Chemical constituents from Morus notabilis and their cytotoxic effect / 药学学报

Une new flavonoids named as notabilisin K (1), together with four known compounds, morusin (2), mulberrofuran A (3), neocyclomorusin (4) and mornigrol F (5) are separated from 95% ethanol extracts of the twigs of Morus notabilis. Compounds 2-5 are separated from this plant for the first time. Notabilisin I, notabilisin J exhibits certain effect against cells of HCT-116, HepG2 and A2780 with IC50 values ranging from 1.47 μmol x L(-1) to 5.46 μmol x L(-1). Morusin exhibits strong effect against five kinds of human cancer cells (BGC823, A2780, HCT-116, HepG2 and NCI-H1650) with IC50 values ranging from 0.74 μmol x L(-1) to 1.58 μmol x L(-1).

Flavonol glycosides from Lysimachia clethroides / 中国中药杂志

Eleven flavonol glycosides were isolated from the ethanol extract of Lysimachia clethroides by a combination of various chromatographic techniques including column chromatography over silica gel, Sephadex LH-20, and reversed-phase HPLC. Their structures were identified as astragalin (1), isoquercitrin (2), isorhamnetin-3-O-β-D-glucopyranoside (3), quercetin-3-O-β-D-6"-acetylglucopyranoside (4), quercetin-7-O-β-D-glucopyranoside (5), prunin (6), 2-hydroxynaringin-5-O-β-D-glucopyranoside (7), kaempferol-3-O-rutinonoside (8), kaempferol-3-O-robinobioside (9), rutin (10) and kaempferol-3,7-di-O-β-D-glucopyranoside (11). Among them, compounds 4, 7 and 11 were obtained from the Lysimachia genus for the first time, while compounds 3, 5 and 9 were firstly reported from this plant. In the preliminary assays, compounds 2, 6 and 8 possessed significant inhibition against aldose reduc- tase, with IC50 values of 2.69, 1.00, 1.80 μmol · L(-1), respectively; none of compounds 1-11 exhibited obvious cytotoxic activity (IC50 > 10 μmol · L(-1)).

High performance liquid chromatography characteristic spectrum of artificial musk / 中国医学科学院学报

<p><b>OBJECTIVE</b>To determine the high performance liquid chromatography(HPLC)characteristic spectrum of artificial musk.</p><p><b>METHODS</b>HPLC was performed on a HiQ Sil C18 analytical column(4.6 mm×250 mm)with the mobile phase of methanol/water(90:10 v/v);the detection wavelength was 254 nm and the column temperature was maintained at 25 ℃. The similarities among 10 batches of artificial musk samples were anlysised in accordance with the System for Evaluating the Similarities among the Chromatographic Fingerprints of Traditional Chinese Drugs,which is recommended by Chinese Pharmacopoeia Commission.</p><p><b>RESULT</b>The similarities among these 10 batches of artificial musk ranged between 0.999 and 1.000.</p><p><b>CONCLUSION</b>HPLC is a convenient,accurate and reliable technique for establishing the specific spectum of artificial musk and therefore can be used for the quality control of this product.</p>

Detection of artificial musk in Xihuangwan by gas chromatography-mass spectrometery / 中国医学科学院学报

<p><b>OBJECTIVE</b>To control the quality of Xihuangwan by improving the qualitative detection of artificial musk inside this pill.</p><p><b>METHOD</b>The qualitative detection of artificial musk was carried out by gas chromatography-mass spectrometery(GC-MS).</p><p><b>RESULT</b>The established GC-MS successfully detected artificial musk in Xihuangwan.</p><p><b>CONCLUSION</b>GC-MS is reliable,accurate,and practical in the identification of artificial must inside Xihuangwan.</p>

Two novel isocoumarins from Erigeron breviscapus / 药学学报

Two novel isocoumarins, erigeronone C (1) and D (2), were isolated from the ethanol extract of the whole plant of Erigeron breviscapus (Vant.) Hand.-Mazz (Compositae). Their structures were respectively elucidated as 8, 9-dihydroxypyrano [3, 2-c] isochromen-4, 6-dione (1) and 4, 7-dihydroxy-3-(3-hydroxy-4-oxo-4H-pyran-2-yl)-1H-isochromen-1-one (2) on the basis of spectral analyses. Both structures of 1 and 2 possess a gamma-pyrone moiety and that is rare in natural products.

