二甲基姜黄素(Dimethylcurcumin) - 药物靶点：AR_在研适应症：去势抵抗性前列腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Dimethyl curcumin

+ [2]

靶点

AR

作用机制

AR 降解剂(雄激素受体降解剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Nazareth College of Rochester (New York)

非在研机构

AndroScience Corp.

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C23H24O6

InChIKeyZMGUKFHHNQMKJI-CIOHCNBKSA-N

CAS号52328-98-0

关联

2

项与二甲基姜黄素相关的临床试验

NCT01289574 / Completed临床2期

Phase 2, Multi-Center, Randomized, Double-Blind, Vehicle-Controlled Clinical Study to Evaluate the Safety and Efficacy of 0.1% and 0.025% ASC-J9 Creams Applied Topically Twice Daily for 12 Weeks for the Treatment of Facial Acne Vulgaris

To evaluate the safety and efficacy of topical 0.1% and 0.025% ASC-J9 creams applied twice daily for facial acne compared to vehicle control.

开始日期2011-02-01

申办/合作机构

AndroScience Corp.

[+1]

NCT00525499 / Completed临床2期

A Phase 2, Multi-Center, Randomized, Double-Blind, Vehicle-Controlled Dose-Ranging Clinical Study to Evaluate the Safety and Efficacy of ASC-J9 Cream Applied Twice Daily for 12 Weeks for the Treatment of Facial Acne Vulgaris

The purpose of this study is to evaluate if topical ASC-J9 cream is effective in treating acne.

开始日期2007-08-01

申办/合作机构

AndroScience Corp.

100 项与二甲基姜黄素相关的临床结果

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100 项与二甲基姜黄素相关的转化医学

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100 项与二甲基姜黄素相关的专利（医药）

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66

项与二甲基姜黄素相关的文献（医药）

2024-07-01·Chemical Biology & Drug Design

Synthesis of curcumin derivatives targeting androgen receptor for castration‐resistant prostate cancer therapy

Article

作者: Zhou, Keyun ; Hu, Liangyong ; Zhu, Tianyu ; Ni, Yaohui ; Liu, Jiangfei ; Xu, Defeng ; Wu, Guanzhao ; Hu, Hang

AbstractIn this work, a series of curcumin derivatives (1a–1h, 2a–2g, and 3a–3c) were synthesized for the suppression of castration‐resistant prostate cancer cells. All synthesized compounds were characterized by 1H NMR, 13C NMR, HRMS, and melting point. The in vitro cytotoxicity study shows that compounds 1a, 1e, 1f, 1h, 2g, 3a, and 3c display similar or enhanced cytotoxicity against 22Rv1 and C4‐2 cells as compared to ASC‐J9, other synthesized compounds display reduced cytotoxicity against 22Rv1 and C4‐2 cells as compared to ASC‐J9. Molecular docking simulation was performed to study the binding affinity and probable binding modes of the synthesized compounds with androgen receptor. The results show that all synthesized compounds exhibit higher cdocker interaction energies as compared to ASC‐J9. Compounds 1h, 2g, and 3c not only show strong cytotoxicity against 22Rv1 and C4‐2 cells but also exhibit high binding affinity with androgen receptor. In androgen receptor suppression study, compounds 1f and 2g show similar androgen receptor suppression effect as compared to ASC‐J9 on C4‐2 cells, compound 3c displays significantly enhanced AR suppression effect as compared to ASC‐J9, 1f and 2g. Compounds 1a, 1e, 1f, 1h, 2g, 3a and 3c prepared in this work have significant potential for castration‐resistant prostate cancer therapy.

2023-12-01·MethodsX

Validated HPLC method for simultaneous quantitative determination of dimethylcurcumin and resveratrol in pluronic-F127 nanomicelles: Formulation with enhanced anticancer efficacy

Article

作者: Arakkunakorn, Wasiporn ; Basit, Abdul ; Nalinbenjapun, Sirinporn ; Sajomsang, Warayuth ; Pholthien, Watchara ; Ovatlarnporn, Chitchamai ; Sripetthong, Sasikarn

