Cyasterone
(Synonyms: 杯苋甾酮) 目录号 : GC38180
Cyasterone，一种天然的 EGFR 抑制剂，主要分离自 Ajuga decumbens Thunb (Labiatae)。Cyasterone 通过诱导细胞凋亡 (apoptosis) 和细胞周期阻滞表现出抗增殖作用。 Cyasterone 可作为抗人类肿瘤的临床治疗性药物。
Cas No.:17086-76-9
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
Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae).Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a clinical therapeutic anti-tumor agent against human tumors[1].
Cyasterone (0-100μM; 24hours) inhibits cell growth in a concentration-and time-dependent manner, IC50 values are 38.50 mg/mL, 32.96 mg/mL in A549 and MGC823 cells ,respectively[1]. Cell Viability Assay[1] Cell Line: A549, HCT116, MGC823 cells
[1]. Lu X, et al. Anti-proliferation effects, efficacy of cyasterone in vitro and in vivo and its mechanism. Biomed Pharmacother. 2016 Dec;84:330-339.
| Cas No. | 17086-76-9 | SDF | |
| 别名 | 杯苋甾酮 | ||
| Canonical SMILES | C[C@@]12[C@]([C@](C)([C@H](O)C[C@@H]3[C@@H](C)OC([C@H]3C)=O)O)([H])CC[C@@]1(O)C4=CC([C@]5([H])C[C@@H](O)[C@@H](O)C[C@]5(C)[C@@]4([H])CC2)=O | ||
| 分子式 | C29H44O8 | 分子量 | 520.65 |
| 溶解度 | Soluble in DMSO | 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。 |
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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 | 1.9207 mL | 9.6034 mL | 19.2068 mL |
| 5 mM | 0.3841 mL | 1.9207 mL | 3.8414 mL |
| 10 mM | 0.1921 mL | 0.9603 mL | 1.9207 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。
Cyasterone accelerates fracture healing by promoting MSCs migration and osteogenesis
J Orthop Translat 2021 Feb 19;28:28-38.PMID:33717979DOI:10.1016/j.jot.2020.11.004.
Background: Mesenchymal Stem Cells (MSCs) therapy has become a new coming focus of clinical research in regenerative medicine. However, only a small number of implanted MSCs could successfully reach the injured areas. The previous studies have shown that fracture healing time is inversely proportional to concentration of MSCs in injured tissue. Methods: The migration and osteogenesis of MSCs were assessed by transwell assay and Alizarin Red S staining. Levels of gene and protein expression were checked by qPCR and Western Blot. On the other hand, the enhanced migration ability of MSCs induced by Cyasterone was retarded by CXCR4 siRNA. In addition, the rat model of femoral fracture was established to evaluate the effect of Cyasterone on fracture healing. What's more, we also checked the effect of Cyasterone on mobilisation of MSCs in vivo. Results: The results showed that Cyasteron increased the number of MSCs in peripheral blood. The concentrations of SDF-1α in serum at different time points were determined by ELISA assay. Micro-CT and histological analysis were used to evaluate the fractured femurs.Our results showed that Cyasterone could promote the migration and osteogenesis capacities of MSCs. The fractured femurs healed faster with treatment of Cyasterone. Meanwhile, Cyasterone could significantly increase the level of SDF-1α in rats with femur fracture. Conclusion: Cyasterone could promote migration and osteogenesis of MSCs, and most importantly, it could accelerate bone fracture healing.Translational Potential statement: These findings provide evidence that Cyasterone could be used as a therapeutic reagent for MSCs mobilisation and osteogenesis. What's more, it could acclerate fracture healing.
Effect of Cyasterone on intestinal flora in a BRAF V600E-mutant mouse model of colorectal cancer
Pharmazie 2022 Oct 1;77(10):291-294.PMID:36273257DOI:10.1691/ph.2022.2422.
BRAF V600E-mutated colorectal cancer (CRC) is very aggressive and responds poorly to standard treatment. In this study, BRAFV600E-mutant mice with CRC were treated with intragastric Cyasterone, a compound commonly used in traditional Chinese herbal medicine, for 21 days. Microbial DNA was extracted from mouse intestinal contents for 16S ribosomal RNA gene amplicon sequencing and analyzed. Our results indicated that Cyasterone enhanced the diversity of the gut microbiota. The abundance of beneficial bacteria, such as Prevotellaceae, Muribaculaceae, and Ruminococcaceae was significantly higher in cyasterone-treated mice than controls. The abundance of Erysipelotrichaceae, a family of bacteria that promotes inflammation in the gut, was significantly positively correlated with tumor weight. Cyasterone is a potential inhibitor of BRAFV600E-mutant CRC via its effects on intestinal flora.
