Research progress and consideration of polymeric prodrugs / 中国药科大学学报

@#Currently the available therapies cannot satisfy all the clinical requirements, therefore advanced technologies are urgently demanded. Delivery system the polymeric prodrug based has both advantages of prodrug strategy and nanoparticle drug delivery strategy. The system can improve the drug bioavailability, enhance the drug stability, and make the drug targeting system more effective. The system can reduce the side effects and improve the therapeutic effect of drug. According to the mechanism of this drug system, passive targeting, active targeting, triggered release and co-administration were reviewed. Finally, the research prospects and issues in this field were pointed out.

Simultaneous Determination of 6 Flavonoids in the Roots of Tetrastigma hemsleyanum by HPLC / 中国药房

OBJECTIVE： To establish a method for simultaneous determination of rutin， isoquercitrin， kaempferol-3-O- rutinoside， daunorubicin， quercetin and kaempferol in the roots of Tetrastigma hemsleyanum.  METHODS： HPLC method was adopted. The determination was performed on Alliance SilGreen C18 column with mobile phase consisted of 0.2％ phosphoric acid solution-acetonitrile solution （gradient elution） at the flow rate of 1.0 mL/min. The detection wavelength was 360 nm and the column temperature was at 35 ℃. The sample size was 15 μL. RESULTS： The linear range of rutin， isoquercitrin， kaempferol-3- O-rutinoside， daunorubicin， quercetin and kaempferol were 21.77-217.77， 12.37-123.75， 13.23-132.31， 4.63-46.30， 5.75-57.50， 3.36-33.66 μg/mL （all r＝0.999 9）， respectively. limit of detection of them were 0.217 8， 0.123 8， 0.066 2， 0.046 3， 0.191 7， 0.112 3 μg/mL， respectively. limit of quantitation of them were 0.435 6， 0.247 5， 0.165 4， 0.154 3， 0.575 0， 0.421 2 μg/mL， respectively. RSDs of precision （n＝6）， stability （24 h， n＝7） and reproducibility tests （n＝6） were lower than 3.20％. The average recoveries of them were 96.23％， 86.88％， 97.51％， 97.67％， 97.50％， 87.46％， RSDs were 1.85％， 1.90％， 1.84％， 1.87％， 1.25％， 2.01％ （n＝9）， respectively. CONCLUSIONS： The method is fast and simple， and could be applied for simultaneous determination of rutin， isoquercitrin， kaempferol-3-O-rutinoside， daunorubicin， quercetin and kaempferol in the roots of T. hemsleyanum.  

Effects of kirenol on bovine type II collagen-induced rat lymphocytes in vivo and in vitro / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the effect of kirenol on bovine type II collagen (CII)-specific lymphocytes in vivo and in vitro, and explore the mechanism of kirenol-induced immunosuppression in antigen-specific lymphocytes.</p><p><b>METHODS</b>Twenty-four Wistar rats were randomized into control group, collagen-induced arthritis (CIA) model group, kirenol group (2 mg/kg), and prednisolone group (2 mg/kg). After CII injection, the rats in the latter two groups received intragastric administration of kirenol and prednisolone for 30 days, and the spleens and draining lymph nodes of the rats were harvested to prepare single cell suspensions for measurement of the cytokine levels using ELISA. In the in vitro experiment, the lymphocytes from the control rats, with or without 20 µg/ml CII treatment in the presence of 0-80 µg/ml kirenol, were evaluated for cell proliferation and apoptosis using [(3)H]-thymidine incorporation and flow cytometry, respectively.</p><p><b>RESULTS</b>Compared with those in CIA group, IFN-γ and TNF-α production was significantly reduced in splenocyte culture supernatant of kirenol group (P<0.05 and P<0.01, respectively), and the level of IL-10 and IL-4 was up-regulated (P<0.05 and P<0.01, respectively); IFN-γ and TNF-α secretion by the cultured lymph node cells (LNCs) significantly decreased (P<0.05 and P<0.001, respectively) and IL-10 and IL-4 production increased (P<0.05, P<0.001) in kirenol group. In the in vitro experiment, kirenol treatment caused obvious suppression of CII-induced LNC proliferation and dose-dependently induced antigen-specific apoptosis of the splenocytes and LNCs.</p><p><b>CONCLUSION</b>Kirenol treatment reduces pro-inflammatory cytokine secretion, increases anti-inflammatory cytokine production, inhibits cell proliferation and induces apoptosis of CII-specific lymphocytes in vitro, suggesting the potential of kirenol as an immunosuppressant.</p>

A New Cyano-compound from Rhodiola kirilowii / 中草药·英文版

Objective To study the chemical constituents of Rhodiola kirilowii.Methods The compounds were separated and purified by various chromatographic techniques and their structures were elucidated on the basis of physicochemical properties and spectroscopic methods.Results Five compounds were purified and their structures were identified as 4-(β-D-glucopyranosyloxy)-3-hydroxy-2-(hydroxymethyl)-butanenitrfle (1),epicatechin (2),arbutin (3),rutin (4),and β-D-glucose (5).Conclusion Compound 1 is a new cyano-compound and other compounds are isolated from the plant for the first time.

