Three new isocoumarin analogues from an endolichenic fungus Aspergillus flavus CPCC 400810.

Five isocoumarin derivatives including three new compounds, aspermarolides A-C (1-3), and two known analogues, 8-methoxyldiaporthin (4) and diaporthin (5) were obtained from the culture extract of Aspergillus flavus CPCC 400810. The structures of these compounds were elucidated by spectroscopic methods. The double bond geometry of 1 and 2 were assigned by the coupling constants. The absolute configuration of 3 was determined by electronic circular dichroism experiment. All compounds showed no cytotoxic activities against the two human cancer cells HepG2 and Hela.

One new benzophenone and one new 1,3-diphenylpropane from the fibrous roots of Anemarrhena asphodeloides Bge. and their cytotoxicity.

One new benzophenone (1) and one new 1,3-diphenylpropane (2) were obtained from the fibrous roots of Anemarrhena asphodeloides Bge. Their structures were determined by comprehensive 1D, 2D NMR and HRESIMS data. By comparing the calculated ECD curves and OR with the experimental data the absolute configurations were determined. The antitumor activity of all isolates was evaluated against two human hepatoma carcinoma cells (HepG2 and Hep3B) in vitro. The results demonstrated that compound 1 and 2 showed potent cytotoxicity against HepG2 and Hep3B cells.

Anti-inflammatory bibenzyls from the stems of Dendrobium huoshanense via bioassay guided isolation.

The stems of Dendrobium huoshanense have long been used to prevent various diseases, including inflammatory diseases. This study was aimed to explain the anti-inflammatory effect of D. huoshanense stems in LPS-induced RAW 264.7 macrophages and to discover potential anti-inflammatory compounds. Results exhibited that D. huoshanense stems ethanol extract could significantly inhibit LPS-induced production of NO, TNF-α and IL-1ß. Based on bioassay guided strategy, four bibenzyls (1-4) were isolated from D. huoshanense stems for the first time. Anti-inflammatory assay showed 1-4 could remarkably inhibit the production of NO in LPS-induced macrophages. Moreover, quantitative RT-PCR analysis displayed that the mRNA levels of iNOs, TNF-α and IL-1ß could also be significantly reduced by 1-4. These results suggested that D. huoshanense stems ethanol extract and bibenzyls 1-4 might be well developed as therapeutic agent to prevent inflammatory diseases.

Structural features and anti-gastric cancer activity of polysaccharides from stem, root, leaf and flower of cultivated Dendrobium huoshanense.

The structure features and anti-gastric cancer activities in vitro of stem, root, leaf and flower polysaccharides from cultivated Dendrobium huoshanense were investigated systematically. Stem polysaccharide (cDHPS) was composed of →4)-ß-D-Glcp-(1→, →4)-ß-D-Manp-(1→, →4)-3-O-acetyl-ß-D-Manp-(1→ with the molecular weight of 2.59 × 105 Da; root polysaccharide (cDHPR) was composed of →3,5)-α-L-Araf-(1→, →4)-ß-D-Glcp-(1→, →4)-ß-D-Manp-(1→, →4,6)-ß-D-Manp-(1→, →6)-α-D-Galp-(1→ and terminal ß-L-Araf with the molecular weight of 1.41 × 104 Da; leaf polysaccharide (cDHPL) was composed of →4)-ß-D-Glcp-(1→, →4)-ß-D-Manp-(1→, →4)-3-O-acetyl-ß-D-Manp-(1→, →3,6)-ß-D-Manp-(1→ and terminal α-D-Galp with the molecular weight of 2.09 × 105 Da; and flower polysaccharide (cDHPF) was composed of →4)-ß-D-Glcp-(1→, →4)-ß-D-Manp-(1→, →3,6)-ß-D-Manp-(1→ and terminal α-D-Galp with the molecular weight of 4.78 × 105 Da. Among these four polysaccharides, cDHPS showed the best anti-gastric cancer activity evidenced by the inhibited growth and c-myc expression as well as the enhanced apoptosis and p53 expression of murine forestomach carcinoma (MFC) cells, suggesting their difference in anti-gastric cancer activity should be contributed to their difference in structure features.

