In order to search for bioactive natural products from marine algae, the chemical constituents of red alga Laurencia saitoi was separated by the combination of normal phase silica gel, Sephadex LH-20 column chromatography and recrystallization. Seven compounds: aplysistatin (1), 5-acetoxypalisadin B (2), palisadin B (3), palisadin A (4), pacifigorgiol (5), stigmast4-en-3alpha, 6beta-diol (6), 2, 3, 5, 6-Tetrabromoindole (7), were isolated and their structures were elucidated by spectroscopic methods including 1H-NMR, 13C-NMR and MS techniques. All compounds were isolated from L. saitoi for the first time. Cytotoxicities of purified compounds were evaluated by MTT method, however, all of them were found inactive (IC50 >10 mg x L(-1).
Cell Line, Tumor ; Humans ; Inhibitory Concentration 50 ; Laurencia ; chemistry ; Organic Chemicals ; chemistry ; isolation & purification ; pharmacology

OBJECTIVETo summarize the studies on chemical constituents and pharmacological activities of lichens of Usnea genus.

METHODA systematic literature survey was conducted to classifiy and summarize chemical constituents of lichens of Usnea genus, and sum up current studies on main pharmacological activities of lichens of the genus.

RESULTLichens of Usnea genus contained multiple chemical constituents, primarily including mono-substituted phenyl rings, depsides, anthraquinones, dibenzofurans, steroids, terpenes, fatty acids and polysaccharides, with such biological activities as antitumor, antibacterial, anti-inflammation, anti-oxidation and antithrombosis.

CONCLUSIONThis essay provides reference for further studies and development of lichens of Usnea genus.

Animals ; Humans ; Medicine, Chinese Traditional ; methods ; Organic Chemicals ; chemistry ; pharmacology ; Usnea ; chemistry

OBJECTIVETo study the hemostatic effect of chemical constituents from Callicarpa nudiflora.

METHODThe chemical constituents were isolated and purified via silica gel and Sephadex LH-20 column chromatography. Their structures were determined on the basis of spectral analysis. prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT) and fibrinogen (FIB) of the constituents rabbit blood samples were tested with rabbit blood in vitro.

RESULTEleven compounds were isolated and identified as two diterpenens: 7alpha-hydroxy sandaracopimaric acid (1), 16, 17-dihydroxy-3-oxophyllocladane (2). Two phenoic glycosides: acteoside (3), samioside(4). Three triterpenes: 2alpha, 3alpha, 24-trihydroxy-ursa-12-en-28-oic acid (5), 2alpha, 3alpha, 19alpha-trihydroxyursa-12-en-28-oic acid-28-0-beta-D-glucopyranosyl ester (6), and 2alpha, 3alpha, 19alpha, 23-tetrahydroxy-ursa-12-en-28-oic acid-28-0-beta-D-glucopyranosyl ester (7). Four flavones: rhamnazin (8), 5-Hydroxy-3, 7, 4'-trimethoxy-flavone (9) , 5-Hydroxy-3, 7, 3', 4'-tetramethoxyflavone (10), and luteoloside (11). All Compounds cannot significantly shorten the PT (P < 0.01), compounds 3, 4, 7, 10 can remarkedly increase APTT (P < 0.01), compound 5 can prolong the T( P < 0.01) obviously, and compound 8 can significantly increase the contents of FIB (P < 0.01).

CONCLUSIONCompounds 2, 4 and 10 were isolated from this genus for the first time, and compounds 1, 3, 5, 6, 7 and 9 had been isolated from this plant for the first time. The hemostatic effect of C. nudiflora may be related to the activation of the intrinsic blood coagulation system.

Animals ; Blood Coagulation Factors ; metabolism ; Callicarpa ; chemistry ; Hemostasis ; drug effects ; Male ; Organic Chemicals ; analysis ; pharmacology ; Rabbits

OBJECTIVETo investigate the chemical constituents of an endophytic fungus, Nodulisporium sp. A4, from the medicinal plant Aquilaria sinensis and search for antitumor natural products.

METHODThe fungus was cultured in liquid medium and extracted with EtOAc. The compounds were isolated by various chromatographic methods (silica gel, reverse silica gel, Sephadex-LH20, preparative TLC and so on) and recrystallization. Structural elucidation was conducted by extensive analysis of spectroscopic data as well as by comparison with literature reports. The antitumor activity of isolated compounds was tested by MTT method in vitro.

