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China Journal of Chinese Materia Medica ; (24): 6075-6081, 2023.
Article in Chinese | WPRIM | ID: wpr-1008806


With the continuous exploration of microemulsions as solvents for traditional Chinese medicine extraction, polyoxyethy-lene(35) castor oil(CrEL), a commonly used surfactant, is being utilized by researchers. However, the problem of detecting residues of this surfactant in microemulsion extracts has greatly hampered the further development of microemulsion solvents. Based on the chemical structures of the components in CrEL and the content determination method of castor oil in the 2020 edition of the Chinese Pharmacopoeia(Vol. Ⅳ), this study employed gas chromatography(GC) and single-factor experiments to optimize the preparation method of methyl ricinoleate from CrEL. The conversion coefficient between the two was validated, and the optimal sample preparation method was used to process microemulsion extracts of Zexie Decoction from three batches. The content of methyl ricinoleate generated was determined, and the content of CrEL in the microemulsion extracts of Zexie Decoction was calculated using the above conversion coefficient. The results showed that the optimal preparation method for CrEL was determined. Specifically, 10 mL of 1 mol·L~(-1) KOH-methanol solution was heated at 60 ℃ for 15 min in a water bath. Subsequently, 10 mL of boron trifluoride etherate-methanol(1∶3) solution was heated at 60 ℃ for 15 min in a water bath, followed by extraction with n-hexane twice. CrEL could stably produce 20.84% methyl ricinoleate. According to this conversion coefficient, the average mass concentration of CrEL in the three batches of Zexie Decoction microemulsion extracts was 11.94 mg·mL~(-1), which was not significantly different from the CrEL mass concentration of 11.57 mg·mL~(-1) during microemulsion formulation, indicating that the established content determination method of this study was highly accurate, sensitive, and repeatable. It can be used for subsequent research on microemulsion extracts of Zexie Decoction and provide a reference for quality control of other drug formulations containing CrEL.

Polyethylene Glycols/chemistry , Castor Oil , Methanol , Surface-Active Agents/chemistry , Solvents , Water/chemistry , Emulsions/chemistry
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 156-163, 2022.
Article in Chinese | WPRIM | ID: wpr-940633


ObjectiveTo optimize the extraction and purification process of Gardeniae Fructus for industrial production, and to obtain the total iridoid and total crocin extracts. MethodOrthogonal test was used to optimize the water extraction process by taking contents of geniposide, genipin gentiobioside, gardenoside, crocin-1 and crocin-2 as indicators and the decocting time, decocting times and water amount as factors. The purification process was optimized by single factor test, and four different types of macroporous adsorption resins were screened. The process conditions such as resin type, maximum loading amount, water washing amount, ethanol concentration, ethanol dosage, and flow rate of sample loading were mainly investigated. In addition, the drying methods (vacuum drying and spray drying) of the extract were investigated, and a pilot scale-up verification test was carried out. ResultThe optimal water extraction process of Gardeniae Fructus was to add 15, 10 times the amount of water for decocting twice, 1 h each time. The optimal purification process was as follows:the water extract through SP825L macroporous resin column, the amount of crude drug-the amount of resin (1∶1.5), the sample loading flow rate of 3 BV h-1, adding 2 BV of water to remove impurities, adding 4 BV of 30% ethanol to obtain the iridoid part, then adding 3 BV of 70% ethanol to obtain the crocin part, collecting the ethanol lotion, and drying at 70 ℃. Under these conditions, the extraction amount of total iridoids was 590.75 mg·g-1 with the transfer rate of 70.48%, and the yield of dry extract was 8.89%. The extraction amount of total crocins was 83.37 mg·g-1 with the transfer rate of 22.20%, and the dry extract yield was 2.60%. ConclusionThe optimized extraction and purification process is stable and feasible with high extraction rate of active components, which is suitable for the industrial extraction and purification of active parts of Gardeniae Fructus.

Chinese Journal of Experimental Traditional Medical Formulae ; (24): 191-197, 2021.
Article in Chinese | WPRIM | ID: wpr-906161


Zexietang is derived from Jingui Yaolue (《金匮要略》), which is composed of Alismatis Rhizoma and Atractylodis Macrocephalae Rhizoma, and has the effect of inducing diuresis and invigorating the spleen to produce water. Compared with western medicine in the treatment of related diseases, Zexietang can not only improve the curative effect, but also reduce the occurrence of adverse reactions, so as to achieve long-term stable administration. The authors sorted out and analyzed the chemical composition, pharmacological effect and clinical application of Zexietang in recent years. It was found that the main active components of Zexietang were alismol A and B, 23-acetyl-alismol B and C, atractylenolides (atractylenolide Ⅰ, Ⅱ, Ⅲ) and polysaccharides. Pharmacological experiments showed that they had diuretic, hypolipidemic, anti-inflammatory and others. And it can be used in the treatment of hypertension, hyperlipidemia, vertigo, cerebral vascular insufficiency and other diseases combined with other Chinese materia medica, and the curative effect is obvious. By summarizing the research status of Zexietang in recent years, its active components and pharmacological mechanism can be further clarified, which provides the basis for the clinical application of Zexietang and guides the direction of its further research.

