RESUMEN
Ben Cao Tu Jing had 48 materia medica illustrations related to the regional names in Shandong province. It was found that 42 of them were plant medicinal materials, distributed in seven areas in Shandong province. This study examined these illustration of plant medicinal materials and found that 26 species of these illustration of plant medicinal materials were identified with three genera and 11 illustrations were unverified. Most materia medica illustrations relating to the regional names in Shandong province were found mainly in Yanzhou, Qizhou and Zizhou. This indicated that materia medica were widely used in these areas in the Northern Song Dynasty. The haustorium of Cuscuta Chinensis were depicted in the "Shanzhou Tu Si Zi" and the habitat of wild poriacocos was described. This showed that the illustrators of Ben Cao Tu Jing might have conducted fieldwork and reflected on the main principles about how to identify materia medica in Ben Cao Tu Jing Zou Chi. Inconsistencies were found between the illustrations and the expressions of plant medicinal materials in some illustrations, such as Gui Jiu, Ginsen and Shan Zhu Yu. This suggested that in the Northern Song Dynasty Stemmacantha Uniflora, Belamcanda chinensis might have been mixed up with Dysosma and Pinellia Pedatisecta might have been mixed up with Pinellia Ternata. This was in line with the compiling theories of Su Song that they could be recorded together when the illustrations and literature were inconsistent with each other.
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Materia Medica , ChinaRESUMEN
Ben Cao Tu Jing had 38 materia medica illustrations related to the regional names in Zhejiang province. It was found that 30 of them were identified as being named after regional names in Zhejiang province, involving 20 families and 29 genera. One of the 38 materia medica illustrations was mineral medicine and seven of them were unverified. The twenty-five of these materia medica illustrations with regional names were found to be consistent with their names used today. Five of them came from similar names in Zhejiang province in the Northern Song Dynasty, another five of the 25 names were known with the names but not entity for the lack of full descriptions and drawings. It was found that the drawing and the text of "Ming Zhou Huang Yao" and "Qin Zhou Hong Yao" in Ben Cao Tu Jing were reversed. By comparing the materia medica illustrations related to regional names in Da Guan Ben Cao by Liu Jia and Zheng He Ben Cao by Zhang Huicun, the name and the illustration of "Jin Zhou Bei Mu" in Zheng He Ben Cao by Zhang Huicun was more believable than "Yue Zhou Bei Mu" in Da Guan Ben Cao by Liu Jia. "Tai Zhou Wu Yao" and "Zhe Ba Wei", as genuine medicinal materials in Zhejiang, can be traced back to the illustrations of "Tai Zhou Wu Yao", "Yue Zhou Bai Zhu", "Mu Zhou Mai Dong", "Wen Zhou Peng 'e Shu", "Yue Zhou Bei Mu" and "Tian Tai Wu Yao" in Ben Cao Tu Jing. These findings provided text and drawing literature of herbs in the Song Dynasty for the research of genuine medicinal materials and their characteristics in Zhejiang province. They also showed that the utilization and development of the resources of traditional Chinese medicine in Zhejiang in the Northern Song Dynasty mainly focused on the coastal areas.
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Materia Medica , Libros , China , Humanos , Medicina Tradicional ChinaRESUMEN
A total of 568 paintings of herbaceous plants and woody plants as medicine were involved in Ben Cao Tu Jing, accounting for 60% of the total drug illustrations and 76% of the botanical medicine paintings. These medicinal paintings can be classified into four types: original plant paintings, medicinal material paintings, plant and medicinal material paintings, and plant and their habitat paintings. The original plant paintings can be specifically divided into five sections: the whole plant paintings with roots, partial aerial part paintings with roots, plant paintings with ground lines, rootless plant paintings, and broken branch paintings. Among them, the drawings of " the broken branch paintings " and " the whole plant paintings with roots " are consistent with the basic principles of collecting plant specimens. Additionally, "the plant and medicinal material paintings " and "the medicinal material paintings "reflect that they were drawn based on the market survey of medicinal materials or collected medicinal materials specimens. These medicine painting demonstrate rich characteristics of medicinal plants and medicinal materials and a high artistic quality with realistic details.These paintings in Ben Cao Tu Jing echoes Tu Jing, combine the art of painting with the cognition ofnatural science, as the rudiment of early paintings of plant science.
