Prostaglandin Bx
(Synonyms: PGBx) 目录号 : GC45551
A mixture of PGB1 oligomers with antioxidant and anti-inflammatory activity
Cas No.:39306-29-1
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
PGBx is a mixture of oligomers of PGB1 with a molecular weight of 1,000-1,500. It has antioxidant and free radical trapping activity that was first studied in isolated mitochondria.1 PGBx has anti-inflammatory and cytoprotective activity which may be attributed to inhibition of the 14 kDa sPLA2.2,3 At a dose of 1 mg/kg, PGBx significantly reduces the incidence of ulcers in rats.2
References
1. Polis, B.D., Polis, E., and Kwong, S. Protection and reactivation of oxidative phosphorylation in mitochondria by a stable free-radical prostaglandin polymer (PGBΧ). Proceedings of the National Academy of Sciences of the United States of America 76, 1598-1602 (1979).
2. Kumashiro, R., Devlin, T.M., Kholoussy, A.M., et al. Prostaglandin BΧ in the prevention of stress ulcers in rats. International Surgery 70, 247-250 (1985).
3. Franson, R.C., Rosenthal, M.D., and Regelson, W. Mechanism(s) of cytoprotective and anti-inflammatory activity of PGB1 oligomers: PGBx has potent anti-phospholipase A2 and anti-oxidant activity. Prostaglandins, Leukotrienes and Essential Fatty Acids 43, 63-70 (1991).
| Cas No. | 39306-29-1 | SDF | |
| 别名 | PGBx | ||
| Canonical SMILES | CN(C)[C@@H](C1=CC=CC=C1)[C@H](C)NC(C2=CC=CC=C23)=NN4C3=NN=C4C.Cl.Cl | ||
| 分子式 | (PGB)nn=3-5 | 分子量 | 1 |
| 溶解度 | DMF: >100 mg/ml,DMSO: >100 mg/ml,Ethanol: >100 mg/ml,PBS pH 7.2: 3.8 mg/ml | 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 | 1000 mL | 5000 mL | 10000 mL |
| 5 mM | 200 mL | 1000 mL | 2000 mL |
| 10 mM | 100 mL | 500 mL | 1000 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。
Acute toxicity of Prostaglandin Bx in male, albino, ICR mice
Res Commun Chem Pathol Pharmacol 1982 Jul;37(1):97-104.PMID:7123004doi
Median lethal doses were estimated for PGBx administered to mice by the intraperitoneal and intravenous routes. The incidence of lethality (and therefore the LD50) was time dependent over a 96 hour period. The animals were active, were responsive and took nourishment during the 4-day post-injection period so that they apparently died from the direct effects of PGBx (or its metabolites) and not as a consequence of depression-induced dehydration or starvation.
Prostaglandin Bx in the prevention of stress ulcers in rats
Int Surg 1985 Jul-Sep;70(3):247-50.PMID:3835168doi
The effect of Prostaglandin Bx (PGBx) on the development of gastric stress ulceration and bleeding in rats was investigated. The rats were divided into five groups and each rat was injected intravenously with either Saline (control), 0.5 mg, 1 mg, 5 mg, or 25 mg/kg of PGBx, according to group. The rats were then placed in wire conduit cages and placed in a cold room at 4 degrees C for three hours and sacrificed immediately afterwards. Results showed a significant increase in gastric bleeding and ulceration in the groups that received 1 and 5 mg/kg (PGBx) when compared to the control group (p less than 0.01). There was, however, a significant increase in gastric acid output in the group that received 1 mg/kg PGBx when compared to the control group (p less than 0.01). Our results suggest that PGBx, by a mechanism other than the inhibition of gastric acid secretion, maintains the integrity of the gastric mucosa.
Role of human sperm phospholipase A2 in fertilization: effects of a novel inhibitor of phospholipase A2 activity on membrane perturbations and oocyte penetration
Biol Reprod 1992 Nov;47(5):751-9.PMID:1477202DOI:10.1095/biolreprod47.5.751.
