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As part of ongoing project on screening plants used in Iranian folk medicine to treatment of diabetes, α-glucosidase inhibition activities of Rosa canina extracts have been tested. The acetone extract of the plant exhibited significant inhibition with IC 50 value of 0.3 µg/ml. The enzyme based assay guided fractionation of the acetone extract led to the isolation of daucosterol (1) and D-glucono-1,4-lactone (2), as highly active α-glucosidase inhibitors. Their structures were determined by 1H- and 13C-NMR spectroscopic evidences. The IC 50 values of daucosterol and D-glucono-1,4-lactone on yeast α-glucosidase were 13.3 and 6.5 µM, respectively, while IC 50 of acarbose was 16.1 µM, as a positive control. The Lineweaver-Burk plots analysis elucidated that both of the compounds inhibited the enzyme competitively. The study suggests that isolated compounds can be good candidates as α-glucosidase inhibitors and provide strong rationale for more in vivo studies.

Allergic transfusion reaction is an anomaly that develops within several hours of transfusion which is usually treated by antihistamine. In the present study, we are looking into daucosterol, an extract of Traditional Chinese Medicine (TCM) Cordyceps, as a potential inhibitor of histidine decarboxylase. The approach of molecular docking and Molecular Dynamics Simulation (MDS) on a traditional anti-inflammatory Chinese medicine gave an atomic insight of the inhibition. The daucosterol was binding with a ΔG of -3.17 Kcal/mol, to inhibit histamine synthesis by binding to histidine decarboxylase, possibly via the flexible catalytic loop. Such inhibitors that were designed to block the flexibility of the catalytic loop are potential candidates for further drug development program.

Previous experimental evidence suggested that Bergenia ciliata (Saxifragaceae) and Terminalia chebula Retzius(Combretaceae) are effective against nephrolithiasis and have potential antioxidant activity. In this regard, hydro-methanolic extracts of B. ciliata rhizomes and T. chebula fruits were investigated for antioxidant potential against sodium oxalate induced oxidative imbalance in the kidney of female Wistar rats. We also performed molecular docking studies of all the reported phenolic compounds of both the plants to evaluate its interaction with the active site of oxalate binding protein (OBP). In summary, our findings showed that sodium oxalate caused significant increase in lipid peroxidation with concurrent decrease in activities of superoxide dismutase and catalase as well as in total reduced glutathione content in a concentration-dependent manner. The hydro-alcoholic extracts, however, when co-administered with sodium oxalate resulted in significant protection with maximum percent protection was achieved by B. ciliata. Thereafter, daucosterol showed best binding efficiency with OBP. However, further work on the purification of isolated bioactive components and pharmacological testing can reveal the therapeutic potential of the plant.

Article history: Received on: 02/02/2015 Revised on: 12/02/2015 Accepted on: 21/03/2015 Available online: 27/04/2015 For the purpose of developing anti-wrinkle cosmetic ingredients, the extracts from branches of a woody plant Sambucus sieboldiana var. pendula were examined on collagen synthesis activities using fibroblast HDFn cells. As a result, the S. sieboldiana ethanol extract (SSE) proved to activate the production of type I procollagen in a dose-dependent manner without showing cell toxicity. Phytochemical study was conducted to isolate the active constituents in the extracts by solvent fractionation followed by chromatographic purifications. From this procedure, two known compounds, kaempferol 3-O-sophoroside (1) and daucosterol (2), were identified by spectroscopic studies. From the isolates, the flavonoid glycoside 1 was verified to induce the synthesis of the type I procollagen dose-dependently. These results suggested that S. sieboldiana extract containing the flavonoid 1 could be useful as an active ingredient in wrinkle-care cosmetics.

Background: Artemisia apiacea is a traditional herbal medicine using treatment of eczema and jaundice in Eastern Asia, including China, Korea, and Japan. Objective: An accurate and sensitive analysis method using high performance liquid chromatography-diode array ultraviolet/visible detector and liquid chromatography-mass spectrometry for the simultaneous determination of three phytosterol compounds, campesterol, stigmasterol and daucosterol in A. apiacea was established. Materials and Methods: The analytes were separated on a Shiseido C 18 column (5 μm, 4.6 mm I.D. ×250 mm) with gradient elution of 0.1% trifluoroacetic acid and acetonitrile. The flow rate was 1 mL/min and detection wavelengths were set at 205 and 254 nm. Results: Validation of the method was performed to demonstrate its linearity, precision and accuracy. The calibration curves showed good linearity (R2 > 0.9994). The limits of detection and limits of quantification were within the ranges 0.55-7.07 μg/mL and 1.67-21.44 μg/mL, respectively. And, the relative standard deviations of intra- and inter-day precision were

Mansoa Alliacea is a native plant from Amazonian basin and has great ancestral value for the local communities. M. alliacea is a traditional medicine for healers and shamans and has multiple uses due to the presence of several chemical constituents with important pharmacological properties. Plant derivate are used as: antiseptic, diuretic, analgesic, antipyretic. Folk medicine is related also to the treatment of many diseases such as: reduction of blood pressure against atherosclerosis, arthritis and rheumatism. Researches have also been proven an appreciable antioxidant property, which revalue it for cosmetic purposes. Chemical composition includes: alidil-sulfoxide, allylindyloxide, allina, allein, allicin, disulfide, propylallyl, divinyl sulfide, diallyl sulfide, dimethyl sulfide, daucosterol, beta-sitosterol, fucosterol, stigmasterol, iridoides and isothiocyanates, naphthoquinones, alkaloids, saponins, flavones, vitamin E, vitamin C and minerals such as chromium and selenium. The present review includes ethnobotanical and pharmacological data that are related to the chemical composition of M. alliacea species.

Hepatocellular carcinoma (HCC) is one of the leading causes of cancer-related death worldwide. The purpose of this study was to determine the effects of daucosterol on HCC by investigating Wnt/β-catenin signaling. In this study, HepG2 and SMMC-7721 cells were treated with varying concentrations of daucosterol, and the corresponding inhibitory effects on HCC cells were examined via CCK-8 assays. Cell migration and invasion abilities were detected via transwell assays. β-Catenin and phospho (p)-β-catenin levels were analyzed via western blotting. Our results showed that daucosterol reduced the proliferation, migration, and invasion capacities of HCC cells in a concentration-dependent manner. In addition, daucosterol reduced the levels of β-catenin and p-β-catenin in HepG2 and SMMC-7721 cells. Furthermore, the Wnt signaling pathway inhibitor SB-216763 was used to treat HepG2 and SMMC-7721 cells with daucosterol. Our results showed that co-treatment with daucosterol and SB-216763 abolished the effects of daucosterol on cell inhibition ratios, cell migration, and cell invasion. These findings indicated that daucosterol inhibited cell migration and invasion in HCC cells via the Wnt/β-catenin signaling pathway. Therefore, our study highlights the use of daucosterol as a promising therapeutic strategy for HCC treatment.

