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1.
FASEB J ; 38(12): e23736, 2024 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-38865202

RESUMO

Subclinical hypothyroidism (SCH) in pregnancy is the most common form of thyroid dysfunction in pregnancy, which can affect fetal nervous system development and increase the risk of neurodevelopmental disorders after birth. However, the mechanism of the effect of maternal subclinical hypothyroidism on fetal brain development and behavioral phenotypes is still unclear and requires further study. In this study, we constructed a mouse model of maternal subclinical hypothyroidism by exposing dams to drinking water containing 50 ppm propylthiouracil (PTU) during pregnancy and found that its offspring were accompanied by severe cognitive deficits by behavioral testing. Mechanistically, gestational SCH resulted in the upregulation of protein expression and activity of HDAC1/2/3 in the hippocampus of the offspring. ChIP analysis revealed that H3K9ac on the neurogranin (Ng) promoter was reduced in the hippocampus of the offspring of SCH, with a significant reduction in Ng protein, leading to reduced expression levels of synaptic plasticity markers PSD95 (a membrane-associated protein in the postsynaptic density) and SYN (synaptophysin, a specific marker for presynaptic terminals), and impaired synaptic plasticity. In addition, administration of MS-275 (an HDAC1/2/3-specific inhibitor) to SCH offspring alleviated impaired synaptic plasticity and cognitive dysfunction in offspring. Thus, our study suggests that maternal subclinical hypothyroidism may mediate offspring cognitive dysfunction through the HDAC1/2/3-H3K9ac-Ng pathway. Our study contributes to the understanding of the signaling mechanisms underlying maternal subclinical hypothyroidism-mediated cognitive impairment in the offspring.


Assuntos
Disfunção Cognitiva , Histona Desacetilase 1 , Histona Desacetilase 2 , Hipotireoidismo , Neurogranina , Efeitos Tardios da Exposição Pré-Natal , Animais , Neurogranina/metabolismo , Neurogranina/genética , Hipotireoidismo/metabolismo , Feminino , Gravidez , Camundongos , Disfunção Cognitiva/metabolismo , Disfunção Cognitiva/etiologia , Histona Desacetilase 2/metabolismo , Histona Desacetilase 2/genética , Efeitos Tardios da Exposição Pré-Natal/metabolismo , Histona Desacetilase 1/metabolismo , Histona Desacetilase 1/genética , Regulação para Baixo , Hipocampo/metabolismo , Masculino , Histona Desacetilases/metabolismo , Histona Desacetilases/genética , Camundongos Endogâmicos C57BL , Plasticidade Neuronal
2.
Cereb Cortex ; 34(1)2024 01 14.
Artigo em Inglês | MEDLINE | ID: mdl-38044469

RESUMO

Brain function changes affect cognitive functions in older adults, yet the relationship between cognition and the dynamic changes of brain networks during naturalistic stimulation is not clear. Here, we recruited the young, middle-aged and older groups from the Cambridge Center for Aging and Neuroscience to investigate the relationship between dynamic metrics of brain networks and cognition using functional magnetic resonance imaging data during movie-watching. We found six reliable co-activation pattern (CAP) states of brain networks grouped into three pairs with opposite activation patterns in three age groups. Compared with young and middle-aged adults, older adults dwelled shorter time in CAP state 4 with deactivated default mode network (DMN) and activated salience, frontoparietal and dorsal-attention networks (DAN), and longer time in state 6 with deactivated DMN and activated DAN and visual network, suggesting altered dynamic interaction between DMN and other brain networks might contribute to cognitive decline in older adults. Meanwhile, older adults showed easier transfer from state 6 to state 3 (activated DMN and deactivated sensorimotor network), suggesting that the fragile antagonism between DMN and other cognitive networks might contribute to cognitive decline in older adults. Our findings provided novel insights into aberrant brain network dynamics associated with cognitive decline.


