Stachydrine
(Synonyms: 水苏碱) 目录号 : GC37686
A pyrrolidine betaine with anticancer and cardiopro
Cas No.:471-87-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Stachydrine is a pyrrolidine betaine first isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits. It has been shown to be a potent anti-metastatic agent and to have cardioprotective effects against models of cardiac hypertrophy.1
1.Zhang, C., Shan, X.-L., Liao, Y.-L., et al.Effects of stachydrine on norepinephrine-induced neonatal rat cardiac myocytes hypertrophy and intracellular calcium transientsBMC Complement. Altern. Med.14474(2014)
| Cas No. | 471-87-4 | SDF | |
| 别名 | 水苏碱 | ||
| Canonical SMILES | C[N+]1(C)[C@H](C([O-])=O)CCC1 | ||
| 分子式 | C7H13NO2 | 分子量 | 143.18 |
| 溶解度 | Water: 100 mg/mL (698.42 mM); DMSO: 100 mg/mL (698.42 mM) | 储存条件 | Store at -20°C |
| 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 | 6.9842 mL | 34.9211 mL | 69.8422 mL |
| 5 mM | 1.3968 mL | 6.9842 mL | 13.9684 mL |
| 10 mM | 0.6984 mL | 3.4921 mL | 6.9842 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。
Stachydrine hydrochloride inhibits hepatocellular carcinoma progression via LIF/AMPK axis
Phytomedicine 2022 Jun;100:154066.PMID:35366490DOI:10.1016/j.phymed.2022.154066.
Background: Hepatocellular carcinoma (HCC) is not only one of the four highest malignancies, but also the principal reason of cancer-related death worldwide, yet no effective medication for anti-HCC is available. Stachydrine hydrochloride (SH), an alkaloid component in Panzeria alaschanica Kupr, exhibits potent antitumor activity in breast cancer. However, the anti-HCC effects of SH remain unknown. Purpose: Our study assessed the therapeutic effect of SH on HCC and tried to clarify the mechanisms by which it ameliorates HCC. No studies involving using SH for anti-HCC activity and molecular mechanism have been reported yet. Study design/methods: We examined the cell viability of SH on HCC cells by MTT assay. The effect of SH on cell autophagy in HCC cells was verified by Western blot and Immunofluorescence test. Flow cytometry was performed to assess cell-cycle arrest effects. Cell senescence was detected using β-Gal staining and Western blot, respectively. An inhibitor or siRNA of autophagy, i.e., CQ and si LC-3B, were applied to confirm the role of autophagy acted in the anti-cancer function of SH. Protein expression in signaling pathways was detected by Western blot. Besides, molecular docking combined with cellular thermal shift assay (CETSA) was used for analysis. Patient-derived xenograft (PDX) model were built to explore the inhibitory effect of SH in HCC in vivo. Results: In vitro studies showed that SH possessed an anti-HCC effect by inducing autophagy, cell-cycle arrest and promoting cell senescence. Specifically, SH induced autophagy with p62 and LC-3B expression. Flow cytometry analysis revealed that SH caused an obvious cell-cycle arrest, accompanied by the decrease and increase in Cyclin D1 and p27 levels, respectively. Additionally, SH induced cell senescence with the induction of p21 in HCC cell lines. Mechanistically, SH treatment down-regulated the LIF and up-regulated p-AMPK. Moreover, PDX model in NSG mice was conducted to support the results in vitro. Conclusion: This study is the first to report the inhibitory function of SH in HCC, which may be due to the induction of autophagy and senescence. This study provides novel insights into the anti-HCC efficacy of SH and it might be a potential lead compound for further development of drug candidates for HCC.
Stachydrine derived from fermented rice prevents diet-induced obesity by regulating adipsin and endoplasmic reticulum homeostasis
J Nutr Biochem 2022 Sep;107:109036.PMID:35533898DOI:10.1016/j.jnutbio.2022.109036.
Makgeolli, a widely consumed traditional alcoholic beverage in Korea, is brewed mainly from rice using Nuruk as a fermentation starter, which contains fungi, yeast, and lactic acid bacteria. Among 58 Makgeolli samples brewed using various Nuruks, we found that one exhibited anti-obesity properties, with Stachydrine shown to be responsible for these properties. Stachydrine promotes lipolysis and inhibits lipid accumulation in 3T3-L1 adipocytes; it also reduces weight gain and improves glucose tolerance and insulin resistance in a mouse model. Stachydrine dramatically suppresses adipsin mRNA levels in liver and adipose tissue, whereas serum adipsin levels were elevated in stachydrine-treated mice compared to mice fed a high-fat diet alone. Moreover, Stachydrine recovers endoplasmic reticulum homeostasis and regulates adipsin expression. We highlight the potential use of Stachydrine as a therapeutic agent for the treatment of obesity and insulin resistance and the use of Makgeolli fermented by Nuruk as a source of novel bioactive compounds.
