Beta-cyclodextrin-enhanced solubilization of phenylsulfonyl carboxylates in water.
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Carboxylic Acids↗
Biomedical subjects
B Cui
Publications and source records attributed to B Cui.
Pervilleine A, a novel tropane alkaloid that reverses the multidrug-resistance phenotype.
P-Glycoprotein-mediated drug efflux can yield a multidrug-resistance (MDR) phenotype that is associated with a poor response to cancer chemotherapy. Pervilleine A, a novel tropane alkaloid obtained from a chloroform extract of Erythroxylum pervillei as the result of bioactivity-guided fractionation, was found to restore the vinblastine sensitivity of cultured multidrug-resistant KB-V1 and CEM/VLB(100) cells, with IC(50) values of 0.36 and 0.02 microM, respectively. Similarly, the chemosensitivity of KB-8-5 cells to colchicine was restored with an IC(50) value of 0.61 microM. The mechanism of this response was evaluated with a number of model systems. First, incubation of multidrug-resistant KB-V1 and CEM/VLB(100) cells with up to 45 microM pervilleine A for 72 h did not significantly affect either the transcription of MDR1, as revealed by reverse transcriptional-PCR-based analysis of MDR1 mRNA, or levels of P-glycoprotein, as shown by Western blots. ATP-dependent binding of [(3)H]vinblastine observed with isolated multidrug-resistant KB-V1 cell membrane vesicles was inhibited by pervilleine A in a dose-dependent manner, and kinetic analysis indicted competitive inhibition with respect to vinblastine binding with a K(i) of 7.3 microM. Consistent with this effect, intracellular accumulation of [(3)H]vinblastine was increased from 0.18 pmol [(3)H]vinblastine/50 x 10(4) cells to approximately 5 pmol [(3)H]vinblastine/50 x 10(4) cells in the presence of 40 microM pervilleine A. To explore the potential relevance of these responses, KB-V1 or KB-8-5 cells were placed in hollow fibers and implanted into NCr nu/nu mice. Cell growth was not significantly inhibited when vinblastine or pervilleine A were administered as single agents, but when used in combination, inhibition of up to 75% was observed. Equimolar doses of verapamil were less effective. These data suggest that pervilleine A is an effective inhibitor of P-glycoprotein and should be further evaluated for clinical utility.
ATP Binding Cassette Transporter, Subfamily B, Mem↗
Cytotoxic polyacetylenes from the twigs of Ochanostachys amentacea.
Bioassay-guided investigation of the twigs of Ochanostachys amentacea using LNCaP (hormone-dependent human prostate cancer) cells as a monitor led to the isolation of three alkynes, the known (S)-17-hydroxy-9,11,13,15-octadecatetraynoic acid (minquartynoic acid, 1) and two novel analogues, (S)-17,18-dihydroxy-9,11,13,15-octadecatetraynoic acid (2) and (S)-17-hydroxy-15E-octadecen-9,11,13-triynoic acid (3). Compounds 1-3 were tested against a panel of human tumor cell lines and found to be significantly cytotoxic.
Alkynes↗
Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei.
Nine tropane alkaloid aromatic esters (1-9) were isolated from the roots of Erythroxylum pervillei by following their potential to reverse multidrug-resistance with vinblastine-resistant oral epidermoid carcinoma (KB-V1) cells. All isolates, including seven new structures (3-9), were evaluated against a panel of human cancer cell lines, and it was found that alkaloids 3 and 5-9 showed the greatest activity with KB-V1 cells assessed in the presence of vinblastine, suggesting that these new compounds are potent modulators of P-glycoprotein. Confirmatory results were obtained with human ovarian adenocarcinoma (SKVLB) cells evaluated in the presence of adriamycin and synergistic studies performed with several cell lines from the NCI tumor panel. The structures of the new compounds were determined using spectroscopic techniques. Single-crystal X-ray analysis was performed on the monoester, tropane-3 alpha,6 beta,7 beta-triol 3-phenylacetate (1).
ATP Binding Cassette Transporter, Subfamily B↗
[An epidemiological survey of thyroid disorders in an area with high iodine content in water supply].
