoptotic bodies were observed in bufotalin-treated Hep 3B cells. The signaling pathway might be via the activation of caspase-8, increase in mitochondrial tBid, disruption of mitochondrial membrane potential, and translocation of apoptosis-inducing factor (AIF). Active caspase-8 might activate caspase-9 and caspase-3 leading to the cleavage of nuclear PARP. Presence of AIF and cleaved PARP in the nuclei might lead to DNA fragmentation. Caspase-8 inhibitor (Z-IETD) or wide-ranging caspase inhibitor (Z-VAD) significantly suppressed the bufotalin-induced apoptosis, while the anti-Fas neutralization antibody had no effect. These data suggest that bufotalin-induced apoptosis in Hep 3B cells might involve caspases and AIF.

Anti-inflammation activity of fruit essential oil from Cinnamomum insularimontanum Hayata.

In this study, the fruit essential oil of Cinnamomum insularimontanum was prepared by using water distillation. Followed by GC-MS analysis, the composition of fruit essential oil was characterized. The main constituents of essential oil were alpha-pinene (9.45%), camphene (1.70%), beta-pinene (4.30%), limonene (1.76%), citronellal (24.64%), citronellol (16.78%), and citral (35.89%). According to the results obtained from nitric oxide (NO) inhibitory activity assay, crude essential oil and its dominant compound (citral) presented the significant NO production inhibitory activity, IC(50) of crude essential oil and citral were 18.68 and 13.18microg/mL, respectively. Moreover, based on the results obtained from the protein expression assay, the expression of IKK, iNOS, and nuclear NF-kappaB was decreased and IkappaBalpha was increased in dose-dependent manners, it proved that the anti-inflammatory mechanism of citral was blocked via the NF-kappaB pathway, but it could not efficiently suppress the activity on COX-2. In addition, citral exhibited a potent anti-inflammatory activity in the assay of croton oil-induced mice ear edema, when the dosage was 0.1 and 0.3mg per ear, the inflammation would reduce to 22% and 83%, respectively. The results presented that the fruit essential oil of C. insularimontanum and/or citral may have a great potential to develop the anti-inflammatory medicine in the future.