Cryptotanshinone(Cryptotanshinone) - 药物靶点：SHP2_在研适应症：肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Cryptotanshinon、Tanshinone C

+ [2]

靶点

SHP2

作用机制

SHP2抑制剂(蛋白酪氨酸磷酸酶-2抑制剂)

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症

纤维化肝硬化非酒精性脂肪性肝炎+ [1]

原研机构

KT&G Life Sciences Corp.

在研机构

Case Western Reserve University

非在研机构

KT&G Life Sciences 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C19H20O3

InChIKeyGVKKJJOMQCNPGB-JTQLQIEISA-N

CAS号35825-57-1

关联

8

项与 Cryptotanshinone 相关的临床试验

ChiCTR2100051329 / Suspended早期临床1期IIT

Oral Tanshinone in the treatment of dry eyes associated with rosacea

开始日期2021-10-01

申办/合作机构-

ITMCTR2100005326 / Suspended早期临床1期IIT

Oral Tanshinone in the treatment of dry eyes associated with rosacea

开始日期2021-10-01

申办/合作机构-

ITMCTR2000003582 / SuspendedN/AIIT

Tanshinone, metformin, or their combination for insulin resistance in women with polycystic ovarian syndrome: a double blind randomised controlled trial

开始日期2020-10-01

申办/合作机构

上海市中医医院

100 项与 Cryptotanshinone 相关的临床结果

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100 项与 Cryptotanshinone 相关的转化医学

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100 项与 Cryptotanshinone 相关的专利（医药）

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2,166

项与 Cryptotanshinone 相关的文献（医药）

2024-12-09·Journal of Biomolecular Structure and Dynamics

Structure-based virtual screening of natural compounds as inhibitors of HCV using molecular docking and molecular dynamics simulation studies

Article

作者: Y. Safhi, Awaji ; H. Sultan, Muhammad ; Alsalhi, Abdullah ; Ahsan, Waquar ; M. Jali, Abdulmajeed ; Salawi, Ahmad ; Almoshari, Yosif ; Ali Bakkari, Mohammed ; A. Madkhali, Osama ; Sabei, Fahad Y.

The hepatitis C virus (HCV), which causes hepatitis C, is a viral infection that damages the liver and causes inflammation in the liver. New potentially effective antiviral drugs are required for its treatment owing to various issues associated with the existing medications, including moderate to severe adverse effects, higher costs, and the emergence of drug-resistant strains. The objective of the current study was to utilize computational techniques to assess the anti-HCV efficacy of certain phytochemicals against tetraspanin (CD81) and claudin 1 (CLDN1) entry proteins. A 200-nanosecond molecular dynamics (MD) simulation was employed to examine the stability of the lead-protein complexes. Free binding energy and molecular docking calculations were conducted utilizing MM/GBSA method, and the selectivity of hit compounds for CD81 and CLDN1 was determined. Five significant CD81 and CLDN1 inhibitors were identified: Petasiphenone, Silibinin, Tanshinone IIA, Taxifolin, and Topaquinone. The MM/GBSA analysis of the compounds revealed high free binding energies. All the identified compounds were stable within the CD81 and CLDN1 binding pockets. This study indicated the promising inhibitory potential of the identified compounds against CD81 and CLDN1 receptors and might develop into potential viral entry inhibitors. However, to validate the chemotherapeutic capabilities of the discovered leads extensive preclinical research is required.Communicated by Ramaswamy H. Sarma.

2024-12-01·Current Molecular Medicine

Tanshinone Alleviates UVA-induced Melanogenesis in Melanocytes via the Nrf2-regulated Antioxidant Defense Signaling Pathway

Article

作者: Zhu, Huilan ; Li, Huaping ; Yin, Zonghao ; Ou, Shanshan ; Yu, Nanji ; Wang, Xue ; Chen, Jiaoquan

