查看更多>>摘要：Liver fibrosis is a dynamic and highly integrated pathological process resulting from repeated liver injury healing accompanied by inflammation and extracellular matrix deposition. Treatment is necessary at the early stage of reversible liver fibrosis to prevent further deterioration to liver cirrhosis and liver cancer. Currently, the inhi-bition of liver fibrosis are mainly focused on prevention the activation of hepatic stellate cells and inhibition of inflammatory pathways involved in liver fibrosis. Previous research in our lab found that natural phenanthrenes derived from Traditional Chinese Medicine Baiyangjie could inhibit liver fibrosis through inhibiting TGF-131, TNF-alpha and promoting the secretion of MMP-9. Herein, in order to optimize the structure of phenanthrenes to maximize their anti-fibrosis activities, a series of phenanthrene derivatives were designed and synthesized in an expeditious manner. Their ability to inhibit LPS-initiated cellular liver fibrosis in HSC-T6 cells were examined and the results indicated that compounds A-1 and B-1 provided the best cellular anti-fibrosis activities. Further studies implied that they inhibited the LPS-initiated cellular liver fibrosis through inhibition the secretion of TNF-alpha, IL-113, TGF-131 and alpha-SMA. From these data, a picture emerges wherein a novel idea using phenanthrenes A-1 and B-1 as potential candidates to treat liver fibrosis for further animal studies.
查看更多>>摘要：Fifteen diterpene derivatives including seven new ones, sinensisins A-G (1, 2, 4, 7, 10, 14, 15), were obtained from the leaves and twigs of Aphanamixis sinensis. Their structures were elucidated by NMR spectroscopic and ECD data analyses. These diverse carbon skeletons containing meroditerpenoids, acyclic diterpenes, and norditerpenoids biogenetically were derived from chain-like diterpenes. Compounds 3, 5, and 6 showed inhibitory effects of nitric oxide (NO) production in LPS-induced RAW 264.7 cells.
查看更多>>摘要：Seven new phenolic acids, 7, 8-epiblechnic acid (1), 8-epiblechnic acid 9-ehthyl-9 & PRIME;-methyl ester (2), 9 & PRIME;-ehyl-isolithospermate (3), 9 & DPRIME;-methyl-isolithospermate (4), 9 & PRIME;-ethyl-9 & DPRIME;-methyl-isolithospermate (5), 9 & PRIME;, 9 & DPRIME;-dimethyl-isolithospermate (6), sebesteniod E (7), were isolated from the roots of Salvia miltiorrhiza. Their structures were elucidated by detailed spectroscopic means including UV, IR, HRESIMS, and NMR data spectra. The bioactive assays of compounds 1-7 against neuroprotection activities were determined. The results suggested that compound 4 exhibited a moderate glutamate-induced neuroprotective activity and the cell survival rate was 24.0% (10-5 mol/L), while compound 2 showed weak activity (survival rate: 7.58%, 10-5 mol/L), using PHPB (survival rate: 7.56%, 10-5 mol/L) as positive control.
查看更多>>摘要：Seven new 2-(2-Phenethyl) chromone derivatives (1-7), including four 2-(2-Phenethyl) chromones (1-4), one 6, 7, 8 trihydroxy-2-(2-Phenethyl) chromone (5), one acetylated 5, 6, 7, 8-tetrahydroxy-2-(2-Phenethyl) chromone (6), and one chlorine-containing 5, 6, 7, 8-tetrahydro-2-(2-Phenethyl) chromone (7), along with eight known compounds (8-15), were isolated from agarwood originating from Aquilaria agallocha Roxb.. Their structures were determined mainly by high-resolution electrospray ionization mass spectrometry (HR-ESI-MS) and nuclear magnetic resonance (NMR) analysis. The absolute configurations of 3-7 were resolved by electronic circular dichroism (ECD) calculations. Nearly all compounds were evaluated for their anti-inflammatory activities in RAW264.7 cells. Compounds 1 and 7-11 displayed significant anti-inflammatory activities with IC50 values ranging from 3.71 to 32.04 mu M.
查看更多>>摘要：Three new triterpenoid saponins, heracleifolianosides A-C (1-3), together with seven known compounds (4-10), were isolated from the whole plants of Clematis heracleifolia. Moreover, three new secondary saponins (1a, 2a and 3a), two known secondary metabolites (5a and 7a) were obtained by alkaline hydrolysis. Their structures were elucidated by extensive spectroscopic analysis and chemical evidences. The cytotoxicity of eight native saponins and five prosapogenins against human breast tumor MDA-MB-231 and gastric carcinoma SGC-7901 cell lines were evaluated by MTT method. Remarkably, the prosapogenin monodesmosidic saponin 7a showed significant cytotoxicity against MDA-MB-231 or SGC-7901 cell lines with IC50 values in the range of 6.05-6.32 mu mol/L. It is suggested that it might be a feasible way to change the inactive bisdesmosic triterpenoid saponins to active monodesmosic saponins by a simple procedure of alkaline hydrolysis.
查看更多>>摘要：Wilsonglucinols H-K (1-4), four new polycyclic polyprenylated acylphloroglucinols (PPAPs), and eight known compounds (5-12) were isolated and identified from the aerial parts of Hypericum wilsonii. Their planner structures were confirmed via extensive NMR and HRESIMS data analysis. The absolute configurations of the new compounds were mainly determined by NMR calculation and electronic circular dichroism (ECD) calcula-tion. Compounds 1, 6, 8, and 10 showed glucose uptake activities at 30 mu g/mL, in which compound 6 showed the strongest effect and increased the glucose uptake by 2.73 folds.
Gehm, Adriana Z.Cunha, Sabrina B.Silva, Bruce W. daMostardeiro, Marco A....
7页
查看更多>>摘要：During the course of a study of Condalia buxifolia (Rhamnaceae), one new cyclopeptide alkaloid condaline B (1), together with six known cyclopeptide alkaloids, condaline A (2), and the scutianines B (3), - D (4) and -E (5), frangulanine (6), and 3,4,28-tris-epi-scutianene N (7), were isolated from the rind bark of Condalia buxifolia. Their structures have been confirmed through spectroscopic analyses such as 1D and 2D NMR experiments. The absolute stereochemistry of condaline A (2), was elucidated by X-ray crystal structure determination of its HI salt. In addition, condaline B (1) was obtained synthetically through a structural transformation of condaline A. Meanwhile, the crude methanol extract, the basic ether fraction, and alkaloids 1-7 were tested against various strains of Gram-positive and Gram-negative bacteria and fungus, showing promising antimicrobial activity
查看更多>>摘要：Four unknown meroterpenoids named as psidials D-G (1-4) together with 5 known compounds (5-9) had been obtained from the leaves of Psidium guajava. Their absolute structures were elucidated by spectral and calculated methods. Psidials D-F (1-3) represented unknown carbon skeleton of the 3,5-diformylbenzyl phloroglucinolcoupled sesquiterpenoid. The possible biosynthetic pathway for 1-3 was postulated. In the bioactivity assay, psidial F (3) was found to possess anti-inflammatory and anticoagulant activities.
NSTL
Elsevier