Anti-proliferation effects, efficacy of Cyasterone in vitro and in vivo and its mechanism
Biomed Pharmacother 2016 Dec;84:330-339.PMID:27668532DOI:10.1016/j.biopha.2016.09.041.
Cyasterone was demonstrated potential inhibition effect in mouse skin carcinoma cells in published report. However, the molecular mechanisms of the Cyasterone on cells remain unknown. Herein, we investigated the effects of cyasterone-induced apoptosis in A549 and MGC823 cells in vitro. MTT assay showed that Cyasterone caused a significantly decreasing of the proliferation of A549 and MGC823 cells in a time-and dose-dependent manner with IC50 values of 38.50±3.73μg/mL on A549 cells and 32.96±1.24μg/mL on MGC823 cells at 48h, respectively. Hoechst staining and TUNEL staining results indicated the quintessential apoptosis features in immunofluorescence image. Apoptosis and cell cycle were determined by flow cytometry. Cyasterone treatment triggered inhibition of epidermal growth factor receptor- phosphatidylinositol 3 kinase/protein kinase B (EGFR-AKT) signaling pathways and activation of P38 pathways. Furthermore, Cyasterone inhibited MGC823 cells xenografted tumor growth in vivo with few changes in body weights. In conclusion, our findings provide the evidence that Cyasterone inhibits growth of A549 and MGC823 cells, via regulating EGFR signaling pathway. Our results indicated that Cyasterone, a natural EGFR inhibitor, maybe a promising anti-cancer agent.
Cyasterone inhibits IL-1β-mediated apoptosis and inflammation via the NF-κB and MAPK signaling pathways in rat chondrocytes and ameliorates osteoarthritisin vivo
Chin J Nat Med 2023 Feb;21(2):99-112.PMID:36871986DOI:10.1016/S1875-5364(23)60388-7.
Osteoarthritis is a prevalent global joint disease, which is characterized by inflammatory reaction and cartilage degradation. Cyasterone, a sterone derived from the roots of Cyathula officinalis Kuan, exerts protective effect against several inflammation-related diseases. However, its effect on osteoarthritis remains unclear. The current study was designed to investigate the potential anti-osteoarthritis activity of Cyasterone. Primary chondrocytes isolated from rats induced by interleukin (IL)-1β and a rat model stimulated by monosodium iodoacetate (MIA) were used for in vitro and in vivo experiments, respectively. The results of in vitro experiments showed that Cyasterone apparently counteracted chondrocyte apoptosis, increased the expression of collagen II and aggrecan, and restrained the production of the inflammatory factors inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), a disintegrin and metalloproteinase with thrombospondin motifs-5 (ADAMTS-5), metalloproteinase-3 (MMP-3), and metalloproteinase-13 (MMP-13) induced by IL-1β in chondrocytes. Furthermore, Cyasterone ameliorated the inflammation and degenerative progression of osteoarthritis potentially by regulating the nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) pathways. For in vivo experiments, Cyasterone significantly alleviated the inflammatory response and cartilage destruction of rats induced by monosodium iodoacetate, where dexamethasone was used as the positive control. Overall, this study laid a theoretical foundation for developing Cyasterone as an effective agent for the alleviation of osteoarthritis.
Structure elucidation of Cyasterone stereoisomers isolated from Cyathula officinalis
Org Biomol Chem 2005 Apr 7;3(7):1227-32.PMID:15785811DOI:10.1039/b416868b.
Chemical investigation of ecdysteroidal constituents of the roots and stems of Cyathula officinalis led to the isolation of two Cyasterone stereoisomers, 2 and 3, together with the known Cyasterone 1. The structures of compounds 2 and 3 were determined to be 28-epi-cyasterone and 25-epi-28-epi-cyasterone, respectively, by means of spectroscopic analysis. X-Ray structures of 1 and 2 confirmed the 24S,25S,28R configuration for 1 and 24S,25S,28S for 2.