Studies on chemical constituents of Rabdosia serra / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of aerial part of Rabdosia serra.</p><p><b>METHOD</b>The compounds were isolated by extraction, coloum chromatography over silica gel and ODS, and preparative HPLC. Their structures were identified by various spectroscopic methods including MS, IR, 1D and 2D NMR data.</p><p><b>RESULT</b>Six compounds were isolated from R. serra and were characterized as ent-1alpha, 7alpha, 14beta, 20-tetrahydroxy-11, 16-kauradien-15-one (1), kamebakaurin (2), dihydrokamebakaurin (3), rabdoinflexin A (4), daucosterol( 5), and beta-sitosterol (6).</p><p><b>CONCLUSION</b>Compound 1 is a new compound, and coumpound 3 was obtained from this plant for the first time.</p>

Steroidal alkaloids of from Veratrum dahuricum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the steroidal alkaloids in Veratrum dahuricum.</p><p><b>METHOD</b>The compounds were isolated and purified by various column chromatographic methods. Their structures were identified by spectroscopic analysis.</p><p><b>RESULT</b>Five compounds were isolated and identified as (20R, 22S, 25S)-veratra-5,13-dien-3beta-ol (1), angeloylzygadenine (2), 15-O-(2-methylbutanoyl)-3-O-veatroylprotoverine (3), 20-isoveratramine (4), veratramine (5).</p><p><b>CONCLUSION</b>Compound 1 was a new compound, compounds 24 were obtained from the plant for the first time.</p>

Chemical constituents of Siegesbeckia pubescens / 中国中药杂志

<p><b>OBJECTIVE</b>To study the components in aerial part of Siegesbeckia pubescens.</p><p><b>METHOD</b>The compounds were isolated and purified by silica gel, sephadex LH-20 and other column chromatography. Structures were elucidated by spectroscopic methods.</p><p><b>RESULT</b>Four compounds were isolated from S. pubescens and were characterized as dimethyl-21-ethenetylene-darutigenol-3-O-beta-D-glucopyranosid (1), darutigenol (2), darutoside (3), stigmaster-3-O-beta-D-glucopyranosid (4).</p><p><b>CONCLUSION</b>Compound 1 is a new compound.</p>

Chemical constituents from chinese marine sponge Cinachyrella australiensis / 北京大学学报(医学版)

Objective: To investigate the secondary metabolites from Chinese marine Sponge Cinachyrella australiensis. Methods: Column chromatography techniques including HPLC were used for the separation and purification of the compounds, and extensive spectral analyses including various 2D NMR spectra were employed for structure elucidation. Results: Nineteen compounds were obtained ,including 2 methyoxy 6,12,15 trien 8 yne octadecanoic acid(1), 2 benzenedicarboxylic acid dibutyl ester(2), 1,2 benzenedicarboxylic acid bis(2 ethylhexyl)ester(3), ( ) (3S) 1,2,3,4 tetrahydro ? carboline 3 carboxylic acid(4), L Tryptophan (5), p hydroxylbenzaldehyde (6), p hydroxyl benzylethanol(7), p hydroxyl benzyl propanol(8), cholesta 4 en 3 ol(9), 2 methyl 6 amino 9 (2 deoxy ? D ribofuranosyl purine(10), 2' Deoxyadenosine (11), 6 amino 9 ? D ribofuranosyl 9H purine (12),uracil(13), thymine(14), thymidine(15), 1 (2 deoxy ? D Ribofuranosyl)uracil(16), 1 ethyl ? (2 deoxy) ? D ribofuranos(17),isolumichrome(18),and zarzissine(19).Conclusion:Compounds 1 and 18 are new natural products,and compounds 2 to 17 as well as 19 are isolated from this species for the first time.

