ABSTRACT
Abstract Cerebrovascular disease is the second most serious disease in the world. It has the features of high morbidity, high mortality and recurrence rate. Numerous research on the compatibility of Chinese medicine with effective ingredients of cerebral ischemia has been made during the past decades. The purpose of this study is to quantitatively analyze the combined pharmacological effect of effective ingredients in Danshen and Honghua (Dan Hong) on rat microvascular endothelial cells after gradually oxygen-glucose deprivation. The experimental concentration range for the compatibility of two effective ingredients were determined in the preliminary experiments by Cell Counting kit-8 (CCK-8) method. Drugs were added to rat brain microvascular endothelial cells at a non-toxic dose level. After that, the cells were cultured for 12 h, and placed in a hypoxic environment. Finally, the cell survival rate was used as a measure of drug effect. In order to determine synergism or antagonism, the combination index (CI)-isobologram method was performed to analyze the data from the experiments. Based on this theory, the potencies of each drug and the shapes of their does-effect curves are both taken into account. The results show that the synergism or the antagonism between two effective ingredients compatibility change with different proportion and dosage. Furthermore, it can be seen from the results of these experiments that when these drugs are used in combination, the dosage required to achieve the same therapeutic effects is greatly reduced compared with the case of single one. It is worth mentioning that our experiments also prove that the median-effect equation and the CI method can be applied in the field of traditional Chinese medicine.
Subject(s)
Animals , Male , Female , Rats , Endothelial Cells/classification , Evaluation Studies as Topic , Pharmaceutical Preparations/administration & dosage , Cerebrovascular Disorders/pathology , Carthamus tinctorius/adverse effectsABSTRACT
The present study investigated the mechanism of components in stasis-resolving and collateral-dredging Chinese herbal medicines, including scutellarin(Scu), paeonol(Pae), and hydroxy safflower yellow A(HSYA), in the treatment of psoriasis by regulating angiogenesis and inflammation. The human umbilical vein endothelial cells(HUVECs) cultured in vitro were divided into a normal group, a model group, a VEGFR tyrosine kinase inhibitor Ⅱ(VRI) group, and Scu, Pae, and HSYA groups with low, me-dium, and high doses. Cell viability was detected by the CCK-8 assay. Cell migration was detected by wound healing assay. Tube formation assay was used to measure the tube formation ability. Western blot was used to detect the protein expression of the VEGFR2/Akt/ERK1/2 signaling pathway. The secretion levels of inflammatory cytokines IFN-γ, IL-1β, IL-6, and TNF-α were detected by ELISA. The results showed that compared with the model group, all the Scu, Pae, and HSYA groups could reduce cell viability, inhibit cell migration and tube formation(P<0.05, P<0.01), and down-regulated the protein expression of VEGFR2, p-VEGFR2, Akt, p-Akt, ERK1/2, and p-ERK1/2. Scu and Pae could down-regulate VEGFR2 expression(P<0.05, P<0.01), while other groups only showed a downward trend. Scu and Pae significantly reduced IFN-γ and IL-6 levels(P<0.01), and HSYA significantly reduced the levels of IFN-γ, IL-1β, and IL-6(P<0.01). Scu, Pae, and HSYA had no significant effect on TNF-α. The results suggested that Scu, Pae, and HSYA may exert a therapeutic role in psoriasis-related angiogenesis and inflammation by inhibiting VEGFR2/Akt/ERK1/2 signaling pathway and inhibiting the secretion of IFN-γ, IL-1β, and IL-6.
Subject(s)
Humans , Angiogenesis Inhibitors/pharmacology , China , Human Umbilical Vein Endothelial Cells , Neovascularization, Pathologic/drug therapy , Vascular Endothelial Growth Factor A/metabolismABSTRACT
Objective@#To optimize the formulation and preparation technology of hydroxy safflower yellow A solid lipid nanoparticles and evaluate its quality.@*Metheds@#Hydroxy safflower yellow A solid lipid nanoparticles were prepared by the method of hot melt emulsification ultrasonic-low temperature using hydroxypropyl methylcellulose as a lipid material and glyceryl monostearate as an emulsifier. Using entrapment efficiency as indexes, the amount of hydroxypropyl methylcellulose, purified water, glyceryl monostearate, and Tween 80 aqueous solution (1%) as factors, orthogonal test was applied to optimize the formulation and preparation technology. Dialysis method was used to measure encapsulation efficiency. The morphology and uniformity of the nanoparticles were observed by transmission scanning electron microscopy. The particle size, polydispersion index and Zeta potential were determined by nano-particle size analyzer. And hydroxy safflower yellow A solid lipid nanoparticles sustained releasing characteristics was evaluated by the percentage of cumulative drug release.@*Results@#The optimal process of prepared hydroxy safflower yellow A solid lipid nanoparticles was 5 mg of hydroxypropyl methylcellulose, 0.2 ml of purified water, 100 mg of glyceryl monostearate, and 1.8 ml of Tween 80 aqueous solution (1%). The size of the prepared nanoparticles was uniform and spherical. And the average particle size were (99.85 ± 3.04) nm, polydispersion index were (0.390 ± 0.021), Zeta potential were (-27.63 ± 2.12) mV, and the encapsulation efficiency of the hydroxy safflower yellow A solid lipid nanoparticles were (63.35 ± 2.65)%. The release rate of the nanoparticles was (44.35 ± 0.49)%.@*Conclusions@#The prepared hydroxy safflower yellow A solid lipid nanoparticles have good uniformity and good sustained release properties.