Assuntos
Encéfalo , Imageamento por Ressonância Magnética , Imageamento por Ressonância Magnética/métodos , Encéfalo/diagnóstico por imagem , Encéfalo/fisiologia , Cognição/fisiologia , Mapeamento Encefálico , Rede Nervosa/diagnóstico por imagem , Rede Nervosa/fisiologia
3.
Cell Mol Life Sci ; 81(1): 20, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-38195774

RESUMO

Accumulating research shows that prenatal exposure to maternal stress increases the risk of behavioral and mental health problems for offspring later in life. However, how prenatal stress affects offspring behavior remains unknown. Here, we found that prenatal stress (PNS) leads to reduced Ahi1, decreased synaptic plasticity and cognitive impairment in offspring. Mechanistically, Ahi1 and GR stabilize each other, inhibit GR nuclear translocation, promote Ahi1 and WDR68 binding, and inhibit DYRK1A and WDR68 binding. When Ahi1 deletion or prenatal stress leads to hyperactivity of the HPA axis, it promotes the release of GC, leading to GR nuclear translocation and Ahi1 degradation, which further inhibits the binding of Ahi1 and WDR68, and promotes the binding of DYRK1A and WDR68, leading to elevated DYRK1A, reduced synaptic plasticity, and cognitive impairment. Interestingly, we identified RU486, an antagonist of GR, which increased Ahi1/GR levels and improved cognitive impairment and synaptic plasticity in PNS offspring. Our study contributes to understanding the signaling mechanisms of prenatal stress-mediated cognitive impairment in offspring.


Assuntos
Disfunção Cognitiva , Sistema Hipotálamo-Hipofisário , Feminino , Gravidez , Humanos , Sistema Hipófise-Suprarrenal , Disfunção Cognitiva/etiologia , Plasticidade Neuronal
4.
Nanotechnology ; 35(41)2024 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-39008958

RESUMO

The rise of gene therapy has solved many diseases that cannot be effectively treated by conventional methods. Gene vectors is very important to protect and deliver the therapeutic genes to the target site. Polyethyleneimine (PEI) modified with mannitol could enhance the gene transfection efficiency reported by our group previously. In order to further control and improve the effective gene release to action site, disulfide bonds were introduced into mannitol-modified PEI to construct new non-viral gene vectors PeiSM. The degrees of mannitol linking with disulfide bonds were screened. Among them, moderate mannitol-modified PEI with disulfide bonds showed the best transfection efficiency, and significantly enhanced long-term systemic transgene expression for 72 hin vivoeven at a single dose administration, and could promote caveolae-mediated uptake through up-regulating the phosphorylation of caveolin-1 and increase the loaded gene release from the nanocomplexes in high glutathione intracellular environment. This functionalized gene delivery system can be used as an potential and safe non-viral nanovector for further gene therapy.


Assuntos
Vetores Genéticos , Glutationa , Polietilenoimina , Transfecção , Polietilenoimina/química , Transfecção/métodos , Glutationa/metabolismo , Glutationa/química , Animais , Humanos , Vetores Genéticos/química , Vetores Genéticos/genética , Manitol/química , Camundongos , Caveolina 1/metabolismo , Caveolina 1/genética , Terapia Genética/métodos , Técnicas de Transferência de Genes , Dissulfetos/química
5.
Cereb Cortex ; 33(13): 8645-8653, 2023 06 20.
Artigo em Inglês | MEDLINE | ID: mdl-37143182

RESUMO

Sex differences in episodic memory (EM), remembering past events based on when and where they occurred, have been reported, but the neural mechanisms are unclear. T1-weighted images of 111 females and 61 males were acquired from the Dallas Lifespan Brain Study. Using surface-based morphometry and structural covariance (SC) analysis, we constructed structural covariance networks (SCN) based on cortical volume, and the global efficiency (Eglob) was computed to characterize network integration. The relationship between SCN and EM was examined by SC analysis among the top-n brain regions that were most relevant to EM performance. The number of SC connections (females: 3306; males: 437, P = 0.0212) and Eglob (females: 0.1845; males: 0.0417, P = 0.0408) of SCN in females were higher than those in males. The top-n brain regions with the strongest SC in females were located in auditory network, cingulo-opercular network (CON), and default mode network (DMN), and in males, they were located in frontoparietal network, CON, and DMN. These results confirmed that the Eglob of SCN in females was higher than males, sex differences in EM performance might be related to the differences in network-level integration. Our study highlights the importance of sex as a research variable in brain science.


