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2.
Lett Appl Microbiol ; 74(4): 564-576, 2022 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-34958703

RESUMEN

Vulvovaginal candidiasis (VVC) is an infectious disease caused mainly by Candida albicans. Kangfuxin (KFX) is a traditional Chinese medicine preparation made from Periplaneta americana extracts, which promotes wound healing and enhances body immunity and also acts as an antifungal agent. Here, we evaluated the effect of KFX in the treatment of VVC in vitro and in vivo. The minimum inhibitory concentration (MIC50 ) of KFX against C. albicans ranged from 7·65 to 20·57%. In addition, KFX was more efficient than fluconazole (FLC) in inhibiting the drug-resistant C. albicans, and the effect was more intense after 8 h. The KFX treatment also exhibited good activity in vivo. It restored the body weight and reduced the vulvovaginal symptoms in mice induced with VVC. It downregulated the expression of the hyphae-related gene, HWP1, thus inhibiting the growth and development of C. albicans hyphae. It also increased the number of neutrophils and promoted the secretion of interleukin-17A (IL-17A); however, the levels of interleukin-8 (IL-8) and interleukin-1ß (IL-1ß) decreased in mice with VVC. We deduce that KFX effectively treats vaginal candidiasis in two ways: by inhibiting the growth and development of mycelia to reduce colonization of C. albicans and by promoting the secretion and release of IL-17A and neutrophils in high numbers to fight C. albicans infection. This study provides a theoretical basis for the use of KFX for the clinical treatment of VVC.


Asunto(s)
Candidiasis Vulvovaginal , Materia Medica , Animales , Antifúngicos/farmacología , Antifúngicos/uso terapéutico , Candida albicans , Candidiasis Vulvovaginal/tratamiento farmacológico , Candidiasis Vulvovaginal/microbiología , Femenino , Fluconazol/farmacología , Fluconazol/uso terapéutico , Materia Medica/farmacología , Materia Medica/uso terapéutico , Ratones
3.
Zhonghua Wai Ke Za Zhi ; 57(9): 666-672, 2019 Sep 01.
Artículo en Chino | MEDLINE | ID: mdl-31474058

RESUMEN

Objective: To analyze the status of domestic surgical treatment of synchronous peritoneal carcinomatosis from colorectal cancer in China. Methods: Clinicopathological data of patients who underwent surgery from October 2003 to October 2018 in 16 domestic medical centers was retrospectively analyzed. Excel database was created which covered 77 fields of 7 parts: baseline information of patients, laboratory tests, imaging tests, chemoradiotherapy information, intra-operative findings, postoperative pathology and follow-up data. The Wilcoxon rank-sum test was used for comparison of the measurement data between groups. The χ(2) test was used for comparison of the categorical data between groups. The survival curve was calculated by the Kaplan-Meier method. Results: Of the 1 003 patients, there were 575 male and 428 female patients with the age of (58.5±14.1) years (range: 18 to 92 years). In a total of 920 patients, the carcinoma of sigmoid colon was performed in 292 cases (31.8%) with the highest ratio. The proportion of patients with liver metastasis and lung metastasis were 27.9% (219/784) and 8.3% (64/769). Preoperative detection of carcino-embryonic antigen level was the most common method in China (87.74%, 880/1 003), and the positive rate was 64.5% (568/880). The correct rate of preoperative imaging tests was 40.7% (280/688). The ratio of peritoneal carcinomatosis index (PCI) scores between 0 and 10 was the highest (59.6%, 170/285). Two hundred and sixty-two (27.0%) patients were performed by totally laparoscopic operation in 971 patients. The resection of primary tumor was performed in 588 of the 817 patients (72.0%). In a total of 457 cases, 253 (55.4%) patients were performed cytoreduction which group scored completeness of cytoreduction (CCR) 0. The postoperative hyperthermic intraperitoneal chemotherapy was implemented in 70 of the 334 cases (21.0%). Among 1 003 cases, 562 cases (56.03%) had complete follow-up data and the median overall survival was 15 months. The primary tumor resection and the CCR scores were affected by the PCI scores. The patients underwent primary tumor resection (187/205 vs. 26/80, χ(2)=105.085, P=0.000) and the patients were performed cytoreduction which scored CCR 0 or CCR 1 (162/204 vs. 8/78, Z=-10.465, P=0.000) had significant difference between the groups of PCI<20 and ≥20. There was a close correlation between the surgical method and the CCR scores (Z=-3.246,P=0.001).When the maximum degree of tumor reduction was planned, most surgeons would choose laparotomy. The overall survival time was longer in patients with primary tumor resection (P=0.000). The median survival time was 18.6 months in the group of primary tumor resection. Conclusions: It is difficult to diagnose the synchronous peritoneal carcinomatosis from colorectal cancer before the operation. Primary tumor resection has an obvious effect to prolong the survival time. It is necessary to standardize the treatment of peritoneal metastasis.


