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1.
J Nanobiotechnology ; 22(1): 33, 2024 Jan 18.
Artículo en Inglés | MEDLINE | ID: mdl-38238760

RESUMEN

BACKGROUND: The complex etiology and pathogenesis underlying Chronic Non-Bacterial Prostatitis (CNP), coupled with the existence of a Blood Prostate Barrier (BPB), contribute to a lack of specificity and poor penetration of most drugs. Emodin (EMO), a potential natural compound for CNP treatment, exhibits commendable anti-inflammatory, anti-oxidant, and anti-fibrosis properties but suffers from the same problems as other drugs. METHODS: By exploiting the recognition properties of lactoferrin (LF) receptors that target intestinal epithelial cells (NCM-460) and prostate epithelial cells (RWPE-1), a pathway is established for the transrectal absorption of EMO to effectively reach the prostate. Additionally, hyaluronic acid (HA) is employed, recognizing CD44 receptors which target macrophages within the inflamed prostate. This interaction facilitates the intraprostatic delivery of EMO, leading to its pronounced anti-inflammatory effects. A thermosensitive hydrogel (CS-Gel) prepared from chitosan (CS) and ß-glycerophosphate disodium salt (ß-GP) was used for rectal drug delivery with strong adhesion to achieve effective drug retention and sustained slow release. Thus, we developed a triple-targeted nanoparticle (NPs)/thermosensitive hydrogel (Gel) rectal drug delivery system. In this process, LF, with its positive charge, was utilized to load EMO through dialysis, producing LF@EMO-NPs. Subsequently, HA was employed to encapsulate EMO-loaded LF nanoparticles via electrostatic adsorption, yielding HA/LF@EMO-NPs. Finally, HA/LF@EMO-NPs lyophilized powder was added to CS-Gel (HA/LF@EMO-NPs Gel). RESULTS: Cellular assays indicated that NCM-460 and RWPE-1 cells showed high uptake of both LF@EMO-NPs and HA/LF@EMO-NPs, while Raw 264.7 cells exhibited substantial uptake of HA/LF@EMO-NPs. For LPS-induced Raw 264.7 cells, HA/LF@EMO-NPs can reduce the inflammatory responses by modulating TLR4/NF-κB signaling pathways. Tissue imaging corroborated the capacity of HA/LF-modified formulations to breach the BPB, accumulating within the gland's lumen. Animal experiments showed that rectal administration of HA/LF@EMO-NPs Gel significantly reduced inflammatory cytokine expression, oxidative stress levels and fibrosis in the CNP rats, in addition to exerting anti-inflammatory effects by inhibiting the NF-κB signaling pathway without obvious toxicity. CONCLUSION: This triple-targeted NPs/Gel rectal delivery system with slow-release anti-inflammatory, anti-oxidant, and anti-fibrosis properties shows great potential for the effective treatment of CNP.


Asunto(s)
Quitosano , Emodina , Nanopartículas , Prostatitis , Humanos , Masculino , Ratas , Animales , Hidrogeles , Emodina/farmacología , Emodina/uso terapéutico , Prostatitis/tratamiento farmacológico , Antioxidantes , FN-kappa B , Sistemas de Liberación de Medicamentos/métodos , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Portadores de Fármacos
2.
Phytother Res ; 38(7): 3782-3800, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38839050

RESUMEN

Pediatric intestinal development is immature, vulnerable to external influences and produce a variety of intestinal diseases. At present, breakthroughs have been made in the treatment of pediatric intestinal diseases, but there are still many challenges, such as toxic side effects, drug resistance, and the lack of more effective treatments and specific drugs. In recent years, dietary polyphenols derived from plants have become a research hotspot in the treatment of pediatric intestinal diseases due to their outstanding pharmacological activities such, as anti-inflammatory, antibacterial, antioxidant and regulation of intestinal flora. This article reviewed the mechanism of action and clinical evidence of dietary polyphenols in the treatment of pediatric intestinal diseases, and discussed the influence of physiological characteristics of children on the efficacy of polyphenols, and finally prospected the new dosage forms of polyphenols in pediatrics.


