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1.
J Tradit Complement Med ; 13(4): 337-344, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37396151

RESUMEN

Background and aim: Skin is one barrier protecting from environmental risk factors that can make skin cells cancerous through DNA damage and oxidative stress. The nuclear factor erythroid 2-related factor 2 (NRF2) pathway is an anti-stress defense system that can be regulated by DNA methylation and histone modification. Dietary phytochemicals have chemopreventive properties that can inhibit or delay carcinogenesis. The lotus leaf is a traditional medicinal plant containing many polyphenols whose extracts show many biological activities, including antioxidant, anti-obesity, and anti-cancer. This study aim to investigate the effect of lotus leaves on neoplastic transformation in murine skin JB6 P+ cells. Experimental procedure: Lotus leaves were extracted with water (LL-WE) and ethanol (LL-EE), and the LL-WE residues were further extracted with ethanol (LL-WREE). JB6 P+ cells were treated with different extracts. The chemoprotective effect would be evaluated by heme oxygenase 1 (HO-1), NAD(P)H quinone oxidoreductase (NQO1), and UDP glucuronosyltransferase family 1 member A1 (UGT1A1) expression. Results and conclusion: LL-EE contained higher total phenolics and quercetin among extracts. In mouse skin JB6 P+ cells with 12-O-tetradecanoylphorbol-13-acetate treatment, LL-EE showed the greatest potential to suppress skin carcinogenesis. LL-EE activated the NRF2 pathway by upregulating antioxidant and detoxification enzymes upregulates antioxidant and detoxification enzymes, including HO-1, NQO1, and UGT1A1, and downregulates DNA methylation, which might be caused by lower DNA methyltransferase and histone deacetylase levels. Therefore, our results show that LL-EE reduces the neoplastic transformation of skin JB6 P+ cells, potentially by activating the NRF2 pathway and regulating epigenetic DNA methylation and histone acetylation.

2.
Antonie Van Leeuwenhoek ; 114(7): 1079-1089, 2021 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-33895906

RESUMEN

Six aerobic Gram-negative bacteria were isolated from seawater in Guangdong Province, P.R. China. Cells were observed to be Gram-negative, aerobic, non-motile and non-spore forming. Growth of the designated type strain 19X3-30T occurred at a temperature range of 14-37 °C (optimum, 28 °C), a pH range of 6.0-8.0 (optimum, pH 7) and up to 7.5% NaCl (optimum, 1.5%; w/v), and was enhanced by CO2 and L-cysteine supplementation. The major polar lipids identified in strain 19X3-30T were diphosphatidylglycerol, phosphatidylethanolamine and phosphatidylglycerol. The principal cellular fatty acids profile showed the presence of anteiso-C15:0, anteiso-C17:0 and C18:0 (> 8% of total fatty acids), and the respiratory quinone was ubiquinone 8 (UQ-8). According to the analysis of 16S rRNA gene sequences, these strains represented a novel species within the family Fastidiosibacteraceae, sharing maximum similarities with Cysteiniphilum litorale DSM 101832T (96.6%) and Cysteiniphilum halobium DSM 103992T (95.3%). Phylogenetic dendrograms based on 16S rRNA gene and protein marker genes from the genomic sequences both indicated that the strains formed a monophyletic lineage closely linked to the genus Cysteiniphilum, which was also supported by the UPGMA dendrogram based on the MALDI-TOF MS profile. The genomic DNA G + C contents of six strains ranged from 38.0% to 38.1%. Based on different taxonomic genomic metrics, phylogeny and phenotypic features, we propose that the strains warrant the assignment to a novel species, for which the name Cysteiniphilum marinum sp. nov. is proposed. The type strain is 19X3-30T (= KCTC 82154T = CGMCC 1.18585T).


Asunto(s)
Fosfolípidos , Agua de Mar , Técnicas de Tipificación Bacteriana , Composición de Base , ADN Bacteriano/genética , Ácidos Grasos , Gammaproteobacteria , Filogenia , ARN Ribosómico 16S/genética , Análisis de Secuencia de ADN
3.
Zhongguo Zhen Jiu ; 40(5): 493-7, 2020 May 12.
Artículo en Chino | MEDLINE | ID: mdl-32394656