Asunto(s)
Neoplasias Colorrectales/patología , Neoplasias Primarias Múltiples/diagnóstico , Neoplasias Primarias Múltiples/terapia , Neoplasias Peritoneales/diagnóstico , Neoplasias Peritoneales/terapia , Adolescente , Adulto , Anciano , Anciano de 80 o más Años , Protocolos de Quimioterapia Combinada Antineoplásica/administración & dosificación , China , Neoplasias Colorrectales/terapia , Terapia Combinada , Procedimientos Quirúrgicos de Citorreducción , Femenino , Humanos , Hipertermia Inducida , Laparoscopía , Masculino , Persona de Mediana Edad , Neoplasias Peritoneales/mortalidad , Neoplasias Peritoneales/secundario , Estudios Retrospectivos , Tasa de Supervivencia , Adulto Joven
4.
Zhonghua Zhong Liu Za Zhi ; 41(2): 118-123, 2019 Feb 23.
Artículo en Chino | MEDLINE | ID: mdl-30862141

RESUMEN

Objective: To investigate the therapeutic effect of Jin Long Capsule (JLC) combined with neoadjuvant chemotherapy on the invasive breast cancer, and to explore the mechanism of JLC in inhibiting multidrug resistance of breast cancer. Methods: 200 patients were divided into experimental group and control group (100 cases per group). The control group used TEC regimen for neoadjuvant chemotherapy. And the experimental group was treated with TEC regimen combined with oral JLC. According to the Miller & Payne grading system (MP), the efficacy of neoadjuvant chemotherapy was evaluated based on histopathological changes of breast cancer after neoadjuvant chemotherapy. Adverse effect was evaluated according to the classification criteria of the National Cancer Institute of the United States-The Common Terminology Criteria for Adverse Events (CTCAE) version 3.0. The expression of P-glycoprotein (P-gp), glutathione thiol transferase (GST)-π and topoisomerase Ⅱα (TopoⅡα) in breast cancer tissues before and after neoadjuvant chemotherapy were detected by immunohistochemical staining. Results: There were 83 effective cases (83%) in the experimental group, which was higher than that in the control group (65.0%, P<0.05). The incidence of leukopenia, gastrointestinal reactions and alopecia in grade 3 to 4 of the experimental group were lower than those of the control group (all P<0.05). The positive rates of P-gp, GST-π and TopoⅡα expression in the control group were 65.0% (65/100), 61.0% (61/100) and 69.0% (69/100), respectively, and they were 80.6% (75/93), 78.5% (73/93) and 37.6% (35/93) after chemotherapy. The positive rates of P-gp and GST-π expression were significantly higher than those before chemotherapy (both P<0.05), whereas the positive rate of TopoⅡα expression was significantly lower than that before chemotherapy (P<0.05). In the experimental group, the positive rates of P-gp, GST-π and TopoⅡα expression before chemotherapy were 62.0% (62/100), 63.0% (63/100) and 69.0% (69/100), respectively, while after chemotherapy, they were 68.2% (60/88), 67.0% (59/88) and 63.6% (56/88). There was no significant difference in the positive rates and expression intensity of P-gp, GST-π and TopoⅡα before and after the chemotherapy (P>0.05). Conclusion: Jin Long Capsule (JLC) can inhibit multidrug resistance, improve the efficacy of neoadjuvant chemotherapy, and reduce adverse reactions of breast cancer.


