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1.
Zhongguo Zhong Yao Za Zhi ; 48(20): 5540-5547, 2023 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-38114146

RESUMO

The effective components of flavonoids in the "Pueraria lobata-Hovenia dulcis" drug pair have low bioavailability in vivo due to their unstable characteristics. This study used microemulsions with amphoteric carrier properties to solve this problem. The study drew pseudo-ternary phase diagrams through titration compatibility experiments of the oil phase with emulsifiers and co-emulsifiers and screened the prescription composition of blank microemulsions. The study used average particle size and PDI as evaluation indicators, and the central composite design-response surface method(CCD-RSM) was used to optimize the prescription; high-dosage drug-loaded microemulsions were obtained, and their physicochemical properties, appearance, and stability were evaluated. The results showed that when ethyl butyrate was used as the oil phase, polysorbate 80(tween 80) as the surfactant, and anhydrous ethanol as the cosurfactant, the maximum microemulsion area was obtained. When the difference in results was small, K_(m )of 1∶4 was chosen to ensure the safety of the prescription. The prescription composition optimized by the CCD-RSM was ethyl butyrate(16.28%), tween 80(9.59%), and anhydrous ethanol(38.34%). When the dosage reached 3% of the system mass, the total flavonoid microemulsion prepared had a clear and transparent appearance, with average particle size, PDI, and potential of(74.25±1.58)nm, 0.277±0.043, and(-0.08±0.07) mV, respectively. The microemulsion was spherical and evenly distributed under transmission electron microscopy. The centrifugal stability and temperature stability were good, and there was no layering or demulsification phenomenon, which significantly improved the in vitro dissolution of total flavonoids.


Assuntos
Polissorbatos , Pueraria , Polissorbatos/química , Flavonoides , Tensoativos/química , Etanol , Emulsões , Tamanho da Partícula , Solubilidade
2.
Zhongguo Zhong Yao Za Zhi ; 48(17): 4819-4824, 2023 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-37802822

RESUMO

Hypertension is the most important risk factor for cardiovascular disease-related deaths among urban and rural residents, and it has become a significant global public health issue. In October 2022, the Clinical Practice Guidelines for the Management of Hypertension in China(hereinafter referred to as the Practice Guidelines) were jointly released by the National Cardiovascular Center and other academic organizations. The Practice Guidelines sparked extensive discussions as they clearly lowered the diagnostic criteria for hypertension, raised the blood pressure targets for elderly patients, and proposed changes in the timing of early medication intervention. While these adjustments have some international evidence-based support, there is still debate regarding the cardiovascular benefits of intensified blood pressure control based on the existing level of evidence. Furthermore, whether the series of new standards proposed in the Practice Guidelines are suitable for the Chinese population and whether the hypertension control level in primary care in China can adapt to the new diagnostic and treatment standards require further in-depth research. In contrast to the strict blood pressure control concept emphasized in the Practice Guidelines, traditional Chinese medicine(TCM) emphasizes the concept of comprehensive prevention and treatment and holistic therapy in the treatment of hypertension, including prehypertension, hypertension, and target organ damage. In recent years, based on abundant clinical trial research and high-quality evidence-based support, the advantages of TCM in treating hypertension have gradually emerged. Previous studies by this research team have found that the pathogenesis of hypertension includes three major types: fire syndrome, fluid retention syndrome, and deficiency syndrome. TCM treatment of hypertension features stable blood pressure reduction, gentle blood pressure lowering, and long-lasting effects. In addition to blood pressure reduction, it also has effects such as reversing risk factors and protecting target organ damage. It demonstrates the characteristics of multiple targets, multiple components, and comprehensive regulation, and can be applied throughout the entire process of prevention and treatment, including prehypertension, hypertension, and target organ damage in the early, middle, and late stages of hypertension. Therefore, it has certain clinical application prospects.


Assuntos
Hipertensão , Pré-Hipertensão , Idoso , Humanos , Anti-Hipertensivos/uso terapêutico , China , Hipertensão/diagnóstico , Hipertensão/tratamento farmacológico , Medicina Tradicional Chinesa , Pré-Hipertensão/tratamento farmacológico , Guias de Prática Clínica como Assunto
3.
Zhongguo Zhong Yao Za Zhi ; 47(12): 3265-3269, 2022 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-35851120

RESUMO

Macroporous resin chromatography, silica gel column chromatography, preparative thin layer chromatography, and semi-preparative high performance liquid chromatography were performed to isolate two compounds from the acid extract of the lateral roots of Aconitum carmichaelii: a new 9-phenylisoquinoline alkaloid(1) and a known pavine alkaloid(2). Their structures were elucidated by spectroscopy. The absolute configuration of compound 1 was identified by electronic circular dichroism(ECD) and it was determined to be(aS)-7,8-dimethoxy-9-(2-carboxy-4,5-dimethoxyphenyl)-3,4-dihydroisoquinoline-1(2H)-one(1). The cardioprotective effects of 1 and 2 against doxorubicin-induced toxicity in H9 c2 cells were evaluated. Both of the isoquinoline alkaloids showed cardioprotective activity.


