Novel Carbon Dots Derived from Moutan Cortex Significantly Improve the Solubility and Bioavailability of Mangiferin.

Background: Mangiferin (MA), a bioactive C-glucosyl xanthone with a wide range of interesting therapeutic properties, has recently attracted considerable attention. However, its application in biomedicine is limited by poor solubility and bioavailability. Carbon dots (CDs), novel nanomaterials, have immense promise as carriers for improving the biopharmaceutical properties of active components because of their outstanding characteristics. Methods: In this study, a novel water-soluble carbon dot (MC-CDs) was prepared for the first time from an aqueous extract of Moutan Cortex Carbonisata, and characterized by various spectroscopies, zeta potential and high-resolution transmission electron microscopy (HRTEM). The toxicity effect was investigated using the CCK-8 assay in vitro. In addition, the potential of MC-CDs as carriers for improving the pharmacokinetic parameters was evaluated in vivo. Results: The results indicated that MC-CDs with a uniform spherical particle size of 1-5 nm were successfully prepared, which significantly increased the solubility of MA in water. The MC-CDs exhibited low toxicity in HT-22 cells. Most importantly, the MC-CDs effectively affected the pharmacokinetic parameters of MA in normal rats. UPLC-MS analysis indicated that the area under the maximum blood concentration of MA from mangiferin-MC-CDs (MA-MC-CDs) was 1.6-fold higher than that from the MA suspension liquid (MA control) after oral administration at a dose of 20 mg/kg. Conclusion: Moutan Cortex-derived novel CDs exhibited superior performance in improving the solubility and bioavailability of MA. This study not only opens new possibilities for the future clinical application of MA but also provides evidence for the development of green biological carbon dots as a drug delivery system to improve the biopharmaceutical properties of insoluble drugs.

Phytochemical and pharmacological review of diterpenoids from the genus Euphorbia Linn (2012-2021).

ETHNOPHARMACOLOGICAL RELEVANCE: Euphorbia is one of the major genera in angiosperms, which is widely distributed all over the world, including Asia, Africa and Central and South America. The roots or tubers of Euphorbia are famous for medicinal purposes, especially in China. Many of them, such as Euphorbia pekinensis Rupr, Euphorbia fischeriana Steud and Euphorbia Kansui S.L.Liou ex S.B.Ho. . are used as Chinese herbal medicines. AIM OF THE STUDY: This paper reviews the diterpenoids isolated from the genus Euphorbia species and the pharmacological activities of these compounds to evaluate its traditional use and potential future development. MATERIALS AND METHODS: Information on the studies of the genus Euphorbia Linn was collected from scientific journals, books and reports via library and electronic data search (Scifinder, Web of Science, PubMed, Elsevier, Scopus, Google Scholar, Springer, Science Direct, Wiley, ACS, CNKI and Kew Plants of the Word Online). Meanwhile, it was also obtained from published works of material medica, folk records, ethnophmacological literatures, Ph.D. and Masters dissertations. RESULTS: Known as the main constituents of the genus Euphorbia Linn, Diterpenoids possess many pharmacological properties such as anti-inflammation, antiviral activities and cytotoxicity. To date, various types of diterpenoids were identified from this genus, including isopimarane, rosane, abietane, ent-kaurane, ent-atisane. cembrane, casbane, lathyrane, myrsinane, jatropholane, tigliane, ingenane, jatrophane, paraliane, pepluane, and euphoractin. CONCLUSIONS: This review describes 14 types of diterpenoid isolated from 45 Euphorbia species from 2012 to 2021, a total of 615 compounds. Among them, mainly include jatrophane (171), lathyrane (92), myrsinane (62), abietane (70), ent-atisane (36), ent-kaurane (7), tigliane (26) and ingenane (19). The possible biological pathways of these compounds were presumed. At the same time, more than 10 biological activities of these compounds were summarized, such as anti-inflammation, antiviral activities and cytotoxicity.