百里香醌(Thymoquinone) - 药物靶点：E2F1 x MUC4 x PTEN_在研适应症：牙龈炎，HR阳性乳腺癌，非小细胞肺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

作用机制

E2F1抑制剂(转录因子E2F1抑制剂)、MUC4 inhibitors(mucin 4, cell surface associated inhibitors)、PTEN stimulators(磷脂酰肌醇-3,4,5-三磷酸3-磷酸酶和双特异性蛋白磷酸酶PTEN刺激剂)

治疗领域

感染口颌疾病肿瘤+ [8]

在研适应症

牙龈炎HR阳性乳腺癌非小细胞肺癌+ [8]

非在研适应症-

原研机构

The Case Comprehensive Cancer Center

在研机构

Beni-Suef University

Barbara Ann Karmanos Cancer Institute

University of Miami

+ [13]

非在研机构-

最高研发阶段早期临床1期

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C10H12O2

InChIKeyKEQHJBNSCLWCAE-UHFFFAOYSA-N

CAS号490-91-5

关联

10

项与百里香醌相关的临床试验

NCT06508372 / Not yet recruitingN/AIIT

Efficacy and Safety of Thymoquinone Ointment as a Potential New Therapeutic Modality of Psoriasis Vulgaris.

A previous trial found that N. sativa oil was more effective as an antipsoriatic agent, particularly when taken as both a cream and a pill. This confirmed that N. sativa possesses antipsoriatic properties and can alleviate psoriasis symptoms

开始日期2024-08-01

申办/合作机构

Assiut University

NCT06070311 / Not yet recruitingN/AIIT

Effect of Thymoquinone and Olive Oil on Wound Healing After Endoscopic Sinus Surgery in Patients With Nasal Polyposis

This study aims to determine the effect of Thymoquinone (0.5%) and olive oil ointment on Wound healing after Endoscopic sinus surgery.

开始日期2023-10-01

申办/合作机构

Assiut University

NCT05497895 / Not yet recruiting早期临床1期IIT

A Randomized Controlled Clinical Trial for the Assessment of Clinical Efficacy of Topical Application of 5% Thymoquinone Gel for Gingivitis Patients

Gingival diseases occur commonly in the global population and herbal products for its intervention have limited body of research evidence. This study to evaluate the clinical efficacy of 5% thymoquinone (TQ) gel as an adjunct to scaling and root planing (SRP) in patients diagnosed with gingivitis.
OBJECTIVE: To evaluate the efficacy of 5% TQ gel using a novel liposome drug delivery as a topical application following SRP in gingivitis patients.
DESIGN: Double-blinded, parallel, randomized controlled clinical trial. SETTING: Faculty of Dentistry, King Abdulaziz University, and Qassim University, Saudi Arabia

开始日期2022-09-01

申办/合作机构

King Abdulaziz University

100 项与百里香醌相关的临床结果

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100 项与百里香醌相关的转化医学

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100 项与百里香醌相关的专利（医药）

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1,745

项与百里香醌相关的文献（医药）

2025-01-01·Current Drug Delivery

Nigella sativa Oil-loaded Ethanolic Vesicular Gel for Imiquimod-induced Plaque Psoriasis: Physicochemical Characterization, Rheological Studies, and In vivo Efficacy

Article

作者: Ranjan Lal, Uma ; Kumar Chellappan, Dinesh ; Vihal, Samar ; Rathore, Charul ; Negi, Poonam ; Gupta, Gaurav ; Pundir, Swati ; Dua, Kamal ; Kumar Singh, Sachin

Background:The therapeutic effect of NS oil in mild to moderate psoriasis is limited owing to low play load of thymoquinone (<15 %w/w), irritation, dripping, low viscosity and thus, less contact time on the lesions.Aims::This study aimed at developing and characterizing the ethanolic vesicular hydrogel system of Nigella sativa (NS) oil (NS EV hydrogel) for the enhancement of anti-psoriatic activity.Objective:The objective of this study was to develop NS EV hydrogel and evaluate its anti-psoriatic activity.Methods:The identification and quantification of TQ content in different NS seed extracts and marketed oil were measured by an HPTLC method using n-hexane and ethyl acetate as solvent systems. Preparation of ethanolic vesicles (EVs) was performed by solvent injection method, while its antipsoriatic activity was evaluated employing an Imiquad (IMQ)-induced plaque psoriasis animal model.Results:A compact HPTLC band was obtained for TQ at an Rf value of 0.651. The calibration plot was linear in the range of 1-10 μg/spot, and the correlation coefficient of 0.990 was indicative of good linear dependence of peak area on concentration. From the different NS sources, the high TQ content was obtained in the marketed cold press oil, i.e., 1.45±0.08mg/ml. Out of various NS oilloaded EVs, the F6 formulation revealed the smallest particle size (278.1nm), with log-normal size distribution (0.459) and adequate entrapment efficiency. A non-uniform shape was observed in the transmission electron microscopy. The viscosity of F6 formulation hydrogel was 32.34 (Pa·s), which exhibited plastic behavior. In vivo, efficacy studies demonstrated decreased inflammation of the epidermis and dermis and a marked decrease in the levels of IL-17 by NS EV hydrogel compared to plain NS oil and standard drugs (Betamethasone and Dr. JRK Psorolin Oil).Conclusion:It may be concluded from the findings that NS-loaded EV gel was as good as betamethasone cream but more efficacious than the other treatments.