Nucleosides from Anthopleura stell / 中草药

To study the chemical constituents of sea anemone, Anthopleura stell Verrill.Methods　The chemical constituents were isolated and purified by chromatographic methods and their structures elucidated by chemical evidences and spectra data.Results　5 nucleosides were obtained and identified from the ethanolic extract as 2-hydroxy purine (Ⅰ); deoxyinosine (Ⅱ); 1-methylxanthosine (Ⅲ); deoxyguanosine (Ⅳ), and deoxyribo-thymidine (Ⅴ).Conclusion　Compound Ⅲ was a new natural product， while the others were found from sea anemone for the first time.

Xanthone derivatives from medicinal plant Swertia mileensis / 中草药

Object Isolation and structural identification of xanthone derivative from medicinal plant Swertia mileensis T N Ho et W L Shih were carried out Methods The chemical constituents were isolated and purified by extensive silica gel column chromatography and their structures were elucidated by chemical evidences and spectral analysis Results There were 12 xanthone analogues named 1 hydroxy 2, 3, 4, 5 tetramethoxyxanthone, (Ⅰ); 1 hydroxy 2, 3, 7 trimethoxyxanthone, (Ⅱ); 1 hydroxy 2, 3, 5, 7 tetramethoxyxanthone, (Ⅲ); 1, 5 dihydroxy 2, 3 dimethoxyxanthone, (Ⅳ); 1, 5 dihydroxy 2, 3, 7 trimethoxyxanthone, (Ⅴ); 1 hydroxy 2, 3, 5 trimethoxyxanthone, (Ⅵ); 1, 5 dihydroxy 2, 3, 4, 7 tetramethoxyxanthone, (Ⅶ); 1, 8 dihydroxy 2, 3, 6 trimethoxyxanthone, (Ⅷ); 1 hydroxy 2, 3, 4, 7 tetramethoxyxanthone, (Ⅸ); 1, 2, 3, 5 tetromethoxyxanthone, (Ⅹ); 1 hydroxyl 2, 3, 4, 6 tetramethoxyxanthone, (Ⅺ); 1 hydroxyl 2, 3, 6, 8 tetramethoxyxanthone, ( ⅩⅡ ) Conclusion Compounds Ⅰ, Ⅲ, Ⅳ, Ⅴ, Ⅶ ⅩⅡ were first isolated from S. mileensis

Study of synergistic effects of Spirulina platensis on inducing IL-2 / 中国海洋药物

It has been shown that Spirulina platensis can regulate imminological functions.We report here that crude extract and purified components (phycocyanin and polysaccharide) from Spirulina platensis can induce secretion of IL 2 in splenocyte of BALB/C mice by means of MTT method.In the present study,we showed that all experimental components can't enhance proliferation of CTLL which was used in MTT method,but induce IL 2 secretion in splenocyte of BALB/C mice in three different concentration (0.01,0.1,1 g?L -1 ).Indeed the purified components especially phycocyanin part showed stronger IL 2 inducing activity than the crude one.IL 2 level was grow up when the incubation time of splenocyte and Spirulina platensis increased.In the concentration of 1 g?L -1 ,detected Spirulina platensis in our study assist IL 2 inducing of ConA (2mg?L -1 ) in splenocyte of BALB/C mice.

Chemical study on secondary metabolites from ascidian Styela clava (Ⅰ) / 中国海洋药物

From 95% alcohol extract of Ascidian Styela clava, collected from the shallow bay near Qingdao City, Shandong Province, six compounds, named, isovaleramide (1), thymine (2), thymidine (3), uracil (4), 2'-deoxyuridine (5) and ?-palmityl glycerin ether (6) were isolated,. Their structures were elucidated by various spectral analysis (IR, MS, ~1HNMR, ~(13)CNMR) and comparison of chemical and physical data with authentic samples reported in literatures. All of these compounds are first reported to be isolated from Ascidian Styela clava.

CHEMICAL CONSTITUENTS FROM CHINESE ANTHO-PLEURA XANTHOGRAMMICA BERKLY(II) / 中国海洋药物

From ethyl acetate fraction of Chinese Anthopleura xanthogrammica B, collected from Qingdao beach, three new glycerolipids named 1-O-hexadecanoyl-2-O (9-oc-tadecenoyl )-3-O-( 9, 12-octadecadienoyl ) glycerol (3)'1-O-hexadecahoyl-3-O-(14-eiosyle-cenoyl)glycerol (4)and l-O-(9,12-octadecadienoyl)-2-O-(9,12-octadecadienoyl)glycerol (5) as well as two lipidic acids named 9,12-octadecadienoic acidd) and 9,14-docosandienoic acid (2) were isolated. Their structures were identified by various spectrial(IR,PNMR ,CNMR, MS,et al)analysis and chemical conversion.