布洛芬赖氨酸盐

布洛芬赖氨酸盐用途

布洛芬(±)-布洛芬)L-赖氨酸是一种有效的口服活性选择性COX-1抑制剂,IC50值为13μM。布洛芬L-赖氨酸抑制细胞增殖、血管生成并诱导细胞凋亡。布洛芬L-赖氨酸是一种非甾体抗炎剂和一氧化氮(NO)供体。布洛芬L-赖氨酸可用于研究疼痛、肿胀、炎症、感染、免疫学、癌症[1][2][3][4][5][6][7][8]。

点击显示

布洛芬赖氨酸盐名称

[ CAS 号 ]:
57469-77-9

[ 中文名 ]:
赖氨洛芬

[ 英文名 ]:
Ibuprofen Lysine

[中文别名 ]:

[英文别名 ]:

S1518_Selleck
Ibuprofen lysine (USAN)
Ibuprofen Lysinate
NeoProfen
Ibuprofen Lysine
EINECS 260-751-7
MFCD01716155
Neoprofen (TN)

布洛芬赖氨酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

[ 靶点 ]

IC50: 13 μM (COX-1), 370 μM (COX-2)

[体外研究]

布洛芬(24小时)赖氨酸抑制COX-1和COX-2活性,IC50值分别为13μM和370μM[1]。布洛芬(500μM,48小时)L-赖氨酸抑制细胞增殖和血管生成,并诱导AGS细胞(腺癌胃细胞系)[2]。布洛芬(500μM,48小时)L-赖氨酸下调Akt、VEGF-A、PCNA、Bcl2、OCT3/4和CD44基因的转录,但上调AGS细胞中野生型P53和Bax基因的RNA水平[2]。布洛芬(500μM,24小时)L-赖氨酸恢复微管重构、微管依赖性细胞内胆固醇转运,并诱导囊性纤维化(CF)细胞模型和原发性CF鼻上皮细胞中的微管延伸至细胞周边[3]。布洛芬(500μM,24小时)L-赖氨酸通过光敏化过程增强MCF-7细胞和MDA-MB-231细胞中UV诱导的细胞死亡[4]。细胞存活率测定[2]细胞系：AGS细胞浓度：100-1000μM孵育时间：24小时,48小时结果：抑制AGS细胞存活率,IC50值为630μM(台盼蓝染色,24小时)、456微米(中性红染色,24 h)、549微米(台盼兰染色,48小时)和408μM(中性红测定,48小时)。

[体内研究]

在产后乳腺癌模型中,布洛芬(300mg/kg；p.o；每日,共14天)L-赖氨酸可降低总体肿瘤生长并增强抗肿瘤免疫特征,而无不良自身免疫反应[5]。布洛芬(60 mg/kg；i.h；第二天,共15天)L-赖氨酸可降低慢性奥沙利铂诱导的周围神经病变大鼠模型的神经病变风险[6]。布洛芬(20mg/kg；p.o.；每12小时,共5剂)L-赖氨酸减少肌肉生长(平均肌纤维横截面积),而不影响冈上肌腱对运动的适应性调节[7]。布洛芬(35 mg/kg；p.o.；每日两次)L-赖氨酸在慢性肺部感染大鼠模型中减弱对铜绿假单胞菌的炎症反应[8]。动物模型：PPBC(产后)的同基因(D2A1)原位Balb/c小鼠模型[5]剂量：300 mg/kg,每日14天给药：以动物饲料喂养(添加到粉碎的标准食物中,混合干燥,然后与水混合,制成食物颗粒并彻底干燥)。结果：抑制肿瘤生长,减少未成熟单核细胞的存在,增加T细胞的数量。增强Th1相关细胞因子以及促进T细胞的肿瘤边界积聚。动物模型：奥沙利铂诱导的周围神经病变[6]剂量：60 mg/kg,连续15天,第二天给药：皮下注射结果：感觉神经传导速度(SNCV)降低。

[参考文献]

[1]. Noreen Y, et al. Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. J Nat Prod. 1998 Jan;61(1):2-7.

[2]. Hassan Akrami, et al. Inhibitory effect of ibuprofen on tumor survival and angiogenesis in gastric cancer cell. Tumour Biol. 2015 May;36(5):3237-43.

[3]. Sharon M Rymut, et al. Ibuprofen regulation of microtubule dynamics in cystic fibrosis epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2016 Aug 1;311(2):L317-27.

[4]. Emmanuelle Bignon, et al. Ibuprofen and ketoprofen potentiate UVA-induced cell death by a photosensitization process. Sci Rep. 2017 Aug 21;7(1):8885.

[5]. Nathan D Pennock, et al. Ibuprofen supports macrophage differentiation, T cell recruitment, and tumor suppression in a model of postpartum breast cancer. J Immunother Cancer. 2018 Oct 1;6(1):98.

[6]. Thomas Krøigård, et al. Protective effect of ibuprofen in a rat model of chronic oxaliplatin-induced peripheral neuropathy. Exp Brain Res. 2019 Oct;237(10):2645-2651.

[7]. Sarah Ilkhanipour Rooney, et al. Ibuprofen Differentially Affects Supraspinatus Muscle and Tendon Adaptations to Exercise in a Rat Model. Am J Sports Med. 2016 Sep;44(9):2237-45.

[8]. M W Konstan, et al. Ibuprofen attenuates the inflammatory response to Pseudomonas aeruginosa in a rat model of chronic pulmonary infection. Implications for antiinflammatory therapy in cystic fibrosis. Am Rev Respir Dis. 1990 Jan;141(1):186-92.

布洛芬赖氨酸盐物理化学性质

[ 沸点 ]:
319.6ºC at 760 mmHg

[ 分子式 ]:
C₁₉H₃₀N₂O₃

[ 分子量 ]:
352.468

[ 精确质量 ]:
352.236206

[ PSA ]:
95.41000

[ LogP ]:
3.91530

[ 外观性状 ]:
粉末

[ 储存条件 ]:
-20℃

布洛芬赖氨酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OL5672000

CHEMICAL NAME :: L-Lysine, mono(alpha-methyl-4-(2-methylpropyl)benzeneacetate)

CAS REGISTRY NUMBER :: 57469-77-9

LAST UPDATED :: 198702

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C13-H18-O2.C6-H14-N2-O2

MOLECULAR WEIGHT :: 352.53

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 841 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 14,126,1978

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 485 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 14,126,1978

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 299 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 14,126,1978

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 14,126,1978