更新于：2024-11-01

Inositol Nicotinate

肌醇烟酸酯

更新于：2024-11-01

概要

概要

基本信息

药物类型

小分子化药

别名

Inositol、Inositol Nicotinatis、Inositol Nictinate

+ [25]

靶点

HCAR3 x NIACR1

作用机制

HCAR3激动剂(烟酸G蛋白偶联受体HM74激动剂)、NIACR1激动剂(羟基酸受体-2激动剂)

治疗领域

心血管疾病内分泌与代谢疾病

在研适应症

高脂血症外周血管疾病

非在研适应症-

原研机构-

在研机构-

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C42H30N6O12

InChIKeyMFZCIDXOLLEMOO-GYSGTQPESA-N

CAS号6556-11-2

关联

100 项与肌醇烟酸酯相关的临床结果

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100 项与肌醇烟酸酯相关的转化医学

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100 项与肌醇烟酸酯相关的专利（医药）

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112

项与肌醇烟酸酯相关的文献（医药）

2024-03-01·European Journal of Pharmacology

Curcumin nicotinate increases LDL cholesterol uptake in hepatocytes through IDOL/LDL-R pathway regulation

Article

作者: Yang, Jia-Tao ; Zhao, Qian ; Liao, Duan-Fang ; Tuo, Qin-Hui ; Zhang, Cai-Ping ; Huang, Ying ; Wang, Jing ; Liu, Fang-Yuan ; Lin, Li-Mei ; Zhu, Mei-Qi ; Long, Shi-Yin

BACKGROUNDCurcumin nicotinate (Curtn), derived from curcumin and niacin, reduces serum LDL-C levels, partly due to its influence on PCSK9. This study investigates IDOL's role in Curtn's lipid-lowering effects.OBJECTIVETo elucidate Curtn's regulation of the IDOL/LDLR pathway and potential molecular mechanisms in hepatocytes.METHODSDifferential metabolites in Curtn-treated HepG2 cells were identified via LC-MS. Molecular docking assessed Curtn's affinity with IDOL. Cholesterol content and LDLR expression effects were studied in high-fat diet Wistar rats. In vitro evaluations determined Curtn's influence on IDOL overexpression's LDL-C uptake and LDLR expression in hepatocytes.RESULTSLipids were the main differential metabolites in Curtn-treated HepG2 cells. Docking showed Curtn's higher affinity to IDOL's FERM domain compared to curcumin, suggesting potential competitive inhibition of IDOL's binding to LDLR. Curtn decreased liver cholesterol in Wistar rats and elevated LDLR expression. During in vitro experiments, Curtn significantly enhanced the effects of IDOL overexpression in HepG2 cells, leading to increased LDL-C uptake and elevated expression of LDL receptors.CONCLUSIONCurtn modulates the IDOL/LDLR pathway, enhancing LDL cholesterol uptake in hepatocytes. Combined with its PCSK9 influence, Curtn emerges as a potential hyperlipidemia therapy.

2023-03-01·Italian Journal of Dermatology and Venereology

Efficacy and tolerability of a repairing moisturizing cream containing amino-inositole and urea 10% in adults with chronic eczematous dermatitis of the hands

Article

作者: Spigariolo, Cristina B ; Ferrucci, Silvia M

BACKGROUNDPatients suffering from eczematous dermatitis always required moisturizing cream as a background therapy with the aim to reduce flares and minimize steroids use. The term emollients plus (EP) refers to a topical formulations with vehicle-type substances and additional active, non-medicated substances. We have conducted a study with a topical emollient containing urea 10% and amino-inositole on 20 patients affected from chronic eczematous dermatitis. Primary outcomes were to evaluate effectiveness, in term of Investigator Global Assessment (IGA), and tolerability of EP. Secondary aims included the comparison of NRS (numerical rating scale) itch and NRS-pain, DLQI (Dermatological Life Quality Index) between day one and day 28 and to evaluate the characteristics of EP.METHODSSubjects were instructed to apply the EP twice daily for 4 weeks on affected skin and use a soft soap while not to put any other topical or systemic product. Statistical analysis was conducted through the test t-Student by comparing IGA, itch-NRS, pain-NRS and DLQI at time 0 and day 28.RESULTSHigh statistically significant difference (P=0.0038) between IGA value at T0 and T4 has been demonstrated as for itch and pain (respectively P=0.0203 and P=0.0146). Almost all the patients (89.5%) have declared a good or better tolerability of EP. Two patients did not complete the study.CONCLUSIONSPatients with chronic eczema could often resolve the dermatitis with the correct choice of emollient without steroids use, especially if it is an EP.

2022-09-01·European Journal of Pharmacology

Curcumin nicotinate decreases serum LDL cholesterol through LDL receptor-mediated mechanism

Article

作者: Yuan, Yulin ; Liao, Duanfang ; Xiang, Debiao ; Zhang, Caiping ; Yang, Huixian ; Long, Shiyin ; Zhao, Qian ; Liu, Xuanyou ; Zeng, Yaling ; Wen, Hongyan ; Tuo, Qinhui ; Huang, Zhixin ; Jiang, Susu ; Huang, Ying ; Wang, Chuyao ; Liu, Zhenguo ; Hao, Hong

Curcumin nicotinate (Curtn) is a synthesized ester derivative of curcumin and niacin. Our previous study has shown that Curtn lowers serum low-density lipoprotein cholesterol (LDL-C) levels in apoE^-/- mice and promotes LDL-C uptake into HepG2 cells in vitro. The present study was to test the hypothesis that Curtn decreases serum LDL-C levels through decreased expression of pro-protein convertase subtilisin/kexin type 9 (PCSK9) and subsequent increase in LDL receptor expression. Male Wistar rats on high-fat diet (HFD) were treated with Curtn or rosuvastatin. Curtn or rosuvastatin treatment significantly decreased serum levels of total cholesterol (TC) and LDL-C in rats on HFD with increased liver LDL receptor expression. LDL-C-lowering effect of Curtn was not observed in LDL receptor deficient (LDLR^-/-) mice on HFD, while rosuvastatin still decreased serum lipid levels in LDLR^-/- mice, indicating that the reduction of serum LDL-C levels by Curtn treatment was LDL receptor-dependent. Curtn treatment also significantly decreased the protein expression of PCSK9 in Wistar rats and LDLR^-/- mice. In HepG2 cells with overexpression of human PCSK9, Curtn treatment significantly increased LDL-C uptakes into hepatocytes, and increased LDL receptor distribution on cell surface in association with decreased PCSK9 protein expression. RNAi-LDLR significantly attenuated the effect of Curtn on LDLR distribution on cell surface. These data indicates that Curtn would decrease serum LDL-C level at least partially through inhibition of PCSK9 expression, and subsequent increase in LDL receptor expression and distribution in hepatocytes, serving as a potential novel compound to treat hyperlipidemia.

100 项与肌醇烟酸酯相关的药物交易

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