Batatasin III
(Synonyms: 山药素Ⅲ) 目录号 : GC64377
Batatasin III 是一种芪类化合物，通过抑制上皮间质转化 (EMT) 和FAK-AKT 信号来抑制癌症迁移和侵袭。Batatasin III 具有抗癌活性。
Cas No.:56684-87-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Batatasin III, a stilbenoid, inhibits cancer migration and invasion by suppressing epithelial to mesenchymal transition (EMT) and FAK-AKT signals. Batatasin III has anti-cancer activities[1].
Batatasin III (25-100 μM; 48 h) exhibits anti-proliferative activity in H460 cells. Batatasin III at concentrations lower than 100 μM has no cytotoxic effects[1]. Batatasin III significantly suppresses EMT indicated by the decrease of N-cadherin and Vimentin, and up-regulation of E-cadherin[1].
[1]. Tatchakorn Pinkhien, et al. Batatasin III Inhibits Migration of Human Lung Cancer Cells by Suppressing Epithelial to Mesenchymal Transition and FAK-AKT Signals. Anticancer Res. 2017 Nov;37(11):6281-6289.
| Cas No. | 56684-87-8 | SDF | Download SDF |
| 别名 | 山药素Ⅲ | ||
| 分子式 | C15H16O3 | 分子量 | 244.29 |
| 溶解度 | 储存条件 | 4°C, away from moisture and 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 | 4.0935 mL | 20.4675 mL | 40.935 mL |
| 5 mM | 0.8187 mL | 4.0935 mL | 8.187 mL |
| 10 mM | 0.4093 mL | 2.0467 mL | 4.0935 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。
Batatasin III, a Constituent of Dendrobium scabrilingue, Improves Murine Pain-like Behaviors with a Favorable CNS Safety Profile
J Nat Prod 2022 Jul 22;85(7):1816-1825.PMID:35707966DOI:10.1021/acs.jnatprod.2c00376.
Batatasin III is a stilbenoid compound present in a wide variety of Dendrobium species. Although the pharmacological efficacy of Batatasin III has been reported in several disease models, its antinociceptive efficacy and central nervous system (CNS) side effects remain unknown. Thus, this study examined the effects of Batatasin III on pain-like behaviors in mouse models of formalin- and lipopolysaccharide (LPS)-induced inflammatory pain. The results revealed a significant antinociceptive effect of Batatasin III in both models, as 50 mg/kg Batatasin III elicited comparable antinociception as 10 mg/kg indomethacin. Further, the anti-inflammatory effect of Batatasin III was assessed in LPS-induced RAW 264.7 macrophages and BV-2 microglial cells. The compound significantly reduced the levels of inflammatory mediators (nitric oxide, TNF-α, and IL-6) in LPS-stimulated cells in a concentration-dependent manner. Following efficacy evaluations, the potential CNS side effects of Batatasin III were evaluated using the rotarod test and the Laboratory Animal Behavior Observation, Registration, and Analysis System. Batatasin III-treated mice exhibited comparable forced, spontaneous, and general locomotive behaviors to vehicle-treated mice, indicating no potential CNS side effects. Overall, this study demonstrated the preclinical antinociceptive efficacy and CNS safety of Batatasin III, suggesting its potential role in the development of new analgesics.
Batatasin III Inhibits Migration of Human Lung Cancer Cells by Suppressing Epithelial to Mesenchymal Transition and FAK-AKT Signals
Anticancer Res 2017 Nov;37(11):6281-6289.PMID:29061811DOI:10.21873/anticanres.12079.
Background/aim: Lung cancer is the leading cause of cancer-related deaths worldwide. Compound Batatasin III isolated from Dendrobium draconis Rchb.f. was tested for the possible anti-cancer activities including anti-proliferative, anti-migration and invasion in human non-small lung cancer H460 cells. Materials and methods: The effect of Batatasin III on viability and proliferation of H460 cells was investigated by the 3-[4,5-dimethylthiazol-2-yl]-2,5diphenyl tetrazoliumbromide (MTT) assay. Migration and invasion assays were performed. Filopodia formation was determined by phalloidin-rhodamine staining. The hallmark signaling proteins in regulation of epithelial to mesenchymal transition (EMT), proliferation, and migration were determined by western blot analysis. Results: Batatasin III at concentrations lower than 100 μM has no cytotoxic effects. The compound at 25-100 μM exhibited anti-proliferative activity at 48 h after treatment. Regarding cell motility, Batatasin III decreased migration and invasion of cells. Filopodia were found to be significantly reduced in Batatasin III treated cells. These effects correlated with the results from western blot analysis showing that the phosphorylation of focal adhesion kinase on Try397 (p-FAK (Try397)), the active protein kinase B (AKT), and cell division cycle 42 (CDC42) were significantly reduced. Besides, Batatasin III significantly suppressed EMT indicated by the decrease of N-cadherin and Vimentin, and up-regulation of E-cadherin. Conclusion: Batatasin III has anti-cancer activities; inhibits cancer migration and invasion by suppressing EMT. Our findings establish Batatasin III as a potential compound for further studies aimed at finding a better, more effective treatment approach for lung cancer.