Assuntos
Memória Episódica , Humanos , Masculino , Feminino , Caracteres Sexuais , Encéfalo , Imageamento por Ressonância Magnética , Mapeamento Encefálico
6.
Ecotoxicol Environ Saf ; 274: 116177, 2024 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-38461573

RESUMO

Triphenyltin (TPT) is a typical persistent organic pollutant whose occurrence in coral reef ecosystems may threaten the survival of reef fishes. In this study, a brightly colored representative reef fish, Amphiprion ocellaris was used to explore the effects of TPT at environmental levels (1, 10, and 100 ng/L) on skin pigment synthesis. After the fish were exposed to TPT for 60 days, the skin became darker, owing to an increase in the relative area of black stripes, a decrease in orange color values while an increase in brown color values, and an increase in the number of melanocytes in the orange part of the skin tissues. To explore the mechanisms by which TPT induces darker body coloration, the enzymatic activity and gene expression levels of the members of melanocortin system that affect melanin synthesis were evaluated. Leptin levels and lepr expression were found to be increased after TPT exposure, which likely contributed to the increase found in pomc expression and α-melanocyte-stimulating hormone (α-MSH) levels. Then Tyr activity and mc1r, tyr, tyrp1, mitf, and dct were upregulated, ultimately increasing melanin levels. Importantly, RT-qPCR results were consistent with the transcriptome analysis of trends in lepr and pomc expression. Because the orange color values decreased, pterin levels and the pteridine metabolic pathway were also evaluated. The results showed that TPT induced BH4 levels and spr, xdh, and gch1 expression associated with pteridine synthesis decreased, ultimately decreasing the colored pterin content (sepiapterin). We conclude that TPT exposure interferes with the melanocortin system and pteridine metabolic pathway to increase melanin and decrease colored pterin levels, leading to darker body coloration in A. ocellaris. Given the importance of body coloration for the survival and reproduction of reef fishes, studies on the effects of pollutants (others alongside TPT) on body coloration are of high priority.


Assuntos
Melanocortinas , Compostos Orgânicos de Estanho , Perciformes , Animais , Pró-Opiomelanocortina , Ecossistema , Melaninas/genética , Pteridinas , Peixes/genética , Perciformes/genética , Pterinas , Redes e Vias Metabólicas
7.
Inflammopharmacology ; 32(3): 1659-1704, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38520574

RESUMO

Curcumol (Cur), a guaiane-type sesquiterpenoid hemiketal, is an important and representative bioactive component extracted from the essential oil of the rhizomes of Curcumae rhizoma which is also known as "Ezhu" in traditional Chinese medicine. Recently, Cur has received considerable attention from the research community due to its favorable pharmacological activities, including anti-cancer, hepatoprotective, anti-inflammatory, anti-viral, anti-convulsant, and other activities, and has also exerted therapeutic effect on various cancers, liver diseases, inflammatory diseases, and infectious diseases. Pharmacokinetic studies have shown that Cur is rapidly distributed in almost all organs of rats after intragastric administration with high concentrations in the small intestine and colon. Several studies focusing on structure-activity relationship (SAR) of Cur have shown that some Cur derivatives, chemically modified at C-8 or C-14, exhibited more potent anti-cancer activity and lower toxicity than Cur itself. This review aims to comprehensively summarize the latest advances in the pharmacological and pharmacokinetic properties of Cur in the last decade with a focus on its anti-cancer and hepatoprotective potentials, as well as the research progress in drug delivery system and potential applications of Cur to date, to provide researchers with the latest information, to highlighted the limitations of relevant research at the current stage and the aspects that should be addressed in future research. Our results indicate that Cur and its derivatives could serve as potential novel agents for the treatment of a variety of diseases, particularly cancer and liver diseases.