RESULTSeven compounds were isolated and identified from the broth culture, their structures were determined to be 5-methyl-2-vinyltetrahydrofuran-3-ol (1), 6-methyl-2-(5-methyl-5-vinyltetrahydrofuran-2-yl) hept-5-en-2-ol (2), 6alpha-hydroxycyclonerolidol (3), rel-(1S,4S, 5R,7R,10R)-10-desmethyl-1-methyl-11-eudesmene (4), tyrosol (5), 8-methoxynaphthalen-1-ol (6), and 1,8-dimethoxynaphthalene (7). Three compounds were isolated and identified from the mycelia as ergosterol (8), ergosterol peroxide (9), and cerevisterol (10). The in vitro pharmalogical evaluation results displayed that compounds 3 and 4 showed 89.1%, 44.2% and 82.3%, 79.8% inhibition against tumor cell lines SF268 and NCI-H460 at 100 mg x L(-1), respectively.

CONCLUSIONCompound 1 was a new natural product, compounds 2, 3, 7 and 10 were reported from the genus Nodulisporium sp. for the first time. Compounds 3 and 4 exhibited weak inhibitory effects on the proliferation of tumor cell lines SF268 and NCI-H460.

Cell Line, Tumor ; Cell Proliferation ; drug effects ; Endophytes ; chemistry ; Humans ; Organic Chemicals ; chemistry ; isolation & purification ; pharmacology ; Thymelaeaceae ; microbiology ; Xylariales ; chemistry

OBJECTIVEThe four major active compositions, namely esculetin, lactucin, lactucopicrin and chlorogenic acid in seed, stem and root of the Cichorium glandulosum Boiss. et Huet that planted in Xinjiang have been quantified by HPLC.

METHODHPLC method was used, with Inertsil ODS-SP column (4.6 mm x 250 mm, 5 pm). The flow rate was 1.0 mL x min(-1). The column temperature was set at 32 degrees C. The mobile phase was methanol--0.2% formic acid, 0-40 min, methanol 30%--70% gradients. Injection volume was 5 microL. The detecting wavelength were 256, 350, 299 and 229 nm, respectively.

RESULTThe percentage recoveries were 98.2%, 99.57%, 100.50%, and 99.46% for chlorogenic acid, esculetin, lactucin, and lactucopicrin, respectively. The correlation coefficients (r) were 1.000, 0.9989, 0.9998, 1.000 and RSD were 1.6%, 1.5%, 0.77%, 2.0% for chlorogenic acid, esculetin, lactucin, and lactucopicrin, respectively. The contents of the chlorogenic acid, esculetin, lactucin and lactucopicrin were 0.0048, 0.0043, 0.6789, 0.7520 mg x g(-1), respectively in the root, and 0.0710, 0.1890, 0.2396 and 0.0520 mg x g(-1) in the seeds of C. glandulosum, respectively.

CONCLUSIONThis method was sensitive, rapid and simple, with good linearity, recovery and reproducibility.

Asteraceae ; chemistry ; Chromatography, High Pressure Liquid ; Linear Models ; Organic Chemicals ; analysis ; chemistry ; pharmacology ; Plant Structures ; chemistry ; Quality Control ; Reproducibility of Results

Polypore fungi is a cluster of important pharmacological fungi with significant antitumor activity. In recent years, the antineoplastic constituents from polypore fungi have been comprehensively studied. Through investigating the domestic and overseas studied paper, the antitumor active constituents derived from polypore fungi including high molecular weight compounds such as polysaccharides, glycopeptides, glycoproteins, lectins, and lipid soluble low molecular weight compounds such as terpenoids, steroids, phenolics, benzopyranones, were reviewed. In addition, the significance in the exploitation of new drug for antitumor by the application of polypore fungi was discussed at the end of this paper.
Animals ; Antineoplastic Agents ; chemistry ; isolation & purification ; pharmacology ; Fungi ; chemistry ; Humans ; Macromolecular Substances ; chemistry ; isolation & purification ; pharmacology ; Molecular Weight ; Organic Chemicals ; chemistry ; isolation & purification ; pharmacology ; Polyporus ; chemistry ; Solubility

OBJECTIVETo investigate the chemical constituents of the culture of Phellinus igniarius and their phamacological activities.

