Protective Effects of Ferulic Acid on Metabolic Syndrome: A Comprehensive Review.

Metabolic syndrome (MetS) is a complex disease in which protein, fat, carbohydrates and other substances are metabolized in a disorderly way. Ferulic acid (FA) is a phenolic acid found in many vegetables, fruits, cereals and Chinese herbs that has a strong effect on ameliorating MetS. However, no review has summarized the mechanisms of FA in treating MetS. This review collected articles related to the effects of FA on ameliorating the common symptoms of MetS, such as diabetes, hyperlipidemia, hypertension and obesity, from different sources involving Web of Science, PubMed and Google Scholar, etc. This review summarizes the potential mechanisms of FA in improving various metabolic disorders according to the collected articles. FA ameliorates diabetes via the inhibition of the expressions of PEPCK, G6Pase and GP, the upregulation of the expressions of GK and GS, and the activation of the PI3K/Akt/GLUT4 signaling pathway. The decrease of blood pressure is related to the endothelial function of the aortas and RAAS. The improvement of the lipid spectrum is mediated via the suppression of the HMG-Co A reductase, by promoting the ACSL1 expression and by the regulation of the factors associated with lipid metabolism. Furthermore, FA inhibits obesity by upregulating the MEK/ERK pathway, the MAPK pathway and the AMPK signaling pathway and by inhibiting SREBP-1 expression. This review can be helpful for the development of FA as an appreciable agent for MetS treatment.

Design and Efficient Synthesis of RalA Inhibitors Containing the Dihydro-α-carboline Scaffold.

Ras-related protein RalA is a member of the Ras small GTPases superfamily. Its activation plays an important role in regulating tumor initiation, invasion, migration, and metastasis. In this study, we designed a new type of RalA inhibitor containing a dihydro-α-carboline scaffold. The structurally new dihydro-α-carboline derivatives could be efficiently synthesized in good yields through a newly developed three-component [3+2+1] cyclization reaction. Evaluation of the biological activity showed that some of the dihydro-α-carboline derivatives can inhibit RalA/B and proliferative activities of NSCLC cell lines. The 4-(pyridin-3-yl)-dihydro-α-carboline compound (3 o) was found to be the most potent derivative, with IC50 values of 0.43±0.03, 0.64±0.07, 0.93±0.10, and 1.54±0.15 µM against A549, H1299, H460, and H1975 cells, respectively. Mechanism investigation suggested that 3 o inhibits the RalA/B activation of A549, down-regulates Bcl-2, stimulates cytochrome c and PARP cleavage, and induces cell apoptosis. A molecular docking study revealed that 3 o can form stable hydrogen bonds with residues of RalA. Moreover, amide-π and alkyl-π interactions also contributed to the affinity between 3 o and RalA.

[Influence of metal ions on stability of 2,3,5,4'-tetrahydroxy stilbene-2-O-ß-D-glucoside contained in Polygoni Multiflori Radix].

Decoction is one of the most commonly used dosage forms of traditional Chinese medicine. The stability of chemical constituents in decoction is closely related to the clinical efficacy and safety. There were few reports about the influence of metal ions in the stability of chemical constituents in traditional Chinese medicine. However, there is no evidence that metal ions in decoction water need to be controlled. In this study, 2,3,5,4'-tetrahydroxy stilbene-2-O-ß-D-glucoside (THSG), one of the main constituents in Polygoni Multiflori Radix was studied. Ordinary tap water, deionized water, and water containing different metal ions were used to investigate and compare the influence on THSG. The results showed that after storage in a dark place at the room temperature for 10 days, the degradation of THSG was 7% in deionized water, while undetectable in tap water. The content of THSG could be decreased by different kinds of metal ions, and the effect was concentration-dependent. Moreover, Fe3+ and Fe2+ showed the greatest influence at the same concentration; and our study has shown that THSG decreased more than 98% in Fe and Fe2+ solutions at 500 ppm concentration. In the same time we found out p-hydroxybenzaldehyde (molecular weight: 122.036 7) and 2,3,5-trihydroxybenzaldehyde-2-O-glycoside (molecular weight: 316.079 4) were the main degradation products of THSG in tap water and water containing Cu2+, Ca2+, Zn2+, Mg2+ and Al3+. The product of THSG dimer with a water molecule was found in water containing Fe3+ and Fe2+. The above results showed that the metal ions in water could significantly influence the stability of THSG in water, indicating that the clinical efficacy and safety of decoction would be affected if the metal ions in water were not under control. It's suggested that deionized water should be used in the preparation of decoction containing Polygoni Multiflori Radix in the clinic to avoid degradation of THSG. Meanwhile, decoction prepared by tap water should be taken by patients in a short time. Our investigation provides important information and reference about the influence of metal ions on the stability of decoctions in other traditional Chinese medicine that have unstable groups such as hydroxyls and unsaturated bonds, etc.

