RESUMO
Rehmanniae Radix is a common medicine of traditional Chinese medicine， which has the function of nourishing Yin and tonifying the kidney， and has a long application history of processing. This medicine was first recorded in Synopsis of Golden Chamber （《金匮要略》）， which was mainly produced by steaming and boiling. Its processing materials were diverse. In addition to rice wine， honey， Amomi Fructus， milk， Aquilariae Lignum Resinatum， and Carthami Flos were also recorded in ancient books， but with the evolution of time， the characteristic excipients gradually disappeared. Based on this， starting with different excipients， the author consulted the classics of materia medica and processing specifications in various regions， sorted out the historical evolution of Rehmanniae Radix processing， and explored new methods and new ideas to exert the maximum efficacy on this basis. At the same time， the effects of different processing excipients on the chemical components and pharmacodynamic effects of Rehmanniae Radix were analyzed. After literature review， it was found that Rehmanniae Radix mainly had the effects of clearing heat and cooling blood， nourishing Yin and generating fluid. Its traditional processing excipients generally used rice wine， Carthami Flos and others. After processing with different excipients， there was different effects on the chemical components and pharmacological effects of Rehmanniae Radix. In summary， this paper can provide useful reference for standardized research on different processed products of Rehmanniae Radix.
RESUMO
To discover novel dihydropyridin-2-one derivatives with higher HDAC inhibitory activity and subtype selectivity, twenty-seven dihydropyridin-2-one derivatives containing triazole unit were synthesized via click chemistry. The structures of these compounds have been confirmed by IR, 1H NMR and HR-MS spectra. Preliminary in vitro pharmacological tests showed that these compounds potently inhibited HDAC1 and HDAC6, which also displayed significant antiproliferative effect on five cancer cells, and most of them were better than that of the parent compound 1A and drug SAHA. Specifically, compound 18g exhibited most potent anti-HDAC1 activity, and also showed the greatest potency against PC-3 and HepG2. Additionally, all compounds were nontoxic to health RWPE-1 and VERO cells, while SAHA showed essential toxicity.
RESUMO
OBJECTIVE: To establish an LC-MS/MS method for determination of Fla-CN in plasma. METHODS: Tiliroside from Potentilla chinensis Ser. was used as the internal standard. After protein precipitation by acetonitrile, samples were separated on Agilent XDB-C18 column by using acetonitrile-water (65:35) as mobile phase. The quantitation was performed on an LC-MS/MS with negative electrospray ionization in multiple reaction monitoring (MRM) mode. Fla-CN was detected at m/z 454.0→-255.0, tiliroside (IS) at m/z 593.2→285.1. RESULTS: Linear calibration curves were obtained in the concentration range of 0.5-1000 ng·mL-1 for Fla-CN. The inter-day and intra-day precision values (RSD) were below 4.6%, and the accuracy (relative error) was within ±4.1%. The method was used to determine the plasma concentration of Fla-CN after oral administration in SD rats in a predinical pharmacokinetic study. CONCLUSION: The LC-MS/MS method for determination of Fla-CN in plasma is sensitive, specific and suitable for the pharmacokinetic study of Fla-CN in rats.