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Medicina , Pinturas , Plantas Medicinales , Medicina Tradicional China , Raíces de PlantasRESUMEN
Being a common materia medica, the confusion of Jixuetengcaused by the homonyms of different substances for Jixuetengis always very complicated. Fengqing JixuetengPaste was first created in the Qing Dynasty. Fengqing Jixuetengwas derived from the dried stems of a variety of species in KadsuraJuss. and SchisandraMichx. from Schisandracea; while Kunming Jixueteng, derived from the dried stem of Millettia dielsianaHarms ex Diels, was firstly recorded in the Zhi wu ming shi tu kao(Textual Research on Reality and Titles of Plants). The earliest records of Spatholobus suberectusDunn as the original plant of Jixuetengwas in Guang xi ben cao xuan bian(Selected Compilation of Chinese Materia Medica in Guangxi). It was not until 1997 that Spatholobus suberectusDunn was recorded as an origin of orthodox product of Jixuetengin the Chinese Pharmacopoeia. At present, the origins of Jixuetengis very complicated as recorded in different provincial standards, including three species of three genus from Leguminosae.The varieties of species from KadsuraJuss. and SchisandraMichx. had long been used as Fengqing Jixueteng, but currently the most extensively used one is Spatholobus suberectusDunn as Jixueteng. There are more differences in records of Jixuetengin history up to the present, hence, further investigation and research on Jixuetengis still necessary.
RESUMEN
The effects of zinc chloride (ZnCl2), disodium zinc ethylenediamine tetraacetate (Zn-EDTA), and zinc gluconate (Zn-GLU) on the antioxidant enzyme activities and levels of interleukins (ILs) in psoriasis-induced mice were studied. One hundred twenty female mice were randomly divided into six groups with 20 mice in each group: the control, positive control (PC), methotrexate (MTX), ZnCl2, Zn-EDTA, and Zn-GLU groups. All animals except the control group were given diethylstilbestrol for three consecutive days. After successfully inducing psoriasis, the control and PC groups were given normal saline (i.g.) daily while the remaining groups were given MTX, ZnCl2, Zn-EDTA, and Zn-GLU, respectively. The results revealed that the zinc supplementation could significantly (p < 0.05) inhibit mitosis in the mouse vaginal epithelium as methotrexate did and the inhibiting efficacy had nothing to do with the zinc forms. After ZnCl2, Zn-EDTA, and Zn-GLU supplementation, the levels of liver superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), and catalase (CAT) activities increased and the concentration of malondialdehyde (MDA) decreased significantly (p < 0.05) compared to the PC group. The levels of SOD, CAT activity, and MDA level between each zinc supplementation group and MTX group were insignificant (p > 0.05). The zinc treatments also caused a significant (p < 0.05) decrease in the raised IL-2 level of animal serum. The results obtained in the present work indicate the potential for zinc as a complementary pharmaceutical intervention for the treatment of topical psoriasis.
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Antioxidantes/metabolismo , Interleucinas/metabolismo , Psoriasis/tratamiento farmacológico , Psoriasis/metabolismo , Zinc/uso terapéutico , Animales , Catalasa/metabolismo , Femenino , Glutatión Peroxidasa/metabolismo , Interleucina-2/sangre , Peroxidación de Lípido/efectos de los fármacos , Hígado/efectos de los fármacos , Hígado/metabolismo , Malondialdehído/metabolismo , Ratones , Estrés Oxidativo/efectos de los fármacos , Psoriasis/sangre , Superóxido Dismutasa/metabolismoRESUMEN
In China, Kudingcha has been used for almost 2,000 years as a tea to quench thirst, remove phlegm, refresh the mind, and improve eyesight. The group of large-leaved Kudingcha is coveted for its potential effects on lipid metabolism, which are attributed to the presence of characteristic ingredients. This contribution reviews studies from the past few decades regarding the plant characteristics, ethnobotanical usages, chemical constituents, and related biological activities of the large-leaved Kudingcha (Ilex latifolia Thunb and Ilex kudingcha C.J. Tseng). Triterpenoids, phenolic acids, flavonoids, and essential oils are the main metabolites in the large-leaved Kudingcha, and these ingredients protect the vascular system, regulate lipid metabolism, and have antioxidant, hypoglycemic, and anti-tumor effects. Moreover, large-leaved Kudingcha shares several properties with the popular green tea and the Yerba maté from South America.
