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1.
Zhongguo Zhong Yao Za Zhi ; 48(22): 6058-6065, 2023 Nov.
Article in Chinese | MEDLINE | ID: mdl-38114212

ABSTRACT

The poor solubility of insoluble components of traditional Chinese medicine(TCM) is an important factor restricting the development of its preparations. Natural polysaccharides of TCM can be used as functional components to increase the solubility of insoluble components. Epimedium flavonoid secondary glycoside components(EFSGC) have been shown to have positive effects on the prevention and treatment of osteoporosis, but they exhibit poor solubility. Therefore, the strategy of solubilizing EFSGC with TCM polysaccharides was adopted, and its effect on the permeability and stability of EFSGC was evaluated in this study. Based on the equilibrium solubility experiment of EFSGC, it was found that Panax notoginseng crude polysaccharide(PNCP) had the best solubilization effect on EFSGC among the ten kinds of TCM polysaccharides, which increased the solubility of EFSGC from 0.8 mg·mL~(-1) to 13.3 mg·mL~(-1). It should be noted that after the solubilization of EFSGC by preparation technology, the effects on permeability and stability should be considered. Therefore, this study also investigated these two properties. The results showed that PNCP increased the effective transmittance of EFSGC from 50.5% to 71.1%, which could increase the permeability of EFSGC significantly. At the same time, it could improve the stability of EFSGC in the simulated gastric juice environment. In order to explain the solubilization mechanism of PNCP on EGSGC, critical micelle concentration, particle size, potential, differential scanning calorimetry, and infrared spectroscopy were analyzed. It was preliminarily inferred that the mechanism was as follows: PNCP and EFSGC could self-assemble into aggregates for solubilization by intermolecular hydrogen bonding interaction in water. In summary, PNCP can not only improve the solubility of EFSGC but also improve its permeability and stability. This study lays the foundation for the application of TCM polysaccharides as a functional component to solubilize insoluble components.


Subject(s)
Cardiac Glycosides , Epimedium , Medicine, Chinese Traditional , Flavonoids/chemistry , Glycosides , Epimedium/chemistry , Solubility , Polysaccharides/chemistry
2.
Zhongguo Zhong Yao Za Zhi ; 48(1): 30-38, 2023 Jan.
Article in Chinese | MEDLINE | ID: mdl-36725255

ABSTRACT

Rare and endangered Chinese medicinal materials are the material basis for innovation and development of Chinese medicinal materials and their curative effects are remarkable. However, the resources are in shortage due to various man-made or natural factors such as rising demand, overexploitation and environmental degradation. Therefore, finding alternatives is a feasible and effective solution. This study systematically sorted out the list of rare and endangered Chinese medicinal materials, and combed relevant policies and regulations. According to existing research, the substitution model of rare and endangered Chinese medicinal materials was constructed from the theoretical level. In view of the slow search for substitutes, the failure to follow the basic theory of traditional Chinese medicine in the process of research and development, the difficulty in breaking through technologies and the incomplete guarantee of the clinical efficacy of substitutes, a multi-component replacement was proposed to replace the originals with more effective components from a wide range of sources. This study was expected to promote the study on the substitutes of rare and endangered Chinese medicinal materials to step into a new stage.


Subject(s)
Drugs, Chinese Herbal , Plants, Medicinal , Humans , Drugs, Chinese Herbal/therapeutic use , Research Design , Medicine, Chinese Traditional , Technology
3.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5689-5699, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471987

ABSTRACT

Pediatric medication in China is characterized by a lack of child-specific drugs and insufficient types, specifications, dosage forms, and delivery devices. In recent years, new dosage forms with good compliance, such as inhalation preparation, rectal delivery system, and transdermal delivery system, have attracted more attention in pediatric medication. Because of the physiological characteristics of delicate viscera, difference in swallowing ability and psychological characteristics of fear of pain and aversion to bitter taste, it is particularly important to select suitable drug delivery route and drug delivery device according to children's physiological characteristics. With the help of the special drug delivery devices, traditional Chinese medicine and innovative Chinese medicine can be administered according to the expected design path, and drug delivery devices can ensure the accurate dose and improve the complia-nce to achieve the purpose of effective and safe drug delivery. It is also a way to realize the re-innovation of traditional Chinese medicine. The present study summarized the research progress in drug delivery devices for common drug delivery routes and new drug deli-very routes, put forward the innovative design idea of children's drug delivery devices according to the special needs of children, poin-ted out the compatibility of drug delivery devices and other problems in the current development, and prospected the application of intelligent information technology and additive manufacturing technology in drug delivery device innovation. This is expected to provide references for the development of innovative drugs and drug delivery devices suitable for children's multidimensional demand for medication.


