erianin and Skin-Neoplasms

Psoriasis is a malignant skin disease characterized as keratinocyte hyperproliferation and aberrant differentiation. Our previous work reported that a bibenzyl compound, erianin, has a potent inhibitory effect on keratinocyte proliferation. To improve its poor water-solubility, increase anti- proliferation activity, and enhance the skin delivery, erianin loaded dendritic mesoporous silica nanospheres (E/DMSNs) were employed.

Topics: Apoptosis; Bibenzyls; Cell Line, Tumor; Cell Proliferation; Cell Survival; Drug Carriers; Drug Delivery Systems; Humans; Keratinocytes; Membrane Potential, Mitochondrial; Nanospheres; Phenol; Silicon Dioxide; Skin; Skin Neoplasms; Solubility

This study evaluated the anti-angiogenic activities of erianin in vivo and in vitro. Erianin, a natural product from Dendrobium chrysotoxum, caused moderate growth delay in xenografted human hepatoma Bel7402 and melanoma A375 and induced significant vascular shutdown within 4 h of administering 100 mg/kg of the drug. Erianin also displayed potent anti-angiogenic activities in vitro: it abrogated spontaneous or basic fibroblast growth factor-induced neovascularisation in chick embryo; it inhibited proliferation of human umbilical vein endothelial cells (EC(50) 34.1+/-12.7 nM), disrupted endothelial tube formation, and abolished migration across collagen and adhesion to fibronectin. Erianin also exerted selective inhibition toward endothelial cells, and quiescent endothelium showed more resistance than in proliferative and tumour conditions. In a cytoskeletal study, erianin depolymerised both F-actin and beta-tubulin, more significantly in proliferating endothelial cells than in confluent cells. In conclusion, erianin caused extensive tumour necrosis, growth delay and rapid vascular shutdown in hepatoma and melanoma models; it inhibited angiogenesis in vivo and in vitro and induced endothelial cytoskeletal disorganisation. These findings suggest that erianin has the therapeutic potential to inhibit angiogenesis in vivo and in vitro.

Topics: 3T3 Cells; Angiogenesis Inhibitors; Animals; Bibenzyls; Carcinoma, Hepatocellular; Drug Evaluation, Preclinical; Female; Liver Neoplasms; Melanoma; Mice; Mice, Inbred BALB C; Neoplasm Transplantation; Phenol; Skin Neoplasms; Tumor Cells, Cultured