Protective effects of a traditional herbal extract from Stellaria dichotoma var. lanceolata against Mycobacterium abscessus infections.

Stellaria dichotoma var. lanceolata (SdLv), a member of the Caryophyllaceae, is a traditional herbal medicine that has been used to treat fever, night sweats, and malaria in East Asia. Inflammation plays an essential role in both host defense and pathogenesis during infection by diverse intracellular pathogens. Herein, we showed that an herbal extract from SdLv effectively attenuated inflammatory responses from infection of Mycobacterium abscessus (Mab), but not Toxoplasma gondii (T. gondii). In primary murine macrophages, Mab infection resulted in the rapid activation of nuclear factor (NF)-κB and mitogen-activated protein kinase (MAPK), as well as in the generation of proinflammatory cytokines, such as tumor necrosis factor α and interleukin-6, which were all significantly inhibited by pretreatment with SdLv. However, herbal extracts from Bupleurum chinense DC. (Buch) or Bupleurum falcatum L. (Bufa) did not affect M. abs-induced activation of proinflammatory responses. Importantly, we demonstrated that generation of intracellular reactive oxygen species, which are important signaling intermediaries in the activation of NF-κB and the MAPK signaling pathway, was rapidly increased in Mab-infected macrophages, and this was effectively suppressed by pretreatment with SdLv, but not Buch and Bufa. We further found that the treatment of Buch and Bufa, but not SdLv, led to the activation of NF-κB and the MAPK signaling pathway and the generation of intracellular reactive oxygen species. Moreover, oral administration of SdLv significantly reduced lethality in Mab-infected mice. Collectively, these results suggest the possible use of SdLv as an effective treatment for Mab infection.

Flavonoids from Stellaria nemorum and Stellaria holostea.

Stellaria nemorum L. and S. holostea L. (Caryophyllaceae) were investigated for their flavonoids. The new flavonoid 6-C-[(α-arabinopyranosyl)-( 1-->2)-O-ß- xylopyranosyl]apigenin (1) and the four known C-glycosides, 6-C-[(α-arabinopyranosyl)-(1-->2)-O-ß-glucopyranosyl]apigenin (2), apigenin 6-C-ß- galactopyranoside-8-C-ß-glucopyranoside (3), apigenin 6-C-ß-glucopyranoside-8-C-α-arabinopyranoside (4), and apigenin 6-C-ß-glucopyranoside-8-C-ß- xylopyranoside (5) were isolated from the aerial parts of S. nemorum for the first time. Furthemore, five known flavonoids, 3,5,7-trihydroxy-3',5'- dimethoxyflavone (9), diosmetin 6-C-ß-glucopyranoside (8), schaftoside (4), isoorientin (6) and orientin (7) were obtained from the aerial parts of S. holostea. Compounds 4, 8 and 9 are reported for the first time from this species. The structures of all isolated compounds were unambiguously elucidated by one- and two- dimensional NMR and mass spectral analysis, by acid hydrolysis, as well as by comparison with literature data. The crude extracts of the investigated species exhibited antimicrobial activity against Staphylococcus aureus, while none of the isolated compounds was found to be active.

Evaluation of hepatoprotective activity of water-soluble polysaccharide fraction of Stellaria media L.

Therapy of rats with CCl4 hepatitis with Stellaria media L. water-soluble polysaccharide fraction in a dose of 100 mg/kg reduces serum activities of transaminases (ALT and AST), alkaline phosphatase, bilirubin, and the thymol test values. In the liver, the density of inflammatory infiltration of the organ parenchyma, total count of necrotic hepatocytes, fatty and protein degeneration are reducing. Hence, water-soluble polysaccharide fraction, isolated from the terrestrial part of Stellaria media L., is characterized by hepatoprotective activity.

Quality assessment and anti-obesity activity of Stellaria media (Linn.) Vill.

BACKGROUND: Obesity is recognized as a social problem, associated with serious health risks and increased mortality. Numerous trials have been conducted to find and develop new anti-obesity drugs through herbal sources to minimize side effects associated with the present anti-obesity drugs. The present study was designed to evaluate the quality control parameters, quantitative phytochemical analysis (total phenolic, total flavonoids and total saponin content), and the anti-obesity effect of lyophilized juice (LJ) of Stellaria media (Linn.) Vill. by employing in vitro and in vivo models. METHODS: In vitro studies were performed to evaluate the inhibitory activity of LJ on pancreatic amylase and lipase. The in vivo pancreatic lipase activity was evaluated by measurement of plasma triacylglycerol levels after oral administration of lipid emulsion to swiss albino mice. Furthermore, the anti-obesity effect of LJ was assessed at two doses, 400 mg/kg and 900 mg/kg body weight in mice fed a high-fat-diet with or without LJ for 6 weeks. RESULTS: The LJ inhibited pancreatic amylase and lipase activity in vitro and elevated plasma triacylglycerol level in mice. LJ suppressed the increase in body weight, retroperitoneal adipose tissue, liver weights and serum parameters viz., total cholesterol, total triglyceride, LDL-cholesterol level at the dose of 900 mg/kg body weight of the mice fed with high fat diet. The total phenolic, flavonoid and saponin contents were found to be 0.26 mg/g, 1.4 mg/g and 1.19 µg/g respectively of LJ. CONCLUSION: The anti-obesity effects of LJ in high-fat-diet fed mice may be partly mediated through delaying the intestinal absorption of dietary fat and carbohydrate by inhibiting digestive enzymes.

