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1.
Article in English | WPRIM | ID: wpr-23108

ABSTRACT

BACKGROUND: Although combined chemotherapy has increased survival rates among children with cancer, such treatments can induce sensorineural hearing loss. Therefore, we aimed to identify risk factors for hearing impairments in patients with childhood cancer. METHODS: Audiograms were obtained from 115 patients with childhood cancer and survivors (age 20 dB based on the weighted mean value in either ear. Severe hearing impairments were observed in 56% of patients with brain tumors. Although cisplatin or vinca alkaloids were significant risk factors for hearing impairment, the use of both cisplatin and vinca alkaloids exhibited the highest odds ratio for hearing impairment (P < 0.001, < 0.001 for R/LA(max); P=0.099, 0.039 for R/LA(avg)). Multivariate analysis revealed that the use of both cisplatin and vinca alkaloids was an independent risk factor for hearing impairment based on RA(max), LA(max), and LA(avg) (P < 0.001, < 0.001, 0.039, respectively). CONCLUSION: Our findings indicate that cisplatin and vinca alkaloids exert an additive effect on the risk of hearing impairment in survivors of childhood cancer. Further prospective studies are thus required to determine the most effective chemotherapeutic regimen for reducing ototoxicity.


Subject(s)
Audiometry , Brain Neoplasms , Child , Cisplatin , Drug Therapy , Ear , Hearing Loss , Hearing Loss, Sensorineural , Hearing , Humans , Multivariate Analysis , Odds Ratio , Prospective Studies , Risk Factors , Survival Rate , Survivors , Vinca Alkaloids , Vinca
2.
Article in English | WPRIM | ID: wpr-788610

ABSTRACT

BACKGROUND: Although combined chemotherapy has increased survival rates among children with cancer, such treatments can induce sensorineural hearing loss. Therefore, we aimed to identify risk factors for hearing impairments in patients with childhood cancer.METHODS: Audiograms were obtained from 115 patients with childhood cancer and survivors (age < 20 years). Pure tone audiometry (PTA) was performed at octave intervals within the range of 250-8000 Hz. We evaluated clinical risk factors associated with hearing impairments. Hearing loss was evaluated based on the maximal decibel (dB) loss in any frequency for each ear (RA(max) or LA(max)) and weighted mean dB loss for specific frequencies (RA(avg) or LA(avg)).RESULTS: Forty percent of patients (N=46) exhibited hearing loss >20 dB based on the weighted mean value in either ear. Severe hearing impairments were observed in 56% of patients with brain tumors. Although cisplatin or vinca alkaloids were significant risk factors for hearing impairment, the use of both cisplatin and vinca alkaloids exhibited the highest odds ratio for hearing impairment (P < 0.001, < 0.001 for R/LA(max); P=0.099, 0.039 for R/LA(avg)). Multivariate analysis revealed that the use of both cisplatin and vinca alkaloids was an independent risk factor for hearing impairment based on RA(max), LA(max), and LA(avg) (P < 0.001, < 0.001, 0.039, respectively).CONCLUSION: Our findings indicate that cisplatin and vinca alkaloids exert an additive effect on the risk of hearing impairment in survivors of childhood cancer. Further prospective studies are thus required to determine the most effective chemotherapeutic regimen for reducing ototoxicity.


Subject(s)
Audiometry , Brain Neoplasms , Child , Cisplatin , Drug Therapy , Ear , Hearing Loss , Hearing Loss, Sensorineural , Hearing , Humans , Multivariate Analysis , Odds Ratio , Prospective Studies , Risk Factors , Survival Rate , Survivors , Vinca Alkaloids , Vinca
3.
Acta Pharmaceutica Sinica ; (12): 276-280, 2013.
Article in Chinese | WPRIM | ID: wpr-235672

ABSTRACT

In order to study the chemical constituents in the water extract of the stem of Nauclea officinalis, column chromatography over D101 macroporous resin and silica gel and an automatic purification system were used to isolate and purify the chemical constituents from the extract. Nine compounds were obtained. By analysis of the physicochemical properties and spectral data, their structures were identified as naucleamide G (1), 3, 4-dimethoxyphenol-beta-D-apiofuranosyl (1-->6)-beta-D-glucopyranoside (2), kelampayoside A (3), 3alpha, 5alpha-tetrahydrodeoxycordifoline lactam (4), naucleamide A-10-O-beta-D-glucopyranoside (5), pumiloside (6), 3-epi-pumiloside (7), strictosamide (8) and vincosamide (9), separately. Among them, compound 1 is a new compound, compound 2 was found in plants of the genus Nauclea for the first time, and compounds 3 and 4 were isolated from this plant for the first time.


