isometric-contractility-measurement-mouse-mesenteric-artery-using

Isometric Contractility Measurement of the Mouse Mesenteric Artery Using Wire Myography

The wire myograph technique is used to assess the contractility of vascular smooth muscles in response to depolarization, GPCR agonists/inhibitors and ...

Nanjing University of Chinese Medicine

The reinvestigation of Strychnos nux-vomica resulted in the isolation of two colorless monoquaternary bisindole alkaloids from the seeds. The structures of the two new compounds named 4-N-hydroxymethyl strychnidin-17-acetic acid (1) and 10, 11-dimethoxy-4-N-hydroxymethyl strychnidin-17-acetic acid (2), were defined by detailed spectral analyses, especially (1)H NMR, (13)C NMR, DEPT, HSQC, (1)H NMR-(1)H NMR, NOESY, HMBC and TOF-MS.

Two new bisindole alkaloids from the seeds of Strychnos nux-vomica.

To determine the mode of action of 5-hydroxymethylfurfural (5-HMF) extracted from wine-processed Fructus corni on hepatoprotective activities, the effects of 5-HMF on H(2)O(2)-induced human L02 hepatocytes injury was examined. MTHODS: Hepatocytes L02 injured by H(2)O(2) was treated by 5-HMF. The morphological changes of the cells were observed under inverted phase-contrast, fluorescence, and transmission electron microscopy and the activities of caspase-9 and caspase-3 were tested by enzyme-linked immunosorbent detector.

Investigation on the morphological protective effect of 5-hydroxymethylfurfural extracted from wine-processed Fructus corni on human L02 hepatocytes.

To investigate the influences of extracts of Oxytropis falcata on proliferation of SMMC-7721 cells and expression of MMP-2 (matrix metalloproteinase-2).

[Influences of Oxytropis falcata on proliferation of SMMC-7721 hepatocarcinoma cells and expression of MMP-2].

Radix Aconiti Lateralis (Fuzi in Chinese, derived from the lateral roots of Aconitum Carmichaeli Debx.) is widely used for the treatment of heart failure, internal cold, arthralgia, diarrhea and edema for thousands of years. It was usually prescribed in combination with Rhizoma Zingiberis (Ganjiang in Chinese, derived from the dry rhizome of Zingiber officinale Rosc.) to decrease toxicity and increase efficacy.

The effects of Rhizoma Zingiberis on pharmacokinetics of six Aconitum alkaloids in herb couple of Radix Aconiti Lateralis-Rhizoma Zingiberis.

This study aimed to clarify the rationality of herbaceous compatibility of a rhubarb peony decoction (DaHuang-Mu-Dan-Tang, RPD) by comparing the pharmacokinetics of aloe-emodin, rhein and emodin in rats' plasma after oral administration of RPD and rhubarb extract. A rapid, sensitive LC-MS method was developed and validated for the determination of the plasma concentrations of the three analytes after oral administration RPD and rhubarb extract. The developed method was successfully applied to a pharmacokinetic study of aloe-emodin, rhein and emodin in rats' plasma after oral administration. Compared with administration of single rhubarb, the C(max) of rhein in RPD was decreased significantly (p < 0.05). Meanwhile, the T1/2 of aloe-emodin and emodin were increased significantly (p < 0.05) after administration of RPD. In addition, the T(max) of rhein and emodin were also increased significantly (p < 0.05) in RPD. These results indicated that the absorption of rhein in rats was suppressed after oral administration RPD. Moreover, The time for rhein and emodin to reach the peak concentration was delayed and the elimination of aloe-emodin and emodin was also postponed in RPD. This study could provide a meaningful basis for evaluating the clinical application of traditional Chinese medicine in terms of pharmacokinetics.

Comparative pharmacokinetics of aloe-emodin, rhein and emodin determined by liquid chromatography-mass spectrometry after oral administration of a rhubarb peony decoction and rhubarb extract to rats.

To investigate the antitumor effects of extracts from Oxytropis falcata on human hepatocellular carcinoma SMMC-7721 cells in vitro and in transplanted murine H22 tumors in vivo.

Antitumor effects of two extracts from Oxytropis falcata on hepatocellular carcinoma in vitro and in vivo.

Radix Scutellariae (RS) is a herbal medicine with various pharmacological activities to treat inflammation, respiratory and gastrointestinal infections, etc. In this study, a rapid, sensitive and selective UPLC-ESI-MS/MS method was developed for simultaneous determination of 10 flavonoids - scutellarin, scutellarein, chrysin, wogonin, baicalein, apigenin, wogonoside, oroxylin A-7-O-glucuronide, oroxylin A and baicalin - from RS aqueous extracts in rat plasma with propyl paraben as internal standard (IS). Chromatographic separation was achieved on a C18 column using gradient elution with the mobile phase consisting of methanol and water (containing 0.1% formic acid) at a flow rate of 0.2 mL/min. The detection was performed in multiple reaction monitoring mode using electrospray ionization in negative mode. The validated method showed good linearity over a wide concentration range (r >0.9935). The intra- and interday assay variabilities were <9.5% and <12.4% for all analytes, respectively. The extraction recovery ranged from 71.2 to 89.7% for each analyte and IS. This method was successfully applied to pharmacokinetic comparision after oral administration of crude and wine-processed RS aqueous extracts. There were significant differences in some pharmacokinetic parameters of most analytes between crude and wine-processed RS. This suggested that wine-processing exerted effects absorption of most flavonoids.

Simultaneous determination of ten flavonoids of crude and wine-processed Radix Scutellariae aqueous extracts in rat plasma by UPLC-ESI-MS/MS and its application to a comparative pharmacokinetic study.

A new skeleton benzylisoquinoline (BI) named neoliensinine (1) was isolated from embryos of lotus seed (Nelumbo nucifera Gaertn.), a traditional Chinese herb. The tribenzylisoquinoline (TBI) structure of 1 was confirmed by interpreting spectroscopic data of UV, IR, MS, 1D and 2D NMR. The stereo-configurations of the new compound, together with two known bisbenzylisoquinolines (BBI), neferine and isoliensinine were established by analyzing H NMR and C NMR spectra. The relaxation of 1, neferine, isoliensinine and liensinine in isolated mesenteric vascular smooth muscle (VSM) was evaluated. All the four BIs could efficiently inhibit MVSM contraction induced by 124mM KCl, with IC values of 2.407μM (1), 1.169μM (neferine), 3.504μM (isoliensinine) and 3.583μM (liensinine), respectively, suggesting that they were all potential relaxants for abnormal smooth muscle contractions. Interestingly, VSM treated by the three BBIs could re-contract when being stimulated by KCl after the drugs were removed, while VSM dealt with the TBI couldn't. It indicated that 1 has much high affinity with the molecular targets on relaxation of VSM contraction, which may relate to the unique skeleton with three BI groups.

Guang Ming Yang

School of Pharmacy

Nanjing University of Chinese Medicine

Isometric Contractility Measurement of the Mouse Mesenteric Artery Using Wire Myography