Gossypin
(Synonyms: 棉纤维素) 目录号 : GC60180A flavonoid glycoside with diverse biological activities
Cas No.:652-78-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Gossypin is a flavonoid glycoside originally isolated from H. vitifolius that has diverse biological activities.1,2,3,4,5 It inhibits RANKL-induced osteoclastogenesis in RAW 264.7 cells when used at a concentration of 5 ?M.1 Gossypin inhibits Aurora B kinase (IC50 = 11.07 ?M in a cell-free assay using the human enzyme), as well as Aurora A kinase and p90 ribosomal S6 kinase 2 (RSK2) at 20 ?M.2,3 It induces cell cycle arrest at the G2/M phase and apoptosis in HGC-27 gastric cancer cells.3 Gossypin decreases lactate dehydrogenase (LDH) release induced by the glutathione-depleting agent D,L-buthionine (S,R)-sulfoximine in primary rat cortical cells (IC50 = 7.4 ?g/ml).4 It reduces acetic acid-induced writhing in mice, an effect that can be reversed by the opioid antagonist naloxone, in a dose-dependent manner.5
1.Kunnumakkara, A.B., Nair, A.S., Ahn, K.S., et al.Gossypin, a pentahydroxy glucosyl flavone, inhibits the transforming growth factor beta-activated kinase-1-mediated NF-κB activation pathway, leading to potentiation of apoptosis, suppression of invasion, and abrogation of osteoclastogenesisBlood109(12)5112-5121(2007) 2.Jung, Y., Shin, S.Y., Yong, Y., et al.Plant-derived flavones as inhibitors of aurora B kinase and their quantitative structure-activity relationshipsChem. Biol. Drug Des.85(5)574-585(2015) 3.Wang, L., Wang, X., Chen, H., et al.Gossypin inhibits gastric cancer growth by direct targeting of AURKA and RSK2Phytother. Res.33(3)640-650(2019) 4.Yoon, I., Lee, K.H., and Cho, J.Gossypin protects primary cultured rat cortical cells from oxidative stress- and beta-amyloid-induced toxicityArch. Pharm. Res.27(4)454-459(2004) 5.Viswanathan, S., Sambantham, P.T., Reddy, K., et al.Gossypin-induced analgesia in miceEur. J. Pharmacol.98(2)289-291(1984)
| Cas No. | 652-78-8 | SDF | |
| 别名 | 棉纤维素 | ||
| Canonical SMILES | O=C1C(O)=C(C2=CC=C(O)C(O)=C2)OC3=C(O[C@H]4[C@@H]([C@H]([C@@H]([C@@H](CO)O4)O)O)O)C(O)=CC(O)=C13 | ||
| 分子式 | C21H20O13 | 分子量 | 480.38 |
| 溶解度 | 30 mg/ml in DMF,PBS (pH 7.2) (1:2): 0.3 mg/ml in DMF,25 mg/ml in DMSO | 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 | 2.0817 mL | 10.4084 mL | 20.8169 mL |
| 5 mM | 0.4163 mL | 2.0817 mL | 4.1634 mL |
| 10 mM | 0.2082 mL | 1.0408 mL | 2.0817 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。
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Gossypin: A flavonoid with diverse pharmacological effects
Chem Biol Drug Des 2023 Jan;101(1):131-137.PMID:36198093DOI:10.1111/cbdd.14152.
Gossypin is a flavonoid compound prepared from chinese medicine Hibiscus, which not only has significant pharmacological activities in antioxidant, anti-inflammatory, neuroprotective, anti-cancer, anti-tumor, and anti-diabetic aspects, but also has the advantages of small side effects and easy preparation because it is extracted from traditional chinese medicine, so it has received widespread attention from scholars and researchers. This paper reviews the pharmacological effects and mechanisms of Gossypin in recent years, and hopes to provide a theoretical basis for its clinical application.
Gossypin inhibits gastric cancer growth by direct targeting of AURKA and RSK2
Phytother Res 2019 Mar;33(3):640-650.PMID:30536456DOI:10.1002/ptr.6253.
Gossypin is a flavone extracted from Hibiscus vitifolius, which has been reported to exhibit anti-inflammatory, antioxidant, and anticancer activities. However, the anticancer properties of Gossypin and its molecular mechanism of action against gastric cancer have not been fully investigated. In the present study, we report that Gossypin is an Aurora kinase A (AURKA) and RSK2 inhibitor that suppresses gastric cancer growth. Gossypin attenuated anchorage-dependent and anchorage-independent gastric cancer cell growth as well as cell migration. Based on the results of in vitro screening and cell-based assays, Gossypin directly binds to and inhibits AURKA and RSK2 activities and their downstream signaling proteins. Gossypin decreased S phase and increased G2/M phase cell cycle arrest by reducing the expression of cyclin A2 and cyclin B1 and the phosphorylation of the CDC protein. Additionally, Gossypin also induced intrinsic apoptosis by activating caspases and PARP and increasing the expression of cytochrome c. Our results demonstrate that Gossypin is an AURKA and RSK2 inhibitor that could be useful for treating gastric cancer.