RESUMEN

OBJECTIVE: To verify the clinical effect of acupoint embedding therapy on post-stroke constipation. METHODS: The multi-central randomized controlled trial was adopted. 210 patients of post-stroke constipation were divided into an acupoint embedding group (105 cases, 4 cases dropped off) and a sham-embedding group (105 cases, 6 cases dropped off). In the acupoint embedding group, the acupoint embedding therapy was used at Tianshu (ST 25), Daheng (SP 15), Xiawan (CV 10), Zhongwan (CV 12), Qihai (CV 6), Guanyuan (CV 4) and Daju (ST 27). In the sham-embedding group, the sham-embedding therapy was given, in which, the acupoint selection, needle devices and manipulation were the same as the acupoint embedding group. But, no absorbable surgical suture was used in the needle tube. The treatment was given once every two weeks and 4 treatments were required in either group. It was to compare the weekly average complete spontaneous bowel movements (CSBMs) during treatment (from the 3rd to the 8th week) between the two groups, the weekly average spontaneous bowel movements (SBMs), Bristol stool form score (BSFS), the score of the patient assessment of constipation quality of life questionnaire (PAC-QOL) and the score of defecation difficulty before and after treatment. RESULTS: The percentage of the cases with weekly average CSBMs ≥ 3 times in the patients of the acupoint embedding group was higher markedly than the sham-embedding group [91.1% (92/101) vs 43.4% (43/99), P<0.01]. Compared with the values before treatment, the weekly average SBMs and BSFS scores after treatment were all increased obviously in the two groups (P<0.01), and PAC-QOL score and the score of defecation difficulty were reduced remarkably (P<0.01). After treatment, the increase range of SBMs and BSFS scores, as well as the decrease range of PAC-QOL score and the defecation difficulty score in the acupoint embedding group were all higher than the sham-embedding group respectively (P<0.05). CONCLUSION: The acupoint embedding therapy remarkably increases the spontaneous bowel movements, improves in feces form and defecation difficulty and strengthens the quality of life in the patients of post-stroke constipation.


Asunto(s)
Terapia por Acupuntura , Estreñimiento/terapia , Accidente Cerebrovascular/complicaciones , Puntos de Acupuntura , Estreñimiento/etiología , Humanos , Calidad de Vida , Resultado del Tratamiento
4.
Artículo en Chino | WPRIM | ID: wpr-826706

RESUMEN

OBJECTIVE@#To verify the clinical effect of acupoint embedding therapy on post-stroke constipation.@*METHODS@#The multi-central randomized controlled trial was adopted. 210 patients of post-stroke constipation were divided into an acupoint embedding group (105 cases, 4 cases dropped off) and a sham-embedding group (105 cases, 6 cases dropped off). In the acupoint embedding group, the acupoint embedding therapy was used at Tianshu (ST 25), Daheng (SP 15), Xiawan (CV 10), Zhongwan (CV 12), Qihai (CV 6), Guanyuan (CV 4) and Daju (ST 27). In the sham-embedding group, the sham-embedding therapy was given, in which, the acupoint selection, needle devices and manipulation were the same as the acupoint embedding group. But, no absorbable surgical suture was used in the needle tube. The treatment was given once every two weeks and 4 treatments were required in either group. It was to compare the weekly average complete spontaneous bowel movements (CSBMs) during treatment (from the 3rd to the 8th week) between the two groups, the weekly average spontaneous bowel movements (SBMs), Bristol stool form score (BSFS), the score of the patient assessment of constipation quality of life questionnaire (PAC-QOL) and the score of defecation difficulty before and after treatment.@*RESULTS@#The percentage of the cases with weekly average CSBMs ≥ 3 times in the patients of the acupoint embedding group was higher markedly than the sham-embedding group [91.1% (92/101) vs 43.4% (43/99), <0.01]. Compared with the values before treatment, the weekly average SBMs and BSFS scores after treatment were all increased obviously in the two groups (<0.01), and PAC-QOL score and the score of defecation difficulty were reduced remarkably (<0.01). After treatment, the increase range of SBMs and BSFS scores, as well as the decrease range of PAC-QOL score and the defecation difficulty score in the acupoint embedding group were all higher than the sham-embedding group respectively (<0.05).@*CONCLUSION@#The acupoint embedding therapy remarkably increases the spontaneous bowel movements, improves in feces form and defecation difficulty and strengthens the quality of life in the patients of post-stroke constipation.


Asunto(s)
Humanos , Puntos de Acupuntura , Terapia por Acupuntura , Estreñimiento , Terapéutica , Calidad de Vida , Accidente Cerebrovascular , Resultado del Tratamiento
5.
Sci Rep ; 6: 34387, 2016 10 03.
Artículo en Inglés | MEDLINE | ID: mdl-27694956

