Two new antimicrobial monoterpenoid indole alkaloids from the roots of Rauvolfia yunnanensis.

Two new monoterpenoid indole alkaloids 3-hydroxylochnerine (1) and 10-hydroxyvinorine (2) were isolated from the roots of Rauvolfia yunnanensis. Their structures were elucidated based on the analysis of spectroscopic data and ECD calculation. Both compounds exhibited potent antimicrobial activity against Bacillus subtilis and Escherichia coli, and their activities were comparable to the well-known antibacterial drug berberine.

Polyhydroxylated eudesmane sesquiterpenoids and sesquiterpenoid glucoside from the flower buds of Tussilago farfara / 中国天然药物

Chemical fractionation of the n-BuOH partition, which was generated from the EtOH extract of the flower buds of Tussilago farfara, afforded a series of polar constituents including four new sesquiterpenoids (1-4), one new sesquiterpenoid glucoside (5) and one known analogue (6) of the eudesmane type, as well as five known quinic acid derivatives (7-11). Structures of the new compounds were unambiguously characterized by detailed spectroscopic analyses, with their absolute configurations being established by X-ray crystallography, electronic circular dichroism (ECD) calculation and induced ECD experiments. The inhibitory effect of all the isolates against LPS-induced NO production in murine RAW264.7 macrophages was evaluated, with isochlorogenic acid A (7) showing significant inhibitory activity.

Effect of siRNA-Interfering β-Catenin Expression on MDR of Human Multiple Myeloma Cell Line / 中国实验血液学杂志

OBJECTIVE@#To investigate the effecr of siRNA-interfering β-catenin expression on drug-resistance of multiple myeloma cells.@*METHODS@#The multiple myeloma cell line RPMI-8226 was cultured in vitro. The maphalan-resistant cell model was established by concentration gradient ascending of durg, then the drug-resistant cell line was instantaneously transfected with β-catenin siRNA, the sensitivity of RPMI 8226 cells to maphalan was detected by CCK-8 meltod before and after the transfection with siRNA; the mRNA and protein expression of β-catenin was detected by qRT-PCR and Western blot respectively, the apoptosis of cells was detected by flow cytometry.@*RESULTS@#IC of maphalan decreased from (5.29±0.19) μmol/L to (1.88±0.64) μmol/L, suggesting that the deplation of β-eatenin restored the sensitivity of drug-resistant cell line RPMI-8226 to malphalan. The Western blot showed that after the instaintaneous transfection with β-catenin siRNA, the β-catenin protein expression level obviously decreased, compared with level before transfection. After transfection, the maplalan-inducing apoptosis rate of cells increased from (35±0.5)% to (54±0.4)%, suggesting that the β-catinin gene may correlated with drug-resistance of cells. Interfering the expression of β-catenin gene could enhance the sensitivity of drug-resistant RPMI-8226 cells to maphalan.@*CONCLUSION@#The β-catenin siRNA interfereuce can inhisit the β-catenin gene expression in Wnt/β-catenin signaling pathway, suppress the cell proliferation, enhence the toxicity of maphalan on drug-resistant RPMI-8226 cells, thus result in increase of cell apoptosis.

Effect of Bushen Yanggu Decoction on Multidrug Resistance of Multiple Myeloma Cell Line KM3/BTZ / 中国实验血液学杂志