Subject(s)
Drug Delivery Systems , Medicine, Chinese Traditional , Child , Humans , Pharmaceutical Preparations , China
4.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5681-5688, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471986

ABSTRACT

This study took the 2020 edition of Chinese Pharmacopoeia(ChP) and the 2018 edition of National Essential Drug List(NEDL) for children as research carriers to systematically analyze the current situation of and problems in the use of Chinese patent medicine for children(CPMC) in China. In view of the problems of imprecise dosage, incomplete safety information, and lack of sui-table varieties, dosage form and specification of CPMC in China, development strategy of CPMC in the future was proposed. It is reco-mmended to carry out systematic post-marketing revaluation studies of CPMC, encourage the development of new varieties or new dosa-ge forms suitable for children, advocate the continuous promotion of real-world studies on children, and expand the information on the use of CPMC with real-world data, so as to lay the foundation for post-marketing revaluation of CPMC and guide the rational use of clini-cal medicines. This study was expected to build a positive policy ecosystem to ensure the supply of CPMC, and promote the high-quality development of CPMC.


Subject(s)
Drugs, Chinese Herbal , Drugs, Essential , Child , Humans , Nonprescription Drugs , Medicine, Chinese Traditional , Ecosystem , China
5.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5700-5707, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471988

ABSTRACT

Under the background of the "14th Five-Year Plan" industry development, the pharmaceutical industry has ushered in a critical period of strategic transformation. Pharmaceutical excipients are a major categoryin drugs in addition tomedicinal substances, and the research and development of industrial technologies and innovative products play a decisive role in the development of high-quality drugs. The special drug for children is the focus ofthe pharmaceutical industry in the new era, and the application of standar-dized excipients is a key step indistinguishingbetween adult drugs and special drugs for children. In the context of the policy background in China, this paper reviewed the status quo of excipient industry, technical bottlenecks, application problems of pediatric excipients, and their development hotspots, interpreted the strategic layout of excipient innovation research and development suitable for pediatric preparations, and put forward prospects for their future development technicalroutes to lay a solid foundation for the industry transformation.


Subject(s)
Drug Industry , Excipients , Humans , Child , China , Pharmaceutical Preparations
6.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5708-5716, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471989

ABSTRACT

There are many kinds of pharmaceutical preparations for children in China, which are generally divided into oral solid preparations and oral liquid preparations. Solid preparations, such as microtablets, pellets, dispersible tablets, and fine granules, have become the development trend of pediatric drugs. Liquid preparations mainly include syrup, suspension, oral solution, and drops. The poor taste and the treatment of drugs in children of different ages are the key factors affecting the efficacy, safety, and compliance of pediatric drugs. To reduce the risk caused by the fluctuation of blood concentration and improve the oral compliance of pediatric drugs, it is urgent to develop new techniques for granulation and flavor maskingto improve the poor taste of solid preparations. For liquid pre-parations with poor taste, the flavor correction technique should be used. This paper summarized the new pharmaceutical techniques for granulation and flavor masking, and it was found that sustained/controlled-releasegranules, fine granules, and chewing solid mini-tablets became the mainstream of oral solid preparations for children. Generally, multiparticle preparation, coating, microencapsulation, and other granulating techniques were involved in these preparations. Granulation and flavor masking are closely related and synergetic. Flavor masking techniques mask the bitter taste of Chinese medicine from four aspects, including confusing the brain taste, changing the compounds, reducing the exposure of bitter molecules to bitter receptors in the mouth, and numbing the taste cells to increase the threshold of bitter perception. At present, the main drugs for children on the market mainly inhibit the oral release of bitter drugs.