Asunto(s)
Enfermedades Intestinales , Polifenoles , Humanos , Polifenoles/farmacología , Niño , Enfermedades Intestinales/tratamiento farmacológico , Enfermedades Intestinales/dietoterapia , Enfermedades Intestinales/prevención & control , Antioxidantes/farmacología , Microbioma Gastrointestinal/efectos de los fármacos , Antiinflamatorios/farmacología , Dieta
3.
Zhongguo Zhong Yao Za Zhi ; 49(10): 2699-2709, 2024 May.
Artículo en Zh | MEDLINE | ID: mdl-38812170

RESUMEN

A systematic evaluation of the differences in the chemical composition and efficacy of the different forms of Galli Gigerii Endothelium Corneum(GGEC) was conducted based on modern analytical techniques and a functional dyspepsia(FD) rat model, which clarifies the material basis of the digestive efficacy of GGEC. Proteins, enzymes, polysaccharides, amino acids, and flavonoids in GGEC powder and decoction were determined respectively. The total protein of the powder and decoction was 0.06% and 0.65%, respectively, and the pepsin and amylase potency of the powder was 27.03 and 44.05 U·mg~(-1) respectively. The polysaccharide of the decoction was 0.03%, and there was no polysaccharide detected in the powder. The total L-type amino acids in the powder and decoction were 279.81 and 8.27 mg·g~(-1) respectively, and the total flavonoid content was 59.51 µg·g~(-1). Enzymes and flavonoids were not detected in the decoction. The powder significantly reduced nutrient paste viscosity, while the decoction and control group showed no significant reduction in nutrient paste viscosity. FD rat models were prepared by iodoacetamide gavage and irregular diet. The results showed that both powder and decoction significantly increased the gastric emptying effect, small intestinal propulsion rate, digestive enzymes activity, gastrin(GAS), motilin(MTL), ghrelin(GHRL) and reduced vasoactive intestinal peptide(VIP), 3-(2-ammo-nioethyl)-5-hydroxy-1H-indolium maleate(5-HT), and somatostatin(SST) content in rats(P<0.05, P<0.01). Comparison of GGEC decoction and powder administration between groups of the same dosage level showed that gastrointestinal propulsion and serum levels of GAS, GHRL, VIP, and SST in the powder group were significantly superior to those in the decoction and that the gastrointestinal propulsion, as well as serum levels of MTL, GAS, and GHRL were slightly higher than those of the decoction with two times its raw dose, and the serum levels of SST, 5-HT, and VIP in the powder group were slightly lower than those of the decoction with two times its raw dose. In conclusion, both decoction and powder have therapeutic effects on FD, but there is a significant difference between the two effects. Under the same dosage, the digestive efficacy of the powder is significantly better than that of the decoction, and the decoction needs to increase the dosage to compensate for the efficacy. It is hypothesized that the digestive efficacy of the GGEC has a duality, and the digestive active ingredients of the powder may include enzymes and L-type amino acids, while the decoction mainly relies on L-type amino acids to exert its efficacy. This study provides new evidence to investigate the digestive active substances of the GGEC and to improve the effectiveness of the drug in the clinic.


Asunto(s)
Dispepsia , Ratas Sprague-Dawley , Animales , Ratas , Masculino , Dispepsia/tratamiento farmacológico , Dispepsia/fisiopatología , Dispepsia/metabolismo , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/química , Humanos , Flavonoides/química , Flavonoides/farmacología , Motilina , Péptido Intestinal Vasoactivo/metabolismo , Ghrelina , Somatostatina
4.
Zhongguo Zhong Yao Za Zhi ; 48(3): 649-659, 2023 Feb.
Artículo en Zh | MEDLINE | ID: mdl-36872228

RESUMEN

Liquid chromatography-mass spectrometry was employed to analyze the chemical components in Curcuma longa tuberous roots(HSYJ), C. longa tuberous roots processed with vinegar(CHSYJ), and rat serum after the administration. The active components of HSYJ and CHSYJ absorbed in serum were identified based on the secondary spectrum of database and literature. The targets of primary dysmenorrhea was screened out from database. The protein-protein interaction network analysis, gene ontology(GO) functional annotation, and Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway enrichment analysis were performed for the common targets shared by the drug active components in serum and primary dysmenorrhea, and the component-target-pathway network was constructed. AutoDock was used to conduct molecular docking between the core components and targets. A total of 44 chemical components were identified from HSYJ and CHSYJ, including 18 absorbed in serum. On the basis of network pharmacology, we identified 8 core components(including procurcumenol, isobutyl p-hydroxybenzoate, ferulic acid, and zedoarondiol) and 10 core targets \[including interleukin-6(IL-6), estrogen receptor 1(ESR1), and prostaglandin-endoperoxide synthase 2(PTGS2)\]. The core targets were mainly distributed in the heart, liver, uterus, and smooth muscle. The molecular docking results showed that the core components were well bound to the core targets, indicating that HSYJ and CHSYJ may exert therapeutic effect on primary dysmenorrhea via estrogen, ovarian steroidogenesis, tumor necrosis factor(TNF), hypoxia-inducible factor-1(HIF-1), IL-17 and other signaling pathways. This study clarifies the HSYJ and CHSYJ components absorbed in serum, as well as the corresponding mechanism, providing a reference for further elucidating the therapeutic material basis and clinical application of HSYJ and CHSYJ.