Assuntos
Sistemas de Liberação de Medicamentos , Sesquiterpenos , Animais , Sesquiterpenos/farmacologia , Sesquiterpenos/farmacocinética , Sesquiterpenos/administração & dosagem , Humanos , Relação Estrutura-Atividade , Sistemas de Liberação de Medicamentos/métodos , Antineoplásicos/farmacocinética , Antineoplásicos/farmacologia , Antineoplásicos/administração & dosagem
8.
Biol Reprod ; 106(4): 687-698, 2022 04 26.
Artigo em Inglês | MEDLINE | ID: mdl-34935917

RESUMO

Assisted reproductive technology (ART) has been used globally among infertile couples. However, many epidemiological investigations have indicated that ART is associated with a range of long-term adverse health outcomes in offspring, including cardiovascular disease, obesity, and increased plasma lipid levels. Until now, direct evidence has been limited regarding the pathological changes in vascular function in fetuses with ART. In this study, human umbilical cords were collected from healthy normal pregnancies and in vitro fertilization and embryo transfer (IVF-ET) pregnancies. Vascular functional studies involving acetylcholine (ACh), antagonists of its specific receptors, and L-type calcium channel/PKC-MLC20 phosphorylation pathway specific inhibitors were conducted. Quantitative real-time PCR, Western blotting, and methylation analyses were performed on umbilical vein samples. We found that the umbilical vein constriction induced by ACh in the IVF-ET group was significantly attenuated compared with that in the healthy normal pregnancy group, which was not only associated with the hypermethylation of ACh muscarinic receptor subtype 3 (CHRM3) and decreased expression of CHRM3, PKCß, and CaV1.2, but was also related to the reduced phosphorylation of MLC20. This study revealed that the hypermethylation of CHRM3, leading to a reduction in CHRM3 expression and downregulation of the CaV1.2/PKC-MLC20 phosphorylation pathway, was responsible for the decreased sensitivity to ACh observed in the umbilical vein under IVF-ET conditions. The hypermethylation of CHRM3 caused by IVF-ET might play an important role in altered vasoconstriction and impact cardiovascular systems in the long run.


Assuntos
Transferência Embrionária , Receptor Muscarínico M3 , Técnicas de Reprodução Assistida , Acetilcolina , Metilação de DNA , Transferência Embrionária/métodos , Feminino , Fertilização in vitro/métodos , Humanos , Gravidez , Receptor Muscarínico M3/metabolismo , Veias Umbilicais
9.
J Transl Med ; 20(1): 135, 2022 03 18.
Artigo em Inglês | MEDLINE | ID: mdl-35303878

RESUMO

Urokinase-type plasminogen activator receptor (uPAR) is an attractive target for the treatment of cancer, because it is expressed at low levels in healthy tissues but at high levels in malignant tumours. uPAR is closely related to the invasion and metastasis of malignant tumours, plays important roles in the degradation of extracellular matrix (ECM), tumour angiogenesis, cell proliferation and apoptosis, and is associated with the multidrug resistance (MDR) of tumour cells, which has important guiding significance for the judgement of tumor malignancy and prognosis. Several uPAR-targeted antitumour therapeutic agents have been developed to suppress tumour growth, metastatic processes and drug resistance. Here, we review the recent advances in the development of uPAR-targeted antitumor therapeutic strategies, including nanoplatforms carrying therapeutic agents, photodynamic therapy (PDT)/photothermal therapy (PTT) platforms, oncolytic virotherapy, gene therapy technologies, monoclonal antibody therapy and tumour immunotherapy, to promote the translation of these therapeutic agents to clinical applications.


Assuntos
Neoplasias , Receptores de Ativador de Plasminogênio Tipo Uroquinase , Humanos , Neoplasias/terapia , Prognóstico , Receptores de Ativador de Plasminogênio Tipo Uroquinase/genética , Receptores de Ativador de Plasminogênio Tipo Uroquinase/metabolismo , Transdução de Sinais , Ativador de Plasminogênio Tipo Uroquinase/genética , Ativador de Plasminogênio Tipo Uroquinase/metabolismo
10.
J Nanobiotechnology ; 20(1): 509, 2022 Dec 03.
Artigo em Inglês | MEDLINE | ID: mdl-36463199

RESUMO

Norcantharidin (NCTD) is a demethylated derivative of cantharidin (CTD), the main anticancer active ingredient isolated from traditional Chinese medicine Mylabris. NCTD has been approved by the State Food and Drug Administration for the treatment of various solid tumors, especially liver cancer. Although NCTD greatly reduces the toxicity of CTD, there is still a certain degree of urinary toxicity and organ toxicity, and the poor solubility, short half-life, fast metabolism, as well as high venous irritation and weak tumor targeting ability limit its widespread application in the clinic. To reduce its toxicity and improve its efficacy, design of targeted drug delivery systems based on biomaterials and nanomaterials is one of the most feasible strategies. Therefore, this review focused on the studies of targeted drug delivery systems combined with NCTD in recent years, including passive and active targeted drug delivery systems, and physicochemical targeted drug delivery systems for improving drug bioavailability and enhancing its efficacy, as well as increasing drug targeting ability and reducing its adverse effects.