Subject(s)
Chemistry, Pharmaceutical , Taste , Child , Humans , Chemistry, Pharmaceutical/methods , Administration, Oral , Tablets , China
7.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5717-5734, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471990

ABSTRACT

This study aimed to forecast the main active components of Xiaoer Chiqiao Qingre Granules(XECQ) in the treatment of children with acute upper respiratory tract infection by UPLC-MS, network pharmacology, molecular docking and cell biology, and explore the mechanism of action, so as to provide certain reference for the research on its pharmacodynamics substances and mechanism of action. The main chemical components of XECQ were comprehensively analyzed by UPLC-Q-TOF-MS combined with UNIFI platform. According to the MS1 and MS2 data of XECQ, comparison and identification were carried out in combination with reference substances and reference articles. On this basis, the chemical components of XECQ were targeted and enriched by network pharmacology, to screen the main pharmacodynamic substances of XECQ in the treatment of acute upper respiratory tract infection in children and discuss the mechanism of action. In addition, the binding degree of core targets and main active components was verified by molecular docking. The results revealed that 202 compounds were identified from XECQ, among which 22 were the main active components, including obovatol, dihydroartemisinin, and longikaurin A. Enrichment analysis of the key target pathways showed that XECQ played its role in the treatment of children with acute upper respiratory tract infection mainly by regulating PI3K/Akt signaling pathway and MAPK signaling pathway. In the experimental verification by Western Blot(WB), it was found that XECQ significantly inhibited the expression of PI3K and Akt, which was consistent with the prediction results of network pharmacology. In conclusion, the potential pharmacodynamic substances of XECQ were obovatol, dihydroartemisinin, longikaurin A and other 19 active components. It treated children with acute upper respiratory tract infection by regulating the PI3K/Akt signaling pathway.


Subject(s)
Artemisinins , Drugs, Chinese Herbal , Respiratory Tract Infections , Child , Humans , Chromatography, Liquid , Molecular Docking Simulation , Phosphatidylinositol 3-Kinases/genetics , Proto-Oncogene Proteins c-akt , Tandem Mass Spectrometry , Respiratory Tract Infections/drug therapy , Drugs, Chinese Herbal/pharmacology
8.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5735-5745, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471991

ABSTRACT

This study aimed to elucidate the digestive characteristics of flavonoid components in Xiaoer Chiqiao Qingre Granules(XECQ) in the gastrointestinal environment of infants. An in vitro model was established to simulate the gastric and intestinal environment of infants. UPLC was used to analyze the content change of flavonoid components in XECQ, and their overall content was integrated through the mass fraction weight coefficient method. UPLC-Q-TOF-MS was employed to determine the digestive products of flavonoid components in gastrointestinal fluids and their metabolic pathways. The results showed that in the process of digestion, 11 digestion products were generated by oxidation, reduction, deglycosylation, methylation and other phase Ⅰ metabolism. From flavonoid content and component changes, it was found that the flavonoid components in XECQ were relatively stable in the gastric fluid, while their content in the intestinal fluid was first increased and then maintained stable. This was mainly because flavonoid components were released from proteins, polysaccharides and other macromolecular substances during gastrointestinal digestion. In addition, phase Ⅰ metabolism occurred, but with relatively low metabolic rate, resulting in their stable content. This study preliminarily explored the digestive characteristics of flavonoid components in XECQ in the infant gastrointestinal environment, which laid a foundation for further studying the absorption, transport and metabolism of pharmacodynamics components in XECQ, and facilitated the study of the biopharmaceutical pro-perties of pediatric Chinese medicine.


Subject(s)
Drugs, Chinese Herbal , Flavonoids , Infant , Humans , Child , Flavonoids/metabolism , Gastrointestinal Tract , Intestines , Drugs, Chinese Herbal/metabolism , Chromatography, High Pressure Liquid
9.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5746-5756, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471992

