ObjectiveTo study the chemical constituents of Bidens pilosa and the in vitro antiproliferative activity of some compounds against gastric cancer cells. MethodsThe chemical constituents were isolated and purified by methods such as silica gel column chromatography， preparative thin layer chromatography， medium pressure preparation chromatography， semi-preparative high performance liquid chromatography（HPLC） and recrystallization， their structures were identified on the basis of physicochemical properties， spectral data and circular dichroism spectra. Thiazole blue（MTT） assay was used to determine the in vitro inhibitory activityies of some isolated compounds against human gastric cancer SGC-7901 cells， and molecular docking was used to predict their potential targets. ResultsTwenty-five compounds were isolated from the petroleum ether fraction of B. pilosa and identified as bidpillignan A（1）， 5α， 8α-epidioxy-（22E， 24R）-ergosta-6， 22-diene-3β-ol（2）， 3β-hydroxysitost-5-en-7-one（3）， （20R）-6β-hydroxystigmasta-4， 22-dien-3-one（4）， 3β-hydroxylstigmasta-5， 22-dien-7-one（5）， （22E， 24S）-24-methyl-5α-choleata-7， 22-diene-3β， 5α， 6β-triol（6）， stigamast-5-ene-3β， 7α-diol（7）， stigmast-5， 22-diene-3β， 7α-diol（8）， 7β-hydroxysitosterol（9）， stigmasterol（10）， artabotrol（11）， cosmosoic acid（12）， ent-4（15）-eudesmene-1β， 6α-diol（13）， clovandiol（14）， 1H-indole-3-carboxaldehyde（15）， 6， 7-dimethoxycoumarin（16）， 3'， 4'-dimethoxyquercetin（17）， 8， 8'-bis-（dihydroconiferyl）-diferuloylate（18）， hydroxydihydrobovolide（19）， 2-deacetyl-11β， 13-dihydroxyxanthinin（20）， loliolide（21）， pubescone（22）， （+）-dehydrovomifoliol（23）， 2， 3-dihydroxypropyl palmitate（24） and n-hexadecane acid（25）. Among them， compound 1 was a new compound， compounds 3-9， 11-12， 18-20， 22-23 were first isolated from Bidens genus plants， and compounds 13 and 14 were isolated from this plant for the first time. Compounds 17 and 18 showed good in vitro proliferation inhibitory activities against SGC-7901 cells with the half inhibitory concentrations（IC₅₀） of 3.11， 7.22 μmol·L^-1， respectively. Molecular docking results showed that the potential targets of the two exerting anti-gastric cancer activity might be vascular endothelial growth factor receptor 2（VEGFR2） and poly（adenosine diphosphate-ribose） polymerase 7（PARP7）. ConclusionOne new compound， 14 genus first compounds， and 2 species first compounds were isolated from B. pilosa， among which compounds 17 and 18 processed anti-gastric cancer cell proliferation activity in vitro， and the targets may be VEGFR2 and PARP7.

Poria is an important medicine for inducing diuresis to drain dampness from the middle energizer. However, the specific effective components and the potential mechanism of Poria remain largely unknown. To identify the effective components and the mechanism of Poria water extract (PWE) to treat dampness stagnancy due to spleen deficiency syndrome (DSSD), a rat model of DSSD was established through weight-loaded forced swimming, intragastric ice-water stimulation, humid living environment, and alternate-day fasting for 21 days. After 14 days of treatment with PWE, the results indicated that PWE increased fecal moisture percentage, urine output, D-xylose level and weight; amylase, albumin, and total protein levels; and the swimming time of rats with DSSD to different extents. Eleven highly related components were screened out using the spectrum-effect relationship and LC-MS. Mechanistic studies revealed that PWE significantly increased the expression of serum motilin (MTL), gastrin (GAS), ADCY5/6, p-PKAα/β/γ cat, and phosphorylated cAMP-response element binding protein in the stomach, and AQP3 expression in the colon. Moreover, it decreased the levels of serum ADH, the expression of AQP3 and AQP4 in the stomach, AQP1 and AQP3 in the duodenum, and AQP4 in the colon. PWE induced diuresis to drain dampness in rats with DSSD. Eleven main effective components were identified in PWE. They exerted therapeutic effect by regulating the AC-cAMP-AQP signaling pathway in the stomach, MTL and GAS levels in the serum, AQP1 and AQP3 expression in the duodenum, and AQP3 and AQP4 expression in the colon.
Animals ; Rats ; Poria ; Spleen ; Albumins ; Chromatography, Liquid ; Cyclic AMP Response Element-Binding Protein

