Morusin is a significant prenylated flavone found in Morus alba (Moraceae) root cortex, which exhibits significant anti-tumor activity in the treatment of prostate cancer[1]. Prenylated flavonoids, a unique class of flavonoids which combine a flavonoid skeleton and a lipophilic prenyl side-chain, possess great potential biological activities including cytotoxicity, anti-inflammation, anti-Alzheimer, anti-diabetes and other effects[2]. Morusin as a candidate for the new efficacious mucoregualtors for inflammatory pulmonary diseases[3].
In vitro, treatment of PC3 cells with morusin (0-10μM) for 48h significantly inhibited cell viability in a time- and concentration-dependent manner and reduced levels of inflammatory cytokines[4]. In NCI-H292 cells deprived of serum for 24h, morusin (1-100μM) administered for 30minutes significantly suppressed the production of mucin 5AC (MUC5AC), thereby controlling various pulmonary inflammatory responses caused by excessive mucus secretion[3]. In cancer cell lines (MKN45 and SGC7901) treated with moracin (1-5mg/L) for 72h, moracin effectively inhibited cancer cell growth and proliferation in a dose-dependent manner[5].
In vivo, administration of morusin (5mg/kg/5days) via intragastric administration for 28days in ovariectomized rats, morusin alleviated estrogen deficiency-induced osteoporosis and reduced the expression of RUNX2 and β-catenin in femoral bone tissue[6]. In a destabilization of the medial meniscus osteoarthritis (DMM) mouse model, administration of morusin (5mg/kg/2days) via intragastric administration for 56days, morusin mitigated cartilage erosion and destruction while decreasing the expression levels of associated inflammatory factors and proteins[7].
References:
[1] Dirir A M, Daou M, Yousef A F, et al. A review of alpha-glucosidase inhibitors from plants as potential candidates for the treatment of type-2 diabetes[J]. Phytochem Rev, 2022, 21(4): 1049-1079.
[2] Shi S, Li J, Zhao X, et al. A comprehensive review: Biological activity, modification and synthetic methodologies of prenylated flavonoids[J]. Phytochemistry, 2021, 191: 112895.
[3] Lee H J, Ryu J, Park S H, et al. Effects of Morus alba L. and Natural Products Including Morusin on In Vivo Secretion and In Vitro Production of Airway MUC5AC Mucin[J]. Tuberc Respir Dis (Seoul), 2014, 77(2): 65-72.
[4] Fadil S A, Albadawi D a I, Alshali K Z, et al. Modulation of inflammatory mediators underlies the antitumor effect of the combination of morusin and docetaxel on prostate cancer cells[J]. Biomed Pharmacother, 2024, 180: 117572.
[5] Wang F, Zhang D, Mao J, et al. Morusin inhibits cell proliferation and tumor growth by down-regulating c-Myc in human gastric cancer[J]. Oncotarget, 2017, 8(34): 57187-57200.
[6] Chen M, Han H, Zhou S, et al. Morusin induces osteogenic differentiation of bone marrow mesenchymal stem cells by canonical Wnt/β-catenin pathway and prevents bone loss in an ovariectomized rat model[J]. Stem Cell Res Ther, 2021, 12(1): 173.
[7] Jia Y, He W, Zhang H, et al. Morusin Ameliorates IL-1β-Induced Chondrocyte Inflammation and Osteoarthritis via NF-κB Signal Pathway[J]. Drug Des Devel Ther, 2020, 14: 1227-1240.
桑辛素(Morusin)是桑科桑白根皮层中发现的一种重要的异戊二烯化黄酮， 在治疗前列腺癌中具有很好的抗肿瘤活性[1]。异戊二烯化黄酮是一类独特的黄酮类化合物，结合了黄酮骨架和亲脂性异戊二烯侧链，具有巨大的潜在生物活性，包括细胞毒性、抗炎、抗阿尔茨海默病、抗糖尿病等作用[2]。桑辛素可作为开发治疗炎性肺病的新型有效粘膜调节剂的候选药物[3]。
在体外，桑辛素（0-10μM）处理PC3细胞48h，通过时间和浓度依赖性显著抑制了细胞的存活率，并降低了炎症细胞因子水平[4]。去血清24h后的NCI-H292细胞经桑辛素（1-100μM）处理30分钟后，桑辛素显著降低了细胞中粘蛋白5AC（MUC5AC）的产生，从而控制伴随粘液分泌过多导致的各种肺部炎症反应[3]。桑辛素（1-5mg/L）处理癌症细胞系（MKN45和SGC7901）72h，以剂量依赖性方式有效抑制癌症细胞的生长和增殖[5]。
在体内，桑辛素（40mg/kg/5days）通过灌胃治疗卵巢切除大鼠28天，可以在一定程度上缓解雌激素缺乏引起的骨质疏松，并减轻卵巢切除大鼠股骨中RUNX2和β-catenin表达[6]。桑辛素（40mg/kg/2days）通过灌胃治疗内侧半月板骨失稳（DMM）模型小鼠56天，能够减轻软骨侵蚀和软骨破坏，并减少相关炎症因子和蛋白的表达水平[7]。