Stereochemical insights into structurally diverse lignanamides from the herbs of Solanum lyratum Thunb.

A chemical investigation of Solanum lyratum Thunb. (Solanaceae) afforded six pairs of enantiomeric lignanamides consisting of twelve undescribed compounds, along with two undescribed racemic mixtures, and the separations of the enantiomers were accomplished by chiral-phase HPLC. The structures of these undescribed compounds were elucidated by the analysis of spectroscopic data, NMR and electronic circular dichroism calculations. All isolated compounds were assessed for neuroprotective activities in H2O2-induced human neuroblastoma SH-SY5Y cells, and acetylcholinesterase (AChE) inhibitory activities. Among tested isolates, some enantiomeric lignanamides exhibited conspicuous neuroprotective effects and AChE inhibitory effect.

Four Pairs of Neuroprotective Aryldihydronaphthalene-Type Lignanamide Enantiomers from the Herbs of Solanum lyratum.

Four pairs of aryldihydronaphthalene-type lignanamide enantiomers were isolated from Solanum lyratum (Solanaceae). The enantiomeric separation was accomplished by chiral-phase HPLC, and five undescribed compounds were elucidated. Analysis by various spectroscopy and ECD calculations, the structures of undescribed compounds were illuminated. The neuroprotective effects of all compounds were evaluated using H2 O2 -induced human neuroblastoma SH-SY5Y cells and AchE inhibition activity. Among them, compound 4 a exhibited remarkable neuroprotective effects at high concentrations of 25 and 50 µmol/L comparable to Trolox. Compound 1 a showed the highest AchE inhibition with the IC50 value of 3.06±2.40 µmol/L. Molecular docking of the three active compounds was performed and the linkage between the compounds and the active site of AchE was elucidated.

Neuroprotective and acetylcholinesterase inhibitory activities of alkaloids from Solanum lyratum Thunb.: An in vitro and in silico analyses.

The n-BuOH extract from the herb of Solanum lyratum Thunb. (Solanaceae) was purified by various chromatographic methods, which led to the isolation of seven undescribed alkaloids ((-)-(7'S)-N-feruloyltyramine A, (+)-(7'R)-N-feruloyltyramine A, (+)-(7'S)-N-solanamide A, (-)-(7'R)-N-solanamide A, 7'S-perillascens, solanpyrrole A, and (Z)-asmurratetra A) and 13 known alkaloids, including four pairs of enantiomers. Extensive spectroscopic data and electronic circular dichroism (ECD) calculations were applied to determine the structures of the undescribed compounds. In in vitro biological activity assays, (-)-(7'S)-N-feruloyltyramine A and (+)-(7'R)-N-feruloyltyramine A exhibited pronounced neuroprotective effects against SH-SY5Y cell damage with survival rates of 75.98% and 76.61%, respectively, at 50 µM. Additionally, (-)-(7'S)-N-feruloyltyramine A and N-cis-feruloyl-3'-methoxy-tyramine displayed acetylcholinesterase (AChE) inhibitory effects with IC50 values of 7.41 ± 1.76 µM and 9.21 ± 0.89 µM, respectively. Molecular docking simulations revealed that (-)-(7'S)-N-feruloyltyramine A had a binding site for AChE. These findings reveal the structural diversity of the bioactive compounds in S. lyratum and provides insights into the use of this information for the production of functional components in the pharmaceutical industry.

Solanoids F - I: Terpenoids from Solanum lyratum with neuroprotective effects against H2O2-induced SH-SY5Y cell injuries.

Four new terpenoids, solanoids F - I (1-4), together with eleven known compounds (5-15), were isolated from the whole herb of Solanum lyratum. The chemical structures were characterized by spectroscopic techniques, and electronic circular dichroism (ECD) data analysis was adopted to confirm the absolute configurations of 1-4. Compounds 1-6, 8 and 12-15 exhibited neuroprotective effects against H2O2-induced oxidative damage of human SH-SY5Y cells. Additionally, this study also combined Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses to explore the potential targets and signaling pathways of active terpenoids components in intervening Alzheimer's disease (AD).