Assuntos
Compostos Bicíclicos Heterocíclicos com Pontes , Neoplasias , Estados Unidos , Sistemas de Liberação de Medicamentos , Meia-Vida , Disponibilidade Biológica , Neoplasias/tratamento farmacológico
11.
Ecotoxicol Environ Saf ; 239: 113682, 2022 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-35643027

RESUMO

Fluoride exposure has a detrimental effect on neurodevelopment, while the underlying processes remain unknown. The goal of this study was to investigate how fluoride impacts synaptogenesis, with a focus on the phosphorylation of Creb1 (p-Creb1)-brain-derived neurotrophic factor (BDNF)-tyrosine kinase B (TrkB) pathway. We generated a sodium fluoride (NaF) model using C57 BL/6 J mice exposed to 100 mg/L NaF from gestation day 1 (GD1) to GD20. It was identified that NaF treatment impaired the learning and memory abilities of the male offspring, reduced dendritic spine density, lowered postsynaptic density protein-95 (PSD95) and synaptophysin (SYN) expression in the male offspring's hippocampus, indicating that synaptic dysfunction may contribute to the cognitive impairment in the NaF model. In addition, in vivo experiment demonstrated that the protein abundance of BDNF and the ratio of p-Creb1 to Creb1 were increased in the hippocampus of NaF offspring, while the level of TrkB was reduced. Similarly, PC12 cells treated with NaF also showed increased expression of BDNF and decreased levels of TrkB. Notably, fluoride treatment increased p-Creb1 in vitro, while inhibiting p-Creb1 by 66615 significantly alleviated the effects of NaF exposure, indicating that p-Creb1 exerts a regulatory function in the BDNF-TrkB pathway. Altogether, these results demonstrated prenatal fluoride exposure triggered neurotoxicity in the male offspring hippocampus was linked to synaptogenesis damage caused by activating p-Creb1, which disrupted the BDNF-TrkB pathway.


Assuntos
Fator Neurotrófico Derivado do Encéfalo , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico , Fluoretos , Efeitos Tardios da Exposição Pré-Natal , Receptor trkB , Animais , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Cognição , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , Feminino , Fluoretos/toxicidade , Hipocampo/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Fosforilação , Gravidez , Efeitos Tardios da Exposição Pré-Natal/fisiopatologia , Proteínas Tirosina Quinases/metabolismo , Ratos , Receptor trkB/metabolismo , Transdução de Sinais
12.
Zhongguo Zhong Yao Za Zhi ; 47(6): 1539-1545, 2022 Mar.
Artigo em Zh | MEDLINE | ID: mdl-35347951

RESUMO

This study aims to acetylate Rehmannia glutinosa polysaccharides by acetic anhydride method, optimize process parameters and evaluate their antioxidant activity. With the degree of substitution(D_s) as a criterion, the effects of reaction time, acetic anhydride-to-polysaccharides ratio and temperature were investigated. Process parameters were optimized by single-factor experiment and response surface methodology. The infrared spectroscopy(IR) and scanning electron microscopy(SEM) proved the successful acetylation and were employed to preliminarily analyze the structural characteristics of acetylated derivatives. The results showed that the D_s was 0.327 under the optimal technological conditions, including m(acetic anhydride):m(R. glutinosa polysaccharides)=2.70, reaction time 3.0 h and temperature 48 ℃. Further, the antioxidant properties of acetylated derivatives were investigated in vitro and acetylation was found effective to improve the antioxidant activity of R. glutinosa polysaccharides. This study provides a reference for the further development and application of R. glutinosa polysaccharides.