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Bebidas , Medicamentos Herbarios Chinos/farmacología , Ilex , Animales , China , Medicamentos Herbarios Chinos/efectos adversos , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/uso terapéutico , Etnofarmacología , Humanos , Ilex/química , Ilex/clasificación , Medicina Tradicional China , Fitoterapia , Hojas de la Planta , Plantas MedicinalesRESUMEN
Embryogenic calli from in vitro grown tillers of Anemarrhena asphodeloides Bunge were successfully cryopreserved by the encapsulation-vitrification technique. Excised embryogenic calli were precultured for 4 days in liquid MS medium supplemented with 2 mg per liter kinetin (KIN), 0.1 mg per liter α-naphthalene acetic acid (NAA) and 0.75 M sucrose, then encapsulated in calcium alginate beads and loaded with a mixture of 2 M glycerol + 0.4 M sucrose for 60 min at 25 +/- 1 degree C. Calli were then dehydrated with the PVS2 solution for 80 min at 0 degree C. After changing the solution with fresh PVS2, calli were directly immersed in liquid nitrogen (LN). After rapid rewarming in a water-bath at 35 degree C for 5 min, calli were washed three times with liquid MS medium supplemented with 2 mg L-1 KIN, 0.1 mg per liter NAA and 1.2 M sucrose, then transferred on solid MS medium supplemented with 2 mg per liter KIN, 0.1 mg per liter NAA, 3 % (w/v) sucrose and 0.75 % (w/v) agar. Cryopreserved cultures were kept in the dark for 5 days prior to exposure to a 14h light/10h dark photoperiod with a light intensity of 36 µmol per square meter per sec provided by white cool fluorescent tubes at 25 +/- 1 degree C. Survival of cryopreserved embryogenic calli reached 80 percent, including after storage for c. 1 year. No significant difference was observed in the morphological development of plants coming from control and cryopreserved embryogenic calli. This encapsulation-vitrification method appears promising for the cryopreservation of A. asphodeloides Bunge germplasm.
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Anemarrhena/embriología , Criopreservación/métodos , Plantas Medicinales/embriología , Semillas/citología , Vitrificación , Alginatos/química , Técnicas de Cultivo de Célula , Células Inmovilizadas/citología , Células Inmovilizadas/metabolismo , Medios de Cultivo/metabolismo , Ácido Glucurónico/química , Glicerol/metabolismo , Ácidos Hexurónicos/química , Cinetina/metabolismo , Semillas/metabolismo , Sacarosa/metabolismoRESUMEN
UNLABELLED: We evaluated vitamin D status in HIV+ and HIV- postmenopausal African-American (AA) and Hispanic women. Most women (74-78%) had insufficient 25-hydroxyvitamin D (25OHD) levels, regardless of HIV status. 25OHD was lower in AA women and women lacking supplement use, providing support for screening and supplementation. Among HIV+ women, 25OHD was associated with current CD4 but not type of antiretroviral therapy. INTRODUCTION: To evaluate vitamin D status and factors associated with vitamin D deficiency and insufficiency in HIV-infected (HIV+) postmenopausal minority women. METHODS: In this cross-sectional study, 89 HIV+ and 95 HIV- postmenopausal women (33% AA and 67% Hispanic) underwent assessment of 25OHD, 1,25-dihydroxyvitamin D, parathyroid hormone, markers of bone turnover and bone mineral density by dual energy X-ray absorptiometry. RESULTS: The prevalence of low 25OHD did not differ by HIV status; the majority of both HIV+ and HIV- women (74-78%) had insufficient levels (<30 ng/ml). Regardless of HIV status, 25OHD was significantly lower in AA subjects, and higher in subjects who used both calcium and multivitamins. In HIV+ women on antiretroviral therapy (ART), 25OHD was directly associated with current CD4 count (r=0.32; p<0.01) independent of age, ethnicity, BMI, or history of AIDS-defining illness. No association was observed between 1,25(OH)(2)D and CD4 count or between serum 25OHD, 1,25(OH)(2)D or PTH and type of ART. CONCLUSIONS: In postmenopausal minority women, vitamin D deficiency was highly prevalent and associated with AA race and lack of supplement use, as well as lower current CD4 cell count. These results provide support for screening and repletion of vitamin D in HIV+ patients.
