RESUMO
Platelet function tests have been increasingly used to assist in the diagnosis of platelet disorders and prethrombotic state, monitoring of the efficacy of antiplatelet therapies, and personalized treatment. On the basis of light transmission aggregometry, new methods for platelet function test have been developed successively. At present, the research and development of platelet function detector is in its infancy in China. The active constituents of antiplatelet Chinese medicines can be classified into terpenoids, flavonoids, saponins, organic acids, lignans, diketones, volatile oils, and stilbenes. The results of dose-antiplatelet effect relationship of Chinese medicines and the active constituents showed that the effective concentration of the extracts or monomers of Chinese medicines was at micromolar level(µmol·L~(-1)), among which salvianolic acid B and ginkgolide K, ginkgolide B, and ginkgolide A had the strongest antiplatelet effect. These results suggest that the antiplatelet effect of Chinese medicine may be weaker than that of chemical drugs and biological products. Therefore, it is necessary to explore the structure-activity relationship of the active constituents in existing Chinese medicines and further improve their efficacy through structure modification. The antiplatelet effect of Chinese medicines and the constituents involves multiple pathways and multiple targets. These research results provide a reference for clinical application of them. However, there is still a lack of large-scale multi-center clinical trials to confirm the efficacy and safety of them. The regularity of the relationship between the structures of various constituents and their corresponding functions is still unknown and the relevant signal transduction pathways and structure-activity relationship need to be further studied. This paper summarized and analyzed the determination methods of platelet functions and the research results of antiplatelet Chinese medicines, which is of reference value for the research of effective and safe antiplatelet Chinese medicines.
Assuntos
Produtos Biológicos , Medicina Tradicional do Leste Asiático , China , Inibidores da Agregação Plaquetária/farmacologia , Testes de Função PlaquetáriaRESUMO
BACKGROUND: Anthraquinones, rhein and aurantio-obtusin were isolated from the herb Duhaldea nervosa for the first time by our group, which were also found in plants that belong to the plant family Compositae. Anthraquinone compounds have a range of pharmacological activities such as anti-inflammatory, anti-cancer, antioxidation, anti-diabetes, etc. and can be used as a laxative, for liver protection, treatment of chronic renal failure, etc. However, in recent years, anthraquinones have been reported to be cytotoxic to the liver and kidneys. Therefore, it is very important to study the pharmacokinetics and metabolism of rhein and aurantio-obtusin, which are common ingredients in many traditional Chinese medicines (TCM). According to our research, the pharmacokinetics and metabolism of rhein and aurantio-obtusin are comprehensively summarized in the paper for the first time. OBJECTIVE: The study provides comprehensive information on pharmacokinetics and metabolism of rhein and aurantio- obtusin in different Species; meanwhile, the aim of this review is also to provide a reference for a reasonable application of TCM enriched with these two ingredients. METHODS: The metabolism and pharmacokinetics of rhein and aurantio-obtusin were searched by the Web of Science, PubMed, Google scholar and some Chinese literature databases. RESULTS: Rhein and aurantio-obtusin exist mainly in the form of metabolites in the body. Rhein and aurantio-obtusin and its metabolites might be responsible for pharmacological effects in the body. Therefore, the significance of studying the in vivo metabolites of rhein and aurantio-obtusin is not only essential to clarify their pharmacological mechanism, but also to find new active compound ingredients. The metabolism of rhein is different in different species, so the toxicity effects of rhein may also be different after oral administration in different species; however, the metabolic profiles of aurantio-obtusin in the liver microsomes of different species are similar. CONCLUSION: This paper not only provides detail regarding the pharmacokinetics of rhein and aurantio-obtusin, but it is anticipated that it will also facilitate further study on the metabolism of rhein and aurantio-obtusin.