Asunto(s)
Miembro 1 de la Subfamilia B de Casetes de Unión a ATP/metabolismo , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapéutico , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/metabolismo , Resistencia a Antineoplásicos , Medicamentos Herbarios Chinos/uso terapéutico , Terapia Neoadyuvante , Subfamilia B de Transportador de Casetes de Unión a ATP , Protocolos de Quimioterapia Combinada Antineoplásica/administración & dosificación , Protocolos de Quimioterapia Combinada Antineoplásica/efectos adversos , Neoplasias de la Mama/patología , Cápsulas , Quimioterapia Adyuvante/efectos adversos , Ciclofosfamida/administración & dosificación , Ciclofosfamida/efectos adversos , ADN-Topoisomerasas de Tipo II/metabolismo , Etopósido/administración & dosificación , Etopósido/efectos adversos , Femenino , Glutatión Transferasa/metabolismo , Humanos , Terapia Neoadyuvante/efectos adversos , Taxoides/administración & dosificación , Taxoides/efectos adversos
5.
Blood Cancer J ; 4: eXX, 2014 Oct 10.
Artículo en Inglés | MEDLINE | ID: mdl-25303370

RESUMEN

Chronic Helicobacter pylori-stimulated immune reactions determine the pathogenesis of gastric mucosa-associated lymphoid tissue (MALT) lymphoma. We aimed to explore the genetic predisposition to this lymphoma and its clinical implication. A total of 68 patients and 140 unrelated controls were genotyped for 84 single-nucleotide polymorphisms in genes encoding cytokines, chemokines and related receptors that play important roles in T cell-mediated gastrointestinal immunity. Five genotypes in IL-22, namely CC at rs1179246, CC at rs2227485, AA at rs4913428, AA at rs1026788 and TT at rs7314777, were associated with disease susceptibility. The former four genotypes resided in the same linkage disequilibrium block (r(2)=0.99) that conferred an approximately threefold higher risk. In vitro experiments demonstrated that co-culturing peripheral mononuclear cells or CD4(+) T cells with H. pylori stimulated the secretion of interleukin-22 (IL-22), and that IL-22 induced the expression of antimicrobial proteins, RegIIIα and lipocalin-2, in gastric epithelial cells. Furthermore, patients with gastric tissue expressing IL-22 were more likely to respond to H. pylori eradication (14/22 vs 4/19, P<0.006). We conclude that susceptibility of gastric MALT lymphoma is influenced by genetic polymorphisms in IL-22, the product of which is involved in mucosal immunity against H. pylori and associated with tumor response to H. pylori eradication.


Asunto(s)
Regulación Neoplásica de la Expresión Génica , Predisposición Genética a la Enfermedad , Infecciones por Helicobacter , Helicobacter pylori , Interleucinas , Linfoma de Células B de la Zona Marginal , Proteínas de Neoplasias , Polimorfismo de Nucleótido Simple , Neoplasias Gástricas , Linfocitos T CD4-Positivos/metabolismo , Línea Celular Tumoral , Femenino , Infecciones por Helicobacter/genética , Infecciones por Helicobacter/metabolismo , Infecciones por Helicobacter/terapia , Humanos , Interleucinas/biosíntesis , Interleucinas/genética , Linfoma de Células B de la Zona Marginal/genética , Linfoma de Células B de la Zona Marginal/metabolismo , Linfoma de Células B de la Zona Marginal/microbiología , Linfoma de Células B de la Zona Marginal/terapia , Masculino , Proteínas de Neoplasias/biosíntesis , Proteínas de Neoplasias/genética , Neoplasias Gástricas/genética , Neoplasias Gástricas/metabolismo , Neoplasias Gástricas/microbiología , Neoplasias Gástricas/terapia , Interleucina-22
6.
Transplant Proc ; 45(10): 3546-9, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-24314955

RESUMEN

OBJECTIVES: Renal ischemia and reperfusion (I/R) injury frequently leads to acute renal failure (ARF) and multiple-organ injury with a substantial morbidity rate. The primary cause of ARF-associated death is, however, cardiac failure instead of renal failure itself, and the pathogenesis of renal I/R-induced cardiac injury is still poorly understood. We evaluated the efficacy of curcumin pretreatment on cardioprotection. METHODS: Thirty Sprague-Dawley rats were evenly divided into 3 groups of sham-operated control, renal I/R injury, and a curcumin pretreatment group. Renal ischemia was conducted by bilateral occlusions of pedicles for 45 minutes, followed by 3 hours of reperfusion. The cardiac function was assessed by the left ventricular end-systolic-pressure-volume-relation (ESPVR), systolic pressure (SP), ejection fraction (EF), and stroke volume (SV). Myocardial injury was assessed based on creatine kinase muscle brain fraction (CK-MB) and Troponin I (cTnI), and kidney injury was assessed based on blood urea nitrogen (BUN) and creatinine. We also assessed the levels of tumor necrosis factor-α (TNF-α) and malondialdehyde (MDA) in the heart tissues. RESULTS: SV, EF, and SP reduced moderately during the ischemic phase with no major change in ESPVR. During reperfusion, SV, SP, and ESPVR initially increased, and then steadily decreased. Myocardial and kidney injury were marked by the increases in serum CK-MB and cTnI, and creatinine and BUN level. Curcumin pretreatment ameliorated ESPVR and attenuated injuries of both the heart and kidney resulting from I/R insult. CONCLUSIONS: Curcumin pretreatment improved cardiac contractility and attenuated myocardial and renal injury through reducing inflammatory response in the kidney and heart and oxidative stress in the myocardium.