Identification and characterization of the in vitro metabolites of Batatasin III by liquid chromatography in combination with Orbitrap mass spectrometry
Rapid Commun Mass Spectrom 2022 Oct 15;36(19):e9361.PMID:35864564DOI:10.1002/rcm.9361.
Rationale: Batatasin III is a biologically active ingredient extracted from Dendrobium scabrilingue, which has been demonstrated to have anticancer activity. To fully understand its action, the present study was performed to investigate the in vitro metabolism of Batatasin III using rat and human liver microsomes and hepatocytes. Methods: Batatasin III (20 μM) was incubated in the presence of NADPH-supplemented rat and human liver microsomes (0.5 mg protein/mL) and hepatocytes (1 million cells/mL) followed by liquid chromatography in combination with hybrid quadrupole Orbitrap tandem mass spectrometric analysis to detect and identify the generated metabolites. The structures of the metabolites were characterized by comparing the accurate masses, elemental compositions as well as indicative fragment ions with those of the parent. Results: A total of 15 metabolites were detected and identified, including 4 phase I and 11 phase II metabolites. Batatasin III is subjected to bioactivation to form reactive quinoid intermediates, which subsequently react with glutathione (GSH) via Michael addition. Glucuronidation and GSH conjugation appear to be the primary elimination pathways in rat hepatocytes, while in human hepatocytes, GSH conjugates are formed to a lesser extent. Phase I metabolic pathways include hydroxylation and demethylation. Conclusions: The present study sheds light on the in vitro metabolic fates of Batatasin III, which is indispensable for an understanding of its efficacy and safety.
Anti-quorum sensing effects of Batatasin III: in vitro and in silico studies
J Biomol Struct Dyn 2023 Mar 5;1-12.PMID:36871957DOI:10.1080/07391102.2023.2187226.
The spread of multidrug resistant bacteria has fueled the development of new antibiotics to combat bacterial infections. Disrupting the quorum sensing (QS) mechanism with biomolecules is a promising approach against bacterial infections. Plants used in Traditional Chinese Medicine (TCM) represent a valuable resource for the identification of QS inhibitors. In this study, the in vitro anti-QS activity of 50 TCM-derived phytochemicals against the biosensor Chromobacterium violaceum CV026 was tested. Among the 50 phytochemicals, 7-methoxycoumarin, flavone, Batatasin III, resveratrol, psoralen, isopsoralen, and rhein inhibited violacein production and showed good QS inhibitory effects. Batatasin III was selected as the best QS inhibitor based on drug-likeness, physicochemical properties, toxicity, and bioactivity score prediction analyses using SwissADME, PreADMET, ProtoxII, and Molinspiration. At 30 μg/ mL, Batatasin III inhibited violacein production and biofilm formation in C. violaceum CV026 by more than 69% and 54% respectively without affecting bacterial growth. The in vitro cytotoxicity evaluation by MTT assay demonstrated that Batatasin III reduced the viability of 3T3 mouse fibroblast cells to 60% at 100 μg/mL. Furthermore, molecular docking studies showed that Batatasin III has strong binding interactions with the QS-associated proteins CViR, LasR, RhlR, PqsE, and PqsR. Molecular dynamic simulation studies showed that Batatasin III has strong binding interactions with 3QP1, a structural variant of CViR protein. The binding free energy value of batatasin III-3QP1 complex was -146.295 ± 10.800 KJ/mol. Overall results suggested that Batatasin III could serve as a lead molecule that could be developed into a potent QS inhibitor.Communicated by Ramaswamy H. Sarma.
Effects of Batatasin III and Its Analogs on Gibberellic Acid-Dependent α-Amylase Induction in Embryoless Barley Seeds and on Cress Growth
Biosci Biotechnol Biochem 1998;62(8):1619-20.PMID:27388847DOI:10.1271/bbb.62.1619.
The effects of Batatasin III and its analogs on gibberellic acid (GA3)-dependent α-amylase induction in embryoless barley seeds and on cress root-growth were examined. Batatasin III was most effective and caused 68% inhibition of α-amylase induction at 4×10(-4) M, but its potency was low compared with that of abscisic acid. In the cress test, p-hydroxybibenzyl had high activity.