Lung cancer is the leading cause of cancer related deaths both in developed and developing countries. Since majority of the existing therapeutic methods harms both normal and malignant cells, a viable alternative is to switch into safe and beneficial traditional medicinal plants. Hence the present study was framed to identify selective anti-lung cancer agents from the medicinal plant Grewia tiliaefolia (GT). Cell viability experiments showed that benzene extract of GT (BGT) leaf effectively inhibited the growth of A549 cells, while being non-toxic to normal human lung L132 and PBMC cells. Ames and comet assays demonstrated that BGT is of non-mutagenic and non-genotoxic nature in untransformed cells. The hematological and histopathological profiles of the in vivo acute and sub-acute toxicity studies demonstrated that BGT is safe and tolerable. Importantly, western blot analysis and Annexin V-FITC staining confirmed that BGT promotes mitochondrial dependent apoptotic cell death in A549 cells by arresting cell cycle at G2/M phase. Bio-assay guided fractionation revealed the presence of phytosteols (β-sitosterol and daucosterol) which significantly inhibited the growth of A549 cells both alone and in combination. This study warrants that these phytosterols in alone or in combination can be considered as safe and potential drug candidates for lung cancer treatment.

Objective To screen Vietnamese medicinal plants for xanthine oxidase (XO) inhibitory activity and to isolate XO inhibitor(s) from the most active plant. Methods The plants materials were extracted by methanol. The active plant materials were fractionated using different organic solvents, including n -hexane, ethyl acetate, and n -butanol. Bioassay-guided fractionation and column chromatography were used to isolate compounds. The compounds structures were elucidated by analysis of spectroscopic data, including IR, MS, and NMR. Results Three hundreds and eleven methanol extracts (CME) belonging to 301 Vietnamese herbs were screened for XO inhibitory activity. Among these plants, 57 extracts displayed XO inhibitory activity at 100 μg/mL with inhibition rates of over 50%. The extracts of Archidendron clypearia ( A. clypearia ), Smilax poilanei , Linociera ramiflora and Passiflora foetida exhibited the greatest potency with IC 50 values below 30 μg/mL. Chemical study performed on the extract of A . clypearia resulted in the isolation of six compounds, including 1-octacosanol, docosenoic acid, daucosterol, methyl gallate, quercitrin and (−)-7-O-galloyltricetiflavan. The compound (−)-7-O-galloyltricetiflavan showed the most potent XO inhibitory activity with an IC 50 value of 25.5 μmol/L. Conclusions From this investigation, four Vietnamese medicinal plants were identified to have XO inhibitory effects with IC 50 values of the methanol extracts below 30 μg/mL. Compound (−)-7-O- galloyltricetiflavan was identified as an XO inhibitor from A . clypearia with IC 50 value of 25.5 μmol/L.

Two new labdane diterpenoids, s-trans-8(17),12E,14-labdatrien-20-oic acid (1), s-trans-12E,14-labdadien-20,8β-olide (2), along with 10 known compounds, hinokiol (3), ursonic acid (4), 2α,3α-dihydroxyolean-12-en-28-oic acid (5), 2α,3β,23-trihydroxyolean-12-en-28-oic acid (6), ethyl 3-(3,4-dihydroxyphenyl)lactate (7), ethyl rosmarinate (8), (Z,E)-2-(3,4-dihydroxyphenyl)ethenyl caffeic ester (9), tridecanoic acid (10), β-sitosterol (11) and daucosterol (12), were isolated from the 70% acetone extract of the rhizomes of Isodon yuennanensis. Their structures were elucidated based on the analyses of extensive spectroscopic data and physicochemical properties.

Objective To study the chemical constituents from the leaves of Oplopanax horridus. Methods The chemical constituents were isolated and purified by column chromatography on silica gel and Sephadex LH-20 gel columns, 1H-NMR and 13C-NMR were applied for the identification of chemical structure. Results Ten compounds were isolated and identified as dammara-20,24-dien-3β-ol acetate (1), phytol (2), 16Z,19Z-pentacosadienoic acid (3), β-sitosterol (4), (3S,8S-falcarindiol (5), maltol (6), acankoreagenin (7), daucosterol (8), stigmasterol-3-O-β-D-glucopyranoside (9), and acankoreoside A (10). Conclusion Compounds 1–3, 6, and 10 are isolated from this plant for the first time. Compounds 1–3 and 6 are isolated from the plants in genus Oplopanax Miq. for the first time. Moreover, Compounds 1, 3, and 6 are isolated from the plants in the family of Araliaceae for the first time.

From Chloranthus multistachys, five terpenoids and two other compounds were isolated and identified as 12(S), 15-dihydroxylabda-8(17), 13E-dien-19-oic acid (1), henrilabdane B (2), zedoarofuran (3) 1β, 8β-Dihydroxy-eudesman 3,7(11)-dien-8α,12-olide (4) , multistalactone E (5), palmitic acid (6), daucosterol (7). The structures of the isolated compounds were established by means of NMR and MS analyses.

FromChloranthushenryi,ten compounds were isolated and identified as 1β,8β-Dihydroxy-eudesman 4(15),7(11)-dien8α,12-olide (1), 4β,8β-dihydroxy-5α (H)- eudesm-7(11) -en-8,12-olide (2), 12-oxo-15-hydroxylabda-8(17), 13E-dien-19-oic acid (3), 12(S), 15-dihydroxy labda - 8(17),13E-dien-19-oic acid (4) , curcolonol (5), flavokawain A (6), 2 ́-hydroxy-4, 3 ́, 4 ́, 6 ́– tetramethoxychalcone (7), daucosterol (8), β-sitosterol (9) and 3,4-dihydroxybenzoic acid (10). The structures of the isolated compounds were established by means of NMR and MS analyses. These compounds were firstly isolated from this plant. Compound 1 have inhibitory activities on the release of β-glucuronidase from rat PMNs induced by PAF.

