Meranzin (hydrate)
(Synonyms: 橙皮内酯水合物) 目录号 : GC36584
A coumarin with diverse biological activities
Cas No.:5875-49-0
Sample solution is provided at 25 µL, 10mM.
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Meranzin is a coumarin that has been found in Murraya exotica and has diverse biological activities.1,2 It is cytotoxic to NSCLC-N6 and KB cancer cells (IC50s = 14.6 and 12.3 ?g/ml, respectively).2 Meranzin (10 mg/kg) increases the latency to paw withdrawal in the hot plate test and reduces xylene-induced ear edema in mice.1 It decreases paw edema induced by carrageenan in rats when administered at the same dose.
1.Wu, L., Li, P., Wang, X., et al.Evaluation of anti-inflammatory and antinociceptive activities of Murraya exoticaPharm. Biol.48(12)1344-1353(2010) 2.Kofinas, C., Chinou, L., Loukis, A., et al.Cytotoxic coumarins from the aerial parts of Tordylium apulum and their effects on a non-small-cell bronchial carcinoma cell linePlanta Med.64(2)174-176(1998)
| Cas No. | 5875-49-0 | SDF | |
| 别名 | 橙皮内酯水合物 | ||
| Canonical SMILES | CC(C)(O)[C@@H](O)CC1=C(O2)C(C=CC2=O)=CC=C1OC | ||
| 分子式 | C15H18O5 | 分子量 | 278.3 |
| 溶解度 | DMSO : 100 mg/mL (359.32 mM; Need ultrasonic) | 储存条件 | Store at 2-8°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 | 3.5932 mL | 17.9662 mL | 35.9324 mL |
| 5 mM | 0.7186 mL | 3.5932 mL | 7.1865 mL |
| 10 mM | 0.3593 mL | 1.7966 mL | 3.5932 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。
Meranzin hydrate elicits antidepressant effects and restores reward circuitry
Behav Brain Res 2021 Feb 1;398:112898.PMID:32905810DOI:10.1016/j.bbr.2020.112898.
The burden of depression is enormous, and numerous studies have found that major depressive disorder (MDD) induces cardiovascular disorders (CVD) and functional dyspepsia (FD). Excitingly, Meranzin hydrate (MH), an absorbed bioactive compound of Aurantii Fructus Immaturus, reverses psychosocial stress-induced mood disorders, gastrointestinal dysfunction and cardiac disease. Pharmacological methods have repeatedly failed in antidepressant development over the past few decades, but repairing aberrant neural circuits might be a reasonable strategy. This article aimed to explore antidepressant-like effects and potential mechanisms of MH in a rat model of unpredictable chronic mild stress (UCMS). Utilizing blood oxygen level-dependent (BOLD) functional magnetic resonance imaging (fMRI), we sought to find reliable neurocircuits or a dominant brain region revealing the multiple effects of MH. The results show that compared with UCMS rats, MH (10 mg/kg/day for 1 week i.g.)-treated rats exhibited decreased depression-like behaviour; increased expression of brain-derived neurotrophic factor (BDNF) in the hippocampal dentate gyrus; and normalized levels of adrenocorticotropic hormone (ACTH), corticosterone (CORT), and acylated ghrelin (AG). Additionally, the UCMS-induced rise in BOLD activation in the reward system was attenuated after MH treatment. A literature search shown that nucleus accumbens (NAc) and hypothalamus of the reward system might reveal multiple effects of MH on MDD-FD-CVD comorbidity. Further research will focus on the role of these two brain regions in treating depression associated with comorbidities.
Meranzin hydrate Improves Depression-Like Behaviors and Hypomotility via Ghrelin and Neurocircuitry
Chin J Integr Med 2022 Jul 26.PMID:35881212DOI:10.1007/s11655-022-3308-2.
Objective: To investigate whether Meranzin hydrate (MH) can alleviate depression-like behavior and hypomotility similar to Chaihu Shugan Powder (CSP), and further explore the potential common mechanisms. Methods: Totally 120 Spraque-Dawley rats were randomly divided into 5-8 groups including sham, vehicle, fluoxetine (20 mg/kg), mosapride (10 mg/kg), CSP (30 g/kg), MH (9.18 mg/kg), [D-Lys3]-GHRP-6 (Dlys, 0.5 mg/kg), and MH+Dlys groups by a random number table, 8 rats in each group. And 32 mice were randomly divided into wild-type, MH (18 mg/kg), growth hormone secretagogue receptor-knockout (GHSR-KO), and GHSR+MH groups, 8 mice in each group. The forced swimming test (FST), open field test (OFT), tail suspension test (TST), gastric emptying (GE) test, and intestinal transit (IT) test were used to assess antidepressant and prokinetic (AP) effects after drug single administration for 30 min with absorbable identification in rats and mice, respectively. The protein expression levels of brain-derived neurotrophic factor (BDNF) and phosphorylated mammalian target of rapamycin (p-mTOR) in the hippocampus of rats were evaluated by Western blot. The differences in functional brain changes were determined via 7.0 T functional magnetic resonance imaging-blood oxygen level-dependent (fMRI-BOLD). Results: MH treatment improved depression-like behavior (FST, OFT) and hypomotility (GE, IT) in the acute forced swimming (FS) rats (all P<0.05), and the effects are similar to the parent formula CSP. The ghrelin antagonist [D-Lys3]-GHRP-6 inhibited the effect of MH on FST and GE (P<0.05). Similarly, MH treatment also alleviated depression-like behavior (FST, TST) in the wild-type mice, however, no effects were found in the GHSR KO mice. Additionally, administration of MH significantly stimulated BDNF and p-mTOR protein expressions in the hippocampus (both P<0.01), which were also prevented by [D-Lys3]-GHRP-6 (P<0.01). Besides, 3 main BOLD foci following acute FS rats implicated activity in hippocampus-thalamus-basal ganglia (HTB) circuits. The [D-Lys3]-GHRP-6 synchronously inhibited BOLD HTB foci. As expected, prokinetic mosapride only had effects on the thalamus and basal ganglia, but not on the hippocampus. Within the HTB, the hippocampus is implicated in depression and FD. Conclusions: MH accounts for part of AP effects of parent formula CSP in acute FS rats, mainly via ghrelin-related shared regulation coupled to BOLD signals in brain areas. This novel functionally connection of HTB following acute stress, treatment, and regulation highlights anti-depression unified theory.
