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烟酰胺

烟酰胺用途

Nicotinamide是一种B3维生素,通过促进NAD +氧化还原稳态和提供NAD +作为催化非氧化还原反应的一类酶的底物,在细胞生理学中发挥重要作用。烟酰胺是 SIRT1 的抑制剂。

烟酰胺名称

[ CAS 号 ]:
98-92-0

[ 中文名 ]:
烟酰胺

[ 英文名 ]:
Nicotinamide

[中文别名 ]:

[英文别名 ]:

Niacinamide
MFCD00006395
Nicotinic acid amide
Vitamin- B3
Witamina PP
3-Pyridinecarboxamide
Nicotinamide
Pyridine-3-carboxamide
T6NJ CVZ
Dipigyl

烟酰胺生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 抗衰老酶

信号通路 >> 表观遗传学 >> 抗衰老酶

研究领域 >> 神经疾病

天然产物 >> 其他

[ 靶点 ]

PARP-1

Human Endogenous Metabolite

[体外研究]

用聚(ADP-核糖)聚合酶(PARP)抑制剂烟酰胺预处理能够预防HCN2细胞死亡。当在t-BuOOH之前加入烟酰胺时,它能够阻止神经元细胞死亡并抑制细胞凋亡。烟酰胺预处理的神经元具有更高的凋亡抑制因子(IAP)基因表达水平[1]。烟酰胺通过ET抑制血管收缩。烟酰胺还可以缓解氧化应激,从而加剧PE和FGR [3]。

[体内研究]

正常和链脲佐菌素-烟酰胺诱导的成年男性糖尿病大鼠口服槲皮素(10,25和50 mg/kg/bw),并导致FBG和心脏损伤标志物水平显着降低,胰岛素水平升高[2]。烟酰胺可改善RUPP小鼠的母体高血压,蛋白尿和肾小球内皮增生症。此外,烟酰胺可延长妊娠期,并可改善RUPP PE小鼠胚胎的存活和生长[3]。

[动物实验]

在注射链脲佐菌素（STZ）（55mg / kg /体重）前15分钟，通过单次腹膜内（ip）注射溶解于生理盐水中的烟酰胺（110mg / kg /体重）诱导DM，将其溶解于新鲜制备的0.1mol / Lcitrate缓冲液（pH4.5）。这些注射是在禁食过夜后给出的。对照大鼠（n = 6）注射相同量的溶剂。为了在STZ注射后的最初24小时内防止低血糖，允许大鼠用5％葡萄糖（D5W）自由饮水。注射STZ-烟酰胺后3天，FBG水平大于7.0mM的大鼠被认为是糖尿病。

[参考文献]

[1]. Bhansali SG, et al. Nicotinamide prevents apoptosis in human cortical neuronal cells. Toxicol Mech Methods. 2006;16(4):173-80.

[2]. Roslan J, et al. Quercetin ameliorates oxidative stress, inflammation and apoptosis in the heart of streptozotocin-nicotinamide-induced adult male diabetic rats. Biomed Pharmacother. 2016 Dec 24;86:570-582

[3]. Fushima T, et al. Nicotinamide ameliorates a preeclampsia-like condition in mice with reduced uterine perfusion pressure. Am J Physiol Renal Physiol. 2016 Dec 7:ajprenal.00501.2016

[4]. Suzuki E, et al. Protective effect of nicotinamide against poly(ADP-ribose) polymerase-1-mediated astrocyte death depends on its transporter-mediated uptake. Life Sci. 2010 Apr 24;86(17-18):676-82.

[相关活性小分子]

烟酰胺物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
257.7±32.0 °C at 760 mmHg

[ 熔点 ]:
128-131 °C(lit.)

[ 分子式 ]:
C₆H₆N₂O

[ 分子量 ]:
122.125

[ 闪点 ]:
109.7±25.1 °C

[ 精确质量 ]:
122.048012

[ PSA ]:
55.98000

[ LogP ]:
-0.24

[ 外观性状 ]:
powder | white

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.590

[ 储存条件 ]:
0-6°C

[ 稳定性 ]:
Stable. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
1000 g/L (20 ºC)

烟酰胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QS3675000

CHEMICAL NAME :: Nicotinamide

CAS REGISTRY NUMBER :: 98-92-0

LAST UPDATED :: 199701

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C6-H6-N2-O

MOLECULAR WEIGHT :: 122.14

WISWESSER LINE NOTATION :: T6NJ CVZ

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 :: 3500 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1680 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - other changes

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2500 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2050 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2 gm/kg

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

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 2500 mg/kg

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

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 5 mmol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 126,63,1984 *** OCCUPATIONAL EXPOSURE LIMITS *** OEL-RUSSIA:STEL 1 mg/m3 JAN 1993 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - M0321 No. of Facilities: 1142 (estimated) No. of Industries: 6 No. of Occupations: 15 No. of Employees: 17336 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M0321 No. of Facilities: 2791 (estimated) No. of Industries: 8 No. of Occupations: 34 No. of Employees: 64950 (estimated) No. of Female Employees: 44524 (estimated)

烟酰胺安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26;S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
1

[ RTECS号 ]:
QS3675000

[ 海关编码 ]:
2933399090

烟酰胺制备

1、 β-甲基吡啶经空气氧化成烟酸，后者与氢氧化铵作用，再加热脱水制得。

2、将烟酸、硼酸和氨水投入反应锅，搅拌下通入氨气，升温溶解；然后蒸馏回收氨，至120~C后移入脱水锅内继续浓缩；当温度达145℃后开始加入液氨，并在185～190℃下继续通氨反应20～30h。然后降温至130℃，加蒸馏水稀释，加入活性炭，并在70~80~C下通氨脱色2h；反应后趁热过滤，滤液在水中冷析24h，分离结晶，并用乙醇洗涤、干燥得成品，收率89%。

3、由烟酸与氨水成盐后再脱水而得。

烟酰胺海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

烟酰胺文献

Epigenetic reprogramming of the type III interferon response potentiates antiviral activity and suppresses tumor growth.

PLoS Biol. 12(1) , e1001758, (2014)

Type III interferon (IFN-λ) exhibits potent antiviral activity similar to IFN-α/β, but in contrast to the ubiquitous expression of the IFN-α/β receptor, the IFN-λ receptor is restricted to cells of ep...

Alisertib, an Aurora kinase A inhibitor, induces apoptosis and autophagy but inhibits epithelial to mesenchymal transition in human epithelial ovarian cancer cells.

Drug Des. Devel. Ther. 9 , 425-64, (2015)

Ovarian cancer is a leading killer of women, and no cure for advanced ovarian cancer is available. Alisertib (ALS), a selective Aurora kinase A (AURKA) inhibitor, has shown potent anticancer effects, ...

Functionalized tetrahydro-1H-pyrido[4,3-b]indoles: a novel chemotype with Sirtuin 2 inhibitory activity.

Eur. J. Med. Chem. 92 , 145-55, (2015)

Sirtuins are protein deacylases with regulatory roles in metabolism and stress response. Functionalized tetrahydro-1H-pyrido[4,3-b]indoles were identified as preferential sirtuin 2 inhibitors, with in...

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烟酰胺