Chemical constituents from rhizomes of Acorus tatarinowii / 中国中药杂志

Fifteen compounds were isolated from the rhizomes of Acorus tatarinowii by means of various chromatographic techniques such as silica gel, ODS, Sephadex LH-20 and preparative HPLC, and their structures were elucidated as tatanone A (1), calamusenone (2), acoronene (3), 2-acetyloxyacoronene (4), acorenone (5), alpha-asarone (6), beta-asarone (7), 1,2-dimethoxy-4-(1'Z-propenyl) benzene (8), methyleugenol (9), asarylaldehyde (10), acoramone (11), gamma-asarone (12), 5-hydroxymethyl-2-furaldehyde (13), galgravin (14) and eudesmin (15) on the basis of spectroscopic data analysis. Compound 1 was a new compound, and compounds 3-5 were separated from Acorus species for the first time.

Advances of chemical constituents and pharmacological activities of schefflera genus / 中国中药杂志

The genus Schefflera (Araliaceae) consists of 1100 species, 35 of which can be found in China. Some species of the genus have been used in traditional medicine to treat rheumatalgia, trauma, fracture, headache, and so on. Phytochemical studies of the genus have demonstrated the presence of large number of triterpenoids and their saponins, along with some long-chain compounds, steroids and sesquiterpenes. Furthermore, many pharmacological activities of the genus such as anti-inflammatory, anticancer and antiviral activities have been reported. In this article, new development of constituents and biological activities of Schefflera genus is reviewed and summarized for its further development and utilization.

Water-soluble constituents from roots of Capparis tenera / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of the roots of Capparis tenera.</p><p><b>METHOD</b>The chemical constituents were isolated and repeatedly purified by kinds of column chromatography and the structures were elucidated by the NMR spectra and physicochemical properties.</p><p><b>RESULT</b>Eight compounds were isolated and identified as erigeside C (1), glucosuringic acid (2), vanillic acid 4-O-beta-D-glucoside (3-methoxy 4-glucosyl-benzoic acid) (3), 4-O-beta-D-glucopyranosylbenzoate (4), 3', 5'-dimethoxy- 4-O-beta-D-glucopyranosyl-cinnamic acid (5), tachioside (6), 2, 3-dihydroxy-1-(4-hydroxyl-3, 5-dimethoxyphenyl)-1-propanone (7) and acacetin 7-rutinoside (8).</p><p><b>CONCLUSION</b>Compounds 1-8 were all isolated from this plant for the first time and the compound 8 was isolated from this gene for the first time.</p>

Study on chemical constituents of Myricaria paniculata I / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Myricaria paniculata.</p><p><b>METHOD</b>Silica gel column chromatography was used to separate and purify the chemical constituents, and the structures were elucidated by spectral analysis.</p><p><b>RESULT</b>Four compounds were isolated from the petroleum ether soluble portion, identified as 28-aldehyde-taraxerenone (1), 28-hydroxy-taraxerenone (2), epi-friedelanol (3), 4-methyl stigmast-7-en-3-ol (4). Three compounds were isolated from the EtOAc soluble portion, identified as morelloflavone (5), methyl 3, 5-dihydroxy-4-methoxybenzoate (6), 3-hydroxy-4-methoxy cinnamic acid (7).</p><p><b>CONCLUSION</b>All of these compounds were isolated from the genus for the first time.</p>

Studies on the flavonoids in stem of Rhododendron anthopogonoide II / 中国中药杂志

<p><b>OBJECTIVE</b>To further investigate the flavonoids of Rhododendron anthopogonoide.</p><p><b>METHOD</b>The compounds were isolated and purified by Sephadex LH-20, polyamide and silica gel column chromatography. Their chemical structures were elucidated on the basis of physicochemical properties and spectral data.</p><p><b>RESULT</b>Six compounds were isolated and identified as: taxifolin (I), guaijaverin (II), reynoutrin (III), quercitrin (IV), polystachoside (V) and quercetin-4'-O-beta-D-galactoside (VI).</p><p><b>CONCLUSION</b>For the first time, compound VI was separated from Ericaceae plant, compounds II and V were isolated from Rhododendron plant, and compounds I and II were obtained from this plant.</p>

Studies on the flavonoid compounds of Rhododendron anthopogonoides / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the flavonoid constituents of the Rhododendron anthopogonoides systematically.</p><p><b>METHOD</b>The chemical components were isolated by sephadex LH-20, polyamide and silica gel column chromatography. The chemical structures were elucidated on the basis of physic-chemical properties and spectral data.</p><p><b>RESULT</b>Eight compounds were isolated and identified as: Quercetin (I), isorhamnetin (II), hyperoside (III), cacticin (IV), hirsutine (V), kaemferol-3-beta-D-galactoside (VI) myricetin-3-beta-D-Xyloside (VII), (6''-O-(4-Hydroxybenzoyl) hyperoside (VIII).</p><p><b>CONCLUSION</b>Compounds II, IV, V, VI, VII, and VIII were obtained from this plant for the first time. Compounds VII and VIII were separated from the Ericaceae plant for the first time.</p>