OBJECTIVE: To investigate the status of thyroid disorders among people aged 14 years and older residing in Huanghua County, an iodine excess intake area in north China. METHODS: 4,230 people were asked to fulfill the questionnaire and 1,074 among them aged (36.97 +/- 12.83) years were accepted to be samples for the test. All subjects who were taken as samples needed to fill the questionnaire on thyroid disorders in detail, accept physical and ultrasound examination. Their morning fasting urine were collected for measurement of iodide concentration, and their sera were measured for thyroid-stimulating hormone(TSH, the third generation), thyroid peroxidase antibody (TPOAb), thyroglobulin antibody (TGAb) and thyroglobulin (TG). If some people had abnormal TSH level, their free T4, free T3 and TSH receptor antibody(TRAb) were measured. RESULTS: The median level of urinary iodide of the sample subjects was 614.61 micrograms/L. The prevalence of clinical and subclinical hyperthyroidism was 1.21% and 1.12% respectively; 92.3% of the clinical hyperthyroidism were of Graves' disease and 75% of the subjects with subclinical hypothyroidism were TRAb positive. The average incidence of clinical hyperthyroidism was not different between 2 periods before and after general iodinization of table salt in this area (1991-1995 and 1996-2000). The prevalence of clinical and subclinical hypothyroidism was 1.96% and 6.05% respectively. All the clinical patients were female, among them 85.71% were TPOAb and/or TGAb positive, while only 29.23% of the subclinical patients were TPOAb and/or TGAb positive. Positive TPOAb and TGAb were seen in 11.6% and 9.3% respectively of the sample subjects with an age-related increase. Positive thyroid autoantibody was more common in the female and those with abnormal TSH. The prevalence of thyroid cancer during the period of 1994-2000 was 91.58/100,000. CONCLUSION: The high prevalence of hypothyroidism and thyroid cancer indicates that excessive iodine intake in this area is not safe.
Adult↗
[Gene transfer of CD80 into a human ovarian cancer cell line and induction of cytotoxic T lymphocyte in vitro].
OBJECTIVE: To investigate the proliferation and cytotoxicity of cytotoxic T lymphocyte (CTL) induced by ovarian cancer cells transfected with a CD80 gene containing retroviral vector. METHODS: The ovarian cancer cell line TYK cells were transfected with retro-virus vector PLXSN-hCD80. After geneticin (G418) selection, the CD80 expression of the transfectants was confirmed by flow cytometry. CTL was induced by co-culture of CD80-expressing TYK cells (TYK-hCD80) and peripheral-blood mononuclear cells (PBMC) in the presence of anti-CD3 monoclonal antibody (McAb). Proliferation of PBMC was measured using 3H-Thymidine incorporation assay. The lysis activity of CTL toward tumor cells was determined using methyl thiazolyl tetrazolium (MTT) assay. RESULTS: After transfection and G418 selection, the CD80 expression was proved by flow cytometry. The highest rate of CD80 expression was 84.9%. The TYK cell line expressing high CD80 was named TYK-hCD80. In the presence of anti-CD3 McAb, TYK-hCD80 significantly enhanced proliferation of PBMC than TYK cells (3H-Thymidine incorporation, (40,604 +/- 842) vs (8,000 +/- 594) cpm (P < 0.05). The lysis activity of CTL activated by TYK-hCD80 was higher than that of TYK(P < 0.05). CONCLUSIONS: Ovarian cancer cells expressing CD80 can induce the production of CTLs which have high lysis activity and high proliferation rate in the presence of anti-CD3 McAb. This study may provide the experimental basis for immunogenic therapy of ovarian cancer.
B7-1 Antigen↗
[Discussion on some basic problems in design of wetland ecosystem].
The design of wetland ecosystem is the key and fundament in wetland restoration and mitigation. In recent years, it has been frequently applied to the proper construction of wetlands. The paper first reviews the concept of wetland ecosystem design, as well as the basis of ecological engineering, and then presented the basic principles in the design of wetland ecosystem. Some major ecological indicators including hydrology, chemical, substrate, soil and biotic indicators were also discussed, and some reference values for ecological indicators were presented. On the base of the designing purposes, three major types in the wetland design were analysed. They include constructing wetlands for wastewater treatment, for mitigation wetlands, and for controlling flooding and non-point source pollution.
Ecosystem↗
A plasmid construct encoding murine interferon beta antagonizes the replication of herpes simplex virus type I in vitro and in vivo.