ABSTRACT

According to the taste analysis of Pudilan Xiaoyan Oral Liquid, the unpleasant taste of the oral liquid is mainly caused by the inherent taste of Chinese medicine and the taste introduced in the preparation process, which leads to its unpopularity among children. Therefore, aiming at the special children patient group, Xiaoer Pudilan Xiaoyan Syrup was developed via technology optimization and dosage form improvement to improve the unpleasant taste and enhance the medication compliance among children. Based on the material properties of Pudilan Xiaoyan Oral Liquid and Xiaoer Pudilan Xiaoyan Syrup extracts, the authors compared the properties(pH, density, turbidity, viscosity, chromaticity, particle size), taste, content of five quality markers and in vivo pharmacokinetic characteristics of these two preparations, to evaluate the suitability of Xiaoer Pudilan Xiaoyan Syrup. The results showed that compared with those of Pudilan Xiaoyan Oral Liquid, the pH, density, turbidity, viscosity and chromaticity of Xiaoer Pudilan Xiaoyan Syrup were significantly changed, and the unpleasant taste was reduced by 26%; the transfer rate of the main active ingredients chicoric acid was increased, while the transfer rate of baicalin had small difference from that of the oral liquid. In addition, pharmacokinetics revealed that the total absorption amount of baicalin in vivo was higher, and the time to peak T_(max) of baicalin and oroxindin in the syrup and the mean residence time MRT_(last )of corynoline in vivo were significantly prolonged. The absorption degree of Xiaoer Pudilan Xiaoyan Syrup and Pudilan Xiaoyan Oral Liquid in the body was the same: baicalin>oroxindin>corynoline. The new dosage form process was simpler than that of the original dosage form, safe, environmentally friendly, reasonable and feasible, meeting the mass production demand. This provided a basis for the reasonable and scientific optimization of Xiaoer Pudilan Xiaoyan Syrup, and also laid a foundation for its further safe and rational use, so as to expand the clinical application in children.


Subject(s)
Drugs, Chinese Herbal , Child , Humans , Glucuronates
10.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5757-5764, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471993

ABSTRACT

Taking Pudilan Xiaoyan Oral Liquid as a demonstration, the effective delivery of quality markers in alcohol precipitation of Chinese medicine oral liquid preparations was studied. With the transfer rates of adenosine, corynoline, cichoric acid, baicalin, and wogonin as evaluation indexes, the effect of the density of concentrate before alcoholic precipitation, volume fraction of ethanol, stirring speed, temperature of concentrated solution, stirring time, alcohol concentration, alcohol precipitation time, alcoholic precipitation temperature, alcohol addition rate, and the pH of concentrate on the alcohol precipitation process was investigated by Plackett-Burman trial design, thus obtaining the key factors that influenced the alcohol precipitation process. The key factors were further optimized by Box-Behnken design to determine the optimal alcohol precipitation conditions. When the density of concentrate before alcoholic precipitation was 1.12 g·mL~(-1), the pH of concentrate was 6.86, and the alcohol concentration was 50.00%, the transfer rates of baicalin and wogonin were 91.86% and 87.78%, respectively. When the density of concentrate before alcoholic precipitation was 1.13 g·mL~(-1), the concentration of alcohol was 74.50%, and the alcoholic precipitation temperature was 17.0 ℃, the transfer rates of adenosine, corynoline, and cichoric acid were 85.95%, 71.62% and 83.19%, respectively. The method of optimizing alcohol precipitation techniques and determining the parameters of Pudilan Xiaoyan Oral Liquid by response surface methodology is reasonable and feasible, which provides guidance and experience for the effective delivery of quality markers in Chinese medicine oral liquid preparations.


Subject(s)
Drugs, Chinese Herbal , Ethanol , Adenosine , Chemical Precipitation
11.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5765-5774, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471994

ABSTRACT

Mineral medicine is a characteristic element of advantage of traditional Chinese medicine(TCM), which embodies unique scientific connotation. Cinnabaris is a characteristic drug in Chinese medicinal preparations, especially in Chinese medicinal pediatric preparations. Because of the adverse reactions caused by mercury contained, the safety and application of Cinnabaris have attracted much attention. To explore the application regularity and the value of the pediatric preparations containing Cinnabaris, this study statistically analyzed 32 Cinnabaris-contained pediatric preparations in the 2020 edition of the Chinese Pharmacopoeia and 105 pediatric preparations containing Cinnabaris in the Dictionary of Traditional Chinese Medicine Prescriptions(Vol. Ⅰ and Ⅱ). The statistical results indicated that the pediatric preparations and formulae containing Cinnabaris had great advantages in the treatment of pediatric convulsions, but there were still problems in dosage form, dosage, and quality control. In this study, ICP-MS and LC-AFS were further used to determine the content of total mercury and soluble mercury in 15 commercially available pediatric preparations containing Cinnabaris. It was found that the total mercury content was far higher than soluble mercury content in the sample preparations, and there was no obvious correlation between them. According to the results, the research and application strategies of Cinnabaris were put forward in order to provide references for the rational application of Cinnabaris in pediatric preparations.


