1.Shanzhiside methylester, the principle effective iridoid glycoside from the analgesic herb Lamiophlomis rotata, reduces neuropathic pain by stimulating spinal microglial β-endorphin expression.
Fan H1, Li TF1, Gong N1, Wang YX2. Neuropharmacology. 2016 Feb;101:98-109. doi: 10.1016/j.neuropharm.2015.09.010. Epub 2015 Sep 9.
Lamiophlomis rotata (L. rotata, Duyiwei) is an orally available Tibetan analgesic herb widely prescribed in China. Shanzhiside methylester (SM) is a principle effective iridoid glycoside of L. rotata and serves as a small molecule glucagon-like peptide-1 (GLP-1) receptor agonist. This study aims to evaluate the signal mechanisms underlying SM anti-allodynia, determine the ability of SM to induce anti-allodynic tolerance, and illustrate the interactions between SM and morphine, or SM and β-endorphin, in anti-allodynia and anti-allodynic tolerance. Intrathecal SM exerted dose-dependent and long-lasting (>4 h) anti-allodynic effects in spinal nerve injury-induced neuropathic rats, with a maximal inhibition of 49% and a projected ED50 of 40.4 μg. SM and the peptidic GLP-1 receptor agonist exenatide treatments over 7 days did not induce self-tolerance to anti-allodynia or cross-tolerance to morphine or β-endorphin. In contrast, morphine and β-endorphin induced self-tolerance and cross-tolerance to SM and exenatide.
2.Simultaneous determination of shanzhiside methyl ester, 8-O-acetylshan- zhiside methyl ester and luteolin-7-O-β-d-glucopyranoside in rat plasma by ultra performance liquid chromatography-tandem mass spectrometry and its application to a pharmacokinetic study after oral administration of Lamiophlomis rotata Pill.
Chen J1, Wang Y1, Liang X1, Sun T1, Luo J1, Guo X1, Zhao L2. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 May 1;1020:62-6. doi: 10.1016/j.jchromb.2016.03.021. Epub 2016 Mar 19.
A rapid, sensitive and specific ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the quantification of shanzhiside methyl ester, 8-O-acetylshanzhiside methyl ester and luteolin-7-O-β-d-glucopyranoside of Lamiophlomis rotata Pill in rat plasma was developed and validated. After liquid-liquid extraction with n-butyl alcohol/ethyl acetate (70:30, v/v), analytes and paeoniflorin (internal standard, IS) were separated on an Acquity BEH UPLC C18 column (100×2.1mm, 1.7μm) with gradient elution at a flow rate of 0.2mL/min. All calibration curves had good linearity (r>0.9929) over the concentration ranges of 1-1000ng/mL for shanzhiside methyl ester and 8-O-acetylshanzhiside methyl ester, 0.3-150ng/mL for luteolin-7-O-β-d-glucopyranoside. The intra- and inter-day precisions were all within 11.1% and the accuracy (relative error, RE%) all ranged from -13.6% to 5.3%. The method also guaranteed an acceptable selectivity, recovery and stability, which was successfully applied to a pharmacokinetic study of the three analytes in rats after oral administration of Lamiophlomis rotata Pill.
3.A new anti-fibrinolytic hemostatic compound 8-O-acetyl shanzhiside methylester extracted from Lamiophlomis rotata.
Fan PC1, Ma HP1, Hao Y2, He XR2, Sun AJ1, Jiang W2, Li MX1, Jing LL1, He L2, Ma J3, Jia ZP4. J Ethnopharmacol. 2016 Apr 13. pii: S0378-8741(16)30206-9. doi: 10.1016/j.jep.2016.04.016. [Epub ahead of print]
BACKGROUND: Fibrinolysis prevents blood clots from growing and becoming problematic. Antifibrinolytics are used as inhibitors of fibrinolysis. Aprotinin was abandoned after identification of major side effects, especially on kidney. Lysine analogues has their own defects and whether they are adequate substitutes for aprotinin is still under doubt. Lamiophlomis rotata (Benth.) Kudo. was previous found to have hemostatic activity. But the active compound in L. rotata and its hemostatic mechanism were unknown.