2024-12-31·Journal of Enzyme Inhibition and Medicinal Chemistry

Effects of thymoquinone and the curcumin analog EF-24 on the activity of the enzyme paraoxonase-1 in human glioblastoma cells U87MG

Article

作者: Sunguroglu, Asuman ; Özgültekin, Nurbanu ; Kilic, Ahmet ; Simsek, Ender ; Ozensoy Guler, O

The spices and aromatic herbs were used not only in cooking to add flavour and smell to dishes but also for medicinal use. Nigella sativa, also called black cumin, is one of the species that contains an important bioactive component, thymoquinone (TQ), which has antioxidant, anti-inflammatory, antimicrobial, and antidiabetic effects. Curcuma longa, which also includes curcumin, has numerous anti-cancer properties. However, the bioavailability of curcumin is lower than that of its analogs. An analog of curcumin (EF-24), which has better bioavailability than curcumin, is capable of exerting a high anti-cancer effect. In our study, we determined the effects of PON1 enzyme activity on the proliferation and aggressiveness of glioblastoma cancer treated with TQ and EF-24 from lysates of the glioblastoma cell line U87MG. The results were determined as increased PON1 activity after treatment with TQ and EF-24 in the U87MG cell line (p < 0.0001).

2024-12-31·Drug Delivery

Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects

Article

作者: Halder, Shimul ; Shill, Manik Chandra ; Shuma, Madhabi Lata ; Sharmin, Nahid ; Afrose, Sanjida ; Rahman, S M Abdur ; Mollick, Patricia Prova ; Muhit, Md Abdul

The present study was designed to develop a self-micellizing solid dispersion (SMSD) containing Thymoquinone (TQM), a phytonutrient obtained from Nigella sativa seeds, aiming to improve its biopharmaceutical and nephroprotective functions. The apparent solubility of TQM in polymer solutions was used to choose an appropriate amphiphilic polymer that could be used to make an SMSD system. Based on the apparent solubility, Soluplus® was selected as an appropriate carrier, and mixing with TQM, SMSD-TQM with different loadings of TQM (5-15%) was made by solvent evaporation and freeze-drying techniques, respectively, and the formulations were optimized. The optimized SMSD-TQM was evaluated in terms of particle size distribution, morphology, release characteristics, pharmacokinetic behavior, and nephroprotective effects in a rat model of acute kidney injury. SMSD-TQM significantly improved the dissolution characteristics (97.8%) of TQM in water within 60 min. Oral administration of SMSD-TQM in rats exhibited a 4.9-fold higher systemic exposure than crystalline TQM. In a cisplatin-induced (6 mg/kg, i.p.) acute kidney-damaged rat model, oral SMSD-TQM (10 mg/kg) improved the nephroprotective effects of TQM based on the results of kidney biomarkers and histological abnormalities. These findings suggest that SMSD-TQM might be efficacious in enhancing the nephroprotective effect of TQM by overcoming biopharmaceutical limitations.

100 项与百里香醌相关的药物交易

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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
牙龈炎	临床1期	沙特阿拉伯	King Abdulaziz University	2022-09-01
原发性渗出性淋巴瘤	临床前	沙特阿拉伯	King Faisal Specialist Hospital & Research Centre	2009-05-01
原发性渗出性淋巴瘤	临床前	美国	Robert H. Lurie Comprehensive Cancer Center of Northwestern Un	2009-05-01
乳腺癌	临床前	美国	The Ohio State University	2008-05-01
乳腺癌	临床前	埃及	Beni-Suef University	2008-05-01
乳腺癌	临床前	埃及	Al-Azhar University	2008-05-01
胰腺癌	临床前	美国	Barbara Ann Karmanos Cancer Institute	2008-05-01
胰腺癌	临床前	美国	The University of Texas MD Anderson Cancer Center	2008-05-01
前列腺癌	临床前	美国	Henry Ford Hospital	2006-06-20

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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


AACR2017	N/A	头颈部鳞状细胞癌	-	Cisplatin	鬱齋鹹願鹽築顧鏇膚衊(餘糧獵窪鹽夢鹹淵糧餘) = 鬱選夢選艱憲築膚鹽遞願構範蓋製鑰夢製鹹繭 (壓鹹艱艱鹽廠鹽壓鹽鬱 ) 更多	-	2017-07-01
				Thymoquinone	鬱齋鹹願鹽築顧鏇膚衊(餘糧獵窪鹽夢鹹淵糧餘) = 顧蓋襯願襯醖鹽膚廠醖願構範蓋製鑰夢製鹹繭 (壓鹹艱艱鹽廠鹽壓鹽鬱 ) 更多