Assuntos
Aconitum , Alcaloides , Medicamentos de Ervas Chinesas , Aconitum/química , Alcaloides/análise , Alcaloides/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Raízes de Plantas/química
4.
Fitoterapia ; 149: 104822, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33387644

RESUMO

Fuzi, a well-known traditional Chinese medicine developed from the lateral roots of Aconitum carmichaelii Debx., has been widely used for the treatment of heart failure. In order to search for active compounds from Fuzi, a phytochemical study was performed, which resulted in the isolation of 14 aminoalcohol-diterpenoid alkaloids, including one new compound (1). Their cardioprotective effects against doxorubicin-induced toxicity in H9c2 cells were evaluated. All of the alkaloids showed cardioprotective effects in a nonmonotonic concentration-response manner, with the maximum protection rates ranging from 17.96 ± 2.93% to 98.31 ± 0.35%. Compound 5 exhibited the most potent cardioprotective activity. Taking the maximum protection rate as an indicator, the preliminary structure-activity relationship analysis indicated that the substitutions of C-1, C-13, C-15, C-16, and N and the configurations of OMe-6 and OH-15 are important structural features for the cardioprotective activities of the aminoalcohol-diterpenoid alkaloids.


Assuntos
Aconitum/química , Alcaloides/farmacologia , Cardiotônicos/farmacologia , Diterpenos/farmacologia , Alcaloides/isolamento & purificação , Cardiotônicos/isolamento & purificação , Linhagem Celular , China , Diterpenos/isolamento & purificação , Doxorrubicina/toxicidade , Medicamentos de Ervas Chinesas/farmacologia , Medicina Tradicional Chinesa , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Raízes de Plantas/química
5.
Molecules ; 24(22)2019 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-31739601

RESUMO

Fuzi is a well-known traditional Chinese medicine developed from the lateral roots of Aconitum carmichaelii Debx. It is rich in alkaloids that display a wide variety of bioactivities, and it has a strong cardiotoxicity and neurotoxicity. In order to discriminate the geographical origin and evaluate the quality of this medicine, a method based on high-performance liquid chromatography (HPLC) was developed for multicomponent quantification and chemical fingerprint analysis. The measured results of 32 batches of Fuzi from three different regions were evaluated by chemometric analysis, including similarity analysis (SA), hierarchical cluster analysis (HCA), principal component analysis (PCA), and linear discriminant analysis (LDA). The content of six representative alkaloids of Fuzi (benzoylmesaconine, benzoylhypaconine, benzoylaconine, mesaconitine, hypaconitine, and aconitine) were varied by geographical origin, and the content ratios of the benzoylmesaconine/mesaconitine and diester-type/monoester-type diterpenoid alkaloids may be potential traits for classifying the geographical origin of the medicine. In the HPLC fingerprint similarity analysis, the Fuzi from Jiangyou, Sichuan, was distinguished from the Fuzi from Butuo, Sichuan, and the Fuzi from Yunnan. Based on the HCA and PCA analyses of the content of the six representative alkaloids, all of the batches were classified into two categories, which were closely related to the plants' geographical origins. The Fuzi samples from Jiangyou were placed into one category, while the Fuzi samples from Butuo and Yunnan were put into another category. The LDA analysis provided an efficient and satisfactory prediction model for differentiating the Fuzi samples from the above-mentioned three geographical origins. Thus, the content of the six representative alkaloids and the fingerprint similarity values were useful markers for differentiating the geographical origin of the Fuzi samples.


Assuntos
Aconitum/química , Alcaloides/química , Raízes de Plantas/química , Cromatografia Líquida de Alta Pressão , Análise por Conglomerados , Análise Discriminante , Análise de Componente Principal
6.
Artigo em Chinês | MEDLINE | ID: mdl-19558855

RESUMO

OBJECTIVE: To investigate the correlation between thresholds in the chirp-ABR and behavior audiogram in order to find out if it is possible to be used as an clinical application of the chirp-ABR in estimating hearing sensitivity. METHODS: Twenty-two cases with hearing loss or normal hearing were enrolled in the study. The behavior audiogram and the response thresholds of chirp ABR (including chirp ABR, L-chirp ABR and U-chirp ABR) were obtained from 35 ears. RESULTS: Twenty-two cases were of both genders. The age was between 3.3- 6.5-years-old with the average age of 4.8-years-old. Divided by the degree of hearing loss, in the 35 ears, there were 6 with normal hearing, 2 with slightly hearing loss, 4 with moderate hearing loss, 10 with severe hearing loss and 13 with profound hearing loss. The Pearson correlation coefficients were 0.939, 0.900 and 0.930, respectively, which got from the data between the average of 0.5 - 4 kHz and chirp ABR respond threshold, 0.5 kHz and L-chirp ABR, and the average of 1 - 4 kHz and U-chirp ABR. CONCLUSION: As an objective test, the response threshold of chirp-ABR and the behavior audiogram were a highly correlated with each other, but more application in more subjects is needed.


Assuntos
Limiar Auditivo/fisiologia , Comportamento Infantil , Potenciais Evocados Auditivos do Tronco Encefálico/fisiologia , Testes Auditivos , Estimulação Acústica , Audiometria de Resposta Evocada , Criança , Pré-Escolar , Feminino , Humanos , Masculino
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