Effects of Meranzin hydrate On the LncRNA-miRNA-mRNA Regulatory Network in the Hippocampus of a Rat Model of Depression
J Mol Neurosci 2022 Apr;72(4):910-922.PMID:35099722DOI:10.1007/s12031-022-01971-6.
Meranzin hydrate (MH) is a frequently used antidepressant drug in China; however it underlying mechanism remains unknown. In this study, we aimed to explore whether MH could ameliorate depression-like behavior in rats by regulating the competitive endogenous RNA (ceRNA) network. We developed a depression-like rat model using an unpredictable chronic mild stress (UCMS) protocol, and the differentially expressed lncRNAs, miRNAs, and mRNAs were identified between the model group and MH group. Then, a ceRNA network responding to MH treatment was constructed by their corresponding relationships in the databases. Finally, Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analyses were conducted to explore molecular mechanisms associated with MH treatment. The study indicated that rats in the model group showed loss of weight and deteriorated behavior in behavior tests compared with rats in the normal group. A total of 826 lncRNAs, 121 miRNAs, and 954 mRNAs were differentially expressed in the hippocampus of UCMS rats after MH treatment. In addition, 13 miRNAs were selected, and 12 of them were validated in the hippocampus by qRT-PCR. Then, we predicted upstream lncRNAs and downstream mRNAs of the validated miRNAs and interacted with the results of microarrays. Eventually, a lncRNA-miRNA-mRNA regulatory network, responding to MH treatment, was constructed based on the 314 lncRNAs, 11 miRNAs, and 221 mRNAs. KEGG pathways suggested that these genes may be highly related to Wnt signaling, axon guidance, and MAPK signaling pathways. All these results suggest that MH may be a potential representative compound for the treatment of depression, and its mechanism of action is related to the ceRNA modification.
Meranzin hydrate from Muraya paniculata
Acta Crystallogr Sect E Struct Rep Online 2010 Feb 13;66(Pt 3):o620.PMID:21580378DOI:10.1107/S1600536810005386.
The coumarin ring system in the title compound, C(15)H(18)O(5) [IUPAC name: 8-(2,3-dihydr-oxy-3-methyl-butyl)-7-meth-oxy-2H-1-benzopyran-2-one], isolated from Muraya paniculata, is planar (r.m.s. deviation 0.017 Å). In the crystal, the two hydr-oxy groups are involved in O-H⋯O hydrogen bonding with adjacent mol-ecules, forming a sheet structure.
Meranzin hydrate induces similar effect to Fructus Aurantii on intestinal motility through activation of H1 histamine receptors
J Gastrointest Surg 2011 Jan;15(1):87-96.PMID:21061180DOI:10.1007/s11605-010-1374-9.
This experiment studied the potential effect of Meranzin hydrate (MH) and decoction of herb Fructus Aurantii (FA) on rat gut motility. It also investigated the prokinetic mechanism of MH. Experiments were performed on male Sprague–Dawley rats (200–220 g). The study included: (1) qualitation of MH and four other known compounds in FA and jejunum after oral administration of FA decoction to rats; (2) in vitro experiment of MH on rat jejunum contractions; (3) in vivo experiment of FA and MH in rats. Dose-dependently, MH (1–100 μM) increased amplitude in longitudinal and circular jejunum muscles. Pretreatment of jejunum longitudinal strips with benzhydramine (1 μM) remarkably inhibited the contractions induced by histamine (1 μM) and MH (10 or 30 μM). Pretreatment of jejunum longitudinal strips with atropine (1 μM) reduced the contractions induced by acetylcholine (1 μM) but did not influence the contractions induced by MH (10 or 30 μM). Interestingly, the antagonism of benzhydramine to MH was also verified in vivo. MH can be absorbed into the jejunum following oral administration of FA decoction. In healthy rats, MH (7, 14, and 28 mg/kg) and FA (3.3, 10, and 20 g/kg) both promoted intestinal transit and gastric emptying in a dose-dependent manner when gavaged acutely. In cisplatin model rats, MH (14 and 28 mg/kg) significantly reversed cisplatin-induced delay in gastric emptying. Meranzin hydrate can induce similar effect to Fructus Aurantii on intestinal motility and it was, at least in part, mediated by stimulation of H1 histamine receptors.