Brevetoxin 3
(Synonyms: PbTx-3) 目录号 : GC49740
A neurotoxin
Cas No.:85079-48-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Brevetoxin 3 is a neurotoxin produced by the dinoflagellate K. brevis.1,2 It binds to site 5 of voltage-gated sodium channels (Navs), prolonging the mean open time and inhibiting inactivation of these channels.2 Brevetoxin 3 induces the release of lactate dehydrogenase (LDH), L-glutamate, and L-aspartate from primary rat cerebellar granule neurons (CGNs; EC50s = 30.9, 45.3, and 50.2 nM, respectively).3 It induces convulsions in, and is lethal to (LD50 = 4 ng/egg), Japanese rice fish embryos.1 Brevetoxin 3 has been found in water samples collected during red tide blooms.4
1.Colman, J.R., and Ramsdell, J.S.The type B brevetoxin (PbTx-3) adversely affects development, cardiovascular function, and survival in Medaka (Oryzias latipes) embryosEnviron. Health Perspect.111(16)1920-1925(2003) 2.Jeglitsch, G., Rein, K.S., Baden, D.G., et al.Brevetoxin-3 (PbTx-3) and its derivatives modulate single tetrodotoxin-sensitive sodium channels in rat sensory neuronsJ. Pharmacol. Exp. Ther.284(2)516-525(1997) 3.Berman, F.W., and Murray, T.F.Brevetoxins cause acute excitotoxicity in primary cultures of rat cerebellar granule neuronsJ. Pharmacol. Exp. Ther.290(1)439-444(1999) 4.Pierce, R.H., and Henry, M.S.Harmful algal toxins of the Florida red tide (Karenia brevis): Natural chemical stressors in South Florida coastal ecosystemsEcotoxicology17(7)623-631(2008)
| Cas No. | 85079-48-7 | SDF | Download SDF |
| 别名 | PbTx-3 | ||
| Canonical SMILES | C[C@@]12[C@](C[C@@]3([H])[C@](O2)(CC[C@@]4([H])[C@]([C@@H](C[C@@]5([H])[C@](C[C@]6([C@](C[C@@]7([H])[C@](C(C)=CC(O7)=O)([H])O6)([H])O5)C)([H])O4)C)([H])O3)C)([H])O[C@@]8([C@@](O[C@]9([H])[C@@](O[C@]%10([H])[C@@](O[C@@]%11([C@@](O[C@@H](C[C@@H]%11O)CC(CO)=C)([H])C%10)C)([H])C9)([H])C=CC8)([H])C1)C | ||
| 分子式 | C50H72O14 | 分子量 | 897.1 |
| 溶解度 | DMSO: soluble,Ethanol: soluble,Methanol: soluble | 储存条件 | -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 | 1.1147 mL | 5.5735 mL | 11.147 mL |
| 5 mM | 0.2229 mL | 1.1147 mL | 2.2294 mL |
| 10 mM | 0.1115 mL | 0.5574 mL | 1.1147 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。
Detection of Brevetoxin in Human Plasma by ELISA
J Anal Toxicol 2022 Mar 21;46(3):322-327.PMID:33515246DOI:10.1093/jat/bkab010.
Florida red tides have become more common and persistent in and around the Gulf of Mexico. When in bloom, red tides can produce brevetoxins in high concentrations, leading to human exposures primarily through contaminated food and ocean spray. The research described here includes adapting and validating a commercial brevetoxin water test kit for human plasma testing. Pooled plasma was fortified with a model brevetoxin, Brevetoxin 3, at concentrations from 0.00500 to 3.00 ng/mL to generate calibration curves and quality control samples. The quantitative detection range was determined to be 0.0400-2.00 ng/mL Brevetoxin 3 equivalents with inter- and intraday accuracies ranging from 94.0% to 109% and relative standard deviations <20%, which is within the US Food and Drug Administration guidelines for receptor-binding assays. Additionally, cross-reactivity was tested using 4 of the 10 known brevetoxins and 12 paralytic shellfish toxins. The cross-reactivity varied from 0.173% to 144% for the commercially available brevetoxin standards and 0% for the commercially available paralytic shellfish toxin standards. Fifty individual unexposed human plasma samples were measured to determine the limit of detection and endogenous interferences to the test. The validated method was used to test 31 plasma samples collected from humans potentially exposed to brevetoxins, detecting 11 positives. This method has been proven useful to measure human exposure to brevetoxins and can be applied to future exposure events.