Subject(s)
Camptothecin , Chemistry , Carbolines , Chemistry , Glucosides , Chemistry , Indole Alkaloids , Chemistry , Molecular Structure , Plant Stems , Chemistry , Plants, Medicinal , Chemistry , Rubiaceae , Chemistry , Vinca Alkaloids , Chemistry
4.
Article in English | WPRIM | ID: wpr-812673

ABSTRACT

AIM@#To identify the structure of the acid-catalyzed product of strictosamide and explore the reaction mechanism.@*METHODS@#The acid-catalyzed reaction process of strictosamide was monitored by HPLC, and a macroporous resin was used to purify the reaction solution. The structure of the product was confirmed by MS, NMR, and ROESY spectra.@*RESULTS@#The acid-catalyzed transformation yield from strictosamide to vincoside lactam was 52%.@*CONCLUSION@#The reaction mechanism of the transformation from strictosamide to vincoside lactam may be related to the stability of the three-dimensional configuration of the compound. These results offer a new way to obtain vincoside lactam from the widely distributed indole alkaloid strictosamide by acid-catalysis.


Subject(s)
Acids , Chemistry , Catalysis , Lactams , Chemistry , Molecular Structure , Vinca Alkaloids , Chemistry
5.
Article in Chinese | WPRIM | ID: wpr-267018

ABSTRACT

<p><b>OBJECTIVE</b>Under various drought conditions and nitrogen application, the content of vindoline, catharanthine, vincristine and vinblastine in the leaf of Catharanthus roseus were illustrated to improve the content of alkaloid theoretically.</p><p><b>METHOD</b>Six groups were set in the experiment, which included: CK (natural control), CN (natural control + nitrogen), LK (low drought), LN (low drought + nitrogen), HK (high drought), HN (high drought + nitrogen) to discuss the change characteristics of total nitrogen, the activity of alkaline POD and TDC, the content of four alkaloids under the different conditions were measured.</p><p><b>RESULT</b>Under LK condition, the activity of POD, TDC were enhanced. In the early stage of stress (0-21 d), vindoline, catharanthine, vincristine and vinblastine accumulated, and reduced in the later stage (28-35 d). For all groups, adding exogenous nitrogen could improve the total content of nitrogen, vindoline and vinblastine, meanwhile the activity of POD and TDC were enhanced as well. The LN, HN treatments were beneficial to accumulating catharanthine and vinblastine.</p><p><b>CONCLUSION</b>Drought stress or additional nitrogen have an influence on both of the activities of POD and TDC, and the four alkaloids were affected as well. Thereinto, the LN condition was the most effective treatment for accumulating the four alkaloids (vindoline, catharanthine, vincristine and vinblastine), which were regulated by improve nitrogen content and enzymatic activity.</p>


Subject(s)
Catharanthus , Metabolism , Nitrogen , Metabolism , Peroxidase , Metabolism , Stress, Physiological , Vinblastine , Metabolism , Vinca Alkaloids , Metabolism , Vincristine , Metabolism , Water , Metabolism
6.
Article in Chinese | WPRIM | ID: wpr-749409

ABSTRACT

OBJECTIVE@#To evaluate the efficiency between two treatments of sudden hearing loss.@*METHOD@#All patients were divided into two groups randomly, basic drug group was treated with ganglioside and vinpocetine injection, combined therapy group was treated with intratympanic dexamethasone and what was used in basic drug group.@*RESULT@#The effective rate of combined therapy group (73.53%) was significantly higher than that of basic drug group (37.78%) (P < 0.05).@*CONCLUSION@#The comprehensive therapy of intratympanic dexamethasone injection, ganglioside and vinpocetine injection have excellent efficiency for sudden hearing loss.