The use of α-glucosidase inhibitors is considered to be an effective strategy in the treatment of diabetes. Using a bioassay-guided fractionation technique, five Bacillus stearothermophilus α-glucosidase inhibitors were isolated from the flowers of Musa spp. (Baxijiao). Using NMR spectroscopy analysis they were identified as vanillic acid (1), ferulic acid (2), β-sitosterol (3), daucosterol (4) and 9-(4′-hydroxyphenyl)-2-methoxyphenalen-1-one (5). The half maximal inhibitory concentration (IC50) values of compounds 1–5 were 2004.58, 1258.35, 283.67, 247.35 and 3.86 mg/L, respectively. Compared to a known α-glucosidase inhibitor (acarbose, IC50 = 999.31 mg/L), compounds 3, 4 and 5 showed a strong α-glucosidase inhibitory effect. A Lineweaver-Burk plot indicated that compound 5 is a mixed-competitive inhibitor, while compounds 3 and 4 are competitive inhibitors. The inhibition constants (Ki) of compounds 3, 4 and 5 were 20.09, 2.34 and 4.40 mg/L, respectively. Taken together, these data show that the compounds 3, 4 and 5 are potent α-glucosidase inhibitors.

Activity-guided isolation of dried seeds of Jatropha curcas L. led to the isolation of two new lignans along with eight known compounds. These compounds were determined by spectroscopic analysis to be jatrophasin C (1), jatrophasin D (2), β-sitosterol (3), jatrophasin A (4), daucosterol (5), isoamericanol A (6), ( ± )-3,3′-bisdemethylpinoresinol (7), 7′-epi-sesamin-dicatechol (8), isoprincepin (9) and americanol A (10), of which 1 and 2 were new compounds. The antioxidative activities along with peroxisome proliferator-activated receptor gamma exciting activity of these compounds were also determined.

Anti-cancer effects were compared amongst Taraxacum coreanum extract, its fractions, and 7 ingredients (β-sitosterol, daucosterol, taraxasteryl acetate, chrysoeriol, diosmetin, luteolin, and luteoloside). Exposure to the ethyl acetate fraction (50 and 100 μg/mL) of T. coreanum extract and luteolin (10 and 50 μM) for 24 h induced the cleavage of poly (ADP-ribose) polymerase (PARP), caspase-3, and caspase-8, in a dose-dependent manner. These findings demonstrate that luteolin is the main active component of T. coreanum extract activating caspases-3 and -8 which contribute to apoptotic cell death.

Neural stem cells (NSCs) are self-regenerating cells, but their regenerative capacity is limited. The present study was conducted to investigate the effect of daucosterol (a sterolin) on the promotion of NSC proliferation and determine the corresponding molecular mechanism. Results of cell counting kit-8 (CCK-8) assay showed that daucosterol significantly increased the quantity of viable cells and the effectiveness of daucosterol was similar to that of basic fibroblast growth factor (bFGF) and epidermal growth factor (EGF). Flow cytometry detection of CFSE-labeled (CFSE, carboxyfluorescein diacetate succinimidyl ester) NSCs showed that Div Index (or the average number of cell divisions) and % Divided (or the percentage of cells that divided at least once) of the cells were increased, indicating that daucosterol increased the percentage of NSCs re-entering the cell cycle. mRNA microarray analysis showed that 333 genes that are mostly involved in the mitotic cell cycle were up-regulated. By contrast, 627 genes that are mostly involved in differentiation were down-regulated. In particular, insulin-like growth factor I (IGF1) was considered as an important regulatory gene that functionally promoted NSC proliferation, and the increased expression of IGF1 protein was validated by ELISA. In addition, the phosphorylation of AKT was increased, indicating that the proliferation-enhancing activity of daucosterol may be involved in IGF1-AKT pathway. Our study provided information about daucosterol as an efficient and inexpensive growth factor alternative that could be used in clinical medicine and research applications.

Objectives To evaluate anti-proliferative as well as apoptotic activities of compounds identified in chloroform extract of Juglans regia leaves, on human breast and oral cancer cell lines (MCF-7 and BHY). Materials and methods Column chromatography, MTT assay, flowcytometry and western blotting have all been used in the study. Results Bioassay-guided fractionation of chloroform extract of J. regia afforded isolation of 5-hydroxy-3,7,4′-trimethoxyflavone [1], lupeol [2], daucosterol [3], 4-hydroxy-α-tetralone [4], β-sitosterol [5], 5,7- dihydroxy-3,4′-dimethoxyflavone [6] and regiolone [7]. Structures of the compounds were established on the basis of spectroscopic analyses [Nuclear magnetic resonance (NMR) and mass]. All compounds inhibited proliferation of MCF-7 (human breast adenocarcinoma) and BHY (human oral squamous carcinoma) cells in a concentration-dependent manner. Compounds 6 and 7 had potent cytotoxic effects on both MCF-7 and BHY cells (IC50 21–51 μm), yet were not toxic to normal cells. MCF-7 growth inhibition was attributed to apoptosis; population of apoptotic cells increased from 1.12% in controls to 5.64 and 8.1% after 48-h treatment with compounds 6 and 7, indicating their potential at inducing early and late apoptosis. The caspase cascade was not activated, as indicated by only insignificant cleavage of caspase-3. Conclusions Our results suggest that compounds 6 and 7 can induce apoptosis in MCF-7 cells through the caspase-3 independent pathway.

Eight compounds were isolated from the ethanol extract of G. algida Pall. the structure of these compounds were identified as: oleic acid (1), linoleic acid (2), octacosanoic acid (3), β-sitosterol (4), 2,3-dihydroxybenzoic acid ethyl ester (5), n-butyl isobutyl phthalate (6), daucosterol (7), 5,8-dimethoxy furocoumarin (8). These structures were identified by NMR MS IR and other spectroscopic techniques. These compounds were isolated from this plant for the first time.

Five compounds were isolated from the EtOAc extract of Euphorbia altotibetica. The structures of these compounds were elucidated as: β-sitosterol (1), daucosterol (2), chrysophanol (3), (-)-epiafzelechin (4), 5,2-dihydroxy-7,8,6-trimethoxyflavanone (5) by NMR datas, the antibacterial activity of all compounds were examined on five species of bacteria Escherichia coli, Staphylococcus aureus, Bacillus licheniformis, Pseudomonas aeruginosa and Streptococcus pneumoniae.

A new hopantenic acid derivative, (R)-methyl-4-(2,4-dihydroxy-3,3-dimethylbutanamido)butanoate (1), was isolated from the rhizomes of Heterosmilax japonica Kunth, together with three known compounds, (3S)-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid (2), daucosterol (3), and ethyl-β-D-xylobioside (4). The structure of 1 was determined by extensive spectroscopic analyses, including 1D and 2D NMR and HR-ESI-MS. Compounds 2 and 4 are new for the genus Heterosmilax.