Chemical constituents from the leaves of Dalbergia hainanensis / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from the leaves of Dalbergia hainanensis.</p><p><b>METHOD</b>Compounds were isolated by chromatographic techniques on silica gel and polyamide column. Their structures were elucidated by chemical and spectroscopic methods.</p><p><b>RESULTS</b>Thirteen compounds were identified as 8-C-glucosylprunetin (1), 8-C-glucosylgenistein (2), 2-hydroxy-5-methoxy biochanin A (3), formononetin (4), 3,5-dimethoxy-4-hydroxybenzaldehyde (5), 1-O-beta-D-glucopyranosyl-(2S, 3S, 4R, 8Z)-2-[(2R)-2-hydroxyl docosylamino]-8-octadecene-1, 3, 4-triol (6), friedelin (7), taxaxerol (8), 3(-hydroxy-glutin-5-ene (9), ursolic acid (10), beta-sitosterol (11), daucosterol (12), lupeol (13).</p><p><b>CONCLUSION</b>All the compounds were isolated from the plant for the first time.</p>

Studies on chemical constituents of Uvaria macrophylia / 药学学报

<p><b>AIM</b>To study the chemical constituents from Uvaria macrophylla Roxb. (Annonaceae).</p><p><b>METHODS</b>Various chromatography techniques were used to separate and purify the constituents. Their structures were elucidated by UV, IR, MS, 1HNMR, 13CNMR, 1H-1H COSY, HMQC and HMBC spectral analysis.</p><p><b>RESULTS</b>Seven compounds have been isolated from the CHCl3 extract of the roots of the U. macrophylla. They were identified as macrophyllin (1), onysilin (2), taraxerol (3), 3,5-dimethoxy benzyl benzoic acid ester (4), benzoic acid (5), beta-sitosterol (6) and daucosterol (7).</p><p><b>CONCLUSION</b>Compound 1 is a new compound. Compounds 2-7 were obtained from this plant for the first time.</p>

Prospect in the study of creating new drugs from Chinese herbal medicine / 中国医学科学院学报

This paper concisely describes the prospect in developing new drugs from Chinese herbal medicine. The search for bioactive constituents or leading compounds from natural sources especially from Chinese herbal medicine will be proved to be one of the most effective ways by changing the traditional concept of study on natural drugs using modern ideas. It is well known that plants in China provide a fertile source of natural compounds dealt with biological and structural diversity, which is the best channel to discover bioactive and leading compounds. Many instances have showed that structural transformation and analogues synthesis of known natural compounds or drugs can provide an important way to find new leading compounds. Study of the bioactive principle of Chinese herbal medicine involves an integration of chemical study and bioassay with intensive screening. It should be emphasized that the investigation of bioactive compounds for creating new drugs is the major task of Chinese pharmaceutical industry.

Syntheses and antitumor activities of the derivatives of P-methyl goniotriol in vitro / 药学学报

<p><b>AIM</b>To find derivatives of p-methyl-goniotriol with more potent antitumor activities and lacking undesirable effects.</p><p><b>METHODS</b>Eighty derivatives of p-methyl-goniotriol have been synthesized in nine steps from alpha-D-glucoheptonic-delta-lactone (2). Compound 2 reacted with acetone in the catalyzer, H2SO4 and anhydrous MgSO4, and then reacted with 60% aqua HOAc, finally was oxidized by NaIO4 at room temperature into aldehyde 3 in a yield of 71.3%. The aldehyde 3 reacted immediately with P-CH3-PhMgBr giving mixture 4. The mixture 4 was oxidized by NaIO4, reacted with Ph3P = CHCO2Et and then induced by catalyzer. 1,8-Diazabicylclo[5, 4, 0]undec-7-ene in THF providing the compounds 6 and 7. The esterfication of 6 with cinnamyl chloride et al in 4-dimethylaminopyridine, Et3N gave the esters 8a-h. Acid hydrolysis of the acetone protecting group of 8a-h in 75% aqua HOAc gave compounds 9a-h. Their chemical structures were confirmed by IR, 1HNMR, MS and element analysis. The antitumor activities of the compounds were screened by MTT methods.</p><p><b>RESULTS</b>Fifteen derivatives of p-methyl-goniotriol (7, 8b-h, 9b-h) are new compounds.</p><p><b>CONCLUSION</b>Pharmacological tests indicate that these compounds showed antitumor activities toward tumor cells (A2780, HCT-8, Bel742, KB) in vitro. The antitumor activities of 8b, 8d, 8g and 9h were more potent than howiinol A.</p>