Background
Betamethasone is a glucocorticoid steroid with anti-inflammatory and immunosuppressive properties.Target: Glucocorticoid ReceptorBetamethasone is a potent glucocorticoid steroid with anti-inflammatory and immunosuppressive properties. Unlike other drugs with these effects, betamethasone does not cause water retention. The median (range) IC50 value for betamethasone butyrate propionate evaluated in the streptococcal pyrogenic enterotoxin A-stimulated peripheral-blood mononuclear cells was 291.6 (0.001-1171.5) ng/ml, which was significantly higher than the value 0.072 (0.01-222.5) ng/ml found in concanavalin A-stimulated peripheral-blood mononuclear cells (P=0.0245) [1]. Children exposed prenatally to betamethasone (n = 121) did not differ in systolic or diastolic blood pressure from children exposed to placebo (n = 102) (mean difference: systolic: -1.6 mm Hg; 95% confidence interval: -4.1 to 0.8 mm Hg; diastolic: -0.3 mm Hg; 95% confidence interval: -2.5 to 1.8 mm Hg) [2]. Intra-articular corticosteroid injection of 6 mg of betamethasone acetate/betamethasone sodium phosphate at the knee joint was not significantly associated with SAI at the time points tested [3].Clinical indications: Dermatitis; Discoid lupus erythematosus; Eczema; Lichen; Prurigo; PsoriasisToxicity: Symptoms of overdose include burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, and miliaria.
参考文献:
[1]. Arai, K., et al., Comparative study of the effects of betamethasone butyrate propionate, vitamin D3 derivatives, and cyclosporine on human lymphocyte-proliferation stimulated with a hemolytic streptococci-derived superantigen. Eur J Pharmacol, 2007. 571(2-3): p. 222-30.
[2]. Dalziel, S.R., et al., Blood pressure at 6 years of age after prenatal exposure to betamethasone: follow-up results of a randomized, controlled trial. Pediatrics, 2004. 114(3): p. e373-7.
[3]. Habib, G., et al., The effect of intra-articular injection of betamethasone acetate/betamethasone sodium phosphate at the knee joint on the hypothalamic-pituitary-adrenal axis: a case-controlled study. J Investig Med, 2013. 61(7): p. 1104-7.
Protocol
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Cell experiment [1]:
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Cell lines
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Human astrocytoma
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Preparation method
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The solubility of this compound in DMSO is >19.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
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Reacting condition
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10 μg/ml
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Applications
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Bexamethasone (1.3-50 μg/ml) decreased cloning efficiency and colony size in cultured human astrocytoma. In MRC5 human diploid fibroblasts, betamethasone (8 μg/ml) increased cloning efficiency by two-fold. Betamethasone (2-16 μg/ml) did not affect colony size.
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Animal experiment [2,3]:
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Animal models
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Pregnant rabbits, Pregnant ewes
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Dosage form
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0.5 mg/kg
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Application
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Pregnant rabbits were injected with either 0.8 mg of betamethasone on days 24 and 25 of gestation and delivered by cesarean section on day 26. Bexamethasone significantly reduced the weight of fetuses and fetal brain, lungs, liver, and placenta. In pregnant ewes, BET (0.5 mg/kg) decreased fetal (121–146 dG) and placental (121 dG) weights. Maternal plasma oPL levels in controls increased across gestation; fetal plasma oPL levels decreased. BNCs were reduced by 24% to 47% after BET. Placental oPL protein levels, maternal and fetal plasma oPL levels were also reduced after BET injections, but recovered to values that were not different to controls near term. BET (0.5 mg/kg) disrupted the normal distribution of BNCs within the placentome.
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Other notes
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Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
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参考文献:
[1]. Guner M, Freshney R I, Morgan D, et al. Effects of dexamethasone and betamethasone on in vitro cultures from human astrocytoma[J]. British journal of cancer, 1977, 35(4): 439.
[2]. Barrada M I, Blomquist C H, Kotts C. The effects of betamethasone on fetal development in the rabbit[J]. American journal of obstetrics and gynecology, 1980, 136(2): 234-238.
[3]. Braun T, Li S, Moss T J M, et al. Maternal betamethasone administration reduces binucleate cell number and placental lactogen in sheep[J]. Journal of Endocrinology, 2007, 194(2): 337-347.
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