RESUMEN

The extraordinary hypolipidemic effects of polyphenolic compounds from tea have been confirmed in our previous study. To gain compounds with more potent activities, using the conformations of the most active compound revealed by molecular docking, a 3D-QSAR pancreatic lipase inhibitor model with good predictive ability was established and validated by CoMFA and CoMISA methods. With good statistical significance in CoMFA (r2cv = 0.622, r2 = 0.956, F = 261.463, SEE = 0.096) and CoMISA (r2cv = 0.631, r2 = 0.932, F = 75.408, SEE = 0.212) model, we summarized the structure-activity relationship between polyphenolic compounds and pancreatic lipase inhibitory activities and find the bulky substituents in R2, R4 and R5, hydrophilic substituents in R1 and electron withdrawing groups in R2 are the key factors to enhance the lipase inhibitory activities. Under the guidance of the 3D-QSAR results, (2R,3R,2'R,3'R)-desgalloyloolongtheanin-3,3'-O-digallate (DOTD), a potent lipase inhibitor with an IC50 of 0.08 µg/ml, was obtained from EGCG oxidative polymerization catalyzed by crude polyphenol oxidase. Furthermore, DOTD was found to inhibit lipid absorption in olive oil-loaded rats, which was related with inhibiting the activities of lipase in the intestinal mucosa and contents.


Asunto(s)
Inhibidores Enzimáticos/química , Lipasa/antagonistas & inhibidores , Simulación del Acoplamiento Molecular , Páncreas/enzimología , Polifenoles/química , Té/química , Animales , Inhibidores Enzimáticos/farmacología , Lipasa/química , Lipasa/metabolismo , Masculino , Polifenoles/farmacología , Ratas , Ratas Sprague-Dawley
6.
Chin J Integr Med ; 22(11): 840-845, 2016 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-27783320

RESUMEN

OBJECTIVE: To ascertain anti-fatigue constituents and mechanisms of Herpetospermum caudigerum. METHODS: The 80% ethanol extracts of Herpetospermum caudigerum were partitioned with chloroform, ethyl acetate and n-butanol, respectively. Male Kunming mice were divided into 13 groups with 16 mice in each group: a control group fed with water, 9 groups treated with 3 fractions of Herpetospermum caudigerum (chloroform fraction, ethyl acetate fraction and n-butanol fraction) at dose of 80, 160 and 320 mg/kg for the low-dose group, medium-dose group and high-dose group, 3 herpetrione (HPE) treated groups fed with HPE at dose of 15, 30, and 60 mg/kg for the low-dose group, medium-dose group and high-dose group. All animals were treated once per day for 30 days. Anti-fatigue activity was assessed through the forced swimming test and serum biochemical parameters including blood lactic acid (BLA), blood urea nitrogen (BUN), malondialdehyde (MDA), hepatic glycogen (HG), lactic dehydrogenase (LDH), superoxide dismutase (SOD) and glutathione peroxidase (GPx) determined following the recommended procedures provided by the commercial kits. RESULTS: Compared with the control group, the lignans extract (ethyl acetate fraction) of Herpetospermum caudigerum and HPE could signifificantly prolonged the exhaustive swimming time (P<0.05 or P<0.01), and also increased the HG levels (P<0.05 or P<0.01) and the activities of antioxidant enzymes (SOD, GPx and LDH, P<0.05 or P<0.01); BLA and MDA levels were decreased considerably in lignans extract and HPE treated groups (P<0.05 or P<0.01). HPE also could significantly decrease the BUN contents compared with the control group (P<0.05). The chloroform and n-butanol fraction showed no effect on swimming time and biochemical parameters. CONCLUSIONS: The lignans extract had antifatigue activities and HPE may be partly responsible for the anti-fatigue effects of Herpetospermum caudigerum. The possible mechanisms of anti-fatigue activity were related to the decrease of BUN and BLA, the increase of the HG storage and protecting corpuscular membrane by preventing lipid oxidation via modifying several enzyme activities.


Asunto(s)
Cucurbitaceae/química , Fatiga/tratamiento farmacológico , Lignanos/uso terapéutico , Extractos Vegetales/uso terapéutico , Animales , Peso Corporal/efectos de los fármacos , Fatiga/sangre , Glucógeno/metabolismo , Lignanos/farmacología , Hígado/efectos de los fármacos , Hígado/metabolismo , Masculino , Ratones , Extractos Vegetales/farmacología , Natación , Factores de Tiempo
7.
J Agric Food Chem ; 64(14): 2893-900, 2016 Apr 13.
Artículo en Inglés | MEDLINE | ID: mdl-26998619

