Object To investigate the effects of ethanol sediments obtained from the tuber of Angelica sinensis (Oliv). Diels (ESA) and its litmusless component (ESA 1) on the secretion of TNF ? and IL 1 by mice peritoneal macrophages in vitro. Methods L929 cell line cytotoxicity was used for the assay of TNF ?. The proliferation of L929 cell line was used for the assay of IL 1. Results The secretion of TNF ? and IL 1 by mice peritoneal macrophages which were co cultured with ESA or ESA 1 in vitro can be significantly promoted. At the concentrations in range of 5～20 ?g/mL, there is a dose dependence in the action of ESA, while there is not the similar effect of ESA 1, even though it showed the marked effect. Conclusion ESA and ESA 1 can enhance the secreting TNF ? and IL 1 of mice peritoneal macrophages in vitro.

EIDD-2801 is an orally bioavailable prodrug, which will be applied for emergency use authorization from the U.S. Food and Drug Administration for the treatment of COVID-19. To investigate the optimal parameters, EIDD-2801 was optimized

Recent progress in targeted metabolic therapy of cancer has been limited by the considerable toxicity associated with such drugs. To address this challenge, we developed a smart theranostic prodrug system that combines a fluorophore and an anticancer drug, specifically 6-diazo-5-oxo-l-norleucine (DON), using a thioketal linkage (TK). This system enables imaging, chemotherapy, photodynamic therapy, and on-demand drug release upon radiation exposure. The optimized prodrug, DON-TK-BM3, incorporating cyanine dyes as the fluorophore, displayed potent reactive oxygen species release and efficient tumor cell killing. Unlike the parent drug DON, DON-TK-BM3 exhibited no toxicity toward normal cells. Moreover, DON-TK-BM3 demonstrated high tumor accumulation and reduced side effects, including gastrointestinal toxicity, in mice. This study provides a practical strategy for designing prodrugs of metabolic inhibitors with significant toxicity stemming from their lack of tissue selectivity.