Chinese Journal of Experimental Traditional Medical Formulae ; (24): 206-215, 2021.
Article in Chinese | WPRIM | ID: wpr-906069


The small size, moderate drug loading, and targeting properties of nano-preparations make them can be excellent delivery tools for drugs, genes or proteins crossing the cell or blood-brain barrier (BBB). Currently, facilitating drug crossing BBB with innovative nano-drug delivery systems is considered as a strategic approach for the prevention, diagnosis and treatment of central nervous system (CNS) diseases. However, with the deepening of the research, the adverse reactions and toxicity of nanocarriers have gradually attracted the attention of researchers. Based on this, this paper summarized the situation of BBB-penetrating targeted nano-preparations at home and abroad in recent years from the perspective of classification of types and properties of nanocarriers, and analyzed the advantages and disadvantages of each carrier. The results showed that nano-preparations with active ingredients of traditional Chinese medicine (TCM) as carriers have become a promising way of cancer treatment, but the complexity and diversity of TCM components limited its application to a certain extent. Further studies should be strengthened to lay a foundation for the application and development of TCM nano-preparations in the field of CNS diseases.

China Journal of Chinese Materia Medica ; (24): 2481-2488, 2021.
Article in Chinese | WPRIM | ID: wpr-879151


The paclitaxel-loaded and folic acid-modified poly(lactic-co-glycolic acid) nano-micelles(PTX@FA-PLGA-NMs) were prepared by the emulsion solvent evaporation method, and the parameters of paclitaxel-loaded nano-micelles were optimized with the particle size and PDI as evaluation indexes. The morphology of the nano-micelles was observed by transmission electron microscopy(TEM), and the stability, drug loading and encapsulation efficiency were systematically investigated. In vitro experiments were performed to study the cytotoxic effects of nano-micelles, apoptosis, and cellular uptake. Under the optimal parameters, the nano-micelles showed the particle size of(125.3±1.2) nm, the PDI of 0.086±0.026, the zeta potential of(-20.0±3.8) mV, the drug loading of 7.2%±0.75%, and the encapsulation efficiency of 50.7%±1.0%. The nano-micelles were in regular spherical shape as observed by TEM. The blank FA-PLGA-NMs exhibited almost no inhibitory effect on the proliferation and growth of tumor cells, while the drug-loaded nano-micelles and free PTX exhibited significant inhibitory effects. The IC_(50) of PTX@FA-PLGA-NMs and PTX was 0.56 μg·mL~(-1) and 0.66 μg·mL~(-1), respectively. The paclitaxel-loaded nano-micelles were potent in inhibiting cell migration as assessed by the scratch assay. PTX@FA-PLGA-NMs had good pro-apoptotic effect on cervical cancer HeLa cells and significantly promoted the uptake of HeLa cells. The results of in vitro experiments suggested that PTX@FA-PLGA-NMs could target and treat cervical cancer HeLa cells. Therefore, as nanodrug carriers, PTX@FA-PLGA-NMs with anti-cancer activity are a promising nano-system for improving the-rapeutic effects on tumors.

Female , Humans , Antineoplastic Agents, Phytogenic/pharmacology , Cell Line, Tumor , Drug Carriers , Folic Acid , Glycolates , HeLa Cells , Micelles , Paclitaxel , Particle Size , Uterine Cervical Neoplasms/drug therapy
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 205-213, 2019.
Article in Chinese | WPRIM | ID: wpr-802187


Gas chromatography (GC) is mainly used to detect the levels of short-chain fatty acids (SCFAs), but with the deepening of research,the drawbacks of GC have become more and more obvious in the fields of food,chemical engineering and clinical application. The analysis on existing research results showed that ultra performance convergence chromatography (UPC2) was appropriate for the analysis of lipid metabolism. The UPC2 is a new kind of chromatographic separation technology developed in recent five years and the level of SCFAs is associated with the research on multiple diseases. Therefore,application of UPC2 in the detection of SCFAs would be helpful for the scholars at home and abroad to carry out deeper researches,and also helpful to guide the treatment for various metabolic disorders. In this paper,the researches on SCFAs in recent ten years were reviewed; the shortcomings of GC and liquid chromatography (LC) in the detection of SCFAs were reviewed; the development process,basic characteristics and research status of UPC2 at home and abroad were introduced; feasibility and innovation of UPC2 in the detection of SCFAs were summarized. Pretreatment methods for UPC2 application to the detection of SCFAs in feces or serum were collected; the problems that should be noticed during the process of sample pretreatment were pointed out; meanwhile, an research outlook on methodology of UPC2 application in the detection of SCFAs was conducted. The effects of extracting solvent,mobile phase,and auxiliaryt solvent on chromatographic behavior as well as the physicochemical property, type and choice of UPC2 chromatographic column were mainly discussed in this paper. In addition, the choices of basic modifier,acid modifier,and salinity modifier were briefly outlined, in order to provide efficient,simple,environmental,and economic detection technologies for the research on SCFAs, and provide better reference solutions for the rapid detection of massive clinical samples.