RESUMEN

Cajaninstilbene acid (CSA) is one of the active components isolated from pigeon pea leaves. In this study, anti-inflammatory effects of CSA and its synthesized derivatives were fully valued with regard to their activities on the production of nitric oxide (NO) and pro-inflammatory cytokines tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) in vitro cell model, as well as their impacts on the migration of neutrophils and macrophages in fluorescent protein labeled zebrafish larvae model by live image analysis. Furthermore, the anti-inflammatory mechanism of this type of compounds was clarified by western-blot and reverse transcription-polymerase chain reaction (RT-PCR). The results showed that CSA, as well as its synthesized derivatives 5c, 5e and 5h, exhibited strong inhibition activity on the release of NO and inflammatory factor TNF-α and IL-6 in lipopolysaccharides (LPS)-stimulated murine macrophages. CSA and 5c greatly inhibited the migration of neutrophils and macrophages in injury zebrafish larvae. CSA and 5c treatment greatly inhibited the phosphorylation of proteins involved in nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) pathways. Moreover, we found that peroxisome proliferator-activated receptor gamma (PPARγ) inhibitor GW9662 could reverse partly the roles of CSA and 5c, and CSA and 5c treatment greatly resist the decrease of PPARγ mRNA and protein induced by LPS stimulation. Our results identified the promising anti-inflammatory effects of CSA and its derivatives, which may serve as valuable anti-inflammatory lead compound. Additionally, the mechanism studies demonstrated that the anti-inflammatory activity of CSA and its derivative is associated with the inhibition of NF-κB and MAPK pathways, relying partly on resisting the LPS-induced decrease of PPARγ through improving its expression.


Asunto(s)
Antiinflamatorios/química , Antiinflamatorios/farmacocinética , Cajanus/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Salicilatos/química , Salicilatos/farmacología , Estilbenos/química , Estilbenos/farmacología , Animales , Interleucina-6/genética , Interleucina-6/inmunología , Macrófagos/efectos de los fármacos , Macrófagos/inmunología , Ratones , Proteínas Quinasas Activadas por Mitógenos/genética , Proteínas Quinasas Activadas por Mitógenos/inmunología , Estructura Molecular , Factor de Necrosis Tumoral alfa/genética , Factor de Necrosis Tumoral alfa/inmunología , Pez Cebra
8.
Drug Deliv ; 23(2): 610-8, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-24963753

RESUMEN

OBJECTIVE: The purpose of this study was to formulate stable Ganoderma lucidum (GLT) nanogels suitable for topical delivery with a view to improve the therapeutic effect for frostbite. METHODS: GLT nanosuspensions were formulated using the high-pressure homogenization technique and then suitably gelled for characterized. In order to confirm the advantages of GLT nanogel for dermal application, skin permeation studies in vitro and pharmacodynamic evaluation in vivo were studied and compared with GLT-carbopol gel. RESULTS: The particle size analysis and SEM studies revealed that GLT nanosuspensions were still stably kept their particle size after suitably gelled by carbopol preparation. The drug content, pH, and spreadability of the GLT nanogel was found to be 99.23 ± 1.8%, 6.07 ± 0.1, and 26.42 (g·cm)/s, which were within acceptable limits. In vitro permeation studies through rat skin indicated that the amount of GLT permeated through skin of GLT nanogel after 24 h was higher than GLT-carbopol gel, and GLT nanogel increased the accumulative amount of GLT in epidermis five times than GLT-carbopol gel. No oedema and erythema were observed after administration of GLT nanogel on the rabbits' skin. Pharmacodynamic study showed that GLT nanogel was more effective than GLT-carbopol gel in treatment of frostbite. CONCLUSION: The GLT nanogel possess superior therapeutic effect for frostbite compared with the GLT-carbopol gel, which indicates that nanogels are eligible for the use as a suitable nanomedicine for dermal delivery of poorly soluble drugs such as GLT.


Asunto(s)
Congelación de Extremidades/tratamiento farmacológico , Nanopartículas , Reishi/química , Piel/efectos de los fármacos , Triterpenos/administración & dosificación , Resinas Acrílicas/química , Administración Cutánea , Animales , Modelos Animales de Enfermedad , Composición de Medicamentos , Estabilidad de Medicamentos , Excipientes/química , Congelación de Extremidades/patología , Geles , Concentración de Iones de Hidrógeno , Masculino , Microscopía Electrónica de Rastreo , Nanotecnología , Tamaño de la Partícula , Permeabilidad , Fitoterapia , Plantas Medicinales , Presión , Conejos , Ratas Sprague-Dawley , Piel/metabolismo , Piel/patología , Absorción Cutánea , Propiedades de Superficie , Tecnología Farmacéutica/métodos , Triterpenos/química , Triterpenos/aislamiento & purificación , Triterpenos/farmacocinética , Viscosidad
9.
Zhongguo Zhong Yao Za Zhi ; 41(17): 3232-3238, 2016 Sep.
Artículo en Chino | MEDLINE | ID: mdl-28920375