Ajania nematoloba (Hand.-Mazz.) Y. Ling & C. Shih, a species of Ajania from the Asteraceae family, is distributed mainly in the northwest of China, and many species of Ajania are used as folk medicinal plants for curing bronchitis, lung diseases, intestinal ulcers, and rheumatism [1]. The chemical constituents of this plant have not yet been reported. In the course of screening for biologically and chemically novel agents in the Asteraceae family, we investigated this plant. Fifteen compounds were isolated from the whole plants of A. nematoloba, and some of the constituents showed significant antitumor and antioxidant activities. The specimen of A. nematoloba was collected in September from Lanzhou, Gansu Province, China and identified by Prof. Guoliang Zhang of Lanzhou University. A voucher specimen is deposited in the Laboratory of Natural Products Chemistry, Fujian Medical University of Fujian Province. The air-dried and powdered whole plants of A. nematoloba (4.5 kg) were cut into small pieces and refluxed three times with 95% ethanol at room temperature for 7 days each time. The ethanol extract was concentrated to an aqueous residue, which was extracted successively with petroleum ether, ethyl acetate, and n-butanol. Each fraction was purified by column chromatography with silica gel, Sephadex LH-20, and RP-18 to yield 1–15. The structures of the isolated compounds were identified on the basis of spectroscopic analyses including 1H, 13C NMR spectroscopy, and mass spectrometry. The 15 compounds were determined as luteolin-7-O-D-glucopyranoside (1) [2], acacetin-7-O-D-glucopyranoside (2) [3], eriodictyol-7-O-D-glucopyranoside (3) [4], 3 -methoxyluteolin-7-OD-glucopyranoside (4) [5], luteolin (5) [2], apigenin (6) [2], cirsilineol (7) [6], jaceosidin (8) [7], centaureidin (9) [8], baihuaqianhuside (10) [9], 5 ,8 -epidioxyergosta-6,22-dien-3 -ol (11) [10], (22E,24R)-ergosta-7,22-dien-3 ,5 ,6 -triol (12) [10], palmitic acid (13) [11], daucosterol (14), and -sitosterol (15). All these compounds were isolated from A. nematoloba for the first time. Cytotoxicities of compounds 1–3, 5, and 7–9 were tested on the three cancer cell lines: human leukemia cells K562, human colon cancer cells Colon26, and human colon cancer cells SW1116. Table 1 shows that 7 exhibited significant cytotoxicity against K562, Colon26, and SW1116, with IC50 values of 6.7, 6.9, and 6.4 g/mL, respectively. The radical-scavenging activity of compounds 1–5, 8, and 9 against DPPH free radical were measured, and compounds 1 and 3–5 showed excellent antioxidant activity (Fig. 1).

An unusual new phenolic component, triticumoside (1), and eight known compounds, isoorientin (2), isoscoparin (3), (2R)-2-O-β-D-glucopyranosyloxy-4,7-dimethoxy-2H-1,4-benzoxazin-3(4H)-one (4), adenosine (5), β-sitosterol (6), daucosterol (7), 6′-O-linolenoyl daucosterol (8), α-tocopherol (9), were isolated fromTriticum aestivum sprouts. The hybrid structure of 1, which is a hybrid between a flavone and a polyoxygenated benzene, is rarely found in natural sources. In addition, the effects of these compounds on LPS-induced NO and TNF-α production in RAW 264.7 cells were evaluated. At a concentration of 2.0 μM, compounds 2-4 significantly inhibited the production of both NO and TNF-α. Compound 1 exhibited inhibitory activity on the secretion of TNF-α at concentrations as low as 2.0 μM, but it did not reduce NO levels at any of the tested concentrations.

Three new ursane-type triterpenoids, 3α,6α,30-trihydroxy-ursan-28-oic acid (1), 3α,30-dihydroxy-6-oxo-ursan-28-oic acid (2) and 3α,6α,7α,30-tetrahydroxy-ursan-28-oic acid (3), together with one known triterpenoid, betulinic acid (4), one known anthraquinone, 1,7-dihydroxy-2-methylanthraquinone (5), four known phenols, 1,3,5-trimethoxybenzene (6), p-hydroxybenzoic acid (7), syringic acid (8), isovanillin (9), two steroids, sitosterol (10) and daucosterol (11), were isolated from the ethanol extract of the stems of S. merrillii. Their structures were elucidated on the basis of physical and spectral techniques, besides comparison with literature data. Compounds 1–3 showed inhibitory activities against the A549, HEPG2, and B16F10 cell lines.

BACKGROUND Rapid urbanisation and nutritional transition is fuelling the increased global incidence of type 2 diabetes. Pineapple fruit residue was explored for its nutraceutical properties as an alternative or adjunct to currently available treatment regime. Ethyl acetate and methanolic extracts of pineapple fruit residue were evaluated for anti-diabetic activity in cell free and cell based systems. Specifically, we assessed: (1) antioxidant potential, (2) anti-glycation potential, (3) carbohydrate digestive enzyme inhibition, and (4) lipid accumulation and glycerol-3-phosphate dehydrogenase activity in differentiating 3T3-L1 cells. RESULTS The active components in the ethyl acetate and methanolic extracts were identified as sinapic acid, daucosterol, 2-methylpropanoate, 2,5-dimethyl-4-hydroxy-3(2H)-furanone, methyl 2-methylbutanoate and triterpenoid ergosterol using DART/HRMS and ESI/HRMS. Micronutrient analysis revealed the presence of magnesium, potassium and calcium. Adipogenic potential, anti-glycation property of the ethyl acetate extract, and DNA damage protection capacity of the methanolic extract are promising. CONCLUSION Results from this study clearly indicate that pineapple fruit residue could be utilised as a nutraceutical against diabetes and related complications. © 2013 Society of Chemical Industry

Amethanolic extract of Dipsacus asper, having anti-diabetic activity, was examined as a possible aldose reductase (ALR2) inhibitor, a key enzyme involved in diabetic complications. Bioactivity guided fractionation led to the isolation of ten compounds, ursolic acid (1), oleanolic acid-3-O-α-L-arabinopyranoside (2), daucosterol (3), hederagenin-3-O-α-L-arabinopyranoside (4), sweroside(5), caffeic acid (6), esculetin (7), protocatechualdehyde (8), loganin (9), and vanilic acid (10) from the ethyl acetate fraction of D. asper methanol extract. Among them, compounds 4, 6, 7, and 8 exhibited inhibitory effects on aldose reductase, with IC50 values of 23.70, 16.71, 34.36, and 21.81 μM, respectively. This is the first report on the isolation of these compounds from D. asper, and the ALR2 inhibitory activity of hederagenin-3-O-α-L-arabinopyranoside. These results suggest the successful use of the extract of D. asper for ameliorating diabetic complications.