Compounds from the Chinese black ant (Polyrhachis dives) and NMR behavior of the isomers with formamide group.

Two new dopamine derivatives divesamides A (1) and B (2), along with six known N-containing compounds were isolated from the Chinese black ant (Polyrhachis dives). Their structures were determined on the basis of spectroscopic methods. Compound 1 is a racemate, and chiral HPLC separation yielded a pair of antipodes. The absolute configuration of (+)-1 was assigned by a computational method. The double signals in the (1)H and (13)C NMR spectra of 2 that resulted from the presence of a formamide group were discussed. The T- and B-lymphocytes proliferation assay showed that 2 has moderate immunosuppressive activity toward T- and B-lymphocytes proliferation at a concentration of 20 µM.

[Effects of acidic soil improvement on active-state Cd content in soil and Cd content in Ligusticum chuanxiong].

OBJECTIVE: To explore the method to reduce the Cd content in Ligusticum chuanxiong, and to offer the reference for planting Ligusticum chuanxiong with low Cd content. METHODS: A field experiment was carried out to improve the acidic Cd-contaminated soils by different quicklime application, and the effect of quicklime on the percentage of active-state Cd in soil and Cd content in Ligusticum chuanxiong was examined. RESULTS: Quicklime could reduce the percentage of active-state Cd in soil by increase the acid soil pH value,and as a result, significantly reduce Cd content in Ligusticum chuanxiong. A highly significant negative correlation was found be- tween the Cd content in Ligusticum chuanxiong and quicklime application rate(P =0. 008). Compared with the blank group, Cd content in Ligusticum chuanxiong was reduced by 27. 66%, 24. 87% and 46. 20%, with 750, 1 125 and 1 500 kg/hm2 quicklime application, respectively; while with 1 500 kg/hm2 quicklime application, the soil pH value increased significantly and kept steadily, and the percentage of active-state Cd in soil showed a regular trend which was decreased firstly and increased subsequently. CONCLUSION: Cd content in Ligusticum chuanxiong can be reduced significantly by quicklime application,and the effect of high application of quicklime on Cd content in Ligusticum chuanxiong, soil pH values and percentage of active-state Cd in soil is more effective and steady.

Study on drug property differences of shexiang (moschus) and bingpian (borneolum synthcticum) based on analysis of biothermodynamics.

OBJECTIVE: To study the drug property differences of Shexiang (Moschus) and Bingpian (Borneolum Synthcticum) with biothermodynamics, and to verify the objectivity and authenticity of the drug property. METHODS: The growth-thermogram curves of Escherichia coli (E. coli) affected by Shexiang (Moschus) and Bingpian (Borneolum Synthcticum) at different concentrations were determined with microcalorimetry, and the power-time curves (thermogram curves) of E. coli metabolism and characteristic parameters, such as growth rate constant (k), maximum output power (P(m)), peak time (t(p)), total heat-output (Q(t)), etc. were analyzed with the principal component analysis (PCA) to find the close correlative parameters, so as to objectively reflect the drug property differences of Shexiang (Moschus) and Bingpian (Borneolum Synthcticum). RESULTS: The values of P2 in the second exponential growth phase increased with the increase of the concentrations of Shexiang (Moschus) and Bingpian (Borneolum Synthcticum), and the P2 of Shexiang (Moschus) was larger than that of Bingpian (Borneolum Synthcticum); Q2 increased with the increase of the concentrations of Shexiang (Moschus), but for Bingpian (Borneolum Synthcticum) it was opposite. It is indicated that they have different effects on P2 and Q2 of E. coli in the second exponential growth phase, and have differences in warm and cold natures. CONCLUSION: The microcalorimetry can accurately and objectively appraise differences of the drug property of Shexiang (Moschus) and Bingpian (Borneolum Synthcticum) and verify the objectivity and authenticity of the drug property, so as to provide a new and useful method for studies of the drug property of Chinese drugs.

[Study on the chemical constituents of Rhizoma Cyperi].

OBJECTIVE: To study the chemical constituents of Rhizoma Cyperi. METHODS: The constituents were separated and purified by silica gel column chromatography, their structures were identified on the basis of physico-chemical properties and spectral data. RESULTS: Six compounds were isolated and identified as physicion (1), hexadecanoic acid (2), beta-sitosterol (3), stigmasterol (4), catenarin (5), daucosterol (6). CONCLUSION: Compounds 1, 4, 5 were isolated from this plant for the first fime.