Subject(s)
Adolescent , Adult , Child , Dexamethasone , Therapeutic Uses , Drug Therapy, Combination , Ear, Middle , Female , Gangliosides , Therapeutic Uses , Hearing Loss, Sudden , Drug Therapy , Humans , Injections , Male , Middle Aged , Treatment Outcome , Vinca Alkaloids , Therapeutic Uses , Young Adult
7.
Article in Chinese | WPRIM | ID: wpr-252954

ABSTRACT

<p><b>OBJECTIVE</b>To study on the purification of strictosamide from Nauclea officinalis by macroporous resin to provide reference for production.</p><p><b>METHOD</b>The best macroporous resin was selected among 10 kinds of resins according to adsorption and desorption of the static adsorption experiments. The adsorption quantity, elution volume of water, concentration and elution volume of alcohol were determined according to the single factor experiment.</p><p><b>RESULT</b>HPD400 was the best resin, and the best adsorption quantity was 20.23 mg x g(-1), the elution volume of water and 30% alcohol was 6 BV, and the elution volume of 70% alcohol was 4 BV.</p><p><b>CONCLUSION</b>This technology is simple, feasible, and it can provide reference for the industrialized production.</p>


Subject(s)
Adsorption , Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Chemistry , Ethanol , Chemistry , Resins, Synthetic , Chemistry , Rubiaceae , Chemistry , Technology, Pharmaceutical , Methods , Vinca Alkaloids , Chemistry
8.
Article in Chinese | WPRIM | ID: wpr-252947

ABSTRACT

<p><b>OBJECTIVE</b>To study the chemical constituents of the leaves of Naudea officinalis.</p><p><b>METHOD</b>The chemical constituents were separated by column chromatography and semi-preparative HPLC techniques, and their structures were determined by spectral analysis.</p><p><b>RESULT</b>Five compounds were isolated and identified as strictosamide (1), 10-hydroxy strictosamide (2), kaempferol-3-O-rutinoside (3), rutin (4), pumiloside(5).</p><p><b>CONCLUSION</b>Among these compounds, 2, 3, 4 are isolated from the leaves of Naudea officinalis for the first time.</p>


Subject(s)
Camptothecin , Chemistry , Chromatography, High Pressure Liquid , Methods , Kaempferols , Chemistry , Magnetic Resonance Spectroscopy , Methods , Plant Extracts , Chemistry , Plant Leaves , Chemistry , Rutin , Chemistry , Vinca Alkaloids , Chemistry
9.
Acta Pharmaceutica Sinica ; (12): 747-751, 2010.
Article in Chinese | WPRIM | ID: wpr-354539

ABSTRACT

To study chemical constituents of the leaves of Nauclea officinalis, eight alkaloids were isolated from 95% ethanol extract by various chromatographic methods. The structures were elucidated on the basis of spectroscopic data (IR, UV, ESI-MS, 1D and 2D NMR) and identified as naucleactonin C (1), strictosamide (2), vincosamide (3), pumiloside (4), angustoline (5), angustine (6), 18, 19-dihydroangustine (7) and naucleofficine D (8). Compound 1 is a new indole alkaloid. Compounds 6 and 7 were isolated from this plant for the first time.


Subject(s)
Alkaloids , Chemistry , Camptothecin , Chemistry , Indole Alkaloids , Chemistry , Indoles , Chemistry , Molecular Structure , Plant Leaves , Chemistry , Plants, Medicinal , Chemistry , Rubiaceae , Chemistry , Vinca Alkaloids , Chemistry
10.
Article in Chinese | WPRIM | ID: wpr-260745

ABSTRACT

<p><b>OBJECTIVE</b>The content of vindoline, catharanthine and vinblastine in the root, stem, leaf, flower and fruit of Catharanthus roseus at various developmental stages were determined, and the biomass allocation was also determined to find the best harvest time.</p><p><b>METHOD</b>The content of vindoline, catharanthine and vinblastine in the root, stem, leaf, flower and fruit of C. roseus were determined by HPLC.</p><p><b>RESULT</b>The content of these alkaloids were influenced by season and it varied in the different tissues of the plant. The content of vindoline and catharanthine in the leaves were the highest, and there was no vindoline detected in the root, but the content of vinblastine in the flower was the highest; the content of vindoline and catharanthine reached the maximum between the August and September, and the content of vinblastine reached the highest after the September. The biomass was the highest in the initial stage of September.</p><p><b>CONCLUSION</b>The best harvest time was in the initial stage of September.</p>