Asunto(s)
Ácido Acético , Curcuma , Femenino , Humanos , Animales , Ratas , Dismenorrea , Simulación del Acoplamiento Molecular , Factor de Necrosis Tumoral alfa , Ciclooxigenasa 2
5.
Zhongguo Zhong Yao Za Zhi ; 48(13): 3498-3507, 2023 Jul.
Artículo en Zh | MEDLINE | ID: mdl-37475002

RESUMEN

This study compared the effects of Curcuma longa before and after processing with vinegar on the rat model of dysmenorrhea with the syndrome of liver depression and Qi stagnation to reveal the mechanism of vinegar processing in improving the role of C. longa in soothing liver and relieving pain. The rat model of dysmenorrhea with the syndrome of liver depression and Qi stagnation was established according to the Preparation of the Animal Model of Dysmenorrhea(Draft) and the chronic unpredictable stress me-thod. The changes in the body weight, organ indexes, writhing latency, writhing score, and serum levels of six liver function indicators, sex hormones, pain factors, and blood rheological indicators were measured to evaluate the efficacy of C. longa processed with vinegar or not in treating dysmenorrhea in the rats with syndrome of liver depression and qi stagnation. Compared with the model group, the C. longa group(processed with vinegar or not) showed slow weight loss, increase in writhing latency, and decrease in writhing response(P<0.05). The inhibition rates on writhing in raw C. longa, vinegar-processed C. longa, and positive groups were 33.780%, 64.611%, and 62.466%, respectively. The significantly higher inhibition rate of the vinegar processing group indicated that vinegar-processed C. longa demonstrated more significant therapeutic effect. The vinegar-processed C. longa group showed lower levels of alanine aminotransferase(ALT), alkaline phosphatase(ALP), aspartate aminotransferase(AST), direct bilirubin(DBIL), and total bilirubin(TBIL) and higher level of albumin(ALB)(P<0.05), which indicated that vinegar processing enhanced the therapeutic effect of C. longa on liver injury. The serum levels of estradiol(E_2) and oxytocin(OT) were lower in the vinegar-processed C. longa group(P<0.05), indicating that the vinegar-processed C. longa could regulate the sex hormone levels, reduce the activity of uterine smooth muscle and contraction of uterus, and alleviate the symptoms of dysmenorrhea in rats. Moreover, the vinegar-processed C. longa group showed lower interleukin-6(IL-6) and arginine vasopressin(AVP) levels and higher beta-endorphin(ß-EP) level(P<0.05), which indicated that vinegar-processed C. longa regulated the levels of pain factors to exert the pain-relieving effect. Drug intervention decreased the whole blood viscosity low-cut, medium-cut and high-cut values, plasma viscosity, whole blood reduction viscosity low-cut and high-cut values, erythrocyte cumulative pressure, and equation K value of erythrocyte sedimentation rate(P<0.05), and the vinegar-processed C. longa group outperformed other groups. This result indicated that vinegar processing enhanced the function of C. longa in improving the local blood rheology. C. longa processed with vinegar can enter the liver to relieve the da-mage to the heart, liver, kidney, and uterus, repair the liver function, and recover the sex hormone levels and immune function by regulating the levels of sex hormones and pain factors and improving the blood rheology. It activates the pain-relieving mechanism to relieve the pain, protect the liver, and fight inflammation, which is consistent with the theory that vinegar processing facilitates C. longa entering the liver to sooth liver and relieve pain.


Asunto(s)
Ácido Acético , Dismenorrea , Humanos , Femenino , Ratas , Animales , Dismenorrea/tratamiento farmacológico , Curcuma , Depresión , Qi , Hígado , Hormonas Esteroides Gonadales , Bilirrubina
6.
Zhongguo Zhong Yao Za Zhi ; 47(20): 5434-5442, 2022 Oct.
Artículo en Zh | MEDLINE | ID: mdl-36471957