Background:As a complex of natural plant compounds, tanshinone is renowned for its remarkable antioxidant properties. However, the potential impact of tanshinone on melanocyte pigmentation regulation has yet to be elucidated. This study aimed to explore the protective effects of tanshinone I (T-I) and dihydrotanshinone (DHT) on melanogenesis by modulating nuclear factor E2-related factor 2 (Nrf2) signaling and antioxidant defenses in human epidermal melanocyte (HEM) cells.Methods:HEM cells and Nrf2 knockdown HEM cells were subjected to ultraviolet A (UVA) and treated with T-I and/or DHT. Then, the anti-melanogenic properties of T-I and DHT were examined by assessing tyrosinase activity, melanogenesis-related proteins, and melanin content in UVA-irradiated HEM cells. Furthermore, the antioxidant activities of T-I and DHT were evaluated by assessing oxidant formation and modulation of Nrf2-related antioxidant defenses, including reactive oxygen species (ROS), glutathione (GSH) content, and the activity and expression of antioxidant enzymes, such as catalase (CAT), heme oxygenase-1 (HO-1), and superoxide dismutase (SOD).Results:Our findings revealed that T-I and DHT diminished melanogenesis in UVAirradiated HEM cells, activated Nrf2-antioxidant response element signaling, and enhanced antioxidant defenses in the irradiated cells. Furthermore, Nrf2 knockdown by shRNA abolished the anti-melanogenesis effects of T-I and DHT on HEM cells against oxidative damage.Conclusion:These results suggest that T-I and DHT inhibit UVA-induced melanogenesis in HEM cells, possibly through redox mechanisms involving Nrf2 signaling activation and increased antioxidant defenses. This indicates that T-I and DHT have potential as whitening agents in cosmetics and medical treatments for hyperpigmentation disorders.

2024-12-01·Phytomedicine

A stepwise integrated strategy to explore quality markers of Qishen Yiqi dripping pills against myocardial ischemia

Article

作者: Tang, Meng ; Zhou, Pei-Pei ; Xue, Lian-Ping ; Liu, Li-Wei ; Jia, Qing-Quan ; Sun, Zhi ; Zuo, Li-Hua ; Zhang, Zhi-Bo ; Zhao, Ling-Guo

BACKGROUNDNumerous experiments and clinical practices have demonstrated the effectiveness of Qishen Yiqi dripping pills (QSYQ) on myocardial ischemia (MI). However, the bioactive ingredients and mechanisms remain unclear, leading to huge gaps between quality control and biological effect of QSYQ. Discovering quality markers (Q-markers) based on effective components is crucial for ensuring stable quality and clinical effectiveness of QSYQ.PURPOSETo explore Q-markers of QSYQ against MI by a stepwise strategy integrating serum pharmacochemistry, network pharmacology, metabolomics, quantitative analysis, and cell experiments.METHODSFirstly, liquid/gas chromatography-mass spectrometry was applied to characterize chemical profiles of QSYQ in vitro and in vivo. Based on the serum migrating constituents, a component-target-MI interaction network was constructed. Subsequently, pharmacodynamics and metabolomics were conducted to evaluate cardioprotective effect and potential mechanism of QSYQ. Next, conjoint analysis of network pharmacology and metabolomics was performed to screen candidate Q-markers. Finally, the measurability and bioactivity were validated to justify their usage as Q-markers.RESULTSA total of 97 components were identified in QSYQ, 24 prototypes of which were detected in serum. The "component-target-disease" interaction network was constructed based on serum migrating constituents. Pharmacodynamic results showed that QSYQ effectively improved cardiac function, attenuated inflammatory cell infiltration, alleviated myocardial fibrosis, and reduced the levels of myocardial enzymes and oxidative stress in MI rats. Metabolomics study demonstrated that 59 metabolites were markedly altered in MI rats, 25 of which were significantly reversely regulated by QSYQ. After integrative analysis of network pharmacology and metabolomics, 12 components were selected as candidate Q-markers of QSYQ, and the contents were quantified. These candidate Q-markers displayed synergistic protective effects against H₂O₂-induced injury in H9c2 cells. Taken together, 12 components with properties of transitivity and traceability, effectiveness, measurability, and compatibility contribution were defined as representative Q-markers of QSYQ, including Astragaloside IV, Ononin, Calycosin, Formononetin, Rosmarinic acid, Cryptotanshinone, Salvianolic acid A, Tanshinol, Ginsenoside Rb1, Ginsenoside Rg1, Nerolidol, and Santalol.CONCLUSIONIn this study, a novel stepwise integrated strategy was presented for discovering Q-markers related to therapeutic effects of traditional Chinese medicine prescriptions. Twelve comprehensive and representative Q-markers of QSYQ were identified for the first time to improve its quality control.

100 项与 Cryptotanshinone 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB15579

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
纤维化	临床2期	-	KT&G Life Sciences Corp.	-
肝硬化	临床2期	韩国	KT&G Life Sciences Corp.	-
非酒精性脂肪性肝炎	临床2期	韩国	KT&G Life Sciences Corp.	-
肥胖	临床2期	韩国	KT&G Life Sciences Corp.	-
肿瘤	临床前	美国	Case Western Reserve University	2013-09-26