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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2,178

项与 Cryptotanshinone 相关的文献（医药）

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 ; Ou, Shanshan ; Yin, Zonghao ; 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.

2024-10-02·Journal of Asian Natural Products Research

Regulation of Fuzheng Huayu capsule on inhibiting the fibrosis-associated hepatocellular carcinogenesis

Article

作者: Lan, Shu-Ting ; Wen, Bi-Chao ; Sun, Jia-Xin ; Guo, Yi-Jing ; Sun, Xiao-Mei ; Chen, Jie ; Liu, Gang ; Zhang, Wen-Qi

In the current study, bioinformatics analysis of the hepatocellular carcinoma (HCC) dataset was conducted with the hepatoprotective effect of the Fuzheng Huayu (FZHY) capsule against the diethylnitrosamine-induced HCC progression analyzed. Eight cell clusters were defined and tanshinone IIA, arachidonic acid, and quercetin, compounds of the FZHY capsule, inhibit HCC progression-related fibrosis by regulating the expression of PLAU and IGFBP3. Combined with the ameliorative effect of the FZHY capsule against liver dysfunctions and expression of PLAU and IGFBP3, our study confirmed the effect of the FZHY capsule on inhibiting the fibrosis-associated HCC progression via regulating the expression of PLAU and IGFBP3.

2024-10-01·Journal of Advanced Research

An integrated in vitro human iPSCs-derived neuron and in vivo animal approach for preclinical screening of anti-seizure compounds

Article

作者: He, Wen ; Kwan, Patrick ; Rollo, Ben ; Xu, Hong ; Shahid Javaid, Muhammad ; Zhao, Chunfang ; Zhang, Chunbo ; Huang, Ziyu

INTRODUCTIONOne-third of people with epilepsy continue to experience seizures despite treatment with existing anti-seizure medications (ASMs). The failure of modern ASMs to substantially improve epilepsy prognosis has been partly attributed to overreliance on acute rodent models in preclinical drug development as they do not adequately recapitulate the mechanisms of human epilepsy, are labor-intensive and unsuitable for high-throughput screening (HTS). There is an urgent need to find human-relevant HTS models in preclinical drug development to identify novel anti-seizure compounds.OBJECTIVESThis paper developed high-throughput preclinical screening models to identify new ASMs.METHODS14 natural compounds (α-asarone, curcumin, vinpocetine, magnolol, ligustrazine, osthole, tanshinone IIA, piperine, gastrodin, quercetin, berberine, chrysin, schizandrin A and resveratrol) were assessed for their ability to suppress epileptiform activity as measured by multi-electrode arrays (MEA) in neural cultures derived from human induced pluripotent stem cells (iPSCs). In parallel, they were tested for anti-seizure effects in zebrafish and mouse models, which have been widely used in development of modern ASMs. The effects of the compounds in these models were compared. Two approved ASMs were used as positive controls.RESULTSEpileptiform activity could be induced in iPSCs-derived neurons following treatment with 4-aminopyridine (4-AP) and inhibited by standard ASMs, carbamazepine, and phenytoin. Eight of the 14 natural compounds significantly inhibited the epileptiform activity in iPSCs-derived neurons. Among them, piperine, magnolol, α-asarone, and osthole showed significant anti-seizure effects both in zebrafish and mice. Comparative analysis showed that compounds ineffective in the iPSCs-derived neural model also showed no anti-seizure effects in the zebrafish or mouse models.CONCLUSIONOur findings support the use of iPSCs-derived human neurons for first-line high-throughput screening to identify compounds with anti-seizure properties and exclude ineffective compounds. Effective compounds may then be selected for animal evaluation before clinical testing. This integrated approach may improve the efficiency of developing novel ASMs.

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

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适应症	最高研发状态	国家/地区	公司	日期
非酒精性脂肪性肝炎	临床1期	韩国	KT&G Life Sciences Corp.	-
肥胖	临床1期	韩国	KT&G Life Sciences Corp.	-
肿瘤	临床前	美国	Case Western Reserve University	2013-09-26
纤维化	药物发现	-	KT&G Life Sciences Corp.	-
肝硬化	药物发现	韩国	KT&G Life Sciences Corp.	-