RESUMEN

Galli Gigerii Endothelium Corneum(GGEC) is commonly used for the clinical treatment of indigestion, vomiting, diarrhea, and infantile malnutrition with accumulation. In recent decades, omnivorous domestic chickens, the original source of GGEC, has been replaced by broilers, which may lead to significant changes in the quality of the yielding GGEC. Through subjective and objective sensory evaluation, biological evaluation, and chemical analysis, this study compared the odor and quality between GGEC derived from domestic chickens and that from broilers. The odor intensity between them was compared by odor profile analysis and it was found that the fishy odor of GGEC derived from domestic chickens was significantly weaker than that of GGEC from broilers. Headspace-solid phase microextraction-gas chromatography-triple quadrupole tandem mass spectrometry(HS-SPME/GC-QQQ-MS/MS) suggested that the overall odor-causing chemicals were consistent with the fishy odor-causing chemicals. According to the odor activity va-lue and the orthogonal partial least squares discriminant analysis(OPLS-DA) result, dimethyl trisulfide, 2-methoxy-3-isobutylpyrazine, and 2-methylisoborneol were responsible for the fishy odor(OAV≥1) and the content of fishy odor-causing chemicals in GGEC derived from broilers was 1.12-2.13 folds that in GGEC from domestic chickens. The average pepsin potency in GGEC derived from broilers was 15.679 U·mg~(-1), and the corresponding figure for the medicinal from domestic chickens was 26.529 U·mg~(-1). The results of pre-column derivatization reverse-phase high-performance liquid chromatography(RP-HPLC) assay showed that the content of total amino acids and digestion-promoting amino acids in domestic chickens-derived GGEC was 1.12 times and 1.15 times that in GGEC from broilers, and the bitter amino acid content was 1.21 times folds that of the latter. In conclusion, GGEC derived from domestic chickens had weaker fishy odor, stronger enzyme activity, higher content of digestion-promoting amino acids, and stronger bitter taste than GGEC from broilers. This study lays a scientific basis for studying the quality variation of GGEC and provides a method for identifying high-quality GGEC. Therefore, it is of great significance for the development and cultivation of GGEC as both food and medicine and breeding of corresponding varieties.


Asunto(s)
Odorantes , Compuestos Orgánicos Volátiles , Animales , Odorantes/análisis , Pollos , Cromatografía de Gases y Espectrometría de Masas/métodos , Espectrometría de Masas en Tándem , Microextracción en Fase Sólida , Aminoácidos , Endotelio/química , Compuestos Orgánicos Volátiles/análisis
7.
Zhongguo Zhong Yao Za Zhi ; 47(20): 5452-5459, 2022 Oct.
Artículo en Zh | MEDLINE | ID: mdl-36471959

RESUMEN

Despite the distinctive characteristics and remarkable efficacy, animal medicine is stenchy, which decreases the comp-liance of patients. At the moment, the research on the method for deodorizing animal medicines lags behind. To be specific, the components related to the odor and the basic properties transformation of the components are unclear and there is a lack of specific deodorizing method. This study aims to clarify the main components related to the stench of animal medicine, such as aldehydes, amines, trimethylamines and sulfur compounds, and their basic properties, and to explore their metabolism and transformation in vivo and in vitro, which is expected to serve as a reference for the research on deodorization of animal medicine and development of new techniques.


Asunto(s)
Aldehídos , Odorantes , Animales
8.
Eur J Nutr ; 60(7): 3525-3542, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-33439332

RESUMEN

Phyllanthus emblica is a fruit widely consumed in subtropical areas, which is rich in polyphenols and other nutrients. There are increasing evidences that as a daily and nutritious fruit, it may have a positive role in controlling diabetic complications. According to the new study, its mechanisms include enhancing the functioning of insulin, reducing insulin resistance, activating the insulin-signaling pathway, protecting ß-cells, scavenging free radicals, alleviating inflammatory reactions, and reducing the accumulation of advanced glycation end products. Owing to its few side effects, and low price, it should be easily accepted by patients and has potential for preventing diabetes. Taken together, Phyllanthus emblica may be an ideal fruit for controlling diabetic complications. This review highlights the latest findings of the role of Phyllanthus emblica in anti-diabetes and its complications, especially clarifies the molecular mechanism of the chemical components related to this effect, and prospects some existing problems and future research directions.


Asunto(s)
Diabetes Mellitus Tipo 2 , Phyllanthus emblica , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Frutas , Humanos , Extractos Vegetales/uso terapéutico , Polifenoles
9.
Zhongguo Zhong Yao Za Zhi ; 46(13): 3171-3179, 2021 Jul.
Artículo en Zh | MEDLINE | ID: mdl-34396734