RESUMEN

To prepare tanshinone ⅡA loaded nanostructured lipid carrier (Tan ⅡA-NLC), and study its in vitro transdermal permeation characteristics. The Tan ⅡA-NLC was prepared by high pressure homogenization technology and optimized by Box-Behnken design-response surface method, and it was characterized in terms of morphology, particle size, zeta potention, et al. The transdermal permeation of Tan ⅡA-NLC was evaluated by using Franz diffusion cells. The results showed that, the optimal formulation was as follows: drug/lipid materials ratio 88, GMS/MCT ratio 2, emulsifier concentration 1%, average particle size (182±14) nm, polydispersity index PDI (0.190 6±0.024 5), zeta potential (-27.8± 5.4) mV, encapsulation efficiency EE (86.44%±9.26%) and drug loading DL (0.98%±0.18%), respectively. The in vitro transdermal permeation results showed that as compared with Tan ⅡA solution, Tan ⅡA-NLC had lower transdermal permeation amount after applying drug for 24 h, but its retention in the epidermis was 3.18 times that of solution. These results indicated that the prepared Tan ⅡA-NLC could effectively increase the regention of Tan ⅡA in the epidermis, and had a broad application prospect.


Asunto(s)
Abietanos/administración & dosificación , Portadores de Fármacos , Lípidos , Nanopartículas , Absorción Cutánea , Administración Cutánea , Técnicas In Vitro , Tamaño de la Partícula
10.
Zhongguo Zhong Yao Za Zhi ; 41(19): 3674-3678, 2016 Oct.
Artículo en Chino | MEDLINE | ID: mdl-28925167

RESUMEN

To study the absorption kinetics of paeoniflorin lipid liquid crystalline nanoparticles (Pae-LLCN) in different intestinal segments of rats and compare them with paeoniflorin(Pae) solution. Rat everted gut sac models were adopted for intestinal absorption test, and Pae content was determined by HPLC method to study the absorption characteristics of Pae-LLCN in rat duodenum, jejunum, ileum and colon, and investigate the effects of different drug concentrations on intestinal absorption. Results showed that Pae-LLCN and Pae were well absorbed at different intestine segments and different concentrations. The absorption constant Ka was increased with the increasing of the drug concentration, indicating possible passive absorption. The accumulative absorption volume Q and absorption constant Ka of Pae-LLCN were higher than those of Pae at each intestinal segment(P<0.05). The results revealed that Pae-LLCN and Pae could be well absorbed in whole intestinal segments and its mechanism may be passive absorption. LLCN can effectively improve the intestinal absorption of Pae.


Asunto(s)
Portadores de Fármacos , Glucósidos/farmacocinética , Absorción Intestinal , Monoterpenos/farmacocinética , Nanopartículas , Animales , Medicamentos Herbarios Chinos , Lípidos , Ratas , Ratas Sprague-Dawley
11.
Artículo en Inglés | WPRIM | ID: wpr-301017

RESUMEN

<p><b>OBJECTIVE</b>To ascertain anti-fatigue constituents and mechanisms of Herpetospermum caudigerum.</p><p><b>METHODS</b>The 80% ethanol extracts of Herpetospermum caudigerum were partitioned with chloroform, ethyl acetate and n-butanol, respectively. Male Kunming mice were divided into 13 groups with 16 mice in each group: a control group fed with water, 9 groups treated with 3 fractions of Herpetospermum caudigerum (chloroform fraction, ethyl acetate fraction and n-butanol fraction) at dose of 80, 160 and 320 mg/kg for the low-dose group, medium-dose group and high-dose group, 3 herpetrione (HPE) treated groups fed with HPE at dose of 15, 30, and 60 mg/kg for the low-dose group, medium-dose group and high-dose group. All animals were treated once per day for 30 days. Anti-fatigue activity was assessed through the forced swimming test and serum biochemical parameters including blood lactic acid (BLA), blood urea nitrogen (BUN), malondialdehyde (MDA), hepatic glycogen (HG), lactic dehydrogenase (LDH), superoxide dismutase (SOD) and glutathione peroxidase (GPx) determined following the recommended procedures provided by the commercial kits.</p><p><b>RESULTS</b>Compared with the control group, the lignans extract (ethyl acetate fraction) of Herpetospermum caudigerum and HPE could signifificantly prolonged the exhaustive swimming time (P<0.05 or P<0.01), and also increased the HG levels (P<0.05 or P<0.01) and the activities of antioxidant enzymes (SOD, GPx and LDH, P<0.05 or P<0.01); BLA and MDA levels were decreased considerably in lignans extract and HPE treated groups (P<0.05 or P<0.01). HPE also could significantly decrease the BUN contents compared with the control group (P<0.05). The chloroform and n-butanol fraction showed no effect on swimming time and biochemical parameters.</p><p><b>CONCLUSIONS</b>The lignans extract had antifatigue activities and HPE may be partly responsible for the anti-fatigue effects of Herpetospermum caudigerum. The possible mechanisms of anti-fatigue activity were related to the decrease of BUN and BLA, the increase of the HG storage and protecting corpuscular membrane by preventing lipid oxidation via modifying several enzyme activities.</p>