Asunto(s)
Lesión Renal Aguda/prevención & control , Curcumina/farmacología , Cardiopatías/prevención & control , Corazón/efectos de los fármacos , Riñón/efectos de los fármacos , Daño por Reperfusión/prevención & control , Lesión Renal Aguda/sangre , Lesión Renal Aguda/fisiopatología , Animales , Biomarcadores/sangre , Nitrógeno de la Urea Sanguínea , Forma MB de la Creatina-Quinasa/sangre , Creatinina/sangre , Citoprotección , Modelos Animales de Enfermedad , Corazón/fisiopatología , Cardiopatías/sangre , Cardiopatías/fisiopatología , Mediadores de Inflamación/metabolismo , Riñón/irrigación sanguínea , Riñón/metabolismo , Malondialdehído/metabolismo , Contracción Miocárdica/efectos de los fármacos , Miocardio/metabolismo , Estrés Oxidativo/efectos de los fármacos , Ratas , Ratas Sprague-Dawley , Daño por Reperfusión/sangre , Daño por Reperfusión/fisiopatología , Volumen Sistólico/efectos de los fármacos , Troponina I/sangre , Factor de Necrosis Tumoral alfa/metabolismo , Función Ventricular Izquierda/efectos de los fármacos , Presión Ventricular/efectos de los fármacos
7.
Opt Express ; 20(1): A119-24, 2012 Jan 02.
Artículo en Inglés | MEDLINE | ID: mdl-22379672

RESUMEN

Vertical GaN-based light-emitting diodes (LEDs) were fabricated with a Si substrate using the wafer-bonding technique. Lapping and dry-etching processes were performed for thinning the sapphire substrate instead of removing this substrate using the laser lift-off technique and the thinning process associated with the wafer-bonding technique to feature LEDs with a sapphire-face-up structure and vertical conduction property. Compared with conventional lateral GaN/sapphire-based LEDs, GaN/Si-based vertical LEDs exhibit higher light output power and less power degradation at a high driving current, which could be attributed to the fact that vertical LEDs behave in a manner similar to flip-chip GaN/sapphire LEDs with excellent heat conduction. In addition, with an injection current of 350 mA, the output power (or forward voltage) of fabricated vertical LEDs can be enhanced (or reduced) by a magnitude of 60% (or 5%) compared with conventional GaN/sapphire-based LEDs.


Asunto(s)
Óxido de Aluminio/química , Galio/química , Indio/química , Iluminación/instrumentación , Semiconductores , Diseño de Equipo , Análisis de Falla de Equipo
8.
Eur J Clin Nutr ; 60(1): 136-41, 2006 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-16234843

RESUMEN

Infant formulas are often heat sterilized in hospitals where water contamination or nosocomial infection is a concern, but there are few studies of the effect of high heat on the nutritional value of infant formula. In particular, the effect of heat sterilization on free amino acid (FAA) concentrations is seldom discussed. In view of the importance of these nutrients for infant growth, we investigated the FAA concentrations of infant formula after heat sterilization. Powdered infant formulas were reconstituted with hot water (80 degrees C) in glass bottles and placed in an autoclave for 5 min at 105 degrees C and 5600 kg/m2 of pressure. Additional samples of formula were prepared by conventional methods to serve as controls. After autoclaving, we measured the FAA concentrations with ion exchange chromatography. The results were compared with those obtained after conventional preparation. We found a 19.5% lower amount of total protein after autoclaving compared with conventional preparation. Concentrations of total FAA were significantly lower after autoclaving (696.5 +/- 101.4 vs 899.4 +/- 152.2 micromol/l, P = 0.01). The concentrations of individual amino acids were also lower in autoclaved infant formulas, with differences ranging from -4.1 to 71.5% (mean 22.6%). Concentrations of certain amino acids were more than 30% lower, such as valine (71.5%), citrulline (61.1%), glutamine (60.6%), ethanolamine (54%), and lysine (39.2%). Both essential and nonessential amino acids were similarly affected by autoclaving, 28.17 and 27.13%, respectively, lower than in controls (P = 0.37). The concentration of ammonia was significantly higher after autoclaving (645.2 +/- 76.2 vs 393.2 +/-140.7 micromol/l, P = 0.0003). However, the urea level was significantly lower after autoclaving than after conventional preparation (1110.8 +/- 162.7 vs 1426.5 +/- 209.5 micromol/l, P = 0.0004). The accumulation of ammonia may reflect degradation of protein and amino acids. Autoclaving clearly results in decreased concentrations of FAA in infant formula. The increased concentration of ammonia after autoclaving is of concern if it leads to deleterious effects.