From the fresh bulbs of Fritillaria monatha Migo., ten compounds were isolated and identified as peimine (1), peiminine (2), isovertifine (3), pengbeimine A(4), pengbeimine B(5), pengbeimine C(6), pengbeimine D(7),stearic acid (8), daucosterol (9) and campesterol (10). Their structures were determined by NMR, MS spectral data.

Phytochemical constituents were isolated from the fruits of Acanthopanax senticosus by repeated chromatography and prep-HPLC. Their structures were identified as β-sitosterol (1), daucosterol (2), p-hydroxybenzoic acid (3), vanillic acid (4), uracil (5), eleutheroside K (6), songoroside A (7), copteroside B (8) and myo-inositol (9) by spectroscopic analysis. Among them, p-hydroxybenzoic acid (3), eleutheroside K (6) and songoroside A (7) were isolated for the first time from the fruits of A. senticosus, and songoroside A (7) was isolated for the first time from Acanthopanax species. Key words: Acanthopanax senticosus, Araliaceae, repeated chromatography, songoroside A.

A new ursane-type triterpenoid, 3β-hydroxy-urs-30-p-Z-hydroxycinnamoyloxy-12-en-28-oic-acid (1), together with three known triterpenoids, 3β-hydroxy-urs-30-p-E-hydroxycinnamoyloxy-12-en-28-oic-acid (2), 2α,3β,19α-trihydroxy-urs-12-en-28-oic-acid (3), and ursolic acid (4), four known lignans, pinoresinol (5), 9α-hydroxypinoresinol (6), (+)-medioresinol (7), and (+)-kobusin (8), and two steroids, β-sitosterol (9), and daucosterol (10), were isolated from the whole parts of Teucrium viscidum. Their structures were established by a combination of spectroscopic data analysis, besides comparison with literature data. Compounds 1–4 were evaluated for their inhibitory activities against 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1).

Background: Caesalpinia gilliesii Hook is an ornamental shrub with showy yellow flowers. It was used in folk medicine due to its contents of different classes of secondary metabolites. In our previous study, dichloromethane extract of C. gilliesii flowers showed a good antioxidant activity. Aim of the Study: Isolation and identification of bioactive hepatoprotective compounds from C. gilliesii flowers dichloromethane fraction. Materials and Methods: The hepatoprotective activity of dichloromethane fraction and isolated compounds were studied in CCl4-intoxicated rat liver slices by measuring liver injury markers (alanine aminotransferase, aspartate aminotransferase and glutathione [GSH]). All compounds were structurally elucidated on the basis of electron ionization-mass spectrometry, one- and two-dimensional nuclear magnetic resonance. Results: A new 12,13,16-trihydroxy-14(Z)-octadecenoic acid was identified in addition to the known β-sitosterol-3-O-butyl, daucosterol, isorhamnetin, isorhamnetin-3-O-rhamnoside, luteolin-7,4’-dimethyl ether, genistein-5-methyl ether, luteolin-7-O-rhamnoside, isovanillic acid, and p-methoxybenzoic acid. Dichloromethane fraction and isorhamnetin were able to significantly protect the liver against intoxication. Moreover, the dichloromethane fraction and the isolated phytosterols induced GSH above the normal level. Conclusion: The hepatoprotective activity of C. gilliesii may be attributed to its high content of phytosterols and phenolic compounds. SUMMARY Bioactive Hepatoprotective phytosterols and phenolics from chloroform extract of Caesalpinia gilliesii Abbreviations used: ALT: Alanine Aminotransferase; AST: Aspartate aminotransferase; GSH: Glutathione; SC50: Scavenging Capacity 50 (SC 50); COSY: Correlation spectroscopy; NMR: Nuclear Magnetic Resonance; CC: Column chromatography; EI-MS: Electron-impact mass spectrometry; HSQC: Heteronuclear single-quantum correlation.

A new naturally occurring ent-kaurane diterpenoid dimer, 15β, 15′β-oxybis (ent-kaur-16-en-19-oic acid) (1) along with six known compounds, 15β-hydroxy-ent-kaur-16-en-19-oic acid (2), 15β-hydroxy-ent-kaur-16-en-19-oate-β-d-glucopyranoside (3), 6-hydroxykaempferol-3, 7-dimethyl ether (4), quercetagetin 3, 7, 3′-trimethyl ether (5), β-sitosterol (6) and β-sitosterol glucoside (daucosterol) (7) were isolated from the aerial parts of Pulicaria inuloides DC. Compounds 2–5 were isolated for the first time from genus Pulicaria. The structures of compounds 1–7 were established on the basis of extensive 1D and 2D NMR spectroscopic techniques in combination with ESI-MS. The antimicrobial activity of the isolated compounds was evaluated against Staphylococcus aureus, Escherichia coli and Candida albicans. Sulphorhodamine B cytotoxic assay against HepG2 (liver cancer) cell line and ABTS antioxidant assay were carried out.

Background: Salvia, known as Maryam Goli in the Persian language, is an important genus that includes approximately 900 species in the Lamiaceae family. There are 58 Salvia species growing naturally in Iran, including Salvia chloroleuca Rech. f. and Allen., which grows wild in the northeastern and central parts of the country. Objectives: This study was designed to determine the chemical composition, in vitro antioxidant activity, and total phenol content of various extracts of S. chloroleuca. Materials and Methods: Dried aerial parts of the plant were crushed, then sequentially extracted with n-hexane, ethyl acetate, and methanol. The fractions of S. chloroleuca were subjected to silica gel column chromatography and Sephedex LH-20. The antioxidant activities of these extracts were measured by ferric reducing antioxidant power (FRAP), and the total phenolic contents of the extracts were evaluated using Folin-Ciocalteu reagent. Results: The separation and purification processes were carried out using different chromatographic methods. Structural elucidation was on the basis 1H-NMR and 13C-NMR spectral data, in comparison with that reported in the literature. The isolated compounds were salvigenin (1), luteolin (2), cirsiliol (3), β-sitosterol (4), and daucosterol (5). Ethyl acetate extract displayed the highest level of total antioxidants and total polyphenols compared to the other analyzed extracts (n-hexane and methanol). In the FRAP assay, ethyl acetate extract had the highest (230.4±10.5) FRAP value, followed by methanol (211.4 ± 8.3) and n-hexane (143.4 ± 12.04). Total phenol contents were calculated to be 13.8 ± 0.3, 58.25 ± 0.05, and 43.48 ± 0.38 mg of gallic acid/100 g in the n-hexane, ethyl acetate, and methanol extracts, respectively. Conclusions: The above-mentioned compounds were isolated for the first time from S. chloroleuca. The antioxidant activity of this plant could be in part related to isolated flavonoids and sterols. The results of this study indicated that S. chloroleuca could be an important dietary source of phenolic compounds with high antioxidant capacity.