Subject(s)
Catharanthus , Chemistry , Metabolism , China , Chromatography, High Pressure Liquid , Flowers , Chemistry , Metabolism , Plant Extracts , Metabolism , Plant Leaves , Chemistry , Metabolism , Plant Roots , Chemistry , Metabolism , Seasons , Vinblastine , Metabolism , Vinca Alkaloids , Metabolism
11.
Rio de Janeiro; s.n; 2010. 99 p. ilus, tab.
Thesis in Portuguese | LILACS | ID: lil-601470

ABSTRACT

O consumo de etanol durante a gestação é um grave problema de saúde pública. Durante o desenvolvimento, o sistema nervoso é especialmente susceptível aos efeitos tóxicos do etanol e a exposição ao etanol durante este período pode gerar um amplo espectro de distúrbios neurocomportamentais, sendo o mais frequente, a hiperatividade. Recentemente, estudos têm sugerido que distúrbios na plasticidade neuronal podem estar relacionados com a hiperatividade. Os inibidores de PDE são drogas que agem impedindo a degradação de segundos mensageiros celulares como AMPc e GMPc, mantendo a ativação de proteínas quinases e de fatores de transcrição como o CREB, levando a expressão de genes relacionados à plasticidade. Neste trabalho, avaliamos através do teste de campo aberto se a administração de Vinpocetina ou Rolipram (inibidores de PDE) seria capaz de amenizar ou reverter a hiperatividade de camundongos Suíços expostos ao etanol no período correspondente ao terceiro trimestre de gestação humana. Para tanto, foram realizadas duas etapas: na primeira etapa, durante o período neonatal, os animais receberam injeções intraperitoneais de etanol (5g/Kg em solução salina a 25%, no 2º, 4º, 6º e 8º dias de vida pós-natal - PN2 a PN8) ou de salina, e 4 horas antes do teste comportamental no campo aberto (10 min), em PN30, receberam Vinpocetina (10mg/Kg ou 20mg/Kg diluídas em DMSO ip) ou somente DMSO ip. Na segunda etapa, os animais foram expostos ao etanol ou à salina no período neonatal nas mesmas condições da primeira etapa e no dia do teste comportamental receberam Rolipram (0,5 mg/Kg diluídas em DMSO ip ou somente DMSO ip). Posteriormente aos testes, foram coletados o córtex cerebral frontal e o hipocampo dos animais para avaliação dos níveis de AMPc. Os resultados comportamentais indicam que somente o tratamento com Vinpocetina (20mg/Kg) reverteu a hiperatividade de camundongos expostos ao etanol, resultado que não foi observado com o tratamento com Rolipram. Desta forma...


Ethanol consumption during gestation is a serious public health problem. During development, the nervous system is particularly susceptible to the toxic effects of ethanol and, in fact, ethanol exposure during perinatal development produces a range of neurobehavioral deficits, among which hyperactivity is one of the most frequently observed. There is evidence that reduced neuronal plasticity could be associated with hiperactivity. PDE inhibitors are drugs that prevent the breakdown of intracellular second-messengers such as cAMP and cGMP, maintaining the activation of protein kinases and of the CREB transcription factor, leading to the expression of plasticity-related genes. In this study we test whether Vinpocetine or Rolipram (PDE inhibitors) treatment can improve or revert hyperactivity in Swiss exposed to alcohol during the third trimester equivalent of human gestation. To that end, two experiments were carried out: In the first one, from postnatal day (PN) 2 to PN8, litters either received ethanol (5g/Kg i.p., 25% in saline solution) of an equivalent volume of saline solution every other day. On PN30, 4 h before the open field test (which lasted for 10 min) animals received Vinpocetine (10mg/Kg of 20mg/Kg diluted in DMSO i.p.) of dimethylsulfoxide (DMSO i.p.). In the second experiment animals were treated almost as before receiving Rolipram (0.5mg/Kg diluted in DMSO i.p.), instead of Vinpocetine, of DMSO i.p. After the tests, animals were sacrificed and frontal cerebral cortices and hippocampuses were dissescted and collected for the analysis of cAMP levels. Behavioral results showed that only the Vinpocetine treatment (20mg/Kg) reversed the ethanol-elicited hyperactivity, a result that was not observed for the Rolipram treatment. In this way, the dosage of cAMP levels was done only for the animals that received Vinpocetine (20mg/Kg). Ethanol neonatal exposure significantly reduced cAMP levels both in the cortex and in the hippocampus. Vinpocetine...