RESUMEN

Traditional Chinese medicine( TCM) processing is a traditional pharmaceutical technology unique to China,which is an important means to ensure the safety and effectiveness of clinical medication. As China' s intangible cultural heritage,it contains a wealth of wisdom. With the evolution and optimization of processing methods,Indigo Naturalis,an ancient dye,has gradually become an effective medicine for the treatment of high fever in children,colitis,psoriasis,and leukemia. However,the quality of Indigo Naturalis pieces is difficult to be fundamentally improved due to the unique traditional processing method,complex technology,unclear principle,and outdated equipment. After spending 20 years in exploring the inheritance,innovation,and transformation of ancient lawtheory-principle-technology-equipment-quality control in Indigo Naturalis processing,our research group has basically expounded the processing principle and realized the modern expression and industrial transformation of traditional technology. As China enters a new era,the TCM industry has begun to undergo the high-quality transformation. It is urgent to carry out new excavations and improve the processing,quality,and clinical application of Indigo Naturalis pieces,to better inherit and innovate traditional processing technologies and meet people's demand for high-quality TCM health services.


Asunto(s)
Medicamentos Herbarios Chinos , Indigofera , Psoriasis , Niño , Humanos , Carmin de Índigo , Medicina Tradicional China
10.
Zhongguo Zhong Yao Za Zhi ; 46(24): 6377-6386, 2021 Dec.
Artículo en Zh | MEDLINE | ID: mdl-34994129

RESUMEN

Breast cancer is a major chronic disease threatening women's health. It has topped the global cancers as the diagnosed cases outnumbered lung cancer patients in 2020. Internal damage due to the seven emotions is an important cause of breast cancer and the disorders of hypothalamic-pituitary-adrenal(HPA) axis and endocrine system and the abnormal immune defense mechanism in response to psychological stress all affect the occurrence and development of breast cancer. It is noteworthy that the theory of seven emotions in traditional Chinese medicine and the psychological stress theory of modern medicine have something in common in some aspects. Therefore, this study explored the correlation between internal damage due to the seven emotions and psychological stress and analyzed the molecular biological mechanisms of psychological stress influencing breast cancer from the perspective of modern medicine, which is helpful to reasonably prevent breast cancer and other related tumors and improve the prognosis of breast cancer patients through emotion regulation.


Asunto(s)
Neoplasias de la Mama , Neoplasias de la Mama/genética , Emociones , Femenino , Humanos , Sistema Hipotálamo-Hipofisario , Medicina Tradicional China , Sistema Hipófiso-Suprarrenal , Estrés Psicológico
11.
Zhongguo Zhong Yao Za Zhi ; 46(13): 3180-3187, 2021 Jul.
Artículo en Zh | MEDLINE | ID: mdl-34396735

RESUMEN

The soaking and fermentation of Baphicacanthus cusia( Nees),the important intermediate link of Indigo Naturalis processing,facilitates the synthesis of indigo and indirubin precursors and the dissolution of endogenous enzymes and other effective components,while the role of microorganisms in the fermentation is ignored. The present study investigated the changes of microbial community structure in Indigo Naturalis processing based on 16 S amplicon sequencing and bioinformatics. Meanwhile,the contents of indigo,indirubin,isatin,tryptanthrin,indole glycoside,etc. were determined to explore the correlation between the microorganisms and the alterations of the main components. As demonstrated by the results,the microbial diversity decreased gradually with the fermentation,which bottomed out after the addition of lime. Proteobacteria,Bacteroidetes,and Firmicutes were the main dominant communities in the fermentation. The relative abundance of Proteobacteria declined gradually with the prolongation of fermentation time,and to the lowest level after the addition of lime. The relative abundance of Firmicutes increased,and that of Bacteroidetes decreased first and then increased. The contents of effective substances in Indigo Naturalis also showed different variation tendencies. As fermentation went on,indole glycoside decreased gradually; indigo first increased and then decreased; indirubin and isatin first decreased and then increased; tryptanthrin gradually increased. Those changes were presumedly related to the roles of microorganisms in the synthesis of different components. This study preliminarily clarified the important role of microorganisms in the soaking and fermentation and provided a scientific basis for the control of Indigo Naturalis processing and the preparation of high-quality Indigo Naturalis.


Asunto(s)
Indigofera , Microbiota , Fermentación , Carmin de Índigo , Indoles
12.
Zhongguo Zhong Yao Za Zhi ; 46(13): 3188-3197, 2021 Jul.
Artículo en Zh | MEDLINE | ID: mdl-34396736