Gossypin-induced analgesia in mice
Eur J Pharmacol 1984 Feb 17;98(2):289-91.PMID:6325219DOI:10.1016/0014-2999(84)90604-6.
A flavonoid, Gossypin, was evaluated for its analgesic action by using acetic acid-induced writhing in mice and was compared with morphine. Gossypin inhibited writhing in a dose-dependent manner. This action was antagonised by naloxone. The pA2 values for morphine-naloxone and gossypin-naloxone were almost identical suggesting a definite involvement of opiate receptors in the analgesic action of Gossypin.
Cardioprotective Effect of Gossypin Against Myocardial Ischemic/Reperfusion in Rats via Alteration of Oxidative Stress, Inflammation and Gut Microbiota
J Inflamm Res 2022 Mar 5;15:1637-1651.PMID:35282267DOI:10.2147/JIR.S348883.
Background: Myocardial ischemic/reperfusion (I/R) injury is a key prognostic factor after the myocardial infarction. However, at the time of reperfusion, the myocardial tissue has undergone for the necrosis and initiated the induction of oxidative stress and inflammation. The current study was to scrutinize the cardioprotective effect of Gossypin against ISO-induced I/R injury in myocardial tissue and explore the possible underlying mechanism. Methods: Sprague Dawley (SD) was used in the current protocol and ISO was used for induction the I/R in rat. The rats were divided into different groups and received the oral administration of Gossypin treatment before the reperfusion. The body weight, heart weight and heart body weight ratio were estimated. The antioxidant, cardiac injury parameters, inflammatory cytokines, inflammatory mediators, gut microbiota and lipid parameters were estimated. At the end, heart tissue histopathological study was carried out. Results: ISO-induced I/R rats received the Gossypin treatment significantly (P < 0.001) enhanced the body weight and decreased the heart weight, along with suppressed the infarct size. Gossypin treatment significantly (P < 0.001) reduced the level of heart parameters, such as creatinine kinase-MB (CK-MB), lactate dehydrogenase (LDH), creatine kinase (CK), cardiac troponin I (CTn-I) and cardiac troponin T (CTn-T) in the serum. Gossypin treatment significantly (P < 0.001) altered the cardiac function, hepatic, antioxidant, inflammatory cytokines and inflammatory mediators. Gossypin significantly (P < 0.001) suppressed the MMP-2 and MMP-9 in ISO-induced I/R rats. Gossypin treatment considerably alleviated the gut dysbiosis through altered Firmicutes to Bacteroidetes (F/B) ratio and also maintained the relative abundance of Butyricicoccus, Clostridium IV, Akkermansia, Roseburia and Clostridium XIVs. Conclusion: Based on result, we can conclude that Gossypin is an alternative drug for the treatment of ISO-induced I/R in rats via alteration of oxidative stress, inflammatory reaction and gut microbiota.
Gossypin induces G2/M arrest in human malignant glioma U251 cells by the activation of Chk1/Cdc25C pathway
Cell Mol Neurobiol 2012 Mar;32(2):289-96.PMID:21984341DOI:10.1007/s10571-011-9760-8.
Gossypin is a flavone that was originally isolated from Hibiscus vitifolius and has traditionally been used for the treatment of diabetes, jaundice, and inflammation. Recently, Gossypin was found to have potent anticancer properties; however, its effect on human gliomas still remain unknown. To investigate the potential anticancer effects of Gossypin on malignant gliomas and analyze the associated molecular mechanisms, we treated human glioma U251 cells with Gossypin. Our study showed that the treatment of U251 cells with Gossypin inhibited cell proliferation in a dose- and time-dependent manner and was observed to be minimally toxic to normal human astrocytes. Gossypin's effect on cell cycle distribution was observed, and we found that it induced G2/M-phase arrest in U251 cells. An analysis of cell-cycle regulatory proteins indicated that the arresting effect of Gossypin on the cell cycle at G2/M phase was involved in the phosphorylation of cell division cycle 25C (Cdc25C) tyrosine phosphatase via the activation of checkpoint kinase 1 (Chk1). These findings indicate that Gossypin is a potential treatment of gliomas because of Gossypin's potential to regulate the proliferation of U251 cells via the cell-cycle regulatory proteins Chk1 and Cdc25C.