Subject(s)
Animals , Pregnancy , Mice , Alcohol-Induced Disorders, Nervous System , Vinca Alkaloids/pharmacology , Vinca Alkaloids/therapeutic use , Ethanol/adverse effects , Ethanol/toxicity , Phosphodiesterase Inhibitors/administration & dosage , Phosphodiesterase Inhibitors/therapeutic use , Models, Animal , Attention Deficit Disorder with Hyperactivity/drug therapy
12.
Acta Pharmaceutica Sinica ; (12): 658-666, 2009.
Article in English | WPRIM | ID: wpr-278202

ABSTRACT

The objective of this study is to compare the differences between self-microemulsifying drug delivery system (SMEDDS) and solid dispersion (SD) technology used to improve the dissolution rate and bioavailability of vinpocetine (VIP). The formulation of VIP-SMEDDS was composed of Labrafac, oleic acid, Cremophor EL, Transcutol P, and gum acacia which was used as solid absorbent. VIP-SD was prepared using poloxamer F68 as the carrier. In the solubility test, the solubility of VIP in SMEDDS was 17.3 times as much as that in SD. In the dissolution test, SMEDDS had shown better enhancement and stability in dissolving VIP than SD. When compared to VIP crude powder, the bioavailability of VIP in SMEDDS (VIP-SMEDDS) was 1.89-fold higher, and was less affected by food intake. However, the bioavailability of VIP in SD (VIP-SD) was bioequivalent to that of VIP crude powder. The tissue uptake of VIP-SMEDDS in Peyer's patches, intestine and liver after administration for 2 hours was more favorable than that of VIP-SD, which was 3.7 times higher in Peyer's patches, 2.2 times higher in intestine and 1.5 times higher in liver. In Caco-2 tests, the apparent permeability (P(app)) of VIP-SMEDDS was 2.65 times of that of VIP-SD. The width of the cell tight junctions of Caco-2 cell monolayer treated with VIP-SMEDDS were 9.6-fold wider, but there was no significant change after treatment with VIP-SD, when compared to the blank control. In conclusion, SMEDDS was more efficient than the traditional SD technology in increasing solubility, dissolution, intestinal permeability, lymphatic absorption and bioavailability of the insoluble drugs such as VIP, which is less affected by food intake.


Subject(s)
Animals , Biological Availability , Caco-2 Cells , Dosage Forms , Drug Delivery Systems , Emulsions , Chemistry , Pharmacokinetics , Humans , Male , Rats , Rats, Sprague-Dawley , Solubility , Vinca Alkaloids , Chemistry , Pharmacokinetics
13.
Article in Chinese | WPRIM | ID: wpr-298450

ABSTRACT

Catharanthine content and agronomic traits in major Catharanthus roseus varieties were analyzed. It was found that there existed great difference in catharanthine content and agronomic traits among the varieties. Catharanthine content was the highest in variety Pacifica Polka Dot (PPD), reaching 3.79 mg g(-1) dry leaf weight, and the lowest in variety Cooler Pink (CP) with only 0.9 mg g(-1) dry leaf weight. Correlation existed in certain extent between catharanthine content and agronomic traits in C. roseus. Path analysis showed that among all the agronomic traits analyzed, internodal distance positively affected catharanthine content at significant level (P<0.05), with the path coefficient being 1.473. This study provides useful information for high-catharanthine content C. roseus introduction and breeding.


Subject(s)
Catharanthus , Chemistry , Metabolism , Plant Leaves , Chemistry , Metabolism , Vinca Alkaloids , Metabolism
14.
J Genet ; 2007 Dec; 86(3): 259-68
Article in English | IMSEAR | ID: sea-114410

ABSTRACT

An integrated genetic linkage map of the medicinal and ornamental plant Catharanthus roseus, based on different types of molecular and morphological markers was constructed, using a F(2) population of 144 plants. The map defines 14 linkage groups (LGs) and consists of 131 marker loci, including 125 molecular DNA markers (76 RAPD, 3 RAPD combinations; 7 ISSR; 2 EST-SSR from Medicago truncatula and 37 other PCR based DNA markers), selected from a total of 472 primers or primer pairs, and six morphological markers (stem pigmentation, leaf lamina pigmentation and shape, leaf petiole and pod size, and petal colour). The total map length is 1131.9 cM (centiMorgans), giving an average map length and distance between two markers equal to 80.9 cM and 8.6 cM, respectively. The morphological markers/genes were found linked with nearest molecular or morphological markers at distances varying from 0.7 to 11.4 cM. Linkage was observed between the morphological markers concerned with lamina shape and petiole size of leaf on LG1 and leaf, stem and petiole pigmentation and pod size on LG8. This is the first genetic linkage map of C. roseus.