A new dilignan from the twigs and leaves of Archidendron clypearia.

Previous work has shown that the lignans from the twigs and leaves of Archidendron clypearia (Jack) I.C.N. possess anti-ß-amyloid aggregation activity. Here we report a new dilignan, archidendronin A (1), along with one known sesquilignan (2). Their structures were determined by extensive spectroscopic methods, including UV, HRESIMS, 1 D and 2 D NMR data. The inhibitory activity on Aß1-42 aggregation was screened by ThT assay with curcumin as the positive control, and compounds 1 and 2 showed inhibition rate of 60.0% and 64.4% at 20 µM, respectively.[Formula: see text].

Dual-Mode Gas Sensor Composed of a Silicon Nanoribbon Field Effect Transistor and a Bulk Acoustic Wave Resonator: A Case Study in Freons.

In this paper, we develop a novel dual-mode gas sensor system which comprises a silicon nanoribbon field effect transistor (Si-NR FET) and a film bulk acoustic resonator (FBAR). We investigate their sensing characteristics using polar and nonpolar organic compounds, and demonstrate that polarity has a significant effect on the response of the Si-NR FET sensor, and only a minor effect on the FBAR sensor. In this dual-mode system, qualitative discrimination can be achieved by analyzing polarity with the Si-NR FET and quantitative concentration information can be obtained using a polymer-coated FBAR with a detection limit at the ppm level. The complementary performance of the sensing elements provides higher analytical efficiency. Additionally, a dual mixture of two types of freons (CFC-113 and HCFC-141b) is further analyzed with the dual-mode gas sensor. Owing to the small size and complementary metal-oxide semiconductor (CMOS)-compatibility of the system, the dual-mode gas sensor shows potential as a portable integrated sensing system for the analysis of gas mixtures in the future.

[Proteomics research of bufalin-induced apoptosis in osteosarcoma cell lines].

OBJECTIVE: To study the apoptosis inducing effects of bufalin on various human osteosarcoma cells and the concerning molecular mechanisms. METHOD: MTT assay was used to detect the growth inhibition rates of osteosarcoma cells U-20S, U-20S/MTX300, SaOS-2, IOR/OS9 treated with bufalin in different concentrations and times. The apoptosis of cells was observed flow cytometry 48 h following bufalin treatment. The proteomic techniques were used to separate and compare the treated and control groups 48 h after bufalin-incubation. Then, the proteomic results were validated by western blot. RESULT: Bufalin inhibited the growth of human osteosarcoma cells U20S, U20S/MTX300 (methotrexate resistant cells), SAOS2, IOR/OS9 in a dose- and time-dependent manner. The 72 h IC50 were (37.43 +/- 4.1), (32.24 +/- 5.3) nmol x L(-1) in U20S,U20S/MTX300 cells,respectivly. Flow cytometry showed that the apoptosis cells were increased following bufalin treatment. The protein expression profile showed 24 differentiated expression proteins. Among these proteins, the level of an anti-apoptotic protein, heat shock protein 27 (Hsp27) decreased significantly and the result was then validated by western blot. Ectopic expression of Hsp27 could reduce the bufalin-induced apoptosis remarkably in U20S and U20S/MTX300 cells. CONCLUSION: Bufalin could inhibit the cell growth and induce apoptosis on human osteosarcoma cells. The effect of bufalin may be related to the joint intervention with multiple protein targets. Among them, downregulation of Hsp27 plays a critical role in the bufalin-induced apoptosis in human osteosarcoma cells.

The value of palliative gastrectomy in gastric cancer with distant metastasis.