In the present study, we employed a plasmid DNA encoding murine interferon (IFN)-beta to assess its antiviral efficacy in an in vitro transfection-infection assay and in an ocular HSV-1 infection model of mice. In the in vitro assay, transfection of mouse fibroblasts with the IFN-beta transgene resulted in a 17-fold or greater reduction in the viral load of HSV-1 at a multiplicity of infection (MOI) of 1 compared to that of those mice treated with the plasmid control. RT-PCR analysis of representative immediate early (ICP27), early (thymidine kinase, TK) and late (VP16) viral genes found no changes in the level of expression comparing the IFN-beta transgene- to the vector-treated control group, suggesting that the IFN-beta transgene may act at the post-transcriptional level of viral replication. In the ocular HSV-1 infection model, topical application of the plasmid DNA encoding murine IFN-beta onto mouse cornea enhanced cumulative survival and significantly reduced the viral load of HSV-1 in the eyes and trigeminal ganglia of mice at both day 3 and 6 post-infection compared with mice treated with the plasmid vector control or normal saline. Neutralizing antibody to IFN-beta blocked the protective effect elicited by the IFN-beta transgene. Unlike the in vitro experiment, viral gene expression was reduced in the trigeminal ganglion of mice pre-treated 24 h with the IFN-beta transgene day 3 (ICP27 and VP16) and day 6 (ICP27, TK, DNA polymerase, and VP16) post-infection in comparison to mice treated with the plasmid vector control as determined by semi-quantitative RT-PCR.
Animals↗
Quinoline alkaloids from Acronychia laurifolia.
Bioassay-directed fractionation of a root extract of Acronychia laurifolia (Rutaceae) using the KB-V1+ human tumor cell line led to the isolation of six quinoline alkaloids. One of these alkaloids is novel, namely, 2,3-methylenedioxy-4,7-dimethoxyquinoline and the other five were identified as the known compounds, evolitrine, gamma-fagarine, skimmianine, kokusaginine and maculosidine. Two known bis-tetrahydrofuran lignans, sesamolin and yangambin, were also identified. The structure of the new alkaloid was determined by spectroscopic methods. All of the isolates were evaluated against a panel of human cancer cell lines; four of the alkaloids showed weak cytotoxic activity.
Alkaloids↗
Cytotoxic sesquiterpenoids from Ratibida columnifera.
Bioassay-directed fractionation of the flowers and leaves of Ratibida columnifera using a hormone-dependent human prostate (LNCaP) cancer cell line led to the isolation of 10 cytotoxic substances, composed of five novel xanthanolide derivatives (2-4, 7, and 8), a novel nerolidol derivative (9), and three known sesquiterpene lactones, 9alpha-hydroxy-seco-ratiferolide-5alpha-O-angelate+ ++ (1), 9alpha-hydroxy-seco-ratiferolide-5alpha-O-(2-methylbut yrate) (5), 9-oxo-seco-ratiferolide-5alpha-O-(2-methylbutyrate) (6), as well as a known flavonoid, hispidulin (10). On the basis of its cytotoxicity profile, compound 5 was selected for further biological evaluation, and was found to induce G1 arrest and slow S traverse time in parental wild type p53 A2780S cells, but only G2/M arrest in p53 mutant A2780R cells, with strong apoptosis shown for both cell lines. The activity of 5 was not mediated by the multidrug resistance (MDR) pump, and it was not active against several anticancer molecular targets (i.e., tubulin polymerization/depolymerization, topoisomerases, and DNA intercalation). While these results indicate that compound 5 acts as a cytotoxic agent via a novel mechanism, this substance was inactive in in vivo evaluations using the murine lung carcinoma (M109) and human colon carcinoma (HCT116) models.
Animals↗
Cytostatic mechanism and antitumor potential of novel 1H-cyclopenta[b]benzofuran lignans isolated from Aglaia elliptica.
A total of five 1H-cyclopenta[b]benzofuran lignans (1-5) isolated from the stems of Aglaia elliptica B1. (Meliaceae) inhibited the growth of human cancer cells in culture. Of particular note, the IC50 values observed with 1 (methyl rocaglate), 2 (4'-demethoxy-3',4'-methylenedioxy-methyl rocaglate) and 5 (1-O-formyl-4'-demethoxy-3',4'-methylenedioxy-methyl rocaglate) were in the 1-30 ng/ml range. Prompted by the high potency of these responses, additional studies were performed with 2, a structurally representative isolate that was available in sufficient quantity as a result of the isolation process. Utilizing cultured Lu1 (human lung carcinoma) cells as a model, compound 2 induced accumulation in the G1/G0 phase of the cell cycle after 24 or 32 h of incubation; normal cell-cycle dynamics were observed at subsequent time periods. Cell proliferation was inhibited in a dose-dependent manner, but during the course of wash-out experiments, colony formation was not reduced. In addition, as judged by [3H]leucine incorporation, the test compound strongly inhibited protein biosynthesis (IC50 = 25 ng/ml). In analogous studies, nucleic acid biosynthesis was not reduced, even when cells were treated with concentrations as high as 1 microg/ml. These data suggest inhibition of protein synthesis is a key mode of action, and the compound functions by a cytostatic mechanism. Utilizing a human breast cancer cell line (BC1) sensitive to compound 2 in culture (IC50 = 0.9 ng/ml), an initial assessment of antitumor potential was performed. In accord with the in vitro results, the growth of BC1 in athymic mice was delayed by treatment with compound 2 (10 mg/kg body weight, three times per week, i.p.). Body weight was unaffected and no signs of overt toxicity were observed. However, growth paralleled that of the control group at later time points. Thus, novel 1H-cyclopenta[b]benzofuran lignans are potent cytostatic inhibitors of protein biosynthesis and are capable of delaying tumor growth in an in vivo model. Their full clinical or basic utility requires further investigation.
