Mechanism of Shengmai Injection on Anti-Sepsis and Protective Activities of Intestinal Mucosal Barrier in Mice.

OBJECTIVE: To study the mechanism of Shengmai Injection (SMI, ) on anti-sepsis and protective activities of intestinal mucosal barrier. METHODS: The contents of 11 active components of SMI including ginsenoside Rb1, Rb2, Rb3, Rd, Re, Rf, Rg1, Rg2, ophioposide D, schisandrol A and schisantherin A were determined using ultra-performance liquid chromatography. Fifty mice were randomly divided into the blank, the model, the low-, medium- and high-dose SMI groups (0.375, 0.75, 1.5 mL/kg, respectively) by random number table, 10 mice in each group. In SMI group, SMI was administrated to mice daily via tail vein injection for 3 consecutive days, while the mice in the blank and model groups were given 0.1 mL of normal saline. One hour after the last SMI administration, except the blank group, the mice in other groups were intraperitoneally injected with lipopolysaccharide (LPS) saline solution (2 mL/kg) at a dosage of 5 mL/kg for development of endotoxemia mice model. The mice in the blank group were given the same volume of normal saline. Inflammatory factors including interferon-γ (INF-γ), tumor necrosis factor-α (TNF-α), interleukin (IL)-2 and IL-10 were measured by flow cytometry. Myosin light-chain kinase (MLCK), nuclear factor κB (NF-κB) levels, and change of Occludin proteins in jejunum samples were analyzed by Western blot. RESULTS: The decreasing trends of INF-γ, TNF-α and IL-2 were found in serum of SMI treatment groups. In SMI-treated mice, the content of Occludin increased and MLCK protein decreased compared with the model group (P<0.05 or P<0.01). The content of cellular and nuclear NF-κB did not change significantly (P>0.05). CONCLUSION: SMI may exert its anti-sepsis activity mainly through NF-κB-pro-inflammatory factor-MLCK-TJ cascade.

Akkermansia muciniphila: A potential novel mechanism of nuciferine to improve hyperlipidemia.

BACKGROUND: Intestinal microbiota is a novel drug target of metabolic diseases, especially for those with poor oral bioavailability. Nuciferine, with poor bioavailability, has an anti-hyperlipidemic effect at low dosages. PURPOSE: In the present study, we aimed to explore the role of intestinal microbiota in the anti-hyperlipidemic function of nuciferine and identify the key bacterial targets that might confer the therapeutic actions. METHODS: The contribution of gut microbes in the anti-hyperlipidemic effect of nuciferine was evaluated by conventional and antibiotic-established pseudo-sterile mice. Whole-metagenome shotgun sequencing was used to characterize the changes in microbial communities by various agents. RESULTS: Nuciferine exhibited potent anti-hyperlipidemic and liver steatosis-alleviating effects at the doses of 7.5-30 mg/kg. The beneficial effects of nuciferine were substantially abolished when combined with antibiotics. Metagenomic analysis showed that nuciferine significantly shifted the microbial structure, and the enrichment of Akkermansia muciniphila was closely related to the therapeutic effect of nuciferine. CONCLUSIONS: Our results revealed that gut microbiota played an essential role in the anti-hyperlipidemic effect of nuciferine, and enrichment of Akkermansia muciniphila represented a key mechanism through which nuciferine exerted its therapeutic effects.

Congmujingnosides B-G, triterpene saponins from the stem of Aralia chinensis and their protective effects against H2O2-induced myocardial cell injury.

Phytochemical investigation of the stem of Aralia chinensis yielded six new oleanane-type triterpene saponins named as congmujingnosides B-G (1-6). The new ones were elucidated on the basis of the chemical and spectroscopic analysis. Protective effects of compounds 1-6 were tested against H2O2-induced H9c2 cardiomyocyte injury, and the data showed that compounds 1 and 5 had significant cell-protective effects. No significant DPPH radical scavenging activity was observed for compounds 1-6.

New Naphthalene Derivatives from the Bulbs of Eleutherine americana with Their Protective Effect on the Injury of HUVECs.

Five new naphthalene derivatives, named Eleutherols A⁻C (1⁻3) and Eleuthinones B⁻C (4,5), together with three known compounds were isolated from the bulbs of Eleutherine americana. Their structures were elucidated on the basis of spectroscopic analysis including HR-ESI-MS, 1D and 2D NMR techniques. These compounds exhibited a potent effect against the injury of human umbilical vein endothelial cell (HUVECs) induced by high concentrations of glucose in vitro.

New polyoxypregnane glycosides from Aspidopterys obcordata vines with antitumor activity.

Nine new polyoxypregnane glycosides, obcordatas A-I (1-9), were isolated from Aspidopterys obcordata Hemsl vines. Their structures were elucidated by extensive spectroscopic methods. Separated compounds were evaluated for antitumor activities against the human cancer cell lines AGS, SW480, HuH-7 and MCF-7, and compounds 1-6 and 9 showed selective cytotoxicity against HuH-7 cells with IC50 values of 8.7, 10.2, 7.5, 12.1, 16.5, 14.3, and 17.4 µM, respectively. Flow cytometry experiments showed that the effects of compound 1 on the cell cycle were attributable to cell cycle arrest at G1/S phase.

Cucurbitane-type triterpenes from the tubers of Hemsleya penxianensis and their bioactive activity.

The tubers of the medicinal plant Hemsleya penxianensis (Cucurbitaceae) yielded 11 cucurbitane-type triterpenes Xuedanencins A-K by silica gel column, ODS column, and pre-HPLC techniques. Their structures were determined by spectroscopic analysis and examined alongside existing data from prior studies. Separated compounds were evaluated for cytotoxic activity against the Hela human cancer cell line and compounds 7 and 8 showed significant cytotoxicity with IC50 values at 1.82 and 2.45 µM, respectively.

New Cassane Diterpenoids from Caesalpinia sappan and their Antiplasmodial Activity.

One new cassane diterpene possessing an unusual N bridge between C-19 and C-20 named caesalsappanin R (1), as well as another new diterpene caesalsappanin S (2), were isolated from the seeds of Caesalpinia sappanwith methanol extract. Their structures were determined by spectroscopic analysis and examined alongside existing data from prior studies. Their biological activities were profiled by their antiplasmodial activity.

New cucurbitane triterpenoids with cytotoxic activities from Hemsleya penxianensis.

Seven new cucurbitane triterpenoids, Pengxianencins A-G (1-7) including one alkaloid, were isolated from the ethanol extract of the tubers of Hemsleya penxianensis. Their structures were elucidated on the basis of extensive spectroscopic data, including 1D and 2D NMR spectra as well as HR-ESI-MS. The evaluation of inhibition activity against human Hela, MCF-7, and A-549 cell lines showed that compounds 1, 4, 6, 7 have different levels of cytotoxic activities, with IC50 values ranging from 1.67 to 45.28µM.