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Negro o Afroamericano , Infecciones por VIH/inmunología , Hispánicos o Latinos , Deficiencia de Vitamina D/etnología , Vitamina D/análogos & derivados , Absorciometría de Fotón , Anciano , Densidad Ósea , Recuento de Linfocito CD4 , Estudios Transversales , Suplementos Dietéticos , Femenino , Infecciones por VIH/complicaciones , Infecciones por VIH/tratamiento farmacológico , Humanos , Persona de Mediana Edad , Ciudad de Nueva York/epidemiología , Hormona Paratiroidea/sangre , Posmenopausia/sangre , Prevalencia , Estudios Prospectivos , Factores de Riesgo , Vitamina D/sangre , Deficiencia de Vitamina D/complicacionesRESUMEN
BACKGROUND: Second-generation oral H1-antihistamines have become a mainstay of treatment for the symptoms of seasonal allergic rhinitis; however, the effect of olopatadine has not been widely reported to date. OBJECTIVES: To evaluate the efficacy of 2 oral H1-antihistamines, olopatadine and fexofenadine, in the treatment of the nasal symptoms of Japanese cedar pollinosis and their possible side effects. METHODS: This was a randomized, double-blind, placebo-controlled, crossover study conducted in an environmental exposure unit (EEU). Twenty volunteers suffering from Japanese cedar pollinosis were randomly divided into 3 groups and exposed to cedar pollen in the EEU with oral administration of olopatadine hydrochloride (5 mg), fexofenadine hydrochloride (60 mg), or placebo 1 hour prior to pollen exposure. Nasal symptoms, activity impairment, and subjective sleepiness were self-assessed during the study period. Attention was measured using the digit cancellation test. The trial was repeated after 4 and 7 weeks. RESULTS: Compared with placebo, olopatadine significantly improved nasal symptoms and activity impairment during pollen exposure (P < .05). There was no significant relief of nasal discharge or nasal congestion with fexofenadine throughout the 5-hour exposure to cedar pollen. Furthermore, olopatadine significantly reduced nasal congestion during the first 2 hours, as well as sneezing and nasal discharge 4 hours after admission to the EEU compared with fexofenadine (P < .05). There was no significant difference in the effect on subjective sleepiness among the 3 groups, and all 3 agents had little effect on attention. CONCLUSIONS: These findings suggest that olopatadine is more effective than placebo and fexofenadine in improving nasal symptoms of Japanese cedar pollinosis.