Asunto(s)
Animales , Masculino , Ratones , Peso Corporal , Cucurbitaceae , Química , Fatiga , Sangre , Quimioterapia , Glucógeno , Metabolismo , Lignanos , Farmacología , Usos Terapéuticos , Hígado , Metabolismo , Extractos Vegetales , Farmacología , Usos Terapéuticos , Natación , Factores de Tiempo
12.
Zhong Yao Cai ; 38(2): 323-6, 2015 Feb.
Artículo en Chino | MEDLINE | ID: mdl-26415410

RESUMEN

OBJECTIVE: To analyze the volatile oil in Piper hongkongense from five different habitats. METHODS: The volatile oil was analyzed by GC-MS. RESULT: The volatile components oil of each sample varied significantly. Caryophyllene, α-caryophyllene and nerolidol 2 were common constituents of five samples. The volatile oil and chemical constituent contents of fresh sample were higher than that of the old sample. CONCLUSION: The volatile oil and chemical constituent contents of Piper hongkongense from different habitats have sig- nificant differences, which are affected by habitats, harvest season, storage time and so on.


Asunto(s)
Ecosistema , Aceites Volátiles/química , Piper/química , Aceites de Plantas/química , Cromatografía de Gases y Espectrometría de Masas , Sesquiterpenos Monocíclicos , Sesquiterpenos Policíclicos , Sesquiterpenos
13.
Int J Pharm ; 489(1-2): 148-57, 2015 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-25882012

RESUMEN

In present study, a novel phospholipid complex loaded cucurbitacin B modified with berberine hydrochloride (CUB-PLC-BER) was prepared by a simple solvent evaporation method with the aim of improving bile duct-targeted drug delivery and therapeutic efficacy for cholangiocarcinoma (CC). The complex's physicochemical properties were systemically investigated in terms of scanning electron microscopy (SEM), x-ray diffraction (XRD) and infrared absorption spectroscopy (IR). In vivo and in vitro antitumor studies, CUB-PLC-BER and the unmodified cucurbitacin B-phospholipid complex (CUB-PLC) presented stronger antitumor efficacy against human cholangiocarcinoma cells (QBC939 cells) than free cucurbitacin B (CUB), while phospholipids (PL) itself had no significant toxicity. Besides that, CUB-PLC showed the advantage over the free CUB and CUB-PLC-BER with regard to the inhibition of tumor growth in vivo antitumor study. Failure to establish the orthotopic CC model, the study attempted to measure the level of CUB in plasma and in bile to explore bile duct-targeted effect indirectly. In the pharmacokinetics study in rats, the average values of Cmax and AUC0-8h of CUB-PLC-BER group in rat bile were higher than those of CUB-PLC, while an opposite result was found in plasma. Meanwhile, the Cmax, AUC0-8h and AUC0-24h of CUB were the least both in plasma and in bile. The results indicated that the CUB-PLC-BER tended to provide a high and prolonged drug concentration to bile duct, and PL played a central role in internalizing CUB into cells to improve the water insoluble drug's permeability, which was of great benefit to enhance the bioavailability of CUB and improve therapeutic efficacy of CC. These results elucidated the potential of CUB-PLC-BER as drug delivery system for improving bile duct-targeted and therapeutic efficacy for CC.


Asunto(s)
Antineoplásicos , Berberina , Neoplasias de los Conductos Biliares/tratamiento farmacológico , Colangiocarcinoma/tratamiento farmacológico , Fosfolípidos , Triterpenos , Animales , Antineoplásicos/administración & dosificación , Antineoplásicos/química , Antineoplásicos/farmacocinética , Antineoplásicos/uso terapéutico , Berberina/administración & dosificación , Berberina/química , Berberina/farmacocinética , Berberina/uso terapéutico , Bilis/química , Conductos Biliares/metabolismo , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Sistemas de Liberación de Medicamentos , Humanos , Masculino , Ratones Desnudos , Fosfolípidos/administración & dosificación , Fosfolípidos/química , Fosfolípidos/farmacocinética , Fosfolípidos/uso terapéutico , Ratas Sprague-Dawley , Resultado del Tratamiento , Triterpenos/administración & dosificación , Triterpenos/química , Triterpenos/farmacocinética , Triterpenos/uso terapéutico
14.
Chem Biol Drug Des ; 86(4): 682-90, 2015 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-25677093

RESUMEN

A series of novel oxazolidinone compounds with a substituted ligustrazine C-ring unit and different substituted groups at the C-5 side chain were designed and synthesized using linezolid as a lead and based on a scaffold hopping strategy. Their antibacterial and anti-inflammatory activities were evaluated. The results of in vitro antibacterial assays showed that all fourteen target compounds displayed potent activity against Gram-positive pathogens, particularly 8b, 13b, 14a, 14b, 15a, and 15b. Moreover, 14a and 14b exhibited significant inhibitory activities on the production of inflammatory mediators, including nitric oxide, interleukin-6, and tumor necrosis factor-alpha. Thus, these derivatives could serve as valuable candidates to develop anti-infective agents for the treatment of chronic wounds.