METHODThe constituents were isolated by using a combination of various chromatographic techniques including column chromatography over silica gel, Sephadex LH-20, and reversed-phase HPLC. Structures of the isolates were identified by spectroscopic data analysis. Cytotoxic, neuroprotective, hepatoprotective, anti-inflammatory, and anti-HIV activities were screened by using cell-based models.

RESULTTwenty-nine constituents were isolated. Their structures were identified as three sesquiterpenes: 3S,9R,10S-3-hydroxy-11, 12-O-isopropyldrimene(1), 3S, 9R, 10S-3, 11, 12-trihydroxydrimene (2), and 3S, 4S, 9R, 10S-11, 12, 14-trihydroxydrimene(3); three steriods: 24R-ergosta-4, 6, 8(14), 22-tetraen-3-one (4), stigmasta-7, 22-diene-3b, 5a, 6a-triol (5), and 5a, 8a-epi dioxyergosta-6, 22-diene-3b-ol (6); fourteen cyclo-dipeptide: cyclo (L-Pro-L-Val) (7), cycle (L-Leu-D-Pro) (8), cyclo (L-Leu-L-Pro) (9), cyclo (ILe-Pro) (10), cyclo (Gly-Leu) (11), cyclo (Phe-Ser) (12), cyclo (Ala-Pro) (13), cyclo (Ala-Phe) (14), cyclo (4-HyP-Phe) (15) , cyclo (L-Phe-D-Pro) (16), cyclo (D-Phe-D-Pro) (17), cyclo (6-HyP-Phe) (18), cycle (Gln-Pro) (19), and cycle (Asn-Leu) (20); and nine other compounds: N-acetyl-phenylalanine (21), adenosine (22), phenyldiethanol (23), o-hydroxy-phenylethanol (24), benzoic acid (25), p-methoxybenzoic acid (26), m-methoxybenzoic acid (27), hexadecanoic acid (28), and 3-pyridinecarboxylic acid (29). In the in vitro assays, at a concentration of 1 x 10(-5) mol x L(-1), compounds 5 and 8 showed neuroprotective activity against MPP+ induced PC12-syn cell damage, with a relative cell proliferation rate of 90.3% and 87.5% (P < 0.05). At 1 x 10(-5) mol x L(-1), compounds 12 and 18 showed hepatoprotective activities against DL-galactosamine-induced toxicity examined in WB-F344 cell, with cell survival rates of 25% and 24%, respectivily.

CONCLUSIONCompounds 1-29 were obtained from P. igniarius for the first time. Compounds 5 and 8 showed potent PC12-syn protective activities, while 12 and 18 showed hepato cytes (WB-F344 cells) protective activities.

Animals ; Basidiomycota ; chemistry ; growth & development ; Cell Proliferation ; drug effects ; Culture Techniques ; Hepatocytes ; cytology ; drug effects ; Neuroprotective Agents ; analysis ; pharmacology ; Organic Chemicals ; analysis ; pharmacology ; PC12 Cells ; drug effects ; Rats

OBJECTIVETo investigate the effect of Angelica polysaccharide (APS), platelet-derived growth factor (PDGF) and thrombopoietin (TPO) on the proliferation and apoptosis of human megakaryocytic cell line M-07e.

METHODSCell count and the viability testing of M-07e cells (trypan blue exclusion assay) were performed at 24 hours, 48 hours and 72 hours after treatment with APS, PDGF or TPO. Three apoptosis related flow cytometric assays including Annexin V, Caspase-3 and JC-1 were performed to determine apoptotic rate of each group at 72 hours after the treatment.

RESULTSAfter the incubation, the number of M-07e cells in the APS, PDGF and TPO group increased and the viabilities of the three groups were significantly higher than the control group (P < 0.05). The dead cells in the APS, PDGF and TPO group were (19.41 +/- 7.59)%, (21.38 +/- 7.25)% and (18.77 +/- 8.00)%, respectively by flow cytometry using Annexin V method, which were significantly lower compared to the control group (34.33 +/- 5.46)%. The expression of the activated caspase-3 in the group of APS, PDGF and TPO were (12.27 +/- 5.18)%, (12.39 +/- 6.26)% and (13.75 +/- 8.25)%, the APS and PDGF group decreased significantly compared to the control group (18.92 +/- 6.09)%. The ratio of total cell deaths in the APS, PDGF and TPO group were (23.64 +/- 6.69)%, (28.00 +/- 10.05)% and (27.99 +/- 8.99)%, the ratio in APS group decreased significantly compared to the control group (39.48 +/- 11.86)% by JC-1 method. Differences between APS and PDGF groups and between APS and TPO groups were not statistically significant.

