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1.
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 193-198, 2023.
Article in Chinese | WPRIM | ID: wpr-962641

ABSTRACT

Dioscoreae Rhizoma formula granules are made from decoction pieces by decocting, extracting, separating, concentrating, drying and granulating, which have the advantages of simple dispensing, convenient use and easy to take without decoction. However, because Dioscoreae Rhizoma is rich in starch and mucus components, its extract powder and formula granules are poorly soluble and difficult to dissolve or disperse completely within 5 min, and the insoluble material is difficult to dissolve completely even after 24 h in water, which affects the quality evaluation of the formula granules and medication psychology of patients. Therefore, by studying the dissolution process and mechanism of Dioscoreae Rhizoma extract and its formula granules, it was found that the special chemical composition of Dioscoreae Rhizoma, the denaturation of starch and its compounding with protein and other substances during the high temperature extraction process, and the contraction of coating membrane during the spray drying process were combined to form the special microstructure of coating membrane covering starch granules, and it is the root cause of poor solubility of Dioscoreae Rhizoma formula granules. Based on the research on the structure, property and function of the powder, this paper proposed a technical strategy to improve the solubility of Dioscoreae Rhizoma formula granules by powder modification process, and experimentally demonstrated that the modified Dioscoreae Rhizoma formula granules could completely dissolve within 2 min, which solved the technical problem and could provide reference for the improvement of solubility of other similar varieties, and promote the high-quality development of traditional Chinese medicine formula granule industry.

2.
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 185-192, 2023.
Article in Chinese | WPRIM | ID: wpr-962640

ABSTRACT

ObjectiveTo establish a rapid screening method for influenza virus neuraminidase(NA) inhibitors sourced from Chinese medicines based on fluorescence detection. MethodThe method was constructed based on the principle that after the reaction of the test sample and a certain amount of NA, the activity of some NA will be inhibited by the test sample, and the NA that is still active after the addition of the substrate can generate fluorescence at a specific wavelength when combined with the fluorescent substrate, and the inhibition rate of the test sample on NA was calculated according to the measured fluorescence intensity, so as to evaluate the in vitro inhibitory activity of the test sample on NA. A total of 49 high-purity chemical components from 12 Chinese medicines were used to evaluate the in vitro anti-NA activity by the established method. The theoretical calculated values of binding energy and inhibition constant after docking between the NA protein receptor and the test sample were used to prove the accuracy of the experimental results. The established method was applied to detect the in vitro NA inhibitory activity of different batches of Banlangen granules and Kangbingdu granules, so as to evaluate the quality consistency among different batches of samples. ResultThe methodological examination results showed that the method had good accuracy and repeatability. The screening results of 49 components showed that 22 of them had strong in vitro inhibitory activity against NA than peramivir [half inhibitory concentration(IC50) was 131.2 μmol·L-1], such as schaftoside, isoorientin, chebulinic acid, menthone and isoschaftoside. The inhibitory activity of the remaining 27 components was weaker than that of peramivir. The molecular docking results showed that the theoretical calculation results of binding energies and inhibition constants of most compounds were basically consistent with the experimental results. The test results of the inhibitory activity of 12 batches of Banlangen granules on NA showed that the quality consistency among samples A1, A2, B2, C1, C2, E2 and F2 was good. The analysis results of the inhibitory activity of 9 batches of Kangbingdu granules produced by the same manufacturer on NA showed that the inhibitory rates of samples K1 to K9 were 37.68%, 36.18%, 31.37%, 33.98%, 40.36%, 33.76%, 40.69%, 41.08%, 40.06% when the concentration of 0.02 g·mL-1, and the average inhibitory rate was 37.24%. ConclusionIn this paper, we successfully established an analytical method that can be used to rapidly evaluate whether Chinese medicines (derived from chemical components of traditional Chinese medicine or proprietary Chinese medicines) have in vitro anti-NA activity, which can be a powerful supplement to the existing screening methods for influenza virus NA inhibitors. And this method was used to screen 22 compounds from 12 Chinese medicines with good in vitro inhibitory activity against NA, which can provide candidate compounds for the development of anti-influenza small molecule drugs.

3.
Chinese Herbal Medicines ; (4): 360-368, 2023.
Article in English | WPRIM | ID: wpr-982508

ABSTRACT

Phyllanthi Fructus is a highly unique medicine and food homologous item, which exhibits distinctive flavor, notable nutritional value, and abundant pharmacological activity. It has enormous potential in the creation of health products and pharmaceuticals. However, due to the unique laws of quality formation and transfer of Phyllanthi Fructus, its appearance, shape, chemical compositions, nutrients, and sensory flavors are frequently greatly influenced by botanical resources, the processing and storage conditions. As a result, the current quality evaluation model is difficult to meet the needs of Phyllanthi Fructus as a medicine and food homologous item in the development of diversified products. This paper constructs the hierarchical utilization mode of Phyllanthi Fructus based on its unique quality formation and transmission laws, explores the quality evaluation model for food-oriented use and medicinal-oriented use, respectively, and systematically describes the quality evaluation idea under diversified application scenarios. This paper aims to serve as a reference for the construction of a quality evaluation model suitable for the medicine and food homologous item of Phyllanthi Fructus.

