•Nineteen lanostane nor-triterpenoids have been obtained from the fungus Ganoderma lucidum.•Five new nor-triterpenoids have been determined.•C27-nor triterpenoids displayed moderate inhibitory effects against AChE.•Docking analysis was performed to investigate the inhibition mechanism.The lanostane nor-triterpenoids (ganoderic acids) of the functional food and folk medicine Ganoderma lucidum have been investigated by chromatographic techniques and spectroscopic data analysis. Nineteen nor-ganoderic acid analogues were obtained and identified, yielding five new lanostane analogues (1–4 and 11). All of the triterpenoids were systemically evaluated for their inhibitory effects against AChE (acetylcholinesterase) in vitro. Triterpenoid 16 was the most potent compound with the IC50 value of 54.5 μM. The docking analysis has been performed to reveal the interaction between ganoderic acid 16 and AChE for developing the new inhibitors of AChE.Download high-res image (118KB)Download full-size image

The bioactive substance investigation of Euphorbia ebracteolata obtained 17 compounds by various chromatographic techniques. Their structures were elucidated using widely spectroscopic data, including ESI-MS, HRESI-MS, CD, 1D- and 2D-NMR, which gave 5 new phenolic glucosides and 4 new monoterpenoids. The phenolic glucosides and monoterpenoids showed the inhibitory effect against the human carboxylesterase-2 (hCE-2) using a fluorescence bioassay in vitro, with the strongest inhibitor compound 4 (IC50 7.17 μM). The antioxidant effects of these isolated compounds were evaluated using a DPPH scavenging assay. All of the phenolic acids displayed the DPPH scavenging effect, especially that eight compounds have better effect than vitamin C, with the IC50 values ranging from 4.52 to 7.52 μM. Additionally, compounds 1–17 showed no cytotoxic effect against five human cancer cell lines by MTT assay.Download high-res image (89KB)Download full-size image

The bioactive substance investigation of Balanophora involucrata obtained 15 phenolic acids, including 5 new compounds (1–3, 8, 9), which were determined by various spectroscopic data analyses. Most isolated compounds displayed inhibitory effects on α-Glucosidase in vitro. For the potential inhibitors 8 (1.95 μM) and 10 (9.02 μM), the inhibition kinetics have been studied, which gave the Ki values as 0.68, 3.15 μM respectively. And, in silico docking analyses have been performed to investigate the inhibitory mechanism of compounds 8 and 10. Additionally, most isolated compounds showed anti-oxidant activities in the DPPH scavenging assay. New compound 8 also could inhibit the acetyl transfer activity of GlmU moderately with the IC50 value of 18.21 μM, which was a new antibacterial target.Download high-res image (105KB)Download full-size image

Quercetin (QT) is a natural flavonoid with various biological activities and pharmacological actions. However, the bioavailability of QT is relatively low due to its low solubility which severely limits its use. In this study, we intended to improve the bioavailability of QT by preparing quercetin-phospholipid complex (QT-PC) and investigate the protective effect of QT-PC against carbon tetrachloride (CCl4) induced acute liver damage in Sprague-Dawley (SD) rats. The physicochemical properties of QT-PC were characterized in terms of infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (XRPD) and water/n-octanol solubility. FTIR, DSC and XRPD data confirmed the formation of QT-PC. The water solubility of QT was improved significantly in the prepared complex, indicating its increased hydrophilicity. Oral bioavailability of QT and QT-PC was evaluated in SD rats, and the plasma QT was estimated by HPLC-MS. QT-PC exhibited higher Cmax (1.58 ± 0.11 vs. 0.67 ± 0.08 μg/mL), increased AUC0–∞ (8.60 ± 1.25 vs. 2.41 ± 0.51 mg/L h) and t1/2z (7.76 ± 1.09 vs. 4.81 ± 0.87 h) when compared to free QT. The greater absorption of QT-PC group suggested the improved bioavailability. Moreover, biochemical changes and histopathological observations revealed that QT-PC provided better protection to rat liver than free QT at the same dose. Thus, phospholipid complexation might be one of the suitable approaches to improve the oral bioavailability of QT and obtain better protective effects against CCl4 induced acute liver damage in SD rats than free QT at the same dose level.Download high-res image (163KB)Download full-size image

A new steroidal saponin, furotrilliumoside (FT) was isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Its structure was elucidated on the basis of 1D- and 2D-NMR spectroscopic data as well as HR-ESI-MS analysis. FT showed superior activity of inhibiting NO production of RAW264.7 cells induced by lipopolysaccharide (LPS) in the preliminary biological screening. In order to develop novel therapeutic drug for acute and chronic inflammatory disorders, the anti-inflammatory activity and underlying mechanism of FT were investigated in LPS-induced RAW264.7 cells. The results showed that FT could reduce LPS-induced expression of inducible nitric oxide synthase (iNOS) and then resulted in the decrement of NO production. More meaningful, FT could down-regulate the expression of cyclooxygenase-2 (COX-2) and decrease the expressions of pro-inflammatory cytokines, tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) and interleukin-1β (IL-1β), in both gene and protein levels. In mechanism study, FT blocked the LPS-induced upregulation of phosphorylated phosphoinositide-3-kinase and Akt (PI3K/Akt). Furthermore, FT inhibited the translocation of nuclear factor-kappa B (NF-κB) through the prevention of inhibitory factor kappa B alpha (IκBα) phosphorylation and degradation and also suppressed the mitogen-activated protein kinases (MAPK) signaling pathway in LPS-stimulated RAW264.7 macrophages. In addition, FT upregulated heme oxygenase-1 (HO-1) expression via nuclear translocation of nuclear factor E2-related factor 2 (Nrf2). Taken together, FT might act as a natural agent to treat some inflammatory diseases by targeting PI3K/Akt, MARK and Nrf2/HO-1 pathways.Download high-res image (113KB)Download full-size image

The total flavonoids from Persimmon leaves (PLF), extracted from the leaves of Diospyros kaki L. Dispryosl and Ebenaceae, is reported to possess many beneficial health effects. However, the oral bioavailability of PLF is relatively low due to its poor solubility. In the present study, the phospholipid complexes of total flavonoids from Persimmon leaves (PLF-PC) was prepared to enhance the oral bioavailability of PLF and to evaluate its antiatherosclerotic properties in atherosclerosis rats in comparison to PLF. A HPLC-MS method was developed and validated for the determination of quercetin and kaempferol in rats plasma to assess the oral bioavailability of PLF-PC. The effect of PLF (50 mg/kg/d) and PLF-PC (equivalent to PLF 50 mg/kg/d) on atherosclerosis rats induced by excessive administration of vitamin D (600,000 IU/kg) and cholesterol (0.5 g/kg/d) was assessed after orally administered for 4 weeks. The relative bioavailabilities of quercetin and kaempferol in PLF-PC relative to PLF were 242% and 337%, respectively. The levels of total cholesterol (TC), triglyceride (TG), low-density lipoprotein-cholesterol (LDL-C), high-density lipoprotein-cholesterol (HDL-C), apolipoprotein A1 (ApoA1) and apolipoprotein B (ApoB) in serum were measured by an automatic biochemistry analyzer. The morphological changes of aorta were observed with optical microscopy. According to the levels of biochemical parameters in serum and the morphological changes of aorta, PLF-PC showed better therapeutic efficacy compared to PLF. Thus, PLF-PC holds a promising potential for increasing the oral bioavailability of PLF. Moreover, PLF-PC exerts better therapeutic potential in the treatment of atherosclerotic disease than PLF.Download high-res image (138KB)Download full-size image