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Alérgenos/inmunología , Dibenzoxepinas , Antagonistas de los Receptores Histamínicos H1 no Sedantes , Polen/inmunología , Rinitis Alérgica Estacional/tratamiento farmacológico , Adulto , Cryptomeria/inmunología , Dibenzoxepinas/administración & dosificación , Dibenzoxepinas/efectos adversos , Método Doble Ciego , Femenino , Estudios de Seguimiento , Antagonistas de los Receptores Histamínicos H1 no Sedantes/administración & dosificación , Antagonistas de los Receptores Histamínicos H1 no Sedantes/efectos adversos , Humanos , Masculino , Persona de Mediana Edad , Actividad Motora/efectos de los fármacos , Actividad Motora/inmunología , Clorhidrato de Olopatadina , Rinitis Alérgica Estacional/inmunología , Sueño/efectos de los fármacos , Estornudo/efectos de los fármacos , Terfenadina/administración & dosificación , Terfenadina/efectos adversos , Terfenadina/análogos & derivados , Resultado del TratamientoRESUMEN
AIM: To study the effects of bilobalide on the expression of glial cell line-derived neurotrophic factor (GDNF) and vascular endothelial growth factor (VEGF) in rat astrocytes in vitro. METHODS: Semiquantification polymerase chain reaction (SQ-PCR) was used to investigate GDNF and VEGF mRNA expression in the astrocytes after bilobalide (5, 15, 50, 100 mumol.L-1) treatment. Immunohistochemistry method was used to detect GDNF and VEGF protein expression in cells treated with bilobalide 50 mumol.L-1 for 24 h. RESULTS: GDNF and VEGF mRNA increased markedly after astrocytes were treated with bilobalide 50 mumol.L-1 for 12 h. GDNF and VEGF protein were detected in the cytoplasm of astrocytes after the cells were treated with bilobalide 50 mumol.L-1 for 24 h. CONCLUSION: Bilobalide induced GDNF and VEGF expression in the cultured astrocytes.
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Astrocitos/metabolismo , Ciclopentanos/farmacología , Diterpenos , Factores de Crecimiento Endotelial/biosíntesis , Furanos/farmacología , Linfocinas/biosíntesis , Neurregulina-1/biosíntesis , Animales , Línea Celular , Ciclopentanos/aislamiento & purificación , Factores de Crecimiento Endotelial/genética , Furanos/aislamiento & purificación , Ginkgo biloba/química , Ginkgólidos , Linfocinas/genética , Neurregulina-1/genética , Plantas Medicinales , ARN Mensajero/biosíntesis , ARN Mensajero/genética , Ratas , Factor A de Crecimiento Endotelial Vascular , Factores de Crecimiento Endotelial VascularRESUMEN
OBJECTIVE: To investigate the incidence of cedar pollinosis in district of Wuhan. METHOD: A survey relative to cedar pollinosis was carried out in 309 students in Hubei Medical University in 1999, including questionnaire investigation, nasal inspection and scratch test. From February to April of 2000, a clinical investigation of cedar pollinosis was adopted among 205 patients of allergic rhinitis including scratch test and nasal mucosa test. RESULT: 1. The positive rate of cedar pollen scratch test of 309 students was 7.8%. 2. 59 cases (28.8%) was hypersensitive to cedar pollen clinically in allergen test. CONCLUSION: Cedar pollinosis is one kind of important pollinosis in district of Wuhan and should be paid high attention to.
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Polen , Rinitis Alérgica Perenne/epidemiología , Rinitis Alérgica Estacional/epidemiología , Adolescente , Adulto , Anciano , Alérgenos , Niño , China/epidemiología , Femenino , Humanos , Incidencia , Masculino , Persona de Mediana Edad , Rinitis Alérgica Perenne/etiología , Rinitis Alérgica Estacional/etiologíaRESUMEN
Antifungal activity and minimal fungicidal concentration (MFC) of extracts of garlic, bakeri garlic, Chinese leek, Chinese chive, scallion, onion bulb and shallot bulb against Aspergillus niger, A. flavus and A. fumigatus were examined. These Allium plants possessed antifungal activity, with garlic showing the lowest MFC. With the exception of scallion, the inhibitory effect of Allium plants against three Aspergillus species decreased with increasing incubation and heating temperature (P < 0.05). Acetic acid treatments of the extracts increased the inhibitory effect for all plants against three fungi (P < 0.05), and there was no significant difference in this effect among the three pH (2, 4, 6) treatments (P > 0.05) investigated. Acetic acid, at pH = 4, plus heat treatments of the extracts resulted in a greater inhibitory effect for all Allium plants against the three fungi than heat treatment alone (P < 0.05). Treatments of the extracts with NaCl, at concentrations of 0.2 and 0.4 M, did not affect the inhibitory effect of the plant extracts. The combination of acetic acid plus Allium plants was indicated to be an effective way to inhibit fungal growth.