Subject(s)
Base Sequence , Catharanthus/anatomy & histology , Chromosome Mapping , DNA Primers/genetics , DNA, Plant/genetics , Expressed Sequence Tags , Genetic Markers , Minisatellite Repeats , Plants, Medicinal/anatomy & histology , Polymorphism, Restriction Fragment Length , Random Amplified Polymorphic DNA Technique , Vinca Alkaloids/metabolism
16.
Acta Pharmaceutica Sinica ; (12): 681-685, 2004.
Article in Chinese | WPRIM | ID: wpr-302737

ABSTRACT

<p><b>AIM</b>To prepare the microemulsion of vinpocetine in order to increase solubility and its in vitro transdermal delivery by using appropriate proportion of oil, surfactant (S), cosurfactant (CoS) and water. The formulation of proportion was optimized. The physicochemical properties and the skin irritation of the microemulsion was studied.</p><p><b>METHODS</b>Pseudo-tertiary phase diagrams were prepared to obtain the concentration ratio of components of the microemulsion. Using simplex lattice method, the formulation of microemulsion was optimized and the physicochemical properties including pH, viscosity, refractive index, conductivity and particle size distribution were examined. The MTT method was applied to test the skin irritation of the microemulsion on the Hacat cell.</p><p><b>RESULTS</b>The diagrams showed that the areas of O/W microemulsion increased with the increasing ratio of surfactant to cosurfactant (S/CoS). The predicted values from simplex lattice system were close to that of the experiment. The property of optimized microemulsion showed to be stable behavior and not irritant to Hacat cell.</p><p><b>CONCLUSION</b>The drug solubility and in vitro perscutaneous permeation flux of the optimized microemulsion was improved significantly and the irritation study showed that optimized microemulsion was safe as an ideal transdermal delivery system.</p>


Subject(s)
Administration, Cutaneous , Animals , Cell Survival , Cells, Cultured , Drug Compounding , Drug Stability , Emulsions , Chemistry , Excipients , Chemistry , Male , Neuroprotective Agents , Chemistry , Pharmacokinetics , Polyethylene Glycols , Chemistry , Rats , Rats, Wistar , Skin , Cell Biology , Skin Absorption , Solubility , Surface-Active Agents , Chemistry , Vinca Alkaloids , Chemistry , Pharmacokinetics
17.
Rev. cuba. invest. bioméd ; 22(2)abr.-jun. 2003. tab, graf
Article in Spanish | LILACS | ID: lil-390192

ABSTRACT

Se estudiaron los efectos antioxidantes del clorhidrato de triacetonamina (THC) in vitro a través de una serie de ensayos, en los que se analizó la capacidad secuestrante del OHú y quelante de Fe, con el ensayo de la 2 desoxi-d-ribosa y la capacidad secuestrante del O2ú por la autooxidación del pirogalol (2-12 mM THC). Se estudió además la actividad prooxidante del THC (0,1-0,6 mM), sobre el ADN inducida por Cu-fenantrolina y Fe-bleomicina. También se valoró la actividad prooxidante del TH-NOú (10-12 mM) y del THNOOú (10-12 mM), radicales derivados del THC. Finalmente se determinó el efecto del THC sobre la peroxidación lipídica en homogenato de cerebro de rata. Los resultados demostraron que el THC posee capacidad secuestrante del O2ú, con un comportamiento dependiente de la concentración y CI50 de 10 mM de THC. Se encontró efecto protector sobre la 2 desoxi-d-ribosa, tanto por acción quelante de Fe, como por secuestro directo de OHú con una Ks de 4.6 ´ 108 M-1s-1. El THC mostró efecto dependiente de la concentración para el daño sobre el ADN, mientras que el THNOú no dañó a esta molécula, a diferencia del THNOOú que si produjo daño a las concentraciones ensayadas. La peroxidación lipídica en homogenato de cerebro de rata no fue inhibida


