Moracin M
(Synonyms: 桑辛素M) 目录号 : GC39539
Moracin M 是桑白皮中的一种酚类成分，有效的磷酸二酯酶 4 (PDE4) 抑制剂，对于 PDE4D2，PDE4B2，PDE5A1 和 PDE9A2 的 IC50 分别为 2.9 μM，4.5 μM，> 40 μM 和 > 100 μM。Moracin M 具有抗炎活性。
Cas No.:56317-21-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Moracin M, a phenolic component in the skin of Morus alba L., is a potent phosphodiesterase-4 (PDE4) inhibitor with IC50 values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. Moracin M has anti-inflammatory activity[1].
[1]. Chen SK, et al. Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor. Bioorg Med Chem Lett. 2012 May 1;22(9):3261-4.
| Cas No. | 56317-21-6 | SDF | |
| 别名 | 桑辛素M | ||
| Canonical SMILES | OC1=CC(C2=CC3=CC=C(O)C=C3O2)=CC(O)=C1 | ||
| 分子式 | C14H10O4 | 分子量 | 242.23 |
| 溶解度 | DMSO: 16.67 mg/mL (68.82 mM) | 储存条件 | 4°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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.1283 mL | 20.6415 mL | 41.2831 mL |
| 5 mM | 0.8257 mL | 4.1283 mL | 8.2566 mL |
| 10 mM | 0.4128 mL | 2.0642 mL | 4.1283 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Potential Moracin M Prodrugs Strongly Attenuate Airway Inflammation In Vivo
Biomol Ther (Seoul) 2020 Jul 1;28(4):344-353.PMID:32388942DOI:10.4062/biomolther.2019.212.
This study aims to develop new potential therapeutic Moracin M prodrugs acting on lung inflammatory disorders. Potential Moracin M prodrugs (KW01-KW07) were chemically synthesized to obtain potent orally active derivatives, and their pharmacological activities against lung inflammation were, for the first time, examined in vivo using lipopolysaccharide (LPS)-induced acute lung injury model. In addition, the metabolism of KW02 was also investigated using microsomal stability test and pharmacokinetic study in rats. When orally administered, some of these compounds (30 mg/kg) showed higher inhibitory action against LPSinduced lung inflammation in mice compared to Moracin M. Of them, 2-(3,5-bis((dimethylcarbamoyl)oxy)phenyl)benzofuran-6-yl acetate (KW02) showed potent and dose-dependent inhibitory effect on the same animal model of lung inflammation at 1, 3, and 10 mg/kg. This compound at 10 mg/kg also significantly reduced IL-1β concentration in the bronchoalveolar lavage fluid of the inflamed-lungs. KW02 was rapidly metabolized to 5-(6-hydroxybenzofuran-2-yl)-1,3-phenylene bis(dimethylcarbamate) (KW06) and Moracin M when it was incubated with rat serum and liver microsome as expected. When KW02 was administered to rats via intravenous or oral route, KW06 was detected in the serum as a metabolite. Thus, it is concluded that KW02 has potent inhibitory action against LPS-induced lung inflammation. It could behave as a potential prodrug of Moracin M to effectively treat lung inflammatory disorders.
Moracin M inhibits lipopolysaccharide-induced inflammatory responses in nucleus pulposus cells via regulating PI3K/Akt/mTOR phosphorylation
Int Immunopharmacol 2018 May;58:80-86.PMID:29558663DOI:10.1016/j.intimp.2018.03.015.
Moracin M, a phenolic component obtained from Mori Cortex, has been reported to have anti-inflammatory activities. The present study was designed to investigate the effects and mechanisms of Moracin M on lipopolysaccharide (LPS)-treated nucleus pulposus cells (NPCs) in intervertebral disc. NPCs were treated with Moracin M at different concentrations for 1 h and then stimulated with LPS (0.5 μg/mL) for 24 h. The result demonstrated that Moracin M could significantly inhibit LPS-induced inflammation. The elevated levels of IL-1β, TNF-α and IL-6 induced by LPS could be reversed by Moracin M in NPCs. Moreover, Moracin M increased the expressions of autophagy-related proteins and up-regulated the phosphorylation of PI3K/Akt/mTOR in LPS-treated NPCs. In conclusion, our data demonstrated that Moracin M might inhibit LPS-induced PI3K and Akt phosphorylation, which leading to promote the autophagy and inhibit the inflammatory mediator production in NPCs.
Moracin M inhibits airway inflammation by interrupting the JNK/c-Jun and NF-κB pathways in vitro and in vivo
Eur J Pharmacol 2016 Jul 15;783:64-72.PMID:27138708DOI:10.1016/j.ejphar.2016.04.055.
The therapeutic effectiveness of moracins as 2-arylbenzofuran derivatives against airway inflammation was examined. Moracin M, O, and R were isolated from the root barks of Morus alba, and they inhibited interleukin (IL)-6 production from IL-1β-treated lung epithelial cells (A549) at 101-00μM. Among them, Moracin M showed the strongest inhibitory effect (IC50=8.1μM). Downregulation of IL-6 expression by Moracin M was mediated by interrupting the c-Jun N-terminal kinase (JNK)/c-Jun pathway. Moracin derivatives inhibited inducible nitric oxide synthase (iNOS)-catalyzed NO production from lipopolysaccharide (LPS)-treated alveolar macrophages (MH-S) at 50-100μM. In particular, Moracin M inhibited NO production by downregulating iNOS. When orally administered, Moracin M (20-60mg/kg) showed comparable inhibitory action with dexamethasone (30mg/kg) against LPS-induced lung inflammation, acute lung injury, in mice with that of dexamethasone (30mg/kg). The action mechanism included interfering with the activation of nuclear transcription factor-κB in inflamed lungs. Therefore, it is concluded that Moracin M inhibited airway inflammation in vitro and in vivo, and it has therapeutic potential for treating lung inflammatory disorders.
Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor
Bioorg Med Chem Lett 2012 May 1;22(9):3261-4.PMID:22483586DOI:10.1016/j.bmcl.2012.03.026.
Phosphodiesterase-4 (PDE4) has been identified to be a promising target for treatment of asthma. Moracin M extracted from Chinese herbal drug 'Sang-Bai-Pi' (Morus alba L.) was studied for the inhibitory affinity towards PDE4. It inhibited PDE4D2, PDE4B2, PDE5A1, and PDE9A2 with the IC(50) values of 2.9, 4.5, >40, and >100 μM, respectively. Our molecular docking and 8ns molecular dynamics (MD) simulations demonstrated that Moracin M forms three hydrogen bonds with Gln369, Asn321, and Asp318 in the active site and stacks against Phe372. In addition, comparative kinetics analysis of its analog moracin C was carried out to qualitatively validate their inhibitory potency as predicted by the binding free energy calculations after MD simulations.
Chemistry of trans-resveratrol with singlet oxygen: [2+2] addition, [4+2] addition, and formation of the phytoalexin Moracin M
Org Lett 2011 Sep 16;13(18):4846-9.PMID:21859123DOI:10.1021/ol201922u.
Resveratrol (1) reacts with singlet oxygen by two major pathways: A [2+2] cycloaddition forming a transient dioxetane that cleaves into the corresponding aldehydes and a [4+2] cycloaddition forming an endoperoxide that, upon heating, undergoes a rearrangement to Moracin M. The rate constant by which singlet oxygen is removed by 1 (k(T)) was determined by time-resolved infrared luminescence spectroscopy to be 1.5 × 10(6) M(-1) sec(-1) in CD(3)OD, smaller than previously reported values. Chemical reaction accounts for ca. 25% of k(T).