Anti-hepatitis B virus activity of chickweed [Stellaria media (L.) Vill.] extracts in HepG2.2.15 cells.

Stellaria media (Linn.) Villars is a traditional Chinese medicine that has been used for over 200 years, mainly for the treatment of dermatitis and other skin diseases. It has also been used as an anti-viral agent. All the fresh chickweed juice samples used in this study were prepared using macroporous resin and ultrafiltration technology. The anti-hepatitis B virus (HBV) activity of S. media was evaluated in vitro using the human HBV-transfected liver cell line HepG2.2.15. The concentrations of hepatitis B surface antigen (HBsAg) and hepatitis B e antigen (HBeAg) in HepG2.2.15 cell culture medium were determined by enzyme-linked immunosorbent assay (ELISA) after S. media-n (SM-n) treatment for 6 or 9 days. HBV DNA was quantified using transcription-mediated amplification and real-time polymerase chain reaction. In HepG2.2.15 cells, 30 µg/mL SM-3 effectively suppressed the secretion of HBsAg and HBeAg with inhibition rates of 27.92% and 25.35% after 6 days of treatment, respectively. Consistent with the reduction in HBV antigens, SM-3 also reduced the level of HBV DNA in a dose-dependent manner. The characterization and quantitation of the chemical composition of SM-3 showed the presence of flavonoid C-glycosides, polysaccharides, and protein, which exhibited diverse antiviral activities. In conclusion, our results demonstrate that SM-3 possesses potential anti-HBV activity in vitro. This is the first report demonstrating the anti-HBV effects of S. media, which is currently under early development as a potential anti-HBV drug candidate.

Inhibition of cell growth by Stellera chamaejasme extract is associated with induction of autophagy and differentiation in chronic leukemia K562 cells.

Stellera chamaejasme has been used as a therapeutic plant for treatment of various inflammatory diseases and solid tumors. Our study was particularly interested in the differentiation inducing activity of the aerial parts of S.chamaejasme using human chronic leukemia cell line K562. The ethanol extract has been shown to be highly cytotoxic against K562 cells at >0.008% (v/v) doses. Cell cycle arrest at G(0)/G(1) phase, not detectable DNA fragmentation as well as positive staining with acridine orange and expression of beclin-1 protein in the treated cells led as to detect autophagic cell death during the plant extract treatment of K562 cells. Moreover, differentiation marker CD11b was also expressed in the treated cells.

Total phenolics level, antioxidant activities and cytotoxicity of young sprouts of some traditional Korean salad plants.

UNLABELLED: The aim of this investigation was to study the antioxidant and anticancer activities of young sprouts of some traditional Korean salad plants. Total phenolics, antioxidant and anticancer activities of the methanol extracts from young sprouts of 11 salad plants were determined. The highest amount of phenolics was found in methanol extracts of Euonymus alatus (235.7 mg kg(-1)), followed by Hypericum ascyron (197.1 mg kg(-1)), Zanthoxylum piperitum (194.1 mg kg(-1)) and Zanthoxylum schinifolium (142.5 mg kg(-1)). Methanol extracts of E. alatus, H. ascyron, and Z. piperitum at 63 mg kg(-1) exhibited the highest dose-depend DPPH radical scavenging activity by 91.2, 91.2 and 83.9%, respectively. According to the MTT results, the methanol extracts from Stellaria aquatica, Eleutherococcus sessilifolrus and Z. schinifolium showed the highest anticancer activities against Calu-6 (IC50<25.0 microg ml(-1)) and from S. aquatica-the highest anticancer activities against SNU-601 (153.3 microg ml(-1)), following by E. sessilifolrus (196.7 microg ml(-1)) and Amaranthus mangostanus (303.1 microg ml(-1)). Total phenolics were highly correlated with the DPPH, suggesting that they contribute to the antioxidant properties of the studied plants. IN CONCLUSION: young sprouts of Korean salad possess antioxidant and anticancer properties and could be used as a supplement to proper drugs.

Antioxidant activity of enzymatic extracts from Stellaria dichotoma.