Assuntos
Rehmannia , Acetilação , Antioxidantes/química , Antioxidantes/farmacologia , Polissacarídeos/química , Polissacarídeos/farmacologia , Rehmannia/química
13.
Zhongguo Yi Liao Qi Xie Za Zhi ; 46(2): 225-229, 2022 Mar 30.
Artigo em Zh | MEDLINE | ID: mdl-35411756

RESUMO

This study introduced the current testing content and standards of ECG medical electronic instruments, combined with actual clinical needs, and discussed the comprehensive verification and evaluation protocol for ECG medical electronic instruments. The protocol mainly includes hardware performance testing, automatic diagnostic function testing and clinical application evaluation. The protocol emphasizes the clinical practicality and importance of the comprehensive verification and evaluation program, and provides a reference for the institutions involved in the program.


Assuntos
Eletrocardiografia , Eletrônica Médica , Padrões de Referência
14.
Pharm Biol ; 59(1): 606-618, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34010591

RESUMO

CONTEXT: The coriander plant Centipeda minima (L.) A. Braun et Aschers (Compositae) is used for the treatment of allergic rhinitis. OBJECTIVE: Analyze the difference of the C. minima volatile oil from 7 geographic areas and its therapeutic effect on allergic rhinitis. MATERIALS AND METHODS: The volatile oils from different geographic areas were extracted and analyzed, the protein and biological pathway for the treatment of allergic rhinitis were predicted by network pharmacology. Established three groups of Sprague-Dawley rat allergic rhinitis models (n = 10). The treatment group was given 100 µL/nostril of 0.1% C. minima volatile oil, the blank and model groups were given the same amount of normal saline. After 15 days, serum inflammatory factors were detected by ELISA. Nasal mucosa tissues were examined by hematoxylineosin staining and immunuhistrochemistry. RESULTS: There are differences in the content of volatile oil in the seven geographic areas. Experiments showed that the concentration of TNF-α in the serum of the administration group decreased from 63.66 ± 2.06 to 51.01 ± 4.10 (pg/mL), IL-4 decreased from 41.90 ± 3.90 to 28.68 ± 3.39 (pg/mL), IgE decreased from 22.18 ± 1.40 to 17.59 ± 1.60 (pg/mL), IL-2 increased from 314.14 ± 10.32 to 355.90 ± 10.01(pg/mL). Immunohistochemistry showed that compared with the model group, the PTGS2 and MAPK3 proteins in the administration group were significantly reduced. DISCUSSION AND CONCLUSIONS: C. minima volatile oil is a multi-target and multi-pathway in the treatment of allergic rhinitis, which provides a new research basis and reference for the treatment of allergic rhinitis.


Assuntos
Asteraceae , Medicamentos de Ervas Chinesas/uso terapêutico , Óleos Voláteis/uso terapêutico , Rinite Alérgica/tratamento farmacológico , Animais , Asteraceae/genética , China/etnologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Etnobotânica , Geografia , Mediadores da Inflamação/antagonistas & inibidores , Mediadores da Inflamação/imunologia , Masculino , Mucosa Nasal/efeitos dos fármacos , Mucosa Nasal/imunologia , Mucosa Nasal/patologia , Óleos Voláteis/isolamento & purificação , Mapas de Interação de Proteínas/genética , Ratos , Ratos Sprague-Dawley , Rinite Alérgica/imunologia , Rinite Alérgica/patologia , Resultado do Tratamento
15.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6011-6019, 2021 Dec.
Artigo em Zh | MEDLINE | ID: mdl-34951227

RESUMO

Solid preparations account for more than 50% of traditional Chinese medicines(TCM). TCM powder is an important raw material for solid preparations of TCM. Its powder properties directly affect the quality of solid preparations, and even clinical safety and effectiveness. Particle design technology based on the characteristics of powder in TCM is an important means to improve and enhance the quality of solid preparations. This study summarized the relevant principles, methods, characteristics, classification, equipment, and other elements of particle design technology in recent years, analyzed the difficulties in its application in the field of TCM powder, and proposed the strategies in conjunction with the development of computer data mining. The present study is expected to provide a reference for the suitability of particle design in the field of TCM powder.