OBJECTIVE@#To explore the effect of Bushen Yanggu Decoction (BYD) on drug resistance and proliferation of human multiple myeloma-resistant KM3/BTZ cells.@*METHODS@#Human multidrug-resistant KM3/BTZ cells were established by Bortezomib (BTZ) gradient induction. The effects of commonly used chemotherapeutic drugs and serum containing Bushen Yanggu Decoction (BYD) on the proliferation of KM3 cells and KM3/BTZ cells were detected by MTT assay. RT-qPCR and Western blot were used to detect the expression of Par-4, HSP27 and P-gp genes. Flow cytometry was used to detect cell apoptosis.@*RESULTS@#The established KM3/BTZ cells could produce varying degree of resistance to commonly used chemotherapeutic drugs. Among them, the highest resistance index (RI) to BTZ was 20.269. MTT assay showed that the proliferation of KM3/BTZ cells treated with serum containing Bushen Yanggu Decoction was inhibited, and the inhibitory effect increased with the serum concentration incranse of Bushen Yanggu Decoction. The serum containing Bushen Yanggu Decoction could inhibit the proliferation of KM3/BTZ cells, and induce apoptosis, significantly reduce the drug-resistance of KM3/BTZ cells, up-regulate the expression of Par-4, down-regulate the expression of HSP27 and P-gp.@*CONCLUSION@#Bushen Yanggu Decoction can effectively inhibit the proliferation of KM3/BTZ cells and induce apoptosis. Bushen Yanggu Decoction can effectively reverse the multidrug-resistance of KM3/BTZ cells. The mechanism may be related with the decrease of expression of HSP27 and P-gp and the increase of expression of Par-4.

Chemical Constituents from Bletilla Ochracea / 昆明医科大学学报

Objective To study the chemical constituents from Bletilla ochracea. Methods The compounds were extracted by 95％ alcohol and isolated by column chromatography on silica gel and Sephadex LH-20. Their structures were identified by spectroscopic analysis (～1 H NMR and 13 CNMR).Results Nine compouds were obtained and identified as lusianthridin (1), 1, 2, 7-trihydroxy-4-methoxy-9, 10-dihydroxyphenanthrene (2), nudol (3), coelonin (4), batatasin Ⅲ (5), 3, 7-dihydroxy-2, 4-dimethoxyphenanthrene (6), daucosterol (7), β-sitosterol (8), stigmasterol (9).Conclus ion Compounds 2, 3, 5 were isolated from this plant for the first time.

Bibenzyls and Phenanthrenes from Arundina Graminifolia / 昆明医科大学学报

Objective To study the bibenzyls and phenanthrenes from Arundina graminifolia.Methods The compounds were extracted by 95％ alcohol and isolated by column chromatography on silica gel and Sephadex LH-20.Their structures were identified by spectroscopic analysis (1H NMR and13CNMR).Results Eleven compouds were obtained and identified as batatasin Ⅲ (1),arundinanin (2),2,8-dihydroxy-4,7-dimethoxy-9,10-dihydrophenanthrene (3),shancidin (4),arundinan (5),isoshancidin (6),erianthridin (7),lusianthridin (8),eulophiol (9),flavanthrin (10),orchinol (11).Conclusion Compounds 3,7,9 were isolated from this plant for the first time.

Construction of the subtracted cDNA library of striatal neurons treated with long-term morphine.

OBJECTIVE: To construct a morphine tolerance model in primarily cultured striatal neurons, and screen the differentially expressed genes in this model using suppression subtractive hybridization (SSH). METHODS: Sbtracted cDNA libraries were constructed using SSH from normal primarily cultured striatal neurons and long-term morphine treated striatal neurons (10-5 mol/L for 72 hours). To check reliability of the cell culture model, RT-PCR was performed to detect the cAMP-responsive element-binding protein (CREB) mRNA expression. The subtracted clones were prescreened by PCR. The clones containing inserted fragments from forward libraries were sequenced and submitted to GenBank for homology analysis. And the expression levels of genes of interest were confirmed by RT-PCR. Results CREB mRNA expression showed a significant increase in morphine treated striatal neurons (62.85 ± 1.98) compared with normal striatal neurons (28.43 ± 1.46, P < 0.01). Thirty-six clones containing inserted fragments were randomly chosen for sequence analysis. And the 36 clones showed homology with 19 known genes and 2 novel genes. The expression of 2 novel genes, mitochondrial carrier homolog 1 (Mtch1; 96.81 ± 2.04 vs. 44.20 ± 1.31, P < 0.01) and thymoma viral proto-oncogene 1 (Akt1; 122.10 ± 2.17 vs. 50.11 ± 2.01, P < 0.01), showed a significant increase in morphine-treated striatal neurons compared with normal striatal neurons. CONCLUSIONS: A reliable differential cDNA library of striatal neurons treated with long-term morphine is constructed. Mtch1 and Akt1 might be the candidate genes for the development of morphine tolerance.