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Allium , Antifúngicos/farmacología , Aspergillus/efectos de los fármacos , Extractos Vegetales/farmacología , Acetatos , Calor , Cloruro de Sodio/farmacologíaRESUMEN
OBJECTIVE: To investigate the prevalence of Orchard Pollinosis in China. METHOD: From 1995 to 1998, an epidemiological survey on orchard pollinosis was carried on among 1,660 primary and middle school students and 2,167 university students, including questionnaire investigation, nasal inspection and scratch test. From April to June of 1998, a clinical investigation of orchard pollinosis was adopted among 30 patients of allergic rhinitis including scratch test and nasal mucosa test. RESULT: 1. The total positive rate of orchard pollen scratch test was 6.7%, and the prevalence of orchard pollinosis was 0.37%. 2. 5 cases (16.7%) were hypersensitive to orchard pollen clinically in allergen test. CONCLUSION: Orchard pollinosis is one kind of important pollinosis and should be paid high attention to.
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Polen/inmunología , Rinitis Alérgica Perenne/epidemiología , Rinitis Alérgica Estacional/epidemiología , Adolescente , Adulto , Niño , China/epidemiología , Femenino , Humanos , MasculinoRESUMEN
The major side effect of cyclosporin A is severe nephrotoxicity. It is likely that cyclosporin A causes vasoconstriction leading to hypoxia-reperfusion injury; therefore, these experiments were designed to attempt to obtain physical evidence for hypoxia and free radical production in kidney following cyclosporin A. Rats were treated daily with cyclosporin A (25 mg/kg ig) for 5 days, and pimonidazole, a hypoxia marker, was injected 2 h after the last dose of cyclosporin A. A dose of alpha-(4-pyridyl-1-oxide)-N-tert-butylnitrone (4-POBN) was injected 3 h after cyclosporin A to trap free radicals. Cyclosporin A doubled serum creatinine and decreased glomerular filtration rates by 65% as expected. Pimonidazole adduct binding in the kidney was increased nearly threefold by cyclosporin A, providing physical evidence for tissue hypoxia. Moreover, cyclosporin A increased 4-POBN/radical adducts nearly sixfold in the urine but did not alter levels in the serum. Glycine, which causes vasodilatation and prevents cyclosporin A toxicity, minimized hypoxia and blocked free radical production; however, it did not alter cyclosporin A blood levels. These results demonstrate for the first time that cyclosporin A causes hypoxia and increases production of a new free radical species exclusively in the kidney. Therefore, it is concluded that cyclosporin A causes renal injury by mechanisms involving hypoxia-reoxygenation, effects which can be prevented effectively by dietary glycine.
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Ciclosporina/toxicidad , Tasa de Filtración Glomerular/efectos de los fármacos , Glicina/farmacología , Riñón/efectos de los fármacos , Daño por Reperfusión/prevención & control , Animales , Creatinina/sangre , Ciclosporina/antagonistas & inhibidores , Ciclosporina/sangre , Alimentos Fortificados , Radicales Libres/metabolismo , Glicina/administración & dosificación , Hipoxia , Riñón/patología , Riñón/fisiología , Masculino , Modelos Biológicos , Nitroimidazoles/farmacocinética , Ratas , Ratas Sprague-Dawley , Circulación Renal , Factores de Tiempo , VasoconstricciónRESUMEN
The inhibitory effect of water-soluble extracts of garlic bulbs, green garlic, green onions, hot peppers, ginger, Chinese parsley, and basil on the growth of Aspergillus niger and Aspergillus flavus was examined. Garlic bulbs, green garlic, and green onions showed an inhibitory effect against these two fungi. The influence of heat, acid, and salt upon the inhibitory effect of these three herbs was further studied. Increasing the temperature from 60 to 100 degrees C resulted in a significant (P < 0.05) decrease in the inhibitory effect of garlic bulbs against the fungi tested. Green garlic and green onion lost their antifungal activity against A. niger after being treated at 80 and 60 degrees, respectively. For A. flavus, the inhibitory effect of green garlic declined significantly (P < 0.05) with an increase in temperature. However, the antifungal activity of green onions against A. flavus was heat stable. For both fungi tested in this study, the antifungal activity of these spice plants was not affected by acid treatments at pH values 2, 4, or 6, or salt by treatments at concentrations of 0.1, 0.2, 0.3, and 0.4 M (P > 0.05).