Background Sanchezia speciosa has been used in traditional medicine for gastritis treatment in Vietnam. Some phytochemical study showed that S. speciosa contains high amounts of flavonoids and cardiac glycoside compounds. In the present study, we isolated four compounds from the ethanol extract of the S. speciosa leaf, and we evaluated the in vitro antioxidant and anti-inflammatory effect of the isolated compound from the ethanol extract of the S. speciosa leaf. Methods The leaf of S. speciosa Leonard was extracted with ethanol 96%. Compounds were isolated using column chromatography and identified by spectroscopic method, including IR, MS, and NMR and by comparing their physicochemical and spectral data with those published in literatures. These isolated compounds were investigated for their antioxidant activity using DPPH and inflammation inhibitory activity by inhibition of albumin denaturation assay. Results We have isolated four compounds quercetin 3-O-α-l-rhamnopyranosid (quercitrin) (1), quercetin 3-O-β-d-galactopyranosid (hyperosid) (2), sitosterol-3-O-β-D-glucopyranosid (daucosterol) (3), and 3-methyl-1H-benz[f]indole-4,9-dione (4) from the ethanolic extract of the S. speciosa leaf. The antioxidant activities were in the following order: compound 2>compound 1>compound 4>compound 3. The IC50 values of scavenging DPPH radicals for compound 2 was 20.83±1.29 μg/mL. For anti-inflammatory activities, the order was compound 4>compound 3>compound 2>compound 1. Compound 4 showed the strongest inhibition, with IC50 values of 193.70±5.24 µg/mL. Conclusions These compounds 1, 2, and 4 were isolated for the first time from the leaves of S. speciosa. These compounds showed strong antioxidant and anti-inflammatory activity.

Glutamate is a neurotransmitter in central nervous system. Overexpression of glutamate leads to oxidative stress, resulting in several neurodegenerative disorders that include Alzheimer's disease. The n-hexane fraction of stems and ethyl acetate (EtOAc) fraction of flowers of Reynoutria sachalinensis provide neuroprotection against glutamate-induced oxidative toxicity in HT22 cells. In this study, 1-decanol (1), β-amyrin (2), dammaran-3β-ol (3), campesterol (4), daucosterol (5), ergosterol peroxide (6), emodin 8-O-β-D-glucopyranoside (7), quercetin (8) and isoquercitrin (9) were isolated from n-hexane fractions of stems and EtOAc fractions of flowers of R. sachalinensis. Their neuroprotective activity was evaluated by MTT assay. 1-Decanol, campesterol, ergosterol peroxide, quercetin and isoquercitrin exhibited neuroprotective activity. These compounds decreased reactive oxygen species level, showed anti-oxidant activity with DPPH radical and in a H2O2 scavenging assay. Therefore, the neuroprotective activity of 1-decanol, campesterol, ergosterol peroxide, quercetin and isoquercitrin are associated with antioxidant activity.

Phytochemical investigation of Cleome iberica DC. aerial parts led to the isolation and characterisation of six triterpenoid including glutinol (1), lupeol (2), β-sitosterol (3), cabraleadiol monoacetate (4), cabraleadiol (6) and daucosterol (8), one flavonoid, calycopterin (5) along with a fatty acid, tricosanoic acid (7). While studied samples showed weak potency in antimicrobial assessment, the acetone extract and some isolated compounds exhibited considerable cytotoxicity against cervical cancer cell line (HeLa) in MTT assay, among them calycopterin with IC50 equals to 5.1 μM was the strongest. The extract showed moderate antioxidant capacity in DPPH assay method (IC50 = 100.2 μg/mL) and total phenolics and total flavonoids contents of the dried extract were also determined as 39.6 and 90.7 mg/g, respectively.

The aim of this research was to investigate the antibacterial activity of Parasenecio pseudotaimingasa, a perennial plant belonging to the Asteraceae, tribe Senecioneae. The methanol extract, n-hexane fraction, and n-butanol fraction of P. pseudotaimingasa leaves all exhibited antibacterial activities against Escherichia coli and Staphylococcus aureus, forming inhibition zones greater than 11 mm in discs. Among them, the n-hexane fraction showed the highest antibacterial activity against E. coli and S. aureus, with an inhibition zone greater than 14 mm. Open-column chromatography was used to isolate the phytochemical constituents from the n-hexane fraction; spectroscopic analysis elucidated their structures as β-sitosterol and daucosterol. Further testing of β-sitosterol and daucosterol also revealed the antibacterial effects against both E. coli and S. aureus, suggesting their potential as antibacterial agents.

Siraitia grosvenorii, an herbaceous perennial vine, is native to Southern China and Northern Thailand. This species is well known for its fruit, which is commonly called “luo han guo” or “luo han kuo” in Chinese; “la han qua” in Vietnamese; or arhat, Buddha, or monk fruit in English. Phytochemical research has shown that the fruit of this species is rich in triterpene glycosides that are very sweet, low in calories, and may be used as a substitute for sugar. In addition, many compounds have been isolated from the vines and leaves of S. grosvenorii, including β-amyrin, aloe emodin, aloe-emodin acetate, 5α,8α-epidioxy-24(R)-methylcholesta-6,22-dien-3β-ol, p-hydroxyl benzyl acid, n-hexadecaoic acid, 12-methyltetradecanoic acid, β-sitosterol, and daucosterol. Moreover, a new flavandiol, siraitiflavandiol, has been obtained from ripe S. grosvenorii fruit, while 2 kaempferol glycosides have been isolated from the unripe fruit. Pharmacological results have also shown that S. grosvenorii extracts and purified mogrosides exhibit antidiabetic, anticarcinogenic, antibacterial, antioxidant, and antiallergic effects. Overall, S. grosvenorii could potentially serve as an important source of pharmaceutical and sweetener compounds for a wide range of food products.

This study describes the activity-guided isolation of antioxidant agents from tartary buckwheat bran (TBB). The ethanol crude extract of oil-free TBB was partitioned sequentially into ethyl acetate, n-butanol, and residual aqueous fractions. The ethyl acetate fraction (EAF) had the highest phenolic and flavonoid contents and showed the strongest antioxidant activity. EAF was superior to rutin and inferior to vitamin C (Vc) in DPPH radical scavenging ability, had an advantage over rutin and Vc in ABTS radical scavenging ability, and again surpassed rutin and quercetin in reducing power. Then EAF was subjected to column chromatography, and isolated compounds were identified using nuclear magnetic resonance data by comparing with those reported in the literature. Finally, the bioassay-guided fractionation of the crude ethanol extract of TBB afforded three known compounds (quercetin, p-hydroxybenzoic acid, and daucosterol) responsible for antioxidant activity. p-Hydroxybenzoic acid and daucosterol we...