RESUMEN

Indigo Naturalis has a long history of medicinal use with particularity and complexity in its processing. Before the Ming dynasty,Indigo Naturalis was extracted from the top layer of zymotic fluid,called " purified Indigo Naturalis". In modern processing,the precipitate " crude Indigo Naturalis" is dried to produce Indigo Naturalis after impurity removal. The form of Indigo Naturalis slices has undergone significant changes in ancient and modern times. In view of this,the quality comparison between crude Indigo Naturalis and purified Indigo Naturalis was conducted in this study with modern analytical techniques. Firstly,chemical composition was analyzed with UPLC-Q-TOF-MS,and the chemical composition of scent with HS-SPME/GC-MS/MS. The content of indigo,indirubin,total ash,and water-soluble extract was determined as well as the inorganic composition in crude Indigo Naturalis and purified Indigo Naturalis. Then,their microscopic morphology was observed and the surface element composition was investigated. Finally,the antipyretic activities of crude Indigo Naturalis and purified Indigo Naturalis were compared in the fever rat model induced by lipopolysaccharide and 2,4-dinitrophenol. The results demonstrated that the purified Indigo Naturalis had a faster and more lasting antipyretic effect,while the crude Indigo Naturalis had almost no antipyretic effect. This study is of great significance to the research on processing technology of Indigo Naturalis and provides reference for the formulation of its quality standards,production specifications and calibration procedures.


Asunto(s)
Carmin de Índigo , Indigofera , Animales , Extractos Vegetales , Ratas , Espectrometría de Masas en Tándem
13.
J Cell Physiol ; 235(3): 3069-3078, 2020 03.
Artículo en Inglés | MEDLINE | ID: mdl-31549403

RESUMEN

Children are more sensitive than adults to bitterness and thus dislike bitter tastes more than adults do. However, why children are more sensitive to bitterness has never been revealed. To elucidate the effects of age on taste perception, a double-bottle preference test was first performed with immature and adult rats. Then, RNA-Seq analysis was performed on tongues obtained from rats of the same ages as those in the double-bottle test. The immature rats exhibited a lower consumption rate of bitter solution than the adult rats. Bioinformatics analysis yielded 1,347 differentially expressed genes (DEGs) between male adult rats (MARs, 80 days old) and male immature rats (MIRs, 20 days old) and 380 DEGs between female adult rats (FARs, 80 days old) and female immature rats (FIRs, 20 days old). These DEGs were mainly associated with growth, development, differentiation, and extracellular processes, among other mechanisms. According to Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis, the DEGs were enriched for bitter taste transduction. Specifically, the Gnb3 and TRPM5 genes were downregulated in FARs compared with FIRs and in MARs compared with MIRs, and the protein expression of TRPM5 was significantly downregulated in MARs compared with MIRs. The data presented herein suggest that transcriptional regulation of taste-associated signal transduction occurs differently in tongue epithelial tissue of rats at different ages, although additional analyses are needed to confirm this conclusion.


Asunto(s)
Epitelio/metabolismo , Regulación de la Expresión Génica/genética , Transducción de Señal/genética , Transcriptoma/genética , Animales , Biología Computacional/métodos , Regulación hacia Abajo , Perfilación de la Expresión Génica/métodos , Ratas , Análisis de Secuencia de ARN/métodos
14.
Mol Pharm ; 17(5): 1586-1595, 2020 05 04.
Artículo en Inglés | MEDLINE | ID: mdl-32186879

RESUMEN

It is a challenging task to suppress the bitterness of liquid preparations, especially for children. Bitter molecules are highly dispersible in liquids, leading to a strong and instant stimulation of the bitter receptors. At present, there is no effective way to correct this issue except for adding sweeteners, resulting in an unsatisfying taste. Based on the three-point contact theory, which is a universally accepted mechanism of bitterness formation, a new idea and application of amphiphilic block copolymers (ABCs) for bitterness suppression was proposed for the first time. We found that ABCs could widely inhibit the bitterness of four typical bitter substances. The mechanism is that ABCs self-assemble to form association colloids, which attract bitter components and reduce their distribution in the molecular form in solution. The bitter components were demonstrated to automatically embed in the spiral hydrophobic cavity of the hydrophobic chain of the ABCs, and their special interaction dispersed the positive electrostatic potential of bitter groups. The combination did not affect the pharmacokinetic parameters and pharmacodynamics of bitter drugs. These findings highlight the novel application of ABCs for the inhibition of bitterness and illuminate the underlying inhibition mechanisms.


