Screening the effective components in treating dampness stagnancy due to spleen deficiency syndrome and elucidating the potential mechanism of Poria water extract / 中国天然药物

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.

Equisetin is an anti-obesity candidate through targeting 11β-HSD1

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.

Synthesis and cytotoxicity study of cembrane triazole derivatives / 中国药科大学学报

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.

Content Determination of Oleanolic Acid and Ursolic Acid from Different Medicinal Parts in Tibetan Medi-cine Pterocephalus hookeri by UPLC-PDA / 中国药房

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.

Chemical constituents from root bark of Tripterygium hypoglaucum / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate chemical constituents of the root bark of Tripterygium hypoglaucum.</p><p><b>METHOD</b>Compounds 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).</p><p><b>RESULT</b>Twelve 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).</p><p><b>CONCLUSION</b>Compounds 1, 2, 3, 7 and 10 were isolated from T. hypoglaucum and 7 from the genus Tripterygium for the first time.</p>

Identification method with significant specificity of volatile oil of Pogostemon cablin / 中国中药杂志

<p><b>OBJECTIVE</b>To develop an identification method with significant specificity for patchouli oil.</p><p><b>METHOD</b>The fingerprint was performed by gas chromatography with patchouli alcohol and pogostone as chemical markers.</p><p><b>RESULT</b>The similarity of 12 samples were higher than 0.9 and it can be used to identify the characteristics of patchouli oil.</p><p><b>CONCLUSION</b>The GC fingerprint can be used for identification of patchouli oil.</p>

Studies on chemical constituents from roots of Polygonum amplexicaule / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents in the roots of Polygonum amplexicaule var. sinense.</p><p><b>METHOD</b>The 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.</p><p><b>RESULT</b>Eight 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.</p><p><b>CONCLUSION</b>All compounds were isolated from this species for the first time and compounds 1, 3-6 were obtained from this genus for the first time.</p>

Studies on chemical constituents from leaves of Cassia alata / 中国中药杂志

<p><b>OBJECTIVE</b>To isolate and identify chemical constituents of Cassia alata.</p><p><b>METHOD</b>Compounds 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.</p><p><b>RESULT</b>Twelve 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).</p><p><b>CONCLUSION</b>Compounds 3-12 were isolated from C. alata for the first time.</p>

Studies on chemical constituents of Uvaria tonkinensis var. subglabra / 中国中药杂志

<p><b>OBJECTIVE</b>To isolate and identify chemical constituents of Uvaria tonkinensis var. subglabra.</p><p><b>METHOD</b>The 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.</p><p><b>RESULT</b>Seven 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).</p><p><b>CONCLUSION</b>Compound 1 was the new natural product; compounds 2-7 were isolated for the first time from U. tonkinensis var. subglabra.</p>

A new glycoside from Alpinia officinarum / 药学学报

Aim To investigate the glycosidic constituents in the rhizomes of Alpinia officinarum Hance. Methods The isolation and purification of glycosides were done with column chromatography on macro porous resin, polyamides and Sephadex LH-20, whilst the structure elucidation was done by HRCI-MS and NMR (1D and 2D ) methods. Results A glycosidic ester identified as 4'-hydroxy-2'-methoxyphenol-β-D-{ 6-O-[ 4"-hydroxy-3", 5"-dimethoxy ( benzoate ) ] }-glucopyranoside ( I), along with a known compound n-butyl-β-D-fructopyranoside (II) , were isolated and characterized. Conclusion Ⅰ was found to be a new compound, named as alpinoside A, whilst Ⅱ was isolated from the genus Alpinia for the first time.