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Aspergillus flavus/efectos de los fármacos , Aspergillus niger/efectos de los fármacos , Magnoliopsida/química , Extractos Vegetales/farmacología , Especias , Calor , Concentración de Iones de Hidrógeno , Pruebas de Sensibilidad Microbiana , Cloruro de Sodio/farmacologíaRESUMEN
Compared with the traditional methods, the separation and preparation of oridonin by column chromatography have the advantages of fast speed, harmlessness and non-pollution of solvent, safety, economy and easily obtained, etc. After re-crystallizing the oridonin content is determined by TLC scanning to be as high as 97.03%.
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Diterpenos/aislamiento & purificación , Medicamentos Herbarios Chinos/química , Lamiaceae/química , Plantas Medicinales/química , Tecnología Farmacéutica/métodos , Antineoplásicos Fitogénicos , Cromatografía/métodos , Cromatografía en Capa Delgada , Densitometría , Diterpenos/análisis , Diterpenos de Tipo KauranoRESUMEN
PURPOSE AND METHODS: Although fluoropyrimidines, in particular, fluorouracil (5-FU) and fluorodeoxyuridine (FdUrd), are active alone and in combination with other agents in a variety of human malignancies, therapeutic selectivity, resistance, and efficacy have been a major limitation in cancer therapy. Preclinical and clinical results in advanced and adjuvant colorectal cancers confirmed that the therapeutic efficacy of fluoropyrimidines, with thymidylate synthase (TS) as a primary target, can be improved significantly with leucovorin (LV) modulation. With the recognition that TS is an important therapeutic target, direct and specific inhibitors have been developed and are under intensive preclinical and clinical evaluation, primarily in patients with colorectal cancer, with demonstrable activity. The direct TS inhibitors have been shown to be potent, with a high level of specificity under therapeutic conditions for TS. This includes ZD1694, AG337, and LY231514. To date, although the therapeutic activity of both direct and indirect inhibitors of TS is similar, differences in the magnitude and profile of toxicity have been observed. A phase III comparative evaluation of a direct inhibitor of TS (ZD1694) with an indirect inhibitor (5-FU/LV) has been completed and showed similar activity but reduced toxicity in favor of ZD1694. RESULTS: Recognition that greater than 95% of the injected dose of 5-FU is rapidly inactivated by dihydropyrimidine dehydrogenase (DPD) to therapeutically inactive products, but with toxicity to normal tissues, led to the development of inhibitors of this enzyme with the aim to modify the therapeutic index of 5-FU. Several inhibitors in combination with 5-FU are under preclinical and clinical evaluation, including uracil and 5-chloro-2,4-dihydroxy pyridine, as modulators of 5-FU derived from its prodrug tegafur and 5-ethynyluracil as a modulator of 5-FU. CONCLUSION: In this review, an update of the present status of direct and indirect inhibitors of TS is discussed, as well as the future prospect for new drugs alone and in combination.