Subject(s)
Drugs, Chinese Herbal , Mercury , Humans , Child , Medicine, Chinese Traditional , Minerals , Quality Control
12.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5775-5788, 2022 Nov.
Article in Chinese | MEDLINE | ID: mdl-36471995

ABSTRACT

To clarify the metabolic transformation mechanism of phenylethanoid glycosides in Xiaoer Chiqiao Qingre Granules in vivo, this study extracted and separated the phenylethanoid glycosides in Xiaoer Chiqiao Qingre Granules. Based on UPLC-Q-TOF-MS/MS technology, the retention time and primary and secondary mass spectrometry information were analyzed by UNIFI software, and 11 phenylethanoid glycosides in Xiaoer Chiqiao Qingre Granules were preliminarily identified. Sixty-nine metabolites related to phenylethanoid glycosides were identified from the plasma samples of juvenile rats after administration of Xiaoer Chiqiao Qingre Granules. In addition, this study simulated the transformation system of intestinal flora in children, and discussed the metabolic effects of intestinal flora on the representative components forsythoside A, forsythoside E, and salidroside of phenylethanoid glycosides. The model of gastrointestinal heat retention in children with food accumulation was established to study the differential metabolites of phenylethanoid glycosides. Through the comparative analysis of the representative components absorbed in blood and the intestinal floral transformation products, it was found that the main metabolic pathways of phenylethanoid glycosides were dehydrogenation, oxidation, acetylation, sulfation, and glucuronidation. The findings of this study revealed the transformation law of phenylethanoid glycosides in the gastrointestinal tract. Through the preliminary discussion of the pharmacological mechanism, this study provides references for further clarifying the pharmacodynamic material basis of Xiaoer Chiqiao Qingre Granules and exploring the pediatric Chinese medicine compound.


Subject(s)
Drugs, Chinese Herbal , Gastrointestinal Microbiome , Rats , Animals , Tandem Mass Spectrometry/methods , Chromatography, High Pressure Liquid/methods , Glycosides/analysis , Drugs, Chinese Herbal/chemistry
13.
Zhongguo Zhong Yao Za Zhi ; 47(16): 4358-4364, 2022 Aug.
Article in Chinese | MEDLINE | ID: mdl-36046862

ABSTRACT

Epimedii Folium possesses many pharmacological activities including immunomodulation, anti-oxidation, and anti-tumor. Polysaccharides are the main components of Epimedii Folium, and their activities are closely related to the structure. The present study isolated a neutral polysaccharide(EPS-1-1) and an acidic polysaccharide(EPS-2-1) from the aqueous extract of Epimedii Folium through DEAE-52 cellulose anion-exchange chromatography and Sephadex G-100. The structures were characterized by chemical composition analysis, high-performance gel permeation chromatography(HPGPC), Fourier-transform infrared spectrometry(FT-IR), 1-phenyl-3-methyl-5-pyrazolone(PMP) derivatization, scanning electron microscopy(SEM), Congo red test, etc. The immunomodulatory activity of polysaccharides in vitro was determined by investigating the effects on the maturation of bone marrow-derived dendritic cells(BMDCs) and the release of inflammatory cytokines. According to the structural characterization analysis, EPS-1-1 was composed of fructose(Fuc), mannose(Man), ribose(Rib), rhamnose(Rha), glucose(Glc), galactose(Gal), xylose(Xyl), and arabinose(Ara) at 1.90∶0.67∶0.05∶0.08∶3.29∶1.51∶0.05∶0.37(molar ratio), while EPS-2-1 was mainly composed of Fuc, Man, Rha, glucuronic acid(GlcA), galacturonic acid(GalA), Glc, Gal, Xyl, and Ara at 5.25∶0.18∶0.32∶0.13∶1.14∶0.16∶0.55∶0.08∶0.2. EPS-1-1 and EPS-2-1 could promote the maturation and function of BMDCs through up-regulating the expression of MHC-Ⅱ, CD86, CD80, and CD40, and increasing the levels of inflammatory cytokines(IL-6, IL-12, and TNF-α) in vitro experiments, which suggested that EPS-1-1 and EPS-2-1 possessed good immunomodulatory activity.


