Bioactive Benzofuran Derivatives from Cortex Mori Radicis, and Their Neuroprotective and Analgesic Activities Mediated by mGluR1.

Four new benzofuran-type stilbene glycosides and 14 known compounds including 8 benzofuran-type stilbenes and 6 flavonoids were isolated from the traditional Chinese medicine, Cortex Mori Radicis. The new compounds were identified as (9R)-moracin P 3'-O-α-l-arabinopyranoside (1), (9R)-moracin P 9-O-ß-d-glucopyranoside (2), (9R)-moracin P 3'-O-ß-d-glucopyranoside (3), and (9R)-moracin O 10-O-ß-d-glucopyranoside (4) based on the spectroscopic interpretation and chemical analysis. Three benzofuran-type stilbenes, moracin O (5), R (7), and P (8) showed significant neuroprotective activity against glutamate-induced cell death in SK-N-SH cells. In addition, moracin O (5) and P (8) also demonstrated a remarkable inhibition of the acetic acid-induced pain. The molecular docking with metabotropic glutamate receptor 1 (mGluR1) results indicated that these neuroprotective benzofuran-type stilbenes might be the active analgesic components of the genus Morus, and acted by mediating the mGluR1 pathway.

The distribution of transcutaneous CO2 emission and correlation with the points along the pericardium meridian.

This study aimed to understand energy metabolism distribution along the pericardium meridian and verify the correlation between the body surface (points), and classic meridian theory. A highly sensitive CO(2) instrument was used to measure the transcutaneous CO(2) emission at 13 points along the pericardium meridian line (12 points on the line and one point beyond the line) and 13 control points beside them. Results showed that the distribution of transcutaneous CO(2) emission is highly related to the position on the body. Transcutaneous CO(2) emission is significantly higher at P7 and P3, than the control points beside them. The points along the meridian and the points beside them were clustered with relative distance by SAS statistics software. Two distance matrixes were then obtained. The correlation coefficients between the points along the line and between the control points were calculated. The results showed that the 13(th) point beyond the line was far from the 12 points on the line (distance, 0.24), while acupoints on the line clustered earlier when compared with the non-acupoints. The average correlation coefficients among the acu-points was 0.65 which was significantly higher than 0.56, among the non-acupoints. No such characteristics were found among the control points. It was concluded that there is a strong correlativity of energy metabolism activity between the body surfaces along the meridian, and an even stronger correlativity between the acupoints on the meridian.

An intact unfolded protein response in Trpt1 knockout mice reveals phylogenic divergence in pathways for RNA ligation.

Unconventional mRNA splicing by an endoplasmic reticulum stress-inducible endoribonuclease, IRE1, is conserved in all known eukaryotes. It controls the expression of a transcription factor, Hac1p/XBP-1, that regulates gene expression in the unfolded protein response. In yeast, the RNA fragments generated by Ire1p are ligated by tRNA ligase (Trl1p) in a process that leaves a 2'-PO4(2-) at the splice junction, which is subsequently removed by an essential 2'-phosphotransferase, Tpt1p. However, animals, unlike yeast, have two RNA ligation/repair pathways that could potentially rejoin the cleaved Xbp-1 mRNA fragments. We report that inactivation of the Trpt1 gene, encoding the only known mammalian homolog of Tpt1p, eliminates all detectable 2'-phosphotransferase activity from cultured mouse cells but has no measurable effect on spliced Xbp-1 translation. Furthermore, the relative translation rates of tyrosine-rich proteins is unaffected by the Trpt1 genotype, suggesting that the pool of (normally spliced) tRNA(Tyr) is fully functional in the Trpt1-/- mouse cells. These observations argue against the presence of a 2'-PO4(2-) at the splice junction of ligated RNA molecules in Trpt1-/- cells, and suggest that Xbp-1 and tRNA ligation proceed by distinct pathways in yeast and mammals.

[Studies on chemical constituents of Halenia elliptica guided by in vivo absorption and distribution of the constituents].

AIM: To investigate the chemical constituents of the Tibetan herbal medicine Halenia elliptica by guidance of in vivo absorption and distribution of the constituents. METHODS: HPLC with a diode array detector (DAD) and HPLC-MS were used for detecting the constituents of extracts of Halenia elliptica and animal samples. Several kinds of column chromatography were used for the isolation and purification of the main in vivo absorbed and distributed compounds from the extract of Halenia elliptica. RESULTS: Six main components detected in the extracts of the animal samples were isolated from the ethanolic extract of Halenia elliptica. CONCLUSION: After rats were treated with different extracts of Halenia elliplica, low polar components xanthone aglycon of Halenia elliptica were clearly observed in the extracts of liver, lipid, blood, hidney, heart and brain tissue of rats, while the polar components xanthone glycosides were detected in very small amounts in the animal samples. The xanthone glycosides can be decomposed into xanthone aglycons during the digestion, absorption and metabolism procedure. Therefore, the in vivo activity of the xanthone glycosides might be exhibited by their decomposed products. It is an accessibly valuable method to investigate chemical components of herbal medicines under the guidance by detecting in vivo absorption and distribution of chemical components of the herbal medicine extract.