Phospholipase A2 was isolated from human sperm and its potential role in the membrane fusion events of fertilization was examined. Highly purified enzyme hydrolyzed the phospholipids of [1-14C]oleate-labeled Escherichia coli optimally at neutral to alkaline pH with 5 mM CaCl2 and 150 mM NaCl (specific activity = 20 mumol/min/mg). Activity was inhibited in a dose-dependent manner by an oligomer of prostaglandin B1 (IC50 = 1.5 microM) reported to inhibit human phospholipases A2 in vitro and in situ. Sperm phospholipase A2 injected into mouse foot pad induced a dose-dependent edema that was inhibited by oral administration of Prostaglandin Bx (IC50 < or = 10 mg/kg) or by pretreatment of the enzyme with 4-bromophenacyl bromide. Human sperm phospholipase A2 (10 micrograms) induced fusion of phosphatidylserine vesicles in the presence of 1 mM calcium chloride by approximately 80% (+/- 10%) as determined by monitoring turbidity (O.D.400) and efficiency of fluorescence resonance energy transfer. This enzyme-induced fusion was accompanied by phospholipid hydrolysis, and both fusion and phospholipid degradation were inhibited by more than 60% when enzyme was preincubated with 5 microM Prostaglandin Bx. Sperm penetration of zona pellucida-free hamster oocytes was inhibited in a dose-dependent fashion when sperm were incubated with Prostaglandin Bx (IC50 approximately 15 microM) during capacitation; sperm motility was not affected by this treatment. Capacitation in the presence of Prostaglandin Bx had little to no effect on the in vitro acrosome reaction. These results suggest that sperm phospholipase A2 and its modulators may contribute to membrane fusion events in mammalian fertilization.
Prostaglandin derivative PGBx improves neurologic recovery after ischemic spinal injury
Pharm Res 1987 Apr;4(2):130-2.PMID:3509135DOI:10.1023/a:1016466902877.
Neurological dysfunction resulting from an ischemic insult in the central nervous system (CNS) is believed to be an indirect outcome of impaired energy production. Recent studies suggest that Prostaglandin Bx (PGBx), an oligomer of PGB1 and 15-keto-PGB1, may be beneficial in protecting mitochondrial function after ischemic insults by preventing uncoupling of oxidative phosphorylation. In the present study, PGBx had a significant influence on neurological outcome after ischemic injury in the rabbit spinal cord. These findings suggest that PGBx may be beneficial in the treatment of CNS ischemic injuries.
Inhibition of human phospholipases A2 by cis-unsaturated fatty acids and oligomers of prostaglandin B1
Adv Exp Med Biol 1990;279:219-30.PMID:2129000DOI:10.1007/978-1-4613-0651-1_15.
Inhibition of human phospholipases A2 by cis-unsaturated fatty acids and their oxidative metabolites and/or polymers was studied using partially purified human phospholipases A2 and [1-14C]oleate labelled, autoclaved E. coli as substrate. As previously reported for other phospholipases A2, oleic and arachidonic acids inhibited human synovial fluid phospholipase A2 with IC50s of 15 and 30 microM respectively. Air oxidation of arachidonic acid or hydroxylation of oleic acid (12-hydroxy-oleate) substantially relieved that inhibition. Similarly, the enzymatically oxidatized metabolite of arachidonate, prostaglandin B1 (PGB1), did not inhibit enzymatic activity. However, Prostaglandin Bx (PGBx), an oligomer (n = 6) of PGB1, was a potent inhibitor of Ca(++)-dependent, neutral-active phospholipase A2 activities. Enzymatic activity in acid extracts from human neutrophils, platelets, sperm, plasma, synovial fluid, endometrium, degenerative disc, and snake venom was inhibited by PGBx with IC50s ranging from 0.5-7.0 microM. Inhibition was independent of substrate phospholipid concentration over a 24-fold range (5-120 microM) and PGBx quenched the tryptophan fluorescence of snake venom phospholipase A2 in a dose-dependent manner. Agonist-induced (A23187) release of arachidonic acid from prelabelled human neutrophils and cultured human endothelial cells was also inhibited by PGBx with IC50s of 3 and 20 microM, respectively. These results illustrate that oxidative reactions of cis-unsaturated fatty acids relieve their natural inhibitory activity, and polymerization of an inactive fatty acid metabolite yields a potent inhibitor of in vitro and in situ phospholipase A2 activity.