The first phytochemical investigation on Saniculiphyllum guangxiense resulted in the isolation of two new triterpenoids, 16 beta-hydroxybryodulcosigenin (3) and 3a-O-feruloylolean-12-en-27-oic acid (6), together with six known compounds, menisdaurin (1), purshianin (2), oleanolic acid (4), 3 beta-hydroxyolean-12-en-27-oic acid (5), beta-sitosterol (7), and daucosterol (8), which were characterized by extensive spectroscopic analyses and in one case by X-ray diffraction. According to this primary investigation, S. guangxiense is rich in nitrile glucosides and triterpenoids, of which menisdaurin (1; 0.06%) and purshianin (2; 0.015%) are the main constituents. Compounds 16 were assayed for their anti-hepatitis B virus (HBV) activities against the secretion of HBsAg and HBeAg, as well as HBV DNA replication on Hep G 2.2.15 cell line in vitro. The most active compound, menisdaurin (1), inhibits HBV DNA replication with an IC50 value of 0.32 mM (SI>11.97).

Aim To investigate the chemical constituents from the aerial parts of Angelica sinensis and their anticoagulative and antibiotic activities. Methods The constituents of the 80% ethanol extract were isolated and purified by various chromatographic methods. Their structures were identified by the physicochemical characteristic and spectral data. The anticoagulative activity of the isolated compounds were tested using the thrombin time method assay, and the antibiotic activity were tested using the serial two-fold dilution method. Results Thirteen known compounds were isolated and identified as 24, 24-dimethyl-9,19-cyclolanostan-3β-ol ( 1 ), β-sitosterol ( 2 ), 2, 3, 6-trimethylbenzoic acid ( 3 ), uracil ( 4 ), daucosterol ( 5 ), hyperoside ( 6 ), allantoin ( 7 ), D-mannitol ( 8 ), 1 S -(4′-hydroxyphenyl)-1, 2-ethanediol ( 9 ), caffeic acid ( 10 ), chlorogenic acid ( 11 ), sucrose ( 12 ) and D-glucose ( 13 ). Compounds 3 , 4 , 6 , 7 , 9 , 10 and 11 moderately prolonged thrombin time. Compounds 1 , 4 , 6 , 7 and 9 significantly inhibited the growth of Aeromonas hydrophila . Conclusion Compounds 1 , 3 , 6 - 9 were isolated from this plant for the first time. Compounds 1 , 3 , 4 , 6 , 7 , 9 , 10 and 11 are the important active constituents of the aerial parts of Angelica sinensis .

Hou J.P., Wu H., Wang Y., Weng X.C. (2012): Isolation of some compounds from nutmeg and their antioxidant activities. Czech J. Food Sci., 30: 164–170. Six compounds, licarin-B (1), dehydrodiisoeugenol (2), malabaricone B (3), malabaricone C (4), β-sitosterol (5), and daucosterol (6) were isolated from the seed (nutmeg) of Myristica fragrans Houtt and identified. Among them, malabaricone B was identified for the first time in nutmeg. Antioxidant activities of the isolated compounds were studied using oil stability index (OSI), reducing power, ABTS ●+ scavenging, and DPPH ● scavenging methods. The results showed that Malabaricone C is an efficient antioxidant agent which exhibits a stronger antioxidant activity than the commonly used synthetic antioxidants in all studied methods. This compound may have a potential to be used as a natural antioxidant in food.

RATIONALE Carbohydrates are good source of drugs and play important roles in metabolism processes and cellular interactions in organisms. Distinguishing monosaccharide isomers in saccharide derivates is an important and elementary work in investigating saccharides. It is important to develop a fast, simple and direct method for this purpose, which is described in this study. METHODS Stock solutions of monosaccharide with a concentration of 400 mu M and sodium chloride at a concentration of 10 mu M were made in water/methanol (50:50, v/v). The samples were subjected to electrospray ionization ion-trap tandem mass spectrometry (ESI-MS) and the detected [2M?+?Na H2O]+ ions were further investigated by tandem mass spectrometry (MS/MS), followed by applying principal component analysis (PCA) on the obtained MS/MS data sets. RESULTS The MS/MS spectra of the [2M?+?Na H2O]+ ions at m/z 365 for hexoses and m/z 305 for pentoses yielded unambiguous fragment patterns, while rhamnose can be directly identified by its ESI-MS [M?+?Na]+ ion at m/z 187. PCA showed clustering of MS/MS data of identical monosaccharide samples obtained from different experiments. By using this method, the monosaccharide in daucosterol hydrolysate was successfully identified. CONCLUSIONS A new strategy was developed for differentiation of the monosaccharides using ESI-MS/MS and PCA. In MS/MS spectra, the [2M?+?Na H2O]+ ions yielded unambiguous distinction. PCA of the archived MS/MS data sets was applied to demonstrate the spatial resolution of the studied samples. This method presented a simple and reliable way for distinguishing monosaccharides by ESI-MS/MS. Copyright (C) 2012 John Wiley & Sons, Ltd.

This study was designed to investigate the mushroom tyrosinase inhibitory activity for the constituents isolated from Neolitsea aciculata. The stems of N. aciculata was extracted with aqueous ethanol and subjected to chromatographic separation, which led to the isolation of 11 compounds: methyl linoleate (1), catechin (2), epicatechin (3), afzelin-7-O-glucopyranoside (4), 2',3'-di-(p-coumaroyl)afzelin (5), 2'-p-coumaroylafzelin (6), feruloyl tyramine (7), β-sitosterol (8), daucosterol (9), oleic acid (10), and trilaurin (11). Their structures were elucidated on the basis of spectroscopic studies as well as by comparison with the data available in the literature. Among these isolates, compounds 5 and 6 were identified as potent mushroom tyrosinase inhibitors with IC₅₀ values of 0.067 and 0.080 mM, respectively. The inhibition kinetics, analysed by Lineweaver-Burk plots, indicated that compounds 5 and 6 are competitive tyrosinase inhibitors when using l-tyrosine as a substrate. Notably, compounds 1-11 were isolated for the first time from this plant. These results provide evidence that this plant might be a potential source of anti-melanogenesis agents.