Inhalation toxicity of Brevetoxin 3 in rats exposed for 5 days
J Toxicol Environ Health A 2004 Sep 24;67(18):1443-56.PMID:15371231DOI:10.1080/15287390490483809.
Brevetoxins are potent neurotoxins produced by the marine dinoflagellate Karenia brevis. Exposure to brevetoxins may occur during a K. brevis red tide when the compounds become aerosolized by wind and surf. This study assesses possible adverse health effects associated with short-term inhalation exposure to Brevetoxin 3. Male F344/Crl/Br rats were exposed to 500 microg Brevetoxin 3/m3 by nose-only inhalation for 0.5 or 2 h/d for 5 consecutive days. Control rats were sham exposed for 2 h to vehicle. Calculated deposited brevetoxin doses were 8.3 and 33 microg/kg/d for the low- and high-dose groups, respectively. At the termination of exposures, only body weights of the high-dose group (Group B) were significantly below control values. By immunohistochemistry (IHC), small numbers of splenic and peribronchiolar lymphoid tissue macrophages stained positive for brevetoxin, while nasal mucosa, liver, and brain were IHC negative for brevetoxin. No gross or microscopic lesions were observed in any tissue examined. There was no biochemical evidence of cytotoxicity or inflammation in bronchoalveolar lavage fluid. Alveolar macrophages showed some evidence of activation following brevetoxin exposure. Humoral-mediated immunity was suppressed in brevetoxin-exposed rats as indicated by a >70% reduction in splenic plaque-forming cells in brevetoxin-exposed animals compared to controls. Results suggest that the immune system may be a target of toxicity following brevetoxin inhalation. Future studies will focus on identification of a no-effect level and mechanisms underlying brevetoxin-induced immune suppression.
Uptake, tissue distribution, and excretion of Brevetoxin 3 administered to rats by intratracheal instillation
J Toxicol Environ Health A 1999 Jul 9;57(5):345-55.PMID:10405188DOI:10.1080/009841099157656.
Brevetoxins are cyclic polyether neurotoxins produced by the marine dinoflagellate Ptychodiscus brevis. Blooms of P. brevis (red tides) are toxic to fish, marine mammals, and humans. Humans exposed to seaspray aerosols containing brevetoxins may experience respiratory tract irritation. Because a major route of human exposure to brevetoxins is via the respiratory tract, the objective of this study was to examine the toxicokinetics of Brevetoxin 3 (PbTx-3) administered to the lung by intratracheal instillation. Twenty-one male F344/Crl BR rats, 12 wk of age, were administered 3H-PbTx-3 (1 microCi, 6.6 microg PbTx-3/kg) by intratracheal instillation. Groups of 3 rats were sacrificed at 0.5, 3, 6, 24, 48, and 96 h after exposure, and tissues were collected. Three additional rats were placed in glass metabolism cages for collection of urine and feces over a 7-d period. PbTx-3-associated activity was cleared rapidly from the lung and distributed throughout the body, chiefly to the carcass, intestines, and liver. Blood, brain, and fat contained the lowest percentages of the administered dose. Although a majority of the PbTx-3 was cleared rapidly from lung, liver, and kidneys, approximately 20% of the initial concentration present in each organ was retained for 7 d. Concentrations of PbTx-3 in brain and fat were low, but remained relatively constant over time. Approximately twice as much PbTx-3-associated activity was excreted in feces than in urine, with the majority of excretion occurring within 48 h after instillation. The results of this study indicate that over 80% of the PbTx-3 is rapidly absorbed from the lung to the blood and distributed to all tissues. The tissues containing the greatest amount of PbTx-3-associated activity reflect the compound's site of deposition, storage compartment, and major route of metabolism and excretion. These results illustrate that brevetoxin exposure by the respiratory route results in systemic distribution of brevetoxin and suggest that the initial respiratory irritation and bronchoconstriction may only be a part of the overall toxicological consequences associated with brevetoxin inhalation.