ABSTRACT
Objective To optimize the formulation and preparation technology of hydroxy safflower yellow A solid lipid nanoparticles and evaluate its quality. Metheds Hydroxy safflower yellow A solid lipid nanoparticles were prepared by the method of hot melt emulsification ultrasonic-low temperature using hydroxypropyl methylcellulose as a lipid material and glyceryl monostearate as an emulsifier. Using entrapment efficiency as indexes, the amount of hydroxypropyl methylcellulose, purified water, glyceryl monostearate, and Tween 80 aqueous solution (1%) as factors, orthogonal test was applied to optimize the formulation and preparation technology. Dialysis method was used to measure encapsulation efficiency. The morphology and uniformity of the nanoparticles were observed by transmission scanning electron microscopy. The particle size, polydispersion index and Zeta potential were determined by nano-particle size analyzer. And hydroxy safflower yellow A solid lipid nanoparticles sustained releasing characteristics was evaluated by the percentage of cumulative drug release. Results The optimal process of prepared hydroxy safflower yellow A solid lipid nanoparticles was 5 mg of hydroxypropyl methylcellulose, 0.2 ml of purified water, 100 mg of glyceryl monostearate, and 1.8 ml of Tween 80 aqueous solution (1%). The size of the prepared nanoparticles was uniform and spherical. And the average particle size were (99.85 ± 3.04) nm, polydispersion index were (0.390 ± 0.021), Zeta potential were (-27.63 ± 2.12) mV, and the encapsulation efficiency of the hydroxy safflower yellow A solid lipid nanoparticles were (63.35 ± 2.65)%. The release rate of the nanoparticles was (44.35 ± 0.49)%. Conclusions The prepared hydroxy safflower yellow A solid lipid nanoparticles have good uniformity and good sustained release properties.
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Objective: To study the application of four kinds of hollow fiber ultrafiltration membranes by taking Qihong Maitong Injection (QMI) microfiltrated liquid as the research object. Methods: Polysulfone, polyether sulfone, polypropylene, and blended composite membranes with the entrapment relative molecular mass of 100000 for ultrafiltration were selected to determine the best appropriate ultrafiltration membrane material. The membrane flux of ultrafiltration was determined by taking the content of active ingredients (Astragalus total saponin, astragaloside IV, and hydroxy safflower yellow A), solid reduction rate, protein reduction rate, related substances, and pyrogen inspection of different membrane materials as the evaluation indexes. Results: The suitability of four different kinds of ultrafiltration membrane materials with the same entrapment relative molecular mass was different. The pure water flux recovery rates of polypropylene, polyether sulfone, and blended composite materials are higher than that of polysulfone material. The component permeation rates of polypropylene and polyether sulfone materials were higher, while the solid and protein reduction rates of polysulfone and blend compound materials were higher. For QMI, the ultrafiltration membrane with entrapment relative molecular mass of 100000 could effectively remove the pyrogen. Conclusion: The polypropylene-100000 ultrafiltration membrane could not only effectively remove the solid and high polymer material, but also keep the active ingredients. It is suitable for the purification of QMI.
ABSTRACT
AIM:To study incorporate changes of compound in safflower infusion solution before and after heating by HPLC fingerprint, in order to provide reference of drug’s safety evaluation. METHODS: Hydroxysafflor yellow A was used as reference substance, safflower infusion solution was detected by HPLC fingerprint in the whole manufacturing process from original raw material、intermediate to finished product.The detector temperature was set at room temperature、100 ℃、115 ℃,and then the change in the peak’ disappearance and appearance was observed and the peak area’ decrease and increase showed by characteristic absorption peak of every sample product at different temperature. RESULTS: As the temperature rose to 105 ℃,new peaks appeared at the retention time of 7、26-27、44 minutes,original peaks would disappear at the time 8、36minutes.As the temperature continued to rise to 115 ℃,the peak at the time of 7、10 minutes disappeared again.the peak area increased during the temperature rising at retention the time of 31-32、44 minutes and decreased at the retention time of 37 minutes. CONCLUSION: It indicates that,heating safflower infusion solution would produce a new compound. As the temperature continues to rise,the new compound would be destroyed.