Novel strategies for promoting tumor penetration of anticancer nanomedicines / 药学学报

There is a broad and urgent need for the clinical application of anticancer nanomedicine in tumor therapy, but the complex biological barrier in solid tumors has always been the main obstacle to infiltrating nanomedicine into the tumor. The traditional design of nanomedicine based on enhanced permeability and retention (EPR) effect still has some limitations in tumor permeability, it is urgent to find other design theories. Therefore, this review summarizes two novel strategies, active transcytosis and immune cell-mediated tumor penetration, for promoting tumor penetration of anticancer nanomedicine.

A new anisotane-type sesquiterpene from Anisodus tanguticus / 药学学报

To investigate the chemical constituents of Anisodus tanguticus, silica gel column chromatography, Sephadex LH-20 column chromatography, preparative thin layer chromatography, and semi-preparative HPLC were used to separate and purify the chemical constituents from the extract of A. tanguticus. The planar structure of the isolated compound was identified by HRMS, IR, and 2D NMR experiments. The absolute configuration of the isolated compound was determined by a combination of NOESY, coupling constant, circular dichroism (CD), and transition metal chelate reagent dimolybdenum tetraacetate [Mo2(OAc)4]-induced circular dichroism (ICD) data analysis. A new compound of the anisotane-type sesquiterpene (1) was isolated, which was determined to be (1R,2S,3R,4R,6R,7R,9R)-anisotane-11(13)-ene-3,4,9-triol and named anisotanol F. This is the second report of anisotane-type sesquiterpene, which has previously been reported as a novel sesquiterpenoid skeleton by our research group. Furthermore, the cytotoxicity against HUVECs and inhibitory effect on NO release in LPS-induced RAW264.7 cells of compound 1 were investigated. However, the results showed that it was inactive. Compound 1 is a new compound isolated from A. tanguticus. It belongs to the unusual anisotane-type sesquiterpene. This result enriches the chemical composition of A. tanguticus.

Toxicological research and safety consideration of coumarins / 中国中药杂志

Coumarin is an important class of natural organic compounds, which widely exists in a variety of plants and microorganisms. Coumarins have many biological activities and wide clinical applications, such as anti-tumor, anti-HIV, anti-bacterial, anti-inflammatory, anti-oxidation, anti-coagulation, but they have obvious toxic effects in rodents. It was found that the toxicity of coumarins in different animals and organs was significantly different, and high dose oral administration was more likely to produce toxic reactions. Based on the research and analysis of domestic and foreign literatures in recent 60 years, this paper mainly summarized the hepatotoxicity and pulmonary toxicity induced by coumarins, and probed into their possible mechanisms. It was found that the toxicity of coumarins had metabolic differences and species differences. The liver of rats and lungs of mice were more susceptible to coumarins. Toxic reactions occurred mainly in the second metabolic pathway of coumarin metabolism in vivo. In order to put forward safety considerations and evaluate the impact of coumarin on human body, it was found that coumarin is unlikely to produce hepatotoxicity at normal exposure level. It was also suggested that species differences due to different metabolic patterns in model animals should be carefully considered when assessing coumarin toxicity, in order to provide reference for clinical research and rational use of coumarins and improve the rational use of coumarins.

Pharmacovigilance in materia medica works of Qing Dynasty / 中国中药杂志

Taking the Zeyao Materia Medica,Benjing Fengyuan,De Pei Materia Medica,Shiyi Materia Medica,Harmful Benefits of Materia Medica as representative works in Qing Dynasty,this paper extracts text information from four aspects: drug identification,drug use,drug prevention and detoxification,constructs a drug pharmacovigilance information table of Qing Dynasty herbal works,and summarizes the drug pharmacovigilance of Qing Dynasty. Thought,in the Qing Dynasty,there were many recordings of drug pharmacovigilance. In the aspect of drug awareness,the main representative was Shi Yi Materia Medica which added many new drugs and introduced more new uses of drugs. In addition,in the aspect of drug use and prevention,the main representatives were Zeyao Materia Medica,Benjing Fengyuan,De Pei Materia Medica,and Harmful Benefits of Materia Medica. In the aspect of taboo of disease and syndrome,attention should be paid to the integration of medicine so as to make drugs closely related to clinical use. Although there is no special introduction on detoxification,it has been introduced in various medicines in the De Pei Materia Medica,Shiyi Materia Medica,which has a relatively systematic and complete drug warning ideology system of " drug identification-use-drug prevention-detoxification".This study found that the traditional pharmacovigilance thought of Qing Dynasty had the characteristics of attaching importance to the clinical application of toxic traditional Chinese medicine and the combination of medicine,which had certain guiding significance for modern clinical medication. This paper aims to explore the traditional drug pharmacovigilance knowledge in representative works of the Qing Dynasty,analyze the characteristics of the drug pharmacovigilance thought in the Qing Dynasty,and lay a foundation for clarifying the traditional drug pharmacovigilance system.

Role of p38 MAP kinase in epigallocatechin-3-gallate-induced apoptosis of human gastric cancer MGC803 cells / 肿瘤

Objective: To determine the role of p38 mitogen-activated protein kinase (MAP) kinase signal transduction pathways in epigallocatechin-3-gallate (EGCG)-induced apoptosis in human gastric cancer MGC803 cells. Methods: The viability of MGC803 cells was measured by MTT assay. Apoptosis of MGC803 cells was observed by AO/EB fluorescence microscopy and detected by flow cytometry with PI staining. Expression of p38MAPK and phosphorylated p38 (pp38) MAPK were determined by Western blot analysis. Results: EGCG induced apoptosis of MGC803 cells and apparently increased the activity of pp38MAPK in MGC803 cells. However, after interference with pp38MAPK inhibitor, the inhibitory effect of EGCG on MGC803 cells was significantly weakened. The apoptotic rate of the cells and the activity of pp38MAPK also decreased dramatically. Conclusions: EGCG can induce apoptosis of MGC803 cells. The effects could be markedly suppressed by pp38MAPK inhibitor, SB203580. EGCG induces apoptosis of MGC803 cells partly by activating p38 MAPK.