Nano-micelles offer a promising vehicle for the delivery various therapeutically significant biologicals. Development of convenient and efficient chromatographic methods for the quantitative determination of the active pharmaceutical ingredients in such systems is of immense importance. In this study pluronic-F-127 nano-micelles were prepared and loaded with dimethylcurcumin (DMC) and resveratrol (Res). A simple, convenient and effective HPLC method was developed for the quantitative estimation of DMC and Res in the polymeric nano-micelles through a single injection. A reverse-phase ACE® C18 column (250 mm × 4.6 mm) was used with a gradient mobile phase system consisting of 1 % MeOH and 0.1 % H₃PO₄:100 % acetonitrile at 1 mL/min flow rate with UV detection for Res, and fluorescence detector for DMC. The calibration curves generated for both the compounds were found linear with r² values of 1.000 over a concentration range of 2-25 µg/mL with low limit of detection (LOD) values of 0.37 and 0.16 µg/mL for DMC and Res respectively and limit of quantification (LOQ) values of 1.23 and 0.55 µg/mL for DMC and Res respectively. Similarly, accuracy was found in a range of 98.80 -102.47 % for DMC and 100.58-101.77 % for Res. Furthermore, the within-run precisions (%RSD) were 0.073 - 0.444% for DMC and 0.159 - 0.917% for Res, while between-run precisions (%RSD) were 0.344 - 1.47 for DMC and 0.458 - 1.651 for Res. Moreover, the DMC with Res co-loaded nanomicelles showed higher activity against MCF-7 and MDA-MB 231 compared to DMC and Res alone. Overall, this study presented a simple, convenient, precise and accurate method for the quantitative determination of DMC and Res in polymeric nano-micelles which have anticancer potential.•A simple HPLC for the quantitative determination of DMC and Res in nanomicelles having anti-cancer potential.•Non complicate with high degree of recoveries of sample preparation process.•This method can be used to determine a mixture of DMC and Res in pharmaceutical formulation in single injection.

2022-08-01·Colloids and Surfaces B: Biointerfaces

Peptide-functionalised magnetic silk nanoparticles produced by a swirl mixer for enhanced anticancer activity of ASC-J9

Article

作者: Hadianamrei, Roja ; Xu, Defeng ; Zhao, Xiubo ; Tomeh, Mhd Anas ; Brown, Stephen

Silk fibroin is an FDA approved biopolymer for clinical applications with great potential in nanomedicine. However, silk-based nanoformulations are still facing several challenges in processing and drug delivery efficiency (such as reproducibility and targetability), especially in cancer therapy. To address these challenges, robust and controllable production methods are required for generating nanocarriers with desired properties. This study aimed to develop a novel method for the production of peptide-functionalized magnetic silk nanoparticles with higher selectivity for cancer cells for targeted delivery of the hydrophobic anticancer agent ASC-J9. A new microfluidic device with a swirl mixer was designed to fabricate magnetic silk nanoparticles (MSNP) with desired size and narrow size distribution. The surface of MSNPs was functionalized with a cationic amphiphilic anticancer peptide, G(IIKK)₃I-NH₂ (G3), to enhance their selectivity towards cancer cells. The G3-MSNPs increased the cellular uptake and anticancer activity of G3 in HCT 116 colorectal cancer cells compared to free G3. Moreover, the G3-MSNPs exhibited considerably higher cellular uptake and cytotoxicity in HCT 116 colorectal cancer cells compared to normal cells (HDFs). Encapsulating ASC-J9 in G3-MSNPs resulted in augmented anticancer activity compared to free ASC-J9 and non-functionalized ASC-J9 loaded MSNPs within its biological half-life. Hence, functionalizing MSNPs with G3 enabled targeted delivery of ASC-J9 to cancer cells and enhanced its anticancer effect. Functionalization of nanoparticles with anticancer peptides could be regarded as a new strategy for targeted delivery and enhanced efficiency of anticancer drugs. Furthermore, the microfluidic device introduced in this paper offers a robust and reproducible method for fabrication of small sized homogenous nanoparticles.

100 项与二甲基姜黄素相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB06133

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
去势抵抗性前列腺癌	临床前	美国	Nazareth College of Rochester (New York)	2012-04-01
脊髓性肌萎缩	药物发现	美国	AndroScience Corp.	2011-01-24
创伤和损伤	药物发现	美国	AndroScience Corp.	2009-02-18
脱发	药物发现	美国	AndroScience Corp.	2008-06-15
寻常痤疮	药物发现	美国	AndroScience Corp.	2007-08-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01289574 (CTgov)	临床2期	寻常痤疮	181	ASC-J9 (Vehicle Control Cream)	醖鏇觸廠鬱積鬱積鑰鹹(糧築鬱餘夢夢餘鬱鹽夢) = 願醖製網製繭觸醖網獵醖淵窪觸淵夢衊餘夢襯 (觸膚衊獵遞醖網製願製, 齋繭餘鹹築壓範餘鏇窪 ~ 製夢築餘憲艱壓繭觸觸) 更多	-	2014-07-25
				ASC-J9 (0.025% ASC-J9 Cream)	醖鏇觸廠鬱積鬱積鑰鹹(糧築鬱餘夢夢餘鬱鹽夢) = 襯觸醖艱願網壓襯網鬱醖淵窪觸淵夢衊餘夢襯 (觸膚衊獵遞醖網製願製, 齋糧窪觸網醖憲齋窪壓 ~ 鹹鏇襯夢廠鑰觸憲製衊) 更多