Definitive identification of original plant species is important for standardizing herbal medicine. Although only the dried roots of Cynanchum wilfordii (Asclepiadaceae) are prescribed as Cynanchi Wilfordii Radix in Korean Pharmacopoeia, the roots of C. wilfordii and C. auriculatum are often misused in the Korean herbal market due to their morphological similarity and similar name. Therefore, it would be very useful to discover an effective chemical marker for the identification of the two species. To this end, we carried out a phytochemical study on the roots of C. wilfordii. As a result, twenty compounds were isolated from the roots of C. wilfordii and their chemical structures were identified as β-sitosterol (1), wilfoside C1N (2), wilfoside C3N (3), wilfoside K1N (4), methyleugenol (5), wilfoside C1G (6), cynauriculoside A (7), daucosterol (8), 2,4-dihydroxyacetophenone (9), cynandione A (10), 2,5-dihydroxyacetophenone (11), acetovanillone (12), p-hydroxyacetophenone (13), sucrose (14), conduritol F (15), geniposide (16), succinic acid (17), 3-(β-D-ribofuranosyl)-2,3-dihydro-6H-1,3-oxazine-2,6-dione (18), bungeiside A (19), cynanoneside B (20). Among them, compounds 15, 16, 18, 19, and 20 were isolated for the first time from this species. Furthermore, conduritol F (15) was demonstrated to be contained only in C. wilfordii. Therefore, it may be useful as a chemical marker to identify the two species C. wilfordii and C. auriculatum.

The rhizomes of Hedychium coronarium have been used for the treatment of inflammation, skin diseases, headache, and sharp pain due to rheumatism in traditional medicine. From this plant, three new labdane-type diterpenes 1-3, named coronarins G-I as well as seven known 4-10, coronarin D, coronarin D methyl ether, hedyforrestin C, (E)-nerolidol, β-sitosterol, daucosterol, and stigmasterol were isolated. Their chemical structures were elucidated by mass, 1D- and 2D-nuclear magnetic resonance spectroscopy. They were evaluated for inhibitory effects on lipopolysaccharide-stimulated production of pro-inflammatory cytokines in bone marrow-derived dendritic cells. Among of them, compounds 1, 2, and 6 were significant inhibitors of LPS-stimulated TNF-α, IL-6, and IL-12 p40 productions with IC(50) ranging from 0.19±0.11 to 10.38±2.34 μM. The remains of compounds showed inactivity or due to cytotoxicity. These results warrant further studies concerning the potential anti-inflammatory benefits of labdane-type diterpenes from H. coronarium.

From the ethyl acetate extract of the seeds of Vietnamese Cnidium monnieri L., three coumarins, osthole (1), xanthotoxin (2), imperatorin (3) and a sterol, daucosterol (4) have been purified. Their structures were elucidated by spectroscopic analysis. Furthermore, 8-(3-hidroxy-3-methylbutyl)-7-methoxycoumarin (5) was synthesised from osthole (1) with a good yield (80%). In addition, compound 1 and its synthesis product (5) show moderate and non-selective cytotoxic activities against four cancer cells, KB (a human epidermal carcinoma), MCF7 (human breast carcinoma), SK-LU-1 (human lung carcinoma) and HepG2 (hepatocellular carcinoma).

Ethnopharmacological relevance Commiphora berryi is traditionally used for the treatment of cold and fever as well as for wound healing in the southern parts of India. Aim of study The present study was designed to investigate in vitro soybean lipoxygenase inhibitory activity of crude extracts and compounds isolated from Commiphora berryi . Materials and methods The bark of Commiphora berryi was extracted with different organic solvents and subjected to chromatographic separation for isolation of bioactive compounds. Structures of isolated compounds were elucidated by spectroscopic methods. The anti-inflammatory activity of bark extracts and bioactive compounds were assessed by in vitro soybean lipoxygenase (SBL) assay. Results 3β-Hydroxyglutin-5-ene ( 1 ), friedelin ( 2 ), cycloeucaneol ( 3 ) nimbiol ( 4 ), sugiol ( 5 ), surianol ( 6 ), daucosterol ( 7 ) and ursolic acid ( 8 ) were isolated from crude bark extracts of the Commiphora berryi . The structure of nimbiol ( 4 ) was also confirmed by single crystal X-ray analysis. The petroleum ether, methanol, chloroform and ethyl acetate extracts of bark of Commiphora berryi showed SBL inhibitory activity with the IC 50 values of 15.3, 54.2, 71.5 and 87.8 μg/ml respectively. Among all the isolates, friedelin ( 2 ) showed significant SBL inhibitory activity with IC 50 35.8 μM. Conclusion The overall results provide evidence that the studied plant might be a potential source of anti-inflammatory agents.

Urtica angustifolia is a traditional medicinal material which has hypoglycemic function. The objectives of this study were to isolate and identify hypoglycemic active ingredients from it. Three groups of mice were gavaged with the decoction of Urtica root, stem and leaf for 14 days at a dose of 20 mg/(kg·d). Area under the curve (AUC) values were 24.62±5.24, 24.33±4.66 and 25.51±4.25, respectively. The AUC in leaf decoction group was significantly lower than the other two groups (P < 0.05), which indicated the leaf extracts did have significant hypoglycemic action. Four kinds of extractions were obtained from leaves and fed to mice. AUC values were 33.44±3.58, 34.24±3.64, 30.44±2.57 and 9.93±1.98, respectively. AUC in group U3 (P < 0.05) and U4 (P < 0.01) were significantly lower than in the group of U1 and U2, which indicated that extraction U3 and U4 obviously decreased the blood sugar. Also, U3 was flavonoid and U4 was daucosterol, which was identified by thin-layer chromatography test, IR and ESI-MS spectral analysis.Key words: Urtica angustifolia, active component, glucose tolerance test, hypoglycemic.

Xanthium sibiricum patrin ex Widder (Compositae) is an annual herb which grows all around China. Chemical investigations of its roots resulted in the identification of 15 compounds: stigmast-4-en-6β-ol-3-one (1), β-sitostenone (2), β-sitosterol (3), nonadecanoic acid (4), 5α,8α-epidioxy-22E-ergosta-6,22-dien-3β-ol (5), scopoletin (6), Jatrocin B (7), (±)syringaresinol (8), 9,9'-O-di-(E)-feruloyl-(-)-secoisolariciresinol (9), cleomiscosin A (10), cleomiscosin C (11), N-trans-feruloyl tyramine (12), daucosterol (13), 5-methyluracil (14) and uracil (15). Structures were elucidated by spectroscopic (NMR and MS) methods and confirmed by comparing with reference samples and literature data. Compounds 1-2, 4-12, 14, and 15 were isolated from this genus for the first time, while this is the first report of coumarinolignoids in the Compositae family, and coumarinoligoids could be considered as valuable chemotaxonomic markers for the plant.