Asunto(s)
Aminoácidos/análisis , Manipulación de Alimentos , Calor/efectos adversos , Fórmulas Infantiles/química , Fenómenos Fisiológicos Nutricionales del Lactante , Amoníaco/efectos adversos , Amoníaco/análisis , Cromatografía por Intercambio Iónico/métodos , Humanos , Lactante , Fórmulas Infantiles/normas , Recién Nacido , Valor Nutritivo
9.
Eye (Lond) ; 18(5): 470-3, 2004 May.
Artículo en Inglés | MEDLINE | ID: mdl-15131676

RESUMEN

BACKGROUND AND PURPOSE: Patients are increasingly well informed about the availability of antioxidant products and the claims made for their benefits in age-related macular degeneration (AMD). Consequently, their use is becoming widespread. The purpose of this study is to conduct a survey of the commonly encountered products, and to compare their ingredients with the current Age-Related Eye Disease Study (AREDS) recommendations. METHODS: A search was undertaken for products sold as 'eye nutrients' at local pharmacies and health food shops, and for products advertised via the Internet. Information about these products was collated and analysed. RESULTS: We identified 22 eye nutrient products. Analysis of their constituents showed that, although over 75% contained all the constituents used in AREDS, only two matched the dosage profiles recommended in the study. CONCLUSION: The authors draw no conclusion on the efficacy of nutritional supplements in the prevention of AMD. In order to advise their patients, ophthalmologists should be familiar with these products. The compiled list in this paper should provide a useful reference for them.


Asunto(s)
Antioxidantes/administración & dosificación , Suplementos Dietéticos , Degeneración Macular/prevención & control , Antioxidantes/química , Antioxidantes/provisión & distribución , Ácido Ascórbico/administración & dosificación , Cobre/administración & dosificación , Suplementos Dietéticos/análisis , Humanos , Degeneración Macular/dietoterapia , Vitamina E/administración & dosificación , Zinc/administración & dosificación , beta Caroteno/administración & dosificación
10.
J Glaucoma ; 7(6): 413-6, 1998 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-9871864

RESUMEN

PURPOSE: To assess the influence of adrenaline and hyaluronidase on pulsatile ocular blood flow and intraocular pressure changes during retrobulbar anesthesia. METHOD: Patients undergoing cataract surgery under local anesthesia received a 5-mL retrobulbar injection of lignocaine with either adrenaline, hyaluronidase, or no addition. Continuous pneumotonometry was performed using the OBF tonograph (OBF Labs, Chippenham, UK), which automatically derives pulsatile ocular blood flow values. Measurements were taken before and one minute after injection, and changes were compared between groups to evaluate the effects of changing the constituents of the injection. RESULTS: There was a marked decrease in pulsatile ocular blood flow during injection in all groups. In the group receiving lignocaine with hyaluronidase, the decrease in pulsatile ocular blood flow (mean -141 microL/min) was significantly less than in either the group receiving lignocaine and adrenaline (mean -249 microL/min) or the group receiving lignocaine alone (mean -245 microL/min). There was no significant change in intraocular pressure in any group. CONCLUSION: Hyaluronidase appears to lessen the reduction in pulsatile ocular blood flow. Injection volumes of 5 mL need not cause significant intraocular pressure change.


