Gossypol是一种从棉花植株中提取的脂溶性多酚类化合物，具有抗生育、抗氧化和抗癌特性。
Cas No.:303-45-7
Sample solution is provided at 25 µL, 10mM.
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Gossypol is a lipid-soluble polyphenolic compound extracted from the cotton plant with antifertility, antioxidant, and anticancer properties [1]. Gossypol can block the release and utilization of ATP in sperm cells, reduce the contents of cytoskeleton and microtubule β-tubulin in spermatogenic cells and sperm cells, and inhibit the calcium influx in the cell membrane of sperm cells, as well as the activities of Mg-ATPase and Ca-Mg-ATPase[2]. Gossypol has been widely used to inhibit the proliferation of various tumor cells and induce mitochondrial dysfunction in cancer cells [3].
In vitro, Gossypol treatment for 12 hours significantly promoted the death of Jurkat cells overexpressing Bcl-2 and Jurkat cells overexpressing Bcl-XL, with IC50 values of 18.1µM and 22.9µM, respectively[4]. Treatment with 80 µM Gossypol for 24 hours significantly induced cell necrosis in U266 cells and enhanced the production of reactive oxygen species and DNA damage[5]. Treatment with 20µM Gossypol for 24 hours significantly induced apoptosis in H1975 cells and inhibited the phosphorylation of EGFR as well as the downstream signaling pathways[6].
In vivo, Gossypol treatment via intraperitoneal injection at a dose of 10mg/kg/day for 4 weeks significantly inhibited tumor growth in the MDA-MB-468 xenograft mouse model and reduced VEGF-mediated angiogenesis[7]. A single intraperitoneal injection of 40mg/kg of Gossypol for 8 hours significantly alleviated lung injury in mice induced by lipopolysaccharide (LPS) and inhibited the production of cytokines[8].
References:
[1] Keshmiri-Neghab H, Goliaei B. Therapeutic potential of gossypol: an overview[J]. Pharmaceutical Biology, 2014, 52(1): 124-128.
[2] Gadelha I C N, Fonseca N B S, Oloris S C S, et al. Gossypol toxicity from cottonseed products[J]. The Scientific World Journal, 2014, 2014(1): 231635.
[3] Paunovic D, Rajkovic J, Novakovic R, et al. The potential roles of gossypol as anticancer agent: Advances and future directions[J]. Chinese Medicine, 2023, 18(1): 163.
[4] Oliver C L, Miranda M B, Shangary S, et al. (−)-Gossypol acts directly on the mitochondria to overcome Bcl-2-and Bcl-XL-mediated apoptosis resistance[J]. Molecular cancer therapeutics, 2005, 4(1): 23-31.
[5] Xu R, Tian E, Tang H, et al. Proteomic analysis of gossypol induces necrosis in multiple myeloma cells[J]. BioMed Research International, 2014, 2014(1): 839232.
[6] Wang Y, Lai H, Fan X, et al. Gossypol inhibits non-small cell lung cancer cells proliferation by targeting EGFRL858R/T790M[J]. Frontiers in pharmacology, 2018, 9: 728.
[7] Xiong J, Li J, Yang Q, et al. Gossypol has anti-cancer effects by dual-targeting MDM2 and VEGF in human breast cancer[J]. Breast Cancer Research, 2017, 19(1): 27.
[8] Liu Z, Yang Z, Fu Y, et al. Protective effect of gossypol on lipopolysaccharide-induced acute lung injury in mice[J]. Inflammation research, 2013, 62(5): 499-506.
Gossypol是一种从棉花植株中提取的脂溶性多酚类化合物，具有抗生育、抗氧化和抗癌特性[1]。Gossypol可阻断精子细胞中ATP的释放和利用，降低生精细胞和精子细胞中细胞骨架及微管蛋白β-微管蛋白的含量，并抑制精子细胞膜上的钙离子内流以及Mg-ATP酶和Ca-Mg-ATP酶的活性[2]。Gossypol已被广泛用于抑制多种肿瘤细胞的增殖，并诱导癌细胞的线粒体功能障碍[3]。
在体外，Gossypol处理12小时显著促进了过表达Bcl-2的Jurkat细胞和过表达Bcl-XL的Jurkat细胞的死亡，IC50值分别为18.1µM和22.9µM[4]。80µM的Gossypol处理U266细胞24小时，显著诱导了细胞坏死，并增强了活性氧的产生和DNA损伤[5]。20µM的Gossypol处理H1975细胞24小时，显著诱导了细胞凋亡，并抑制了EGFR的磷酸化及下游信号通路[6]。
在体内，每日腹腔注射10mg/kg剂量的Gossypol，持续4周，显著抑制了MDA-MB-468异种移植小鼠模型中的肿瘤生长，并减少了VEGF介导的血管生成[7]。单次腹腔注射40mg/kg的Gossypol，作用8小时，显著减轻了脂多糖（LPS）诱导的小鼠肺损伤，并抑制了细胞因子的产生[8]。
| Cell experiment [1]: | |
Cell lines | H1975 cells |
Preparation Method | H1975 cells were grown in RPMI-1640 medium with 10% (v/v) fetal bovine serum (FBS), antibiotic/antimycotic solution at 37°C in 5% CO2/atmosphere. Cells were seeded in 96-well plates at a density of 3×103 cells and cultured overnight. After 72h of treatment with different concentrations of Gossypol (0, 10, 20, 30, 40, and 50µM), the cell viability was measured. |
Reaction Conditions | 0, 10, 20, 30, 40, and 50µM; 72h |
Applications | Gossypol treatment significantly inhibited the cell viability of H1975 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male BALB/c mice |
Preparation Method | Male BALB/c mice (6 weeks old; 18-22g) were housed singly in a standard environment with food and water ad libitum. Gossypol (40mg/kg) was given by intraperitoneal injection (i.p.). Blank control and LPS group mice were given an equal volume of distilled water by i.p. 1h later, mice were slightly anesthetized with an inhalation of diethyl ether, 10μg of LPS in 50μl PBS was instilled intranasally (i.n.) to induce lung injury. Blank control group mice were given a 50μl PBS by i.n. without LPS. All the mice were alive after 7h LPS treatment. The mice were killed by exsanguination at 7h after the administration of LPS. Collection of bronchoalveolar lavage fluid (BALF) for analysis. |
Dosage form | 40mg/kg for once; i.p. |
Applications | Gossypol treatment significantly reduced the production of inflammatory cytokine in in the BALF of LPS-induced mice. |
References: | |
| Cas No. | 303-45-7 | SDF | |
| 别名 | 棉酚; BL 193 | ||
| 化学名 | 7-(8-formyl-1,6,7-trihydroxy-3-methyl-5-propan-2-ylnaphthalen-2-yl)-2,3,8-trihydroxy-6-methyl-4-propan-2-ylnaphthalene-1-carbaldehyde | ||
| Canonical SMILES | CC1=C(C(=C2C(=C1)C(=C(C(=C2C=O)O)O)C(C)C)O)C3=C(C=C4C(=C3O)C(=C(C(=C4C(C)C)O)O)C=O)C | ||
| 分子式 | C30H30O8 | 分子量 | 518.55 |
| 溶解度 | ≥ 25.95mg/mL 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 | 1.9285 mL | 9.6423 mL | 19.2845 mL |
| 5 mM | 385.7 μL | 1.9285 mL | 3.8569 mL |
| 10 mM | 192.8 μL | 964.2 μL | 1.9285 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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