Asunto(s)
Polímeros/farmacología , Gusto/efectos de los fármacos , Animales , Berberina/farmacología , Masculino , Ratones , Micelas , Simulación del Acoplamiento Molecular , Poliésteres/farmacología , Polietilenglicoles/farmacología , Soluciones
15.
Pharmacol Res ; 161: 105109, 2020 11.
Artículo en Inglés | MEDLINE | ID: mdl-32738494

RESUMEN

Protocatechuic acid is a natural phenolic acid, which widely exists in our daily diet and herbs. It is also one of the main metabolites of complex polyphenols, such as anthocyanins and proanthocyanins. In recent years, a large number of studies on the pharmacological activities of protocatechuic acid have emerged. Protocatechuic acid has a wide range of pharmacological activities including antioxidant, anti-inflammatory, neuroprotective, antibacterial, antiviral, anticancer, antiosteoporotic, analgesia, antiaging activties; protection from metabolic syndrome; and preservation of liver, kidneys, and reproductive functions. Pharmacokinetic studies showed that the absorption and elimination rate of protocatechuic acid are faster, with glucuronidation and sulfation being the major metabolic pathways. However, protocatechuic acid displays a dual-directional regulatory effect on some pharmacological activities. When the concentration is very high, it can inhibit cell proliferation and reduce survival rate. This review aims to comprehensively summarize the pharmacology, pharmacokinetics, and toxicity of protocatechuic acid with emphasis on its pharmacological activities discovered in recent 5 years, so as to provide more up-to-date and thorough information for the preclinical and clinical research of protocatechuic acid in the future. Moreover, it is hoped that the clinical application of protocatechuic acid can be broadened, giving full play to its characteristics of rich sources, low toxicity and wide pharmacological activites.


Asunto(s)
Dieta , Hidroxibenzoatos/farmacología , Extractos Vegetales/farmacología , Animales , Relación Dosis-Respuesta a Droga , Humanos , Hidroxibenzoatos/administración & dosificación , Hidroxibenzoatos/farmacocinética , Hidroxibenzoatos/toxicidad , Extractos Vegetales/administración & dosificación , Extractos Vegetales/farmacocinética , Extractos Vegetales/toxicidad
16.
Pharmacol Res ; 155: 104738, 2020 05.
Artículo en Inglés | MEDLINE | ID: mdl-32151681

RESUMEN

Breast cancer remains the leading cause of cancer-related death among women worldwide, and its incidence is also increasing. High recurrence rate and metastasis rate are the key causes of poor prognosis and death. It is suggested that abnormal glycosylation plays an important role in the growth, invasion, metastasis and resistance to therapy of breast cancer cells. Meanwhile, it can be used as the biomarkers for the early detection and prognosis of breast cancer and the potential attractive targets for drug treatment. However, only a few attentions have been paid to the molecular mechanism of abnormal glycosylation in the epithelial-mesenchymal transition (EMT) of breast cancer cells and the related intervention of drugs. This manuscript thus investigated the relationship between abnormal glycosylation, the EMT, and breast cancer metastasis. Then, the process of abnormal glycosylation, the classification and their molecular regulatory mechanisms of breast cancer were analyzed in detail. Last, potential drugs are introduced in different categories, which are expected to reverse or intervene the abnormal glycosylation of breast cancer. This review is conducive to an in-depth understanding of the metastasis and drug resistance of breast cancer cells, which will provide new ideas for the clinical regulation of glycosylation and related drug treatments in breast cancer.


Asunto(s)
Antineoplásicos/uso terapéutico , Neoplasias de la Mama , Glicosilación/efectos de los fármacos , Animales , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/metabolismo , Neoplasias de la Mama/patología , Humanos
17.
Zhongguo Zhong Yao Za Zhi ; 45(10): 2353-2359, 2020 May.
Artículo en Zh | MEDLINE | ID: mdl-32495592

RESUMEN

Animal medicines have been called "medicine with affinity to flesh and blood" by doctors of all ages, which always act as an important branch of Chinese medicine. They have various types, extensive sources and long application history, with unique cli-nical effects in anti-coagulation, anti-thrombosis, anti-fatigue, immune regulation, anti-tumor, anti-convulsion and so on. Most animal medicines contain proteins, fatty acids, and trimethylamine oxides, which are prone to decomposition and produce substances such as biological amines, aldehydes, ketones, alcohols, trimethylamine and ammonia with unpleasant odors. The stench produced by the combination of various odors can easily cause side effects such as nausea and vomiting, which would probably affect the drug compliance and clinical efficacy in patients, and block the development of high-quality animal medicines. At present, we have insufficient understanding on sources and formation mechanism of the stench of animal medicines, lacking development of taste-masking technology. Therefore, the universality, formation, vomiting mechanism, evaluation methods, and masking technology of stench of animal medicines were summarized in this paper, so as to deepen the recognition of stench, provide references for the development of animal medicines deodorization technology, enhance patients' compliance with animal medicines, and promote animal drugs to better serve public health in the new era.


