Xanthomonas albilineans (Ashby) Downson is a quarantine pest for importing plants to China that causes leaf scald bacterial disease on sugarcane. X. albilineans produces a potent phytotoxin/antibiotic called albicidin. As a pathogenic factor, albicidin causes typical white leaf stripes by inhibiting plastid DNA gyrase and disturbing chloroplast differentiation. Meanwhile, the antibacterial activity of albicidin gives X. albilineans a competitive advantage against rival bacteria during their colonization. Furthermore, albicidin has a rapid bactericidal activity against a variety of Gram-positive and Gram-negative pathogenic bacteria of human species at nanomolar concentrations, making it a potential antimicrobial drug for clinical application. This article reviews the advances of albicidin from the aspects of its molecular structure, traditional extraction methods, mechanism of action, biosynthetic genes and processes, chemical synthesis method and improvement, in order to provide insights into the prevention and treatment of the sugarcane leaf scald disease, and the development of new antibiotics.
Anti-Bacterial Agents/pharmacology* ; China ; Humans ; Organic Chemicals ; Xanthomonas/genetics*

OBJECTIVETo study the effects of LIF combined with bFGF on the proliferation, stemness and senescence of hUC-MSC.

METHODSExperiments were divided into 4 groups: control group, in which the cells were treated with complete medium (α-MEM containing 10% FBS); group LIF, in which the cells were treated with complete medium containing 10 ng/ml LIF; group bFGF, in which the cells were treated with complete medium containing 10 ng/ml bFGF; combination group, in which the cells were treated with complete medium containing 10 ng/ml LIF and 10 ng/ml bFGF. The growth curves of hUC-MSC at passage 4 in different groups were assayed by cell counting kit 8. Cellular morphologic changes were observed under inverted phase contrast microscope; hUC-MSC senescence in different groups was detected by β-galactosidase staining. The expression of PCNA, P16, P21, P53, OCT4 and NANOG genes was detected by RT-PCR.

RESULTSThe cell growth curves of each group were similar to the S-shape; the cell proliferation rate from high to low as follows: that in the combination group > group bFGF > group LIF > control group. Senescence and declining of proliferation were observed at hUC-MSC very early in control group; the cells in group LIF maintained good cellular morphology at early stage, but cell proliferation was slow and late senescence was observed; a few cells in group bFGF presented signs of senescence, but with quick proliferation; the cells in combination group grew quickly and maintained cellular morphology of hUC-MSC for long time. The LIF and bFGF up-regulated the expression of PCNA, OCT4 and NANOG, while they down-regulated the expression of P16, P21, P53, and their combinative effects were more significant.

CONCLUSIONLIF combined with bFGF not only can promote the proliferation and maintenance of stemness of hUC-MSC, but also can delay the senescence of hUC-MSC.

Cell Cycle ; Cell Differentiation ; Cell Proliferation ; Cells, Cultured ; Cyclin-Dependent Kinase Inhibitor p16 ; metabolism ; Cyclin-Dependent Kinase Inhibitor p21 ; metabolism ; Fibroblast Growth Factor 2 ; pharmacology ; Genes, Homeobox ; Humans ; Leukemia Inhibitory Factor ; pharmacology ; Mesenchymal Stromal Cells ; cytology ; drug effects ; Octamer Transcription Factor-3 ; metabolism ; Organic Chemicals ; Proliferating Cell Nuclear Antigen ; metabolism ; Tumor Suppressor Protein p53 ; metabolism ; Umbilical Cord ; cytology

OBJECTIVETo investigate the effect of transforming growth factor-β1 (TGF-β1) on the differentiation of bone marrow-derived mesenchymal stem cells (MSCs) into cancer-associated fibroblasts(CAFs).

METHODSMSCs were cultured in α-MEM with recombinant human TGF-β1 or in tumor-conditioned medium.The expression of CAFs markers were detected by immunofluorescence and quantitative RT-PCR.

RESULTSThe qRT-PCR assay showed that the expression of CAFs markers FAP, ACTA, CAV, CCL5, CXCR4, FSP1, SDF-1 and vimentin were 9.92±2.16, 7.76±1.28, 3.04±0.95, 3.28±2.16, 2.13±0.71, 1.41±0.66, 2.25±0.86 and 1.38±0.56, respectively, significantly upregulated in the MSCs co-cultured with TGF-β1 or TCM. The relative levels of FAP, ACTA, CAV, CCL5, CXCR4, FSP1, SDF-1 and vimentin mRNA in the TCM group were 7.52±1.76, 5.02±1.18, 1.98±1.19, 1.82±1.19, 2.95±0.86, 1.44±0.67, 2.08±0.74 and 1.47±0.55, respectively, indicating that MSCs can express CAFs phenotype.TGF beta signaling pathway inhibitor SB-431542 could inhibit the differentiation. Both immunofluorescence and Western blot confirmed the above results.

