No abstract

Twenty-two derivatives belonging to the cis-1,2-diacyloxy-6-methoxy-3,3,14-trimethyl-1,2,3,14-tetrahydro-7H-benzo[a]pyrano[3,2-h]acridin-7-one series were synthesized in nine steps starting from 3,5-dimethoxyacetanilide (5) and 2-methoxy-1-naphthalenecarboxylic acid (7). Most of them exhibited submicromolar cytotoxicity when tested against murine leukemia (L1210) and human epidermoid carcinoma (KB-3-1) cell lines. The cytotoxic activity correlated strongly with the ability of the compounds to form covalent adducts with purified DNA. Among the most active compounds, 25, with IC50 values of 0.7 and 0.15 microM against L1210 and KB-3-1, respectively, was selected for evaluation in vivo against Colon 38 adenocarcinoma implanted in mice. This compound was active at 3 mg/kg i.v. (day 12 and 24) with 3/7 tumor free mice by day 80.

Synopsis Electrospinning is a process used to produce ultrafine fibers with diameters in the nanometer range. Electrospun fiber mats have high potentials for biomedical uses, due to their high surface area and ease of drug incorporation into the fibers. They can be used as carriers for drug delivery and can enhance drug release and skin permeability. The aim of this study was to prepare electrospun fiber mats and to incorporate extracts from the fruit hull of mangosteen. Anti‐oxidant activity and extract release were determined and compared between the extract incorporated in the electrospun fiber mats and in the cast films. Poly (vinyl alcohol) (PVA) was selected as the polymer matrix. Extracts in the amount of 2.5%, 5%, and 10% w/w, based on the weight of PVA, were incorporated with 10% w/w PVA to finally obtain electrospun fiber mats and cast films. The extract content was evaluated by anti‐oxidative activity using the 2,2‐diphenyl‐1picryhydrazyl (DPPH) method. The morphology of the electrospun fiber mats was analyzed using a scanning electron microscope (SEM). The results showed that the diameters of the fibers were in nanoscales and that no crystal of the extract was found at any concentration of the extract. The extract contents in the electrospun fiber mats prepared at 2.5%, 5%, and 10% w/w of the extract were 9.6%, 9.7%, and 10.8% of the initial loading concentration, respectively, whereas, those in the cast films were 23.9%, 14.5%, and 21.0%, respectively. The release of the extract from the electrospun fiber mats prepared at 2.5%, 5%, and 10% w/w of the extract at 120 min were 73.2%, 83.6%, and 81.3% w/w, respectively. However, much slower release from the cast films was observed (i.e. 4.3%, 29.1%, and 40.8% w/w, respectively).