Subject(s)
Animals , Rats , Antioxidants , In Vitro Techniques , Melanoma, Experimental , Lipid Peroxidation , Triacetoneamine-N-Oxyl , Vinca Alkaloids
18.
Article in Korean | WPRIM | ID: wpr-10664

ABSTRACT

OBJECTIVE: A number of disease-modifying anti-rheumatic drugs (DMARDs) have been shown to be more effective than placebo in the management of rheumatoid arthritis (RA). However, most course of DMARDs, except methotrexate, are discontinued after 2 or 3 years, because of toxicity, lack of efficacy or escape from control. The multi-drug resistance (MDR) is a phenomenon in which cells develop cross-resistance to many agents such as anthracyclin, vinca alkaloids and colchicine. In our hypothesis, MDR phenomenon could be implicated in acquired resistance to DMARDs in RA. We have established a mdr1 cell line and tested whether DMARDs are substrate for P-glycoprotein (P-gp). METHODS: The mdr1-cDNA was cloned into retroviral vector, and the recombinant retroviral vector was transfected into PA317 cells. The target cells, NIH3T3, were infected with recombinant retroviruses. A colony most resistant to vinblastin was selected for the following experiments; expression of mdr1 gene in NIH3T3 cells was confirmed by RT-PCR, and biological function of mdr1 gene product, P-gp, was tested using Rhodamine-123 (Rh123) efflux assay. Resistance of the target cells expression P-gp which can survive against hydroxychloroquine (HCQ) and methotrxate (MTX) were measured by MTT assay. RESULTS: RT-PCR for mdr1 gene showed successful transfer of the gene into the NIH3T3 cells. Rh123 assay revealed expression of P-gp on the selected cells as follows; Rh123 efflux activity of uninfected NIH3T3 cells was 6%, that of PLXSN was 0.2%, and that of selected cells was 44%. The 50% proliferation inhibitory capacity of the selected cells were twice for HCQ but there was no difference of that for MTX. CONCLUSION: We established a mdr1 cell line and using the cell line, HCQ was a substrate of MDR, but MTX was not related to MDR.


Subject(s)
Antirheumatic Agents , Arthritis, Rheumatoid , Cell Line , Clone Cells , Colchicine , Drug Resistance, Multiple , Hydroxychloroquine , Methotrexate , ATP Binding Cassette Transporter, Subfamily B, Member 1 , Retroviridae , United Nations , Vinca Alkaloids , Zidovudine
19.
PAFMJ-Pakistan Armed Forces Medical Journal. 2003; 53 (2): 168-171
in English | IMEMR | ID: emr-64122

ABSTRACT

Anthracyclines and vinorelbine have shown good response rates as single agent chemotherapy in metastatic breast cancer. A pahse I study has shown improved results by combining these two drugs. On the basis of this we carried out a phase II study in Oncology Department, Combined Military Hospital, Rawalpindi, in which the efficacy and side effects of epirubicin-vinorelbine as first-line chemotherapy in metastatic breast cancer evaluated. The purpose of this phase II study was to observe the effects of combination of epirubicin and vinorelbine in metastatic breast cancer as first-line chemotherapy in our population. From July 2000 to June 2001, chemo naive patients with metastatic breast cancer were given combination chemotherapy comprising epirubicin 100 mg/m2 i.v. infusion on day 1 and vinorelbine 25 mg/m2 i.v infusion on day 1 and 8. A total of six cycles were given to all patients with 3 weekly intervals. Patients with grade 3 and 4 neutropenia were also given G-CSF support. Seven out of 26 patients were pre menopausal and 73.07% were post menopausal. All patients had WHO performance status of > 3. Four [15.38%] out of 26 patients had complete response [CR] and 53.84% had partial response [PR] making and overall response of 69.22 and. Stable disease was observed in 5[19.23%] patients whereas 3 [11.53%] had progressive disease. Neutropenia was the most common side effect observed which was grade 4 in 6[23.07%] patients and grade 3 in 10 [38.46%] patients. Other side effects were mild to moderate. As first line chemotherapyv in treatment of metastatic breast cancer, the combination of epirubicin and vinorelbine is an active and cost effective regimen, with less side effects and excellent tolerability


Subject(s)
Humans , Female , Neoplasm Metastasis , Epirubicin , Antineoplastic Combined Chemotherapy Protocols , Vinca Alkaloids
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