Alkaloids from Corydalis saxicola and their antiproliferative activity against cancer cells.

Eight undescribed alkaloids named corydalisine D-K (1-7), including one isoquinoline benzopyranone alkaloid (1), one benzocyclopentanone alkaloid (2), four benzofuranone alkaloids (3, 4, and 5a/5b) and two protoberberine alkaloids (6 and 7), along with fourteen known ones, were isolated from the Corydalis saxicola. Their structures, including absolute configurations, were unambiguously identified using spectroscopic techniques, single-crystal X-ray diffraction and electron circular dichroism calculation. Compounds 2, 14 and 21 exhibit antiproliferative activity against five cancer cell lines. The aporphine alkaloid demethylsonodione (compound 14), which exhibited the best activity (IC50 = 3.68 ± 0.25 µM), was subjected to further investigation to determine its mechanism of action against the T24 cell line. The molecular mechanism was related to the arrest of cell cycle S-phase, inhibition of CDK2 expression, accumulation of reactive oxygen species (ROS), induction of cell apoptosis, inhibition of cell migration, and activation of p38 MAPK signaling pathway. The results indicated that 14 could be used as a potential candidate agent for further development of anti-bladder transitional cell carcinoma.

Ginsenoside Rb1 from Panax notoginseng Suppressed TNF-α-Induced Matrix Metalloproteinase-9 via the Suppression of Double-Strand RNA-Dependent Protein Kinase (PKR)/NF-κB Pathway.

Chronic inflammation is commonly accompanied by the stimulation of matrix metalloproteinases (MMPs) production and the degradation of the extracellular matrix. The overexpression of MMP-9 (Gelatinase B) highly participates in the progression of pathetic cardiac remodeling and liver cancer metastasis. Panax notoginseng (Burkill) F. H. Chen (Sanqi), a widely used traditional Chinese medicinal herb, shows myocardial protective and anti-tumor effects. In this study, we examined the inhibitory effect of different PNG extracts on tumor necrosis factor (TNF)-α-induced MMP-9 expression in cardiac myoblast H9c2 cells. Using a bioassay-guided fractionation scheme, the most active extract was fractionated by silica gel column chromatography and high-performance liquid chromatography until an active compound was obtained. The compound was identified as Ginsenoside Rb1 by nuclear magnetic resonance. Ginsenoside Rb1 inhibited TNF-α-induced MMP-9 production in both H9c2 and liver carcinoma HepG-2 cells. Interestingly, it did not affect the MMP-2 (Gelatinase A) level and the cell proliferation of the two cell lines. The inhibitory effects of Ginsenoside Rb1 may be due to its modulation of double-strand RNA-dependent protein kinase and nuclear factor kappa B signaling pathways. The results reveal the potential use of Ginsenoside Rb1 for the treatment of inflammatory and MMP-9-related cardiac remodeling and metastasis of hepatocellular carcinomas.

[Effects of long-term fertilization on evolution of S forms in a red soil and a black soil].

Sulfur (S) forms in two contrasting soils (a red soil and a black soil) under different long-term fertilization treatments (from 1990 to 2011) from the National Long-term Monitoring Network of Soil Fertility and Fertilizer Effects of China were investigated using a fractionation scheme in order to explore the distribution and transportation of S with different forms in the soils. The soil samples were collected from the topsoil (0-20 cm) and subsoil (20-40 cm) horizons that were treated with no fertilizers (CK), nitrogen, phosphorus, and potassium fertilizers (NPK), or NPK plus organic manures (MNPK) since 1990. The results indicated that when compared with the CK, total S contents in the topsoil layers treated with NPK and MNPK were increased by 42% and 33% for the red soil, and by 6% and 76% for the black soil, respectively, while the total S in the subsoil layer was less affected by the fertilization treatments and obviously lower than in the topsoil layer except for the red soil treated with NPK. The main forms of inorganic S in the red soil and black soil were found to be available S and HCl-extracted S, respectively. The application of NPK and MNPK increased the available S by 447% and 102% in the topsoil layer of the red soil compared with CK, and facilitated the transportation of available S into the lower depth. In contrast, NPK and MNPK only increased the available S by 54% and 93% in the topsoil layer of the black soil, and showed a slight influence on available S in the subsoil. The organic S forms were predominantly composed of ester S and residual S in the two soils. Under long-term fertilization, the residual S significantly increased over 32% and 55% in the topsoil and subsoil layers, respectively, compared with CK. The ester S and carbon-bonded S, which were relatively active, were less affected by the fertilization treatments, but positively related to the level of organic carbon in each soil (P < 0.05). In addition, the results from the long-term experiments indicated that the contribution of S input from atmospheric deposition was significant and should not be neglected.