Benzophenones from Anemarrhena asphodeloides Bge. Exhibit Anticancer Activity in HepG2 Cells via the NF-κB Signaling Pathway.

A chemical investigation of the fibrous roots of Anemarrhena asphodeloides Bge. led to the isolation of four benzophenones, including one new compound (1) and three known ones (2-4). Comprehensive 1D, 2D NMR and HRESIMS data established the structures of the isolated compounds. The absolute configurations were determined by comparison of the calculated optical rotation (OR) with experimental data. All the isolates were evaluated for their cytotoxicities on hepatocellular carcinoma cell lines (HepG2 and Hep3B). Compound 1 showed strong cytotoxicity against HepG2 and Hep3B cells, with IC50 values at 153.1 and 180.6 nM. Through MTT assay, flow cytometry and Western blot analysis, compound 1 demonstrated the ability to stimulate apoptosis via the NF-κB signaling pathway in HepG2 cells. These benzophenones are potential lead compounds for the development of better treatments for hepatocellular carcinoma.

Dendrobium huoshanense polysaccharide regulates hepatic glucose homeostasis and pancreatic ß-cell function in type 2 diabetic mice.

In the present study, the hypoglycemic mechanism of a homogeneous Dendrobium huoshanense polysaccharide (GXG) was investigated using type 2 diabetic (T2D) mouse model. With a 5-week oral administration of GXG, the levels of fasting blood glucose, glycosylated serum protein and serum insulin in T2D mice were decreased, and the glucose tolerance and the insulin sensitivity were improved. The histological analysis, the periodic acid-schiff staining and the immunofluorescence staining of insulin, glucagon and apoptosis showed that the hypoglycemic effect of GXG was related to the improvement of pancreatic ß-cell quantity and function and the regulation of hepatic glucose metabolism. Western blot analysis indicated that the up-regulated IRS1-PI3K-Akt phosphorylation followed by the down-regulated FoxO1/GSK 3ß phosphorylation contributed to the enhanced glycogen synthesis and the decreased gluconeogenesis by GXG, suggesting that the response of insulin-mediated IRS1-PI3K-Akt-FoxO1/GSK 3ß signaling to GXG might be the required mechanism for GXG-ameliorated development of type 2 diabetes.

Mimengosides J and K: two new neuroprotective triterpenoids from the fruits of Buddleja lindleyana.

Two new 11-methoxyl substituted triterpenoids, named as mimengosides J (1) and K (2), along with seven known compounds, were isolated from the fruits of Buddleja lindleyana. Their structures were elucidated on the basis of spectroscopic analysis. In addition, the new ones were evaluated for protective effects against damage of SH-SY5Y cells induced by 1-methyl-4-phenylpyridinium ion (MPP+) and the results indicated that those may be one of the candidate compositions of Buddleja lindleyana for the treatment of neurodegenerative disease.

The effect of ethyl acetate extract from persimmon leaves on Alzheimer's disease and its underlying mechanism.