Subject(s)
Cytokines , Polysaccharides , Cytokines/metabolism , Drugs, Chinese Herbal , Gas Chromatography-Mass Spectrometry , Humans , Immunomodulation , Polysaccharides/chemistry , Spectroscopy, Fourier Transform Infrared
14.
Zhongguo Zhong Yao Za Zhi ; 47(16): 4446-4453, 2022 Aug.
Article in Chinese | MEDLINE | ID: mdl-36046874

ABSTRACT

In this study, the secondary osteoporosis model was induced by oral administration of retinoic acid for two weeks in SD male rats. The efficacy and mechanism of LG on secondary osteoporosis in rats were explored through the bone morphogenetic protein 2(BMP-2)/Runt-related transcription factor 2(Runx2)/Osterix signaling pathway. With Xianling Gubao Capsules(XLGB) as the positive control, three dose groups of low glycoside from Epimedii Folium flavonoids(LG), i.e., low-dose group(LG-L), medium-dose group(LG-M), and high-dose group(LG-H), were set up. After modeling, the rats in each group were treated correspondingly by gavage for eight weeks. The action target of LG in the treatment of secondary osteoporosis in rats was analyzed by measuring the body weight and the organ indexes of rats including heart index and testis index. The efficacy of LG was characterized by the pathological changes of the femur, the microstructural parameters of the trabecular bone, and the biomechanical properties of femoral tissues in rats. The mechanism of LG was explored by measuring the relevant biochemical indexes and the changes in BMP-2, Runx2, and Osterix content in rats with secondary osteoporosis. The results showed that the action target of LG in the treatment of secondary osteoporosis in rats was the testis. LG can improve the bone loss of the femur, increase the number and thickness of the trabecular bone, reduce the porosity and separation of the trabecular bone, potentiate the resistance of bone to deformation and destruction, up-regulate the serum content of Ca, P, aminoterminal propeptide of type Ⅰ procollagen(PINP), and osteocalcin(OC), promote bone matrix calcification and the expression of BMP-2, Runx2, and Osterix proteins, and accelerate bone formation, thereby reducing the risk of fractures, and ultimately exerting anti-secondary osteoporosis efficacy.


Subject(s)
Core Binding Factor Alpha 1 Subunit , Osteoporosis , Animals , Bone Density , Core Binding Factor Alpha 1 Subunit/genetics , Core Binding Factor Alpha 1 Subunit/metabolism , Drugs, Chinese Herbal , Flavonoids/therapeutic use , Glycosides/therapeutic use , Male , Osteoporosis/chemically induced , Osteoporosis/drug therapy , Osteoporosis/metabolism , Rats , Rats, Sprague-Dawley , Tretinoin/adverse effects
15.
Zhongguo Zhong Yao Za Zhi ; 47(14): 3773-3780, 2022 Jul.
Article in Chinese | MEDLINE | ID: mdl-35850834

ABSTRACT

In this study, the microwave-assisted method was used to synthesize seleno-polysaccharides from Lonicerae Japonicae Flos, and the optimal process conditions were optimized.Meanwhile, the immunological activity of seleno-polysaccharides from Lonicerae Japonicae Flos was investigated.The results showed that under the conditions of nitric acid concentration of 0.512%, reaction temperature of 70.0 ℃, microwave power of 600 W, reaction time of 44.0 min, and m(Na_2SeO_3)∶m(polysaccharides)=1.0, the selenium content of Lonicerae Japonicae Flos seleno-polysaccharides was 3.89 mg·g~(-1).The results of in vitro immunoassay showed that polysaccharides and seleno-polysaccharides from Lonicerae Japonicae Flos could promote the proliferation of mouse RAW264.7 macrophages as compared with the conditions in the normal group.Compared with Lonicerae Japonicae Flos polysaccharides, Lonicerae Japonicae Flos seleno-polysaccharides could significantly facilitate the proliferation of mouse RAW264.7 macrophages and promote the production of IL-1ß and TNF-α at the concentration of 20-160 µg·mL~(-1).This study provided references for broadening the application of polysaccharides from Lonicerae Japonicae Flos.