Inhalation toxicity of Brevetoxin 3 in rats exposed for twenty-two days
Environ Health Perspect 2005 May;113(5):626-31.PMID:15866775DOI:10.1289/ehp.7497.
Brevetoxins are potent neurotoxins produced by the marine dinoflagellate Karenia brevis. Exposure to brevetoxins may occur during a K. brevis red tide when the compounds become aerosolized by wind and surf. This study assessed possible adverse health effects associated with inhalation exposure to Brevetoxin 3, one of the major brevetoxins produced by K. brevis and present in aerosols collected along beaches affected by red tide. Male F344 rats were exposed to Brevetoxin 3 at 0, 37, and 237 microg/m3 by nose-only inhalation 2 hr/day, 5 days/week for up to 22 exposure days. Estimated deposited Brevetoxin 3 doses were 0.9 and 5.8 microg/kg/day for the low- and high-dose groups, respectively. Body weights of the high-dose group were significantly below control values. There were no clinical signs of toxicity. Terminal body weights of both low- and high-dose-group rats were significantly below control values. Minimal alveolar macrophage hyperplasia was observed in three of six and six of six of the low- and high-dose groups, respectively. No histopathologic lesions were observed in the nose, brain, liver, or bone marrow of any group. Reticulocyte numbers in whole blood were significantly increased in the high-dose group, and mean corpuscular volume showed a significant decreasing trend with increasing exposure concentration. Humoral-mediated immunity was suppressed in brevetoxin-exposed rats as indicated by significant reduction in splenic plaque-forming cells in both low- and high-dose-group rats compared with controls. Results indicate that the immune system is the primary target for toxicity in rats after repeated inhalation exposure to relatively high concentrations of brevetoxins.
Brevetoxin-induced neural insult in the retrosplenial cortex of mouse brain
Inhal Toxicol 2006 Dec;18(14):1109-16.PMID:17043031DOI:10.1080/08958370600945804.
Brevetoxins (polyether breve toxins; PbTx) are polyether neurotoxins produced by the marine dinoflagellate Karenia brevis, an organism associated with red tide blooms in the Gulf of Mexico and along the Atlantic coast from Florida to North Carolina. Brevetoxin-3 (PbTx-3) is a major component of the array of brevetoxins found in marine aerosols measured along red tide affected beaches. Humans exposed to aerosolized brevetoxins for short periods of time often suffer a variety of adverse health effects. It was consequently of interest to assess the potential for aerosolized brevetoxin to produce a neurotoxic response. Female BALB/c mice were exposed nose-only for 2 consecutive days to PbTx-3 aerosol, with a 2-h exposure on the first day and a 4-h exposure on the second day. The average PbTx-3 exposure concentrations on days 1 and 2 were 312 +/- 113 mug Brevetoxin 3/m3 and 278 +/- 24 mug Brevetoxin 3/m3, respectively. The brevetoxin-containing aerosol had a mass median aerodynamic diameter of 0.92 mum with a geometric standard deviation of 1.38. Coronal sections of mouse brains were evaluated for neuronal damage using both silver and Fluoro-Jade B staining to identify degenerating neuronal elements. PbTx-3 inhalation exposure produced neuronal degeneration in the posterior cingulate/retrosplenial cortex of mice as evidenced by silver-positive degenerating neurons in this region. No staining was found in other regions of the PBTx-3-exposed mouse brains or in brains of control, sham-exposed mice. The existence of a neurotoxic insult in PbTx-3-exposed mice was confirmed using Fluoro-Jade B to label degenerating neurons. Fluro-Jade-positive neurons were observed in the retrosplenial cortex of PBTx-3 exposed, but not control, mice. These results suggest that subacute exposure to PbTx-3 for 2 days is sufficient to induce neuronal degeneration in a discrete region of the mouse cerebral cortex.