Asunto(s)
Antibacterianos/química , Antibacterianos/farmacología , Oxazolidinonas/química , Animales , Antibacterianos/síntesis química , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacología , Línea Celular/efectos de los fármacos , Línea Celular/metabolismo , Técnicas de Química Sintética , Evaluación Preclínica de Medicamentos/métodos , Bacterias Grampositivas/efectos de los fármacos , Interleucina-6/antagonistas & inhibidores , Interleucina-6/metabolismo , Lipopolisacáridos/farmacología , Macrófagos/efectos de los fármacos , Ratones , Pruebas de Sensibilidad Microbiana , Óxido Nítrico/metabolismo , Pirazinas/química , Relación Estructura-Actividad , Factor de Necrosis Tumoral alfa/antagonistas & inhibidores , Factor de Necrosis Tumoral alfa/metabolismo
15.
Artículo en Chino | WPRIM | ID: wpr-462556

RESUMEN

Objective To know the understanding of acupuncture and moxibustion and learning interest of students in western medical colleges and universities;To analyze the feasibility and possibility of establishing acupuncture and moxibustion course in western medical colleges and universities. Methods A survey was made among 535 medical students in five majors from grade one to grade three in Medical School in Nanchang University:clinical specialty, anesthesiology, medical imaging, prophylactic medicine and nursing. Data were statistically analyzed by analysis of variance and Kruskal-Wallis test. Results Among all the students, 46.2%of them did not know anything about acupuncture and moxibustion, but 97% of them were interested in learning it. 76.8% students wished to learn the acupuncture theories based on modern science and clinical research. In addition, 79.3%students chose elective course as teaching form. Compared with the freshmen and junior students, sophomores were more interested in accepting acupuncture and moxibution course, with statistical significance (P0.05). Conclusion Students of western medical colleges and universities are interested in learning acupuncture and moxibustion. The feasibility and possibility of establishing acupuncture and moxibustion course in western medical colleges and universities are affirmed.

16.
Zhongguo Zhong Yao Za Zhi ; 39(10): 1799-804, 2014 May.
Artículo en Chino | MEDLINE | ID: mdl-25282885

RESUMEN

A novel drug delivery system combining oral fast dissolving film with sodium deoxycholate/phospholipid mixed micelles was prepared to increase the absorption of cucurbitacin B that is a poor aqueous solubility substance. Encapsulation efficiency, particle size, zeta potential, polydispersity coefficient, investigated the morphology, disintegration time of oral fast dissolving film and the pharmacodynamic properties of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles before and after solidified in mice were evaluated and compared. The oral fast dissolving film prepared in this study showed a homogeneous pale yellow and could completely disintegrated in the 30 s. It could meet the requirements of rapidly disintegrating fully. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles loaded in oral fast dissolving film were (43.36 +/- 2.12)%, (108.82 +/- 5.2) nm, (-34.18 +/- 1.07) mV, 0.088 +/- 0.012, respectively. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles in solution were (41.26 +/- 2.22)%, (181.82 +/- 4.48) nm, (-30.67 +/- 0.81) mV, 0.092 +/- 0.012, respectively. The difference of pharmacodynamics among film of cucurbitacin B-loaded micelles, cucurbitacin B-loaded micelles and free cucurbitacin B in vivo was compared. Solubility of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles has also been greatly improved. The tumor inhibition rate of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles was significantly improved and did not change significantly before and after solidified. These showed that the sodium deoxycholate/phospholipid-mixed micelles could enhance the antitumor activities of cucurbitacin B and the stability of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles was improved significantly after solidified by oral fast dissolving film technology without pharmacodynamic properties changed significantly.


Asunto(s)
Antineoplásicos/administración & dosificación , Ácido Desoxicólico/química , Portadores de Fármacos/química , Neoplasias/tratamiento farmacológico , Fosfolípidos/química , Triterpenos/administración & dosificación , Animales , Antineoplásicos/química , Línea Celular Tumoral , Humanos , Masculino , Ratones , Solubilidad , Triterpenos/química
17.
Food Chem Toxicol ; 48(8-9): 2344-9, 2010.
Artículo en Inglés | MEDLINE | ID: mdl-20561948

RESUMEN

The hypoglycemic effect of cinnamon oil (CO) in a type 2 diabetic animal model (KK-A(y) mice) was studied. The main component of CO was cinnamaldehyde, and other nineteen components were also determined. CO was administrated at doses of 25, 50 and 100mg/kg for 35 days. It was found that fasting blood glucose concentration was significantly decreased (P<0.05) with the 100mg/kg group (P<0.01) the most efficient compared with the diabetic control group. In addition, there was significant decrease in plasma C-peptide, serum triglyceride, total cholesterol and blood urea nitrogen levels while serum high density lipoprotein (HDL)-cholesterol levels were significantly increased after 35 days. Meanwhile, glucose tolerance was improved, and the immunoreactive of pancreatic islets beta-cells was promoted. These results suggest that CO had a regulative role in blood glucose level and lipids, and improved the function of pancreatic islets. Cinnamon oil may be useful in the treatment of type 2 diabetes mellitus.