Subject(s)
Drugs, Chinese Herbal , Lonicera , Animals , Chromatography, High Pressure Liquid , Mice , Microwaves , Polysaccharides/pharmacology , Quality Control
16.
Zhongguo Zhong Yao Za Zhi ; 47(12): 3166-3174, 2022 Jun.
Article in Chinese | MEDLINE | ID: mdl-35851108

ABSTRACT

Modern liquid forms of Chinese medicine(CM), such as oral liquid, are similar to traditional decoction, but there are deficiencies in the selection and design of the dosage form, and the solubility of the pre-preparation material is critical. The property system for Chinese medicinal materials(CMMs) was established according to the previous research. The present study established the dosage form design strategy of oral liquid preparations of CM with the solubility as the core, and pointed out the relationship between the saturated volume of component(V_(i-n)) and daily dosage of preparation(V_d) was the key to the dosage form design. To be specific, the prescription can be designed into liquid preparation directly when V_(i-n)≤V_d, while V_(i-n)>V_d, the suitable solubilization technologies are needed. At present, the available solubilization technologies include the addition of excipients such as solubilizers/cosolvents, pH adjustment of the solution, and synergistic solubilization of intermediates and components for the preparation of pharmaceuticals. As reported, the polysaccharides of CM have shown great potential in the solubilization of insoluble components of CM, and they have certain prospects as a new solubilizing excipient.


Subject(s)
Drugs, Chinese Herbal , China , Drugs, Chinese Herbal/chemistry , Excipients , Medicine, Chinese Traditional , Solubility , Technology
17.
Zhongguo Zhong Yao Za Zhi ; 47(12): 3215-3223, 2022 Jun.
Article in Chinese | MEDLINE | ID: mdl-35851114

ABSTRACT

Advanced glycation end products(AGEs) can lead to many diseases such as diabetes and its complications. In this study, an in vitro non-enzymatic glycosylation reaction model-bovine serum albumin/methylglyoxal(BSA/MGO) reaction system was constructed and incubated with Cortex Moutan extract. High performance liquid chromatography(HPLC) and ultra-high performance liquid chromatography with quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS/MS) were used to detect and identify the active components that inhibited the formation of AGEs in the co-incubation solution of Cortex Moutan extract and MGO, and differential components such as salvianan, paeoniside, benzoylpaeoniflorin, mudanpioside J, galloyloxypaeoniflorin, benzoyloxy-paeoniflorin, 5-hydroxy-3 s-hydroxymethyl-6-methyl-2,3-dihydro benzofuran, and galloylpaeoniflorin were screened out, which were inferred to be the potential active components of Cortex Moutan extract to capture MGO. In addition, BSA-glucose reaction system was performed to investigate the influence of different concentrations of Cortex Moutan extract(decoction concentrations: 40, 80, 120, 160, and 200 mg·mL~(-1)) on inhibiting the production of AGEs in vitro. The inhibitory effects of Cortex Moutan extract and the differential components galloylpaeoniflorin and benzoyl paeoniflorin on the production of AGEs in human umbilical vein endothelial cells(HUVECs) induced by high glucose was further evaluated. Cell apoptosis was observed by acridine orange and ethidium bromide(AO/EB) double fluorescence staining. The results showed that Cortex Moutan Cortex extract and its differential components had certain inhibitory effects on the formation of AGEs, and could reduce cell apoptosis. This study provided reference for the treatment of diabetic vascular complications by Cortex Moutan inhibiting the toxic AGEs.


Subject(s)
Drugs, Chinese Herbal , Tandem Mass Spectrometry , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacology , Glucose , Glycation End Products, Advanced , Human Umbilical Vein Endothelial Cells , Humans , Magnesium Oxide
18.
Zhongguo Zhong Yao Za Zhi ; 47(11): 2938-2946, 2022 Jun.
Article in Chinese | MEDLINE | ID: mdl-35718515

