White crystalline powder
Fritillaria cirrhosa,Fritillaria thunbergii
Peimine/Isodihydroimperialin/5α-Cevane-3β,6α,20-triol/verticine/(3β,5α,6α)-Cevane-3,6,20-triol/Verticine,Zhebeinine,Wanpeinine A/ISODIHYDROIMPERIALINE/Dihydroisoimperialine/(3b,5a,6a)-cevane-3,6,20-triol/cevane-3,6,20-triol, (3b,5a,6a)-/Cevane-3,6,20-triol, (3β,5α,6α)-
568.4±50.0 °C at 760 mmHg
HS Code Reference
Personal Projective Equipment
For Reference Standard and R&D, Not for Human Use Directly.
provides coniferyl ferulate(CAS#:23496-41-5) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
Background and objective: Fritillaria is a Chinese traditional herb. It has a long history and many medicinal usages including antitussive, anti-inflammatory and pain relieving actions. It is also used as food. However, its cardiac safety has not been tested. Peimine is one of the main active compounds of Fritillaria. To be listed as an herb in the Chinese Pharmacopoeia, a special minimal percentage of Peimine in the dry sample of Fritillaria is required. The main concern for cardiac safety determination is the possible inhibition of hERG ion channels. Thus, Peimine was chosen to investigate its inhibitory effects on hERG channels.
Methods: Whole cell patch clamp technique was used.
Results and conclusion: We found that Peimine inhibited the hERG peak tail currents in a concentration dependent manner with an IC50 value of 43.7μM (n=4) by whole cell patch clamp techniques. Multiple results suggest that the inhibition was related to the channel inactivation. First, Peimine inhibition was significantly increased when the prepulse voltage was increased from -30mV to +10mV. Second, increasing prepulse length also significantly increased blockade by Peimine. Third, our finding that the inhibition by Peimine was use-dependent is related to changes in the inactivated state of the channel. Finally, the result that Peimine significantly decreased inactivation constant also suggested that Peimine affect the channel inactivation state. Mutation of Y652 to Alanine reduced sensitivity to Peimine, suggesting that Y652 is an important hERG binding sites for Peimine.
Cardiac safety; Fritillaria; Inactivation; Peimine; hERG.
Peimine Inhibits hERG Potassium Channels Through the Channel Inactivation States
Liandi Kan 1 , Wei Zhao 2 , Lanying Pan 2 , Jianwei Xu 2 , Qingmao Chen 3 , Kai Xu 3 , Liping Xiao 2 , Yuan Chen 4
Osteoarthritis (OA) is the most common type of degenerative joint disease and secreted inflammatory molecules serve a pivotal role in it. Peimine has been reported to have anti‑inflammatory activity. In order to investigate the potential therapeutic role of Peimine in OA, mouse articular chondrocytes were treated with IL‑1β and different doses of Peimine in vitro. The data revealed that Peimine not only suppressed IL‑1β‑induced production of nitric oxide (NO) and prostaglandin E2, but also reduced the protein levels of inducible NO synthase (iNOS) and cyclooxygenase‑2 (COX‑2). In addition, Peimine inhibited the IL‑1β‑induced mRNA expression of matrix metalloproteinase (MMP)‑1, MMP‑3, MMP‑9, MMP‑13, a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS)‑4 and ADAMTS‑5. Furthermore, Peimine inhibited IL‑1β‑induced activation of the mitogen‑activated protein kinase (MAPK) pathway. The protective effect of Peimine on IL‑1β‑treated chondrocytes was attenuated following activation of the MAPK pathway, as demonstrated by the increased expression levels of MMP‑3, MMP‑13, ADAMTS‑5, iNOS and COX‑2 compared with the Peimine group. The in vivo data suggested that Peimine limited the development of OA in the mouse model. In general, the data indicate that Peimine suppresses IL‑1β‑induced inflammation in mouse chondrocytes by inhibiting the MAPK pathway, suggesting a promising therapeutic role for Peimine in the treatment of OA.
Cardiac safety; Fritillaria; Inactivation; Peimine; hERG.
Peimine Suppresses interleukin‑1β‑induced Inflammation via MAPK Downregulation in Chondrocytes
Kun Chen 1 , Zheng-Tao Lv 1 , Chen-He Zhou 2 , Shuang Liang 1 , Wen Huang 3 , Zheng-Gang Wang 1 , Wen-Tao Zhu 1 , Yu-Ting Wang 1 , Xing-Zhi Jing 1 , Hui Lin 4 , Feng-Jing Guo 1 , Peng Cheng 1 , An-Min Chen 1
Background: Peimine is a major biologically active component of Fritillaria ussuriensis. Peimine was investigated in chronic inflammation response, but it has not been studied in mast cell-related immediate allergic reaction. The present study aimed to evaluate anti-allergic effect of peimine in human mast cell (HMC-1).
Materials and methods: The effect of peimine on cell viability was measured by MTS assay in HMC-1. Histamine release was investigated in rat peritoneal mast cells (RPMCs). Interleukin (IL)-6, IL-8, and tumor necrosis factor-α (TNF-α) expressions were measured by ELISA assay and reverse transcription-polymerase chain reaction. Mitogen-activated protein kinases (MAPKs) and nuclear factor-kappaB (NF-κB) were examined by Western blot. Passive cutaneous anaphylaxis (PCA) reactions were evaluated using Sprague-Dawley (SD) rats.
Results: Peimine inhibited the production of pro-inflammatory cytokines, such as IL-6, IL-8, and TNF-α. Moreover, peimine reduced MAPKs phosphorylation and the nuclear NF-κB expression in PMACI-induced HMC-1. Peimine decreased PCA reactions in rats as well.
Conclusion: Our study proved that peimine might be suitable for the treatment of mast cell-derived allergic inflammatory reactions.
Summary: Peimine inhibited the production of pro-inflammatory cytokines, such as IL-6, IL-8, and TNF-αPeimine reduced MAPKs phosphorylation and the nuclear NF-κB expression in PMACI-induced HMC-1Peimine decreased PCA reactions in ratsPeimine has anti-allergic effect through regulation of pro-inflammatory mechanism on mast cell. Abbreviations used: HMC-1: Human mast cell, MTS: 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, RPMCs: Rat peritoneal mast cells. IL-6: Interleukin 6, IL-8: Interleukin 8, TNF-α: Tumor necrosis factor-α, MAPKs: Mitogen-activated protein kinases; NF-κB: Nuclear factor-kappaB, PCA: Passive cutaneous anaphylaxis reactions, SD: Sprague-Dawley.
MAP kinases; cytokine; human mast cell (HMC-1); inflammation; nuclear factor-kappaB (NF-κB); peimine.
Peimine Inhibits the Production of Proinflammatory Cytokines Through Regulation of the Phosphorylation of NF-κB and MAPKs in HMC-1 Cells
Ji Hye Park 1 , Bina Lee 1 , Hyun Kab Kim 1 , Eun-Young Kim 1 , Jae-Hyun Kim 1 , Ju-Hee Min 1 , Sunkook Kim 2 , Youngjoo Sohn 1 , Hyuk-Sang Jung 1
Peimine(Dihydroisoimperialine; Verticine) is a natural compound with good anti-inflammatory effects in vivo.IC50 value:Target:Peimine (0-25 mg/L) significantly inhibited tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-1β, and increased IL-10 production. Furthermore, peimine significantly inhibited the phosphorylation of p38, ERK and c-jun N-terminal kinase (JNK) as well as decreased p65 and IκB.