PURPOSE: The purpose of this study was to examine the value of surgical resection and to find prognostic factors for metastatic gastric cancer. METHODS: Clinicopathological data of 257 cM1 gastric cancer patients who underwent an operation at Seoul National University Hospital from January 1999 to December 2004 were reviewed. Patients were grouped into the resection (RS, n=165) and nonresection groups (NR, n=92). To evaluate whether there was any selection bias, patients were stratified according to chemotherapy and preoperative CT findings were compared. RESULTS: There were no significant differences in clinicopathologic features and preoperative CT findings between the RS and NR groups. For chemotherapy, the RS group had a survival benefit (median survival; 12.7 vs. 11.2 months, p=0.0107). In the subanalysis, there was a survival benefit to the RS group when metastasis was confined to one site (14 vs. 9.7 months, p=0.04). In patients with no chemotherapy, the RS group had no benefit (p=0.151). In univariate and multivariate analyses, resection (p=0.001), chemotherapy (p<0.001), the number of organs with metastatic lesions (p=0.003), and elective operation (p<0.001) were significant prognostic factors. CONCLUSIONS: This retrospective study suggests that surgical resection in metastatic gastric cancer may improve survival when combined with chemotherapy, especially when metastasis is confined to one site.

[In vitro screening of 32 traditional Chinese herbal extracts against U2OS human osteosarcoma cells].

OBJECTIVE: To test 32 traditional Chinese medicinal herbs with effects against osteosarcoma in vitro. METHODS: U(2)OS human osteosarcoma cell line was treated with the extracts of the Chinese herbs at various concentrations. The changes in cell proliferation in response to the treatment were examined by MTT assay, and the effects of these extracts against human osteosarcoma growth were compared. Morphological observation, flow cytometry and Annexin V were employed to detect the cell apoptosis after the treatments. RESULTS: According to the results of MTT assay, several of the 32 Chinese herbs, especially Venenum Bufonis and oxgall powder, were identified to produce growth inhibition against U(2)OS cells. Further study of the aqueous extracts of Venenum Bufonis and oxgall powder demonstrated their effects in inducing U(2)OS cell apoptosis, and Venenum Bufonis showed the strongest effect. In spite of the obvious growth inhibitory effect of oxgall powder, its extract induced cell apoptosis only at high concentrations. CONCLUSION: Several of the traditional Chinese herbs, especially Venenum Bufonis and oxgall powder, may inhibit the growth of U(2)OS cell line, and the results of this study pave the way for further identification of the effective components in the herbs that inhibit osteosarcoma growth both in vivo and in vitro.

In vitro screening of 32 traditional Chinese herbal extracts against U2OS human osteosarcoma cells / 南方医科大学学报

<p><b>OBJECTIVE</b>To test 32 traditional Chinese medicinal herbs with effects against osteosarcoma in vitro.</p><p><b>METHODS</b>U(2)OS human osteosarcoma cell line was treated with the extracts of the Chinese herbs at various concentrations. The changes in cell proliferation in response to the treatment were examined by MTT assay, and the effects of these extracts against human osteosarcoma growth were compared. Morphological observation, flow cytometry and Annexin V were employed to detect the cell apoptosis after the treatments.</p><p><b>RESULTS</b>According to the results of MTT assay, several of the 32 Chinese herbs, especially Venenum Bufonis and oxgall powder, were identified to produce growth inhibition against U(2)OS cells. Further study of the aqueous extracts of Venenum Bufonis and oxgall powder demonstrated their effects in inducing U(2)OS cell apoptosis, and Venenum Bufonis showed the strongest effect. In spite of the obvious growth inhibitory effect of oxgall powder, its extract induced cell apoptosis only at high concentrations.</p><p><b>CONCLUSION</b>Several of the traditional Chinese herbs, especially Venenum Bufonis and oxgall powder, may inhibit the growth of U(2)OS cell line, and the results of this study pave the way for further identification of the effective components in the herbs that inhibit osteosarcoma growth both in vivo and in vitro.</p>