Morusin
(Synonyms: 桑辛素; Mulberrochromene) 目录号 : GN10436
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。
Cas No.:62596-29-6
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
Cell lines | PC3 (Human Prostate Cancer Cells) |
Preparation Method | In 96-well culture plates, PC3 cells were planted at a density of 4×104 cells/well. They were cultured for 24h to allow them to stick to the plates before being subjected to the medications. Serial dilutions of morusin (0, 1.25, 2.5, 5, 10µM) was applied to the cells to measure the inhibitory concentration 50. Following a 48h treatment period, the cells were immobilized by applying 10% trichloroacetic acid at a temperature of 4℃ for a duration of 1h. Afterwards, the cells were treated with Sulforhodamine-B (0.4%) for a duration of 30minutes, then rinsed with 1% acetic acid and allowed to dry in the air. The dye was eliminated by rinsing the plate with a solution of 10mM tris base at a pH of 10.5. Subsequently, the optical density of the wells was quantified at a wavelength of 570nm using an ELISA microplate reader. |
Reaction Conditions | 0, 1.25, 2.5, 5, and 10μM; 48h |
Applications | Morusin significantly inhibited cell viability and reduced levels of inflammatory cytokines. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice (males and females) |
Preparation Method | Mice were randomly divided into three groups (Sham group, DMM group and morusin treated group), and were anesthetized, at which the mice knee joints were carefully, and aseptically, exposed with a scalpel, followed by resectioning of the medial meniscuses. The wound was later sutured carefully, and penicillin was injected intramuscularly for the following 3days. The mourusin-treated group was administered morusin, dissolved in saline (40mg/kg), intragastrically once every 2days for 8weeks; while mice in the Sham and DMM groups received 5% DMSO (dimethyl-sulfoxide) in saline once every 2days for 8weeks. |
Dosage form | 40mg/kg/2days for 56days; Intragastric administration |
Applications | Morusin mitigated cartilage erosion and destruction and decreased the expression levels of associated inflammatory factors and proteins. |
References: | |
| Cas No. | 62596-29-6 | SDF | |
| 别名 | 桑辛素; Mulberrochromene | ||
| 化学名 | 2-(2,4-dihydroxyphenyl)-5-hydroxy-8,8-dimethyl-3-(3-methylbut-2-enyl)pyrano[2,3-h]chromen-4-one | ||
| Canonical SMILES | CC(=CCC1=C(OC2=C3C=CC(OC3=CC(=C2C1=O)O)(C)C)C4=C(C=C(C=C4)O)O)C | ||
| 分子式 | C25H24O6 | 分子量 | 420.47 |
| 溶解度 | ≥ 49.3mg/mL in DMSO | 储存条件 | Store at -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3783 mL | 11.8915 mL | 23.7829 mL |
| 5 mM | 0.4757 mL | 2.3783 mL | 4.7566 mL |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3783 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.50%
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