ABSTRACT
In order to study the contraindications of the compatibility of Flos Genkwa-Radix et Rhizoma Glycyrrhizae, in this study, the solubilizing and poisoning essence were explored. In this experiment, chromatographic assay, field emission scanning electron microscopy, MTT cytotoxicity evaluation, and other methods were used to study the main chemical components, morphology and toxicity of the ethyl acetate part of Flos Genkwa and its co-decoction with glycyrrhizic acid, in order to clarify Flos Genkwa-Radix et Rhizoma Glycyrrhizae incompatibility provides a new idea for the research on incompatibility of Flos Genkwa-Radix et Rhizoma Glycyrrhizae. The results showed that after co-decoction of the ethyl acetate part of Flos Genkwa with glycyrrhizic acid, high performance liquid chromatography (HPLC) detected the dissolution of the toxic component yuanhuacine of 54.8%, while yuanhuacine chromatographic peak was not detected in the Flos Genkwa ethyl acetate part of the single decoction. The increase of co-decoction dissolution rate was observed by scanning electron microscopy, and it was found that glycyrrhizic acid uniformly dispersed the fat-soluble components of Flos Genkwa into nano-scale particles, which improved the solubility and stability in the solution. Furthermore, the results of cytotoxicity evaluation showed that the survival rate of cells decreased after co-decoction, 4',6-diamidino-2-phenylindole (DAPI) staining also gave the same results. In summary, the co-decoction of the ethyl acetate part of Flos Genkwa with glycyrrhizic acid promotes the dissolution of the toxic component yuanhuacine, and makes the part form uniformly distributed nanoparticles, which is conducive to the absorption of the ingredient and increases the toxicity.
ABSTRACT
Yuanhuacine is a daphne-type diterpene isolated from Daphne genkwa. It is also isolated from the plant of Daphne and Euphorbia. With the further research on yuanhuacine, it has been found that yuanhuacine has strong anti-tumor activity, and it also exhibits significant anti-virus, anti-inflammatory, neuroprotective and anti-fertility activities. Yuanhuacine can enter various tissues with the blood, and pass through the blood-brain barrier. The bioavailability of yuanhuacine is good, which has potential therapeutic significance for the lesions of all tissues. However, the researches on yuanhuacine mainly focus on the preclinical research and yuanhuacine is only used to induce labor clinically. The purpose of this study is to systematically summarize and analyze the pharmacological activity, drug metabolism in vivo, and clinical application of yuanhuacine, so as to provide a theoretical basis for its development and application.
ABSTRACT
The aim of the present study was to increase distribution of yuanhuacine in the lungs and achieve the purpose of reducing toxicity and increasing efficiency.Therefore,yuanhuacine was designed to be dry powder inhalers innovatively and directly delivered to the lungs.Accordingly,inhaled lactose was used as a carrier to adsorb yuanhuacine on the surface of lactose.Fine particle fraction (FPF) was utilized as evaluation index to filtrate the optimal prescription for pulmonary administration.Besides,an UHPLC-MS/MS method was established for the analysis of heart,liver,spleen,lung,kidney,brain and reproductive system of rats.Intravenous injection was taken as reference to investigate the distribution of yuanhuacine and calculate relevant targeting parameters.The experimental result indicated that the prescription (rough lactose ∶fine lactose =10 ∶ 1) has the highest FPF,which can be chosen as the most suitable prescription for pulmonary administration of yuanhuacine.Moreover,by comparing the distribution of yuanhuacine through pulmonary administration and intravenous injection,it was found that the concentration of yuanhuacine in the lung tissue was greatly increased by pulmonary administration,which decreased the distribution in heart,liver,spleen,kidney,brain and reproductive system,thus sequentially reducing the toxicity in other tissues and increased the efficiency.
ABSTRACT
PGF2. What we observsd suggests that PGE2 has the ability to inhibit the decidual cells directly; neither the contraction of the uterus nor the metabolism of estrogen or progestogen may be responsible for this effect. This inhibitory effect of PGE2 on decidual cells may be one of the mechanisms for the termination of the early pregnancy.