Asunto(s)
Neoplasias , Gusto , Animales , Fatiga , Humanos , Tecnología
18.
Zhongguo Zhong Yao Za Zhi ; 45(9): 2073-2081, 2020 May.
Artículo en Zh | MEDLINE | ID: mdl-32495556

RESUMEN

The iterative innovation of processing technology is one of the important tasks in studies on processing of traditional Chinese medicine(TCM). It is also the prerequisite for modern, refined, automatic and intelligent manufacturing of TCM pieces. Microwave processing is a new fire processing technique developed in the recent 30 years, with a unique thermodynamic form, and energy transfer and transformation laws. Moreover, it owns the advantages of a high processing efficiency, good product properties and low production energy consumption, with great application prospects. This paper introduced the study overview of microwave expansion technology in the food industry, reviewed the origin of microwave processing technology of TCM, and expounded the basic concept, principle and main purpose of microwave processing technology used in TCM. Then, the impacts of drug factors and microwave factors on the microwave processing effect were summarized, the industrial equipment that could be used for microwave processing was listed, and the impacts of microwave heating on starch, polysaccharide, protein and other components in Chinese herbal medicines were analyzed. Furthermore, the study advance of microwave processing of 14 herbs was investigated, including Aconiti Lateralis Radix Praeparaia, Galli Gigerii Endothelium Corneum and Asini Corii Colla; and the appearance and components of herbs processed by traditional processing method and microwave processing method were compared, so as to reveal the opportunities and challenges of microwave processing technology in the industrial transformation. We hoped that the systematic study of microwave processing technology could provide new ideas and techniques for the high-quality and high-level development of the TCM pieces industry in the new era, and promote its inheritance, innovation and transformation.


Asunto(s)
Aconitum , Medicamentos Herbarios Chinos , Medicina Tradicional China , Microondas , Control de Calidad
19.
Zhongguo Zhong Yao Za Zhi ; 45(15): 3608-3616, 2020 Aug.
Artículo en Zh | MEDLINE | ID: mdl-32893550

RESUMEN

Fatigue is a widespread and complex physiological phenomenon. Chronic fatigue can lead to cardiovascular dysfunction, mental disorders and other serious pathological reactions. Therefore, how to relieve fatigue accurately and effectively is an important proposition to implement the concept of "Healthy China" in the new era. As an important part of Chinese medicine health industry, Chinese medicine health food has been developing rapidly in recent years. At present, there are 1 157 kinds of anti-fatigue health food on the market in China, most of which are single Chinese medicine and its compound. However, their functions are generally labeled as "anti-fatigue", and their function positioning is too extensive and unclear. With the deepened understanding of fatigue classification and its physiological and pathological basis, it is urgent to be combined with the progress of modern chemical and pharmacological stu-dies to differentiate and precisely position the anti-fatigue health effects of traditional Chinese medicine. For this purpose, the classifications of fatigue were summarized in this paper, and the mechanism of fatigue was explained from the aspects of energy metabolism, accumulation of metabolites, oxidative stress, inflammation, hypothalamus pituitary adrenal axis and so on. We selected 10 traditional Chinese medicines which are most frequently used in health food, analyzed their anti-fatigue effect mechanisms, and summarized the best types of anti-fatigue food, so as to promote the scientific development of anti-fatigue health food industry, expand the market application scope of anti-fatigue health food, better respond to the construction of a healthy China and serve for people's health.


Asunto(s)
Medicamentos Herbarios Chinos , Plantas Medicinales , China , Alimentos , Medicina Tradicional China
20.
Pharmacol Res ; 148: 104409, 2019 10.
Artículo en Inglés | MEDLINE | ID: mdl-31446039

RESUMEN

It is a common phenomenon that people are in a sub-health condition and facing "unexplained fatigue", which seriously affects their health, work efficiency and quality of life. Meanwhile, fatigue is also a common symptom of many serious diseases such as HIV/AIDS, cancer, and schizophrenia. However, there are still no official recommendations for the treatment of various forms of fatigue. Some traditional natural medicines are often used as health care products, such as ginseng, Cordyceps militaris (L.ex Fr.Link) and Rhodiola rosea L., and these have been reported to have specific anti-fatigue effects with small toxic and side effects and rich pharmacological activities. It may be promising treatment strategy for sub-health. In this review, we first outline the generation of fatigue. Furthermore, we put emphasis on the anti-fatigue mechanism, bioactive components, and clinic trials of natural medicines, which will contribute to the development of potential anti-fatigue agents and open up novel treatments for sub-health.


Asunto(s)
Productos Biológicos/farmacología , Productos Biológicos/uso terapéutico , Fatiga/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Animales , Humanos , Medicina Tradicional/métodos , Fitoterapia/métodos , Calidad de Vida
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