丝石竹的化学成分

Eleven compounds were isolated from Gypsophila oldhamiana and identified as octadecyl E-p-coumarate(1),octadecyl caffeate (2), ferulic acid (3), soya-cerebrosideⅠ(4), soya-cerebrosideⅡ(5), D-3-methyl-chiroinsitol (6), α-spinasterol-3-O-β-D-glucopyranoside (7), α-spinasterol(8), β-sitosterol(9),daucosterol (10), sucrose (11). Compounds 1～7 were obtained from this plant for the first time; Compounds 1～3 were isolated from caryophllaceae family for the first time.

A new caffeic ester from Incarvillea mairei var.granditlora (Wehrhahn) Grierson

A new cafferic ester, （＋）-2-（1-hydroxyl-4-oxocyclohexyl） ethyl caffeate, was isolated from the 80% ethanol extract of the whole plants of Incarvillea mairei var. granditlora （Wehrhahn） Grierson. The structure of the compound was established by spectroscopic methods.

Effect of Farnesyl Caffeate-Induced Apoptosis of Lung Carcinoma Cell Line from Damage to DNA

Farnesyl caffeate, synthesis of propolis and polar bud excretion, has been reported to exhibit anti-allergic effects in mice. However, little is known about anti-tumor effects. In this study, we investigated the effect of Farnesyl caffeate in cell proliferation of lung carcinoma cell line (H157). Antiproliferative effect and apoptosis on H157 cell were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay (MTT) and DNA fragmentation assay, respectively. Farnesyl caffeate inhibited the growth of H157 cell in dose-dependent manner. Morphological changes of nuclei by staining Hoechst 33258 and DNA fragmentation suggested that Farnesyl caffeate induced death involved in a mechanism of apoptosis. Moreover, caspase-3, caspase-7 and caspase-9 were activated by Farnesyl caffeate on H157 cell. The protein expressions of Bax and Bcl-2 were down-regulated by Farnesyl caffeate, resulting in cytochrome c release from the mitochondria. Farnesyl caffeate significantly increased the expression of p53 proteins which indicates that p53 plays a pivotal role in the initiation phase of Farnesyl caffeate-induced HepG2 cell apoptosis. These results demonstrated Farnesyl caffeate-induced apoptosis in human lung carcinoma cell line. More detailed mechanism of ?Farnesyl caffeate-induced H157 apoptosis remains to be elucidated.

Selection of quality markers of Jasminum amplexicaule based on its anti-diarrheal and anti-inflammatory activities: Effect-target affiliation-traceability-pharmacokinetics strategy

Objective:To investigate therapeutic mechanism in Jasminum amplexicaule(Oleaceae)and verify its main active component as quality control markers Methods:Established mouse models of diarrhea,intestinal angina,and inflammation were firstly used to select herb fractions with optimum efficacy,followed by an in vitro experiment to determine key targets associated with effects of J.amplexicaule extract.The selected fractions were isolated and purified,its components were identified,and the obtained compounds were verified for their effects on NF-κB and i NOS.Finally,effective compounds were administered to rats,their plasma pharmacokinetic parameters were calculated,and quality markers(QMs)reflecting therapeutic activities of J.amplexicaule were confirmed.Results:Trichloromethane and ethyl acetate fractions had significant anti-diarrheal,anti-inflammatory,and analgesic effects.The trichloromethane fraction also reduced BDNF,p38 MAPK,p-p38 MAPK,NF-κB p65,and p-NF-κB p65 levels in the ileum in a rhubarb-induced diarrhea mouse model.Additionally,it inhibited LPS-induced NF-κB transcription and nitric oxide(NO)production in RAW264.7 macrophages,which suppressed i NOS expression.Therefore,the trichloromethane fraction was further investigated.QMs candidate selection identified 17 compounds,and results of in-vitro therapeutic validation indicated that methyl caffeate and isochlorogenic acid B had the strongest anti-diarrheal,anti-inflammatory,and analgesic activities.After being validated by a UHPLC–MS-MS method,concentrations of these target compounds were accurately determined in the rat plasma and pharmacokinetic parameters were calculated.Cmax,tmax,and t1/2 were respectively 575.35 ng/mL(2.963 nmol/mL),0.5 h,and 0.45 h for methyl caffeate and 262.03 ng/m L(0.5034 nmol/mL),0.25 h,and 2.03 h for isochlorogenic acid B.Because these candidate compounds exhibited favorable pharmacokinetics,they were considered as QMs of J.amplexicaule.Conclusions:The present study accurately and effectively identified QMs of J.amplexicaule that act as indicators of efficacy and quality.

An ROS-Responsive Antioxidative Macromolecular Prodrug of Caffeate for Uveitis Treatment

Uveitis is a sophisticated syndrome showing a high relevance with reactive oxygen species(ROS).Herein,an ROS-responsive PEGylated polypeptide based macromolecular prodrug of herbaceous antioxidant ethyl caffeate(EC)is designed via phenylboronic esters with improved solubility for the alleviation of uveitis.The antioxidative 4-hydroxybenzyl alcohol(HBA)and EC can be released from the macromolecular EC prodrug under the stimulation of ROS,which can effectively protect cells against oxidative stress-induced injury in an ROS-depletion way.The antioxidative and protective effects of the macromolecular EC prodrug in vivo are further verified in a uveitis mouse model.Overall,this work not only provides a handy method to synthesize a phenylboronic ester-bearing EC prodrug which is highly sensitive to pathological ROS,but also depicts a promising future to apply macromolecular antioxidative prodrugs in the treatment of uveitis as well as other ROS-related diseases.