BACKGROUND: Alzheimer's disease (AD) is one of the most prevalent neurodegenerative disorders characterized by neuronal loss in the brain and cognitive impairment. AD is now considered to be the third major cause of death in developed countries, after cardiovascular disease and cancer. Persimmon leaves are used as a popular folk medicine to treat hypertension, angina and internal haemorrhage in Cyangbhina, and it has been reported that ethyl acetate extract of persimmon leaves (EAPL) displays a potential therapeutic effect on neurodegenerative diseases. HYPOTHESIS/PURPOSE: This study was designed to investigate the effects of EAPL on AD, to clarify the possible mechanism by which EAPL exerts its beneficial effects and prevents AD, and to determine the major constituents involved. STUDY DESIGN: AD model was established by bilateral injection of Aß1-42 into the hippocampus of rats. The cognitive performance was determined by the Morris water maze and step-down tests. Superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), malondialdehyde (MDA), apoptosis, total and phosphorylated c-Jun NH2-terminal kinase (JNK/p-JNK), caspase-3, Bax and Bcl-2 were determined. In addition, a sensitive and reliable LC-QTOF-MS method was applied to identify the major compounds present in EAPL. RESULTS: EAPL at doses of 200mg/kg, 400mg/kg could markedly reduce the latency, significantly increase the time in the first quadrant and number of the target crossing times in Morris water maze test, markedly increase the latency and reduce the number of errors in the step-down test, significantly inhibit the reductions in SOD and GSH-Px activities, and increase the level of MDA. In addition, EAPL treatment attenuated neuronal apoptosis in the hippocampus, reduced the expression of p-JNK, caspase-3, and the relative ratio of Bax/Bcl-2. Meanwhile, 32 constituents were identified by LC-QTOF-MS/MS assays. CONCLUSION: The results indicate that EAPL has a potent protective effect on cognitive deficits induced by Aß in rats and this effect appears to be associated with the regulation of the antioxidative defense system and the mechanism of mitochondrial-mediated apoptosis. Furthermore, analysis of the LC-MS data suggests that flavonoids and triterpenoids may be responsible for the potential biological effects of EAPL.

A Novel Light-Emitting Wire Enhances the Marking and Visualization of Pathologic Mammary Ducts During Selective Microdochectomy.

BACKGROUND: Methylene blue injection of lesions often is inaccurate, and ductoscopic wire marking does not facilitate easy identification of lesions during microdochectomy in patients with pathologic nipple discharge. The authors designed a light-emitting wire that can be inserted into pathologic mammary ducts to facilitate intraoperative duct identification and evaluated the efficacy of this device in patients undergoing selective microdochectomy. METHODS: In this study, 69 patients being evaluated for pathologic discharge were randomized to undergo selective microdochectomy with either methylene blue pathologic duct marking or light-emitting wire pathologic duct marking. The patient clinical characteristics and surgical outcomes were compared and evaluated. RESULTS: Of the 69 study patients, 36 underwent selective microdochectomy guided by methylene blue injection, and 33 underwent light-emitting wire marking. No differences existed between the clinical and histologic characteristics or the diagnostic accuracies of the groups. In 11 (30.56%) of the 36 patients who underwent methylene blue marking, the ducts ruptured after the methylene blue was injected, and normal tissue around the duct was stained. Light-emitting wire marking was associated with a shorter surgical time and smaller surgical specimens. CONCLUSIONS: The use of light-emitting wire marking enabled selective microdochectomy of pathologic ducts under visual guidance. Resection volume was reduced, and blinded extended resection was avoided.

Two new compounds from the fruits of Buddleja lindleyana with neuroprotective effect.

Two new triterpenoid glycosides, mimengosides H (1) and I (2), were isolated from the fruits of Buddleja lindleyana Fort. Their structures were determined by extensive spectroscopic methods. Neuroprotective effects of these isolates against 1-methyl-4-phenylpyridinium ion-induced neurotoxicity in PC12 cells were evaluated. Pretreatment with compound 1 had potential protective effect in a concentration range from 0.1 to 1 µmol l⁻¹.

[Study on the chemical composition of triterpenoid from the fruit of Buddleja lindleyana and their neuroprotective activitiy].

OBJECTIVE: To study the chemical composition of triterpenoid from the fruit of Buddleja lindleyana. METHODS: The chemical components were isolated by chromatography. The structures were identified by spectral data. The neuroprotective activity of these compounds were evaluated by using MPP+ induced injury in PC12 cells. RESULTS: 3 compounds were separated and identified as oleanane, alpha-L-msnnopyranoside derive (1), 13, 28-epoxy-3beta,23-dihydroxy-11-oleanene (2), 3, 23, 28-trihydroxyolean-11,13 (18)-diene (3). Compounds 1-3 showed obviously neuroprotective activity. CONCLUSION: The data of compound (1) is reported for the first time. The neuroprotective activities of compounds 1, 2, 3 are reported for the first time.