草苁蓉中2个单萜苷类化合物的NMR研究

从草苁蓉75%乙醇提取物中分离得到了2个单萜苷类化合物,结合其理化性质,并通过1DNMR(1 H NMR,13 C NMR)及1 H-1 H COSY、HSQC、HMBC、NOESY等多种波谱学方法进行结构鉴定,鉴定2个化合物分别为β-D-glucopyranose 1-(3,7-dimethyl-2-trans-6-octa-dienoate)(化合物1)和6,7-dihydrofoliamenthoic acid diglucoside(化合物2),其中化合物1为新化合物,化合物2为第1次从列当科植物中获得.

Discovery of human pancreatic lipase inhibitors from root of Rhodiola crenulata via integrating bioactivity-guided fractionation,chemical profiling and biochemical assay

Although herbal medicines(HMs)are widely used in the prevention and treatment of obesity and obesity-associated disorders,the key constituents exhibiting anti-obesity activity and their molecular mechanisms are poorly understood.Recently,we assessed the inhibitory potentials of several HMs against human pancreatic lipase(hPL,a key therapeutic target for human obesity),among which the root-extract of Rhodiola crenulata(ERC)showed the most potent anti-hPL activity.In this study,we adopted an integrated strategy,involving bioactivity-guided fractionation techniques,chemical profiling,and biochemical assays,to identify the key anti-hPL constituents in ERC.Nine ERC fractions(retention time=12.5e35 min),obtained using reverse-phase liquid chromatography,showed strong anti-hPL activity,while the major constituents in these bioactive fractions were subsequently identified using liquid chromatography-quadrupole time-of-flight mass spectrometry(LC-Q-TOF-MS/MS).Among the identified ERC constituents,1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose(PGG)and catechin gallate(CG)showed the most potent anti-hPL activity,with pIC50 values of 7.59±0.03 and 7.68±0.23,respectively.Further investigations revealed that PGG and CG potently inhibited hPL in a non-competitive manner,with inhibition constant(Ki)values of 0.012 and 0.082 mM,respectively.Collectively,our integrative analyses enabled us to efficiently identify and characterize the key anti-obesity constituents in ERC,as well as to elucidate their anti-hPL mechanisms.These findings provide convincing evidence in support of the anti-obesity and lipid-lowering properties of ERC.

Pomolic acid and its glucopyranose ester promote apoptosis through autophagy in HT-29 colon cancer cells

BACKGROUND Colon cancer remains a leading cause of death globally.Pomolic acid(PA)can be separated from the ethyl acetate fraction of achyrocline satureioides.AIM To determine the effects of PA and its glucopyranose ester,pomolic acid-28-O-β-D-glucopyranosyl ester(PAO),on colon cancer HT-29 cells.METHODS 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay was used to measure cell viability.Apoptosis was detected via hoechst 33342 staining.PI single staining was identified by flow cytometry to determine the cycle and scratch assay was used to observe the migration of HT-29 cells.The levels of mRNA and proteins were evaluated by q polymerase chain reaction and western blotting,respectively.RESULTS PA and PAO considerably inhibited the growth of the HT-29 cell line in a time and dose-dependent manner.After the administration of PA and PAO for 24 and 48 h,cell apoptosis was significantly promoted and HT-29 cells were arrested in the G0/G1 stage.The Bax/Bcl2 ratio was also increased,which activated cysteinyl aspartate specific proteinase 3,leading to apoptosis;it also increased the expression of light chain 3 II/I and Beclin1,which activated autophagy and caused cell death.This in turn increased the expression of p62 to promote cell apoptosis,inhibiting the levels of signal transducer and activator of transcription 3(STAT3)and p-STAT3,suppressing the level of Bcl2,and promoting cell.CONCLUSION Both PA and PAO provide novel therapeutic strategies for treating colorectal cancer.

Hydrolyzable tannins from Balanophora polyandra

This study reports an investigation of the chemical constituents of Balanophora polyandra Griff.Fifteen compounds were isolated by column chromatography on silica gel,Toyo-pearl HW-40C,Sephadex LH-20 and by HPLC.Their structures were elucidated as 1,4-di-O galloy-2-O-[(E)-p-coumaroyl]-β-D-glucopyranose(1),1-O-galloyl-β-D-pyranglucose(2),1-p-coumaryl-β-D-pyranglu-cose(3),1-O-(E)-caffeoyl-β-D-pyranglucose(4),1,3-di-O-galloyl-β-D-pyranglucose(5),1,6-di-O-galloyl-β-D-pyranglucose(6),1-O-(E)-caffeoyl-4-O-galloyl-β-D-pyranglucose(7),1-O-(E)-caffeoy1-6-O galloyl-β-D-pyranglucose(8),1-0-(E)-caffeoy1-4,6-di-O-galloyl-β-D-pyranglucose(9),1-O-(E)-caffeoyl-4,6-(S)-HHDP-B-D-pyranglucose(10),1,23,6-tetra-O-galloyl-β-D-pyranglucose(11),4,6-(S)-hexahydroxydi-phenoyl-(α/β)-D-glucose(12),1-O-(E)-caffeoyl-4,6-[1′,1″-3′,3″,4′,4″-tetrahydroxydibenzofurandicar-boxyl)]-β-D glucopyranose(13),flavogallonic acid(14),and phloretin-4′-O-β-D-glucoside(15)on the basis of spectral analysis.Compound 1 was a new hydrolyzable tannin,9 was obtained from this genus for the first time,and compounds 5,6 and 11-14 were isolated from this plant for the first time.