Obesity is increasingly prevalent globally, searching for therapeutic agents acting on adipose tissue is of great importance. Equisetin (EQST), a meroterpenoid isolated from a marine sponge-derived fungus, has been reported to display antibacterial and antiviral activities. Here, we revealed that EQST displayed anti-obesity effects acting on adipose tissue through inhibiting adipogenesis in vitro and attenuating HFD-induced obesity in mice, doing so without affecting food intake, blood pressure or heart rate. We demonstrated that EQST inhibited the enzyme activity of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), a therapeutic target of obesity in adipose tissue. Anti-obesity properties of EQST were all offset by applying excessive 11β-HSD1's substrates and 11β-HSD1 inhibition through knockdown in vitro or 11β-HSD1 knockout in vivo. In the 11β-HSD1 bypass model constructed by adding excess 11β-HSD1 products, EQST's anti-obesity effects disappeared. Furthermore, EQST directly bond to 11β-HSD1 protein and presented remarkable better intensity on 11β-HSD1 inhibition and better efficacy on anti-obesity than known 11β-HSD1 inhibitor. Therefore, EQST can be developed into anti-obesity candidate compound, and this study may provide more clues for developing higher effective 11β-HSD1 inhibitors.

A series of triazole derivatives were designed and synthesized based on a natural product cembrane separated from Croton laevigatus Vahl which showed potential antitumor activity against HeLa cells.Twelve novel compounds were synthesized and their structures were characterized by 1H NMR, 13C NMR and HRMS.Their cytotoxicities in vitro were evaluated for HeLa,K562 and K562/A02 cells by MTT assay.The results showed that some cembrane derivatives possessed antitumor activities.Substituted triazole connected to cembrane derivatives exhibited potent activity toward drug-resistant K562/A02 cells.

OBJECTIVE:To establish the method for the determination of oleanolic acid and ursolic acid in different medicinal parts of Tibetan medicine Pteocephalus hookeri,and compare the differences among the different parts. METHODS:The contents of oleanolic acid and ursolic acid from different medicinal parts(whole plant,aerial part,underground part)of P. hookeri were de-termined by UPLC-PDA. The separation was performed on Acquity UPLC HSS T3 column(150 mm×2.1 mm,1.8 μm)with mobile phase consisted of methanol-0.1 mol/L ammonium acetate(88:12,V/V)at the flow rate of 0.2 mL/min. The detection wavelength was set at 210 nm,and column temperature was 30 ℃. The sample size was 5 μL. RESULTS:The linear ranges of oleanolic acid and ursolic acid were 10.65-1065 μg/mL (r=0.9996) and 18.8-1880 μg/mL (r=0.9994),separately. The recoveries were 96.95%(RSD=1.24%,n=9) and 98.12%(RSD=2.13%,n=9),separately. RSDs of precision,stability and reproducibility tests were all less than 3%. The contents of oleanolic acid and ursolic acid from different medicinal parts in P. hookeri were in de-scending order of aerial part>whole plant>underground part;the average total content of oleanolic acid and ursolic acid from whole plants was 0.35%,the aerial part reached 0.56% and underground part was 0.09%. CONCLUSIONS:The method is rapid, accurate and reproducible,and it is suitable for the content determination of oleanolic acid and ursolic acid in different medicinal parts of Tibetan medicine P. hookeri. The contents of oleanolic acid and ursolic acid from aerial part of P. hookeri are higher than whole plant and underground part. It is suggested to use aerial parts of medicine.

OBJECTIVETo investigate chemical constituents of the root bark of Tripterygium hypoglaucum.

METHODCompounds were isolated by column chromatography on silica gel and Sephadex LH-20, and their structures were identified on the basis of spectral data (MS, 1H-NMR and 13C-NMR).