Assuntos
Medicamentos de Ervas Chinesas , Medicina Tradicional Chinesa , Pós , Tecnologia
16.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6028-6034, 2021 Dec.
Artigo em Zh | MEDLINE | ID: mdl-34951229

RESUMO

Targeting the deficiencies of Lingzhu Powder, this study introduced the particle design technology to improve its quality. Based on the mechanism of particle design for powder and the characteristics of solvent evaporation method, composite particles consisting of Succinum, Cinnabaris, and artificial Bovis Calculus were prepared. And the powder properties of composite particles and physical mixtures as well as the content uniformity of toxic components were investigated for exploring the technological advantages of particle design in improving the quality of Lingzhu Powder. The results showed that the composite particles prepared using solvent evaporation method and particle design technology were micro-particles, and the stable agglomerate structure could be observed under SEM. Composite particles exhibited better fluidity and compliance in oral intake than physical mixtures. The differences in chromatism, bulk density, and content uniformity of the composite particles were smaller than those of physical mixtures, and the corresponding RSD values \[4.8%, 1.8%, 3.4%(bilirubin), and 0.63%(HgS), respectively\] were smaller. The solvent evaporation combined with particle design technology can be utilized to significantly improve the quality of Lingzhu Powder, which has provided new ideas for the optimization of the quality of traditional Chinese medicinal powder.


Assuntos
Tecnologia , Tamanho da Partícula , Pós , Solventes
17.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6035-6044, 2021 Dec.
Artigo em Zh | MEDLINE | ID: mdl-34951230

RESUMO

Due to the complex source and different physical and chemical properties of traditional Chinese medicines(TCM) powder, there are many common pharmaceutical problems in its preparation, such as large particle size difference, poor mixing uniformity, and poor compliance with oral intake, which has directly affected the quality of solid preparations as well as their clinical efficacy and safety. This study observed the property of Zhuhuang Chuihou Powder and extract its pharmaceutical defects. It was found that realgar and calcined Borax in Zhuhuang Chuihou Powder were heavy in texture and toxic, and they were easy to be isolated, indicating the potential safety hazard. At the same time, Coptidis Rhizoma and Phellodendri Chinensis Cortex were the main sources of its bitterness. Therefore, based on the idea of "drug-excipients unity", the particle design technology was used to prepare core/shell-type composite particles with bitter medicines as the core and mineral medicines as shell. Both infrared spectroscopy and scanning electron microscopy results indicated the formation of composite particles, and the taste of these composite particles were improved. Compared with the physical mixtures, the composite particles exhibited significantly decreased RSD values in the content uniformity of berberine hydrochloride, arsenic disulfide, and sodium tetraborate and appearance uniformity. The introduction of particle design technology solved the problem of uneven dispersion of Zhuhuang Chuihou Powder, thus ensuring its uniform dispersion, stability, and control and improving the quality of the original preparation. This has provided a scientific basis for the quality control of TCM powder.


Assuntos
Medicamentos de Ervas Chinesas , China , Tamanho da Partícula , Pós , Paladar
18.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6045-6052, 2021 Dec.
Artigo em Zh | MEDLINE | ID: mdl-34951231

RESUMO

Targeting the poor powder characteristics of the contents in Hewei Jiangni Capsules, this study characterized the powder properties of the contents and employed particle design technique for improving the content quality. The content composite particles of Hewei Jiangni Capsules prepared by the particle design technique were evaluated by scanning electron microscopy(SEM), followed by infrared ray(IR), content uniformity, and in vitro dissolution detection. It was found that there was a good correlation between the crushed particle size of slices and the crushing time, and the calcined Haematitum was responsible for the poor content uniformity. After the fine powder of calcined Haematitum was super-finely ground for 8.5 min and those of the other contents in the capsule for 1 min, they were prepared into the composite particles, whose property characterizations were compared with those of the physical mixtures. The content uniformity of the prepared composite particles was significantly improved, and the preparation process was stable and reliable. The adoption of particle design technology to correct the poor uniformity of the physical mixture, solve the pharmaceutical defects of Hewei Jiangni Capsules, and improve the quality of prescriptions has provided important reference for the clinical application and development of Chinese medicinal preparations.