Animals↗
Limonoids from Azadirachta excelsa.
Activity-directed fractionation of a stem extract of Azadirachta excelsa using KB (human oral epidermoid carcinoma) cells led to the isolation of four meliacin-type limonoids. Two of these constituents were novel, namely, 2,3-dihydronimbolide and 3-deoxymethylnimbidate, and these were purified along with the known compounds, nimbolide and 28-deoxonimbolide. The structures of the new compounds were determined by spectroscopic methods. Nimbolide and 28-deoxonimbolide were broadly cytotoxic when evaluated against a panel of human cancer cell lines, while the two novel compounds were inactive in this regard. The defection of nimbolide and 28-deoxonimbolide as cytotoxic constituents was facilitated by an electrospray LC/MS dereplication procedure.
Antineoplastic Agents, Phytogenic↗
Novel cytotoxic acylated oligorhamnosides from Mezzettia leptopoda.
Activity-guided fractionation of a stem extract of Mezzettia leptopoda using human oral epidermoid carcinoma (KB) cells led to the isolation of seven highly acylated oligorhamnosides. Four of these constituents are novel, namely, n-octyl 2-O-acetyl-alpha-L-rhamnopyranosyl-(1-->3)-2, 4-di-O-acetyl-alpha-L-rhamnopyranosyl-(1-->3)-4-O-hexanoyl-alpha-L-rh amnopyranoside (mezzettiaside 8) (1); n-octyl 2, 3-di-O-acetyl-alpha-L-rhamnopyranosyl-(1-->3)-4-O-hexanoyl-alpha-L-rh amnopyranoside (mezzettiaside 9) (2); n-octyl 2, 4-di-O-acetyl-alpha-L-rhamnopyranosyl-(1-->3)-4-O-hexanoyl-alpha-L-rh amnopyranoside (mezzettiaside 10) (3); and n-octyl 2,3, 4-tri-O-acetyl-alpha-L-rhamnopyranosyl-(1-->3)-4-O-hexanoyl-alpha-L-r hamnopyranoside (mezzettiaside 11) (4). Three known compounds were identified as mezzettiasides 2 (5), 3 (6), and 4 (7), respectively, previously isolated from this same plant. The structures of novel compounds 1-4 were determined by spectroscopic methods. All the isolates were evaluated against a panel of human cancer cell lines in this study, and compounds 1-2 and 4-7 were found to be weakly cytotoxic toward KB and/or human colon and lung cancer cell lines.
Animals↗
CT scan directed transbronchial needle aspiration biopsy for mediastinal nodes.
STUDY OBJECTIVES: This study was performed to determine whether transbronchial needle aspiration (TBNA) biopsy under CT guidance can increase its diagnostic yield so that this technique can be used for staging of lung cancer at our institution. STUDY DESIGN: After an initial unacceptable low yield of TBNA on the first 10 patients (20% positive), we switched the biopsy procedure from the bronchoscopy suite to the CT room. After each passage of the needle to the mediastinum lymph node, CT scan was performed to locate the tip of the needle. If the initial attempt was not successful, TBNA was repeated at the same setting until CT documented that the tip of the needle was exactly inside the lymph node. RESULT: A total of 49 patients with 69 mediastinum adenopathies were enrolled in this study. There were 31 patients with malignant mediastinal adenopathy proven by TBNA (60% sensitivity). Fifteen patients showed normal results of needle aspiration despite the presence of primary lung cancer. Three patients showed mediastinal abscesses. CONCLUSION: Despite numerous successful reports in the literature, the general application of the TBNA procedure appears to be limited because of its low sensitivity, although this could be due to numerous factors. However, using CT guidance to be sure that the tip of the needle is exactly inside the node can increase its sensitivity markedly. It may also increase the specificity of normal results of TBNA biopsy.
Abscess↗
[A clinical analysis on 131 senile cases with diplopia].