RESULTTwelve compounds were isolated and identified as friedelin (1), 3-oxo-olean-9(11),12-diene (2), canophyllal (3), 3-acetoxy oleanolic acid (4), triptophenolide (5), triptonoterpene methyl ether (6), tricosanoic acid (7), beta-sitosterol (8), stearic acid (9), glut-5-en-3beta,28-diol (10), palmitic acid (11) and daucostorol (12).

CONCLUSIONCompounds 1, 2, 3, 7 and 10 were isolated from T. hypoglaucum and 7 from the genus Tripterygium for the first time.

Chromatography ; methods ; Diterpenes ; chemistry ; isolation & purification ; Fatty Acids, Unsaturated ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; methods ; Mass Spectrometry ; methods ; Oleanolic Acid ; chemistry ; isolation & purification ; Organic Chemicals ; chemistry ; isolation & purification ; Palmitic Acid ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; metabolism ; Sitosterols ; chemistry ; isolation & purification ; Stearic Acids ; chemistry ; isolation & purification ; Tripterygium ; chemistry ; metabolism ; Triterpenes ; analysis ; chemistry ; isolation & purification

OBJECTIVETo develop an identification method with significant specificity for patchouli oil.

METHODThe fingerprint was performed by gas chromatography with patchouli alcohol and pogostone as chemical markers.

RESULTThe similarity of 12 samples were higher than 0.9 and it can be used to identify the characteristics of patchouli oil.

CONCLUSIONThe GC fingerprint can be used for identification of patchouli oil.

Chromatography, Gas ; methods ; Lamiaceae ; chemistry ; Oils, Volatile ; analysis ; Plant Oils ; analysis ; Sesquiterpenes ; analysis

OBJECTIVETo investigate the chemical constituents in the roots of Polygonum amplexicaule var. sinense.

METHODThe compounds were isolated by column chromatography on silica gel and Sephadex LH-20. The structures were identified by means of IR, 1H-NMR, 13C-NMR and MS analyses.

RESULTEight compounds were isolated and identified as friedelin (1), beta-sitosterol (2), simiarenone (3), angelicin (4), psoralen (5), palmitic acid (6), (-)-epicatechin (7), and quercetin (8), respectively.

CONCLUSIONAll compounds were isolated from this species for the first time and compounds 1, 3-6 were obtained from this genus for the first time.

Magnetic Resonance Spectroscopy ; Mass Spectrometry ; Organic Chemicals ; analysis ; isolation & purification ; Plant Roots ; chemistry ; Polygonum ; chemistry

OBJECTIVETo isolate and identify chemical constituents of Cassia alata.

METHODCompounds were separated and purified by column chromatography with silica gel and Sephadex LH-20, elucidated by spectroscopic methods including 1D and 2D NMR, IR and MS techniques.

RESULTTwelve compounds were isolated from C. alata, which were identified as chrysoeriol (1), kaempferol (2), quercetin (3), 5,7,4'-trihydroflavanone (4), kaempferol-3-O-beta-D-glucopyranoside (5), kaempferol-3-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranoside (6), 17-hydrotetratriacontane (7), n-dotriacontanol (8), n-triacontanol (9), palmitic acid ceryl ester (10), stearic acid (11), palmitic acid (12).

CONCLUSIONCompounds 3-12 were isolated from C. alata for the first time.

Cassia ; chemistry ; Organic Chemicals ; analysis ; chemistry ; isolation & purification ; Plant Leaves ; chemistry

OBJECTIVETo isolate and identify chemical constituents of Uvaria tonkinensis var. subglabra.

METHODThe column chromatographic techniques were applied to isolate constituents, and their structures were elucidated by means of spectral data analysis including 1D and 2D NMR, IR and MS techniques.

RESULTSeven compounds were isolated and identified as subglain C (1), beta-senepoxide (2) , 2, 4-dioxohexahydro-1, 3-diazepin (3), kaempferol-3, 7-di-O-alpha-L-rhamnoside (4), anolobine (5), (-)-lyoniresinol (6) and schizandriside (7).

CONCLUSIONCompound 1 was the new natural product; compounds 2-7 were isolated for the first time from U. tonkinensis var. subglabra.

Chromatography ; Drugs, Chinese Herbal ; chemistry ; Mass Spectrometry ; Nuclear Magnetic Resonance, Biomolecular ; Uvaria ; chemistry