Stachydrine, a potential drug for the treatment of cardiovascular system and central nervous system diseases
Biomed Pharmacother 2023 May;161:114489.PMID:36940619DOI:10.1016/j.biopha.2023.114489.
Cardiovascular disease (CVD) is the leading cause of death globally and poses at significant challenge in terms of effective medical treatment. Leonurus japonicus Houtt, a traditional Chinese herb, is widely used in China for the treatment of obstetrical and gynecological disorders, including menstrual disorders, dysmenorrhea, amenorrhea, blood stasis, postpartum bleeding, and blood-related diseases such as CVD. Stachydrine, the main alkaloid component of Leonurus, has been shown to exhibit a wide range of biological activities including anti-inflammatory, antioxidant, anti-coagulant, anti-apoptotic, vasodilator, angiogenic promoter. Additionally, it has been demonstrated to have unique advantages in the prevention and treatment of CVD through regulation of various disease-related signaling pathways and molecular targets. In this comprehensive review, we examine the latest pharmacological effects and molecular mechanisms of Stachydrine in treating cardiovascular and cerebrovascular diseases. Our aim is to solid scientific basis for the development of new CVD drug formulations.
Stachydrine is effective and selective against blast phase chronic myeloid leukaemia through inhibition of multiple receptor tyrosine kinases
Pharm Biol 2022 Dec;60(1):700-707.PMID:35348419DOI:10.1080/13880209.2022.2044862.
Context: Resistance to BCR-ABL tyrosine kinase inhibitor (TKI) is the cause of treatment failure in blast phase chronic myeloid leukaemia (BP-CML). Agents that act synergistically with BCR-ABL TKI are required to improve response. Objective: This work investigated the effects of Stachydrine in CML. Materials and methods: CML cells were treated with control or Stachydrine at 20, 40 and 80 µM. Proliferation and apoptosis were examined after 72 h treatment. Combination studies were performed in four groups: control, TKI, Stachydrine and the combination of Stachydrine and TKI. Immunoblotting analysis was performed in CML cells after 24 h treatment. Results: Stachydrine inhibited K562 (IC50 61 µM), KCL22 (IC50 141 µM), LAMA84 (IC50 86 µM), Ba/F3 T315I (IC50 26 µM), Ba/F3 WT (IC50 22 µM) and KU812 (IC50 35 µM) proliferation, and induced apoptosis in these CML cell lines. Stachydrine significantly induced apoptosis, inhibited colony formation and self-renewal in BP-CML CD34+ cells. The combination index of Stachydrine and TKI combination was <1. Compared to TKI alone, the combination of Stachydrine and TKI significantly induced more apoptosis and decreased colony formation in BP-CML CD34+ cells. Stachydrine decreased phosphorylation levels of multiple receptor tyrosine kinases in CML cells. Discussion and conclusions: Our study is the first to demonstrate (1) the anticancer activity of Stachydrine on primary patient cancer cells; (2) the inhibitory effects of Stachydrine on cancer stem cells; (3) the synergism between Stachydrine and other anticancer drugs.
Stachydrine hydrochloride ameliorates cardiac hypertrophy through CaMKII/HDAC4/MEF2C signal pathway
Am J Transl Res 2022 Jun 15;14(6):3840-3853.PMID:35836883doi
Stachydrine hydrochloride (Sta), an activated alkaloid, is isolated from traditional Chinese medicine Yimucao. In previous studies, the cardioprotective effects of Sta were found in our laboratory. However, the underling mechanisms of Sta is not fully elucidated. The aim of this study was to provide a detailed account of the anti-hypertrophic effects of Sta on transcriptional regulation. In vivo, C57BL/6J mice were subjected to transverse aortic constriction (TAC) and were orally treated with Sta. Morphological assessments, echocardiographic parameters, histological analyses and immunofluorescence were used to evaluate cardiac hypertrophy. In vitro, cardiomyocytes were stimulated by phenylephrine (PE), and cell surface and hypertrophy markers were tested by immunofluorescence and real-time polymerase chain reaction (RT-PCR). Moreover, western blotting, RT-PCR and luciferase reporter genes were used to assess the expression of proteins, mRNA and the activity of the CaMKII/HDAC4/MEF2C signal pathway in vivo and in vitro. We found that Sta blocked cardiac hypertrophy induced by pressure overload. We also demonstrated that Sta inhibited nuclear export or promoted nuclear import of HDAC4 through regulation of p-CaMKII, and it further improved the repression of MEF2C. Taken together, our findings demonstrated that Sta ameliorates cardiac hypertrophy through CaMKII/HDAC4/MEF2C signal pathway.