Determination of Biflavones in Ginkgo biloba Leaves of Different Ages by UPLC-TQ-MS / 中国实验方剂学杂志

Objective: To establish an ultra-high performance liquid chromatography coupled with triple quadrupole mass for the determination of five biflavones. Method: Chromatographic separation was carried out on a ACQUITY UPLC BEH C18 column (2.1 mm×100 mm,1.7 μm) with gradient elution of acetonitrile and 0.10%formic acid at a flow rate of 0.3 mL·min-1,and the column temperature was set at 35℃. Result: Amentoflavone,bilobetin,ginkgetin,isoginkgetin,sciadopitysin showed a good linearity within the ranges of 0.02-13.20 mg·L-1(r=0.996 3),0.05-23.60 mg·L-1(r=0.995 5),0.09-18.60 mg·L-1(r=0.992 7),0.10-21.00 mg·L-1(r=0.998 8),0.06-16.00 mg·L-1(r=0.996 7),with average recoveries of 101.50%,98.78%,97.59%,97.24%,101.09%, and RSDs of 2.7%,2.7%,3.1%,2.8%,1.3%. The contents of amentoflavone,bilobetin,ginkgetin,isoginkgetin,sciadopitysin ranged between 121.30-434.74,268.39-847.14,251.80-1 297.10,195.87-691.10,477.48-3 003.90 μg·g-1. The total biflavones ranged between 1 474.45-5 635.40 μg·g-1. It shows a certain regularity that the low-vinegar leaves contain higher total flavonoids,and the total flavonoid content gradually decreases with the increase of tree age. Conclusion: The method was simple, and can be used for qualitative and quantitative analysis of biflavones.

Effect and mechanism of hesperetin on P-selectin mediated breast cancer MDA-MB-231 metastasis / 中草药

Objective: To study the effect of hesperetin on the migration of P-selectin mediated MDA-MB-231 breast cancer cells and its mechanism. Methods: Using computer virtual docking to evaluate the capacity of hesperetin binding to P-selectin in vitro; MTS test was observed with different concentration of hesperetin or P-selectin on the growth capacity of MDA-MB-231; The effect of hesperetin on P-selectin secretion by activated platelet was detected by Elisa kit; Adhesion experiments examined hesperetin on P-selectin-mediated MDA-MB-231 and endothelial cell adhesion; Transwell experiment was performed to analyze the effect of P-selectin on MDA-MB-231 breast cancer cell migration affected by hesperetin; Western blotting investigated MDA-MB-231 cell surface glycoprotein Mucin-1, Integrin β3, β1 and matrix metalloproteinase expression of MMP-2 and MMP-9 protein expression influenced by hesperetin; impact of hesperetin on MDA-MB-231 cell integrin-matrix metalloproteinase signaling pathway was analyzed to clarify the anti-tumor metastasis mechanism of hesperetin. Results: Hesperetin inhibited P-selectin-induced MDA-MB-231 cell migration and reduced HUVEC-breast cancer cell adhesion. Hesperetin down-regulated the expression of β1 and β3 integrins, and MMP-2 and MMP-9 at protein levels in MDA-MB-231 cells. Conclusion: Hesperetin can inhibit the growth capacity of MDA-MB-231 breast cancer cells, block P-selectin-induced breast cancer MDA-MB-231 tumor cell migration and adhesion, and the mechanism for hesperetin is through competitive P-selectin binding to Mucin-1.Subsequently, hesperetin could block PI3K/AKT/Paxillin/FAK/Src signaling pathway and down-regulate P-selectin mediated Integrins, MMP-2, and MMP-9 expression.

Three new triterpenoids isolated from the aerial parts of Ilex cornuta and protective effects against HO-induced myocardial cell injury / 中国天然药物

In the present study, three new triterpenoids, 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-α-L-arabinopyranoside (1), 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (2), and urs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (3), and a known triterpenoid, 3β-hydroxy-urs-2, 18-dien-28-oic acid (4, randialic acid B), were isolated from the aerial parts of Ilex cornuta. Their structures were identified by the spectroscopic analyses (IR, ESI-MS, HR-ESI-MS, and 1D and 2D NMR) and chemical reactions. Compound 4 showed significant cell-protective effects against HO-induced H9c2 cardiomyocyte injury. Compounds 1-4 did not show any significant DPPH radical scavenging activity.

Chemical constituents in stems of Ilex cornuta / 中草药

Objective: To investigate the chemical constituents in the stems of Ilex cornuta and the ability of scavenging free radicals of compounds 1-9. Methods: The compounds were isolated and purified by silica gel, medium pressure column chromatography, and semi-preparative liquid chromatography, and their structures were elucidated by chemical properties and spectroscopic analyses. The antifreeradical efficiency of compounds 1-9 was evaluated by DPPH radical scavenging assay. Results: Fifteen compounds were isolated and their structures were identified as isochlorogenic acid B (1), 3,4,5-tricaffeoylquinic acid (2), 4,5-di-O-caffeoyl quinic acid methyl ester (3), 3,4-di-O-caffeoyl quinicacid methyl ester (4), 3,5-di-O-caffeoyl quinicacid methyl ester (5), 3,4,5-tri-O-caffeoyl quinic acid methyl ester (6), 3,5-dimethoxy-4-hydroxybenzaldehyde (7), ethyl gallate (8), dihydrosyringenin (9), 2,6-dimethoxy-1,4-benzoquinone (10), arctigenin (11), 1-O-(vanillic acid)-6-O-(3″, 5″-dimethoxy-galloyl)-β-D-glycoside (12), (+)-1-hydroxypinoresinol-1-O-β-D-glucopyranoside (13), (+)-(7S,8S)-syringylglycerol 8-O-β-D-glucopyranoside (14), and schaftoside (15). Compounds 1-7 had good antifreeradical efficiency. Conclusion: Compounds 6,8-10,14, and 15 are obtained from the plants of Ilex L. the first time, and compounds 2,7,11, and 12 are obtained from this plant for the first time. Compounds 1-6 have good antifreeradical efficiency.

Study thought of pharmaceutical preparations quality standards by dynamic quality control technology / 中国中药杂志

Pharmaceutical preparations, particularly as a "secret recipe" of traditional Chinese medicine in medical institutions, are the product of China's medical and health industry, and they are also an important means of competing of different medical institutions. Although pharmaceutical preparations have advantages and characteristics than institutes for drug and pharmaceutical companies, the quality standards of pharmaceutical preparations in medical institutions has not reached the desired level over the years. As we all know, the quality of pharmaceutical preparations is important to ensure the efficacy, especially under the environment of people pay more sttention on drug safety and effectiveness and contry increase emphasis on the stste of pharmaceutical preparations. In view of this, we will improve the grade, stability, and clinical efficacy of pharmaceutical preparations by the advanced equipment, testing instruments and the process dynamic quality control technology. Finally, we hope we can provide new ideas for the quality control of pharmaceutical preparations.