ABSTRACT

The present study explored the optimum synthesis process of Rehmannia glutinosa seleno-polysaccharides with acetic acid as a catalyst, characterized the structure of R. glutinosa seleno-polysaccharides by Fourier transform infrared spectroscopy(FT-IR), scanning electron microscopy(SEM), thermogravimetry(TG), and atomic force microscopy(AFM), and preliminarily investigated the immunological activity of R. glutinosa seleno-polysaccharides. The results showed that the optimal conditions for the synthesis of R. glutinosa seleno-polysaccharides included m(acetic acid)∶m(R. glutinosa polysaccharides)=0.80, m(Na_2SeO_3)∶m(R. glutinosa polysaccharides)=1.25, reaction temperature of 80.0 ℃, and reaction time of 7.0 h. Under these conditions, the selenium content of R. glutinosa seleno-polysaccharides was 2.239 mg·g~(-1). The acetic acid catalysis method was milder than the nitric acid method, without affecting the structure of polysaccharides. The results of IR, SEM, TG, and AFM showed that R. glutinosa seleno-polysaccharides were properly prepared. The results of immunological activity showed that compared with the control group, R. glutinosa seleno-polysaccharides could significantly promote the phagocytic capacity of mouse monocyte macrophages and improve the spleen index and thymus index of mice. In the concentration range of 15-240 µg·mL~(-1), the proliferation of spleen lymphocytes of mice was strengthened, and the IL-2 and IFN-γ secretion by Th1 cytokines was promoted. This study can provide references for the further development and application of R. glutinosa polysaccharides.


Subject(s)
Rehmannia , Animals , Cytokines , Mice , Polysaccharides/chemistry , Polysaccharides/pharmacology , Rehmannia/chemistry , Spectroscopy, Fourier Transform Infrared , Spleen
19.
Zhongguo Zhong Yao Za Zhi ; 47(5): 1153-1160, 2022 Mar.
Article in Chinese | MEDLINE | ID: mdl-35343139

ABSTRACT

Chinese medicine undergoes complex chemical changes during processing and identifying these changes is the key to the processing mechanism. In the past 20 years of the 21 st century, research on the chemical changes in Chinese medicine after processing has focused the changes in the biopharmaceutical process in addition to the variation during processing. With the surging of information technologies, various identification technologies(instrumental analysis techniques, molecular biological techniques, data mining techniques, and biotransformation techniques) have developed rapidly and been widely applied to the research on processing mechanism. Thus, based on the chemical changes in the processing and biopharmaceutical process, the author suggested a research tactic of multimodal identification as the core by reorganizing key technologies for chemical identification from studies of the processing mechanism of Chinese me-dicine, aiming at establishing an interdisciplinary multi-dimensional research model for the processing mechanism of Chinese medicine.


Subject(s)
Drugs, Chinese Herbal , Medicine, Chinese Traditional , Drugs, Chinese Herbal/chemistry , Technology
20.
Zhongguo Zhong Yao Za Zhi ; 47(5): 1161-1169, 2022 Mar.
Article in Chinese | MEDLINE | ID: mdl-35343140

ABSTRACT

The research on the processing mechanism of Chinese medicine is the key and core foundation to improve processing technologies of Chinese medicine, formulate the quality standards of Chinese medicinal pieces, enhance the clinical efficacy of Chinese medicine, enrich Chinese medicine processing theories, and promote the development of Chinese medicine processing. Many researc-hers have conducted in-depth exploration on the processing mechanism of Chinese medicine in the 20 years in the 21 st century. Significant progress has been made in the transformation of chemical components during the processing, the change of active components in the body, the law of toxicity attenuation in the processing of toxic Chinese medicine, the mechanism of efficacy enhancement and toxicity attenuation of processing with auxiliary materials, and the application of new biomedical technologies. At present, the processing mechanism of multiple Chinese medicines has been preliminarily clarified, which has greatly promoted the development of Chinese me-dicine processing. The development of the processing mechanism of Chinese medicine reveals that the in vitro transformation of chemical components is combined with the in vivo absorption, transport, and metabolism, and the macroscopic biological effects of the organism are combined with the cells, molecules, targets, and pathways in the study of the processing mechanism of Chinese medicine. More attention has been paid to exploring the processing mechanism from the overall level, and a modern systematic research system on the processing mechanism of Chinese medicine has been initially formed. To further promote the scientific development of Chinese me-dicine processing, the present study proposed that the research on the processing mechanism of Chinese medicine should take Chinese medicine properties into account, focus on the influence of disease condition on the mode of action and effect strength of the drugs, comply with the characteristics of clinical compound compatibility of Chinese medicine, use the holistic view research strategies of systems bio-logy, and deeply explore the processing mechanism of Chinese medicine from traditional Chinese medicine theories and the characteristics of clinical medication of Chinese medicine.


Subject(s)
Drugs, Chinese Herbal , Medicine, Chinese Traditional , Drugs, Chinese Herbal/pharmacology , Reference Standards , Research Design , Technology
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