CONCLUSIONSTGF-β1 induces differentiation of local MSCs to CAFs by upregulating the expression of pSmad3, so as to further promote the growth of cancer cells.

Benzamides ; pharmacology ; Bone Marrow Cells ; cytology ; Cell Differentiation ; drug effects ; Cell Line, Tumor ; Chemokine CXCL12 ; metabolism ; Coculture Techniques ; Culture Media, Conditioned ; Dioxoles ; pharmacology ; Fibroblasts ; cytology ; Humans ; Mesenchymal Stromal Cells ; cytology ; drug effects ; Organic Chemicals ; Receptors, CXCR4 ; metabolism ; Recombinant Proteins ; pharmacology ; Smad3 Protein ; metabolism ; Transforming Growth Factor beta1 ; antagonists & inhibitors ; pharmacology ; Vimentin ; metabolism

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 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

OBJECTIVETo compare the applicability of the SYBR Green-I assay with the standard schizont maturation assay, for determination of sensitivity of Plasmodium vivax (P. vivax) to chloroquine and a new antifolate WR 99210.

METHODSThe study was conducted at Mae Tao Clinic for migrant workers, Tak Province during April 2009 to July 2010. A total of 64 blood samples (1 mL blood collected into sodium heparinized plastic tube) were collected from patients with mono-infection with P. vivax malaria prior to treatment with standard regimen of a 3-day chloroquine. In vitro sensitivity of P. vivax isolates was evaluated by schizont maturation inhibition and SYBR Green-I assays.

RESULTSA total of 30 out of 64 blood samples collected from patients with P. vivax malaria were successfully analyzed using both the microscopic schizont maturation inhibition and SYBR Green-I assays. The failure rates of the schizont maturation inhibition assay (50%) and the SYBR Green-I assay (54%) were similar (P=0.51). The median IC10s, IC50s and IC90s of both chloroquine and WR99210 were not significantly different from the clinical isolates of P. vivax tested. Based on the cut-off of 100 nM, the prevalences of chloroquine resistance determined by schizont maturation inhibition and SYBR Green-I assays were 19 and 11 isolates, respectively. The strength of agreement between the two methods was very poor for both chloroquine and WR99210.

CONCLUSIONSOn the basis of this condition and its superior sensitivity, the microscopic method appears better than the SYBR Green-I Green assay for assessing in vitro sensitivity of fresh P. vivax isolates to antimalarial drugs.

Antimalarials ; pharmacology ; Chloroquine ; pharmacology ; Humans ; Inhibitory Concentration 50 ; Malaria, Vivax ; parasitology ; Organic Chemicals ; Parasitemia ; parasitology ; Parasitic Sensitivity Tests ; Plasmodium vivax ; drug effects ; isolation & purification ; Schizonts ; drug effects

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

This study is to observe the effect of ilexonin A (IA) on the expression of basic fibroblast growth factor (bFGF) and growth associated protein-43 (GAP-43), and neurogenesis after cerebral ischemia-reperfusion in rats and explore its possible mechanism of protecting neuronal injury. Models of middle cerebral artery occlusion (MCAO) were established in SD rats. Before and after two hours ischemia-reperfusion, IA (20 and 40 mg x kg(-1)) was injected immediately and on 3, 7, 14, and 28 d once a day. The neurological severity was evaluated by neurological severity scores (NSS); neuronal injury in the boundary zone of the infarction area was evaluated by TUNEL and Niss1 staining. The expressions of bFGF and GAP-43 and neurogenesis were evaluated by Western blotting and 5-bromodeoxyuridine (Brdu) fluorescence staining, respectively. After treatment with IA, the NSS of treatment groups were lower than that of the models (3 and 7 d). The number of TUNEL positive neurons decreased and Nissl positive neurons increased at the same time (3 d). The expressions of bFGF and GAP-43 increased significantly in the boundary zone of the infarction area when compared to model group. Moreover, IA markedly enhanced the neurogenesis in the brain after ischemia-reperfusion, which revealed an increase of Brdu/NeuN positive cells in the boundary zone of the infarction area. The possible mechanism of protecting neuronal injury of IA may be related to inhibition on neuronal apoptosis, upregulation of bFGF and GAP-43, and neurogenesis in boundary zone of infarction after cerebral ischemia-reperfusion.
Animals ; Apoptosis ; drug effects ; Brain Ischemia ; etiology ; Bromodeoxyuridine ; metabolism ; Fibroblast Growth Factor 2 ; metabolism ; GAP-43 Protein ; metabolism ; Infarction, Middle Cerebral Artery ; complications ; Male ; Neurogenesis ; drug effects ; Neurons ; pathology ; Neuroprotective Agents ; pharmacology ; Organic Chemicals ; pharmacology ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Reperfusion Injury ; etiology ; metabolism

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

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