Assuntos
Cápsulas , Microscopia Eletrônica de Varredura , Tamanho da Partícula , Pós
19.
Zhongguo Zhong Yao Za Zhi ; 46(18): 4757-4764, 2021 Sep.
Artigo em Zh | MEDLINE | ID: mdl-34581086

RESUMO

A spectrum-activity relationship is established with high performance liquid chromatography(HPLC) fingerprints and the in vitro antioxidant activity to improve the quality evaluation system of Aralia taibaiensis. The HPLC profiles of 12 batches of samples were collected, and the similarity evaluation, heat map analysis and principal component analysis were conducted for the chemometric study of the fingerprint data. Combined with grey correlation analysis, the contributions of the common peaks in the fingerprints to the antioxidant activity were clarified, and the important peaks reflecting the efficacy were identified. The results showed that 17 common peaks were found in 12 batches of A. taibaiensis samples, and 6 of them were identified as saponins. Similarity evaluation, heat map analysis and principal component analysis roughly classified the A. taibaiensis herbs into two categories, i.e.,(1) S1-S10, S12 and(2) S11. Twelve batches of samples showed different antioxidant activities in a dose-dependent manner. In particular, S9 had the strongest antioxidant activity, while S11 was the weakest in antioxidant capacity, which was basically consistent with the overall score results. The results of grey correlation analysis demonstrated that the 17 common peaks scavenged DPPH radicals in the following order: X_3>X_(17)>X_4>X_8>X_7>X_(13)>X_2>X_6>X_(11)>X_(10)>X_(16)>X_(12)>X_9>X_5>X_(14)>X_1>X_(15), and scavenged ABTS radicals in the order of X_4>X_3>X_7>X_8>X_2>X_(17)>X_(13)>X_6>X_(16)>X_(11)>X_5>X_(12)>X_(10)>X_9>X_(14)>X_1>X_(15). Among them, X_3, X_4, X_7(araloside C), X_8 and X_(17) were the important peaks reflecting the efficacy of A. taibaiensis, which were basically consistent with those contained in the principal component 1. In this study, the correlation between the HPLC fingerprints of 12 batches of A. taibaiensis and its antioxidant activity provides a reference for the Q-marker screening and quality control of A. taibaiensis.


Assuntos
Aralia , Medicamentos de Ervas Chinesas , Saponinas , Antioxidantes , Cromatografia Líquida de Alta Pressão
20.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6053-6061, 2021 Dec.
Artigo em Zh | MEDLINE | ID: mdl-34951232

RESUMO

Based on the defects in powder properties of the contents of Ziyin Yiwei Capsules, this study screened out the main medicinal slice powders causing the poor powdery properties, and introduced the powder modification process to improve the powdery properties of these slice powders, the pharmaceutical properties of the capsule contents, and the content uniformity of Ziyin Yiwei Capsules, so as to provide a demonstration for the application of powder modification technology to the preparation of Chinese medicinal solid preparations. Through the investigation on the powder properties of the contents of Ziyin Yiwei Capsules, it was clarified that the pulverized particle size of the capsule contents had a good correlation with the pulverization time. According to the measurement results of the powder fluidity and wettability, the quality defects of the capsule contents were caused by the fine powders of Taraxaci Herba and Lungwortlike Herba. "Core-shell" composite particles were prepared from medicinal excipients magnesium stearate and fine powders of Taraxaci Herba and Lungwortlike Herba slices after ultra-fine pulverization to improve the powder properties of the problematic fine powders. Powder characterization data including fluidity and wettability were measured, followed by scanning electron microscopy(SEM) and infrared ray(IR) detection. It was determined that the optimal dosage of magnesium stearate was 2%, and the compositing time was 3 min. The composite particles were then used as content components of the Ziyin Yiwei Capsules. The powder characteristics between the original capsule and the modified composite capsule including the particle size, fluidity, wettability, uniformity of bulk density, and uniformity of chromatism as well as the content uniformity and in vitro dissolution were compared. The results showed that the powder characteristics and content uniformity of the prepared composite capsule were significantly improved, while the material basis of the preparation was not changed before and after modification. The preparation process was proved to be stable and feasible. The powder modification technology solved the pharmaceutical defects that were easy to appear in the preparation of traditional capsules, which has provided experimental evidence for the use of powder modification technology for improving the quality of Chinese medicinal solid preparations and promoting the secondary development and upgrading of traditional Chinese medicinal dosage forms such as capsules.


Assuntos
Excipientes , Cápsulas , Tamanho da Partícula , Pós , Molhabilidade
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