Asunto(s)
Anestésicos Locales/administración & dosificación , Epinefrina/administración & dosificación , Ojo/irrigación sanguínea , Hialuronoglucosaminidasa/administración & dosificación , Presión Intraocular/efectos de los fármacos , Lidocaína/administración & dosificación , Anestesia Local , Velocidad del Flujo Sanguíneo/efectos de los fármacos , Presión Sanguínea/efectos de los fármacos , Extracción de Catarata , Combinación de Medicamentos , Sinergismo Farmacológico , Frecuencia Cardíaca/efectos de los fármacos , Humanos , Inyecciones , Órbita , Flujo Pulsátil , Tonometría Ocular
11.
Zhongguo Yao Li Xue Bao ; 14 Suppl: S28-30, 1993 Nov.
Artículo en Chino | MEDLINE | ID: mdl-8010069

RESUMEN

A semi-solid cell culture technique was used to study the sensitivity of K562, HL-60, and Raji leukemic cell lines to the inhibitory effect of psoralen plus ultraviolet irradiation. Results indicated that: 1) the inhibition rate of K562, HL-60, and Raji cell lines were 86%, 35%, and 36%, respectively; and 2) K562, HL-60, and Raji cell lines were treated with psoralen (20 micrograms.ml-1) for 1 h, then irradiated with ultraviolet (1 J/cm2) for 10 min, none of the leukemic cell lines showed colony or cluster formation. These suggested that the cytocidal effect of psoralen plus ultraviolet might be useful to eradicate the residual leukemic cells in the bone marrow transplantation.


Asunto(s)
Leucemia Eritroblástica Aguda/patología , Terapia PUVA , Ficusina/farmacología , Humanos , Leucemia de Células B/patología , Leucemia Promielocítica Aguda/patología , Células Tumorales Cultivadas/efectos de los fármacos , Ensayo de Tumor de Célula Madre
12.
Zhongguo Yao Li Xue Bao ; 13(1): 69-71, 1992 Jan.
Artículo en Chino | MEDLINE | ID: mdl-1605039

RESUMEN

The effects of silybin (Sil) on myocardial infarction size and ischemia- and reperfusion-induced arrhythmias were studied in anesthetized open chest Sprague-Dawley rats. It was found that pretreatment with Sil 20, 50, and 80 mg.kg-1 iv reduced significantly infarct size by 34.7%, 35.0%, and 50.6% respectively at 4 h after ligation. Sil prevented ischemic arrhythmia only at the dose of 80 mg.kg-1. In reperfusion experiment, pretreatment with Sil 20 mg.kg-1 decreased significantly reperfusion-induced arrhythmia.


Asunto(s)
Arritmias Cardíacas/prevención & control , Infarto del Miocardio/tratamiento farmacológico , Silimarina/uso terapéutico , Animales , Arritmias Cardíacas/etiología , Masculino , Infarto del Miocardio/patología , Daño por Reperfusión Miocárdica/complicaciones , Ratas , Ratas Endogámicas
15.
Adv Exp Med Biol ; 163: 101-14, 1983.
Artículo en Inglés | MEDLINE | ID: mdl-6613723

RESUMEN

A variety of quinazoline analogues of folic acid (5,8-dideazafolates) are of interest as potential antineoplastic agents, biochemical probes, and/or affinity ligands for the purification of folate requiring enzymes. Chief among these are 5,8-dideazaisopteroylglutamate, 5,8-dideazaisoPteGlu, (IAHQ), a compound with proven activity against the growth of human colon adenocarcinoma cells in vitro, and 10-formyl-5,8-dideazapteroylglutamic acid, which serves as a substrate for glycinamide ribonucleotide transformylase and is also an effective inhibitor of mammalian thymidylate synthase. New methods for preparing these compounds in excellent purity as determined by high performance liquid chromatography (HPLC) have been developed. In each case the carboxyl groups of L-glutamic acid are protected with t-butyl ester groups, since these can subsequently be removed readily using trifluoroacetic acid without decomposition or racemization of the final product. This approach has proven to be of particular value in the formation of gamma-L-glutamyl derivatives of IAHQ containing 1-3 additional glutamyl residues.


Asunto(s)
Ácido Fólico/análogos & derivados , Ácidos Pteroilpoliglutámicos/síntesis química , Quinazolinas/síntesis química , Línea Celular , Supervivencia Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Neoplasias del Colon/fisiopatología , Evaluación Preclínica de Medicamentos , Humanos , Indicadores y Reactivos , Ácidos Pteroilpoliglutámicos/toxicidad , Quinazolinas/toxicidad , Relación Estructura-Actividad
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