Isolation and anticancer activity evaluation of rare Bisaryl anthraquinone antibiotics from novel Streptomyces sp. strain of NW Himalayan region

Biosynthesis of bisaryl preanthraquinone antibiotics by various microorganisms differs in monomeric subunits as well as their dimerization positions leading to different configurations. The present study relates to the production of rare bisaryl anthraquinone antibiotics by a new Streptomyces strain isolated from Shivalik region of NW Himalayas. In vitro anticancer and anti-migratory effects of Setomimycin (9,9′ bisanthraquinone antibiotic) was seen with a significant reduction in the expression of both MEK as well as ERK pathways in a dose dependent manner at 6.5 μM & 8 μM concentration in HCT-116 and 5.5 μM & 7 μM concentration in MCF-7 cells. In vivo studies in aggressive orthotopic mouse mammary carcinoma model (4T1) demonstrated about 76% reduction of primary tumor weight and 90.5% reduction in the tumor volume within two weeks. In vivo pharmacokinetics study of setomimycin revealed that it can be rapidly absorbed with an adequate plasma exposure and half-life which can be linked to its in vivo efficacy. [Display omitted] •Setomimycin, a rare bisaryl anthraquinones isolated from novel Streptomyces sp. strain from NW Himalayas.•An optima increase of par-4 was observed at 8 μM in HCT-116 cells and 7 μM in MCF-7 cells.•In-vivo studies in 4T1 mice model resulted in 90.5% reduction in the tumor volume within two weeks.•Setomimycin could absorbe rapidly (Tmax< 20 min) with a maximum plasma concentration level (Cmax>1 μM).