CONCLUSIONAPS, PDGF and TPO have similar effect in stimulating proliferation and inhibiting serum-free-culture induced apoptosis of M-07e cells.

Angelica ; chemistry ; Apoptosis ; drug effects ; Benzimidazoles ; pharmacology ; Carbocyanines ; pharmacology ; Caspase 3 ; metabolism ; Cell Proliferation ; drug effects ; Flow Cytometry ; Fluorescent Dyes ; pharmacology ; Humans ; Megakaryocytes ; drug effects ; physiology ; Organic Chemicals ; pharmacology ; Platelet-Derived Growth Factor ; pharmacology ; Thrombopoiesis ; Thrombopoietin ; pharmacology

Epidemiologic studies have suggested the association between environmental exposure to volatile organic compounds (VOCs) and polycyclic aromatic hydrocarbons (PAHs) and the increased risk of incurring asthma. Yet there is little data regarding the relationship between personal exposure to air pollution and the incidence of asthma in children. This study was designed to evaluate the effect of exposure to air pollution on children with asthma by using exposure biomarkers. We assessed the exposure level to VOCs by measuring urinary concentrations of hippuric acid and muconic acid, and PAHs by 1-OH pyrene and 2-naphthol in 30 children with asthma and 30 children without asthma (control). The mean level of hippuric acid was 0.158+/-0.169micromol/mol creatinine in the asthma group and 0.148+/-0.249micromol/mol creatinine in the control group, with no statistical significance noted (p=0.30). The mean concentration of muconic acid was higher in the asthma group than in the control group (7.630+/-8.915micromol/mol creatinine vs. 3.390+/-4.526micromol/mol creatinine p=0.01). The mean level of urinary 1-OHP was higher in the asthma group (0.430+/-0.343micromol/mol creatinine) than the control group (0.239+/-0.175micromol/mol creatinine), which was statistically significant (p=0.03). There was no difference in the mean concentration of 2-NAP between the two groups (9.864+/-10.037micromol/mol in the asthma group vs. 9.157+/-9.640micromol/mol in the control group, p=0.96). In conclusion, this study suggests that VOCs and PAHs have some role in asthma.
Air Pollutants/*pharmacology ; Asthma/*physiopathology/urine ; Case-Control Studies ; Child, Preschool ; Creatinine/urine ; Female ; Hippurates/urine ; Humans ; Male ; Naphthols/urine ; Organic Chemicals/chemistry/*pharmacology ; Polycyclic Hydrocarbons, Aromatic/*pharmacology ; Pyrenes/metabolism ; Sorbic Acid/*analogs & derivatives/metabolism ; Volatilization

The difference between absorption of unfractionated heparin (UFH) and low molecular weight heparin (LMWH) after oral and oral cavity administration were studied respectively, and the compatible enhancer for oral cavity delivery system of both drugs was found. The LMWH and UFH films were prepared with two bioadhesive materials Carbopol and alginate sodium for oral cavity delivery. The activated partial thromboplastin time (APTT) was used to determine LMWH and UFH in plasma after oral, oral cavity and sc administration in rats. The results show that the enhancer (Labrasol) can increase the absorption of LMWH and UFH through oral cavity in rats but not obviously. The oral cavity iontophoretic delivery system is a useful method to improve the absorption of LMWH and UFH through oral cavity mucosa.
Absorption ; Acrylic Resins ; Administration, Oral ; Alginates ; chemistry ; Animals ; Anticoagulants ; administration & dosage ; pharmacokinetics ; Drug Carriers ; Drug Delivery Systems ; Glucuronic Acid ; chemistry ; Glycerides ; Heparin ; administration & dosage ; pharmacokinetics ; Heparin, Low-Molecular-Weight ; administration & dosage ; pharmacokinetics ; Hexuronic Acids ; chemistry ; Injections, Intradermal ; Iontophoresis ; Male ; Mouth ; Organic Chemicals ; pharmacology ; Partial Thromboplastin Time ; Polyvinyls ; chemistry ; Rats ; Rats, Sprague-Dawley