The antioxidant properties of enzymatic extracts from Stellaria dichotoma were evaluated using seven carbohydrases (Promozyme, Celluclast, Maltogenase, Viscozyme, Termamyl, Dextrozyme, and AMG 300L) and five proteases (Protamex, Flavourzyme, Neutrase, pancreatic trypsin, and Alcalase) (all from Novo Co., Novozyme Nordisk, Bagsvaerd, Denmark) for 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, hydroxyl radical, and alkyl radical scavenging activity using an electron spin resonance spectrometer. The DPPH radical scavenging activities of pancreatic trypsin and Celluclast extracts from S. dichotoma were the highest among various protease and carbohydrate extracts, and the 50% inhibitory concentration (IC(50)) values were 10.45 and 13.80 microg/mL, respectively. The Flavourzyme and Promozyme extracts of S. dichotoma showed the highest hydroxyl radical scavenging activities among the tested protease and carbohydrase extracts, with IC(50) values of 1.51 and 1.23 microg/mL, respectively. The S. dichotoma enzymatic extracts also exhibited alkyl radical scavenging activity in a dose-dependent manner. In addition, the ability of the enzymatic extracts to inhibit the oxidative damage of DNA was assessed in vitro by measuring the conversion of supercoiled pBR322 plasmid DNA to the open circular form. It was found that the enzymatic extracts could significantly and dose-dependently protect against hydroxyl radical-induced DNA damage. These results indicate that enzymatic extracts of S. dichotoma possess potent antioxidant activity.

[Studies on chemical constituents from stellaria media. I].

OBJECTIVE: To study the chemical constituents of Stellaria media. METHOD: The compounds were isolated with various column chromatography and semi-preparative HPLC. The structures were determined by modem spectroscopic methods (IR, UV, 1H-NMR, 13C-NMR, HMBC, ESI-MS). RESULT: Five compounds were isolated and identified as apigenin 6-C-beta-D-galactopyranosyl-8-C-alpha-L-arabinopyranoside (1), apigenin 6-C-alpha-L-arabinopyranosyl-8-C-beta-D-galactopyranoside (2), apigenin 6-C-beta-D-galactopyranosyl-8-C-beta-L-arabinopyranoside (3), apigenin 6-C-beta-D-glucopyranosyl-8-C-beta-D-galactopyranoside (4), apigenin 6, 8-di-C-alpha-L-arabinopyranoside (5). CONCLUSION: Compounds 1-5 were obtained from Stellaria genus for the first time.

Dichotomins J and K, vasodilator cyclic peptides from Stellaria dichotoma.

Two new cyclic peptides, dichotomins J (1) and K (2), have been isolated from the roots of Stellaria dichotoma, and their structures were elucidated by chemical degradation and extensive 2D NMR methods. Dichotomins J (1) and K (2) showed a moderate vasorelaxant effect on rat aorta.

Structures of new beta-carboline-type alkaloids with antiallergic effects from Stellaria dichotoma(1,2).

The aqueous ethanolic extract from the roots of Stellaria dichotoma showed an antiallergic effect on ear passive cutaneous anaphylaxis (PCA) reaction in mice (in vivo) and inhibitory activity on the release of beta-hexosaminidase in RBL-2H3 cells (in vitro). From the aqueous ethanolic extract, new beta-carboline-type alkaloids, dichotomines A (1), B (2), C (3), and D (4) and dichotomides I (5) and II (6), were isolated. The structures of the new constituents (1-6) were determined on the basis of chemical and physicochemical evidence, including the application of the modified Mosher's method. The effects of the isolated constituents on the release of beta-hexosaminidase in RBL-2H3 cells were examined, and 3 was found to show inhibitory activity (IC(50) = 62 microM). Moreover, 3 also inhibited the releases of antigen-IgE-mediated TNF-alpha and IL-4 (19 and 15 microM, respectively) in RBL-2H3 cells, both of which participate in the late phase of type I allergic reactions.

[Studies on identification of yinchaihu by UV and IR].

OBJECTIVE: To study the identification of nine species of Yinchaihu derived from four genera of Caryophyllaceae, namely, Stellaria dichotoma var. lanceolata, St. dichotoma var. dichotoma, Arenaria juncea, A. capillaris var. glandulifera, Silene fortunei, Si. jenisseensis, Gypsophila pacifica, G. oldhamiana and G. licentiana. METHOD: UV and IR of alcohol extraction. RESULTS: The UV and IR spectra of these 9 plant roots have some difference. CONCLUSION: St. dichotoma var. lanceolata specified in the Chinese Pharmacopoeia can be distinguished from the other plants and all these 4 genera can be differentiated from one another by both UV and first derivative spectra. The genus Stellaria can be identified from the other 3 genera by IR.