Smart albumin-loaded Rose Bengal and doxorubicin nanoparticles for breast cancer therapy.

Objective: To synthesise HSA-RB-DOX nanoparticles, measure its characteristics and preliminarily evaluate its anti-cancer effects.Methods: Doxorubicin (DOX) and Rose Bengal (RB) were co-delivered using albumin as a carrier. HSA-RB-DOX nanoparticles were prepared by RB-induced self-assembly of albumin. Its characteristics were measured and anti-cancer effects were tested in MCF-7 cells and tumour-bearing mice.Results: HSA-RB-DOX nanoparticle with a mean size of 42 nm was stable in different medium and behaved controlled release characteristic. It was well took in MCF-7 cells and inhibited MCF-7 cells proliferation by inducing reactive oxygen species (ROS) production. It retained a much higher blood concentration up to 12 h and accumulated more in tumour tissues. In tumour-bearing mice, HSA-RB-DOX nanoparticles inhibited tumour growth and even decreased its volume from 100 to 50 mm3, with barely no influence on body weight.Conclusions: HSA-RB-DOX nanoparticles may be potentially used for enhanced treatment of breast cancer.

1,2,3-thiadiazole thioacetanilides. Part 2: Synthesis and biological evaluation of a new series of 2-{[4-(3,4-dichlorophenyl)-1,2,3-thiadiazol-5-yl]sulfanyl}acetanilides as HIV-1 inhibitors.

As part of our studies to discover new HIV-1 reverse transcriptase inhibitors, a series of 3,4-dichlorophenyl substituted 1,2,3-thiadiazole thioacetanilide (TTA=[(1,2,3-thiadiazole-5-yl)sulfanyl]acetanilide) derivatives were synthesized, and in vitro anti-HIV activity was evaluated. The results revealed that nearly half of the compounds show moderate-to-good inhibitory potency against HIV-1. In particular, compound 7f is highly potent, with an EC(50) value of 0.95+/-0.33 microM. The preliminary structure-activity relationship among the newly synthesized congeners is discussed.