4.
Acta Pharmaceutica Sinica B ; (6): 1098-1116, 2021.
Article in English | WPRIM | ID: wpr-881187

ABSTRACT

Heart failure (HF) is a global public health problem with high morbidity and mortality. A large number of studies have shown that HF is caused by severe energy metabolism disorders, which result in an insufficient heart energy supply. This deficiency causes cardiac pump dysfunction and systemic energy metabolism failure, which determine the development of HF and recovery of heart. Current HF therapy acts by reducing heart rate and cardiac preload and afterload, treating the HF symptomatically or delaying development of the disease. Drugs aimed at cardiac energy metabolism have not yet been developed. In this review, we outline the main characteristics of cardiac energy metabolism in healthy hearts, changes in metabolism during HF, and related pathways and targets of energy metabolism. Finally, we discuss drugs that improve cardiac function

5.
Acta Pharmaceutica Sinica B ; (6): 209-217, 2018.
Article in English | WPRIM | ID: wpr-690918

ABSTRACT

Traditional Chinese herbs (TCH) are currently gaining attention in disease prevention and health care plans. However, their general bitter taste hinders their use. Despite the development of a variety of taste evaluation methods, it is still a major challenge to establish a quantitative detection technique that is objective, authentic and sensitive. Based on the two-bottle preference test (TBP), we proposed a novel quantitative strategy using a standardized animal test and a unified quantitative benchmark. To reduce the difference of results, the methodology of TBP was optimized. The relationship between the concentration of quinine and animal preference index (PI) was obtained. Then the PI of TCH was measured through TBP, and bitterness results were converted into a unified numerical system using the relationship of concentration and PI. To verify the authenticity and sensitivity of quantified results, human sensory testing and electronic tongue testing were applied. The quantified results showed a good discrimination ability. For example, the bitterness of Coptidis Rhizoma was equal to 0.0579 mg/mL quinine, and Nelumbinis Folium was equal to 0.0001 mg/mL. The validation results proved that the new assessment method for TCH was objective and reliable. In conclusion, this study provides an option for the quantification of bitterness and the evaluation of taste masking effects.

6.
Acta Pharmaceutica Sinica ; (12): 116-21, 2016.
Article in Chinese | WPRIM | ID: wpr-505100

ABSTRACT

Decoction is one of the most commonly used dosage forms of traditional Chinese medicine. The stability of chemical constituents in decoction is closely related to the clinical efficacy and safety. There were few reports about the influence of metal ions in the stability of chemical constituents in traditional Chinese medicine. However, there is no evidence that metal ions in decoction water need to be controlled. In this study, 2,3,5,4'-tetrahydroxy stilbene-2-O-β-D-glucoside (THSG), one of the main constituents in Polygoni Multiflori Radix was studied. Ordinary tap water, deionized water, and water containing different metal ions were used to investigate and compare the influence on THSG. The results showed that after storage in a dark place at the room temperature for 10 days, the degradation of THSG was 7% in deionized water, while undetectable in tap water. The content of THSG could be decreased by different kinds of metal ions, and the effect was concentration-dependent. Moreover, Fe3+ and Fe2+ showed the greatest influence at the same concentration; and our study has shown that THSG decreased more than 98% in Fe and Fe2+ solutions at 500 ppm concentration. In the same time we found out p-hydroxybenzaldehyde (molecular weight: 122.036 7) and 2,3,5-trihydroxybenzaldehyde-2-O-glycoside (molecular weight: 316.079 4) were the main degradation products of THSG in tap water and water containing Cu2+, Ca2+, Zn2+, Mg2+ and Al3+. The product of THSG dimer with a water molecule was found in water containing Fe3+ and Fe2+. The above results showed that the metal ions in water could significantly influence the stability of THSG in water, indicating that the clinical efficacy and safety of decoction would be affected if the metal ions in water were not under control. It's suggested that deionized water should be used in the preparation of decoction containing Polygoni Multiflori Radix in the clinic to avoid degradation of THSG. Meanwhile, decoction prepared by tap water should be taken by patients in a short time. Our investigation provides important information and reference about the influence of metal ions on the stability of decoctions in other traditional Chinese medicine that have unstable groups such as hydroxyls and unsaturated bonds, etc.

7.
Acta Pharmaceutica Sinica ; (12): 1148-55, 2013.
Article in Chinese | WPRIM | ID: wpr-445580

ABSTRACT

The hydrophilicity of the normal decoction pieces (NDP) of Indigo Naturalis is not good, therefore, it is not suit for decoctions. In this paper, powder modification technology is used and some NDP and alcohol are ground together in the vibromill to prepare the hydrophilic decoction pieces (HDP) of Indigo Naturalis. Initially, the properties of NDP, ultrafine decoction pieces (UDP) and HDP are compared, the hydrophilicity of UDP was promoted slightly, that of HDP is promoted dramatically. Then, three batches of Indigo Naturalis are prepared to HDP separately, but there is no obvious difference in the contact angle. Furthermore, the size distribution, surface area and micro-shape of HDP are bigger than that of UDP and smaller than NDP. The contents of indigo and indirubin in three decoction pieces are the same, as well as the species of inorganic substance, although there is a little difference in the proportion of five inorganic substances. The fact suggests the change of physical state and the qualitative and quantitative change of organism and inorganic substances are not the main factors to influence the hydrophilicity. In addition, hydroxyl, methylene and methyl can be identified at the wavenumber of 3 356 cm(-1) and 1 461 cm(-1) in infrared spectrum; the content of alcohol in HDP is 0.67% measured by gas chromatogram. The stability of HDP in the heating condition is studied, the fact suggests the hydrophilic effect of HDP at 40 degrees C is relatively stable. All above research suggests that the alcohol is the main factor to influence the hydrophilicity and maybe the intermolecular force which fixed alcohol molecule on the surface of Indigo Naturalis is the basic principle to produce the hydrophilicity.

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