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Antimetabolitos Antineoplásicos/uso terapéutico , Neoplasias Colorrectales/tratamiento farmacológico , Timidilato Sintasa/antagonistas & inhibidores , Antimetabolitos Antineoplásicos/metabolismo , Neoplasias Colorrectales/genética , Daño del ADN , ADN de Neoplasias/efectos de los fármacos , Resistencia a Medicamentos , Fluorouracilo/metabolismo , Fluorouracilo/uso terapéutico , Antagonistas del Ácido Fólico/farmacología , Antagonistas del Ácido Fólico/uso terapéutico , Predicción , Humanos , Profármacos/metabolismo , Profármacos/uso terapéutico , Quinazolinas/uso terapéutico , Tiofenos/uso terapéuticoRESUMEN
Adenosine 3',5'-cyclic monophosphate (cAMP) prevents epidermal growth factor (EGF)-induced DNA synthesis in many types of cultured cells, including hepatocytes, but its effects on cellular proliferation in vivo are unknown. This study compares the effects of supplemental cAMP on hepatocyte proliferation induced in vivo by 70% partial hepatectomy (PH) and in vitro by EGF and determines the effects of cAMP on AP-1, a family of growth-regulatory transcription factors, and the kinase cascades that normally activate AP-1. Although injection of dibutyryladenosine 3',5'-cyclic monophosphate (30 mg/kgip) at the time of PH increased liver cAMP concentrations at least 100-fold for several hours, it did not inhibit hepatic incorporation of [3H]thymidine or proliferating cell nuclear antigen expression 24 h after PH. cAMP treatment led to a complete inhibition of extracellular signal-related kinase (ERK) activity and transiently reduced NH2-terminal Jun nuclear kinase (JNK) activity after PH but did not decrease the expression of c-jun mRNA or protein. Consistent with the known cAMP stimulation of jun-B in cultured cells, cAMP treatment increased jun-B mRNA, protein, and DNA binding activity post-PH. Surprisingly, cAMP treatment enhanced Raf kinase activity after PH in rats. In primary hepatocyte cultures, supplemental cAMP inhibited JNK and ERK activity, total AP-1 and c-Jun transcriptional activities, and DNA synthesis. Thus elevated cAMP inhibited ERK and JNK activity in culture and in vivo and inhibited hepatocyte proliferation in culture but not in vivo. This suggests that in vivo mechanisms compensate for cAMP inhibition of certain growth-related signaling cascades and emphasizes potential risks of extrapolating from simple cell culture systems to explain physiology in intact animals.
Asunto(s)
AMP Cíclico/metabolismo , ADN/biosíntesis , Regeneración Hepática , Hígado/citología , Hígado/metabolismo , Proteínas Quinasas Activadas por Mitógenos , Proteínas Quinasas/metabolismo , Animales , Bucladesina/farmacología , Proteínas Quinasas Dependientes de Calcio-Calmodulina/metabolismo , División Celular , Núcleo Celular/metabolismo , Células Cultivadas , Factor de Crecimiento Epidérmico/farmacología , Hepatectomía , Proteínas Quinasas JNK Activadas por Mitógenos , Proteínas Serina-Treonina Quinasas/metabolismo , Proteínas Proto-Oncogénicas/metabolismo , Proteínas Proto-Oncogénicas c-jun/biosíntesis , Proteínas Proto-Oncogénicas c-raf , ARN Mensajero/biosíntesis , Ratas , Factores de Tiempo , Factor de Transcripción AP-1/metabolismo , Transcripción GenéticaRESUMEN
Vitamins E and C are important antioxidants in animals. Their antemortem activity continues to function in postmortem muscle (meat), where they have a critical role in maintaining quality in the food product. Dietary supplementation of vitamin E, and intravenous infusion of vitamin C immediately before harvest, are efficacious techniques for increasing the concentration of these vitamins in beef skeletal muscle. Meat with elevated levels of either and probably both of these antioxidant vitamins possesses greater stability of oxymyoglobin and lipid, which results in less discoloration and rancidity, respectively. A model is proposed for the redox relationships between myoglobin and phospholipid in beef with emphasis on vitamins E and C. Antemortem nutritional intervention appears to be a promising approach for improving the quality of fresh meat products subsequently obtained from livestock.
Asunto(s)
Ácido Ascórbico/administración & dosificación , Bovinos/metabolismo , Carne , Vitamina E/administración & dosificación , Fenómenos Fisiológicos Nutricionales de los Animales , Animales , Ácido Ascórbico/metabolismo , Oxidación-Reducción , Vitamina E/metabolismoRESUMEN
Roots of D. aurantiocaulis and D. pleianthum contain ten lignans: picropodophyllin, podophyllotoxin, 4'-demethylpodophyllotoxin, diphyllin, dehydropodophyllotoxin, podophyllotoxone, picropodophyllone, isopicropodophyllone, 4'-demethylpodophyllotoxone and dysosmajol; two anthraquinones: physcion and dysoanthraquinone. A HPLC method for the identification of aryltetralin lignans is described.