Abstract：
Melanoma, a cancer arising from melanocytes, requires a novel treatment strategy because of the ineffectiveness of conventional therapies in certain patients. Fustin is a flavanonol found in young fustic (Cotinus coggygria). However, little is known about its antimelanoma effects. Our study demonstrates that fustin suppresses the growth of B16 melanoma cells. Phalloidin staining of cytoskeletal actin revealed that fustin induced a conformational change in the actin structure of melanoma cells, accompanied by suppressed phosphorylation of myosin regulatory light chain 2 (MLC2), a regulator of actin structure. Furthermore, the protein kinase A (cAMP-dependent protein kinase) inhibitor H89 completely attenuated fustin-induced downregulation of phosphorylated myosin phosphatase targeting subunit 1, which is involved in dephosphorylation of MLC2. In a mouse model, administration of fustin suppressed tumor growth in B16 melanoma cells without adverse effects. In conclusion, our findings suggest that fustin effectively suppresses melanoma cell growth both in vitro and in vivo.
摘要：
黑色素瘤,由黑素细胞引起的癌症，由于常规疗法对某些患者无效，因此需要一种新的治疗策略。Fustin是在年轻的fustic（Cotinuscoggygria）中发现的黄酮醇。然而,对其抗黑色素瘤的作用知之甚少。我们的研究表明，fustin抑制B16黑色素瘤细胞的生长。细胞骨架肌动蛋白的Phalloidin染色显示，融合蛋白诱导黑色素瘤细胞肌动蛋白结构的构象变化，伴随着肌球蛋白调节轻链2（MLC2）的磷酸化抑制，肌动蛋白结构的调节剂。此外，蛋白激酶A（cAMP依赖性蛋白激酶）抑制剂H89完全减弱融合蛋白诱导的磷酸化肌球蛋白磷酸酶靶向亚基1（MYPT1）的下调，参与MLC2的去磷酸化。在老鼠模型中，施用fustin抑制了B16黑色素瘤细胞中的肿瘤生长，而没有不良反应。总之,我们的发现表明，fustin在体外和体内都能有效抑制黑色素瘤细胞的生长。