Asunto(s)
Cinnamomum zeylanicum/química , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Hipoglucemiantes , Aceites de Plantas/farmacología , Animales , Análisis Químico de la Sangre , Glucemia/metabolismo , Diabetes Mellitus Tipo 2/genética , Diabetes Mellitus Tipo 2/patología , Cromatografía de Gases y Espectrometría de Masas , Prueba de Tolerancia a la Glucosa , Inmunohistoquímica , Islotes Pancreáticos/patología , Lípidos/sangre , Ratones , Ratones Endogámicos C57BL , Ratones Endogámicos
18.
J Integr Plant Biol ; 50(3): 375-83, 2008 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-18713371

RESUMEN

Single pollen grain polymerase chain reaction (PCR) has succeeded in several species, however only limited numbers of pollen grains were involved due to difficulties in pollen isolation and lysis. This has limited its application in genetic analysis and mapping studies in plants. A high-throughput (HT) procedure for collecting and detecting genetic variation in a large number of individual pollen grains by PCR is reported. The HT procedure involved the collection of individual pollen grains by a pair of special forceps and the lysis of pollen grains in a heated alkali/detergent solution followed by neutralization with a tris-ethylenediamine tetraacetic acid (TE) buffer. These resulting template solutions yielded PCR reactions involving the 5S ribosomal RNA intergenic spacers, randomly amplified polymorphic DNA, and simple sequence repeats markers. Using this procedure, one person with experience could collect and process up to 288 single pollen grain PCR reactions per day. The method worked well on sugarcane, corn, Miscanthus spp., snap bean, sorghum, and tomato. The ability to collect and conduct PCR on individual pollen grains on a large scale offers a new approach to genetic analyses and mapping studies in an easily controllable environment with a considerable cost reduction. The method will also significantly benefit studies in species that are difficult subjects for classical genetic research.


Asunto(s)
Plantas/genética , Polen/citología , Reacción en Cadena de la Polimerasa/métodos , Supervivencia Celular , Etidio , Calor , Células Vegetales , Polen/genética , Técnica del ADN Polimorfo Amplificado Aleatorio , Reproducibilidad de los Resultados , Soluciones , Factores de Tiempo
19.
Artículo en Chino | WPRIM | ID: wpr-303054

RESUMEN

<p><b>OBJECTIVE</b>To summarize 4 schools of thought in studies of meridians.</p><p><b>METHODS</b>Consult literature and review the history of studies of meridians.</p><p><b>RESULTS</b>The studies of meridians in the past dozens years at home and abroad have gradually formed four main theories, namely the nerve-conduction meridian theory of neurophysiology, body fluid circulation meridian theory of the physio-biochemistry, bio-field meridian theory of biophysics, and the connective tissue structure meridian theory of the overall-gap viewpoint, which are summarized and analyzed.</p>


Asunto(s)
Humanos , Puntos de Acupuntura , Calcio , Metabolismo , Células Gigantes , Fisiología , Magnetismo , Meridianos , Conducción Nerviosa , Neurotransmisores , Fisiología
20.
Chinese Journal of Biotechnology ; (12): 630-633, 2002.
Artículo en Chino | WPRIM | ID: wpr-256149

RESUMEN

The effect of antioxidants on the in vitro life span of mouse keratinocytes was investigated in this work. It was found that the life span of the keratinocytes cultured in the medium supplemented with antioxidants was extended significantly. The most beneficial antioxidant used in this work was the mercaptoethanol, followed by the catalase and SOD. However, the growth rates of keratinocytes in vitro under all the experimental conditions still declined with the culture time. It was also found that the antioxidants added in the medium were also helpful to enhance the keratinocyte colony formation. In addition, the aging kinetics of the mouse epidermal keratinocytes in vitro were analyzed, and finally the aging rate constants corresponding to antioxidants used were calculated.


Asunto(s)
Animales , Ratones , Antioxidantes , Farmacología , Catalasa , Farmacología , División Celular , Células Cultivadas , Senescencia Celular , Queratinocitos , Biología Celular , Mercaptoetanol , Farmacología , Superóxido Dismutasa , Farmacología
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