OBJECTIVE: To approach the pathogenic features of senile diplopia to elevate the rate of accurate clinical diagnosis and the therapeutic effect of treatment. METHODS: Prism, synoptophore, Hess' screen and red glass test were used to examine the ocular position, muscle movement and diplopia image in 131 cases (aged 60 or older). Biochemical examination of blood and imaging diagnosis were also involved. RESULTS: Among 131 cases, 120 (91.6%) suffered from binocular diplopia and 11 cases (8.4%) monocular diplopia. The majority of cases (110/120) with binocular diplopia were of ocular dyscinesia type resulting from intracranial vascular diseases, while the majority of cases with monocular diplopia resulted from complications of intraocular operation. CONCLUSIONS: Most of the diplopia in the aged are binocular one whose main cause is ocular dyscinesia resulting from vascular diseases. The cause of monocular diplopia in most of the cases is frequently due to the complications of intraocular operation. The authors emphasize a thorough examination of patients with diplopia.
Aged↗
YAG laser resection for the membrane on anterior surface of intraocular lenses.
The results and methods of YAG laser resection for the membrane forming postoperatively on the anterior surface of intraocular lens (IOL) in 33 eyes (31 cases) were reported. A monomode single pulse YAG laser was used to do a circular incision along the pupilar margin and blow it up. A multimode defocus burst was used to peel off the shrunk flap from the lens surface. The membrane in 27 eyes (81.8%) was completely removed in the first resection. The mean burst number was 49.2 +/- 26.3. The average energy of each burst was 1.3 mJ and the average total energy of each treatment was 62.1 +/- 37.1 mJ. Except 3 eyes with little blood oozing from iris near the pupilar margin, 4 eyes having foggy spots on IOL surface and 2 eyes with mild transient increased intraocular pressure (IOP) after resection, there were no other complications. The resection is safe and effective, could be instead of the second operation for unabsorbable organized membranes or the membrane causing blockage glaucoma, could accelerate the recovery of visual acuity and shorten or substitute medical treatment for thick membranes.
Adolescent↗
Triterpene glycosides from the bark of Robinia pseudo-acacia L. II.
From the bark of Robinia pseudo-acacia L., six new triterpene glycosides, Robiniosides E--J, were isolated and their structures were elucidated as abrisapogenol B 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D-galactopyranosyl(1-->2)-beta-D - glucuronopyranoside (1), abrisapogenol B 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D- glucopyranosyl(1-->2)-beta-D-glucuronopyranoside (2), 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D-galactopyranosyl(1-->2)-beta-D - glucuronopyranosyl abrisapogenol B 22-O-alpha-L-rhamnopyranoside (3), 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D- glucopyranosyl(1-->2)-beta-D-glucuronopyranosyl abrisapogenol B 22-O-alpha-L-rhamnopyranoside (4), 3-O-alpha-L- rhamnopyranosyl(1-->2)-beta-D-galactopyranosyl(1-->2)-beta-D-glucuron opyranosyl abrisapogenol E 30-O-beta-D-apiofuranosyl(1-->6)-beta-D-glucopyranoside (5) and 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D-glucopyranosyl(1-->2)-beta-D- glucuronopyranosyl abrisapogenol E 30-O-beta-D-apiofuranosyl(1-->6)-beta-D-glucopyranoside (6), respectively.
Carbohydrate Sequence↗
Triterpene glycosides from the bark of Robinia pseudo-acacia L. I.
From the bark of Robinia pseudo-acacia L., five new triterpene glycosides, robiniosides A-D (3, 5-7) and compound III (4), were isolated and their structures were elucidated as 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D-glucopyranosyl(1-->2)-beta-D- glucuronopyranosyl 3 beta,22 beta-dihydroxyolean-12-en-29-oic acid (3), 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D-galactopyranosyl(1-->2)-beta-D -glucuronopyranosyl 3 beta,22 beta,24-trihydroxyolean-12-en-29-oic acid (4), whose sapogenol was unambiguously characterized and designated as oxytrogenin, 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D-glucopyranosyl(1-->2)-beta-D glucuronopyranosyl oxytrogen (5), 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D galactopyranosyl(1-->2)-beta-D-glucuronopyranosyl oxytrogenin 22-O-alpha-L-rhamnopyranoside (6), 3-O-alpha-L- rhamnopyranosyl(1-->2)-beta-D-glucopyranosyl(1-->2)-beta-D-glucuronop yranosyl oxytrogenin 22-O-alpha-L-rhamnopyranoside (7), respectively, together with two known triterpene glycosides, kaikasaponin III (1) and 3-O-alpha-L-rhamnopyranosyl(1-->2)-beta-D-galactopyranosyl(1-->2)-beta-D - glucuronopyranosyl 3 beta,22 beta-dihydroxyolean-12-en-29-oic acid (2).
Carbohydrate Sequence↗